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1. 发明申请

WO2012013282A8 BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K 审中-公开
标题翻译：双环氮杂环碳酰胺作为激酶P70S6K的抑制剂
公开(公告)号：WO2012013282A8
公开(公告)日：2012-03-29
申请号：PCT/EP2011003272
申请日：2011-07-01
申请人： MERCK PATENT GMBH , HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO C , DESELM LIZBETH CELESTE , XIAO YUFANG , KARRA SRINIVASA R , LAN RUOXI , MOCHALKIN IGOR , SUTTON AMANDA E , RICHARDSON THOMAS E
发明人： HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO C , DESELM LIZBETH CELESTE , XIAO YUFANG , KARRA SRINIVASA R , LAN RUOXI , MOCHALKIN IGOR , SUTTON AMANDA E , RICHARDSON THOMAS E
IPC分类号： C07D239/74 , A61K31/517 , A61P35/00 , C07D403/12
CPC分类号： C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
摘要： The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译：本发明提供了根据式（I）的新型双环氮杂杂环羧酰胺化合物，它们的制造和用于治疗过度增殖性疾病例如癌症的用途。

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. 发明专利

IL243223A Imidazole derivatives, their preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IL243223A
公开(公告)日：2019-07-31
申请号：IL24322315
申请日：2015-12-20
申请人： MERCK PATENT GMBH , YU HENRY , RICHARDSON THOMAS E , DONNELLY MARIANNE , NGUYEN NGAN , JIANG XULIANG
发明人： YU HENRY , RICHARDSON THOMAS E , DONNELLY MARIANNE , NGUYEN NGAN , JIANG XULIANG
IPC分类号： A61K31/4188 , A61P5/06
摘要： The present invention relates to imidazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR).

5. 发明专利

AU2013208082B2 Benzamide derivatives as modulators of the follicle stimulating hormone 未知
公开(公告)号：AU2013208082B2
公开(公告)日：2017-07-20
申请号：AU2013208082
申请日：2013-01-09
申请人： BHARATHI PANDI , FOGLESONG ROBERT J , HEASLEY BRIAN H , JENKS MATTHEW G , MERCK PATENT GMBH , RICHARDSON THOMAS E , YU HENRY
发明人： YU HENRY , RICHARDSON THOMAS E , BHARATHI PANDI , HEASLEY BRIAN H , JENKS MATTHEW G , FOGLESONG ROBERT J
IPC分类号： C07D405/12 , A61K31/496 , A61P15/08 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Novel benzamide derivatives of formula (I) wherein W

6. 发明申请

WO2007008942A3 PHENYLAMINO-ACETIC ACID [1-(PYRIDIN-4-YL)-METHYLIDENE]-HYDRAZIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF G PROTEIN-COUPLED RECEPTOR KINASES FOR THE TREATMENT OF EYE DISEASES 审中-公开
标题翻译：作为用于治疗眼病的G蛋白偶联受体激动剂的调节剂的苯甲酸乙酸[1-（吡啶-4-基） - 甲基] - 乙酰衍生物和相关化合物
公开(公告)号：WO2007008942A3
公开(公告)日：2007-04-12
申请号：PCT/US2006026976
申请日：2006-07-11
申请人： AERIE PHARMACEUTICALS INC , DELONG MITCHELL A , SZNAIDMAN MARCOS L , OAKLEY ROBERT H , ECKHARDT ALLEN E , HUDSON CHRISTINE , YINGLING JEFFREY D , PEEL MICHAEL , RICHARDSON THOMAS E , MURRAY CLAIRE LOUISE , RAO BYAPPANAHALLY N NARASINGA , HEASLEY BRIAN H , PATEL PARESMA R
发明人： DELONG MITCHELL A , SZNAIDMAN MARCOS L , OAKLEY ROBERT H , ECKHARDT ALLEN E , HUDSON CHRISTINE , YINGLING JEFFREY D , PEEL MICHAEL , RICHARDSON THOMAS E , MURRAY CLAIRE LOUISE , RAO BYAPPANAHALLY N NARASINGA , HEASLEY BRIAN H , PATEL PARESMA R
IPC分类号： C07D213/61 , A61K31/341 , A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/47 , A61K31/513 , A61P27/02 , C07C251/86 , C07D213/36 , C07D215/42 , C07D233/88 , C07D239/54 , C07D307/52 , C07D333/36
CPC分类号： C07D401/12 , C07D213/53 , C07D213/61 , C07D213/75 , C07D215/12 , C07D215/42 , C07D233/64 , C07D239/52 , C07D239/54 , C07D307/14 , C07D307/52 , C07D333/22 , C07D401/14
摘要： Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X 1 , X 2 , X 3 and X 4 are, independently, CH, O, S or N-R 6 , with the proviso that at least one of X 2 or X 3 is O, S or N-R 6 ; and a heteroaryl group (ii): wherein X 5 and X 9 are CH or C-halogen, X 6 and X 8 are CH, and X 7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R 1 , R 2 , R 3 , R 4 , and R 5 are, independently, hydrogen; halogen; C 1 -C 4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C 1 -C 4 alkyl-heterocycle; -C(O)NH-C 1 -C 4 alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C 1 -C 4 alkyl; aryl, heteroaryl, C 1 -C 4 alkyl aryl or C 1 -C 4 alkyl heteroaryl; R 6 is H or C 1 -C 4 alkyl; R 7 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and X is N-R 6 .
摘要翻译：提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。还提供了使用化合物和/或组合物影响疾病状态或病症如癌症骨质疏松症和青光眼的各种方法。（式（I））。 A选自杂芳基（i）：其中X 1，X 2，X 3和X 4 >独立地是CH，O，S或NR 6，条件是X 2或X 3中的至少一个是O ，S或NR 6; 和杂芳基（ii）：其中X 5和X 9是CH或C-卤素，X 6和X 8 H是CH，X 7是N，并且其中六元杂芳基可以进一步与未取代的六元芳基稠合; R 1，R 2，R 3，R 4和R 5，独立地是氢; 卤素; C 1 -C 4烷基; 氨基; 硝基; 氰基; 杂; 羧基，羰基氨基; 氨基磺酰基; 磺酰; 氨; 硫代; 磺酰基; 酰基; 杂环; -要么; -O-C _{1 -C _{4 烷基 - 杂环; -C（O）NH-C _{1 -C _{4 烷基 - 杂环; -C（O）NH杂芳基; -C（O）NH-芳基; 或羧基氨基; 其中R是C 1 -C 4烷基; 芳基，杂芳基，C 1 -C 4烷基芳基或C 1 -C 4烷基杂芳基; R 6是H或C 1 -C 4烷基; R 7是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 烷氧基; X为N-R 6。}}}}

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

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.

9. 发明专利

CA2806610C BICYCLIC AZAHETEROCYCLIC CARBOXAMIDES AS INHIBITORS OF THE KINASE P70S6K 未知
公开(公告)号：CA2806610C
公开(公告)日：2018-08-28
申请号：CA2806610
申请日：2011-07-01
申请人： MERCK PATENT GMBH
发明人： HUCK BAYARD R , NEAGU CONSTANTIN , JONES REINALDO C , DESELM LIZBETH CELESTE , XIAO YUFANG , KARRA SRINIVASA R , LAN RUOXI , SUTTON AMANDA E , RICHARDSON THOMAS E , MOCHALKIN IGOR
IPC分类号： C07D239/74 , A61K31/517 , A61P35/00 , C07D403/12
摘要： The invention provides novel bicyclic azaheterocyciic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

10. 发明专利

ES2663972T3 Derivados de benzamida como moduladores de la hormona folículo estimulante 未知
公开(公告)号：ES2663972T3
公开(公告)日：2018-04-17
申请号：ES13700819
申请日：2013-01-09
申请人： MERCK PATENT GMBH
发明人： YU HENRY , RICHARDSON THOMAS E , BHARATHI PANDI , HEASLEY BRIAN H , JENKS MATTHEW G , FOGLESONG ROBERT J
IPC分类号： C07D405/12 , A61K31/496 , A61P15/08 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compuestos de fórmula (I) **(Ver fórmula)** donde W1, W2 denota N; R1 denota -(CY2)n-E-Het3, -(CY2)n-Cyc-Het3,-(CY2)n-Het1, -(CY2)n-CONH-Het1, -(CY2)n-NHCO-Het1, -(CY2)n-Cyc, -(CY2)n-CONH-Cyc, -(CY2)n-NHCO-Cyc, A, -(CYR8)n-OY, -(CY2)n-COOY, -(CY2)n-SO2Y, -(CYR8)n-CONY2, -(CYR8)n-NY2, -(CYR8)n-NYCOY, -(CY2)n-NYCOOY, -(CY2)n-NYCONY2 o -(CY2)n-NHCO-CH>=CH2; R2 denota H; R1, R2 juntos también denotan -(CY2)P-NH-(CY2)P-, -(CY2)p-NHCO-(CY2)p-, -(CY2)p-CONH-(CY2)p-, -(CY2)p-N(COA)-(CY2)p-, -(CY2)p-N(COOA)-(CY2)p-, **(Ver fórmula)** R3 denota furilo o oxazolilo, que puede estar monosustituido con A o Cyc; R4 denota H; R5 denota fenilo, que puede estar mono o disustituido con A o Hal, o piridilo, que puede estar monosustituido con A o Hal; R6, R7 juntos denotan -(CY2)2-; R8 denota Y o Ar; R9 denota Y; R10 denota Hal, Y, OY, -O(CY2)n-OY, NY2, Cyc, COOY, CONH2, NHCOY o CN; con la condición de que R 9 y R10 no sean simultáneamente H; R2, R10 juntos también denotan -(CY2)P- o -(CY)2-; X denota CO; E denota -(CY2)m-, O, CO, -COO- o SO2; Y denota H o A; A denota alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H se pueden reemplazar en forma independiente entre sí por Hal y/o >=O; Cyc denota cicloalquilo con 3-6 átomos de C, en donde 1-3 átomos de H se pueden reemplazar en forma independiente entre sí por OH o COOH; Ar denota un carbociclo mono o biciclico insaturado o aromático con 3-10 átomos de C, que puede estar sustituido con al menos un sustituyente seleccionado entre el grupo formado por A, Hal, OY, COOY, CONH2, NHCOY, -(CY2)n-NY2, NO2, SO2Y, CN y Het2, o que se puede fusionar a Cyc; Het1 denota un heterociclo mono o bicíclico insaturado o aromático con 1-10 átomos de C y 1-4 átomos de N, O y/o S, que puede estar sustituido con al menos un sustituyente seleccionado entre el grupo formado por Hal, A, Cyc, OY, COOY, CONH2, NHCOY, NY2, SO2Y, SO2NY2, NHSO2Y, CN y Ar; Het2 denota un heterociclo monocíclico insaturado de 5 miembros con 1-3 átomos de C y 2-4 átomos de N y/o S, que puede estar sustituido con A; Het3 denota un heterociclo saturado mono o biciclico con 3-7 átomos de C y 1-4 átomos de N, O y/o S, que puede estar sustituido con al menos un sustituyente seleccionado entre el grupo formado por >=O, A, Hal, -(CY2)n- Cyc, -(CY2)n-OY, COY, COOY, CONY2, NHCOY, NY2, CN, SO2Y y -(CY2)n-Ar; Hal denota F, CI, Br o I; m, n denotan en forma independiente uno del otro 0, 1,2, 3, 4, 5 o 6; y p denota 1, 2 o 3; y/o sus sales fisiológicamente aceptables.

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