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    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis
    52.
    发明授权
    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis 失效
    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。

    Tetrahydro-quinolinyl/isoquinolinyl-terminal alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    55.
    发明授权
    Tetrahydro-quinolinyl/isoquinolinyl-terminal alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
    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。

    Use of N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    56.
    发明授权
    Use of N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders 失效
    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

    Oxazopinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    57.
    发明授权
    Oxazopinyl terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
    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。