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1. 发明授权

US4675328A Phenyl-pyridinium salts and use thereof in inhibiting intestinal resorption 失效
标题翻译：苯基吡啶鎓盐及其在抑制肠吸收中的应用
公开(公告)号：US4675328A
公开(公告)日：1987-06-23
申请号：US819187
申请日：1986-01-15
申请人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
发明人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/4425 , A61P1/00 , A61P3/04 , A61P3/06 , A61P9/10 , C07C49/84 , C07D211/72 , C07D213/04 , C07D213/20 , C07D233/60 , C07D239/26 , C07D277/22 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22 , C07D211/84 , C07D213/69 , C07D213/78
CPC分类号： C07D213/20 , C07C205/45 , C07C49/84 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22
摘要： Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.5,with the proviso that the N-atom in the 3-position of an imidazolium group XN.sup.+ is substituted by Ar,Ar-C.sub.1-4 -alkyl or C.sub.1-4 -alkyl,R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 individually are H, halogen, CF.sub.3, NO.sub.2, CN, C.sub.1-4 - -(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO.sub.2 N(R,Q), C(O)N(Q.sup.4,Q.sup.5), C(O)Q.sup.4, C(O)OQ.sup.4 or OC(O)Q.sup.4,R, Q, Q.sup.1, Q.sup.2 and Q.sup.3 individually are H orC.sub.1-4 -alkyl, andQ.sup.4 and Q.sup.5 individually are C.sub.1-4 -alkyl inhibit the intestinal resorption of cholesterol and of bile salts in the enterohepatic circulation. These salts containing a quaternary N-atom can be manufactured starting from corresponding amines.
摘要翻译：式A-XN + CH2-（Y）n-（CH2）p-（Z）q-L-（T）r-MⅠ的多环盐，其中A-是强有机或无机酸的阴离子; XN +是被R1，R2和R3取代的吡啶鎓，嘧啶鎓，噻唑鎓或咪唑鎓; n，q和r分别为整数1或0，p为1至15的整数; Y是CH 2，C（H，OH）或C（O）：Z是O，S，CH 2，C（O），NQ 1，SO 2，C（O）O，OC（O） Q1）或N（Q1）C（O）; L是被R4取代的对亚苯基; 并且M是被R 5和R 6取代的苯基，T具有以上给出的含义之一，对于Z或是C（CH 3）2，C 2 H 4，C（Q 2）= C（Q 3），C 3 D C，CH 2 C（O） C（O）CH 2，CH 2 O或OCH 2，R 1是Ar，Ar-C 1-4 - 烷基，ArO或ArC（O）基团，Ar是被R 7，R 8和R 9取代的苯基; R 2和R 3分别是H，C 1-4 - 烷基，C 1-4 - 烷氧基或C 6 H 5，条件是咪唑鎓基团XN +的3-位上的N-原子被Ar取代，Ar-C 1-4 - 烷基或C 1-4 - 烷基，R 4，R 5，R 6，R 7，R 8和R 9分别是H，卤素，CF 3，NO 2，CN，C 1-4 - （烷基，烷氧基，烷硫基或烷基磺酰基），SO 2 N（R， Q），C（O）N（Q4，Q5），C（O）Q4，C（O）OQ4或OC（O）Q4，R，Q，Q1，Q2和Q3分别为H或C1-4烷基，Q4和Q5分别为C1-4烷基，抑制肠肝循环中胆固醇和胆汁盐的肠道吸收。这些含有季氮原子的盐可以从相应的胺开始制备。

2. 发明授权

US4692450A Phenyl-pyrimidinium, thiazolium or imidazolium salts and use in inhibiting intestinal resorption of cholesterol and bile salts 失效
标题翻译：苯基嘧啶鎓，噻唑鎓或咪唑鎓盐，用于抑制胆固醇和胆汁盐的肠吸收
公开(公告)号：US4692450A
公开(公告)日：1987-09-08
申请号：US817638
申请日：1986-01-10
申请人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
发明人： Jean-Marie Cassal , Albrecht Edenhofer , Henri Ramuz
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/4425 , A61P1/00 , A61P3/04 , A61P3/06 , A61P9/10 , C07C49/84 , C07D211/72 , C07D213/04 , C07D213/20 , C07D233/60 , C07D239/26 , C07D277/22 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22 , C07D211/70 , C07D211/82 , C07D213/46 , C07D239/02
CPC分类号： C07D213/20 , C07C205/45 , C07C49/84 , C07D303/22 , C07D303/34 , C07D303/36 , C07D317/22
摘要： Polycyclic salts of the formulaA.sup.- XN.sup.+ CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O);Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar--C.sub.1-4 -alkyl, ArO or Arc(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.5,with the proviso that the N-atom in the 3-position of an imidazolium group XN.sup.+ is substituted by Ar, Ar-C.sub.1-4 -alkyl or C.sub.1-4 -alkyl,R.sup.4 ', R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 individually are H, halogen, CF.sub.3, NO.sub.2, CN, C.sub.1-4 -(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO.sub.2 N(R,Q), C(O)N(Q.sup.4, Q.sup.5), C(O)Q.sup.4, C(O)OQ.sup.4 or OC(O)Q.sup.4,R, Q, Q.sup.1 Q.sup.2 and Q.sup.3 individually are H or C.sub.1-4 -alkyl, andQ.sup.4 and Q.sup.5 individually are C.sub.1-4 -alkyl inhibit the intestinal resorption of cholesterol and of bile salts in the enterohepatic circulation. These salts containing a quaternary N-atom can be manufactured starting from corresponding amines.
摘要翻译：式A-XN + CH2-（Y）n-（CH2）p-（Z）q-L-（T）r-MⅠ的多环盐，其中A-是强有机或无机酸的阴离子; XN +是被R1，R2和R3取代的吡啶鎓，嘧啶鎓，噻唑鎓或咪唑鎓; n，q和r分别为整数1或0，p为1至15的整数; Y是CH 2，C（H，OH）或C（O）; Z是O，S，CH2，C（O），NQ1，SO2，C（O）O，OC（O），C（O）N（Q1）或N（Q1）C（O） L是被R4取代的对亚苯基; 并且M是被R 5和R 6取代的苯基，T具有以上给出的含义之一，对于Z或是C（CH 3）2，C 2 H 4，C（Q 2）= C（Q 3），C 3 D C，CH 2 C（O） C（O）CH 2，CH 2 O或OCH 2，R 1为Ar，Ar-C 1-4 - 烷基，ArO或C a（O），Ar为被R 7，R 8和R 9取代的苯基; R 2和R 3分别是H，C 1-4 - 烷基，C 1-4 - 烷氧基或C 6 H 5，条件是咪唑鎓基团XN +的3-位上的N-原子被Ar，Ar-C 1-4 - 烷基或C1-4 - 烷基，R4'，R5，R6，R7，R8和R9分别是H，卤素，CF3，NO2，CN，C1-4-（烷基，烷氧基，烷硫基或烷基磺酰基），SO2N（R， Q），C（O）N（Q4，Q5），C（O）Q4，C（O）OQ4或OC（O）Q4，R，Q，Q1 + L，Q2和Q3分别为H或C1-4 - 烷基，Q4和Q5各自为C1-4烷基，可抑制肠肝循环中胆固醇和胆汁盐的肠道吸收。这些含有季氮原子的盐可以从相应的胺开始制备。

3. 发明授权

US5962682A Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists 失效
标题翻译：芳基和杂芳基磺酰胺衍生物，它们的制备及其作为内皮素拮抗剂的用途
公开(公告)号：US5962682A
公开(公告)日：1999-10-05
申请号：US860985
申请日：1997-08-18
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： C07D239/34 , A61K31/00 , A61K31/18 , A61K31/195 , A61K31/27 , A61K31/35 , A61K31/357 , A61K31/36 , A61K31/41 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/50 , A61K31/505 , A61K31/535 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P43/00 , C07C311/21 , C07C311/29 , C07C323/67 , C07D213/40 , C07D213/44 , C07D213/46 , C07D213/64 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/79 , C07D257/04 , C07D257/06 , C07D295/192 , C07D317/68 , C07D405/12 , C07D413/10
CPC分类号： C07D213/76 , C07C311/21 , C07C311/29 , C07C323/67 , C07D295/192
摘要： Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.8, --NHC(O)NHR.sup.8 or --NHC(O)OR.sup.8 ; R.sup.8 signifies heterocyclyl, phenyl, substituted phenyl or lower-alkyl; A and Y each independently signify oxygen or sulphur, X signifies nitrogen or CH; m signifies 0, 1 or 2; and n signifies 0, 1 or 2; and pharmaceutically usable salts thereof are inhibitors of endothelin receptors. They can therefore 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： PCT No.PCT / EP95 / 04762 Sec。 371日期：1997年8月18日 102（e）日期1997年8月18日PCT提交1995年12月4日PCT公布。 WO96 / 19455 PCT公开号日期：1996年6月27日，式（I）的化合物，其中R 1表示苯基，取代的苯基或杂环基; R2表示苯基或取代的苯基; R3表示氢，低级烷基，氰基，羧基，酯化羧基，苯基，取代的苯基，杂环基或残基-CONR5R6或-NR5COR7; R4表示氢或低级烷基; R5表示氢或残基R7，R6表示 - （CH2）mR7; 或R 5和R 6与与它们相关的N原子一起表示杂环残基; R7表示苯基，取代的苯基，环烷基，杂环基，低级烷基，氰基 - 低级 - 烷基，羟基 - 低级 - 烷基，二 - 低级 - 烷基氨基 - 低级 - 烷基，羧基 - 低级 - 烷基，低级 - 烷氧基羰基 - 低级 - ，低级烷氧基羰基氨基 - 低级 - 烷基或苯基 - 低级 - 烷氧基羰基; R a表示氢，低级烷基或羟基; Rb表示氢或低级烷基; Z表示羟基，氨基或残基-OR8，-OC（O）NHR8，-OC（O）OR8，-NHC（O）NHR8或-NHC（O）OR8; R8表示杂环基，苯基，取代的苯基或低级烷基; A和Y各自独立地表示氧或硫，X表示氮或CH; m表示0，1或2; n表示0,1或2; 及其药学上可用的盐是内皮素受体的抑制剂。因此，它们可用于治疗与内皮素活性相关的疾病，特别是循环性疾病如高血压，局部缺血，血管痉挛和心绞痛。

4. 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。

5. 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。

6. 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.

7. 发明授权

US6133442A Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists 失效
标题翻译：芳基和杂芳基磺酰胺衍生物，它们的制备及其作为内皮素拮抗剂的用途
公开(公告)号：US6133442A
公开(公告)日：2000-10-17
申请号：US263034
申请日：1999-03-05
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： C07D239/34 , A61K31/00 , A61K31/18 , A61K31/195 , A61K31/27 , A61K31/35 , A61K31/357 , A61K31/36 , A61K31/41 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/50 , A61K31/505 , A61K31/535 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P43/00 , C07C311/21 , C07C311/29 , C07C323/67 , C07D213/40 , C07D213/44 , C07D213/46 , C07D213/64 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/79 , C07D257/04 , C07D257/06 , C07D295/192 , C07D317/68 , C07D405/12 , C07D413/10
CPC分类号： C07D213/76 , C07C311/21 , C07C311/29 , C07C323/67 , C07D295/192
摘要： Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.8, --NHC(O)NHR.sup.8 or --NHC(O)OR.sup.8 ;R.sup.8 signifies heterocyclyl, phenyl, substituted phenyl or lower-alkyl;A and Y each independently signify oxygen or sulphur,X signifies nitrogen or CH;m signifies 0, 1 or 2; andn signifies 0, 1 or 2;and pharmaceutically usable salts thereof are inhibitors of endothelin receptors.They can therefore 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：其中R 1表示苯基，取代的苯基或杂环基的式I化合物; R2表示苯基或取代的苯基; R3表示氢，低级烷基，氰基，羧基，酯化羧基，苯基，取代的苯基，杂环基或残基-CONR5R6或-NR5COR7; R4表示氢或低级烷基; R5表示氢或残基R7，R6表示 - （CH2）mR7; 或R 5和R 6与与它们相关的N原子一起表示杂环残基; R7表示苯基，取代的苯基，环烷基，杂环基，低级烷基，氰基 - 低级 - 烷基，羟基 - 低级 - 烷基，二 - 低级 - 烷基氨基 - 低级 - 烷基，羧基 - 低级 - 烷基，低级 - 烷氧基羰基 - 低级 - ，低级烷氧基羰基氨基 - 低级 - 烷基或苯基 - 低级 - 烷氧基羰基; R a表示氢，低级烷基或羟基; Rb表示氢或低级烷基; Z表示羟基，氨基或残基-OR8，-OC（O）NHR8，-OC（O）OR8，-NHC（O）NHR8或-NHC（O）OR8; R8表示杂环基，苯基，取代的苯基或低级烷基; A和Y各自独立地表示氧或硫，X表示氮或CH; m表示0，1或2; n表示0,1或2; 及其药学上可用的盐是内皮素受体的抑制剂。因此，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。

8. 发明授权

US6004965A Sulfonamides 失效
标题翻译：磺胺类
公开(公告)号：US6004965A
公开(公告)日：1999-12-21
申请号：US860107
申请日：1997-08-15
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： C07D239/34 , A61K31/00 , A61K31/505 , A61K31/506 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D239/46 , C07D239/69 , C07D401/04 , C07D401/14 , C07D403/10 , C07D405/14 , A01N43/54 , C07D401/00 , C07D403/00 , C07D413/00
CPC分类号： C07D401/04 , C07D239/69 , C07D401/14 , C07D403/10
摘要： Compounds of the formula: ##STR1## where A, B, R.sup.1 -R.sup.8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
摘要翻译： PCT No.PCT / EP95 / 04843 Sec。 371日期：1997年8月15日 102（e）日期1997年8月15日PCT提交1995年12月8日PCT公布。 WO96 / 19459 PCT公开号日期1996年6月27日下列化学式：其中A，B，R 1 -R 8如本文所述，其可用于治疗与内皮素相关的疾病，例如高血压的内皮素抑制剂。这些化合物的化学合成和含有这些化合物的药物组合物也是有用的。

9. 发明授权

US5541186A Sulfonylaminopyrimidines 失效
标题翻译：磺酰氨基嘧啶
公开(公告)号：US5541186A
公开(公告)日：1996-07-30
申请号：US266072
申请日：1994-06-27
申请人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael L offler , Marcel M uller , Werner Neidhart , Henri Ramuz
发明人： Volker Breu , Kaspar Burri , Jean-Marie Cassal , Martine Clozel , Georges Hirth , Bernd-Michael L offler , Marcel M uller , Werner Neidhart , Henri Ramuz
IPC分类号： A61K31/505 , A61K20060101 , A61K31/33 , A61K31/495 , A61K31/535 , A61K31/55 , A61K31/63 , A61K31/635 , A61P1/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , A61P25/04 , A61P27/02 , C07C311/20 , C07D20060101 , C07D233/46 , C07D239/02 , C07D239/22 , C07D239/24 , C07D239/28 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/49 , C07D239/50 , C07D239/52 , C07D239/545 , C07D239/56 , C07D239/69 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/00 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/00 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/00 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D401/14 , C07D239/69 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.
摘要翻译：其中R1至R，Ra，RbX，Y，Z，m和n具有在描述中给出的含义的式I化合物可用作药物，特别是用于治疗和预防相关的病症与内皮素活动。

10. 发明授权

US5250517A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US5250517A
公开(公告)日：1993-10-05
申请号：US879522
申请日：1992-05-04
申请人： Quirico Branca , Albrecht Edenhofer , Eva-Maria Gutknecht , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
发明人： Quirico Branca , Albrecht Edenhofer , Eva-Maria Gutknecht , Werner Neidhart , Henri Ramuz , Wolfgang Wostl
IPC分类号： C07D233/54 , C07D233/64 , C07K5/02 , C07K5/097 , C07K5/117 , C07K5/10 , A61K37/02 , C07D235/14 , C07K5/08
CPC分类号： C07D233/64 , C07K5/0227 , C07K5/0823 , C07K5/1024
摘要： Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.
摘要翻译：化合物是氨基酸衍生物并且具有式I的化合物，其中R 1是氢或甲基，R 2是乙基，丙基或咪唑-4-基，R 3是异丁基，环己基甲基或苄基，A如本文所定义是有用的作为肾素抑制剂。

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