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Isoquinolin

Isoquinolin-related patent applications - as published by the U.S. Patent and Trademark Office (USPTO).


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Crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2...
Glaxosmithkline Intellectual Property Development Limited
April 12, 2018 - N°20180099948

Disclosed are novel crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.
Isoquinolin-3-yl carboxamides and preparation and use thereof
Samumed, Llc
April 05, 2018 - N°20180093970

Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of wnt pathway signaling (e. G., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by ...
Condensed-cyclic compound and organic light-emitting device comprising the same
March 15, 2018 - N°20180076392

Wherein, in formulae 1, 2a, and 2b, ring a1 is selected from a benzene group, a naphthalene group, a pyridine group, a pyrimidine group, a pyrazine group, a quinoline group, an isoquinoline group, a quinoxaline group, a quinazoline group, and a cinnoline group; ring a2 is selected from a pyridine group, a pyrimidine group, a pyrazine group, a quinoline group, an ...
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Isoquinoline amide and isoquinoline amide-substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating ...
Vanderbilt University
March 01, 2018 - N°20180057491

Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mglur4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
Ophthalmic compositions
Aerie Pharmaceuticals, Inc.
March 01, 2018 - N°20180055833

The present disclosure provides an ophthalmic composition comprising 4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate or its pharmaceutically acceptable salts; about 0. 01% weight/volume to about 1. 0% weight/volume of a buffer; and about 0. 01% weight/volume to about 10% weight/volume of a tonicity agent.
Beta-amino-isoquinolinyl amide compounds
Aerie Pharmaceuticals, Inc.
February 22, 2018 - N°20180050990

Disclosed are alpha-aryl-beta-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. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular ...
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Bromodomain inhibitor
Celgene Quanticel Research, Inc.
February 15, 2018 - N°20180042914

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. In some ...
Substituted pyrazino[2,2-a]isoquinoline derivatives
Hoffmann-la Roche Inc.
February 08, 2018 - N°20180037582

The present invention relates to compounds of formula of formula i wherein r, r1, r2 and l are as described herein, compositions containing compounds of formula i, methods of manufacture of compounds of formula i and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula i.
Salt of a pyrimido[6,1-a]isoquinolin-4-one compound
Verona Pharma Plc
January 25, 2018 - N°20180021337

The present invention relates to a pharmaceutically acceptable acid addition salt of: (i) 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 (rpl554); and (ii) ethane-1,2-disulfonic acid, ethanesulfonic acid, methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, phosphoric acid or sulfuric acid.
Use of ergot alkaloids as an anthelmintic agent
January 25, 2018 - N°20180021334

Methods for preventing, inhibiting or treating parasitic flatworm infection in a vertebrate are provided that include administering an effective amount of a composition comprising one or more ergot alkaloids, one or more lysergic acid amides, or one or more dimethoxyisoquinoline derivatives
New class of organic phosphors based on derivatives of benzimidazoxanthenoisoquinolinone for led lighting
Philips Lighting Holding B.v.
January 18, 2018 - N°20180016491

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 ...
Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
January 18, 2018 - N°20180016275

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. ...
Pharmaceutical combinations
Novartis Ag
January 18, 2018 - N°20180015092

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 ...
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Tetrahydroisoquinolines as selective nadph oxidase 2 inhibitors
January 11, 2018 - N°20180009762

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 ...
Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them
January 04, 2018 - N°20180002313

Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
Preparative method for carboxylic acids
Zhejiang Zhuji United Chemicals Co., Ltd
December 28, 2017 - N°20170369412

A preparative method for carboxylic acids is disclosed in the present invention. The method is characterized in that: compounds (ii) are reacted in the presence of hydrogen peroxide and base to produce target products (i), as represented by the following reaction scheme: wherein r1 is aryl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, benzothienyl, benzofuranyl, quinolinyl, isoquinolinyl, thiadiazolyl, c1-6 alkyl, c3-6 ...
2-phenethenyltetrahydro isoquinolines useful as anti-hiv compounds
Prosetta Antiviral, Inc.
December 28, 2017 - N°20170368051

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.
Pharmacotherapy for preventing or treating glaucoma
Kowa Company, Ltd.
December 21, 2017 - N°20170360782

A pharmacotherapy is provided for preventing glaucoma or preventing or treating ocular hypertension, the pharmacotherapy providing potent intraocular pressure-lowering action with fast-acting properties and prolonged duration. A combination of (s)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate of (s)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or the salt ...
Heteroaryl substituted pyrrolotriazine amine compounds as pi3k inhibitors
Bristol-myers Squibb Company
December 14, 2017 - N°20170355698

Disclosed are compounds of formula (i); or a salt thereof; wherein qi is (i) cl, br, i, —cn, —ch3, or —cf3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with r1; q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with r2 and r3; and r1, r2, and r3 are defined herein. Also disclosed are methods ...
[9,10-dimethoxy-3-(2-methylpropyl)-1h,2h,3h,4h,6h,7h,11bh-pyrido-[2,1-a]isoquinolin-2-yl]methanol ...
December 07, 2017 - N°20170349586

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. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier or diluent, as well as methods relating to the use in a subject in need thereof.
Tetrahydro- and dihydro-isoquinoline prmt5 inhibitors and uses thereof
Epizyme, Inc.
November 23, 2017 - N°20170334861

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. Methods of using the compounds for treating prmt5-mediated disorders are also described.
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