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31. 发明专利

JP2010254714A Methylene urea derivative 审中-公开
标题翻译：甲基脲衍生物
公开(公告)号：JP2010254714A
公开(公告)日：2010-11-11
申请号：JP2010179074
申请日：2010-08-09
申请人： Merck Patent Gmbh , メルクパテントゲゼルシャフトミットベシュレンクテルハフツングMerck Patent Gesellschaft mit beschraenkter Haftung
发明人： BUCHSTALLER HANS-PETER , WIESNER MATTHIAS , SCHADT OLIVER , AMENDT CHRISTIANE , ZENKE FRANK , SIRRENBERG CHRISTIAN , GRELL MATTHIAS , FINSINGER DIRK
IPC分类号： C07D213/81 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61P13/08 , A61P15/08 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P43/00 , C07D213/68 , C07D213/79 , C07D401/12 , C07D409/12 , C07D417/12
CPC分类号： C07D213/68 , A61K31/44 , A61K31/4439 , A61K45/00 , C07D213/75 , C07D213/79 , C07D213/81 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide methylene urea derivatives, the methylene urea derivatives as pharmaceuticals, the methylene urea derivatives as inhibitors of raf-kinase, use of the methylene urea derivatives for the manufacture of pharmaceuticals, and a method for producing pharmaceutical compositions comprising the methylene urea derivatives, pharmaceutical compositions obtained by the methods and methods of treatment comprising administering the pharmaceutical compositions.
SOLUTION: The present invention relates to methylene urea derivatives of formula (I): A-D-B, the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of the pharmaceutical compositions and a method of treatment comprising administering the pharmaceutical compositions to a patient.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：为了提供亚甲基脲衍生物，作为药物的亚甲基脲衍生物，作为raf激酶抑制剂的亚甲基脲衍生物，用于制备药物的亚甲基脲衍生物的用途，以及制备药物的方法包含亚甲基脲衍生物的组合物，通过治疗方法和方法获得的药物组合物，包括给予药物组合物。解决方案：本发明涉及式（I）的亚甲基脲衍生物：ADB，式（I）化合物作为raf-激酶抑制剂的用途，式（I）化合物用于药物组合物的制备和治疗方法，包括向患者施用药物组合物。版权所有（C）2011，JPO＆INPIT

32. 发明申请

WO2013164061A8 PYRROLOTRIAZINONE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO2013164061A8
公开(公告)日：2014-11-06
申请号：PCT/EP2013001026
申请日：2013-04-06
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , BUCHSTALLER HANS-PETER
IPC分类号： C07D487/04 , A61K31/53 , A61P9/00 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04 , A61K31/53
摘要： Compounds of the formula (I) in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase and PARP-1 and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of imflamination.
摘要翻译：其中X，R 1和Y具有权利要求1所述含义的式（I）化合物是阻聚剂和PARP-1的抑制剂，可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的污染。

33. 发明申请

WO2014023390A3 (AZA-)ISOQUINOLINONE DERIVATIVES 审中-公开
标题翻译：（AZA-）异喹啉酮衍生物
公开(公告)号：WO2014023390A3
公开(公告)日：2014-04-10
申请号：PCT/EP2013002085
申请日：2013-07-12
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , BUCHSTALLER HANS-PETER
IPC分类号： C07D217/24 , A61K31/4375 , A61K31/472 , A61K31/4725 , A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/10 , C07D405/10 , C07D471/04
CPC分类号： C07D471/04 , A61K31/4375 , A61K31/472 , A61K31/4725 , C07D217/24 , C07D401/10 , C07D405/10
摘要： Compounds of the formula (I), in which R1, X, Y and n have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
摘要翻译：式（I）的化合物，其中R 1，X，Y和n具有权利要求1所示的含义，是阻聚剂，可以用于治疗疾病如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症。

34. 发明申请

WO2013117288A1 TETRAHYDRO-QUINAZOLINONE DERIVATIVES AS TANK AND PARP INHIBITORS 审中-公开
标题翻译：作为罐和PARP抑制剂的四氢喹诺酮酮衍生物
公开(公告)号：WO2013117288A1
公开(公告)日：2013-08-15
申请号：PCT/EP2013000078
申请日：2013-01-14
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , ESDAR CHIRSTINA , LEUTHNER BIRGITTA
IPC分类号： C07D403/12 , A61K31/517 , A61P25/00 , A61P29/00 , A61P35/00 , C07D239/95 , C07D401/04 , C07D401/12
CPC分类号： A61K31/517 , A61K31/5377 , C07D239/95 , C07D401/04 , C07D401/12 , C07D403/12
摘要： Compounds of the formula I in which U, V and W have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
摘要翻译：其中U，V和W具有权利要求1所述的含义的式I化合物是阻聚剂，可用于治疗疾病如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症。

35. 发明专利

NZ721726A N1-(3,3,3-trifluoro-2-hydroxo-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase 未知
公开(公告)号：NZ721726A
公开(公告)日：2021-07-30
申请号：NZ72172614
申请日：2014-11-19
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER
IPC分类号： C07D401/14 , A61K31/454 , A61P3/00 , A61P35/00 , C07D401/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： Compounds of the formula (I) in which R, R1 and R3 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.

36. 发明专利

ES2797301T3 Derivados de piperidinil-propanona 未知
公开(公告)号：ES2797301T3
公开(公告)日：2020-12-01
申请号：ES17712526
申请日：2017-03-27
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER
IPC分类号： C07D401/06 , A61K31/454 , A61P3/00 , A61P35/00 , C07D401/08 , C07D413/06 , C07D413/08
摘要： Compuestos de formula I **(Ver fórmula)** donde X indica NH u O, Q indica C(CH3)2 o 1,1-ciclopropileno, R1 indica H, A, Cic, Ar o Het, R2 indica H o CH3, R3 indica H o A', Ar indica fenil, que no esta sustituido o esta mono-, di- o trisustituido por Hal, NO2, CN, A, OR3, S(O)mR3, N(R3)2, COA, COOR3, CON(R3)2, SO2N(R3)2, NR3COR3, NR3SO2A y/o NR3CON(R3)2, Het indica un heterociclo mono o biciclico saturado, insaturado o aromatico con 1 a 4 atomos de N, O y/o S, que no esta sustituido o esta mono o disustituido por Hal, NO2, CN, A, OR3 S(O)mR3, N(R3)2, COA, COOR3, CON(R3)2, SO2N(R3)2, NR3COR3, NR3SO2A y/o NR3CON(R3)2, A indica alquilo ramificado o no ramificado con 1-10 atomos de C, donde uno o dos grupos CH y/o CH2 no adyacentes pueden estar sustituidos por atomos de N, O y/o S y/o donde 1-7 atomos de H pueden estar sustituidos por R4, R4 indica F, Cl u OH, A' indica alquilo ramificado o no ramificado con 1-6 atomos de C, donde 1-5 atomos de H pueden estar sustituidos por F, Cic indica alquilo ciclico con 3, 4, 5, 6 o 7 atomos de C, que no esta sustituido o esta monosustituido por OH, Hal indica F, Cl, Br o I, m indica 0, 1 o 2, y sales, tautomeros y estereoisomeros farmaceuticamente aceptables de los mismos, incluidas sus mezclas en todas las proporciones.

37. 发明专利

CA2863991C TETRAHYDRO-QUINAZOLINONE DERIVATIVES AS TANK AND PARP INHIBITORS 未知
公开(公告)号：CA2863991C
公开(公告)日：2020-08-11
申请号：CA2863991
申请日：2013-01-14
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , ESDAR CHRISTINA , LEUTHNER BIRGITTA
IPC分类号： C07D403/12 , A61K31/517 , A61P25/00 , A61P29/00 , A61P35/00 , C07D239/95 , C07D401/04 , C07D401/12
摘要： Compounds of the formula l are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

38. 发明专利

CA3121697A1 4-HETEROARYLCARBONYL-N-(PHENYL OR HETEROARYL) PIPERIDINE-1-CARBOXAMIDES AS INHIBITORS OF TANKYRASES 未知
公开(公告)号：CA3121697A1
公开(公告)日：2020-06-11
申请号：CA3121697
申请日：2019-11-29
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , ROHDICH FELIX
IPC分类号： C07D401/06 , A61K31/454 , A61P35/00 , C07D401/14
摘要： Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.

39. 发明专利

HUE047608T2 (AZA-)izokinolin-származékok 未知
公开(公告)号：HUE047608T2
公开(公告)日：2020-05-28
申请号：HUE13737146
申请日：2013-07-12
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , BUCHSTALLER HANS-PETER
IPC分类号： A61P9/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00

40. 发明专利

CA2816896C 1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES 未知
公开(公告)号：CA2816896C
公开(公告)日：2019-01-08
申请号：CA2816896
申请日：2011-10-12
申请人： MERCK PATENT GMBH
发明人： HEINRICH TIMO , WUCHERER-PLIETKER MARGARITA , BUCHSTALLER HANS-PETER
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： The invention relates to 1H-pyrrolo[2,3-b]pyridine compounds, which are inhibitors of cell proliferation/cell vitality and can be used to treat tumors.

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