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 Quinazolinone and isoquinolinone derivative patent thumbnailQuinazolinone and isoquinolinone derivative
The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (i) or pharmaceutically acceptable salts thereof.. .
Chugai Seiyaku Kabushiki Kaisha


 Class of green/yellow emitting phosphors based on derivatives of benzimidazoxanthenoisoquinolinone for led lighting patent thumbnailClass of green/yellow emitting phosphors based on derivatives of benzimidazoxanthenoisoquinolinone for led lighting
The invention provides a lighting device (1) comprising (a) a light source (10) configured to generate light source light (11), and (b) a light converter (100) configured to convert at least part of the light source light (11) into visible converter light (111), wherein the light converter (100) comprises a matrix (120) containing a luminescent material (140) based on derivatives of benzimidazoxanthenoisoquinolinone. The lighting device may further comprise a further luminescent material (130)..
Philips Lighting Holding B.v.


 Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a) patent thumbnailSubstituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)
Or a pharmaceutically acceptable salt thereof, wherein r′, r1 through r7 and ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (pde10a) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type ii diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases..

 Aminoisoquinoline derivatives as protein kinase inhibitors patent thumbnailAminoisoquinoline derivatives as protein kinase inhibitors
The present invention provides novel aminoisoquinoline compounds as defined in the specification, compositions thereof use of these compounds as protein kinase inhibitors and as therapeutic agents for treatment of raf kinase, in particular brafv600e kinase, related diseases or disorders, such as cancers. In addition, the invention also includes methods and processes for preparing these novel aminoisoquinoline compounds..
Eternity Bioscience Inc.


 Injectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity patent thumbnailInjectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity
Injectable pharmaceutical compositions containing 6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione dimaleate as active ingredient in the form of a lyophilised powder with a carrier selected from lactose and dextran, mixed with sodium chloride.. .
Cti Biopharma Corp.


 H3 receptor antagonist for use in the treatment of alzheimer's disease patent thumbnailH3 receptor antagonist for use in the treatment of alzheimer's disease
The disclosure relates to the compound 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide or a pharmaceutically acceptable salt thereof, intended for the treatment of alzheimer's disease and other types of dementia.. .
Sanofi


 Benzylisoquinoline alkaloid (bia) precursor producing microbes, and methods of making and using the same patent thumbnailBenzylisoquinoline alkaloid (bia) precursor producing microbes, and methods of making and using the same
Host cells that are engineered to produce benzylisoquinoline alkaloid (bias) precursors, such as norcoclaurine (nc) and norlaudanosoline (nl), are provided. The host cells may have one or more engineered modifications selected from: a feedback inhibition alleviating mutation in a enzyme gene; a transcriptional modulation modification of a biosynthetic enzyme gene; an inactivating mutation in an enzyme; and a heterologous coding sequence.
The Board Of Trustees Of The Leland Stanford Junior University


 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders. patent thumbnailNovel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders.
The present invention relates to novel compounds according to formula i that antagonize gpr84, a g-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (ibd), rheumatoid arthritis, vasculitis, lung diseases (e.g. Chronic obstructive pulmonary disease (copd) and lung interstitial diseases (e.g.

 Combination therapy patent thumbnailCombination therapy
Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog.
Aerie Pharmaceuticals, Inc.


 Rho kinase inhibitors patent thumbnailRho kinase inhibitors
Disclosed are novel substituted 2h-isoquinolin-1-one and 3h-quinazolin-4-one derivatives useful as inhibitors of rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.. .
Aerie Pharmaceuticals, Inc.


Isoquinoline compounds


Described herein are compounds of formula (i) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.. .
Gilead Sciences, Inc.


N-substituted indenoisoquinolines and syntheses thereof


N-substituted indenoisoquinoline compounds, and pharmaceutical formulations of n-substituted indenoisoquinoline compounds are described. Also described are processes for preparing n-substituted indenoisoquinoline compounds.
Purdue Research Foundation


Novel pyridyloxyacetyl tetrahydroisoquinoline compounds useful as nampt inhibitors


The present invention provides novel pyridyloxyacetyl tetrahydroisoquinoline compounds that inhibit nampt and may be useful in the treatment of cancer.. .
Eli Lilly And Company


3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use


The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit parp (e.g., parp1, tnks1, tnks2, etc.) and/or wnt signalling.
Institute Of Cancer Research Royal Cancer Hospital (the)


Production of isoquinoline alkaloids and flavonoids in plant cell cultures of goldenseal (hydrastis canadensis)


Natural product preparations of isoquinoline alkaloids are obtained from plant callus cells of goldenseal, hydrastis canadensis, grown in suspension cell culture. The natural product preparations can be extracted from the cells and/or obtained from the culture medium in which the cells are grown.
Dianaplantsciences Inc.


Compositions and methods for producing benzylisoquinoline alkaloids


The present invention relates to host cells that produce compounds that are characterized as benzylisoquinolines, as well as select precursors and intermediates thereof. The host cells comprise one, two or more heterologous coding sequences wherein each of the heterologous coding sequences encodes an enzyme involved in the metabolic pathway of a benzylisoquinoline, or its precursors or intermediates from a starting compound.
California Institute Of Technology


Substituted 1,2,3,4-tetrahydroisoquinoline derivatives for the treatment of hormone-dependent diseases


Provided are compounds of general formula a and a′, wherein x1 and x2 are each c, ch or n; r3 and r4 are each h, optionally substituted c1-c30 saturated or unsaturated chemical group, or together form an optionally substituted c5-c8 cycle; z1; z2 and z3 are each n or ch; v is c═o, c═s or ch2; n is from 1 to 12; w1 and w2 are each h, ch2, o or s; and r1 and r2 are each h, cr1c6 alkyl, c1c6 aryl, c1c12 alkylaryl, optionally substituted phenyl, c1c6 alkoxy, c1c6 thioalkoxy, f, cl, br or i. These compounds inhibit steroid sulfatase (sts), act as selective estrogen receptor modulators (serms), increase alkaline phosphatase (alp) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer..
UniversitÉ Laval


Organic electroluminescent materials and devices


Formula i, is disclosed. In the structure of formula i: x is selected from a group consisting of o, s and se; g2 and g3 are each independently selected from benzene, biphenyl, fluorene, naphthalene, phenanthrene, tripheylene, dibenzofuran, dibenzothiophene, dibenzoselenophene, pyridine, pyrimidine, quinoline, isoquinoline, phenanthroline, aza-fluorene, and combinations thereof; l is selected from phenyl, biphenyl, terphenyl and pyridine, and combinations thereof; g2, g3 and l are each optionally further substituted with one or more unfused substituents; r1, r2, and each r3, r4, r5 and r6 are an unfused substituent selected from hydrogen, deuterium, alkyl, alkoxyl, cycloalkyl, cycloalkoxyl, halogen, nitro, nitrile, silyl, benzene, biphenyl, terphenyl, pyridine, and combinations thereof; and r1 and r2 are optionally joined to form a ring.

Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them


Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.. .

Process for making isoquinoline compounds


The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing hif hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (hif)..
Fibrogen, Inc.


Anti-hiv compounds


This invention provides, among other things, tetrahydroisoquinolines useful for treating viral infections, pharmaceutical formulations containing such compounds, as well as methods of inhibiting the replication of a virus, such as hiv, or treating a disease, such as aids.. .
Prosetta Antiviral, Inc.


Processes for preparing isoquinolinones and solid forms of isoquinolinones


Polymorphs of chemical compounds that modulate kinase activity, including pi3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including pi3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof..
Infinity Pharmaceuticals, Inc.


Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors


The present invention provides compounds of formula (i), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor xia inhibitors or dual inhibitors of fxia and plasma kallikrein.
Bristol-myers Squibb Company


Heterocyclic compounds and methods of their use


The present invention relates generally to compounds that are useful in antagonizing the angiotensin ii type 2 (at2) receptor. More particularly, the invention relates to substituted isoquinoline compounds and their use as at2 receptor antagonists.
Novartis Ag


Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds


Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (i), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described.
Rexahn Pharmaceuticals, Inc.


Novel photochromic tetrahydroindolizines


Photochromic tetrahydroindolizines (this) bearing dihydroisoquinoline derivatives as heterocyclic bases and central fluorene groups have been synthesized via different chemical and photochemical pathways. Three alternative pathways for the synthesis of the target photochromic thi-based pyridazinopyrrolo[1,2-b]isoquinolines via in situ trapping with hydrazine hydrate are also provided.
Umm Al-qura University


Pharmaceutical formulations of a hif hydroxylase inhibitor


The present disclosure relates to pharmaceutical formulations of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid and methods of use thereof.. .
Fibrogen, Inc.


H3 receptor antagonist for use in the treatment of alzheimer's disease


This disclosure relates to methods of using 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of alzheimer's disease, other tauopathies and related neurodegenerative diseases.. .

Phthalazinones and isoquinolinones as rock inhibitors


Or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective rock inhibitors.

Pyrazinoisoquinoline compounds


Where the designation (r) indicates that the designated carbon has the (r) stereochemistry; and wherein z1 is hydrogen or fluorine; z2 is hydrogen, deuterium, or fluorine; z3 is deuterium; z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both z1 and z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel..

Tetrahydroisoquinolines as selective nadph oxidase 2 inhibitors


Wherein “” represents a single or double bond, r1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; ra is hydrogen, —ch2r2, r3, or —so2r4; r2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; r3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; r4 is lower aliphatic, or substituted or unsubstituted aryl; and r5 is hydrogen, halogen, or lower aliphatic.. .

Synthesis and use of dual tyrosyl-dna phosphodiesterase i (tdp1) - topoisomerase i (top1) inhibitors


The invention described herein pertains to the synthesis and use of certain n-substituted indenoisoquinoline compounds which inhibit the activity tyrosyl-dna phosphodiesterase i (tdp1) or topoisomerase i (top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel n-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel n-substituted indenoisoquinoline compounds..
Purdue Research Foundation


Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


Or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, r15, a, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, r15, a, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, a, b, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof


Wherein r1 to r6, n and m are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.. .

Pyrazinoisoquinoline compounds


This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel.
Concert Pharmaceuticals, Inc.


Phenoxyethyl dihydro-1h-isoquinoline compounds


The present invention provides a compound of the formula i: wherein r is h or f; or a pharmaceutically acceptable salt thereof.. .
Eli Lilly And Company


Substituted 7-azabicycles and their use as orexin receptor modulators


The present invention is directed to compounds of formula i: wherein ring a is phenyl, naphihalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyi, tlisazolyl, isoxazolvl, pyrazolyl, imidazothiazolyi, benzimidazolyl, or indazolyi; r1 is h, alky], aikoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazofyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazmyl, piperazinyl, pyrazolyl, oxadiazolvl, pyrrolidinyl, thiophenyi, morpholinyl, or dialkyiamino; r2 is h, alkyl, aikoxy, hydroxyalkylene, or halo; z is nh, n-alkyl, or o; r5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazmyl, qumazolinyi, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, aikoxy, or halo; and n is 0 or 1, methods of making the compounds of formula 1 are also described. The invention also relates to pharmaceutical compositions comprising compounds of formula i.
Janssen Pharmaceutica Nv


Isoquinoline derivatives


For the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, parkinson's disease, dementia, alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine or cocaine.. .

Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)


Wherein cy, l1, g, and r1 are as described herein. The present invention relates to novel compounds according to formula (i) that antagonize gpr84, a g-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (ibd), rheumatoid arthritis, vasculitis), lung diseases (e.g.

Method for producing 3,4-dihydroisoquinoline derivatives and production intermediates of same


Provided are an efficient method for producing 3,4-dihydroisoquinoline derivatives and useful production intermediates thereof. Provided is a method for producing 3,4-dihydroisoquinoline derivatives represented by general formula (1), comprising converting a compound represented by general formula (3) in the presence of acid after reacting with an aniline derivative, or converting a compound represented by general formula (3) by reacting with an aniline derivative in the presence of an acid..
Mitsui Chemicals Agro, Inc.


Methods and compositions useful for treating diseases involving bcl-2 family proteins with isoquinoline and quinoline derivatives


The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell lymphoma).

Salts and solid forms of isoquinolinones and composition comprising and methods of using the same


Solid forms of chemical compounds that modulate kinase activity, including pi3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including pi3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof..
Infinity Pharmaceuticals, Inc.


Processes for preparing tetrahydroisoquinolines


Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and compositions comprising the tetrahydroisoquinolines and other compounds, e.g, intermediates and by-products of the processes described herein. Pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression are also disclosed..
Bristol-myers Squibb Company


Novel mixed μ agonist/ δ antagonist opioid analgesics with reduced tolerance liabilities and uses thereof


An opioid narcotics used for the treatment of moderate-to-severe pain that primarily exert their analgesic effects through μ receptors. Although, traditional μ agonists can cause undesired side effects, including tolerance, addition of δ antagonists can attenuate said side effects.
West Virginia University


Novel naphthyridines and isoquinolines and their use as cdk8/19 inhibitors


The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cdk8/19, and for the treatment of cdk8/19-related disorders.. .
Cancer Research Technology, Ltd.


Isoquinolines as potassium ion channel inhibitors


A compound of formula (i) (i) wherein a, r1, r1a, r3 and r24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, ikur-associated disorders, and other disorders mediated by ion channel function..
Bristol-myers Squibb Company


Cyanoisoquinoline compounds and methods of use thereof


The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoictin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:.
Fibrogen, Inc.


Drug combination


The invention provides a composition which comprises (a) a pde3/pde4 inhibitor which is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β2-adrenergic receptor agonist.. .
Verona Pharma Plc


Crystalline forms of -acetic acid


The present disclosure relates to crystalline forms of {[1-cyano-5-(4-chlorophenoxy)-4-hydroxy-isoquinoline-3-carbonyl]-amino}-acetic acid (compound a), the process of preparing crystalline forms of compound a, the pharmaceutical compositions containing them, and the methods of use thereof.. .
Fibrogen, Inc.


Drug combination


The invention provides a composition which comprises (a) a pde3/pde4 inhibitor which is 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2h-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.. .
Verona Pharma Plc


Crystalline form of 6-[(4s)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine


The present disclosure generally relates to a crystalline form of 6-[(4s)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form..
Albany Molecular Research, Inc.


Iridium complex and organic light-emitting device including the same


The present invention provides a novel iridium complex and an organic light-emitting device including the novel iridium complex. The novel iridium complex includes three ligands, and two of them have a phenyl-naphtho[2,1-f]isoquinoline skeleton.
Canon Kabushiki Kaisha


Substituted dihydroisoquinolinone compounds


In which r1, r2, r3, r4, l, x and z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.. .

Tetrahydroisoquinolin-1-one derivative or salt thereof


To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (ibs). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (bb2) receptor antagonistic action.
Seldar Pharma Inc.


Phthalazinones and isoquinolinones as rock inhibitors


The present invention provides compounds of formula (i) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective rock inhibitors.
Bristol-myers Squibb Company


Substituted isoquinolines as crth2 receptor modulators


The invention provides certain substituted isoquinolines of the formula (i), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of crth2 function..
Merck Sharp & Dohme Corp.


Tetrahydro- and dihydro-isoquinoline prmt5 inhibitors and uses thereof


Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity.
Epizyme, Inc.


Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof


Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity.
Epizyme, Inc.


Process for the preparation of a dpp-iv inhibitor


Wherein r1, r2 and r3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2s,3s,11bs)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-3-yl)-4(s)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form a and form b and to an amorphous form of said compound..

Isoquinoline alkaloid derivative for activating amp-dependent protein kinase


The present invention provides a method for activating the amp-dependent protein kinase (ampk) in a subject comprising administering the subject with a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound having the general formula i, preferably salsolinol or reticuline. The pharmaceutical composition is able to activate ampk, and thus is effective in the regulation of cell growth and metabolism, and the treatment of ampk associated diseases..
Zih Yuan Tang Biotechnology Co., Ltd


Organic light-emitting element and display apparatus


Provided is an organic light-emitting element having high luminous efficiency and a long lifetime. The organic light-emitting element includes a pair of electrodes and an organic compound layer placed between the pair of electrodes, in which the organic compound layer includes an iridium complex having a benzo[f]isoquinoline of a specific structure as a ligand and a metal complex compound of a specific structure..
Canon Kabushiki Kaisha


Thermoplastic resin composition


In the chemical formulae (1) and (2) above, r1 and r2 each independently represent a substituted or unsubstituted linear, branched, or cyclic alkyl group having from 1 to 30 carbon atoms, a substituted or unsubstituted aryl group having from 6 to 30 carbon atoms, or a substituted or unsubstituted arylalkyl group having from 7 to 31 carbon atoms, a is a linear or branched alkylene group having from 2 to 4 carbon atoms, n represents an integer of 0 to 50, q1 and q2 each independently represent at least one kind selected from the group consisting of an ammonium ion, an imidazolium ion, a pyridinium ion, a pyrrolidinium ion, a pyrrolinium ion, a piperidinium ion, a pyrazinium ion, a pyrimidinium ion, a triazolium ion, a triazinium ion, a quinolinium ion, an isoquinolinium ion, an indolinium ion, a quinoxalinium ion, a piperazinium ion, an oxazolinium ion, a thiazolinium ion, and a morpholinium ion.. .

Substituted 7-azabicycles and their use as orexin receptor modulators


Wherein ring a is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; r1 is h, alkyl, alkoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; r2 is h, alkyl, alkoxy, hydroxyalkylene, or halo; z is nh, n-alkyl, or o; r5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of formula i are also described.

Crystalline forms of a prolyl hydroxylase inhibitor


The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.. .
Fibrogen, Inc.


Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


Or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..

Organic light-emitting device and display apparatus


Provided is an organic light-emitting device improved in emission efficiency and lifetime. The organic light-emitting device includes a pair of electrodes and an organic compound layer disposed between the pair of electrodes, in which: the organic compound layer includes a benzo[f]isoquinoline iridium complex of a specific structure and a hydrocarbon compound of a specific structure; and the hydrocarbon compound is a compound formed only of an sp2 carbon atom and a hydrogen atom..
Canon Kabushiki Kaisha


N-substituted indenoisoquinolines and syntheses thereof


N-substituted indenoisoquinoline compounds, and pharmaceutical formulations of n-substituted indenoisoquinoline compounds are described. Also described are processes for preparing n-substituted indenoisoquinoline compounds.
The Government Of The Usa As Represented By The Secretary Of The Dept Of Health And Human Services


Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds


Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents.
Aerie Pharmaceuticals, Inc.


Rho kinase inhibitors


Disclosed are novel substituted 2h-isoquinolin-1-one and 3h-quinazolin-4-one derivatives useful as inhibitors of rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.. .
Aerie Pharmaceuticals, Inc.


Organic light-emitting element


Provided is an organic light-emitting element improved in luminous efficiency and lifetime. The organic light-emitting element includes a pair of electrodes and an organic compound layer placed between the pair of electrodes, in which the organic compound layer includes an iridium complex having a benzo[f]isoquinoline of a specific structure as a ligand and a heterocycle-containing compound of a specific structure..

Drug composition for treating tumors and application thereof


The present invention belongs to the field of medicine and pharmaceutical chemistry, specifically relates to novel antitumor pharmaceutical combination, and particularly relates to pharmaceutical combination of bisbenzylisoquinoline alkaloids (e.g. Berbamine and tetrandrine) and anthracene compounds (e.g.

Inhibitors of bruton's tyrosine kinase


This application discloses the btk inhibitor compounds 6-tert-butyl-8-fluoro-2-{3-hydroxymethyl-4-[1-methyl-5-(1′-methyl-1′,2′,3′,4′,5′,6′-hexahydro-[3,4′]bipyridinyl-6-ylamino)-6-oxo-1,6-dihydro-pyridazin-3-yl]-pyridin-2-yl}-2h-phthalazin-1-one, 2-(2-{3-[5-(5-azetidin-1-ylmethyl-1-methyl-1h-pyrazol-3-ylamino)-1-methyl-6-oxo-1,6-dihydro-pyridazin-3-yl]-2-hydroxy methyl-phenyl}-8-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl)-2-methyl-propionitrile, and 6-tert-butyl-2-[2-hydroxymethyl-3-(5-{5-[(2-methoxy-ethylamino)-methyl]-pyridin-2-ylamino}-6-oxo-1,6-dihydro-pyridin-3-yl)-phenyl]-3,4-dihydro-2h-isoquinolin-1-one, formulations thereof, and methods of treatment of asthma, as described herein.. .

The synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indenes


A procedure for the synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indene is described. The process involves the use of osmium tetroxide to cleave the indene double bond forming the keto aldehyde product, which is then combined with a substituted amine forming the substituted isoquinoline.

Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin


With r1, r2, r3, r4, r5, r6, r7, r8, and r14 defined herein.. .

Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors


The present invention provides compounds of formula (i): (formula (i)) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
Bristol-myers Squibb Company


Compositions and methods for producing benzylisoquinoline alkaloids


The present invention relates to host cells that produce compounds that are characterized as benzylisoquinolines, as well as select precursors and intermediates thereof. The host cells comprise one, two or more heterologous coding sequences wherein each of the heterologous coding sequences encodes an enzyme involved in the metabolic pathway of a benzylisoquinoline, or its precursors or intermediates from a starting compound.
California Institute Of Technology


Crystalline forms of a factor xia inhibitor


The instant invention provides crystalline forms of (s,e)-4-(2-(3-(3-chloro-2-fluoro-6-(1h-tetrazol-1-yl)phenyl)acryloyl)-5-(4-methyl-2-oxopiperazin-1-yl)-1,2,3,4-tetrahydroisoquinoline-1-carboxamido)benzoic acid and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.. .
Bristol-myers Squibb Company


Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors


The present invention provides compounds of formula (i): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
Bristol-myers Squibb Company


Process for the preparation of pyrido[2,1-a] isoquinoline derivatives by catalytic asymmetric hydrogenation of an enamine


Wherein r2, r3, r4 and prot are as defined in the specification.. .

Drug composition for treating tumors and application thereof


The present invention belongs to the field of medicine and pharmaceutical chemistry, specifically relates to novel antitumor pharmaceutical combinations, and particularly relates to pharmaceutical combinations of bisbenzylisoquinoline alkaloids (e.g. Berbamine and tetrandrine) and imatinib mesylates and their use in treating tumors..
Hangzhou Bensheng Pharmaceutical Co., Ltd.


Process for preparing (1s)-1-phenyl-3,4-dihydro-2(1h)-isoquinoline-carboxylate


In formula i and ii, r is an alkyl or a substituted alkyl; lg is a leaving group.. .

N-substituted indenoisoquinolines and syntheses thereof


N-substituted indenoisoquinoline compounds, and pharmaceutical formulations of n-substituted indenoisoquinoline compounds are described. Also described are processes for preparing n-substituted indenoisoquinoline compounds.
The Government Of The United States Of America As Represented By The Secretary Of The Department Of


Pesticide having an insecticide, acaricide and nematicide action based on isoquinoline alkaloids and flavonoids


The present invention relates to a pesticide having an insecticide, acaricide and nematicide action obtained from plant extracts that have important synergic interactions in their pesticide activity, the characteristics of which are efficient control of insects, mites and nematodes; low toxicity for mammals and low persistence in the environment. This pesticide is a composition based on plant extracts which is characterized because it is constituted by: isoquinoline alkaloids and their derivatives (0.1-20%) and flavonoids and their glycosylated derivatives (0.001-10%).
Promotora Tecnica Industrial, S.a. De C.v.


(aza-)isoquinolinone derivatives


In which r1, x, y and n have the meanings indicated in claim 1, are inhibitors of tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.. .

Alpha adrenergic receptor modulators


Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure.
Allergan, Inc.


Tetrahydroisoquinolines and intermediates therefor


Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4s)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form..
Albany Molecular Research, Inc.


Asymmetrical reversible neuromuscular blocking agents of ultra-short, short, or intermediate duration


We describe ultra-short, short, and intermediate duration neuromuscular blocking compounds, reversible by cysteine or similar compounds, that are bisquaternary diesters of chlorofumaric, fumaric, or maleic acids where the quaternary groups are very different, creating a highly asymmetrical molecule where one quaternary includes an isoquinolinium ring system and the other includes a morpholinium, piperidinium, piperazinium, or pyrrolidinium system, pharmaceutical compositions, methods to use such compounds and compositions, and kits.. .
Cornell University


Isoquinoline-5-carboxamide derivative having inhibitory activity for protein kinase


A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (i), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases.. .
Hanmi Pharm. Co., Ltd.


Process for making isoquinoline compounds


The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing hif hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (hif)..
Fibrogen, Inc.


Ionically bonded salt having reactive group and thermoplastic resin composition containing same


In chemical formulas (1) and (2) above, r1 and r2 each independently represent a substituted or unsubstituted linear, branched, or cyclic alkyl group having from 1 to 30 carbon atoms, a substituted or unsubstituted aryl group having from 6 to 30 carbon atoms, or a substituted or unsubstituted arylalkyl group having from 7 to 31 carbon atoms, a is a linear or branched alkylene group having from 2 to 4 carbon atoms, n represents an integer of 0 to 50, and q1 and q2 each independently represent at least one kind selected from the group consisting of an ammonium ion having an ethylenically unsaturated bond, an imidazolium ion having an ethylenically unsaturated bond, a pyridinium ion having an ethylenically unsaturated bond, a pyrrolidinium ion having an ethylenically unsaturated bond, a pyrrolinium ion having an ethylenically unsaturated bond, a piperidinium ion having an ethylenically unsaturated bond, a pyrazinium ion having an ethylenically unsaturated bond, a pyrimidinium ion having an ethylenically unsaturated bond, a triazolium ion having an ethylenically unsaturated bond, a triazinium ion having an ethylenically unsaturated bond, a quinolinium ion having an ethylenically unsaturated bond, an isoquinolinium ion having an ethylenically unsaturated bond, an indolinium ion having an ethylenically unsaturated bond, a quinoxalinium ion having an ethylenically unsaturated bond, a piperazinium ion having an ethylenically unsaturated bond, an oxazolinium ion having an ethylenically unsaturated bond, a thiazolinium ion having an ethylenically unsaturated bond, and a morpholinium ion having an ethylenically unsaturated bond.. .

Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)


Or a pharmaceutically acceptable salt thereof, wherein r′, r1 through r7 and ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (pde10a) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type ii diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases..

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


Or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..

Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase i inhibitors


The invention described herein pertains to substituted indenoisoquinoline compounds as described herein, wherein ra, rd, w, x and y are defined herein, pharmaceutical compositions and formulations comprising the indenoisoquinoline compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.. .
Purdue Research Foundation


Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto


The disclosure relates to compounds and compositions for bone formation, fracture treatment, bone grafting, bone fusion, cartilage maintenance and repair, and methods related thereto. In certain embodiments, the disclosure relates to compositions comprising one or more compound(s) disclosed herein, such as 2-(2-methoxybenzylidene)-1-indan-one; n-(4-arsonophenyl)glycine; 1,2-benzenedicarboxylic acid, 1-(1-methylheptyl)ester; (4′-hydroxybiphenyl-4-yl) (phenyl)methanone; 2,2-dimethylchroman-6-carboxylic acid, (4,7-dihydroxy-8-methyl-2-oxo-2h-chromen-3-yl)amide; ethyl 2-((4-chlorophenyl)thio)-1,3-benzothiazol-6-yl carbamate; ethyl (2-(azepan-1-yl)benzo[d]thiazol-6-yl) carbamate; porfiromycin; 1,3-benzodioxol-5-yl-[4-(3,4,5-trimethoxybenzoyl)-3-furyl]methanone; tricinolone acetophenonide; 2,4-bis(3,4-dimethoxyphenyl)-4h-pyrano[3,2-c]chromen-5-one; methyl 5-fluoro-4-methoxy-2,6-dioxohexahydro-5-pyrimidine carboxylate; 5-(naphthalen-1-yl)-1-phenyl-1h-tetrazole; 5-(2-phenylquinolin-4-yl)-1,3,4-oxadiazol-2-ol; n-[2,4,5-trimethyl-4-(trichloromethyl)cyclohexa-2,5-dien-1-ylidene]hydroxylamine; 4-benzoyl-3,4-dihydro-benzo[f]quinoline-3-carbonitrile; 2-nitro-3-phenylspiro[cyclopropane-1,9′-fluorene]; 3-[4-(furan-2-ylmethyl)-5-sulfanylidene-1,2,4-dithiazolidin-3-ylidene]-1,1-dimethyl-thiourea; (6-acetamido-7-methyl-5,8-dioxo-2,3-dihydro-1h-pyrrolo[1,2-a]benzimidazol-3-yl)2-methoxyacetate; 5-iodo-1h-indole-2,3-dione; 4,5-dihydro-1,2,9,10-tetramethoxy dibenzo[de,g]quinoline-6-carboxylic acid, ethyl ester; [2,6-bis(2,4-dimethylphenyl)-4-(2-methoxyacetyl)oxy-phenyl]2-methoxyacetate; 5,11-dimethyl-2-(2-piperidin-1-ylethyl)-6h-pyrido[4,3-b]carbazol-2-ium-9-ol; 2-[3-[[4-[(3-nitroacridin-9-yl)amino]phenyl]sulfamoyl]propyl]guanidine; 1-[[2-(dimethylamino)ethyl]amino]-7-hydroxy-4-methyl-9h-thioxanthen-9-one; 5-amino-1h-1,2,4-triazole-3-carboxylic acid, methyl ester; methyl n-cyano-n′-prop-2-en-1-ylcarbamimidothioate; 5,7-dinitro-8-quinolinol; 5-nitrosoquinolin-8-ol; cantharidin; 1,7-diaminoacridine; 3-methyl-3-(1-naphthyl)-2-benzofuran-1(3h)-one; dichlorolapachol; lycobetaine; 6-(1-aziridinyl)-2,3-dihydro-3-(propionyl)-7-methyl-1h-pyrrolo[1,8]-dione; 4-nitroestrone 3-methyl ether; 5,11-dimethyl-6h-pyrido[4,3-b]carbazole-1-carboxamide hydrochloride; 5-methoxysterigmatocysin; (6-acetamido-7-methyl-5,8-dioxo-2,3-dihydro-1h-pyrrolo[1,2-a]benzimidazol-3-yl)2-methoxyacetate; horminon; 7′,8′-dimethyl-2′-oxo-4′,4a′,6a′,7′-tetrahydro-2′h-spiro[oxirane-2,1′-pentaleno[1,6a-c]pyran]-5′-carboxylate; nybomycin acetate; 5h-[1,6]indeno[1,2-c]isoquinoline-5,12-dione; 2,3-dimethoxy-6-methyl-nitidine; iproplatin; 3-[(deoxyhexosyl)oxy]-2-(3,4-di-hydroxyphenyl)-6,8-dihdroxy-4h-1-benzopyran-4-one; 2-o-benzyl 8-o-methyl 3-(4-methylphenyl)sulfonyl-4,5-dioxo-6h-pyrrolo[3,2-e]indole-2,8-dicarboxylate; 6-bromo-5,8-dihydroxy-7-[4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl]naphthalene-1,4-dione; 5-methylbenzo[c]phenanthridin-5-ium-2,3,8,9-tetrol; (6-acetyl-4-oxo-1,3-diphenyl-2-sulfanylidenethieno[2,3-d]pyrimidin-5-yl)-2,4-dichlorobenzoate; n—[c-[4-[bis(2-cyanoethyl)amino]-2-methylphenyl]-n-(4-methylanilino)carbonimidoyl]imino-4-methylbenzamide; gelcohol; curcumin; tirandamycin; noscapine; aristolochic acid; himbacine; fumagillin; fumitremorgin c; physalin b; derivatives, or salt thereof, for use in bone growth processes.
Emory University


Method of cleaning residue from a surface using a high efficiency disposable cellulosic wiper


An absorbent paper sheet for tissue or towel includes an amount by weight of pulp-derived papermaking fibers, and an amount by weight of fibrillated regenerated cellulosic microfibers prepared from a cellulosic dope of dissolved cellulose comprising a solvent selected from tertiary amine n-oxides, cellulose dissolving imidazolium salts, cellulose dissolving pyridinium salts, cellulose dissolving pyridazinium salts, cellulose dissolving pyrimidinium salts, cellulose dissolving pyrazinium salts, cellulose dissolving pyrazolium salts, cellulose dissolving oxazolium salts, cellulose dissolving 1,2,3-triazolium salts, cellulose dissolving 1,2,4-triazolium salts, cellulose dissolving thiazolium salts, cellulose dissolving piperidinium salts, cellulose dissolving pyrrolidinium salts, cellulose dissolving quinolinium salts, and cellulose dissolving isoquinolinium salts.. .
Georgia-pacific Consumer Products Lp


Pyrazinoisoquinoline compounds


Where the designation (r) indicates that the designated carbon has the (r) stereochemistry; and wherein z1 is hydrogen or fluorine; z2 is hydrogen, deuterium, or fluorine; z3 is deuterium; z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both z1 and z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel..

Tritoqualine for use in the treatment of cystic fibrosis


The present invention relates to the use of a histamine h4 agonist molecule, the enantiomers of the (amino-7 triethoxy-4,5,6 oxo-1 dihydro-1,3 isobenzofurannyl-3)-1methoxy-8 methyl-2 methylenedioxy-6,7 tetrahydro-,2,3,4 isoquinoline or tritoqualine for the treatment of respiratory impairment caused by cystic fibrosis and the reduction and prevention of bronchial superinfections.. .

Synthesis and use of dual tyrosyl-dna phosphodiesterase i (tdp1) - topoisomerase i (top1) inhibitors


The invention described herein pertains to the synthesis and use of certain n-substituted indenoisoquinoline compounds which inhibit the activity tyrosyl-dna phosphodiesterase i (tdp1) or topoisomerase i (top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel n-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel n-substituted indenoisoquinoline compounds..

Thiazolyl- and oxazolyl-isoquinolinones and methods for using them


The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(adp-ribose) polymerase (parp). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders..



Isoquinolin topics:
  • Isoquinolin
  • Quinoline Derivatives
  • Carbon Atoms
  • Praziquantel
  • Crystallin
  • Pharmaceutically Acceptable Salt
  • Cycloalkyl
  • Alkyl Group
  • Sulfonamide
  • Solifenacin
  • Cancer Cells
  • Cancer Cell
  • Viral Infection
  • Human Immunodeficiency Virus
  • Immunodeficiency


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