公开(公告)号：US20230346753A1

公开(公告)日：2023-11-02

申请号：US18073768

申请日：2022-12-02

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

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：US20220241279A1

公开(公告)日：2022-08-04

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

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：US11337977B2

公开(公告)日：2022-05-24

申请号：US15672505

申请日：2017-08-09

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：US11325912B2

公开(公告)日：2022-05-10

申请号：US16869512

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 regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.

公开(公告)号：US11192924B2

公开(公告)日：2021-12-07

申请号：US16581116

申请日：2019-09-24

Applicant: Genentech, Inc.

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

IPC: C07K7/64 ,  C07K1/06

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：US20210244717A1

公开(公告)日：2021-08-12

申请号：US17018196

申请日：2020-09-11

Applicant: Valo Early Discovery, 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: A61K31/4355 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  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：US20170247338A1

公开(公告)日：2017-08-31

申请号：US15514188

申请日：2015-09-25

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

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

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

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：US09290458B2

公开(公告)日：2016-03-22

申请号：US14401092

申请日：2013-05-17

Applicant: Genentech, Inc.

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

IPC: C07D239/70 ,  A61K31/496 ,  C07D403/04 ,  A61K31/517

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：US20150099880A1

公开(公告)日：2015-04-09

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 ,  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。