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1. 发明公开

EP2547664A1 MORPHOLINYLCHINAZOLINE 有权
公开(公告)号：EP2547664A1
公开(公告)日：2013-01-23
申请号：EP11704552.6
申请日：2011-02-17
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , FUCHSS, Thomas , ZENKE, Frank
IPC分类号： C07D239/86 , C07D239/94 , C07D401/04 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D295/155 , A61K31/517 , A61P35/00
CPC分类号： C07D239/94 , C07D239/86 , C07D295/155 , C07D401/04 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The invention relates to compounds of the formulae (I), (II) and (III), where R1, R2, R3, R4, Y, W
1 , W
2 , L, A, Alk, Cyc, Ar, Het
1 , Het
2 , HaI and n have the meaning stated in claim 1, and/or physiologically harmless salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for inhibiting serine-threonine protein kinases and also for sensitizing cancer cells to anticarcinogens and/or ionizing radiation. The invention also relates to the use of compounds of the formula (I) in prophylaxis, therapy or control of the progress of cancer, tumours, metastases or disorders of angiogenesis, in combination with radiotherapy and/or an anticarcinogen. The invention further relates to a method for producing compounds of the formula (I) by reacting compounds of the formulae (II) and (III) and optionally converting a base or acid of the compounds of the formula (I) into one of the salts thereof.
摘要翻译：（I），（II）和（III）的化合物，其中R1，R2，R3，R4，Y，W 1，W 2，L，A，Alk，Cyc，Ar，Het 1， Het 2，HaI和n具有权利要求1中所述的含义，和/或其生理上无害的盐，互变异构体和立体异构体，包括其所有比例的混合物。式（I）化合物可用于抑制丝氨酸 - 苏氨酸蛋白激酶，也可用于使癌细胞对抗癌剂和/或电离辐射敏感。本发明还涉及式（I）化合物与放射疗法和/或抗癌剂组合用于预防，治疗或控制癌症，肿瘤，转移或血管生成病症的进展。本发明进一步涉及通过使式（II）和（III）的化合物反应并且任选地将式（I）的化合物的碱或酸转化成其中一种盐来制备式（I）的化合物的方法它们。

2. 发明授权

EP1984324B1 MANDELSÄUREHYDRAZIDE 有权
公开(公告)号：EP1984324B1
公开(公告)日：2011-05-18
申请号：EP07702867.8
申请日：2007-01-18
申请人： Merck Patent GmbH
发明人： GERICKE, Rolf , KLEIN, Markus , MEDERSKI, Werner , BEIER, Norbert , LANG, Florian
IPC分类号： C07C243/38 , A61K31/15 , A61P3/00
CPC分类号： C07C243/38
摘要： New mandelic hydrazides of the formula (I) in which R1 - R11 are as defined in claim (1) are SGK inhibitors and can be used to treat SGK-associated illnesses and afflictions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertension, cardiovascular diseases and renal diseases, generally in connection with any kind of fibroses and inflammatory processes.

3. 发明公开

EP2032571A1 3 -AMINO- IMIDAZO [1, 2-A]PYRIDINDERIVATE ALS SGLT INHIBITOREN 有权
标题翻译： 3-氨基 - 咪唑并[1,2-A] AS SGLT抑制剂的吡啶衍生物
公开(公告)号：EP2032571A1
公开(公告)日：2009-03-11
申请号：EP07725570.1
申请日：2007-05-25
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , BEIER, Norbert , CEZANNE, Bertram , GERICKE, Rolf , KLEIN, Markus , TSAKLAKIDIS, Christos
IPC分类号： C07D471/04 , A61K31/437 , A61P3/10
CPC分类号： C07D471/04
摘要： Disclosed are novel compounds of formula (I), wherein X, Y, R, R', R1, R1', R1', R2, R2', R2', R3, R3', R4, R4', and n have the meanings indicated in claim 1. Said novel compounds are suitable as antidiabetics.

4. 发明公开

EP1802583A1 HETEROCYCLISCHE CARBONYLVERBINDUNGEN 审中-公开
标题翻译：杂环羰
公开(公告)号：EP1802583A1
公开(公告)日：2007-07-04
申请号：EP05734868.2
申请日：2005-04-04
申请人： Merck Patent GmbH
发明人： DORSCH, Dieter , GERICKE, Rolf , MEDERSKI, Werner , BEIER, Norbert , LANG, Florian
IPC分类号： C07D233/90 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , A61K31/341 , A61K31/381 , A61K31/416 , A61K31/42 , A61K31/426
CPC分类号： A61K31/421 , A61K31/341 , A61K31/416 , A61K31/4178 , A61K31/422 , C07D231/56 , C07D233/54 , C07D233/68 , C07D263/34 , C07D277/56 , C07D307/34 , C07D307/68 , C07D333/38 , C07D413/00 , C07D413/02
摘要： The invention relates to novel heterocyclic compounds of formula (I) wherein R1, D, W, T and T' have the meaning cited in the claim 1. Said compounds are SGK-inhibitors and can be used in the treatment of SGK-related diseases and disorders such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonal hypertension, cardiovascular diseases and renal diseases, and generally for any kind of fibroses and inflammatory processes.

5. 发明公开

EP1797079A1 PROLINDERIVATE 审中-公开
标题翻译：脯氨酸
公开(公告)号：EP1797079A1
公开(公告)日：2007-06-20
申请号：EP05787227.7
申请日：2005-09-16
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , TSAKLAKIDIS, Christos , DORSCH, Dieter , CEZANNE, Bertram , GLEITZ, Johannes
IPC分类号： C07D413/14 , C07D413/12 , C07D417/14 , A61K31/4025 , A61P7/02 , A61P9/10 , A61P35/00
CPC分类号： C07D413/14 , C07D413/12 , C07D417/14
摘要： The invention relates to novel compounds of formula (I), wherein X, Y, R1, R2, R3, R4 and n have the meaning cited in claim 1, are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

6. 发明公开

EP1797071A1 CARBONYLVERBINDUNGEN VERWENDBAR ALS INHIBITOREN DES KOAGULATIONSFAKTORS XA 审中-公开
标题翻译：羰基用作凝血因子Xa抑制剂的
公开(公告)号：EP1797071A1
公开(公告)日：2007-06-20
申请号：EP05790356.9
申请日：2005-09-01
申请人： Merck Patent GmbH
发明人： CEZANNE, Bertram , DORSCH, Dieter , MEDERSKI, Werner , TSAKLAKIDIS, Christos , GLEITZ, Johannes
IPC分类号： C07D401/12 , C07D413/12 , A61K31/4439 , A61K31/497 , A61P7/00 , A61P9/00
CPC分类号： C07D413/12 , C07D401/12
摘要： Disclosed are novel compounds of formula (I), wherein D, E, G, W, X, Y, T, R1, and R2 have the meaning indicated in claim 1. Said compounds are coagulation factor Xa inhibitors and can be used for preventing and/or treating thromboembolic diseases and treating tumors.

7. 发明授权

EP1441726B1 DERIVATE DES PHENOXY-N-'4-(ISOTHIAZOLIDIN-1,1-DIOXID-2YL)PHENY]-VALERIAN-SÄUREAMIDS UND ANDERE VERBINDUNGEN ALS INHIBITOREN DES KOAGULATIONSFAKTORS XA ZUR BEHANDLUNG VON THROMBOEMBOLISCHEN ERKRANKUNGEN UND TUMOREN 有权
标题翻译：导数的PHENOXY-N-'4-（异噻唑烷-1,1-二氧化物-2-基）苯基] -VALERIAN酸酰胺和其它化合物作为用于肿瘤和疾病的血栓栓塞于治疗凝血因子Xa的抑制剂
公开(公告)号：EP1441726B1
公开(公告)日：2006-12-20
申请号：EP02802623.5
申请日：2002-10-10
申请人： Merck Patent GmbH
发明人： DORSCH, Dieter , CEZANNE, Bertram , TSAKLAKIDIS, Christos , MEDERSKI, Werner , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： A61K31/425 , A61K31/445 , C07D275/02 , C07D417/12
CPC分类号： C07D275/02 , A61K31/425 , C07D417/12
摘要： Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meanings cited in Claim 1, are inhibitors of coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors.

8. 发明公开

EP1517685A1 2-(PHENYL)-2H-PYRAZOL-3-CARBONSÄURE-N-4-(THIOXO-HETEROCYCLYL)-PHENYL-AMID DERIVATE UND ENTSPRECHENDE IMINO-HETEROCYCLYL DERIVATE SOWIE VERWANDTE VERBINDUNGEN ALS INHIBITOREN DER KOAGULATIONSFAKTOREN XA UND/ODER VIIA ZUR BEHANDLUNG VON THROMBOSEN 审中-公开
标题翻译： 2-（苯基）-2H-吡唑-3-羧酸N-4-（硫代杂环基） - 苯基 - 酰胺衍生物和相应的亚氨基 - 杂环基衍生物和相关化合物作为凝血XA的抑制剂和/或VIIA血栓形成的治疗中
公开(公告)号：EP1517685A1
公开(公告)日：2005-03-30
申请号：EP03732540.4
申请日：2003-06-05
申请人： MERCK PATENT GmbH
发明人： CEZANNE, Bertram , DORSCH, Dieter , MEDERSKI, Werner , TSAKLAKIDIS, Christos , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： A61K31/4155 , A61K31/4178 , A61K31/433 , A61K31/42 , C07D403/12 , C07D417/12 , C07D413/14 , C07D403/14
CPC分类号： C07D403/12 , A61K31/4155 , A61K31/4178 , A61K31/42 , A61K31/433 , C07D403/14 , C07D413/14 , C07D417/12 , Y02P20/55
摘要： The invention relates to the novel compounds of formula (I), wherein D, M, W, X, Y, T, R1 and R1’ are defined as in patent claim 1. The inventive compounds are inhibitors of coagulation factor Xa and can be used in the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumors.

9. 发明公开

EP1414456A1 PHENYLDERIVATE ALS FAKTOR XA INHIBITOREN 有权
标题翻译：苯基衍生物作为Xa因子抑制剂
公开(公告)号：EP1414456A1
公开(公告)日：2004-05-06
申请号：EP02760242.4
申请日：2002-07-12
申请人： MERCK PATENT GmbH
发明人： DORSCH, Dieter , CEZANNE, Bertram , TSAKLAKIDIS, Christos , MEDERSKI, Werner , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： A61K31/4725 , A61K31/4412 , A61K31/4439 , A61K31/5377 , C07D401/12 , C07D417/12 , C07D413/12 , C07D211/76 , A61P7/02
CPC分类号： C07D401/12 , C07D211/76 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Novel compounds of formula (I), wherein D, W, X, Y, T and R1 have the meaning as cited in Claim 1, are inhibitors of coagulation factor Xa and can be used in the prophylaxis and/or therapy of thromboembolic diseases and in the treatment of tumours.

10. 发明公开

EP1309549A1 ACETAMIDDERIVATE UND IHRE VERWENDUNG ALS INHIBITOREN DES KOAGULATIONSFAKTORS XA UND VIIA 审中-公开
标题翻译：乙酰胺衍生物及其作为凝血因子Xa和VIIA抑制剂的用途
公开(公告)号：EP1309549A1
公开(公告)日：2003-05-14
申请号：EP01960449.5
申请日：2001-07-03
申请人： MERCK PATENT GmbH
发明人： MEDERSKI, Werner , JURASZYK, Horst , DORSCH, Dieter , TSAKLAKIDIS, Christos , GLEITZ, Johannes , BARNES, Christopher
IPC分类号： C07C333/08 , C07C317/44 , C07C311/16 , C07C257/18 , C07D413/12 , C07D271/06 , C07D213/30 , C07D211/46 , A61K31/18
CPC分类号： C07D271/06 , C07C257/18 , C07C311/16 , C07C317/44
摘要： The invention relates to novel compounds of formula (I) wherein R, R?1 and R2¿ have the designation cited in patent claim 1. Said compounds are inhibitors of the coagulation factors Xa and VIIa, and can be used to treat thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty, intermittent claudication, tumours, tumour diseases and/or tumour metastases.

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