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1. 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.

2. 发明公开

EP2313380A1 OXADIAZOLDERIVATE FÜR DIE BEHANDLUNG VON DIABETES 有权
标题翻译：恶二唑用于糖尿病的治疗
公开(公告)号：EP2313380A1
公开(公告)日：2011-04-27
申请号：EP09777077.0
申请日：2009-07-09
申请人： Merck Patent GmbH
发明人： KLEIN, Markus , BEIER, Norbert , LANG, Florian
IPC分类号： C07D271/113 , C07D413/04 , A61K31/4245 , A61P3/10
CPC分类号： C07D271/113 , C07D413/04
摘要： The invention relates to novel oxadiazole derivatives of formula (I) wherein R, R', Y, X
1 , X
2 and X
3 have the designations cited in claim 1. Said derivatives are kinase inhibitors and can be used to treat illnesses and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonal hypertonia, cardiovascular diseases and kidney diseases, any type of fibrosis, inflammatory processes, tumours, and tumour diseases.

3. 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.

4. 发明公开

EP1984324A1 MANDELSÄUREHYDRAZIDE 有权
公开(公告)号：EP1984324A1
公开(公告)日：2008-10-29
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.
摘要翻译：其中R1-R11如权利要求（1）中定义的式（I）的新型扁桃酰肼为SGK抑制剂，可用于治疗SGK相关疾病和病痛，如糖尿病，肥胖症，代谢综合征（血脂障碍），全身性和肺动脉高压，心血管疾病和肾脏疾病，通常与任何类型的纤维化和炎症过程有关。

5. 发明授权

EP1866280B1 ACYLHYCLRAZIDE ALS KINASE INHIBITOREN INSBESONDERE FÜR SGK 有权
标题翻译： ACYLHYCLRAZIDE作为激酶抑制剂特别FOR SGK
公开(公告)号：EP1866280B1
公开(公告)日：2008-08-13
申请号：EP06723338.7
申请日：2006-03-10
申请人： Merck Patent GmbH
发明人： GERICKE, Rolf , DORSCH, Dieter , MEDERSKI, Werner , KLEIN, Markus , BEIER, Norbert , LANG, Florian
IPC分类号： C07C243/40 , C07C255/57 , C07C243/38 , C07C323/62 , A61P3/00 , A61K31/166
CPC分类号： C07C323/62 , C07C243/38 , C07C255/57
摘要： Novel acyl hydrazides of the formula (I), in which R 1 - R 9 have the meanings defined in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonary hypertension, cardiovascular diseases and kidney diseases, and generally any types of fibroses and inflammatory processes.

6. 发明公开

EP1917249A1 3-OXO-INDAZOL-QUADRATSÄUREDERIVATE 审中-公开
标题翻译： 3-氧代吲唑QUADRATSÄUREDERIVATE
公开(公告)号：EP1917249A1
公开(公告)日：2008-05-07
申请号：EP06776564.4
申请日：2006-08-02
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , GERICKE, Rolf , KLEIN, Markus , BEIER, Norbert , LANG, Florian
IPC分类号： C07D231/56 , A61K31/4188 , A61P35/00
CPC分类号： C07D231/56
摘要： The invention relates to novel squaric acid compounds of formula (I), wherein R1, R2, R2', R2'' and X have the designations cited in patent claim 1. Said compounds can be inhibitors of CHK1 CHK2 and SGK kinases, and can be used to treat diseases and illnesses such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonal hypertonia, cardiovascular diseases and kidney diseases, generally for all types of fibroses and inflammatory processes.

7. 发明公开

EP1838662A1 QUADRATSÄUREDERIVATE 审中-公开
公开(公告)号：EP1838662A1
公开(公告)日：2007-10-03
申请号：EP05849991.4
申请日：2005-12-09
申请人： Merck Patent GmbH
发明人： MEDERSKI, Werner , GERICKE, Rolf , DORSCH, Dieter , KLEIN, Markus , BEIER, Norbert , LANG, Florian
IPC分类号： C07C225/20 , A61K31/135 , A61P3/00 , A61P9/00 , A61P13/12
CPC分类号： C07C225/20 , C07C225/22 , C07C255/59 , C07C311/37 , C07C311/39 , C07C2601/02 , C07C2601/04
摘要： The invention relates to novel squaric acid compounds of formula (I) wherein R, Rl, R1', R2 and X have the designations cited in patent claim (1). Said compounds are SGK inhibitors and can be used to treat SGK-related diseases and illnesses such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonal hypertonia, cardiovascular diseases and kidney diseases, and generally all types of fibroses and inflammatory processes.
摘要翻译：式（I）的新型方酸化合物，其中R 1，R 1，R 1，R 2，R 2和X具有如下含义：权利要求（1）所述的是SGK抑制剂，可用于治疗SGK诱发的疾病和投诉，例如糖尿病，肥胖症，代谢综合征（血脂异常），全身性和肺性高血压，心血管疾病和肾脏疾病，通常在纤维和任何类型的炎症过程。

8. 发明授权

EP2349983B1 DIFLUORPHENYL-DIACYLHYDRAZID-DERIVATE 有权
标题翻译：二氟苯基diacylhydrazide衍生物
公开(公告)号：EP2349983B1
公开(公告)日：2016-09-14
申请号：EP09744090.3
申请日：2009-11-02
申请人： Merck Patent GmbH
发明人： FUCHSS, Thomas , GRAEDLER, Ulrich , BEIER, Norbert , GERICKE, Rolf , LANG, Florian
IPC分类号： C07C243/38 , A61K31/166
CPC分类号： C07C243/38 , A61K31/15 , A61K45/06 , A61K2300/00

9. 发明授权

EP2242738B1 SGK1-INHIBITOREN ZUR PROPHYLAXE UND/ODER THERAPIE VON VIRALEN ERKRANKUNGEN UND/ODER KARZINOMEN 有权
标题翻译： SGK1抑制剂用于预防和/或治疗病毒性疾病和/或癌症
公开(公告)号：EP2242738B1
公开(公告)日：2012-03-28
申请号：EP09712743.5
申请日：2009-02-17
申请人： Merck Patent GmbH
发明人： FUCHSS, Thomas , GERICKE, Rolf , BEIER, Norbert , LANG, Florian , LANG, Philipp , LANG, Karl
IPC分类号： C07C243/38 , A61K31/166
CPC分类号： C07C243/38
摘要： The present invention relates to a compound of formulas I, Ia, and Ib, and to the pharmaceutically suitable tautomers, salts, sterioisomers, and the enantiomers thereof, including the mixtures thereof in all ratios. The present invention further relates to compounds of formula Il for the prophylaxis and/or treatment of viral diseases and/or carcinomas, where R
1 , R
2 independently of each other are H, CHO, or acetyl, R
3 , R
4 , R
5 , R
6 , R
7 , R
8 , R
9 , R
10 , R
11 independently of each other are H, A, OSO
2 A, HaI, NO
2 , OR
12 , N(R
12 )
2 , CN, O-COA, -[C(R
12 )
2 ]
n COOR
12 , O-[C(R1
12 )
2 ]
o COOR
12 , SO
3 H, -[C(R
12 )
2 ]
n Ar, -CO-Ar, O-[C(R
12 )
2 ]
n Ar, -[C(R
12 )
2 ]
n Het, -[C(R
12 )
2 ]
n C≡CH, O-[C(R
12 )
2 ]
n C≡CH, -[C(R
12 )
2 ]
n CON(R
12 )
2 , -[C(R
12 )
2 ]
n CONR
12 N(R
12 )
2 , O-[C(R
12 )
2 ]
n CON(R
12 )
2 , O-[C(R
12 )
2 ]
o CONR
12 N(R
12 )
2 , NR
12 COA, NR
12 CON(R
12 )
2 , NR
12 SO
2 A, N(SO
2 A)
2 , COR
12 , S(O)
m Ar, SO
2 NR
12 , or S(O)
m A, R
3 ,
and R
4 together also are CH=CH-CH=CH, R
3 and R
4 , R
7 and R
8 or R
8 and R
9 together also are alkylene having 3, 4, or 5 C atoms, wherein one or two CH
2 groups may be substituted by oxygen, A is unbranched or branched alkyl having 1-6 C atoms, wherein 1 -7 H atoms may be substituted by F, or cyclic alkyl having 3-7 C atoms, Ar is unsubstituted phenyl, naphthyl, or biphenyl or phenyl, naphthyl, or biphenyl once, twice, or three times substituted by HaI, A, OR
12 , N(R
12 )
2 , NO2, CN, Phenyl, CON(R
12 )
2 , NR
12 COA, NR
12 CON(R
12 )
2 , NR
12 SO
2 A, COR
12 , SO
2 N(R
12 )
2 , S(O)
m A, -[C(R
12 )
2 ]
n -COOR
12 and/or -O[C(R
12 )
2 ]
O -COOR
12 , Het is a one or two-core, saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O, and/or S atoms, which may be substituted once, twice, or three times by HaI, A, OR
12 , N(R
12 )
2 , NO
2 , CN, COOR
12, CON(R
12 )
2 , NR
12 COA, NR
12 SO
2 A, COR
12 , SO
2 NR
12 , S(O)
m A, =S, =NR
12 , and/or =O (carbonyl oxygen), R
12 is H or A, HaI is F, Cl, Br, or I, m is O, 1 or 2, n is O, 1, 2 or 3, o is 1, 2 or 3, for the prophylaxis and/or treatment of viral diseases and/or carcinomas, and to the pharmaceutically suitable tautomers, salts, sterioisomers, and the enantiomers thereof, including the mixtures thereof in all ratios.

10. 发明公开

EP2349983A2 DIFLUORPHENYL-DIACYLHYDRAZID-DERIVATE 有权
标题翻译：二氟苯基 - DIACYLHYDRAZID衍
公开(公告)号：EP2349983A2
公开(公告)日：2011-08-03
申请号：EP09744090.3
申请日：2009-11-02
申请人： Merck Patent GmbH
发明人： FUCHSS, Thomas , GRAEDLER, Ulrich , BEIER, Norbert , GERICKE, Rolf , LANG, Florian
IPC分类号： C07C243/38 , A61K31/166
CPC分类号： C07C243/38 , A61K31/15 , A61K45/06 , A61K2300/00
摘要： The invention relates to novel difluorphenyl diacylhydrazide derivates of formula I, where R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , and R
7 have the meanings indicated in Claim 1, said derivates being kinase inhibitors and useable for treating illnesses and diseases such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonary hypertension, cardiac circulatory diseases, and kidney diseases, in general for all types of fibroses, inflammatory processes, tumors, and tumor illnesses.

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