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206 条记录 (耗时 0.058 秒)

    4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as α2 adrenergic agonists
    35.
    发明授权
    4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as α2 adrenergic agonists 失效
    作为α2肾上腺素能激动剂的4-（缩合环状甲基） - 咪唑-2-硫酮

    公开(公告)号：US07396849B2

    公开(公告)日：2008-07-08

    申请号：US11232383

    申请日：2005-09-20

    申请人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gil ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    发明人： Todd M. Heidelbaugh ,  Ken Chow ,  Phong X. Nguyen ,  Daniel W. Gil ,  John E. Donello ,  Michael E. Garst ,  Larry A. Wheeler

    IPC分类号： A61K31/4174 ,  C07D233/42

    CPC分类号： C07D405/06 ,  C07D233/84 ,  C07D401/06 ,  C07D409/06 ,  C07D417/06

    摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

    摘要翻译： 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开内容的若干化合物优先于α2A2肾上腺素能受体是特异性或选择性的α2B2和/或α2C2N2肾上腺素能受体。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或减轻对α2肾上腺素能受体的激动剂治疗有反应的病症。 没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。

    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
    37.
    发明授权
    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
    使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法

    公开(公告)号：US06323204B1

    公开(公告)日：2001-11-27

    申请号：US09222844

    申请日：1998-12-30

    申请人： James A. Burke ,  Michael E. Garst ,  Larry A. Wheeler

    发明人： James A. Burke ,  Michael E. Garst ,  Larry A. Wheeler

    IPC分类号： A61K31495

    CPC分类号： A61K31/495 ,  A61K31/498

    摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.

    摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供所需治疗效果，所述化合物选自具有下式的那些化合物：及其药学上可接受的酸加成盐及其混合物，其中R 1 并且R 2各自选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以在5-，6-，7- - 或8-位的喹喔啉核，R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自Cl ，Br，H和含有1至3个碳原子的烷基。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛。

    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
    39.
    发明授权
    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
    使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法

    公开(公告)号：US5552403A

    公开(公告)日：1996-09-03

    申请号：US332029

    申请日：1994-10-31

    申请人： James A. Burke ,  Michael E. Garst ,  Larry A. Wheeler

    发明人： James A. Burke ,  Michael E. Garst ,  Larry A. Wheeler

    IPC分类号： C07D401/12 ,  A61K31/495 ,  A61K31/498 ,  A61P1/12 ,  A61P1/14 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/02 ,  A61P13/02 ,  A61P13/12 ,  A61P15/00 ,  A61P23/00 ,  A61P23/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P27/16 ,  A61P29/00 ,  C07D403/12

    CPC分类号： A61K31/498 ,  A61K31/495

    摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is independently selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide treatment for ischemia.

    摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物及其药学上可接受的酸加成盐及其混合物 其中R 1和R 2各自独立地选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以是5-， 喹喔啉核的6-，7-或8-位，且R 3，R 4和R 5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并独立地选自 由Cl，Br，H组成的基团和含有1至3个碳原子的烷基。 当向哺乳动物施用时，这些化合物提供缺血治疗。

    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
    40.
    发明授权
    Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
    使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法

    公开(公告)号：US5373010A

    公开(公告)日：1994-12-13

    申请号：US195184

    申请日：1994-02-10

    申请人： Charles Gluchowski ,  Michael E. Garst ,  James A. Burke ,  Larry A. Wheeler

    发明人： Charles Gluchowski ,  Michael E. Garst ,  James A. Burke ,  Larry A. Wheeler

    IPC分类号： A61K31/495 ,  C07D403/12 ,  A61K31/50

    CPC分类号： C07D403/12 ,  A61K31/495 ,  Y10S514/816 ,  Y10S514/854 ,  Y10S514/93

    摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## , pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as constriction of one or more blood vessels and decongestion of one or more nasal passages.

    摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-,6,7或8-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个中，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供所需的治疗效果，例如一个或多个血管的收缩和一个或多个鼻通道的减充血。