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    Substituted cyclopentenes for the treatment of inflammation
    1.
    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。

    1,2 diarylcyclopentenyl compounds for the treatment of inflammation
    6.
    发明授权
    1,2 diarylcyclopentenyl compounds for the treatment of inflammation 失效
    1,2二芳基环戊烯基化合物用于治疗炎症

    公开(公告)号：US5420287A

    公开(公告)日：1995-05-30

    申请号：US253534

    申请日：1994-06-03

    申请人： David B. Reitz ,  Jinglin Li

    发明人： David B. Reitz ,  Jinglin Li

    IPC分类号： C07D317/56 ,  A61K31/10 ,  A61K31/18 ,  A61K31/275 ,  A61K31/357 ,  A61K31/36 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/4418 ,  A61P1/00 ,  A61P1/02 ,  A61P3/06 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07C311/16 ,  C07C311/29 ,  C07C317/14 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65 ,  C07D213/34 ,  C07D213/16

    CPC分类号： C07C311/16 ,  C07C317/14 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65

    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 I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, methyl, ethyl, fluoro, hydroxymethyl, carbomethoxy, trifluoromethyl, carboxyl and fluoromethyl; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.9, R.sup.11 and R.sup.12 is independently selected from hydrido, methyl, fluoro and chloro; and wherein each of R.sup.5 and R.sup.10 is independently selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, methoxy, methylthio, cyano, trifluoromethyl, hydroxymethyl, methoxymethyl, methylsulfonyl and sulfamyl; provided that when A is ##STR3## R.sup.5 cannot be hydrido when R.sup.10 is selected from hydrido, cyano, halo, methyl, trifluoromethyl and methoxy.; further provided that R.sup.10 cannot be hydrido when R.sup.5 is selected from cyano, halo, methyl, trifluoromethyl and methoxy; and further provided that R.sup.5 and R.sup.10 are not both methoxy; or a pharmaceutically suitable 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I定义：其中A选自，其中R 1和R 2各自独立地选自氢，甲基，乙基，氟，羟甲基，甲酯基，三氟甲基，羧基 和氟甲基; 其中R 3，R 4，R 6至R 9，R 11和R 12各自独立地选自氢，甲基，氟和氯; R 5和R 10各自独立地选自氢，氟，氯，溴，碘，甲基，乙基，甲氧基，甲硫基，氰基，三氟甲基，羟甲基，甲氧基甲基，甲基磺酰基和氨磺酰基。 条件是当R 1选自氢，氰基，卤素，甲基，三氟甲基和甲氧基时，当A为时，R 5不能为氢。 当R 5选自氰基，卤素，甲基，三氟甲基和甲氧基时，R 10不能是氢的; 并且进一步提供R5和R10不都是甲氧基; 或其药学上合适的盐。

    1,2 diarylcyclopentenyl compounds for the treatment of inflammation
    7.
    发明授权
    1,2 diarylcyclopentenyl compounds for the treatment of inflammation 失效
    1,2二芳基环戊烯基化合物用于治疗炎症

    公开(公告)号：US5344991A

    公开(公告)日：1994-09-06

    申请号：US146359

    申请日：1993-10-29

    申请人： David B. Reitz ,  Jinglin Li

    发明人： David B. Reitz ,  Jinglin Li

    IPC分类号： C07D317/56 ,  A61K31/10 ,  A61K31/18 ,  A61K31/275 ,  A61K31/357 ,  A61K31/36 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/4418 ,  A61P1/00 ,  A61P1/02 ,  A61P3/06 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07C311/16 ,  C07C311/29 ,  C07C317/14 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65 ,  C07D213/34 ,  C07C311/15

    CPC分类号： C07C311/16 ,  C07C317/14 ,  C07C317/22 ,  C07C317/44 ,  C07C323/65

    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 I: ##STR1## wherein A is selected from ##STR2## each of R.sup.1 and R.sup.2 is independently selected from hydrido, methyl, ethyl, fluoro, hydroxymethyl, carbomethoxy, trifluoromethyl, carboxyl and fluoromethyl; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.9, R.sup.11 and R.sup.12 is independently selected from hydrido, methyl, fluoro and chloro; and wherein each of R.sup.5 and R.sup.10 is independently selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, methoxy, methylthio, cyano, trifluoromethyl, hydroxymethyl, methoxymethyl, methylsulfonyl and sulfamyl; provided that when A is ##STR3## R.sup.5 cannot be hydrido when R.sup.10 is selected from hydrido, cyano, halo, methyl, trifluoromethyl and methoxy; further provided that R.sup.10 cannot be hydrido when R.sup.5 is selected from cyano, halo, methyl, trifluoromethyl and methoxy; and further provided that R.sup.5 and R.sup.10 are not both methoxy; or a pharmaceutically suitable 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I定义：其中A选自，其中R 1和R 2各自独立地选自氢，甲基，乙基，氟，羟甲基，甲酯基，三氟甲基，羧基和 氟甲基; 其中R 3，R 4，R 6至R 9，R 11和R 12各自独立地选自氢，甲基，氟和氯; R 5和R 10各自独立地选自氢，氟，氯，溴，碘，甲基，乙基，甲氧基，甲硫基，氰基，三氟甲基，羟甲基，甲氧基甲基，甲基磺酰基和氨磺酰基。 当A选自氢化，氰基，卤代，甲基，三氟甲基和甲氧基时，当A为时，R 5不能为氢。 当R 5选自氰基，卤素，甲基，三氟甲基和甲氧基时，R 10不能是氢的; 并且进一步提供R5和R10不都是甲氧基; 或其药学上合适的盐。

    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis
    9.
    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。

    Use of N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    10.
    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