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公开(公告)号:US07135587B2
公开(公告)日:2006-11-14
申请号:US10450855
申请日:2001-11-30
申请人: Wolfgang Staehle , Alfred Jonczyk , Oliver Schadt , Simon Goodman
发明人: Wolfgang Staehle , Alfred Jonczyk , Oliver Schadt , Simon Goodman
IPC分类号: C07C229/00
CPC分类号: C07D213/74 , C07D235/30
摘要: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.
摘要翻译: 其中R1,R2,R3,R5,R5',X,Y,B,m,n和o如专利权利要求1中所定义的通式(I)的新型尿素和氨基甲酸酯衍生物及其生理学上可接受的盐或溶剂合物 是整联蛋白抑制剂,可用于对抗血栓形成,心肌梗死,冠心病,动脉硬化,炎症,肿瘤。 血管成形术后的骨质疏松症,感染和再狭窄或通过抗血管生成保持或传播的病理过程。
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公开(公告)号:US07632951B2
公开(公告)日:2009-12-15
申请号:US10471836
申请日:2002-02-21
申请人: Oliver Schadt , Alfred Jonczyk , Wolfgang Staehle , Simon Goodman
发明人: Oliver Schadt , Alfred Jonczyk , Wolfgang Staehle , Simon Goodman
IPC分类号: A61K31/44 , C07D213/02
CPC分类号: C07D213/74 , C07D401/12 , C07D409/12
摘要: Novel biphenyl derivatives of the general formula (I) in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments.
摘要翻译: 通式(I)的新型联苯衍生物,其中R 1,R 1',R 1“,R 2,R 2',R 3和n如权利要求1中所定义,其立体异构体及其生理学上可接受的盐或溶剂化物是新的整联蛋白抑制剂 优先抑制alphavbeta6整联蛋白受体。 新化合物特别可用作药物。
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公开(公告)号:US07138417B2
公开(公告)日:2006-11-21
申请号:US10503616
申请日:2003-01-15
申请人: Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
发明人: Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
IPC分类号: C07D213/74 , A61K31/4402
CPC分类号: C07D213/74
摘要: Novel biphenyl derivatives of the general formula I in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments
摘要翻译: 通式I的新型联苯衍生物,其中R 1,R 1,R 2,R 1',R 2, R 3和R 2如专利权利要求1中所定义,其立体异构体和其生理学上可接受的盐或溶剂合物是新的整联蛋白抑制剂,其优先抑制α2/ β6整联蛋白受体。 新化合物特别可用作药物
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公开(公告)号:US20050153902A1
公开(公告)日:2005-07-14
申请号:US10503616
申请日:2003-01-15
申请人: Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
发明人: Wolfgang Staehle , Oliver Schadt , Alfred Jonczyk , Simon Goodman
IPC分类号: A61K31/44 , A61K31/4402 , A61P1/04 , A61P1/18 , A61P3/14 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , C07D213/74 , A61K38/04 , C07D213/72
CPC分类号: C07D213/74
摘要: Novel biphenyl derivatives of the general formula I in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel integrin inhibitors which preferentially inhibit the αvβ6 integrin receptor. The novel compounds can be used, in particular, as medicaments.
摘要翻译: 通式I的新型联苯衍生物,其中R 1,R 1,R 1,R 2,R 2, R 3和R 2如在专利权利要求1中所定义,其立体异构体和其生理学上可接受的盐或溶剂合物是优选抑制α-角蛋白6整联蛋白受体的新型整联蛋白抑制剂。 新化合物特别可用作药物。
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公开(公告)号:US06645991B1
公开(公告)日:2003-11-11
申请号:US10069187
申请日:2002-06-21
申请人: Alfred Jonczyk , Oliver Schadt , Simon Goodman
发明人: Alfred Jonczyk , Oliver Schadt , Simon Goodman
IPC分类号: C07D21374
CPC分类号: C07D213/74
摘要: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.
摘要翻译: 本发明描述了具有生物活性的新颖的式I化合物,其作为整合素α2β2的配体,其中X,Y,Z,R 1,R 2,R 4和R 5如权利要求1中所定义 ,及其生理上可接受的盐和溶剂合物。
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公开(公告)号:US07547695B2
公开(公告)日:2009-06-16
申请号:US10579222
申请日:2004-10-14
申请人: Guenter Hoelzemann , Helene Crassier , Karl-August Ackermann , Wolfgang Staehle , Alfred Jonczyk , Wilfried Rautenberg , Francesc Mitjans , Elisabet Rosell-Vives , Jaume Adan , Marta Soler Riera
发明人: Guenter Hoelzemann , Helene Crassier , Karl-August Ackermann , Wolfgang Staehle , Alfred Jonczyk , Wilfried Rautenberg , Francesc Mitjans , Elisabet Rosell-Vives , Jaume Adan , Marta Soler Riera
IPC分类号: A61K31/5355 , A61K31/519 , C07D413/12 , C07D471/04 , A61P35/00
CPC分类号: C07D471/04
摘要: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and X′ have the designations cited in patent claim 1. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumors.
摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9,X和X'具有专利权利要求1中引用的名称。所述化合物是酪氨酸激酶抑制剂, 特别是TIE-2和Raf激酶,并且可以特别地用于治疗肿瘤。
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公开(公告)号:US07528139B2
公开(公告)日:2009-05-05
申请号:US11578375
申请日:2005-03-17
IPC分类号: C07D471/04 , A61K31/497 , A61P35/00
CPC分类号: C07D471/04
摘要: Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
摘要翻译: 其中R 6,R 7,R 8,R 9和X具有权利要求1所示含义的式(I)化合物是酪氨酸激酶,特别是TIE-2和Raf激酶的抑制剂, 用于治疗肿瘤。
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公开(公告)号:US20090082404A1
公开(公告)日:2009-03-26
申请号:US12328320
申请日:2008-12-04
IPC分类号: A61K31/4439 , C07D401/12
CPC分类号: C04B35/632 , C07D401/12 , C07D403/12 , C07D409/14
摘要: Novel compounds of the formula I in which R1, R1′, L, E, G, M, Q, U, R2, m, p and q have the meanings indicated in Claim 1 and are, for example, inhibitors of tyrosine kinases, for example TIE-2, and can be employed, for example, for the treatment of tumours or other diseases.
摘要翻译: 其中R1,R1',L,E,G,M,Q,U,R2,m,p和q具有权利要求1所述的含义的新颖的式I化合物是例如酪氨酸激酶抑制剂, 例如TIE-2,并且可以用于例如治疗肿瘤或其他疾病。
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公开(公告)号:US07470702B2
公开(公告)日:2008-12-30
申请号:US10577033
申请日:2004-10-14
IPC分类号: A01N43/40 , A61K31/435 , C07D213/00
CPC分类号: C04B35/632 , C07D401/12 , C07D403/12 , C07D409/14
摘要: Novel compounds of the formula I in which R1, R1′, L, E, G, M, Q, U, R2, m, p and q have the meanings indicated. Further, the compounds of formula I can be used as, for example, inhibitors of tyrosine kinases, for example TIE-2 , and can be employed, for example, for the treatment of tumours or other diseases.
摘要翻译: 其中R1,R1',L,E,G,M,Q,U,R2,m,p和q具有所示含义的式I的新型化合物。 此外,式I化合物可用作例如酪氨酸激酶抑制剂,例如TIE-2,并且可用于例如治疗肿瘤或其它疾病。
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公开(公告)号:US20070244135A1
公开(公告)日:2007-10-18
申请号:US11578375
申请日:2005-03-17
IPC分类号: A61K31/519 , C07D471/04
CPC分类号: C07D471/04
摘要: Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
摘要翻译: 式(I)的化合物,其中R 6,R 7,R 8,R 9和/或 X具有权利要求1中所示的含义,是酪氨酸激酶,特别是TIE-2和Raf激酶的抑制剂,特别可用于治疗肿瘤。
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