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1. 发明授权

US06569884B2 Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 失效
标题翻译：用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物
公开(公告)号：US06569884B2
公开(公告)日：2003-05-27
申请号：US09846399
申请日：2001-05-01
申请人： Stephen A. Munk , James A. Burke , Michael E. Garst
发明人： Stephen A. Munk , James A. Burke , Michael E. Garst
IPC分类号： A61K31415
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译：式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

2. 发明授权

US06319935B1 Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 有权
标题翻译：用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物
公开(公告)号：US06319935B1
公开(公告)日：2001-11-20
申请号：US09542216
申请日：2000-04-04
申请人： Stephen A. Munk , Michael E. Garst , James A. Burke
发明人： Stephen A. Munk , Michael E. Garst , James A. Burke
IPC分类号： A61K31425
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译：式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

3. 发明授权

US06329369B1 Methods of treating pain and other conditions 有权
标题翻译：治疗疼痛等症状的方法
公开(公告)号：US06329369B1
公开(公告)日：2001-12-11
申请号：US09679919
申请日：2000-10-05
申请人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk
发明人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk
IPC分类号： A61R314168
CPC分类号： C07D233/56 , C07D233/06 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04 , Y10S514/816 , Y10S514/913
摘要： Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.
摘要翻译：通过用有需要的哺乳动物治疗α2B或α2B / 2C肾上腺素能受体的激动剂来治疗青光眼或升高压力的其它疾病及其副作用降低的方法。还描述了具有这种选择性激动剂活性的化合物。

4. 发明授权

US5731337A Conformationally rigid bicycle and adamantane derivatives useful as .alpha. 2 失效
标题翻译：用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物
公开(公告)号：US5731337A
公开(公告)日：1998-03-24
申请号：US538694
申请日：1995-10-03
申请人： Stephen A. Munk , Michael E. Garst , James A. Burke
发明人： Stephen A. Munk , Michael E. Garst , James A. Burke
IPC分类号： A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61P3/06 , A61P3/08 , A61P25/00 , A61P25/24 , A61P25/26 , A61P37/06 , A61P43/00 , C07C211/39 , C07D233/50 , C07D263/28 , C07D277/18 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/08
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译：式I的化合物其中：环A是所示的五种备选的多环之一，其中与键相邻的虚线表示单键或双键可以是出席会议; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解眼内压升高，非胰岛素依赖性糖尿病，男性阳ence和肥胖症。

5. 发明授权

US06841684B2 Imidiazoles having reduced side effects 失效
标题翻译：具有减少副作用的咪唑类
公开(公告)号：US06841684B2
公开(公告)日：2005-01-11
申请号：US09815362
申请日：2001-03-21
申请人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk , Dario G. Gomez , Todd M. Heidelbaugh
发明人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk , Dario G. Gomez , Todd M. Heidelbaugh
IPC分类号： C07D233/58 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/435 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/538 , A61P1/12 , A61P7/12 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/54 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
CPC分类号： C07D233/56 , C07D233/06 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.
摘要翻译：用于治疗包括疼痛，特别是慢性疼痛，青光眼或升高的眼内压，降低心血管或镇静剂副作用的病症的方法和化合物。还包括制备和使用这些化合物的方法。

6. 发明授权

US06706747B2 Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 失效
标题翻译：用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物
公开(公告)号：US06706747B2
公开(公告)日：2004-03-16
申请号：US10393313
申请日：2003-03-19
申请人： Stephen A. Munk , James A. Burke , Michael E. Garst
发明人： Stephen A. Munk , James A. Burke , Michael E. Garst
IPC分类号： A61K31421
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译：式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可以存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

7. 发明授权

US6150389A Comformationally rigid bicyclic and adamantane derivatives useful as .alpha..sub.2 -adrenergic blocking agents 失效
标题翻译：用作α2肾上腺素能阻断剂的组合刚性双环和金刚烷衍生物
公开(公告)号：US6150389A
公开(公告)日：2000-11-21
申请号：US3902
申请日：1998-01-07
申请人： Stephen A. Munk , Michael E. Garst , James A. Burke
发明人： Stephen A. Munk , Michael E. Garst , James A. Burke
IPC分类号： A61P3/04 , A61P3/10 , A61P15/10 , A61P25/24 , A61P27/02 , C07D233/50 , C07D233/54 , C07D263/28 , C07D277/18 , C07D413/12 , A61K31/421 , C07D263/08
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译：式I化合物，其中：环A是所示的五种替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解眼内压升高，非胰岛素依赖性糖尿病，男性阳ence和肥胖症。

8. 发明授权

US5418234A Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法
公开(公告)号：US5418234A
公开(公告)日：1995-05-23
申请号：US298494
申请日：1994-08-30
申请人： Charles Gluchowski , Michael E. Garst , James A. Burke , Larry A. Wheeler , Michael E. Garst
发明人： Charles Gluchowski , Michael E. Garst , James A. Burke , Larry A. Wheeler , Michael E. Garst
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 reduction in peripheral pain and reduction in or prevention of at least one effect of 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所需治疗效果，所述化合物选自下列化合物：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-或7-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，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，这些化合物提供期望的治疗效果，例如减少外周疼痛和减少或预防至少一种局部缺血的作用。

9. 发明授权

US5756503A Methods for using (2-imidazolin-2-ylamino) Quinoxaline derivatives 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法
公开(公告)号：US5756503A
公开(公告)日：1998-05-26
申请号：US636740
申请日：1996-04-19
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 is disclosed comprising 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 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 desired therapeutic effects, such as reduction in peripheral pain.
摘要翻译：公开了一种治疗哺乳动物的方法，其包括向哺乳动物施用有效量以在哺乳动物中提供期望的治疗效果，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，以及其混合物，其中R 1和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-基氨基可以是5- 喹喔啉核的6-，7-或8-位，并且R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自由Cl，Br，H组成的组和含有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。

10. 发明授权

US5561132A Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法
公开(公告)号：US5561132A
公开(公告)日：1996-10-01
申请号：US390265
申请日：1995-02-15
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 comprising administering an effective amount of a compound of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, is disclosed wherein R.sub.1 and R.sub.2 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 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 wherein the desired therapeutic effect is an alteration in the rate of fluid transport in the gastrointestinal tract.
摘要翻译：公开了一种治疗哺乳动物的方法，其包括施用有效量的下式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各自选自含有1个至4个碳原子和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以在喹喔啉核中的5-，6-，7-或8-位任何一个，R3，R4 并且R 5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，其中期望的治疗效果是胃肠道中流体输送速率的改变。

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