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1. 发明授权

US5484812A Propargyl glycine amino use of propargyl diol compounds for treatment of ophthalmic disorders 失效
标题翻译：炔丙基甘氨酸氨基使用炔丙基二醇化合物治疗眼科疾病
公开(公告)号：US5484812A
公开(公告)日：1996-01-16
申请号：US199237
申请日：1994-02-28
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： C07C237/22 , C07C271/20 , C07D277/30 , A61K31/27
CPC分类号： C07C237/22 , C07C271/20 , C07D277/30 , C07C2101/14
摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US92 / 08840 Sec。 371日期1994年2月28日 102（e）1994年2月28日PCT于1992年10月22日提交PCT。化合物通常表征为甘草酸氨基炔丙基二醇衍生物可用作治疗眼部疾病的肾素抑制剂。特别感兴趣的化合物是式I的化合物，其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，b，b，b-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R5是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R8选自乙基，正丙基，异丁基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环己基甲基，环己基乙基，烯丙基，乙烯基和氟乙烯基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

2. 发明授权

US5484811A Use of ethynyl alanine amino diol compounds for treatment of ophthalmic disorders 失效
标题翻译：使用乙炔基丙氨酸氨基二醇化合物治疗眼科疾病
公开(公告)号：US5484811A
公开(公告)日：1996-01-16
申请号：US199211
申请日：1994-02-23
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/165 , A61K31/18 , A61K31/27 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , C07C237/22 , C07C271/20 , C07C311/13 , C07C311/18 , C07C311/31
CPC分类号： A61K31/18 , A61K31/165 , C07C237/22 , C07C271/20 , C07C311/13 , C07C2101/02 , C07C2101/14
摘要： Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 B is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexyimethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US92 / 08842 Sec。 371日期1994年2月28日 102（e）日期1994年2月28日PCT提交1992年10月22日PCT公布。出版物WO93 / 09087 日期：1993年5月13日。通常以乙炔基丙氨酸氨基二醇衍生物为特征的化合物可用作治疗眼科疾病的肾素抑制剂。特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R B B各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，b，b，b-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和 R9可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基二甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R5是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R8选自乙基，正丙基，异丁基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环己基甲基，环己基乙基，烯丙基，乙烯基和氟乙烯基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

3. 发明授权

US5424319A Piperidinyl-terminated non-peptidyl .alpha.-succinamidoacyl aminodiols as anti-hypertensive agents 失效
标题翻译：哌啶基封端的非肽基α-琥珀酰氨基酰氨基二醇作为抗高血压药
公开(公告)号：US5424319A
公开(公告)日：1995-06-13
申请号：US168748
申请日：1993-12-16
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/395 , A61K31/16 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/46 , A61K31/47 , A61K31/535 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61P9/12 , A61P43/00 , C07D207/08 , C07D207/12 , C07D209/08 , C07D209/10 , C07D209/30 , C07D209/44 , C07D215/08 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D263/04 , C07D265/30 , C07D265/36 , C07D277/06 , C07D279/06 , C07D279/16 , C07D295/18 , C07D295/185 , C07D451/02 , C07D498/08 , C12N9/99 , A61K31/445 , C07D211/16 , C07D295/104
CPC分类号： C07D295/185
摘要： Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a piperidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
摘要翻译：通常以N-末端具有哌啶基型基团的α-琥珀酰氨基酰基氨基二醇特征的非肽基化合物可用作治疗高血压的肾素抑制剂。

4. 发明授权

US5416119A Alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkyl-alanine amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的烷基氨基烷基封端的硫化物/含磺酰基的环烷基 - 丙氨酸氨基二醇化合物
公开(公告)号：US5416119A
公开(公告)日：1995-05-16
申请号：US141771
申请日：1993-10-25
申请人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
发明人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/16 , A61K31/165 , C07C317/44 , C07C323/60 , C07C323/25
CPC分类号： C07C323/60 , A61K31/16 , A61K31/165 , C07C317/44 , C07C2101/04 , C07C2101/14 , Y10S514/912 , Y10S514/913
摘要： Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常作为烷基氨基烷基封端的硫化物/含磺酰基的环烷基烷基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式II的化合物：其中m为2或3; 其中x为0或2; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，氟萘基甲基和氯萘基甲基; 其中R 5选自含有3至约12个碳原子的环烷基烷基; 其中R 7为环己基甲基; 其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基，乙基和异丙基; 或其药学上可接受的盐。

5. 发明授权

US5411958A Benzothiomorpholinyl-terminated non-peptidyl .alpha.-succinamidoacyl aminodiols as anti-hypertensive agents 失效
标题翻译：苯硫基吗啉基封端的非肽基α-琥珀酰氨基酰基氨基二醇作为抗高血压药
公开(公告)号：US5411958A
公开(公告)日：1995-05-02
申请号：US198423
申请日：1994-02-22
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/395 , A61K31/16 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/46 , A61K31/47 , A61K31/535 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61P9/12 , A61P43/00 , C07D207/08 , C07D207/12 , C07D209/08 , C07D209/10 , C07D209/30 , C07D209/44 , C07D215/08 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D263/04 , C07D265/30 , C07D265/36 , C07D277/06 , C07D279/06 , C07D279/16 , C07D295/18 , C07D295/185 , C07D451/02 , C07D498/08 , C12N9/99
CPC分类号： C07D295/185
摘要： Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a benzothiomorpholinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
摘要翻译：通常以N-末端具有苯并硫代吗啉基型基团的α-琥珀酰氨基酰氨基二醇表征的非肽基化合物可用作治疗高血压的肾素抑制剂。

6. 发明授权

US5314920A Ethynyl-alanine aryl/alkylsulfonyl-terminated amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的乙炔基 - 丙氨酸芳基/烷基磺酰基封端的氨基二醇化合物
公开(公告)号：US5314920A
公开(公告)日：1994-05-24
申请号：US916447
申请日：1992-07-20
申请人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
发明人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
IPC分类号： C07C317/44 , A61K31/16
CPC分类号： C07C317/44 , C07C2101/02 , C07C2101/14
摘要： Compounds characterized generally as ethynyl alanine aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl-containing moeity; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
摘要翻译：通常表示乙炔基丙氨酸芳基/烷基磺酰基封端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是下式的化合物，其中R 1选自异丙基，异丁基，仲丁基，叔丁基，苯基，氟苯基，氯苯基，苄基，氟苄基，氯苄基，萘基，氟萘基，氯萘基，氟萘基甲基和氯萘基甲基 ; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，氟萘基甲基和氯萘基甲基; 其中R5是炔丙基或含炔丙基的摩尔; 其中R 7为环己基甲基; 并且其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基。

7. 发明授权

US5223514A Quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives 失效
标题翻译：喹啉基/喹啉基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物
公开(公告)号：US5223514A
公开(公告)日：1993-06-29
申请号：US889865
申请日：1992-05-28
申请人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
发明人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
IPC分类号： C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07D471/04
CPC分类号： C07D471/04 , C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07C2101/14
摘要： Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以喹啉基/喹啉基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物为特征的非肽基化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物具有式“IMAGE”，其中R 1选自，其中Y和Z各自独立地选自氢，氯，氟，甲氧基和二甲基氨基; 其中n是选自0至4的数字，包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6和R7一起形成含有5-8个环成员的部分饱和或完全饱和的杂环，其中一个或两个环成员是氧原子，其余的环成员是碳原子，并且该杂环可以任选地被低级烷基或其药学上可接受的盐。

8. 发明授权

US5217991A Cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives 失效
标题翻译：环烷基/环烷基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物
公开(公告)号：US5217991A
公开(公告)日：1993-06-08
申请号：US889738
申请日：1992-05-28
申请人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
发明人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
IPC分类号： C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07D471/04
CPC分类号： C07D471/04 , C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07C2101/14
摘要： Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl: wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以环烷基/环烷基烷基-N-端环烷氧基-C末端氨基羟基β-氨基酸衍生物表征的非肽基化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物具有下式：其中R 1选自环烷基和环烷基烷基，其中所述环烷基含有3至约8个碳原子，所述环烷基烷基的无环烷基部分含有1至约8个碳原子; 其中R2和R4各自独立地选自氢和甲基; 其中R 3是甲基或乙基：其中R 5是环己基甲基; 其中R6和R7一起形成含有5-8个环成员的部分饱和或完全饱和的杂环，其中一个或两个环成员是氧原子，其余的环成员是碳原子，并且该杂环可以任选地被低级烷基或其药学上可接受的盐。

9. 发明授权

US5180744A Aralkyl-N-terminal amino hydroxy 失效
标题翻译：芳烷基-N-末端氨基羟基
公开(公告)号：US5180744A
公开(公告)日：1993-01-19
申请号：US736869
申请日：1991-07-29
申请人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
发明人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
IPC分类号： C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07D471/04
CPC分类号： C07D471/04 , C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07C2101/14
摘要： Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof. g
摘要翻译：通常为芳烷基-N-端氨基羟基β-氨基酸衍生物的非肽基化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物具有式“IMAGE”，其中R 1选自，其中Y和Z各自独立地选自氢，氯，氟，甲氧基和二甲基氨基; 其中n是选自0至4的数字，包括端值; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6是羟基; 其中R 7是异丁基或乙基; 并且其中R8和R9各自是氢的; 或其药学上可接受的盐。

10. 发明授权

US5175181A Imidazolyl/imidazolylalkyl-N-terminal amino hydroxy 失效
标题翻译：咪唑基/咪唑烷基-N-末端氨基羟基
公开(公告)号：US5175181A
公开(公告)日：1992-12-29
申请号：US736868
申请日：1991-07-29
申请人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
发明人： Gunnar J. Hanson , John S. Baran , Dave Weissing , Mark Russell
IPC分类号： C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07D471/04
CPC分类号： C07D471/04 , C07C237/22 , C07D209/18 , C07D209/42 , C07D215/48 , C07D241/44 , C07D307/85 , C07D311/22 , C07D311/24 , C07C2101/14
摘要： Non-peptidyl compounds characterized generally as imidazolyl/imidazolylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is imidazolyl or imidazolylmethyl; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以咪唑基/咪唑烷基-N-端氨基羟基β-氨基酸衍生物表征的非肽基化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物具有下式：其中R 1是咪唑基或咪唑基甲基; 其中R2和R4各自独立地选自氢和甲基; 其中R3是甲基或乙基; 其中R5是环己基甲基; 其中R6是羟基; 并且其中R 7是异丁基或乙基; 或其药学上可接受的盐。

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