公开(公告)号：US10457648B2

公开(公告)日：2019-10-29

申请号：US15514188

申请日：2015-09-25

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

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

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

摘要： 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：US20200010428A1

公开(公告)日：2020-01-09

申请号：US16574933

申请日：2019-09-18

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH INC.

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

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

摘要： 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：US20170247338A1

公开(公告)日：2017-08-31

申请号：US15514188

申请日：2015-09-25

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

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

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

摘要： 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：US11661424B2

公开(公告)日：2023-05-30

申请号：US17102086

申请日：2020-11-23

申请人： Genentech, Inc.

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

IPC分类号： C07D487/04 ,  B01J31/24

CPC分类号： C07D487/04 ,  B01J31/2409 ,  B01J31/2414 ,  B01J2231/40 ,  B01J2531/824 ,  C07B2200/09

摘要： 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

申请人： Valo Health, Inc. ,  Genentech, Inc.

发明人： 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分类号： 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

摘要： 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

申请人： Genentech, Inc.

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

IPC分类号： C07D487/04 ,  C07F9/24

摘要： 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

申请人： Forma TM, LLC ,  Genentech, Inc.

发明人： 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分类号： 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

摘要： 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

申请人： Forma TM, LLC ,  Genentech, Inc.

发明人： 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分类号： 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

摘要： 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

申请人： GENENTECH, INC.

发明人： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

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

CPC分类号： C07D239/70 ,  C07B2200/07 ,  C07C269/06 ,  C07C271/22 ,  C12P17/165

摘要： 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

申请人： Genentech, Inc.

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

IPC分类号： C07D239/70

CPC分类号： C07D239/70 ,  A61K31/517 ,  C07D403/04

摘要： 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.