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1. 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。

2. 发明授权

US5373010A 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：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。

3. 发明授权

US5231096A 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：US5231096A
公开(公告)日：1993-07-27
申请号：US820329
申请日：1992-01-13
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： C07D403/12 , A61K31/495 , A61P7/10 , A61P9/08 , A61P9/10 , A61P27/02
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816
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, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.
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，这些化合物提供期望的治疗效果，例如减少周围疼痛，中枢神经系统麻醉，一个或多个血管的收缩，减少或预防至少一种缺血作用，减压一个或多个鼻通道，以及减少至少一种炎症性疾病的作用。

4. 发明授权

US5326763A 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：US5326763A
公开(公告)日：1994-07-05
申请号：US10954
申请日：1993-01-29
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 reduction inflammation 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.
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的还原性炎症：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。

5. 发明授权

US4725620A 2H-pyran-2,6-(3H)-dione derivatives with anti-allergic activity 失效
标题翻译： 2_H-吡喃-2,6-（3H） - 二酮衍生物具有抗过敏活性
公开(公告)号：US4725620A
公开(公告)日：1988-02-16
申请号：US905822
申请日：1986-09-10
申请人： Michael E. Garst , Charles Gluchowski , Lester J. Kaplan
发明人： Michael E. Garst , Charles Gluchowski , Lester J. Kaplan
IPC分类号： C07D309/36 , A61K31/35
CPC分类号： C07D309/36
摘要： Achiral compounds of a 2H-pyran-2,6(3H)-dione derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof, where R is --(CH.sub.2).sub.m OH or --CH((CH.sub.2).sub.n CH.sub.2 OH).sub.2 where m is 1-5 and n is 0-4. These compounds are useful in the treatment of allergic conditions.
摘要翻译：其中R是 - （CH 2）m OH或-CH（（CH 2）n CH 2 OH）2的式（I）的2 H-吡喃-2,6（3H） - 二酮衍生物或其药学上可接受的盐，其中m 是1-5，n是0-4。这些化合物可用于治疗过敏性疾病。

6. 发明申请

US20050261298A1 Methods of treating conditions associated with an Edg-7 receptor 审中-公开
标题翻译：治疗与Edg-7受体相关的病症的方法
公开(公告)号：US20050261298A1
公开(公告)日：2005-11-24
申请号：US10390428
申请日：2003-03-14
申请人： David Solow-Cordero , Geetha Shankar , Juliet Spencer , Charles Gluchowski
发明人： David Solow-Cordero , Geetha Shankar , Juliet Spencer , Charles Gluchowski
IPC分类号： A61K31/165 , A61K31/382 , A61K31/426 , A61K31/455 , A61K31/4709 , A61K31/498
CPC分类号： A61K31/165 , A61K31/382 , A61K31/426 , A61K31/455 , A61K31/4709 , A61K31/498
摘要： In one aspect, the present invention provides a method for modulating an Edg-7 receptor mediated biological activity in a cell. A cell expressing the Edg-7 receptor is contacted with a modulator of the Edg-7 receptor which is capable of modulating an Edg-7 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating an Edg-7 receptor mediated biological activity in a subject. A therapeutically effective amount of a modulator of the Edg-7 receptor is administered to the subject.
摘要翻译：一方面，本发明提供了调节细胞中Edg-7受体介导的生物活性的方法。表达Edg-7受体的细胞与能够调节Edg-7受体介导的生物活性的Edg-7受体的调节剂接触。另一方面，本发明提供了调节受试者中Edg-7受体介导的生物活性的方法。向受试者施用治疗有效量的Edg-7受体的调节剂。

7. 发明授权

US06727257B1 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines 失效
标题翻译： 5-（杂环烷基）-6-芳基 - 二氢嘧啶
公开(公告)号：US06727257B1
公开(公告)日：2004-04-27
申请号：US09730458
申请日：2000-12-05
申请人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski , Bharat Lagu , Shou Wu Miao
发明人： Dhanapalan Nagarathnam , George Chiu , T. G. Murali Dhar , Wai C. Wong , Mohammad R. Marzabadi , Charles Gluchowski , Bharat Lagu , Shou Wu Miao
IPC分类号： C07D40106
CPC分类号： C07D239/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D491/04
摘要： This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及下式的二氢嘧啶化合物：其中A是人α1C受体的选择性拮抗剂。本发明还涉及这些化合物用于降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ence，心律失常以及用于治疗任何α1C受体拮抗作用的疾病有用本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

8. 发明授权

US06436982B1 Benzimidazole derivatives 失效
公开(公告)号：US06436982B1
公开(公告)日：2002-08-20
申请号：US09992956
申请日：2001-11-05
申请人： Yoon T. Jeon , Charles Gluchowski
发明人： Yoon T. Jeon , Charles Gluchowski
IPC分类号： A61K31415
CPC分类号： C07D403/12
摘要： This invention provides compounds having the structure: wherein each of R1, R2, R3 and R9 is independently H; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl or cycloalkenyl; acyl, phenyl, substituted phenyl, or heteroaryl; wherein each dashed line represents a single bond or a double bond with the proviso that if R1 is present, R3 is absent and there is a double bond between N at position 3 and C at position 2 and a single bond between C at position 2 and N at position 1 and if R3 is present, R1 is absent and there is a double bond between N at position 1 and C at position 2 and a single bond between C at position 2 and N at position 3; wherein each of R4, R5 and R6 is independently H, F, Cl, Br, I; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl or cycloalkenyl; phenyl, substituted phenyl, heteroaryl, —OH, —OR7, —CN, —COR7, —CO2R7, —CON(R7)2, —OCOR7, —SR7, —N(R7)2, —NR7COR7, —(CH2)nOR7, —(CH2)nN(R7)2, —(CH2)nNR7COR7, wherein n is an integer from 1 to 4; and wherein each of R7 and R8 is independently H; straight chain or branched, substituted or unsubstituted C1-C7 alkyl, C2-C7 alkenyl or alkynyl; phenyl or substituted phenyl. These compounds are selective for cloned human alpha 2 receptors and are useful as analgesic, sedative or anaesthetic agents.

9. 发明授权

US06391877B1 Aryl sulfonamides and sulfamide derivatives and uses thereof 失效
标题翻译：芳基磺酰胺和磺酰胺衍生物及其用途
公开(公告)号：US06391877B1
公开(公告)日：2002-05-21
申请号：US09709036
申请日：2000-11-08
申请人： Imadul Islam , Daljit S. Dhanoa , John M. Finn , Ping Du , Charles Gluchowski , Yoon T. Jeon
发明人： Imadul Islam , Daljit S. Dhanoa , John M. Finn , Ping Du , Charles Gluchowski , Yoon T. Jeon
IPC分类号： A61K3118
CPC分类号： C07D405/12 , C07C311/18 , C07C311/29 , C07C311/39 , C07C2601/14 , C07C2602/10 , C07D207/48 , C07D211/96 , C07D215/06 , C07D215/54 , C07D217/26 , C07D241/44
摘要： This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
摘要翻译：本发明涉及新的芳基磺酰胺和磺酰胺化合物，它们选择性地结合并抑制人Y5受体的活性。本发明还涉及这些化合物用于治疗哺乳障碍如肥胖症，神经性厌食症，神经性贪食症和异常病症如性/生殖障碍，抑郁症，癫痫发作，高血压，脑出血，充血性心力衰竭或睡眠障碍和用于治疗任何可能使用Y5受体拮抗作用的疾病。

10. 发明授权

US6159998A Substituted indoles and uses thereof 失效
标题翻译：取代的吲哚及其用途
公开(公告)号：US6159998A
公开(公告)日：2000-12-12
申请号：US492505
申请日：2000-01-27
申请人： Yoon T. Jeon , Charles Gluchowski
发明人： Yoon T. Jeon , Charles Gluchowski
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/425 , A61K31/427 , A61K31/428 , A61P1/00 , A61P1/12 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P13/00 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/06 , A61P25/20 , A61P25/30 , A61P25/32 , A61P27/00 , A61P27/02 , A61P29/00 , C07D277/62 , C07D403/12 , C07D417/12 , A61K31/404 , A61K31/4168 , A61K31/422
CPC分类号： C07D277/62 , C07D403/12 , C07D417/12
摘要： This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及对克隆的人α2受体是选择性的新的吲哚和苯并噻唑化合物。本发明还涉及这些化合物在使用α2激动剂可能适合时的任何适应症的用途。具体来说，这包括用作止痛剂，镇静剂和麻醉剂。此外，本发明包括使用这些化合物降低眼内压，老花眼，治疗偏头痛，高血压，酒精戒断，药物成瘾，类风湿性关节炎，缺血性疼痛，痉挛性，腹泻，鼻减肥，尿失禁以及用作认知增强剂和眼血管收缩剂。本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

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