PATENTSCOPE: EN_ALL:nmr AND PA:(Gilead)

THERAPEUTIC HETEROCYCLIC COMPOUNDS (Fri, 01 Mar 2019)
Compounds having the following Formula (I) and/or Formula (II) and methods of their use and preparation are disclosed.
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SOLID FORMS OF AN HIV CAPSID INHIBITOR (Fri, 22 Feb 2019)
The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N-((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
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CHOLINE SALT FORMS OF AN HIV CAPSID INHIBITOR (Fri, 22 Feb 2019)
The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N-((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-lH-cyclopropa[3,4]cyclopenta[l,2-c]pyrazol-l-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.
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CRYSTALLINE FORMS OF ETHYL ((S)-((((2R,5R)-5-(6-AMINO-9H-PURIN-9-YL)-4-FLUORO-2,5-DIHYDROFURAN-2-YL)OXY)METHYL)(PHENOXY)PHOSPHORYL)-L-ALANINATE (GS-9131) FOR TREATING VIRAL INFECTIONS (Fri, 08 Feb 2019)
Crystalline and amorphous forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate (GS-9131), the vanillate, phosphate and xinafoate salts as well as the phosphate acetonitrile solvate thereof, for treating viral infections, such as e.g. HIV.
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CRYSTALLINE FORMS OF (S) 2 ETHYLBUTYL 2 (((S) (((2R,3S,4R,5R) 5 (4 AMINOPYRROLO[2,1-F] [1,2,4]TRIAZIN-7-YL)-5-CYANO-3,4-DIHYDROXYTETRAHYDROFURAN-2 YL)METHOXY)(PHENOXY) PHOSPHORYL)AMINO)PROPANOATE (Fri, 09 Nov 2018)
The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1- f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl) methoxy)(phenoxy)phosphoryl)amino)propanoate (Formula I) for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Fil oviridae, Fiaviviridae,and Paramyxoviridae.
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PD-1/PD-L1 INHIBITORS (Fri, 26 Oct 2018)
Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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APOPTOSIS SIGNAL-REGULATING KINASE INHIBTOR (Fri, 21 Sep 2018)
Provided is a compound of Formula (I) or a pharmaceutically acceptable salt thereof for use in treatment of non-alcoholic steatohepatitis, alcoholic hepatitis, pulmonary arterial hypertension, heart failure with preserved ejection fraction, and diabetic kidney disease. Also provided are amorphous and crystalline forms of the compound of Formula (I) and salts, co-crystals, solvates, and hydrates thereof.
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PHARMACEUTICAL COMPOSITIONS COMPRISING A JAK INHIBITOR (Fri, 21 Sep 2018)
Pharmaceutical compositions comprising filgotinib maleate Form I and uses thereof are described herein.
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PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF (Sat, 08 Sep 2018)
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I which exhibits Acetyl-CoA carboxylase ("ACC") inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.
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PROCESSES FOR THE PREPARATION OF FUNGICIDAL COMPOUNDS (Sat, 08 Sep 2018)
Provided herein are processes for the preparation of stereomerically enriched compounds of Formulas I-014, I-020, I-064, I-074, I-082, I-089, I-090, I-095, I-171, I-181, I-184, I-186, I-189, I-191, I-192, I-193, I-205, I-206, I-208, I-211, I-212, I-213, I-220, I-229, I-231, I-233, I-234, I-246, I-251, I-258, I-259, I-262, I-263, I-285, I-323 and I-400. The compounds described herein exhibit activity as pesticides and are useful, for example, in methods for the control of fungal pathogens and diseases caused by fungal pathogens in plants. A preferred process is directed to preparing a stereomerically enriched compound of Formula V-1 or V-2-F by assymetrical reduction in the presence of a chiral organometallic catalyst.
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 31 Aug 2018)
Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.
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INHIBITORS OF BRUTON'S TYROSINE KINASE (Fri, 31 Aug 2018)
Provided are salts and crystalline forms of 6-amino-9-[(3R)-l-(2- butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, compositions thereof, methods for their preparation, and methods for their use.
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ATAZANAVIR (ATV) ANALOGUES FOR TREATING HIV INFECTIONS (Fri, 10 Aug 2018)
The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, the compound of formula (I) for use in therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I. Preferred compounds are N-[(2S) -1-[2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-(methoxycarbonylamino) -3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(phenyl) methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate atazanavir (ATV) analogues substituted by several heterocycles, such as e.g. pyrazole (Rl); e.g. oxetane (substituent of X2); e.g. pyridine or pyrimidine (X1); e.g. piperazine or 3,8-diazabicyclo[3.2.1]octan (X2).
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COMPOUNDS FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTION (Fri, 10 Aug 2018)
The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.
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PYRAZOLOPYRIMIDINE DERIVATIVES AS CAM KINASE INHIBITORS (Fri, 08 Jun 2018)
The present disclosure relates to compounds that are CaM Kinase inhibitors and to their use in the treatment of various disease states, including atrial fibrillation and myocardial infarction. In particular embodiments, the general structure of the compounds is given by Formula I: (I) wherein R1, R2, R3, R4, R5, R6, R9 and R10 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
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CRYSTALLINE FORMS OF A PHOSPHATE COMPLEX OF A BET INHIBITOR (Fri, 01 Jun 2018)
Salts of (2-cyclopropyl-6-(3,5-dimethylisoxazol-4-yl)-1H- benzo[d]imidazol-4-yl)di(pyridin-2-yl)methanol (Compound I) were prepared and characterized in the solid state: Compound I. Also provided are processes of manufacture and methods of using the salt forms of Compound I.
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SYNTHESIS OF A COMPOUND THAT MODULATES THE ACTIVITY OF BROMODOMAIN-CONTAINING PROTEINS (Fri, 01 Jun 2018)
The present disclosure provides processes for the preparation of a compound of formula I: or a salt or co-crystal thereof, that modulates the activity of bromodomain-containing proteins. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
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CRYSTALLINE FORMS OF DARUNAVIR FREE BASE, HYDRATE, SOLVATES AND SALTS (Fri, 04 May 2018)
The present invention relates to crystalline forms of darunavir free base, hydrate, acetic acid solvate, esylate, besylate, hemisulfate, napsylate, hemiedisylate, tosylate, methyl ethyl ketone (MEK) solvate, methyl tetrahydrofuran (MeTHF) solvate, methyl acetate (MeOAc) solvate and ethyl formate solvate, and to pharmaceutical formulations thereof for treating viral infections.
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BENZOTHIAZOL-6-YL ACETIC ACID DERIVATIVES AND THEIR USE FOR TREATING HIV INFECTION (Fri, 06 Apr 2018)
Compounds disclosed herein including compounds of Formula I: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
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BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS (Fri, 30 Mar 2018)
The present application provides the compounds of formula I or IA or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein s, t, m, n, R1, R2, R3, R4, R5, R6 and R7are as described herein. The compounds of formula I or IA selectively inhibit the activities of PI3K isoforms and are therefore useful in therapeutic treatments, in particular in the treatment of cancer and inflammatory conditions.
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