公开(公告)号：US10442819B2

公开(公告)日：2019-10-15

申请号：US15532549

申请日：2015-12-01

申请人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

发明人： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

IPC分类号： A61K31/351 ,  A61K31/4353 ,  A61K31/5355 ,  A61K31/551 ,  C07D471/04 ,  C07D471/14 ,  C07D498/08 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10 ,  A01N43/00

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US20150368247A1

公开(公告)日：2015-12-24

申请号：US14764616

申请日：2014-02-04

申请人： Matthew P. CHRISTOPHER ,  Francesc Xavier FRADERA LLINAS ,  Michelle MACHACEK ,  Michelle MARTINEZ ,  Michael Hale REUTERSHAN ,  Manami SHIZUKA ,  Binyuan SUN ,  Christopher Francis THOMPSON ,  Wesley B. TROTTER ,  Matthew E. VOSS ,  Liping YANG ,  Merck Sharp & Dohme Corp.

发明人： Matthew P. Christopher ,  Francesc Xavier Fradera Llinas ,  Michelle Machacek ,  Michelle Martinez ,  Michael Hale Reutershan ,  Manami Shizuka ,  Binyuan Sun ,  Christopher Francis Thompson ,  B. Wesley Trotter ,  Matthew E. Voss ,  Liping Yang

IPC分类号： C07D473/34 ,  C07D473/00 ,  C07D473/30

CPC分类号： C07D473/34 ,  C07D473/00 ,  C07D473/30

摘要： The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

摘要翻译： 本发明提供2,6,7本文所述的取代嘌呤或其药学上可接受的盐。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

公开(公告)号：US20150353552A1

公开(公告)日：2015-12-10

申请号：US14443294

申请日：2013-11-15

申请人： Abdelghani Abe ACHAB ,  Michael D. ALTMAN ,  Yongqi DENG ,  Timothy GUZI ,  Solomon KATTAR ,  Jason D. KATZ ,  Joey L. METHOT ,  Hua ZHOU ,  Meredeth MCGOWAN ,  Matthew P. CHRISTOPHER ,  Yudith GARCIA ,  Neville John THONY ,  Francesc Xavier FRADERA LLINAS ,  Changwei MU ,  Sixing ZHANG ,  Rong ZHANG ,  Kin Chiu FONG ,  Xiansheng LENG ,  MERCK SHARP & DOHME CORP.

发明人： Abdelghani Abe Achab ,  Michael D. Altman ,  Yongqi Deng ,  Timothy Guzi ,  Solomon Kattar ,  Jason D. Katz ,  Joey L. Methot ,  Hua Zhou ,  Meredeth McGowan ,  Matthew P. Christopher ,  Yudith Garcia ,  Neville John Anthony ,  Francesc Xavier Fradera Llinas ,  Kin Chiu Fong ,  Xiansheng Leng ,  Changwei Mu ,  Sixing Zhang ,  Rong Zhang

IPC分类号： C07D473/30 ,  A61K31/5377 ,  A61K31/52

CPC分类号： A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/00 ,  C07D473/06 ,  C07D473/30 ,  C07D473/38 ,  C07D519/00 ,  A61K2300/00

摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

摘要翻译： 本发明提供了作为PI3K-δ抑制剂的式I化合物，因此可用于治疗PI3K-δ介导的疾病如炎症，哮喘，COPD和癌症。

公开(公告)号：US20150329548A1

公开(公告)日：2015-11-19

申请号：US14652466

申请日：2013-12-18

申请人： Michelle MACHACEK ,  B. Wesley TROTTER ,  Christopher DISNMORE ,  Francesc Xavier FRADERA LLINAS ,  Amit Ashokrao KUDALE ,  Michael Hale REUTERSHAN ,  Christopher Francis THOMPSON ,  Liping YANG ,  Michael D. ALTMAN ,  Stephane L. BOGEN ,  Ronald J. DOLL ,  Matthew E. VOSS ,  MERCH SHARP & DOHME CORP.

发明人： Christopher Dinsmore ,  Francesc Xavier Fradera Llinas ,  Amit Ashokro Kudale ,  Michelle Machacek ,  Michael Hale Reutershan ,  Christopher Francis Thompason ,  B. Wesley Trotter ,  Liping Yang ,  Michael D. Altman ,  Stephane L. Bogen ,  Ronald J. Doll ,  Matthew E. Voss

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

摘要翻译： 本发明提供如本文所述的取代吡咯并嘧啶或其药学上可接受的盐或溶剂化物。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。