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1.
公开(公告)号:US5559111A
公开(公告)日:1996-09-24
申请号:US416242
申请日:1995-04-04
申请人: Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
发明人: Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
IPC分类号: C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18 , C07D237/20 , C07D294/14
CPC分类号: C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译: 式I(Ⅰ)的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质,可用作抗高血压药用活性成分。
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2.
公开(公告)号:US5627182A
公开(公告)日:1997-05-06
申请号:US687878
申请日:1996-07-25
申请人: Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
发明人: Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
IPC分类号: C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18 , C07D293/14
CPC分类号: C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译: 式I(Ⅰ)的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质,可用作抗高血压药用活性成分。
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3.
公开(公告)号:US5646143A
公开(公告)日:1997-07-08
申请号:US687277
申请日:1996-07-25
申请人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
发明人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
IPC分类号: C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18 , C07D413/12
CPC分类号: C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1##
摘要翻译: (I)的△-Amin-γ-羟基-ω-芳基 - 链烷酸酰胺
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公开(公告)号:US5705658A
公开(公告)日:1998-01-06
申请号:US800671
申请日:1997-02-14
申请人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
发明人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
IPC分类号: C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18
CPC分类号: C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译: 式I(Ⅰ)的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质,可用作抗高血压药用活性成分。
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公开(公告)号:US5654445A
公开(公告)日:1997-08-05
申请号:US674555
申请日:1996-07-02
申请人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
发明人: Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
IPC分类号: C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18
CPC分类号: C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译: 式I(Ⅰ)的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质,可用作抗高血压药用活性成分。
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6.Aromatically substituted .omega.-amino-alkanoic acid amides and alkanoic acid diamides 失效
标题翻译: 芳基取代的ω-氨基 - 链烷酸酰胺和链烷酸二酰胺公开(公告)号:US5641778A
公开(公告)日:1997-06-24
申请号:US568332
申请日:1995-12-06
申请人: Jurgen Klaus Maibaum , Pascal Rigollier , Peter Herold , Nissim Claude Cohen , Richard Goschke , Stefan Stutz
发明人: Jurgen Klaus Maibaum , Pascal Rigollier , Peter Herold , Nissim Claude Cohen , Richard Goschke , Stefan Stutz
IPC分类号: C07D295/12 , A61K31/16 , A61K31/165 , A61K31/27 , A61K31/38 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/695 , A61P9/12 , C07C231/02 , C07C231/12 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C237/36 , C07C237/42 , C07D207/00 , C07D207/06 , C07D209/04 , C07D209/08 , C07D209/42 , C07D211/00 , C07D211/32 , C07D211/46 , C07D213/02 , C07D213/81 , C07D213/82 , C07D241/00 , C07D241/04 , C07D257/04 , C07D263/04 , C07D263/14 , C07D265/28 , C07D279/12 , C07D295/092 , C07D295/15 , C07D295/18 , C07D295/185 , C07D307/32 , C07D307/33 , C07D401/04 , C07D401/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D521/00 , C07F7/10 , C07D295/145
CPC分类号: C07D213/81 , C07C237/08 , C07C237/22 , C07C237/36 , C07C237/42 , C07D209/42 , C07D211/46 , C07D213/82 , C07D257/04 , C07D263/04 , C07D295/088 , C07D295/15 , C07D295/185 , C07D307/32 , C07D401/04 , C07D405/12 , C07D413/12 , C07D413/14
摘要: Compounds of formula I ##STR1## wherein R.sub.1 is a 2-R.sub.A -3-R.sub.B -phenyl radical, a 2-R.sub.A -4-R.sub.C -phenyl radical, a 2-R.sub.A -pyridin-3-yl radical, a 3-R.sub.A -pyridin-2-yl radical or a 1-R.sub.D -indol-3-yl radical, wherein one of the radicals R.sub.A and R.sub.B is an aliphatic or heterocycloaliphatic-aliphatic radical or free or aliphatically, araliphatically or heteroaraliphatically etherified hydroxy and the other is hydrogen, an aliphatic radical or free or esterified or amidated carboxy, R.sub.C is hydrogen, an aliphatic radical, free or aliphatically, araliphatically, heteroaraliphatically or heteroarylaliphatically etherified hydroxy or an unsubstituted or heteroaliphatically substituted amino group, and R.sub.D is an aliphatic, araliphatic or heteroaliphatic radical, one of the radicals X.sub.1 and X.sub.2 is carbonyl and the other is methylene, R.sub.2 is an aliphatic radical, R.sub.3 is unsubstituted or aliphatically substituted amino, R.sub.4 is an aliphatic or araliphatic radical, and R.sub.5 is an aliphatic or cycloaliphatic-aliphatic radical or an optionally hydrogenated and/or oxo-substituted heteroaryl radical or an optionally hydrogenated and/or oxo-substituted heteroaryl or heteroaliphatyl radical bonded via a carbon atom, and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive active ingredients of medicaments.
摘要翻译: 式I的化合物其中R1是2-RA-3-RB-苯基,2-RA-4-RC-苯基,2-RA-吡啶-3-基, 3-RA-吡啶-2-基或1-RD-吲哚-3-基,其中基团RA和RB之一是脂族或杂环脂族 - 脂族基或自由或脂族,芳烃或杂芳烃醚化的羟基和 另一个是氢,脂族基团或游离的或酯化的或酰胺化的羧基,RC是氢,脂族基团,游离或脂族的,芳香烃,杂芳烃或杂芳基醚化的羟基或未取代的或杂芳基取代的氨基,RD是脂族, 芳基脂族或杂脂族基团,基团X 1和X 2之一是羰基,另一个是亚甲基,R 2是脂族基团,R 3是未取代的或脂族取代的氨基,R 4是脂族或芳脂族基团,R 5是脂族或脂环族基团, 脂肪族基 任选氢化和/或氧取代的杂芳基或任选氢化和/或氧取代的通过碳原子键合的杂芳基或杂芳基与其盐具有肾素抑制性质,并且可以用作抗高血压活性成分 的药物。
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公开(公告)号:US08324235B2
公开(公告)日:2012-12-04
申请号:US12450521
申请日:2008-03-27
申请人: Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Bibia Bennacer
发明人: Peter Herold , Robert Mah , Stefan Stutz , Vincenzo Tschinke , Aleksandar Stojanovic , Nathalie Jotterand , Bibia Bennacer
IPC分类号: A61K31/4188 , C07D401/14 , C07D235/02
CPC分类号: C07D491/20
摘要: The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译: 该专利申请涉及通式(I)的新的杂环化合物,其中R,R 1,R 2,Q,T,n和p具有在说明书中更详细阐述的定义,涉及其制备方法和 使用这些化合物作为药物,特别是作为醛固酮合成酶抑制剂。
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公开(公告)号:US20110212950A1
公开(公告)日:2011-09-01
申请号:US12734321
申请日:2008-10-24
申请人: Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
发明人: Dirk Behnke , Peter Herold , Stjepan Jelakovic , Nathalie Jotterand , Isabelle Lyothier , Robert Mah , Stefan Stutz , Vincenzo Tschinke
IPC分类号: A61K31/538 , C07D413/12 , C07D413/14 , A61P9/00
CPC分类号: C07D413/12 , C07D413/14
摘要: The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R2, has the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.
摘要翻译: 本申请涉及通式(I)的4,4-二取代哌啶及其盐,优选其药学上可接受的盐,其中R2具有说明书中所述的含义,其制备方法和这些化合物的用途 作为药物,特别是作为肾素抑制剂。
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公开(公告)号:US20110144197A1
公开(公告)日:2011-06-16
申请号:US13030419
申请日:2011-02-18
申请人: Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
发明人: Peter Herold , Robert Mah , Vincenzo Tschinke , Stefan Stutz , Aleksandar Stojanovic , Stjepan Jelakovic , Christiane Marti
IPC分类号: A61K31/341 , C07D307/14 , C07D309/06 , A61K31/351 , C07D307/00 , A61K31/343 , C07D307/93 , A61P9/00 , A61P27/06 , A61P9/12 , A61P9/10 , A61P13/12
CPC分类号: A61K31/335
摘要: Compounds of the general formula (formula I) in which the meanings of the substituents R1 and R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
摘要翻译: 取代基R 1和R 6的含义如权利要求1所示的通式(式I)的化合物具有肾素抑制性质,可用作药物。
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公开(公告)号:US07799779B2
公开(公告)日:2010-09-21
申请号:US11887355
申请日:2006-03-30
申请人: Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Christiane Marti , Nathalie Jotterand , Stefan Stutz , Michael Quirmbach
发明人: Peter Herold , Robert Mah , Vincenzo Tschinke , Dirk Behnke , Christiane Marti , Nathalie Jotterand , Stefan Stutz , Michael Quirmbach
IPC分类号: C07D413/12 , C07D413/14 , A61K31/538
CPC分类号: C07D413/12 , C07D413/14
摘要: Compounds of the general formula (I) in which the meanings of the substituents R1, R2, R3, R4, X, Z and n as stated in claim 1 have renin-inhibiting properties and can be used as medicines.
摘要翻译: 具有权利要求1所述的取代基R 1,R 2,R 3,R 4,X,Z和n的含义的通式(I)的化合物具有肾素抑制性质并可用作药物。
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