公开(公告)号：US10772874B2

公开(公告)日：2020-09-15

申请号：US16538208

申请日：2019-08-12

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： Kenneth W. Bair ,  Timm R. Baumeister ,  Alexandre J. Buckmelter ,  Karl H. Clodfelter ,  Peter Dragovich ,  Francis Gosselin ,  Bingsong Han ,  Jian Lin ,  Dominic J. Reynolds ,  Bruce Roth ,  Chase C. Smith ,  Zhongguo Wang ,  Po-Wai Yuen ,  Xiaozhang Zheng

IPC: C07D491/048 ,  C07D487/04 ,  A61K31/4355 ,  A61K31/4365 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

公开(公告)号：US10385058B2

公开(公告)日：2019-08-20

申请号：US15841828

申请日：2017-12-14

Applicant: Genentech, Inc.

Inventor： Danial Beaudry ,  Theresa Cravillion ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Sushant Malhotra ,  Qingping Tian ,  Haiming Zhang ,  Alexander Gmehling ,  Alec Fettes ,  Stephan Bachmann

IPC: C07D487/04 ,  B01J31/24

Abstract: 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. Methods for preparing tricyclic lactam compounds are also provided.

公开(公告)号：US20190105307A1

公开(公告)日：2019-04-11

申请号：US16212360

申请日：2018-12-06

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： Kenneth W. Bair ,  Timm R. Baumeister ,  Alexandre J. Buckmelter ,  Karl H. Clodfelter ,  Peter Dragovich ,  Francis Gosselin ,  Bingsong Han ,  Jian Lin ,  Dominic J. Reynolds ,  Bruce Roth ,  Chase C. Smith ,  Zhongguo Wang ,  Po-Wai Yuen ,  Xiaozhang Zheng

IPC: A61K31/4355 ,  A61K31/496 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/519 ,  C07D471/04 ,  A61K31/55 ,  C07D487/04 ,  C07D491/048 ,  A61K45/06 ,  C07D495/04 ,  C07D491/04 ,  A61K31/5377

CPC classification number: A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

公开(公告)号：US09975856B2

公开(公告)日：2018-05-22

申请号：US15287023

申请日：2016-10-06

Applicant: Genentech, Inc.

Inventor： Stephan Bachmann ,  Serena Maria Fantasia ,  Francis Gosselin ,  Chong Han ,  Stefan Hildbrand ,  Theresa Humphries ,  Christian Jenny ,  Ngiap-Kie Lim ,  Andrew McClory ,  Christian Moessner ,  Pankaj Rege ,  Scott Savage ,  Haiming Zhang

IPC: C07D231/56 ,  C07D405/04 ,  C07C309/73 ,  C07C69/73 ,  C07F5/04 ,  C07C69/612 ,  C07F5/02

CPC classification number: C07D231/56 ,  C07C69/612 ,  C07C69/73 ,  C07C69/738 ,  C07C309/73 ,  C07D405/04 ,  C07F5/025 ,  C07F5/04

Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.

公开(公告)号：US20180086722A1

公开(公告)日：2018-03-29

申请号：US15827985

申请日：2017-11-30

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: C07D239/70 ,  C12P17/16 ,  C07C271/22 ,  C07C269/06

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US09315471B2

公开(公告)日：2016-04-19

申请号：US14401089

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Francis Gosselin ,  Yingqing Ran ,  Travis Remarchuk ,  Scott J. Savage ,  Jeffrey Stults ,  Herbert Yajima

IPC: C07D239/70 ,  C07D403/04 ,  C12P17/16

CPC classification number: C07D239/70 ,  C07D403/04 ,  C12P17/165

Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract translation: 本发明提供了用于制备和纯化羟基化环戊并嘧啶化合物的盐的新方法，其可用作用于治疗诸如癌症的疾病的AKT抑制剂，包括（S）-2-（4-氯苯基）-1- （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） 1-one。

公开(公告)号：US11999749B2

公开(公告)日：2024-06-04

申请号：US17852227

申请日：2022-06-28

Applicant: Genentech, Inc. ,  Hoffmann-La Roche Inc.

Inventor： Francis Gosselin ,  Stefan G. Koenig ,  Eduardo V. Mercado-Marin ,  Andreas Stumpf ,  Daniel Zell ,  Haiming Zhang ,  Stephan Bachmann ,  Diane E. Carrera ,  Michael E. Dalziel ,  Yonghui Ge ,  Jie Zhang ,  Raphael Bigler ,  Laure Elizabeth Simone Finet ,  Regis Jean Georges Mondiere ,  Yuki Nakagawa

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.

公开(公告)号：US11702452B2

公开(公告)日：2023-07-18

申请号：US17517103

申请日：2021-11-02

Applicant: Genentech, Inc.

Inventor： Filip Petronijevic ,  Ngiap-Kie Lim ,  Nicholas Wong ,  Allen Hong ,  Haiyun Hou ,  Xin Linghu ,  Francis Gosselin

IPC: C07K7/64 ,  C07K1/06

CPC classification number: C07K7/64 ,  C07K1/061

Abstract: Methods for making an arylomycin ring of formula t




or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.

公开(公告)号：US10882864B2

公开(公告)日：2021-01-05

申请号：US16460889

申请日：2019-07-02

Applicant: Genentech, Inc.

Inventor： Danial Beaudry ,  Theresa Cravillion ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Sushant Malhotra ,  Qingping Tian ,  Haiming Zhang ,  Alexander Gmehling ,  Alec Fettes ,  Stephan Bachmann

IPC: C07D487/04 ,  B01J31/24

Abstract: 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. Methods for preparing tricyclic lactam compounds are also provided.

公开(公告)号：US10858324B2

公开(公告)日：2020-12-08

申请号：US16555842

申请日：2019-08-29

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: A61K31/517 ,  C07D239/70 ,  C07C269/06 ,  C07C271/22 ,  C12P17/16

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.