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Isoquinolin

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


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NEW New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
Boehringer Ingelheim International Gmbh
February 15, 2018 - N°20180044335

The present invention encompasses compounds of general formula (i) wherein the groups r1 to r9, x1 and x2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e. G. Cancer, pharmaceutical preparations containing such compounds and their uses as ...
NEW 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.
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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. ...
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Isoquinoline derivatives as mgat2 inhibitors
Merck Sharp & Dohme Corp.
January 11, 2018 - N°20180009796

The compounds of formula i act as mgat2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
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 ...
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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.
Tetrahydroisoquinoline estrogen receptor modulators and uses thereof
November 09, 2017 - N°20170320871

And stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituent and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the formula i compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen ...
Substituted 1,2,3-triazol-1-yl-methyl-2,3-dihydro-2-methyl-6-nitroimidazo[2,1-b]oxazoles as anti-mycobacterial agents and a process for ...
November 02, 2017 - N°20170313721

The present invention relates to new generation of triazole functionality containing 6-nitro-2,3-dihydroimidazooxazole agents for general formula i, their method of preparation and their use as drugs for treatment of tuberculosis, mdr-tb and xdr-tb either alone or in combination with other anti-tubercular agents. In general formula 1, x is selected from a group (ch2)n or a direct bond, where n ...
Isoquinolin-3-yl carboxamides and preparation and use thereof
November 02, 2017 - N°20170313682

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 ...
Isoquinolin-3-yl carboxamides and preparation and use thereof
November 02, 2017 - N°20170313681

Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure 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, alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated ...
Tyrosine hydroxylase variants and methods of use thereof
The Regents Of The University Of California
October 26, 2017 - N°20170306301

The present disclosure provides a variant tyrosine hydroxylase that provides for increased production of l-dopa in a host cell that expresses the tyrosine hydroxylase. The present disclosure provides nucleic acids encoding the variant tyrosine hydroxylase, and host cells genetically modified with the nucleic acids. The present disclosure provides methods of making l-dopa in a host cell. The present disclosure provides ...
Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
October 26, 2017 - N°20170305880

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.
Tetrahydroisoquinoline derivatives
Ucb Biopharma Sprl
October 26, 2017 - N°20170304292

The present invention relates to tetrahydroisoquinoline derivatives according to formula (i), which are positive allosteric modulators of d1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which d1 receptors play a role.
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