公开(公告)号：US10329288B2

公开(公告)日：2019-06-25

申请号：US14913635

申请日：2014-08-21

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

Inventor： Chong Han ,  Keena Green ,  Francis Gosselin ,  Michelangelo Scalone ,  Paul J. Nichols ,  Weidong Liu ,  Keith L. Spencer ,  Zackary D. Crane ,  Peter J. Stengel ,  Sagar Shakya

IPC: C07D471/04

Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.

公开(公告)号：US11661424B2

公开(公告)日：2023-05-30

申请号：US17102086

申请日：2020-11-23

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

CPC classification number: C07D487/04 ,  B01J31/2409 ,  B01J31/2414 ,  B01J2231/40 ,  B01J2531/824 ,  C07B2200/09

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：US11547701B2

公开(公告)日：2023-01-10

申请号：US17018196

申请日：2020-09-11

Applicant: Valo Health, Inc. ,  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: C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  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：US11136330B2

公开(公告)日：2021-10-05

申请号：US16869475

申请日：2020-05-07

Applicant: Genentech, Inc.

Inventor： Kyle Bradley Pascual Clagg ,  Nicholas Andrew White ,  Haiming Zhang ,  Francis Gosselin ,  William Nack ,  Paul D. O'Shea

IPC: C07D487/04 ,  C07F9/24

Abstract: A method of synthesizing comprising a step of making an imidazo-pyrimidine compound by coupling a first compound of formula (II) with a second compound of formula (III) Followed by a deprotection and tosylation step. The methods are able to produce an isotopically substituted molecule having upwards of 95% purity relative to non-isotopically substituted molecules.
The invention further comprises compounds of formula:

公开(公告)号：US10696692B2

公开(公告)日：2020-06-30

申请号：US14382141

申请日：2013-03-01

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： Kenneth W Bair ,  Timm R Baumeister ,  Alexandre J Buckmelter ,  Karl H Clodfelter ,  Peter Dragovich ,  Francis Gosselin ,  Janet Gunzner-Toste ,  Bingsong Han ,  Jian Lin ,  Xiongcai Liu ,  Dominic J Reynolds ,  Chase C Smith ,  Zhongguo Wang ,  Mark Zak ,  Yamin Zhang ,  Guiling Zhao ,  Xiaozhang Zheng ,  Po-Wai Yuen

IPC: A61K51/00 ,  A61M36/14 ,  C07D519/00 ,  C07D471/04 ,  C07D495/04 ,  C07D487/04 ,  C07D491/048 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06

Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

公开(公告)号：US10456382B2

公开(公告)日：2019-10-29

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: C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K31/496 ,  A61K31/437 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4365 ,  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：US09862689B2

公开(公告)日：2018-01-09

申请号：US15036741

申请日：2014-11-13

Applicant: GENENTECH, INC.

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

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

CPC classification number: C07D239/70 ,  C07B2200/07 ,  C07C269/06 ,  C07C271/22 ,  C12P17/165

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：US20160152575A1

公开(公告)日：2016-06-02

申请号：US15018636

申请日：2016-02-08

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.

公开(公告)号：US20250009749A1

公开(公告)日：2025-01-09

申请号：US18605258

申请日：2024-03-14

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

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.

公开(公告)号：US10781219B2

公开(公告)日：2020-09-22

申请号：US16441765

申请日：2019-06-14

Applicant: Genentech, Inc.

Inventor： Francis Gosselin ,  Chong Han ,  Theresa Cravillion ,  Sean M. Kelly ,  Scott Savage

IPC: C07D498/04

Abstract: Methods of making benzoxazepin oxazolidinone compounds as well as synthetic intermediates are described, including compound 18, having the structure: