Patent classifications
C07D231/38
Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
- David J. Maloney ,
- Alex Gregory Waterson ,
- Ganesh Rai Bantukallu ,
- Kyle Ryan Brimacombe ,
- Plamen Christov ,
- Chi V. Dang ,
- Victor Darley-Usmar ,
- Xin Hu ,
- Ajit Jadhav ,
- Somnath Jana ,
- Kwangho Kim ,
- Jennifer L. Kouznetsova ,
- William J. Moore ,
- Bryan T. Mott ,
- Leonard M. Neckers ,
- Anton Simeonov ,
- Gary Allen Sulikowski ,
- Daniel Jason Urban ,
- Shyh Ming Yang
Provided is a compound of formula (I), ##STR00001##
in which Ar.sup.1, R.sup.1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.
Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.
Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof
The invention provides pyrazolyl guanidine compounds that inhibit F.sub.1F.sub.o-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
Alkylpyrazolyl guanidine F1F0-ATPase inhibitors and therapeutic uses thereof
The invention provides pyrazolyl guanidine compounds that inhibit F.sub.1F.sub.o-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS
The present invention encompasses compounds of the formula (I)
##STR00001##
wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
SULFONYLUREA DERIVATIVES AND USES THEREOF
The present disclosure relates to compounds of Formula (I)
##STR00001##
and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
SULFONYLUREA DERIVATIVES AND USES THEREOF
The present disclosure relates to compounds of Formula (I)
##STR00001##
and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
SYNTHETIC METHOD FOR THE PREPARATION OF A 3-[5-AMINO-4-(3-CYANOBENZOYL)- PYRAZOL COMPOUND
Provided is a process for preparing a compound, comprising the steps of a) Reacting a compound of Formula A (Formula A) with the compound 3 (3) to provide the compound 5 (5) or a salt or solvate thereof, wherein R is a linear or branched C1-C5 alkyl. Further provided is the compound 5 or a salt or solvate thereof. (5) The use of these compounds in the synthesis of 3-[5-Amino-4-(3-Cyanobenzoyl)-Pyrazol-1-yl]-N-Cyclopropyl-4-Methylbenzamide is also provided.