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1. 发明申请

WO2014093230A3 COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开
标题翻译：生产具有BTK抑制活性的嘧啶和吡啶类化合物的组合物和方法
公开(公告)号：WO2014093230A3
公开(公告)日：2014-08-28
申请号：PCT/US2013073895
申请日：2013-12-09
申请人： MERCK PATENT GMBH , LIU-BUJALSKI LESLEY , JOHNSON THERESA L , GOUTOPOULOS ANDREAS , QIU HUI
发明人： LIU-BUJALSKI LESLEY , JOHNSON THERESA L , GOUTOPOULOS ANDREAS , QIU HUI
IPC分类号： C07D403/12 , C07D213/73 , C07D213/74 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D413/14 , C07D495/04
CPC分类号： C07D403/12 , A61K31/4418 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D471/10 , C07D487/10 , C07D495/04
摘要： The present invention provides novel pyrimidine and pyridine compounds which are attached to a warhead, and the manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. The invention also describes kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
摘要翻译：本发明提供附着于弹头的新型嘧啶和吡啶化合物，以及用于治疗过度增殖性疾病的制造和用途，所述过度增殖性疾病包括但不限于癌症，狼疮，变应性疾病，舍格伦病和类风湿性关节炎。本发明还描述了激酶抑制剂，包括但不限于布鲁顿酪氨酸激酶抑制剂。

2. 发明申请

WO2013006308A3 DIHYDROPYRAZOLES, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF FERTILITY DISORDERS 审中-公开
标题翻译：二氢吡喃，其药物组合物及其用于治疗肥胖症的用途
公开(公告)号：WO2013006308A3
公开(公告)日：2013-05-10
申请号：PCT/US2012044169
申请日：2012-06-26
申请人： MERCK PATENT GMBH , YU HENRY , RICHARDSON THOMAS E , FOGLESONG ROBERT JAMES , DESELM LIZBETH CELESTE , GOUTOPOULOS ANDREAS
发明人： YU HENRY , RICHARDSON THOMAS E , FOGLESONG ROBERT JAMES , DESELM LIZBETH CELESTE , GOUTOPOULOS ANDREAS
IPC分类号： C07D231/12 , A61K31/4152 , A61K31/4155 , A61P15/08 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/06 , C07D413/06
CPC分类号： A61K31/415 , A61K9/0014 , A61K9/0019 , A61K9/0031 , A61K9/0048 , A61K9/0078 , A61K9/06 , A61K9/19 , A61K9/2018 , A61K9/2059 , A61K9/48 , A61K31/4155 , A61K31/423 , A61K31/427 , A61K31/437 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K45/06 , A61K47/06 , C07D231/06 , C07D231/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/06 , C07D413/06 , C07D413/10 , C07D417/10 , C07D471/04
摘要： Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
摘要翻译：式（I）的新型二氢吡唑衍生物其中L，R，R3，R4，R5，R6，R7，X1，X2，X3，X4，Y，m和n具有根据权利要求的含义，是正变构调节剂 FSH受体，并且可以特别用于治疗生育障碍。

3. 发明申请

WO2012170976A3 COMPOSITIONS AND METHODS FOR THE PRODUCTION OF PYRIMIDINE AND PYRIDINE COMPOUNDS WITH BTK INHIBITORY ACTIVITY 审中-公开
标题翻译：用BTK抑制活性生产吡嗪和吡啶化合物的组合物和方法
公开(公告)号：WO2012170976A3
公开(公告)日：2013-04-11
申请号：PCT/US2012041803
申请日：2012-06-10
申请人： MERCK PATENT GMBH , HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
发明人： HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
IPC分类号： C07D239/47 , A61K31/4418 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P35/02 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D495/04
CPC分类号： A61K31/69 , A61K31/44 , A61K31/4545 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D471/10 , C07D495/04 , C07F5/022
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
摘要翻译：本发明提供了式（I），式（II），式（III），式（IV）和式（V））的新型嘧啶和吡啶化合物用于治疗过度增殖性疾病的制造和用途，包括但不限于癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。在优选的实施方案中，本发明描述不可逆激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。

4. 发明申请

WO2010002779A3 NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS 审中-公开
标题翻译：萘啶类化合物作为AURORA激酶抑制剂
公开(公告)号：WO2010002779A3
公开(公告)日：2011-03-03
申请号：PCT/US2009049035
申请日：2009-06-29
申请人： MERCK PATENT GMBH , XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
发明人： XIAO YUFANG , CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS
IPC分类号： C07D471/04 , A61K31/436 , A61P35/00
CPC分类号： C07D471/04 , A61K31/436 , A61K45/06 , A61K2300/00
摘要： Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译：公开了抑制极光激酶的萘吡啶酮衍生物化合物以及包含这些化合物的药物组合物及其合成方法。这些化合物可用于治疗由不规则和/或扰乱的极光激酶如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。

5. 发明专利

ES2927587T3 Derivados de indolizina que se pueden aplicar a enfermedades neurodegenerativas 未知
公开(公告)号：ES2927587T3
公开(公告)日：2022-11-08
申请号：ES15747950
申请日：2015-07-31
申请人： MERCK PATENT GMBH
发明人： KARRA SRINIVASA R , GOUTOPOULOS ANDREAS
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28
摘要： La presente invención se refiere a compuestos de indolizina y composiciones farmacéuticamente aceptables de los mismos, útiles como antagonistas de P2X7 y para el tratamiento de trastornos relacionados con P2X7. (Traducción automática con Google Translate, sin valor legal)

6. 发明专利

RU2742122C2 СОЕДИНЕНИЯ ГЕТЕРОАРИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ ТКБ И ИХ ПРИМЕНЕНИЕ 未知
公开(公告)号：RU2742122C2
公开(公告)日：2021-02-02
申请号：RU2017115852
申请日：2015-10-06
申请人： MERCK PATENT GMBH
发明人： GAILLARD PASCALE , SEENISAMY JEYAPRAKASHNARAYANAN , GARDBERG ANNA , JOHNSON THERESA L , SHERER BRIAN A , GOUTOPOULOS ANDREAS , WON ANNIE CHO , JONES REINALDO , NEAGU CONSTANTIN , QIU HUI , CALDWELL RICHARD D , POTNICK JUSTIN , LIU-BUJALSKI LESLEY
IPC分类号： C07D471/04 , A61K31/437 , A61K31/553 , A61P29/00 , A61P37/00 , C07D519/00
摘要： Настоящееизобретениеотноситсяк соединениюимидазопиридинаформулыIиегофармацевтическиприемлемымсолям, структурныеформулыкоторогоприведеныв формулеизобретения. Соединенияимидазопиридинапоизобретениюпредназначеныв качествеингибиторатирозинкиназыБрутона (BTK). 3 н.п. ф-лы, 5 табл., 190 пр.I

7. 发明专利

ES2796774T3 Dihidropirazoles, composiciones farmacéuticas de los mismos y su uso para el tratamiento de trastornos de fertilidad 未知
公开(公告)号：ES2796774T3
公开(公告)日：2020-11-30
申请号：ES12735378
申请日：2012-06-26
申请人： MERCK PATENT GMBH
发明人： YU HENRY , RICHARDSON THOMAS E , FOGLESONG ROBERT JAMES , DESELM LIZBETH CELESTE , GOUTOPOULOS ANDREAS
IPC分类号： C07D231/12 , A61K31/4152 , A61K31/4155 , A61P15/08 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/06 , C07D413/06
摘要： Compuesto de formula (I-B) **(Ver fórmula)** en la que R1 indica Hal, A, CN, -E-fenilo o Het3; R2 indica Hal, A, OA, NH2, CN, SA, SO2A, SO2NH2, O-fenilo o Het1; R3, R4 indican H, y R5, R6 indican A; E indica O o un enlace sencillo; A indica alquilo ramificado o no ramificado que tiene 1-5 atomos de C, Het1 indica pirrolilo, furilo, tiofenilo, imidazolilo, pirazilo, isoxazilo, tiazilo o piridilo, que puede estar mono o disustituido por al menos un sustituyente seleccionado del grupo de Hal, A y OA; Het3 indica pirrolidinilo, tetrahidrofurilo, oxazolidinilo, dioxalanilo, piperazinilo, morfolinilo o dioxanilo, que puede estar mono o disustituido por al menos un sustituyente seleccionado del grupo de Hal, COA y =O; Hal indica F, Cl o Br; y m indica 0; y/o una sal fisiologicamente aceptable de los mismos.

8. 发明专利

ES2746756T3 Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa 未知
公开(公告)号：ES2746756T3
公开(公告)日：2020-03-06
申请号：ES14715758
申请日：2014-03-10
申请人： MERCK PATENT GMBH
发明人： LAN RUOXI , CHEN XIAOLING , XIAO YUFANG , HUCK BAYARD R , GOUTOPOULOS ANDREAS
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： Compuesto seleccionado del grupo que consiste en: 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoropiperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("1"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoropiperidin-1-il}- pirimidin-5-carboxamida (racémica) ("2"); 4-amino-6-[(3R,4S)-4-[1-[2-(azetidin-1-il)etil]-4-[4-fluoro-3-(trifluorometil)fenil]imidazol-2-il]-3-fluoro-1- piperidil]pirimidin-5-carboxamida (quiral) ("3"); 4-amino-6-[(3S,4R)-4-[1-[2-(azetidin-1-il)etil]-4-[4-fluoro-3-(trifluorometil)fenil]imidazol-2-il]-3-fluoro-1- piperidil]pirimidin-5-carboxamida (quiral) ("4"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-metil-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("5"); 4-amino-6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-metil-piperidin-1-il}- pirimidin-5-carboxamida (racémica) ("6"); 4-amino-6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("7"); 4-amino-6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carboxamida (racémica) ("8"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilaminoetil)-4-(4-fluoro-3-metil-fenil)imidazol-2-il]-3-fluoro-1-piperidil]}-pirimidin-5- carbonitrilo (racémico) ("9"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-cloropirimidin- 4-ilamina (racémica) ("10"); 6-{3,4-trans-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-cloropirimidin- 4-ilamina (racémica) ("11"); 5-cloro-6-{3,4-cis--4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-metil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-pirimidin- 4-ilamina (racémica) ("12"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-etilpirimidin- 4-ilamina (racémica) ("13"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("14"); 4-amino-6-{3,4-cis-4-[1-(2-dimetilamino-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}- pirimidin-5-carbonitrilo (racémico) ("15"); 6-{3,4-cis-4-[1-(2-azetidin-1-il-etil)-4-(4-fluoro-3-trifluorometil-fenil)-1H-imidazol-2-il]-3-fluoro-piperidin-1-il}-5-etoxipirimidin- 4-ilamina (racémica) ("16"), o sales farmacéuticamente aceptables, solvatos o solvatos de sales del mismo.

9. 发明专利

AU2017204191B2 Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders 未知
公开(公告)号：AU2017204191B2
公开(公告)日：2019-10-31
申请号：AU2017204191
申请日：2017-06-21
申请人： MERCK PATENT GMBH
发明人： RICHARDSON THOMAS E , FOGLESONG ROBERT JAMES , DESELM LIZBETH CELESTE , GOUTOPOULOS ANDREAS , YU HENRY
IPC分类号： C07D231/12 , A61K31/4152 , A61K31/4155 , A61P15/08 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/06 , C07D413/06
摘要： - 238 Novel dihydropyrazole derivatives of formula (1) x N 2 (CY2 ) N X (CYR)' R (1) wherein L, R, RR4, R,R,R, X', X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, 10 inter alia, for the treatment of fertility disorders.

10. 发明专利

NZ706418A Azaquinazoline carboxamide derivatives 未知
公开(公告)号：NZ706418A
公开(公告)日：2019-09-27
申请号：NZ70641813
申请日：2013-11-27
申请人： MERCK PATENT GMBH
发明人： JOHNSON THERESA L , HUCK BAYARD R , LAN RUOXI , POTNICK JUSTIN , DESELM LIZBETH CELESTE , CRONIN MARK W , CHEN XIAOLING , BOIVIN ROCH , GOUTOPOULOS ANDREAS , NEAGU CONSTANTIN
IPC分类号： C07D403/12 , A61K31/519 , A61K31/53 , A61P35/00 , C07D253/08 , C07D401/12 , C07D471/04
摘要： Novel azaquinazoline carboxamide derivatives of formula (I) wherein each W1, W2, W3, W4 is independently N or CH, wherein at least one of W1, W2, W3 or W4 is N and R1, R2, R3 and m are as defined herein, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

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