公开(公告)号：US20200062717A1

公开(公告)日：2020-02-27

申请号：US16555842

申请日：2019-08-29

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：US20200010428A1

公开(公告)日：2020-01-09

申请号：US16574933

申请日：2019-09-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH INC.

Inventor： Francis Gosselin ,  Chong Han ,  Hans Iding ,  Reinhard Reents ,  Scott Savage ,  Beat Wirz

IPC: C07D239/70 ,  C07B57/00 ,  C07D239/42 ,  C07D239/54 ,  C12N9/78 ,  C12P41/00 ,  C07C253/30 ,  C07C253/34 ,  C07C255/22

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (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). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

公开(公告)号：US20190388405A1

公开(公告)日：2019-12-26

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

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：US10272072B2

公开(公告)日：2019-04-30

申请号：US15352184

申请日：2016-11-15

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： Kenneth W. Bair ,  Timm R. Baumeister ,  Alexandre Joseph 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: A61K31/4353 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4355 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/496 ,  A61K31/519 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D491/048

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：US20170101380A1

公开(公告)日：2017-04-13

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 ,  C07C309/73 ,  C07C69/73 ,  C07F5/04 ,  C07D405/04

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：US20150274677A1

公开(公告)日：2015-10-01

申请号：US14401092

申请日：2012-05-17

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Sanjeev Kothari ,  Francis Gosselin ,  Scott J. Savage ,  Jeffrey Stults

IPC: C07D239/70

CPC classification number: C07D239/70 ,  A61K31/517 ,  C07D403/04

Abstract: Disclosed is (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 monohydrochloride, forms, formulations, pharmaceutical compositions, processes of manufacturing and methods of use thereof.

Abstract translation: 公开了（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] 哌啶-1-基）-3-（异丙基氨基）丙-1-酮单盐酸盐，形式，制剂，药物组合物，制备方法及其使用方法。

公开(公告)号：US08895729B2

公开(公告)日：2014-11-25

申请号：US14049477

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Francis Gosselin ,  Pirmin Hidber ,  Ursula Hoffmann ,  Theresa Humphries ,  Reinhard Reents ,  Qingping Tian ,  Herbert Yajima

IPC: C07D495/04 ,  C07D295/185 ,  C07D491/00

CPC classification number: C07D495/04 ,  C07D295/185

Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Abstract translation: 制备双重mTOR / PI3K抑制剂GDC-0980的方法，命名为（S）-1-（4 - （（2-（2-氨基嘧啶-5-基）-7-甲基-4-吗啉代噻吩并[3,2 d]嘧啶-6-基）甲基）哌嗪-1-基）-2-羟基丙-1-酮，其具有以下结构：立体异构体，几何异构体，互变异构体及其药学上可接受的盐。

公开(公告)号：US20140100366A1

公开(公告)日：2014-04-10

申请号：US14049477

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Francis Gosselin ,  Pirmin Hidber ,  Ursula Hoffmann ,  Theresa Humphries ,  Reinhard Reents ,  Qingping Tian ,  Herbert Yajima

IPC: C07D495/04 ,  C07D295/185

CPC classification number: C07D495/04 ,  C07D295/185

Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Abstract translation: 制备双重mTOR / PI3K抑制剂GDC-0980的方法，命名为（S）-1-（4 - （（2-（2-氨基嘧啶-5-基）-7-甲基-4-吗啉代噻吩并[3,2 d]嘧啶-6-基）甲基）哌嗪-1-基）-2-羟基丙-1-酮，其具有以下结构：立体异构体，几何异构体，互变异构体及其药学上可接受的盐。

公开(公告)号：US12172982B2

公开(公告)日：2024-12-24

申请号：US17398345

申请日：2021-08-10

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

Inventor： Ngiap-Kie Lim ,  Jeff Shen ,  Lauren Elizabeth Sirois ,  Jacob C. Timmerman ,  Etienne Trachsel ,  Nicholas Andrew White ,  Jie Xu ,  Haiming Zhang ,  Stephan Bachmann ,  Raphael Bigler ,  Kyle Bradley Pascual Clagg ,  Antonio Giovanni Dipasquale ,  Francis Gosselin ,  Ugo Jonathan Orcel ,  Roland Christoph Meier

IPC: C07D401/04 ,  C07D401/14

Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.

公开(公告)号：US11969426B2

公开(公告)日：2024-04-30

申请号：US17724045

申请日：2022-04-19

Applicant: Genentech, Inc.

Inventor： Reinhard Reents ,  Pirmin Hidber ,  Andre Hell ,  Peter Steidle ,  Martin Wunderlich ,  Marie Pepelnjak ,  Francis Gosselin ,  Edward Yost

IPC: A61K31/517 ,  A61K9/20 ,  A61K9/28

CPC classification number: A61K31/517 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2077 ,  A61K9/2095 ,  A61K9/28 ,  A61K9/284

Abstract: The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.