C07D231/00

Crystalline forms of a TLR7/TLR8 inhibitor

This application relates to various crystalline forms of (S)N-(4-((5-(1,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-4-yl)-3-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)bicyclo[2.2.2]octan-1-yl)morpholine-3-carboxamide in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (hydrates). These materials are useful in the treatment of various autoimmune diseases, including systemic lupus erythematosus, cutaneous lupus, discoid lupus, mixed connective tissue disease, primary biliary cirrhosis, immune thrombocytopenia purpura, hidradenitis suppurativa, dermatomyositis, polymyositis, Sj?gren's syndrome, arthritis, rheumatoid arthritis and psoriasis.

CRYSTALLINE FORMS OF A TLR7/TLR8 INHIBITOR

This application relates to various crystalline forms of (S)N-(4-((5-(1,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-4-yl)-3-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)bicyclo[2.2.2]octan-1-yl)morpholine-3-carboxamide in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (hydrates). These materials are useful in the treatment of various autoimmune diseases, including systemic lupus erythematosus, cutaneous lupus, discoid lupus, mixed connective tissue disease, primary biliary cirrhosis, immune thrombocytopenia purpura, hidradenitis suppurativa, dermatomyositis, polymyositis, Sjgren's syndrome, arthritis, rheumatoid arthritis and psoriasis.

CRYSTALLINE FORMS OF A TLR7/TLR8 INHIBITOR

This application relates to various crystalline forms of (S)N-(4-((5-(1,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-4-yl)-3-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl)methyl)bicyclo[2.2.2]octan-1-yl)morpholine-3-carboxamide in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (hydrates). These materials are useful in the treatment of various autoimmune diseases, including systemic lupus erythematosus, cutaneous lupus, discoid lupus, mixed connective tissue disease, primary biliary cirrhosis, immune thrombocytopenia purpura, hidradenitis suppurativa, dermatomyositis, polymyositis, Sjgren's syndrome, arthritis, rheumatoid arthritis and psoriasis.

Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists

Compounds of the formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein, R.sup.1 is optionally substituted pyrazolyl, and R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X.sub.3 and/or a P2X.sub.2/3 receptor antagonists and methods of making the compounds.

Substituted pyrazoles showing serotonin 5-HT receptor activity

The present invention relates to a medicament for treating neuropsychiatric diseases, comprising a compound of Formula (1): ##STR00001##
or a pharmaceutically acceptable salt thereof, as an active ingredient.

N-hydroxylsulfonamide derivatives as new physiologically useful nitroxyl donors

The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

Substituted pyrazolylpyrazole derivative and use of same as herbicide
09593112 · 2017-03-14 · ·

Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems. ##STR00001##

Histone deacetylase inhibitors

This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Multisubstituted aromatic compounds as inhibitors of thrombin

There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.

T cells having enhanced anti-tumor activity

The invention provides compositions and methods for using adoptive cell therapy (ACT) for treating cancer in a mammal. Cultured T-cells are provided by (a) obtaining an isolated population of T cells, and (b) culturing the isolated T cells ex vivo in the presence of a cytokine and a lactate dehydrogenase inhibitor. The cultured T-cells then can be administered to the mammal.