Pyrrolo[1,2-f][1,2,4]triazines useful for treating respiratory syncitial virus infections
Granted: August 28, 2018
Patent Number:
10059716
Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.
Compounds and combinations for the treatment of HIV
Granted: August 28, 2018
Patent Number:
10059697
Provided are compounds, compositions, combinations, kits, uses, and methods for treating HIV in a human being using such compounds or combinations with proteasome inhibitors.
Cot modulators and methods of use thereof
Granted: August 28, 2018
Patent Number:
10059695
The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
Tank-binding kinase inhibitor compounds
Granted: August 7, 2018
Patent Number:
10040781
Compounds having the following formula (I) and methods of their use and preparation are disclosed:
Use of solid carrier particles to improve the processability of a pharmaceutical agent
Granted: August 7, 2018
Patent Number:
10039718
The invention provides a composition comprising, a compound of formula (I): or a pharmaceutically acceptable salt thereof and a plurality of solid carrier particles, as well as methods for using the composition to inhibit the activity of cytochrome P-450.
Substituted 2,3,4,5,7,9,13,13a-octahydro-1,5-methanopyrido[1?,2?:4,5]pyrazino[1,2-a][1,3]diazepines and methods for treating viral infections
Granted: July 31, 2018
Patent Number:
10035809
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Synthesis of an antiviral compound
Granted: July 24, 2018
Patent Number:
10030033
The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
Processes and intermediates for the preparation of 1?-substituted carba-nucleoside analogs
Granted: July 17, 2018
Patent Number:
10023600
Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,2-f][1,2,4]triazinyl heterocycles of Formula I.
Benzimidazole derivatives as bromodomain inhibitors
Granted: July 10, 2018
Patent Number:
10017501
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, and R5 are described herein.
Syk inhibitors
Granted: June 26, 2018
Patent Number:
10005774
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods…
Method for treating a pulmonary hypertension condition
Granted: June 12, 2018
Patent Number:
9993475
A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
2?-chloro aminopyrimidinone and pyrimidine dione nucleosides
Granted: May 29, 2018
Patent Number:
9982006
Provided herein are formulations, methods and substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds.
Methods for treating cancers
Granted: May 22, 2018
Patent Number:
9974792
Disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I: or a pharmaceutically acceptable salt thereof. The subject may be very high risk or high risk for the cancer. The subject who has the cancer may also be refractory to at least one chemotherapy treatment, or is in relapse after treatment with chemotherapy, or both. The cancer may be a…
Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
Granted: May 15, 2018
Patent Number:
9968601
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods…
Pyrazolo[1,5-A]pyrimidines for antiviral treatment
Granted: May 1, 2018
Patent Number:
9957275
The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
Benzimidazole and imadazopyridine carboximidamide compounds
Granted: April 24, 2018
Patent Number:
9951065
The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.
Therapeutic compounds
Granted: April 24, 2018
Patent Number:
9951043
Compounds of formula (I) or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
Methods for treating virus infections
Granted: April 24, 2018
Patent Number:
9949994
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Apoptosis signal-regulating kinase inhibitors
Granted: April 17, 2018
Patent Number:
9943521
The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary…
Compounds for the treatment of HIV
Granted: April 17, 2018
Patent Number:
9944619
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
