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1. 发明申请

WO2014197345A2 IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开
标题翻译：咪唑衍生物及其用于改善药物药物动力学的方法
公开(公告)号：WO2014197345A2
公开(公告)日：2014-12-11
申请号：PCT/US2014040441
申请日：2014-06-02
申请人： MERCK SHARP & DOHME , COBURN CRAIG A , MALETIC MILANA , LUO YUNFU , QI ZHIQI , LI CHUNSING , YU TINGTING , SOLL RICHARD
发明人： COBURN CRAIG A , MALETIC MILANA , LUO YUNFU , QI ZHIQI , LI CHUNSING , YU TINGTING , SOLL RICHARD
IPC分类号： A61K31/55 , C07D401/14
CPC分类号： C07D487/04 , A61K31/4375 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5365 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
摘要翻译：本发明涉及式（I）的咪唑衍生物及其药学上可接受的盐，其中A，B，Y，R 1和R 2如本文所定义。本发明还涉及包含至少一种咪唑衍生物的组合物，以及使用咪唑衍生物抑制CYP450A 3A的方法。 CYP450 3A的抑制可用于改善由CYP450 3A4代谢的药物的药代动力学。

2. 发明申请

WO2015026685A1 7A-HETEROCYCLE SUBSTITUTED- 6, 6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES 审中-公开
标题翻译： 7-取代的6,6-二氟二苯并咪唑衍生物
公开(公告)号：WO2015026685A1
公开(公告)日：2015-02-26
申请号：PCT/US2014051403
申请日：2014-08-18
申请人： MERCK SHARP & DOHME , YANG ZHIQIANG , DONG GUIZHEN , MALETIC MILANA
发明人： YANG ZHIQIANG , DONG GUIZHEN , MALETIC MILANA
IPC分类号： A61K31/44 , C07D405/06
CPC分类号： A61K31/60 , A61K31/4155 , A61K31/4245 , A61K31/4365 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D405/14 , C07D413/14 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula, stnjctrually represented, or a pharmaceutically acceptable salt thereof wherein: R1 is any of the recited compounds, W is any of the recited compounds and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
摘要翻译：本发明涉及式（II）的双环烟肼衍生物或其药学上可接受的盐，其中：R 1是任何所述化合物，W是任何所述化合物，其余变量在本文中描述。本发明的化合物是PAR-1受体的有效抑制剂。本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。

3. 发明专利

CA2876240A1 SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 未知
公开(公告)号：CA2876240A1
公开(公告)日：2014-01-03
申请号：CA2876240
申请日：2013-06-25
申请人： MERCK SHARP & DOHME
发明人： COBURN CRAIG A , MALETIC MILANA , SOLL RICHARD , LI CHUNSING , LUO YUNFU , QI ZHIQI
IPC分类号： C07D401/14 , A61K31/454 , A61K31/496 , A61K31/4985 , A61P31/18 , C07D403/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.

4. 发明专利

ES2742309T3 Derivados de piperazina-imidazol y métodos de uso de los mismos para mejorar la farmacocinética de un fármaco 未知
公开(公告)号：ES2742309T3
公开(公告)日：2020-02-13
申请号：ES14861810
申请日：2014-11-07
申请人： MERCK SHARP & DOHME
发明人： COBURN CRAIG , MALETIC MILANA , LUO YUNFU , QI ZHIQI , YU TINGTING , SOLL RICHARD
IPC分类号： C07D401/06 , A61K31/454 , A61P31/18 , C07D233/64 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10
摘要： Un compuesto que tiene la fórmula (Ib):**Fórmula** o una sal farmacéuticamente aceptable de los mismos, en donde: R3 se selecciona entre Y, -O-Y, -C(O)-Y, -(alquileno C1-C6)-Y, -(alquileno C1-C6)-C(O)-Y, -(alquileno C1-C6)-C(O)- O-Y y -(alquileno C1-C6)-O-Y, en donde cada Y se selecciona independientemente entre: (1) alquilo C1-C6, (2) haloalquilo C1-C6, (3) hidroxialquilo C1-C6, (4) ciclohaloalquilo C3-C6, (5) cicloalquilo C3-C6, (6) fenilo, en donde dicho grupo fenilo puede estar opcionalmente sustituido hasta con cuatro grupos R7, (7) heteroarilo de 5 o 6 miembros, en donde dicho grupo heteroarilo de 5 o 6 miembros puede estar opcionalmente sustituido hasta con cuatro grupos R7, y (8) heterocicloalquilo monocíclico de 5 o 6 miembros o heterocicloalquilo bicíclico de 9 o 10 miembros, en donde dicho grupo heterocicloalquilo monocíclico de 5 o 6 miembros puede formar opcionalmente un espirociclo con un grupo cicloalquilo C3-C6 u otro grupo heterocicloalquilo monocíclico de 5 o 6 miembros, y en donde dicho grupo heterocicloalquilo monocíclico de 5 o 6 miembros y dicho grupo heterocicloalquilo bicíclico de 9 o 10 miembros puede estar opcionalmente sustituido en uno o más átomos de carbono del anillo hasta con cuatro grupos R7, que pueden ser iguales o diferentes, y en donde un átomo de carbono del anillo de un grupo heterocicloalquilo monocíclico de 5 o 6 miembros puede estar funcionalizado en forma de un grupo carbonilo; R5 se selecciona entre H, alquilo C1-C6, fenilo, -C(O)N(R8)2 y -C(O)-Z, en donde Z se selecciona entre piperidinilo, piperazinilo y morfolinilo y en donde dicho Z está opcionalmente sustituido con 1 a 3 grupos halo y el fenilo está opcionalmente sustituido con -N(R8)2, R6 es H, cada vez que aparece R7 y cada vez que aparece R9, se seleccionan independientemente entre alquilo C1-C6, fenilo, bencilo, heteroarilo de 5 o 6 miembros, -CH2-(heteroarilo 5 o 6 miembros), heterocicloalquilo de 5 o 6 miembros, -CH2- (heterocicloalquilo 5 o 6 miembros), hidroxialquilo C1-C6, haloalquilo C1-C6, halo, -CN, -N(R8)2, - (alquileno C1-C6)-N(R8)2, -OR8, -C(O)OR8, -SR8, -S(O)2R8, -C(O)N(R8)2, -(alquileno C1-C6)-C(O)OR8, -(alquileno C1- C6)-SR8, -(alquileno C1-C6)-S(O)2R8 y -(alquileno C1-C6)-C(O)N(R8)2, en donde dichos grupos fenilo, heteroarilo de 5 o 6 miembros y heterocicloalquilo de 5 o 6 miembros pueden estar opcionalmente sustituidos con uno a tres grupos seleccionados entre alquilo C1-C6, halo, hidroxialquilo C1-C6, haloalquilo C1-C6, halo, -CN, -N(R8)2 y -OR8; y cada vez que aparece R8 es independientemente H, alquilo C1-C6 o bencilo opcionalmente sustituido con uno o dos grupos metoxi.

5. 发明专利

AU2012240122A1 Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment 未知
公开(公告)号：AU2012240122A1
公开(公告)日：2013-09-26
申请号：AU2012240122
申请日：2012-04-05
申请人： MERCK SHARP & DOHME
发明人： EDMONDSON SCOTT , GUO ZHIQIANG , GEISS WILLIAM B , WOOD HAROLD B , STAMFORD ANDREW W , MILLER MICHAEL W , DEMONG DUANE E , MORRIELLO GREGORI J , ANAND RAJAN , COLANDREA VINCENT J , MACALA MEGAN , MALETIC MILANA , ZHU CHENG , ZHU YUPING , SUN WANYING , ZHAO KAKE , HUANG YONG , HARRIS JOEL M , CHANG LEHUA , KAR NAM FUNG , HU ZHIYONG , WANG LIPING , WANG BOWEI , LIU PING , SZEWCZYK JASON W
IPC分类号： A01N43/54 , A01N43/40 , A61K31/445 , A61K31/505
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

6. 发明专利

AT472531T 未知
公开(公告)号：AT472531T
公开(公告)日：2010-07-15
申请号：AT05777427
申请日：2005-08-03
申请人： MERCK SHARP & DOHME
发明人： WADDELL SHERMAN , BALKOVEC JAMES , SANTORELLI GINA , LEEMAN AARON , MALETIC MILANA , GU XIN
IPC分类号： C07D209/02 , A61K31/403 , A61K31/46 , C07D221/22

7. 发明专利

AU2012240122B2 Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment 未知
公开(公告)号：AU2012240122B2
公开(公告)日：2016-08-25
申请号：AU2012240122
申请日：2012-04-05
申请人： MERCK SHARP & DOHME
发明人： EDMONDSON SCOTT , GUO ZHIQIANG , GEISS WILLIAM B , WOOD HAROLD B , STAMFORD ANDREW W , MILLER MICHAEL W , DEMONG DUANE E , MORRIELLO GREGORI J , ANAND RAJAN , COLANDREA VINCENT J , MACALA MEGAN , MALETIC MILANA , ZHU CHENG , ZHU YUPING , SUN WANYING , ZHAO KAKE , HUANG YONG , HARRIS JOEL M , CHANG LEHUA , KAR NAM FUNG , HU ZHIYONG , WANG LIPING , WANG BOWEI , LIU PING , SZEWCZYK JASON W
IPC分类号： C07D211/22 , A01N43/40 , A01N43/54 , A61K31/445 , A61K31/505
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

8. 发明专利

CA2831334A1 SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 未知
公开(公告)号：CA2831334A1
公开(公告)日：2012-10-11
申请号：CA2831334
申请日：2012-04-05
申请人： MERCK SHARP & DOHME
发明人： EDMONDSON SCOTT , GUO ZHIQIANG , GEISS WILLIAM B , WOOD HAROLD B , STAMFORD ANDREW W , MILLER MICHAEL W , DEMONG DUANE E , MORRIELLO GREGORI J , ANAND RAJAN , COLANDREA VINCENT J , MACALA MEGAN , MALETIC MILANA , ZHU CHENG , ZHU YUPING , SUN WANYING , ZHAO KAKE , HUANG YONG , HARRIS JOEL M , CHANG LEHUA , KAR NAM FUNG , HU ZHIYONG , WANG LIPING , WANG BOWEI , LIU PING , SZEWCZYK JASON W
IPC分类号： A01N43/54 , A01N43/40 , A61K31/445 , A61K31/505
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

9. 发明专利

AU2013280599A1 Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug 未知
公开(公告)号：AU2013280599A1
公开(公告)日：2014-12-18
申请号：AU2013280599
申请日：2013-06-25
申请人： MERCK SHARP & DOHME
发明人： COBURN CRAIG A , MALETIC MILANA , SOLL RICHARD , LI CHUNSING , LUO YUNFU , QI ZHIQI
IPC分类号： C07D401/14 , A61K31/454 , A61K31/496 , A61K31/4985 , A61P31/18 , C07D403/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04
摘要： The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R

10. 发明专利

DE602005022089D1 SULFONYLVERBINDUNGEN ALS HEMMER VON 11-BETA-HYDROXYSTEROIDDEHYDROGENASE-1 未知
公开(公告)号：DE602005022089D1
公开(公告)日：2010-08-12
申请号：DE602005022089
申请日：2005-08-03
申请人： MERCK SHARP & DOHME
发明人： WADDELL SHERMAN T , BALKOVEC JAMES M , SANTORELLI GINA M , LEEMAN AARON H , MALETIC MILANA , GU XIN
IPC分类号： C07D209/02 , A61K31/403 , A61K31/46 , C07D221/22

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