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Isoquinolin patents



      
           
This page is updated frequently with new Isoquinolin-related patent applications. Subscribe to the Isoquinolin RSS feed to automatically get the update: related Isoquinolin RSS feeds. RSS updates for this page: Isoquinolin RSS RSS


Date/App# patent app List of recent Isoquinolin-related patents
10/16/14
20140309253
 Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde 10a) patent thumbnailSubstituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde 10a)
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..
10/09/14
20140302987
 Use of substituted isoquinolinones, isoquinolindiones, isoquinolintriones and dihydroisoquinolinones or in each case salts thereof as active agents against abiotic stress in plants patent thumbnailUse of substituted isoquinolinones, isoquinolindiones, isoquinolintriones and dihydroisoquinolinones or in each case salts thereof as active agents against abiotic stress in plants
For enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.. .
10/02/14
20140296214
 Substituted tetrahydroisoquinoline compounds as factor xia inhibitors patent thumbnailSubstituted 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..
09/18/14
20140275161
 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.
09/18/14
20140275160
 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.
09/18/14
20140275158
 Cyclohexyl isoquinolinone compounds patent thumbnailCyclohexyl isoquinolinone compounds
The invention relates to compounds of formula (i): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of mdm2 and/or mdm4, or variants thereof..
09/18/14
20140275135
 Salts and solid forms of isoquinolinones and composition comprising and methods of using the same patent thumbnailSalts 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..
09/18/14
20140275129
 Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds patent thumbnailTetrahydroisoquinolin-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.
09/18/14
20140275101
 Crystalline form of 6-[(4s)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine patent thumbnailCrystalline 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..
09/18/14
20140275065
 Substituted 7-azabicyles and their use as orexin receptor modulators patent thumbnailSubstituted 7-azabicyles 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.
09/18/14
20140275061
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..
09/18/14
20140274960
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..
09/18/14
20140273109
Benzylisoquinoline alkaloids (bia) producing microbes, and methods of making and using the same
Aspects of the invention include host cells that are engineered to produce benzylisoquinoline alkaloids (bias). The host cells include heterologous coding sequences for a variety of enzymes involved in synthetic pathways from starting compounds to bias of the host cell.
09/04/14
20140249201
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.
08/28/14
20140243524
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.. .
08/28/14
20140243333
Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods
A functionalized polycyclic compound can have a structure of formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined diels-alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor.
08/21/14
20140235862
Method for producing 4, 4-difluoro-3,4-dihydroisoquinoline derivatives
Is reacted with hydrogen fluoride.. .
08/21/14
20140235593
Substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies
In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention..
08/14/14
20140228576
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..
08/14/14
20140228575
Process for the preparation of solifenacin and salts thereof
The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (r)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (s,r)—((r)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1h)-carboxylate of formula (iv) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (r)-quinuclidin-3-yl phenethylcarbamate involved in the process.
08/07/14
20140221656
Crystalline solvates of 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one hydrochloride
The present invention relates to crystalline solvates of 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.. .
07/24/14
20140206686
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.
07/03/14
20140187785
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.. .
07/03/14
20140187547
Azaindenoisoquinoline topoisomerase i inhibitors
The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase i, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.. .
06/26/14
20140175406
Phosphorescent compounds and organic light emitting diode devices using the same
Where x, y, and z are each selected from the group consisting of carbon and nitrogen, and when x, y, and z are all carbon, r is any one selected from the group consisting of carbazole, α-carboline, β-carboline, γ-carboline, fluorine, dibenzothiophene, dibenzofuran, triphenylsilane, tetraphenylsilane, pyridine, quinoline, isoquinoline, pyrimidine, diphenylphosphineoxide, and substituents thereof.. .
06/05/14
20140154272
Compound and method for modulating opioid receptor activity
The invention provides a compound of formula (i), wherein r1 is h, c(nh)nh2, an amino acid, or a peptide; x is oh, nh2, nhr2, nr2r3, an amino acid, or a peptide; r2 and r3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each r4 and r5 is independently h or ch3; z is 2-amino-2,3-dihydro-1h-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5h-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1h-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that x is not nh2 when r1 is h, r4 is h, r5 is ch3, z is aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided..
05/15/14
20140135306
Hdyroxy substituted isoquinolinone derivatives
The invention relates to compounds of formula (i): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of mdm2 and/or mdm4, or variants thereof..
05/01/14
20140121204
Novel 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.
04/24/14
20140113877
Novel 3,4,4a,10b-tetrahydro-1h-thiopyrano[4,3-c] isoquinoline compounds
In which a, x, r1, r2, r3 and r7 have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.. .
04/24/14
20140112868
Novel tetrahydroisoquinoline compounds for use in the diagnosis and treatment of neurodegenerative diseases
The invention relates to a new class of compounds with high affinity and selectivity towards p-glycoprotein. The invention also relates to the utilization of such compounds in the in vivo diagnosis of neurodegenerative diseases and as medicaments for use in the prevention and treatment of neurodegenerative disease involving p-glycoprotein..
04/17/14
20140107127
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.
04/17/14
20140107117
Thienyl- and furanyl-isoquinolinones and methods for using them
The present invention relates to substituted thienyl- and furanyl-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 thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders..
03/20/14
20140080865
Salts and solvates of a tetrahydroisoquinoline derivative
(s)-2-(diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described..
02/27/14
20140058100
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.
02/13/14
20140046066
Process for the preparation of 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..
02/13/14
20140045846
Isoquinolin-1(2h)-one derivatives as parp-1 inhibitors
There are provided substituted isoquinolin-1(2h)-one derivatives which selectively inhibit the activity of poly (adp-ribose) polymerase parp-1 with respect to poly (adp-ribose) polymerase parp-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
02/06/14
20140038961
3-ureidoisoquinolin-8-yl derivatives
These compounds are useful for the prevention or the treatment of bacterial infections.. .
01/23/14
20140024676
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.. .
01/23/14
20140024675
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.. .
01/16/14
20140018360
Azaindenoisoquinoline topoisomerase i inhibitors
The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase i, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.. .
12/26/13
20130345252
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..
12/19/13
20130338366
Process for the preparation of pyrido [2,1-a] isoquinoline derivatives comprising optical resolution of an enamine
Wherein rco2− is the conjugate base of the resolving agent.. .
12/19/13
20130338187
Novel 1-(1-oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives as n-formyl peptide receptor like-1 (fprl-1) receptor modulators
The present invention relates to novel 1-(1-oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the n-formyl peptide receptor like-1 (fprl-1) receptor.. .
11/28/13
20130317010
Tetrahydroisoquinoline derivative
To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-ht5a receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a n atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-ht5a receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.. .
11/21/13
20130310569
Triazolide based ionic liquids
A method of synthesizing an ionic liquid, includes reacting a 1,2,3-triazole including at least one of a 4-substituent or a 5-substituent with a hydroxide compound having the formula r+oh− in a dehydration reaction, wherein r+ is an ionic liquid cation. R+ is a five-membered heterocyclic cation, an aromatic cation, a sulfonium cation, an ammonium cation, or a phosphonium cation.
11/21/13
20130310370
Drug therapy for preventing or treating glaucoma
There is provided a drug therapy for prevention of glaucoma or prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. Disclosed is a combination of (s)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, and a prostaglandin for prevention or treatment of glaucoma..
11/14/13
20130303565
Use of a new histamine h4 agonist for the treatment of acute leukemia
A method of treating leukemia by administering an h4 agonist of histamine, 7-amino-4,5,6-triethoxy-3-(5,6,7,8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl) phthalide (tritoqualine), to a subject is provided.. .
11/14/13
20130303522
Inhibitor compounds of 11-beta-hydroxysteroid dehydrogenase type 1
The compounds of formula (i) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-hsd1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, alzheimer's disease or neurodegeneration.. .
11/14/13
20130302414
Solubilized capsule formulation of 1,1-dimethylethyl [(1s)-1-carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate
The present disclosure includes various embodiments directed to a solubilized capsule formulation of asunaprevir, 1,1-dimethylethyl[(1s)-1-{[(2s,4r)-4-(7-chloro-4methoxyisoquinolin-1-yloxy)-2-({(1r,2s)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl}carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate, and to methods including asunaprevir.. .
11/07/13
20130296363
Quinoline and isoquinoline derivatives for use as jak modulators
Provided herein are compounds for treatment of jak kinase mediated diseases, including jak2 kinase-, jak3 kinase- or tyk2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions..
10/31/13
20130289275
Process for the preparation of praziquantel
The present disclosure describes a novel, cost-effective process for preparation of a 4-oxo-1,2,3,6,7,11b-hexahydro-4h-pyrazino-[2,1-a]isoquinoline derivatives. Specifically, it discloses a process for the preparation of the anthelmintic drug praziquantel through the use of a novel intermediate, 2-[(2,2-dimethoxyethyl)benzyl amino]-n-phenethylacetamide.
10/31/13
20130289066
Anti-angiogenic compound
A styrylquinoline derivative of structure i or iv or a benzodioxol isoquinoline of structure ii or iii for use in the treatment of an angiogenesis-related disease or disorder. The invention also provides a composition comprising a styrylquinoline derivative of structure i or iv or a benzodioxol isoquinoline of structure ii or iii for use as a medicament..
10/31/13
20130289027
Isoquinoline compounds and methods for treating hiv
Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the human immunodeficiency virus (hiv).. .
10/24/13
20130281473
Substituted isoquinolinones and quinazolinones
Wherein z is ch2 or n—r4 and x, r1, r2, r4, r6, r7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of mdm2 and/or mdm4, or variants thereof..
10/17/13
20130274287
Phenyl-tetrahydroisoquinoline derivatives
Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, a and n are as described herein, compositions including the compounds and methods of using the compounds.. .
10/17/13
20130274286
Nicotinamide phosphoribosyltransferase (nmprtase) inhibitor for glioma therapy
The present invention relates to identification of a compound which inhibits the enzyme nmprtase and glioma cancer cell growth and further used for glioma therapy. Pre-b-cell colony enhancing factor 1 gene (pbef1) encodes nicotinamide phosphoribosyltransferase (nmprtase), which catalyses the rate limiting step in the salvage pathway of nad metabolism in mammalian cells.
10/17/13
20130274269
Novel substituted isoquinoline derivative
The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein r1 and r2 each independently represent a hydrogen atom, or the like; r3 and r4 each independently represent a hydrogen atom, an alkyl group, or the like; r5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and a represents a linear or branched alkylene group having 2 to 6 carbon atoms..
10/10/13
20130267557
Combined use of an alpha-adrenergic receptor antagonist and an anti-muscarinic agent
The combined use of (r)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzene-1-sulfonamide (tamsulosin), or its pharmaceutically acceptable salt, and (1s)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid (3r)-quinuclidin-3-yl ester (solifenacin), or its pharmaceutically acceptable salt, for the preparation of a medicament for the improvement of lower urinary tract symptoms associated with benign prostatic hyperplasia (luts/bph) with a substantial storage component is provided.. .
10/10/13
20130264553
Materials for organic light emitting diode
Organometallic compounds comprising a phenylquinoline or phenylisoquinoline ligand having the quinoline or isoquinoline linked to the phenyl ring of the phenylquinoline or phenylisoquinoline, respectively, via two carbon atoms. These compounds also comprise a substituent other than hydrogen and deuterium on the quinoline, isoquinoline or linker.
10/10/13
20130264529
Near-infrared absorbing synthetic resin composition
A near-infrared ray absorbing synthetic resin composition containing a bipyrrolo isoquinoline compound represented by the following general formula (1) and a synthetic resin. In the formula, r1 and r2 may be identical with or different from each other, and each represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 20 carbon atoms optionally having substituents, an alkoxy group having 1 to 20 carbon atoms optionally having substituents, an aryl group having 6 to 20 carbon atoms optionally having substituents, an arylalkyl group having 7 to 20 carbon atoms optionally having substituents, or a cycloalkyl group having 5 to 12 carbon atoms optionally having substituents.
09/19/13
20130245268
Enantioselective organic anhydride reactions
Disclosed herein is enantioselective synthetic method comprising reacting an enolisable c4-c50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a michael acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones..
09/19/13
20130245036
Crystalline form of an inhibitor of mdm2/4 and p53 interaction
A crystalline form of (s)-1-(4-chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2h-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and mdm2 and/or mdm4, or variants thereof, respectively.. .
08/29/13
20130225616
Crystalline form of pyrimidio[6,1-a] isoquinolin-4-one compound
The current invention is directed towards a polymorph of n-{2-[(2e)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2h-pyrimido[6,1-a]-isoquinolin-3(4h)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of n-{2-[(2e)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2h-pyrimido[6,1-a]-isoquinolin-3(4h)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (i) of n-{2-[(2e)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2h-pyrimido[6,1-a]-isoquinolin-3(4h)-yl]ethyl}urea, wherein said polymorph is determined by single crystal x-ray structural analysis and x-ray powder diffraction pattern.. .
08/29/13
20130224310
Noscapine analogs and their use in treating cancers
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs.
08/08/13
20130203749
Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy
The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are glyt1 inhibitors..
08/01/13
20130197227
Method of preparing tetrabenazine and dihydrotetrabenazine
The present invention relates to a method for preparing tetrabenazine (tbz) and dihydrotetrabenazine (dtbz), and more specifically to a method for preparing tetrabenazine (tbz) and dihydrotetrabenazine (dtbz) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an aza-prins cyclization reaction in the presence of an oxidant and an oxidation reaction.. .
07/25/13
20130190499
Azaisoquinolinone derivatives as nk3 antagonists
The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.. .
07/11/13
20130177655
Preventing or treating agent for glaucoma
A preventing or treating agent for glaucoma is provided. This drug has a strong action of reducing intraocular pressure such that the intraocular pressure can be reduced even from the normal intraocular pressure.
07/04/13
20130172343
Derivatives of 1h-isoindol-3-amine, 1h-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors
The present invention comprises a new class of compounds useful for the modulation of beta-secretase enzyme activity and for the treatment of beta-secretase mediated diseases, including alzheimer's disease (ad) and related conditions. In one embodiment, the compounds have a general formula i: (i).
06/27/13
20130165437
Novel 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.
06/13/13
20130150402
Pharmaceutical composition for treating overactive bladder
A pharmaceutical composition comprising (r)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3r)-quinuclidin-3-yl (1s)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular a pharmaceutical composition for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.. .


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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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