Abstract: The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2?. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 15, 2021
Date of Patent:
April 25, 2023
Assignee:
NiKang Therapeutics, Inc.
Inventors:
Jiping Fu, Yan Lou, Yigang He, Yuetao Shi, Peng Zhou, Xingxing Li
Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: The present disclosure provides certain tri-substituted heteroaryl derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: The present disclosure is directed certain Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and their use in the treatment of diseases mediated by HIF-2? such as cancer. Also provided is the use of HIF-2? inhibitors in combination with a poly (ADP-ribose) polymerase (PARP) inhibitor. In particular, the present disclosure is directed to methods for the treatment of cancers using a HIF-2? inhibitor in combination with a PARP inhibitor and pharmaceutical compositions comprising the same.
Abstract: The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2?. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.