Roche Palo Alto LLC

Hoffmann-la Roche Inc.

Nikang Therapeutics, Inc.

Newave Pharmaceutical Inc.

Novartis Ag

Principia Biopharma Inc.

Chugai Pharmaceutical Co.

F. Hoffmann-la Roche Ag

Chugai Seiyaku Kabushiki Kaisha

Guangzhou Lupeng Pharmaceutical Company Ltd.

Yan Lou

Timothy D Owens

Rama K Kondru

Michael Soth

Jiping Fu

Yigang He

Yi Heng Chen

Nolan James Dewdney

Francisco Javier Lopez-Tapia

Robert Than Hendricks

Johannes Cornelius Hermann

Savithri Ramurthy

Matthew T Burger

Christine E Brotherton-Pleiss

Benjamin R Taft

Gisele A Nishiguchi

Joel McIntosh

David Michael Goldstein

Stacy W Remiszewski

Kenneth Albert Brameld

Sharadha Subramanian

Paul Andrew Barsanti

Lifeng Wan

Lina Quattrocchio Setti

Alice C Rico

Bradley E Loe

Valery Rostislavovich Polyakov

Zachary Kevin Sweeney

Michael Patrick Dillon

Aaron Matthew Smith

Todd Richard Elworthy

Naeem Yusuff

Huw Roland Tanner

Robert John Aversa

David Bernard Smith

Eric Brian Sjogren

Sung-Sau So

Fariborz Firooznia

Robert Francis Kester

Roland Joseph Billedeau

Kang Le

Norman Kong

Stephen Matthew Lynch

Cheng Hu

Christophe Michoud

Andrew Forrest Donnell

Buelent Kocer

Xiaochun Han

Daisy Joe DuBois

Hanbiao Yang

Saul Jaime-Figueroa

Kenneth Carey Rupert

Alan Dipesa

Ramona Hilgenkamp

Peter Michael Wovkulich

Steven Gregory Mischke

Romyr Dominique

Tobias Gabriel

Calvin Wesley Yee

Steven Joseph Berthel

Joan Heather Hogg

Daisy Joe Du Bois

Yue Pan

Joshua Paul Gergely Taygerly

Stephen Deems Gabriel

Jenny Tan

Remy Lemoine

Joshua Kennedy-Smith

Joe Timothy Bamberg

Lucja Orzechowski

Huw Rowland Tanner

Yuetao Shi

Peng Zhou

Xingxing Li

Yimin Qian

Ronald Charles Hawley

Matthew C Lucas

Martin Sendzik

Alam Jahangir

Weiya Yun

Shaoqing Chen

Keshab Sarma

Kshitij Chhabilbhai Thakkar

Vivek Rauniyar

John Anthony Moliterni

Jutta Wanner

Yingjie Lai

Jaehyeon Park

Omar Jose Morales

Yan Dong

Martin Weisel

Thomas A Dineen, Jr

Daniel Fishlock

Calvin Yee

Steven Berthel

Jun-Bae Hong

Mark Bartlett

Bradley E Loc

Charles M Cook

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 disclosure includes compounds of Formula (A): wherein R, R, R, R, R, R, R, R, R, R, R, and R, j, k, m, n, Y, W, W, W, W, V, L, Z, Q, Q, Q, and Q, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

Condensed heterocyclic derivates as BCL-2 inhibitors for the treatment of neoplastic diseases

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 sulfonamido derivatives that are Cyclin-dependent kinase 2 (CDK2) inhibitors of Formula (I): for the treatment of diseases treatable by inhibition of CDK2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors

Provided herein are compounds, such as a compound of Formula (I), or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Immunoproteasome 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

Provided herein are compounds, such as a compound of Formula (I), or a pharmaceutically acceptable salt thereof that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

The disclosure includes compounds of Formula (A):

BCL-2 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.

The disclosure includes compounds of Formula (A): wherein R, R, R, R, R, R, R, R, R, R, R, and R, j, k, m, n, Y, W, W, W, W, V, L, Z, Q, Q, Q, and Q, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neurodegenerative disease with these 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

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Pleasanton, CA, United States of America

Yan Lou