Novartis Ag

Nikang Therapeutics, Inc.

Novartis Pharma Gmbh

Jiping Fu

Yan Lou

Yigang He

Subramanian Karur

Peichao Lu

Zachary Kevin Sweeney

Xianming Jin

Aregahegn Yifru

Rui Zheng

Mohindra Seepersaud

David Thomas Parker

Joseph Michael Young

Prakash Raman

Pascal Rigollier

Guillaume Lapointe

Patrick Lee

Michael A Patane

Keith Bruce Pfister

Trixi Brandl

Oliver Simic

David Weninger Barnes

Ann Marie Madera

Wooseok Han

Scott Louis Cohen

Branko Radetich

Francois Lenoir

Xiaolin Li

Mahavir Prashad

Yugang Liu

Lei Shu

Alexey A Rivkin

Meiliana Tjandra

Lech Andrzej Ciszewski

Shawn D Britt

Wosenu Mergo

Yuetao Shi

Peng Zhou

Xingxing Li

Mitsunori Kato

Wei Zhang

Andrew Weiss

Andreas Kordikowski

Siyi Jiang

Rajiv Chopra

Yan Dong

Charles M Cook

Rongzhen Chen

David Barnes

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.

Process of preparing 3-fluoro-5(((1R,2AR)-3,3,4,4-tetrafluoro-1,2A-dihydroxy-2,2A,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)-oxy)benzonitrile

The present disclosure provides certain processes of making 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 (Compound 1) and certain polymorphs thereof. Also provided are pharmaceutical compositions comprising a crystalline polymorph form of Compound 1 and processes for preparing such polymorph forms.

Processes of making 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 and polymorphs thereof

The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Tetrahydro-1H-cyclopenta[cd]indene derivatives as hypoxia inducible factor-2(alpha) inhibitors

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.

Fused tricyclic ring derivatives as SRC homology-2 phosphate inhibitors

The present disclosure provides certain 2,3-dihydrobenzo[b]thiophene compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

2,3-dihydrobenzo[b]thiophene derivatives as hypoxia inducible factor-2(alpha) inhibitors

The present disclosure provides certain indane compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Indane derivatives as hypoxia inducible factor-2(α) inhibitors

The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2&#x3b1; (HIF-2&#x3b1;) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2&#x3b1;. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Process of preparing 3-fluoro-5(((1R,2aR)-3,3,4,4-tetrafluoro-1,2a-dihydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)-oxy)benzonitrile

Fused tricyclic ring derivatives as Src homology-2 phosphate inhibitors

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.

Tri-substituted heteroaryl derivatives as Src homology-2 phosphatase inhibitors

The present disclosure is directed certain Hypoxia Inducible Factor 2&#x3b1; (HIF-2&#x3b1;) inhibitors and their use in the treatment of diseases mediated by HIF-2&#x3b1; such as cancer. Also provided is the use of HIF-2&#x3b1; 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&#x3b1; inhibitor in combination with a PARP inhibitor and pharmaceutical compositions comprising the same.

Hypoxia inducible factor-2(alpha) inhibitors and their use in the treatment of diseases

Tetrahydro-1H-cyclopenta[cd]indene derivatives as hypoxia inducible factor-2&#x3b1; inhibitors

The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions and pharmaceutical combinations containing such compounds, as well as methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus (HBV), and for reducing the occurrence of serious conditions associated with HBV. 

Fused tricyclic pyrazolo-dihydropyrazinyl-pyridone compounds as antivirals

The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.

Fused indazole pyridone compounds as antivirals

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Danville, CA, United States of America

Jiping Fu