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81. 发明授权

US07012073B2 Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US07012073B2
公开(公告)日：2006-03-14
申请号：US10896445
申请日：2004-07-22
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 , A61K31/55 , 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.
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。

82. 发明授权

US06686381B2 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US06686381B2
公开(公告)日：2004-02-03
申请号：US10374573
申请日：2003-02-26
申请人： Patrizio Mattei , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Sven Taylor
发明人： Patrizio Mattei , Werner Neidhart , Matthias Heinrich Nettekoven , Philippe Pflieger , Sven Taylor
IPC分类号： A61K31425
CPC分类号： C07D417/06 , C07D277/42
摘要： Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
摘要翻译：提供式I化合物以及其药学上可接受的盐和酯，其中R 1至R 5，n，m和A具有说明书中公开的含义，并且可用于治疗或预防关节炎，心血管疾病，糖尿病，肾衰竭，饮食失调和肥胖。

83. 发明授权

US06521631B2 Heterocyclic sulfonamides 有权
公开(公告)号：US06521631B2
公开(公告)日：2003-02-18
申请号：US10094126
申请日：2002-03-08
申请人： Volker Breu , Philippe Coassolo , Werner Neidhart , Sébastien Roux , Peter Weiss
发明人： Volker Breu , Philippe Coassolo , Werner Neidhart , Sébastien Roux , Peter Weiss
IPC分类号： C07D40114
CPC分类号： C07D401/14 , C07D417/14
摘要： The compounds of formula (I) wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.

84. 发明授权

US5856484A Sulfonylaminopyrimidine carboxylic acid derivatives having endothelin inhibiting activity 失效
标题翻译：具有内皮素抑制活性的磺酰氨基嘧啶羧酸衍生物
公开(公告)号：US5856484A
公开(公告)日：1999-01-05
申请号：US726712
申请日：1996-10-07
申请人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
发明人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
IPC分类号： C07D239/52 , A61K31/495 , A61K31/505 , A61K31/535 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D239/46 , C07D239/557 , C07D239/56 , C07D239/58 , C07D239/69 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D239/47 , C07D403/14
CPC分类号： C07D239/69
摘要： Compounds of formula I: ##STR1## are disclosed. The compounds inhibit the binding of endothelin to its receptors.
摘要翻译：式I化合物：我公开了。该化合物抑制内皮素与其受体的结合。

85. 发明授权

US5837708A Sulphonamides 失效
标题翻译：磺酰胺
公开(公告)号：US5837708A
公开(公告)日：1998-11-17
申请号：US730422
申请日：1996-10-15
申请人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
发明人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D239/69 , A61K31/505 , C07D403/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
摘要翻译：下式定义的式（Ⅰ）化合物。式I化合物是内皮素受体的抑制剂。它们可用于治疗与内皮素活性相关的疾病，特别是循环系统疾病如高血压，局部缺血，血管痉挛和心绞痛。

86. 发明授权

US5420129A Phenylsulfonylamide pyrimidine 失效
公开(公告)号：US5420129A
公开(公告)日：1995-05-30
申请号：US164167
申请日：1993-12-08
申请人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
发明人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael Loffler , Marcel Muller , Werner Neidhart , Henri Ramuz
IPC分类号： A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5377 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/52 , C07D239/56 , C07D239/69 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , A61K31/50
CPC分类号： C07D239/47 , C07D239/48 , C07D239/52 , C07D239/56 , C07D239/69 , C07D401/12 , C07D405/12
摘要： The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.4 is hydrogen, lower-alkyl, trifluoromethyl, lower-alkoxy, lower-alkylthio, hydroxy-lower-alkyl, hydroxy-lower-alkoxy, hydroxy-lower-alkoxy-lower-alkyl, hydroxy-lower-alkoxy-lower-alkoxy, alkoxy-lower-alkyl, alkoxy-lower-alkyloxy, lower-alkylsulfinyl, lower-alkylsulfonyl, 2-methoxy-3-hydroxypropoxy, 2-hydroxy-3-phenylpropyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, di-lower-alkylamino-lower-alkyl, amino, lower-alkylamino, di-lower-alkylamino, arylamino, aryl, arylthio, aryloxy, aryl-lower-alkyl, heterocyclyl, heterocyclo-lower-alkyl, heterocyclylamino, heterocyclylthio, heterocyclyloxy, --CHO, --CH.sub.2 OH or --CH.sub.2 Cl;R.sup.5 to R.sup.8 are independently hydrogen, halogen, trifluoromethyl, lower-alkoxy, lower-alkylthio or cyano;R.sup.6 and R.sup.5 or R.sup.7 together are butadienyl, methylene-dioxy, ethylenedioxy or isopropylidenedioxy;X is --O-- or --S--;Y is --CHO, C.sub.1-4 -alkyl, --(CH.sub.2).sub.1-4 --Z--R.sup.9, --(CH.sub.2).sub.1-4 --OC(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.1-4 NHC(O)R.sup.10, --(CH.sub.2).sub.1-4 OCH.sub.2 CH(OH)CH.sub.2 OH and cyclic ketals thereof, --(CH.sub.2).sub.1-4 NR.sup.9 CH.sub.2 CH(OH)CH.sub.2 OH, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 S(O)CH.sub.3, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 --Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)R.sup.10, --(CH.sub.2).sub.1-4 NR.sup.9 (CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.0-3 CH(OH)R.sup.10, --(CH.sub.2).sub.0-3 CH(OH)(CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.0-3 CH(OH)CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)CH.sub. 2 S(O)CH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)OCH.sub.2 CH.sub.2 OH, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 Z R.sup.11, --(CH.sub.2).sub.0-3 C(O)CH.sub.2 Hal, --(CH.sub.2).sub.1-4 Hal, --(CH.sub.2).sub.1-4 CN, --(CH.sub.2).sub.0-3 C(O)OR.sup.9, --OR.sup.12 or --SR.sup.12 ;R.sup.9 is hydrogen or C.sub.1-4 -alkyl;R.sup.10 is C.sub.1-4 -alkyl;R.sup.11 is hydrogen, C.sub.1-4 -alkanoyl or heterocyclylcarbonyl;R.sup.12 is C.sub.1-4 -alkyl or --(CH.sub.2).sub.0-4 -aryl;Z is --O--, --S-- or --NR.sup.9 --;Het is a heterocyclic residue;Hal is halogen; andn is 0 or 1; and salts thereof.

87. 发明授权

US5393875A Amino acid derivatives having renin inhibiting activity 失效
标题翻译：具有肾素抑制活性的氨基酸衍生物
公开(公告)号：US5393875A
公开(公告)日：1995-02-28
申请号：US100959
申请日：1993-08-03
申请人： Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
发明人： Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
IPC分类号： A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/535 , A61P9/00 , A61P9/04 , A61P9/12 , C07C317/44 , C07C317/50 , C07C323/51 , C07D207/08 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D277/20 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00 , C07H15/12 , C07D295/12 , A61K37/00
CPC分类号： C07D207/08 , C07C317/44 , C07C317/50 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significance given in claim 1,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 form of pharamaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be manufactured according to various methods which are known per se.
摘要翻译：其中A，R 1，R 2，R 3，R 4和R 5具有权利要求1中给出的含义的化合物，其为光学纯非对映异构体，非对映异构体的混合物，非对映体外消旋物或非对映异构体外消旋物的混合物作为其药学上可用的盐抑制天然酶肾素的活性，因此可以以药物制剂的形式用于控制或预防高血压和心脏功能不全。它们可以根据本身已知的各种方法制造。

88. 发明授权

US5256645A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5256645A
公开(公告)日：1993-10-26
申请号：US872736
申请日：1992-04-22
申请人： Quirico Branca , Werner Neidhart , Henri Ramuz , Heinz Stadler , Wolfgang Wostl
发明人： Quirico Branca , Werner Neidhart , 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功能不全的药物制剂的形式使用。

89. 发明授权

US5140011A Amino acid derivatives which have renin inhibiting activity 失效
标题翻译：具有疝抑制活性的氨基酸衍生物
公开(公告)号：US5140011A
公开(公告)日：1992-08-18
申请号：US501694
申请日：1990-03-29
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 , A61K38/00 , A61P9/04 , A61P9/12 , C07C237/06 , C07C271/20 , C07C279/12 , C07D231/12 , C07D233/54 , C07D233/58 , C07D233/64 , C07D277/22 , C07D333/10 , C07D401/12 , C07K5/02 , C07K5/065 , C07K5/097
CPC分类号： C07D233/54 , C07D401/12 , C07K5/021 , C07K5/06078 , C07K5/0823 , A61K38/00
摘要： The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in claim 1, 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 form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.
摘要翻译：其中A，R 1，R 2，R 3和R 4具有权利要求1给出的含义的化合物，其形式为光学纯非对映异构体，非对映异构体的混合物，非对映体外消旋体或非对映体外消旋体的混合物，以及药学上其可用的盐抑制天然酶肾素的活性，因此可以以药物制剂的形式用于控制或预防高血压和心脏功能不全。

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