公开(公告)号：US11254679B2

公开(公告)日：2022-02-22

申请号：US16631915

申请日：2018-07-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Burcu Selin Aytar ,  Alina Borovika ,  Collin Chan ,  Joerg Deerberg ,  Nathan R. Domagalski ,  Martin D. Eastgate ,  Yu Fan ,  Michael David Bengt Fenster ,  Robert V. Forest ,  Francisco Gonzalez-Bobes ,  Rebecca A. Green ,  Matthew R. Hickey ,  Nathaniel David Kopp ,  Thomas E. La Cruz ,  Kathleen Lauser ,  Hong Geun Lee ,  David K. Leahy ,  Helen Y. Luo ,  Thomas M. Razler ,  Scott A. Savage ,  Chris Sfouggatakis ,  Maxime C. D. Soumeillant ,  Serge Zaretsky ,  Bin Zheng ,  Ye Zhu

IPC: C07D487/04

Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.

公开(公告)号：US20220177482A1

公开(公告)日：2022-06-09

申请号：US17677312

申请日：2022-02-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Burcu Selin Aytar ,  Alina Borovika ,  Collin Chan ,  Joerg Deerberg ,  Nathan R. Domagalski ,  Martin D. Eastgate ,  Yu Fan ,  Michael David Bengt Fenster ,  Robert V. Forest ,  Francisco Gonzalez-Bobes ,  Rebecca A. Green ,  Matthew R. Hickey ,  Nathaniel David Kopp ,  Thomas E. La Cruz ,  Kathleen Lauser ,  Hong Geun Lee ,  David K. Leahy ,  Helen Y. Luo ,  Thomas M. Razler ,  Scott A. Savage ,  Chris Sfouggatakis ,  Maxime C.D. Soumeillant ,  Serge Zaretsky ,  Bin Zheng ,  Ye Zhu

IPC: C07D487/04

Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.

公开(公告)号：US20200223852A1

公开(公告)日：2020-07-16

申请号：US16631915

申请日：2018-07-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Burcu Selin Aytar ,  Alina Borovika ,  Collin Chan ,  Joerg Deerberg ,  Nathan R. Domagalski ,  Martin D. Eastgate ,  Yu Fan ,  Michael David Bengt Fenster ,  Robert V. Forest ,  Francisco Gonzalez-Bobes ,  Rebecca A. Green ,  Matthew R. Hickey ,  Nathaniel David Kopp ,  Thomas E. La Cruz ,  Kathleen Lauser ,  Hong Geun Lee ,  David K. Leahy ,  Helen Y. Luo ,  Thomas M. Razler ,  Scott A. Savage ,  Chris Sfouggatakis ,  Maxime C.D. Soumeillant ,  Serge Zaretsky ,  Bin Zheng ,  Ye Zhu

IPC: C07D487/04

Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolodin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.

公开(公告)号：US20140121155A1

公开(公告)日：2014-05-01

申请号：US14142081

申请日：2013-12-27

Applicant: Bristol-Myers Squibb Company

Inventor： Jack Z. Gougoutas ,  Mary F. Malley ,  John D. DiMarco ,  Xiaotian S. Yin ,  Chenkou Wei ,  Jurong Yu ,  Truc Chi Vu ,  Gregory Scott Jones ,  Scott A. Savage

IPC: C07D209/52 ,  A61K45/06 ,  A61K31/403

CPC classification number: C07D209/52 ,  A61K31/403 ,  A61K45/06 ,  A61K2300/00

Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

Abstract translation: 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。