Hoffmann-la Roche Inc.

Genentech, Inc.

F. Hoffmann-la Roche Ag

Alec Fettes

Francis Gosselin

Haiming Zhang

Ngiap-Kie Lim

Stephan Bachmann

Sushant Malhotra

Qingping Tian

Theresa Cravillion

Danial Beaudry

Alexander Gmehling

Hans Iding

Karthik Nagapudi

Paroma Chakravarty

Andrew McClory

Stefan Abrecht

Cheol Keun Chung

Sarah Robinson

Patrizio Mattei

Rudolf Schmid

Kurt Puentener

Stefan Hildbrand

Jean-Michel Adam

Jie Xu

Michael Dalziel

Kyle Clagg

Ulrich Zutter

Bruno Lohri

Ursula Hoffmann

Joseph Foricher

Serena Maria Fantasia

Sung Won Kim

Gerard Moine

Rene Lebl

Lukas Chytil

Christian Oliver Kappe

Jason Douglas Williams

Kyeong Eun Jung

Hongrim Choi

Leonhard Jaitz

Achim Geiser

Paolo Tosatti

Andrew Mcclory

Kartik Nagapudi

Methods for preparing the Bruton's Tyrosine Kinase ('BTK') inhibitor compound 2-{3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4′]bipyridinyl-2′-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided.

Process for preparing BTK inhibitors

Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use

Methods for preparing the Bruton's Tyrosine Kinase ('BTK') inhibitor compound 2-{3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4&#x2032;]bipyridinyl-2&#x2032;-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.

Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3- fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use

The present invention relates to a novel process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R, Rand Rare each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a]isoquinoline derivatives of the formula I are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Process for the preparation of pyrido[2,1-a] isoquinoline derivatives

This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one useful in the preparation of the DPP-IV inhibitor (S)-1 ((2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7, 11b-hexahydro-2H-pyrido[2,1-a] isoquinolin-3-yl)-4-fluoromethyl-pyrrolidin-2-one

Growing community of inventors

Basel, Switzerland

Alec Fettes