公开(公告)号：US09242984B2

公开(公告)日：2016-01-26

申请号：US14409133

申请日：2013-06-18

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： Michelle R. Machacek ,  Michael D. Altman ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Brandon Cash ,  Tony Siu ,  Hua Zhou ,  Matthew Christopher ,  Solomon D. Kattar ,  Andrew M. Haidle ,  Kaleen Konrad Childers ,  Matthew L. Maddess ,  Michael H. Reutershan ,  Yves Ducharme ,  David J. Guerin ,  Kerrie Spencer ,  Christian Beaulieu ,  Vouy Linh Truong ,  Daniel Guay ,  Alan B. Northrup ,  Brandon M. Taoka ,  Jongwon Lim ,  Christian Fischer ,  John W. Butcher ,  Ryan D. Otte ,  Binyuan Sun ,  John Michael Ellis

IPC: C07D401/00 ,  A61K31/00 ,  C07D471/04 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型吡唑衍生物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：US20150353552A1

公开(公告)日：2015-12-10

申请号：US14443294

申请日：2013-11-15

Applicant: 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.

Inventor： 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: C07D473/30 ,  A61K31/5377 ,  A61K31/52

CPC classification number: A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/00 ,  C07D473/06 ,  C07D473/30 ,  C07D473/38 ,  C07D519/00 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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：US20150299125A1

公开(公告)日：2015-10-22

申请号：US14440517

申请日：2013-11-04

Applicant: Andrew M. HAIDLE ,  Brandon CASH ,  James P. JEWELL ,  Kerrie SPENCER ,  Michael D. ALTMAN ,  Ryan D. OTTE ,  Alan B. NORTHRUP ,  MERCK SHARP & DOHME CORP.

Inventor： Andrew M. Haidle ,  Brandon Cash ,  James P. Jewell ,  Kerrie Spencer ,  Michael D. Altman ,  Ryan D. Otte ,  Alan B. Northrup

IPC: C07D213/74 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D213/74 ,  C07D401/14 ,  C07D405/14 ,  C07D451/10 ,  C07H13/08

Abstract: The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.

Abstract translation: 本发明提供式（I）化合物，其为反式-4 - [（1R） - （6 - {[4-（二氟甲基）吡啶-2-基]氨基} -4-甲基-2,3 “ - 联吡啶-6'-基）-1-羟乙基]环己烷羧酸，Syk的有效抑制剂。 该化合物可用于治疗和预防由酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：US09006444B2

公开(公告)日：2015-04-14

申请号：US14349558

申请日：2012-10-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Maria Emilia Di Francesco ,  John Michael Ellis ,  Sandra Lee Knowles ,  Alan B. Northrup

IPC: C07D215/38 ,  C07D213/74 ,  C07D401/04 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/47 ,  A61K31/5377

CPC classification number: C07D213/74 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/47 ,  A61K31/5377 ,  C07D215/38 ,  C07D401/04

Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

Abstract translation: 本发明提供某些含有苯甲酰胺的式（I）化合物; 或其药学上可接受的盐，其中A和B如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。

公开(公告)号：US08987456B2

公开(公告)日：2015-03-24

申请号：US14349563

申请日：2012-10-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Kaleen Konrad Childers ,  Anthony Donofrio ,  John Michael Ellis ,  Sandra Lee Knowles ,  Alan B. Northrup

IPC: C07D215/38 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4709

CPC classification number: C07D401/12 ,  A61K31/444 ,  A61K31/4709 ,  C07D401/14 ,  C07D405/14

Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

Abstract translation: 本发明提供了具有式（I）（I）的某些3-吡啶基甲酰胺化合物或其药学上可接受的盐，其中A和B如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。

公开(公告)号：US08962611B2

公开(公告)日：2015-02-24

申请号：US14465577

申请日：2014-08-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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 ,  Michael D. Altman ,  Stephane L. Bogen ,  Ronald J. Doll

IPC: A61K31/553 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention provides substituted imidazopyridines 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.

Abstract translation: 本发明提供如本文所述的取代的咪唑并吡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。

公开(公告)号：US08846657B2

公开(公告)日：2014-09-30

申请号：US14132946

申请日：2013-12-18

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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 ,  Michael D. Altman ,  Stephane L. Bogen ,  Ronald J. Doll

IPC: A61K31/553 ,  C07D471/04 ,  C07D471/08 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention provides substituted imidazopyridines 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.

Abstract translation: 本发明提供如本文所述的取代的咪唑并吡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。