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1. 发明申请

WO2014031438A3 SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS 审中-公开
标题翻译：取代的苯基酪氨酸激酶（Syk）抑制剂
公开(公告)号：WO2014031438A3
公开(公告)日：2014-04-17
申请号：PCT/US2013055133
申请日：2013-08-15
申请人： MERCK SHARP & DOHME , MERCK CANADA INC , HAIDLE ANDREW M , BURCH JASON , GUAY DANIEL , GAUTHIER JACQUES YVES , ROBICHAUD JOEL , FOURNIER JEAN FRANCOIS , ELLIS JOHN MICHAEL , CHRISTOPHER MATTHEW , KATTAR SOLOMON D , SMITH GRAHAM , NORTHRUP ALAN B
发明人： HAIDLE ANDREW M , BURCH JASON , GUAY DANIEL , GAUTHIER JACQUES YVES , ROBICHAUD JOEL , FOURNIER JEAN FRANCOIS , ELLIS JOHN MICHAEL , CHRISTOPHER MATTHEW , KATTAR SOLOMON D , SMITH GRAHAM , NORTHRUP ALAN B
IPC分类号： A61K31/54 , A61K31/505 , A61K31/506
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t 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).
摘要翻译：本发明提供了式（I）的某些取代的苯基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5c和t如本文所定义。本发明还提供了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）介导的疾病或病症的方法。

2. 发明公开

EP2863913A4 IMIDAZOLYL ANALOGS AS SYK INHIBITORS 有权转让
标题翻译： IMIDAZOLYLANALOGA作为SYK-HEMMER
公开(公告)号：EP2863913A4
公开(公告)日：2015-12-16
申请号：EP13807108
申请日：2013-06-18
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： LIM JONGWON , REUTERSHAN MICHAEL H , ELLIS JOHN MICHAEL , CHILDERS KALEEN KONRAD , DONOFRIO ANTHONY , ALTMAN MICHAEL D , HAIDLE ANDREW M , ZABIEREK ANNA , CHRISTOPHER MATTHEW , GRIMM JONATHAN , BURCH JASON , FRANCESCO MARIA EMILIA DI , PETROCCHI ALESSIA , BEAULIEU CHRISTIAN , TRUONG VOUY LINH , NORTHRUP ALAN B , BLOUIN MARC
IPC分类号： A61K31/50 , A61K31/501 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention provides novel imidazole analogs 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.
摘要翻译：本发明提供了式I的新型咪唑类似物，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。

3. 发明公开

EP2863916A4 SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权转让
标题翻译： SUBSTITUIERTE PYRIDIN-MILZ-TYROSINKINASEINHIBITOREN
公开(公告)号：EP2863916A4
公开(公告)日：2015-12-16
申请号：EP13807050
申请日：2013-06-17
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： HAIDLE ANDREW M , KNOWLES SANDRA LEE , KATTAR SOLOMON D , DESCHENES DENIS , BURCH JASON , ROBICHAUD JOEL , CHRISTOPHER MATTHEW , ALTMAN MICHAEL D , JEWELL JAMES P , NORTHHRUP ALAN B , BLOUIN MARC , ELLIS JOHN MICHAEL , ZHOU HUA , FISCHER CHRISTIAN , SCHELL ADAM J , REUTERSHAN MICHAEL H , TAOKA BRANDON M , DONOFRIO ANTHONY
IPC分类号： C07D401/12 , A61K31/506 , A61P11/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04
CPC分类号： C07D401/12 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04 , A61K2300/00
摘要： The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t 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.
摘要翻译：本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t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。

4. 发明公开

EP2900665A4 TRIAZOLYL DERIVATIVES AS SYK INHIBITORS 有权转让
标题翻译： TRIAZOLYLDERIVATE作为SYK-HEMMER
公开(公告)号：EP2900665A4
公开(公告)日：2016-03-23
申请号：EP13841430
申请日：2013-09-24
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： MACHACEK MICHELLE R , ROMEO ERIC T , KATTAR SOLOMON D , CHRISTOPHER MATTHEW , ALTMAN MICHAEL D , NORTHRUP ALAN B , ELLIS JOHN MICHAEL , BOYLE BRENDAN O' , DONOFRIO ANTHONY , GRIMM JONATHAN , REUTERSHAN MICHAEL H , CHILDERS KALEEN KONRAD , OTTE RYAN D , CASH BRANDON , DUCHARME YVES , HAIDLE ANDREW M , SPENCER KERRIE , VITHARANA DILRUKSHI , WU LINGYUN , ZHANG LI , ZHANG PENG , BEAULIEU CHRISTIAN , GUAY DANIEL
IPC分类号： C07D417/12 , A61K31/506 , A61P11/06 , A61P29/00 , A61P35/00 , C07D239/50 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译：提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。三唑衍生物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。

5. 发明公开

EP2863914A4 PYRAZOLYL DERIVATIVES AS SYK INHIBITORS 有权转让
标题翻译：吡唑烷酮酸酯
公开(公告)号：EP2863914A4
公开(公告)日：2015-12-16
申请号：EP13807800
申请日：2013-06-18
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： MACHACEK MICHELE R , ALTMAN MICHAEL D , ROMEO ERIC T , WITHARANA DILRUKSHI , CASH BRANDON , SIU TONY , ZHOU HUA , CHRISTOPHER MATTHEW , KATTAR SOLOMON D , HAIDLE ANDREW M , CHILDERS KALEEN KONRAD , MADDESS MATTHEW H , REUTERSHAN MICHAEL H , DUCHARME YVES , GUERIN DAVID J , SPENCER KERRIE , BEAULIEU CHRISTIAN , TRUONG VOUY LINH , GUAY DANIEL , NORTHRUP ALAN B , TAOKA BRANDON M , LIM JONGWON , FISCHER CHRISTIAN , BUTCHER JOHN W , OTTE RYAN D , SUN BINYUAN , ELLIS JOHN MICHAEL
IPC分类号： A61K31/50 , A61K31/501 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： 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.
摘要翻译：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。

6. 发明公开

EP2884982A4 SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS 有权转让
标题翻译： SUBSTITUIERTE PHENYL-MILZ-TYROSINKINASEINHIBITOREN
公开(公告)号：EP2884982A4
公开(公告)日：2016-03-30
申请号：EP13831537
申请日：2013-08-15
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： HAIDLE ANDREW M , BURCH JASON , GUAY DANIEL , GAUTHIER JACQUES YVES , ROBICHAUD JOEL , FOURNIER JEAN FRANCOIS , ELLIS JOHN MICHAEL , CHRISTOPHER MATTHEW , KATTAR SOLOMON D , SMITH GRAHAM , NORTHRUP ALAN B
IPC分类号： A61K31/54 , A61K31/505 , A61K31/506
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10

7. 发明专利

ES2670878T3 Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa 未知
公开(公告)号：ES2670878T3
公开(公告)日：2018-06-01
申请号：ES12834379
申请日：2012-09-21
申请人： MERCK SHARP & DOHME
发明人： BRUBAKER JASON , CHILDERS MATTHEW LLOYD , CHRISTOPHER MATTHEW , CLOSE JOSHUA , KATZ JASON DAVID , JUNG JOON , PETERSON SCOTT , SILIPHAIVANH PHIENG , SIU TONY , SMITH GRAHAM FRANK , TORRES LUIS , WOO HYUN CHONG , YOUNG JONATHAN , ZHANG HONGJUN
IPC分类号： C07D401/14 , A61K31/415 , A61P11/06 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Un compuesto de fórmula I o una sal farmacéuticamente aceptable o un estereoisómero del mismo:**Fórmula** cada uno de Ra y R4 se selecciona independientemente entre hidrógeno y alquilo C1-4; A se selecciona entre arilo y heteroarilo; n is independientemente 0, 1, 2, 3 o 4; p es 2 o 3; X se selecciona independientemente entre C, N, O y S; cada uno de R3 y R7 se selecciona independientemente entre hidrógeno, halógeno, alquilo C1-10, alquenilo C2-10, heteroalquilo C1-10, arilalquil C0-10 alquilo C0-10, cicloalquil C3-8 alquilo C0-10, heteroarilalquilo C0-10, heterocicloalquil (C3-8) alquilo C0-10, y en donde cada uno de R3 y R7 se sustituyen independientemente con 0, 1, 2, 3 o 4 sustituyentes R5a; R5a se selecciona entre: halógeno, alquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroalquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquenil C2-10 (oxi)0-1(carbonil)0-1alquilo C0-10, arilo C0-10 alquil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquenil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquinil(oxi)0-1(carbonil)0-1alquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroarilalquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heterocicloalquil (C3-8)alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquil C1-10 (carbonil)0-1oxialquilo C0-10, heteroalquil C1-10 (carbonil)0-1oxi alquilo C0-10, alquenil C2-10 (carbonil)0-1oxi alquilo C0-10, heteroalquil C1-10 (carbonil)0-1oxi alquilo C0-10, aril C0-10 alquil (carbonil)0-1oxi alquilo C0-10, cicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, heteroarilalquil C0-10 (carbonil)0-1oxialquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, (alquil (C0-10))1-2aminocarboniloxi, heteroalquil (C0-10)aminocarboniloxi, arilalquil (C0-10) aminocarboniloxi, cicloalquil (C3-8) alquil (C0-10) aminocarboniloxi, heteroarilalquil (C0-10)aminocarboniloxi, heterocicloalquil (C3-8) alquil (C0-10)aminocarboniloxi, alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heteroalquil (C0-10) amino(oxi)0-1carbonilalquilo C0-10, cicloalquil C3-8 alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, arilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heteroarilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, alquil C1-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heteroalquil C1-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, arilalquilo C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heteroarilalquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, -CO2(alquilo C0-10), -(alquil C0-10)CO2H, Oxo (>=O); alquilsulfonilo C1-10, heteroalquilsulfonilo C1-10, cicloalquilsulfonilo (C3-8), cicloheteroalquilsulfonilo (C3-8), heteroarilsulfonilo, arilsulfonilo, aminosulfonilo, -SO2N(alquilo C1-6)1-2, -SO2alquilo C1-6, -SO2CF3, -SO2CF2H, alquilsulfinilo C1-10, -Si(CH3)3, amino, (alquil C0-10)1-2 amino, acil C1-4aminoalquilo C0-10, hidroxi, (alquilo C1-10)OH, alquilalcoxi C0-10, ciano, (alquilo C1-6 )ciano y haloalquilo C1-6; en donde dos R5a y el átomo al que están unidos pueden formar opcionalmente un sistema de anillo saturado de 4, 5 o 6 miembros; en donde cada R5a está opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes R6 y R6 se selecciona independientemente entre: halógeno, alquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroalquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquenil C2-10 (oxi)0-1(carbonil)0-1alquilo C0-10, arilo C0-10 alquil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquenil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquinil(oxi)0-1(carbonil)0-1alquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroarilalquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heterocicloalquil (C3-8)alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquil C1-10 (carbonil)0-1oxialquilo C0-10, alquenil C2-10 (carbonil)0-1oxi alquilo C0-10, heteroalquil C1-10 (carbonil)0-1oxi alquilo C0-10, aril C0-10 alquil (carbonil)0-1oxi alquilo C0-10, cicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, heteroarilalquil C0-10 (carbonil)0-1oxialquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, (alquil (C0-10))1-2aminocarboniloxi, arilalquil (C0-10) aminocarboniloxi, cicloalquil (C3-8) alquil (C0-10) aminocarboniloxi, heteroarilalquil (C0-10)aminocarboniloxi, heterocicloalquil (C3-8) alquil (C0-10)aminocarboniloxi, alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, cicloalquil C3-8 alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, arilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heteroarilalquilo C0-10 amino (oxi)0-1carbonilalquilo C0-10, heterocicloalquil (C3-8)alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, alquil C1-10 (oxi)0-1carbonilaminoalquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1carbonilaminoalquilo C0-10, arilalquilo C0-10 (oxi)0-1carbonilaminoalquilo C0-10, heteroarilalquilo C0-10 (oxi)0-1carbonilaminoalquilo C0-10,

8. 发明专利

AU2012312303B2 Cyanomethylpyrazole carboxamides as janus kinase inhibitors 未知
公开(公告)号：AU2012312303B2
公开(公告)日：2016-09-15
申请号：AU2012312303
申请日：2012-09-21
申请人： MERCK SHARP & DOHME
发明人： BRUBAKER JASON , CHILDERS MATTHEW LLOYD , CHRISTOPHER MATTHEW , CLOSE JOSHUA T , KATZ JASON DAVID , JUNG JOON , PETERSON SCOTT , SILIPHAIVANH PHIENG , SIU TONY , SMITH GRAHAM FRANK , TORRES LUIS E , WOO HYUN CHONG , YOUNG JONATHAN R , ZHANG HONGJUN
IPC分类号： C07D231/02 , A61K31/415
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

9. 发明专利

CA2849336A1 CYANOMETHYLPYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS 未知
公开(公告)号：CA2849336A1
公开(公告)日：2013-03-29
申请号：CA2849336
申请日：2012-09-21
申请人： MERCK SHARP & DOHME
发明人： BRUBAKER JASON , CHILDERS MATTHEW LLOYD , CHRISTOPHER MATTHEW , CLOSE JOSHUA T , KATZ JASON DAVID , JUNG JOON , PETERSON SCOTT , SILIPHAIVANH PHIENG , SIU TONY , SMITH GRAHAM FRANK , TORRES LUIS E , WOO HYUN CHONG , YOUNG JONATHAN R , ZHANG HONGJUN
IPC分类号： A61K31/415 , A61K31/395 , A61K31/4155 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61P19/02 , A61P37/06 , C07D231/02
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

10. 发明专利

AU2012312303A1 Cyanomethylpyrazole carboxamides as janus kinase inhibitors 未知
公开(公告)号：AU2012312303A1
公开(公告)日：2014-04-03
申请号：AU2012312303
申请日：2012-09-21
申请人： MERCK SHARP & DOHME
发明人： BRUBAKER JASON , CHILDERS MATTHEW LLOYD , CHRISTOPHER MATTHEW , CLOSE JOSHUA T , KATZ JASON DAVID , JUNG JOON , PETERSON SCOTT , SILIPHAIVANH PHIENG , SIU TONY , SMITH GRAHAM FRANK , TORRES LUIS E , WOO HYUN CHONG , YOUNG JONATHAN R , ZHANG HONGJUN
IPC分类号： C07D231/02 , A61K31/415
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

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