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Isoquinolin patents

      

This page is updated frequently with new Isoquinolin-related patent applications.




 Crystalline form of 6-[(4r)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl]isoquinoline-1-carbonitrile patent thumbnailCrystalline form of 6-[(4r)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl]isoquinoline-1-carbonitrile
This invention relates to a novel crystalline form of 6-[(4r)-4-methyl-1,1-dioxido-1,2,6-thiadiazinan-2-yl]isoquinoline-1-carbonitrile which is useful as a selective androgen receptor modulator (sarm), and to compositions thereof and suitable processes for the preparation thereof.. .
Pfizer Inc.


 Substituted tetrahydroisoquinoline compounds as factor xia inhibitors patent thumbnailSubstituted 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..

 Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds patent thumbnailBeta- 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.


 Treatment of hyperkinetic movement disorders patent thumbnailTreatment of hyperkinetic movement disorders
Methods for treating hyperkinetic diseases and disorders, such as tardive dyskinesia, are provided. In a certain embodiment, the potent vmat2 inhibitor (+)α-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-ol ((+)α-htbz) is used in the methods described herein for treating a subject in need thereof..
Neurocrine Biosciences, Inc.


 Isoquinoline derivatives and use thereof patent thumbnailIsoquinoline derivatives and use thereof
The invention provides compounds of formula (i) and pharmaceutically acceptable salts, solvates, hydrates, n-oxides, or diastereomers thereof: wherein w1, w2, w3, j1, j2, a, r1, r2, r3, r4, r5, a, and b are defined as set forth in the specification. The invention also provides uses of the compounds of any one of formulae (i)-(viii) and the pharmaceutically acceptable salts, solvates, hydrates, n-oxides, or diastereomers thereof.
Purdue Pharma L.p.


 Organic electroluminescent materials and devices patent thumbnailOrganic electroluminescent materials and devices
Novel phosphorescent metal complexes containing 2-phenylisoquinoline ligands with at least two substituents on the isoquinoline ring are provided. The disclosed compounds have low sublimation temperatures that allow for ease of purification and fabrication into a variety of oled devices..
Universal Display Corporation


 Isoquinolinesulfonyl derivative as rho kinase inhibitor patent thumbnailIsoquinolinesulfonyl derivative as rho kinase inhibitor
The present invention discloses a class of isoquinolinesulfonyl derivatives as rho kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereof. Specifically, the present invention relates to a compound as represented by formula (i), or a pharmaceutically acceptable salt thereof..
Medshine Discovery Inc.


 Selective androgen receptor degrader (sard) ligands and methods of use thereof patent thumbnailSelective androgen receptor degrader (sard) ligands and methods of use thereof
This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (sard) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other ar-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, kennedy's disease, amyotrophic lateral sclerosis (als), abdominal aortic aneurysm (aaa), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (ar-fl) including pathogenic and/or resistance mutations, ar-splice variants (ar-sv), and pathogenic polyglutamine (polyq) polymorphisms of ar in a subject.. .
University Of Tennessee Research Foundation


 Drug therapy for preventing or treating glaucoma patent thumbnailDrug 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..
Kowa Co., Ltd.


 Preventive/therapeutic method and preventive/therapeutic agent for complications after cataract surgery patent thumbnailPreventive/therapeutic method and preventive/therapeutic agent for complications after cataract surgery
The present invention relates to a preventive/therapeutic method comprising administering to a subject a medicine containing 4-fluoro-5-{[(2s)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline (ripasudil) or a salt thereof, or a solvate thereof as an active ingredient.. .

Substituted 7-azabicycles and their use as orexin receptor modulators

Wherein 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, or 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.

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.. .

Naphthyl- or isoquinolinyl-substituted isothiazoline compounds

Wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes.

Dupa-indenoisoquinoline conjugates

A targeting ligand-cytotoxic drug conjugate, for example, a dupa-indenoisoquinoline conjugate, is useful for treating cancers, e.g., prostate cancer.. .
Purdue Research Foundation

Indenotriphenylene-based iridium complexes for organic electroluminescence device

Wherein a ring represents an imidazole, a pyridine, a quinoline and an isoquinoline, x1-x2 represents a bidentate ligand, and m, n and r1 to r4 are the same definition as described in the present invention.. .

Combination 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.

Method of making a benzylisoquinoline alkaloid (bia) metabolite, enzymes therefore

There is provided a method of preparing a benzylisoquinoline alkaloid (bia) metabolite comprising: a. Culturing a host cell under conditions suitable for protein production, including a ph of between about 7 and about 10 said host cell comprising: b.
Valorbec SociÉtÉ En Commandite

Therapeutic agent for ocular fundus disease

Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (s)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient..
Kowa Company, Ltd.

Pharmaceutical compositions

The disclosure relates to a pharmaceutical combination of a mdm2/4 inhibitor, namely (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 or (s)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1h-pyrrolo[3,4-d]imidazol-4-one, and a cyclin dependent kinase 4/6 (cdk4/6) inhibitor 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide. In addition, the disclosure relates to a pharmaceutical combination product.
Novartis Ag

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.

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

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

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..

Bromodomain inhibitor

Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion.
Celgene Quanticel Research, 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

[9,10-dimethoxy-3-(2-methylpropyl)-1h,2h,3h,4h,6h,7h,11bh-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto

Wherein r1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (vmat2) and have utility for treating, for example, hyperkinetic disorders.

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..

6-aminoisoquinoline compounds

6-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided.
Aerie Pharmaceuticals, Inc.

Quinazolinone 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

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)

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

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

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

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

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.

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

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

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



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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    This listing is a sample listing of patent applications related to Isoquinolin for is only meant as a recent sample of applications filed, not a comprehensive history. There may be associated servicemarks and trademarks related to these patents. Please check with patent attorney if you need further assistance or plan to use for business purposes. This patent data is also published to the public by the USPTO and available for free on their website. Note that there may be alternative spellings for Isoquinolin with additional patents listed. Browse our RSS directory or Search for other possible listings.


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