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1. 发明授权

US06642268B2 Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors 失效
公开(公告)号：US06642268B2
公开(公告)日：2003-11-04
申请号：US10076091
申请日：2002-02-15
申请人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
发明人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
IPC分类号： A61K3138
CPC分类号： C08G65/329 , A61K31/22 , A61K31/366 , A61K31/38 , A61K31/405 , A61K45/06 , C07D337/06 , C07D337/08 , C07D409/10 , C07D495/04 , C07D495/10 , A61K2300/00
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co—A reductase inhibitors for the treatment of hyperlipidemic conditions.

2. 发明授权

US06492397B1 N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis 失效
标题翻译：用于治疗动脉硬化的N-芳基杂芳基烷基咪唑-2-酮化合物
公开(公告)号：US06492397B1
公开(公告)日：2002-12-10
申请号：US09616639
申请日：2000-07-26
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A01N4330
CPC分类号： C07D401/06 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis. Compounds of particular interest are angiotensin II antagonists of Formula I: wherein Ar is selected from wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R0 is hydrido; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R3, R4, R6, R7, R8, R9, R10 and R11 is hydrido and R5 may be selected from COOH and tetrazolyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗动脉硬化的N-芳基杂芳基烷基咪唑-2-酮化合物。特别感兴趣的化合物是式I的血管紧张素II拮抗剂：其中Ar选自其中m是1;其中R 1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基， 4-甲基丁基，2-乙基丁基，正戊基，新戊基，苯基，甲基苯基，二氟苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基， 1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R 0是氢的; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基，和羟烷基; 其中R 3，R 4，R 6，R 7，R 8，R 9，R 10和R 11各自为氢，R 5可以选自COOH和四唑基; 或其互变异构体或其药学上可接受的盐。

3. 发明授权

US06420417B1 Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors 失效
标题翻译：使用回肠胆汁酸转运抑制苯并噻二嗪和HMG Co-A还原酶抑制剂的联合治疗
公开(公告)号：US06420417B1
公开(公告)日：2002-07-16
申请号：US09676466
申请日：2000-09-29
申请人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
发明人： Bradley T. Keller , Kevin C. Glenn , Robert E. Manning
IPC分类号： A61K3138
CPC分类号： C07D495/04 , A61K31/22 , A61K31/366 , A61K31/38 , A61K31/405 , A61K45/06 , C07D337/06 , C07D337/08 , C07D409/10 , C07D495/10 , C08G65/329 , A61K2300/00
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。还提供了使用回肠胆汁酸转运抑制剂和HMG Co-A还原酶抑制剂联合治疗高脂血症的组合物和方法。

4. 发明授权

US5945408A Hydroxyanidino derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译：羟基亚氨基衍生物可用作一氧化氮合酶抑制剂
公开(公告)号：US5945408A
公开(公告)日：1999-08-31
申请号：US689463
申请日：1996-08-08
申请人： R. Keith Webber , Foe S. Tjoeng , Robert E. Manning
发明人： R. Keith Webber , Foe S. Tjoeng , Robert E. Manning
IPC分类号： A61K31/00 , A61K31/155 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/42 , A61K31/535 , A61K31/5377 , A61K31/5395 , A61K31/55 , A61P9/00 , A61P25/04 , A61P29/00 , A61P37/00 , C07C257/14 , C07C259/14 , C07C271/22 , C07C275/16 , C07C313/28 , C07C313/34 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D233/56 , C07D233/76 , C07D261/08 , C07D273/02 , C07F7/08 , C07K5/068 , C07F7/10 , A01N55/00
CPC分类号： C07F7/0818 , C07C257/14 , C07C259/14 , C07C275/16 , C07C313/28 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07D261/08
摘要： The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了可用作一氧化氮合酶抑制剂的羟基脒基衍生物。

5. 发明授权

US5563154A Tetrahydro-quinolinyl/isoquinolinyl-terminal alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的四氢 - 喹啉基/异喹啉基 - 末端烷基氨基乙炔基丙氨酸氨基二醇化合物
公开(公告)号：US5563154A
公开(公告)日：1996-10-08
申请号：US456364
申请日：1995-06-01
申请人： Gunnar J. Hanson , Robert E. Manning
发明人： Gunnar J. Hanson , Robert E. Manning
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/47 , A61K31/472 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , C07D213/40 , C07D213/42 , C07D215/12 , C07D215/18 , C07D217/14 , C07D217/16 , C07D233/54 , C07D215/14
CPC分类号： C07D213/40 , C07D213/42 , C07D215/12 , C07D217/14
摘要： Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-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 G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl 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).sbsb.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：通常以四氢 - 喹啉基或四氢 - 异喹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G是四氢 - 喹啉基或四氢 - 异喹啉基; 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 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。

6. 发明授权

US5441970A Use of N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders 失效
标题翻译：使用N-芳基杂芳基烷基咪唑-2-酮化合物治疗循环系统疾病
公开(公告)号：US5441970A
公开(公告)日：1995-08-15
申请号：US107742
申请日：1993-08-19
申请人： David B. Reitz , Robert E. Manning
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/10 , C07D401/14 , A61K31/44
CPC分类号： C07D401/06 , A61K31/4439 , C07D401/10 , C07D401/14
摘要： ##STR1## A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of formula (I) wherein A is selected from (a), (b), (c), (d), (e) and (f), wherein m is one; R
1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenetyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R
0 is hydrido; wherein R
2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R
3 , R
4 , R
6 , R
7 , R
8 , R
9 , R
10 and R
11 is hydrido and R
5 must be seleted from COOH, SH, PO
3 H
2 , SO
3 H, CONHNH
2 , CONHNHSO
2 CF
3 , OH, (g), (h) and (i) wherein each of R
42 and R
43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US92 / 02439 Sec。 371日期：1993年8月19日 102（e）日期1993年8月19日PCT提交1992年4月1日PCT公布。第WO92 / 17469号公报（i）（g）（h）（i）（a）（b）（c）< （f）（f）描述了一类N-芳基杂芳基烷基咪唑-2-酮化合物用于治疗循环系统疾病如高血压和充血性心力衰竭。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中A选自（a），（b），（c），（d），（e）和（f） R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，2-乙基丁基，正戊基，新戊基，苯基，甲基苯基，二氟苯基，苯乙酰基，环己基，环己基甲基，环己基乙基，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R 0是氢的; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙基

7. 发明授权

US5411953A Oxazopinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的恶唑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：US5411953A
公开(公告)日：1995-05-02
申请号：US168561
申请日：1993-12-16
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
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as oxazopinyl-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 an oxazopinyl 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 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。

8. 发明授权

US5411950A Benzo-fused oxazocinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：苯并稠合的恶唑烷基封端的烷基氨基乙炔丙氨酸二氨基二醇化合物用于治疗高血压
公开(公告)号：US5411950A
公开(公告)日：1995-05-02
申请号：US198424
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 , C07D267/22
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as benzo-fused oxazocinyl-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 oxazocinyl 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：通常以苯并稠合的恶嗪酰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是苯并稠合的恶唑烷基; 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。

9. 发明授权

US5409925A Oxazobicyclo terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：恶唑二环封端的烷基氨基乙炔丙氨酸二氨基二醇化合物治疗高血压
公开(公告)号：US5409925A
公开(公告)日：1995-04-25
申请号：US186728
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 , C07D265/28
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as oxazobicyclo-terminated alkylamino ethynyl alanine amino diol derivatives 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 an 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：化合物通常表示为恶唑二环封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物高血压。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。

10. 发明授权

US5409922A Thiozopinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
标题翻译：硫唑嘌呤封端的烷基氨基乙炔丙氨酸二氨基二醇化合物治疗高血压
公开(公告)号：US5409922A
公开(公告)日：1995-04-25
申请号：US168747
申请日：1993-12-16
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 , C07D281/06
CPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D277/04 , C07D285/00 , C07D295/13
摘要： Compounds characterized generally as thiazopinyl-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 thiazopinyl 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：通常以噻嗪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。

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