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    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis
    3.
    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。

    Substituted cyclopentenes for the treatment of inflammation
    4.
    发明授权
    Substituted cyclopentenes for the treatment of inflammation 失效
    用于治疗炎症的取代环戊烯

    公开(公告)号：US5663180A

    公开(公告)日：1997-09-02

    申请号：US276006

    申请日：1994-07-15

    申请人： David B. Reitz ,  Jinglin Li

    发明人： David B. Reitz ,  Jinglin Li

    IPC分类号： A61K31/10 ,  A61K31/18 ,  C07C311/16 ,  C07C317/14 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65 ,  C07D213/32 ,  C07D317/50 ,  A01N43/42

    CPC分类号： C07C317/14 ,  A61K31/10 ,  A61K31/18 ,  C07C311/16 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65 ,  C07D213/32 ,  C07D317/50 ,  C07C2101/10 ,  Y10S514/825 ,  Y10S514/916

    摘要： A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R.sup.5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类1,2-二芳基环戊烯基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式III定义：其中R 1和R 2各自独立地选自烷基，羟基，羟基烷基，卤素，卤代烷基，烷氧基羰基和羧基; 其中R5选自烷基磺酰基，卤代烷基磺酰基和氨磺酰基; 并且其中B是苯基或吡啶基，其中B任选在可取代的位置被烷基，卤素，烷硫基，氰基，卤代烷基，烷氧基，羟基烷基和烷氧基烷基取代; 或其药学上可接受的盐。

    Use of N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    5.
    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

    1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
    6.
    发明授权
    1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders 失效
    1-苯基咪唑-2-酮联苯甲基化合物，用于治疗循环系统疾病

    公开(公告)号：US06858636B2

    公开(公告)日：2005-02-22

    申请号：US10649210

    申请日：2003-08-27

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： A61K31/415 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P27/02 ,  A61P27/06 ,  C07D233/70 ,  C07D403/10 ,  A61K31/4166 ,  A61K31/4178

    CPC分类号： C07D403/10 ,  C07D233/70

    摘要： A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述了一类用于治疗循环障碍的1-苯基咪唑-2-酮联苯甲基化合物。 R 1，R 2和R 3各自独立地选自氢，烷基，烷氧基，氰基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基。 ; 烷基羰基和卤代烷基羰基; 条件是R 1，R 2和R 3中的至少一个必须是除氢环以外的取代基，另外条件是当R 1和R 3各自为氢时 那么R 2不能是氯; 其中R 4是氢的; 其中R 5是烷基; 并且其中R 6是四唑基; 或其立体异构体或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    8.
    发明授权
    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders 失效
    用于治疗循环系统疾病的N-芳基杂芳基烷基咪唑-2-酮化合物

    公开(公告)号：US5861420A

    公开(公告)日：1999-01-19

    申请号：US784223

    申请日：1997-01-16

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  A01N43/40 ,  C07D401/00 ,  C07D413/00 ,  C07D417/04

    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 circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.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, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is hydrido; wherein R.sup.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.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 is hydrido and R.sup.5 must be selected from COOH, SH, P0.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR3## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof.

    摘要翻译： 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下式的血管紧张素II拮抗剂：其中A选自 和，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， 苯乙基，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必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，

    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
    10.
    发明授权
    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
    用于治疗循环障碍的N-取代的N-（α-三唑基 - 甲苯酰基）吡咯化合物

    公开(公告)号：US5484937A

    公开(公告)日：1996-01-16

    申请号：US117269

    申请日：1993-09-07

    申请人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D521/00 ,  C07D403/10 ,  A61K31/41

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from alkyl; and wherein R.sup.2 is selected from alkyl; and wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自烷基; 并且其中R 2选自烷基; R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基， 甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。