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61. 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。

62. 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。

63. 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。

64. 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。

65. 发明授权

US5416084A Benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的苯并稠合的硫代吗啉基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5416084A
公开(公告)日：1995-05-16
申请号：US198412
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D279/16
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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 B is a benzo-fused thiomorpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以苯并稠合的硫代吗啉基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物表征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IO 2的化合物; 其中X选自氧原子和亚甲基; 其中B是苯并稠合的硫代吗啉基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C = C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

66. 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。

67. 发明授权

US5409945A Benzyo-fused thiazolidinyl terminated alkylamino ethylnyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：苯偶姻稠合噻唑烷基封端的烷基氨基乙基丙氨酸二氨基二醇化合物治疗高血压
公开(公告)号：US5409945A
公开(公告)日：1995-04-25
申请号：US198425
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D277/62 , C07D277/64
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused thiazolidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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 B is a benzo-fused thiazolidinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为苯并稠合噻唑烷基封端的烷基氨基乙炔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B是苯并稠合噻唑烷基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C 3 CON C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

68. 发明授权

US5409924A Benzo-fused oxazobicyclo terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的苯并稠合的恶唑二环端基烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5409924A
公开(公告)日：1995-04-25
申请号：US198419
申请日：1994-02-22
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , C07D265/34
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused oxazobicyclo-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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 B is a benzo-fused oxazobicyclo group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为苯并稠合的恶唑二环端基的烷基氨基乙炔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B是苯并稠合的恶唑二环基团; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

69. 发明授权

US5409913A Oxazocinyl/thiazocinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的氧嗪酰基/噻嗪基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5409913A
公开(公告)日：1995-04-25
申请号：US186748
申请日：1994-01-25
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： C07D295/12 , A61K31/395 , A61K31/425 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D265/06 , C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13 , C07D498/08 , A61K31/38 , C07D267/22 , C07D281/18
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as oxazocinyl/thiazocinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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 B is a oxazocinyl/thiazocinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C--Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以恶唑烷基/噻嗪基封端的烷基氨基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高血压的肾素抑制剂。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B是恶唑烷基/噻嗪基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C 3 CON C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

70. 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。

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