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公开(公告)号:US5278148A
公开(公告)日:1994-01-11
申请号:US499852
申请日:1990-03-27
申请人: Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
发明人: Quirico Branca , Hans P. Marki , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
IPC分类号: A61K31/16 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/4427 , A61K31/445 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , C07C237/06 , C07C271/16 , C07C271/18 , C07C271/20 , C07D231/12 , C07D233/54 , C07D233/64 , C07D277/20 , C07D277/30 , C07D333/24 , C07D401/12 , C07D403/12 , C07K5/02 , C07K5/065 , A61K37/02 , A61K37/43 , C07C233/08 , C07C235/02 , C07C237/02 , C07K5/06 , C07K5/08
CPC分类号: C07D231/12 , C07D233/64 , C07D277/30 , C07D333/24 , C07D401/12 , C07D403/12 , C07K5/0207 , C07K5/06078 , A61K38/00
摘要: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.-naphthyl, Y is a bivalent residue in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译: 丙基,异丙基,咪唑-2-基,咪唑-4-基,吡唑-3-基,噻唑-4-基,噻吩-2-基,噻吩-2-基,噻吩-2-基,噻吩-2-基, 叔丁基羰基甲基,苄氧基羰基甲基或叔丁氧基,R 3是异丁基,环己基甲基或苄基,R 4是硝基,氨基或式-N(R 5)(R 6)的基团, 其中R5和R6是烷基或烷氧基烷基; 或任选取代的苯基,苯基烷基或苯基磺酰基烷基等,条件是当R6为烷酰基,烷氧基羰基或芳基烷氧基羰基时,A不为(b)组,虚线可为附加键,R7为苯基或取代苯基,R8为氢或 有机羰基烷基,条件是当R 7是苯基,苄基或α-萘基时,R 8不是烷氧基羰基氨基或芳基烷氧基羰基氨基,Y是光学纯非对映异构体形式的二价残基,非对映异构体的混合物,非对映体外消旋物或非对映体外消旋物的混合物,以及 其药学上可用的盐抑制天然酶肾素的活性,因此可用于控制或预防高血压和心脏功能不全。
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公开(公告)号:US07265109B2
公开(公告)日:2007-09-04
申请号:US10915190
申请日:2004-08-10
IPC分类号: A61K31/5377 , A61K31/454 , A61K31/427 , C07D295/18 , C07D417/14 , C07D413/14 , C07D277/20
CPC分类号: C07D417/14 , C07D417/12
摘要: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagonists which are useful in the treatment of obesity.
摘要翻译: 式I化合物及其药学上可接受的盐和酯,其中取代基具有说明书中给出的意义,并且该化合物是可用于治疗肥胖症的神经肽Y(NPY)拮抗剂。
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公开(公告)号:US07253197B2
公开(公告)日:2007-08-07
申请号:US10634431
申请日:2003-08-05
申请人: Wolfgang Guba , Patrizio Mattei , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger
发明人: Wolfgang Guba , Patrizio Mattei , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger
IPC分类号: A61K31/426 , A61K31/427 , C07D277/42 , C07D401/12
CPC分类号: C07D417/06 , C07D277/42 , C07D417/12 , C07D417/14
摘要: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in the specification, and the compounds, salts and esters can be used for the treatment of obesity.
摘要翻译: 式I化合物及其药学上可接受的盐和酯,其中R 1至R 4具有说明书中给出的含义,并且化合物,盐和酯可以 用于治疗肥胖。
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公开(公告)号:US07166589B2
公开(公告)日:2007-01-23
申请号:US11376976
申请日:2006-03-16
申请人: Michael G. Klug , Patrizio Mattei , Werner Mueller , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Jean-Marc Plancher
发明人: Michael G. Klug , Patrizio Mattei , Werner Mueller , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Jean-Marc Plancher
IPC分类号: C07D403/04 , C07D403/14 , A61K31/551 , A61P3/04
CPC分类号: C07D401/04 , C04B35/632 , C07D215/42 , C07D401/12 , C07D405/14
摘要: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
摘要翻译: 式I化合物及其药学上可接受的盐和酯,其中R 1,R 2,R 3,A 1, 具有权利要求1给出的意义的化合物可以以用于治疗或预防关节炎,心血管疾病,糖尿病,肾功能衰竭,饮食失调的药物制剂的形式使用, 肥胖。
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公开(公告)号:US07064134B2
公开(公告)日:2006-06-20
申请号:US11272207
申请日:2005-11-10
申请人: Michael G. Klug , Patrizio Mattei , Werner Mueller , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Jean-Marc Plancher
发明人: Michael G. Klug , Patrizio Mattei , Werner Mueller , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Jean-Marc Plancher
IPC分类号: C07D401/04 , C07D401/14 , A61K31/4709 , A61P3/04
CPC分类号: C07D401/04 , C04B35/632 , C07D215/42 , C07D401/12 , C07D405/14
摘要: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
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公开(公告)号:US20050038089A1
公开(公告)日:2005-02-17
申请号:US10915199
申请日:2004-08-10
IPC分类号: A61P3/04 , C07D277/42 , C07D277/56 , C07D417/12 , A61K31/426
CPC分类号: C07D417/12 , C07D277/42
摘要: Thiazole derivatives of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, a and b have the significance given in the specification. The compounds are neuropeptide Y Y5 receptor antagonists which can be used for the treatment of obesity.
摘要翻译: 提供式I的噻唑衍生物以及其药学上可接受的盐和酯,其中R 1至R 5,a和b具有说明书中给出的含义。 该化合物是可用于治疗肥胖症的神经肽Y Y5受体拮抗剂。
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公开(公告)号:US20050038073A1
公开(公告)日:2005-02-17
申请号:US10915190
申请日:2004-08-10
IPC分类号: A61P19/02 , C07D417/12 , C07D417/14 , A61K31/4545 , A61K31/454
CPC分类号: C07D417/14 , C07D417/12
摘要: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagonists which are useful in the treatment of obesity.
摘要翻译: 式I化合物及其药学上可接受的盐和酯,其中取代基具有说明书中给出的意义,并且该化合物是可用于治疗肥胖症的神经肽Y(NPY)拮抗剂。
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公开(公告)号:US06818767B2
公开(公告)日:2004-11-16
申请号:US10151505
申请日:2002-05-20
IPC分类号: C07D21542
CPC分类号: C07D401/12 , C07D215/42 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/12
摘要: Quinoline derivatives are useful as neuropeptide Y (NPY) receptor ligands and are particularly effective as neuropeptide Y (NPY) antagonists. These compounds are useful in pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders, or obesity.
摘要翻译: 喹啉衍生物可用作神经肽Y(NPY)受体配体,并且作为神经肽Y(NPY)拮抗剂是特别有效的。 这些化合物可用于治疗或预防关节炎,心血管疾病,糖尿病,肾衰竭,进食障碍或肥胖症的药物制剂。
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公开(公告)号:US06657060B2
公开(公告)日:2003-12-02
申请号:US10008166
申请日:2001-11-08
IPC分类号: C07D40304
CPC分类号: C07D239/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06
摘要: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.
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公开(公告)号:US5389616A
公开(公告)日:1995-02-14
申请号:US99028
申请日:1993-07-29
申请人: Quirico Branca , Werner Neidhart , Jenri Ramuz , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人: Quirico Branca , Werner Neidhart , Jenri Ramuz , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
IPC分类号: C07C215/26 , C07C237/00 , C07C317/44 , C07D233/54 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12 , A61K37/00
CPC分类号: C07D233/64 , C07C215/26 , C07C237/00 , C07C317/44 , C07D263/04 , C07D263/24 , C07D277/30 , C07D307/52 , C07D333/24 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译: 其中A,R 1,R 2,R 3,R 4,R 5和R 6如上所述的式Ⅺ化合物被描述。 式I的化合物对天然酶肾素具有抑制活性,因此可以以用于控制或预防高血压和心脏功能不全的药物制剂的形式使用。
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