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51. 发明授权

US5198442A (2-imidazolin-2-ylamino) quinoxaline derivatives and methods for using same 失效
标题翻译：（2-咪唑啉-2-基氨基）喹喔啉衍生物及其使用方法
公开(公告)号：US5198442A
公开(公告)日：1993-03-30
申请号：US836061
申请日：1992-02-12
申请人： Charles Gluchowski
发明人： Charles Gluchowski
IPC分类号： C07D403/12
CPC分类号： C07D403/12
摘要： A compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts 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 each of H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are each H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo, provided that the R.sub.2 s or the R.sub.3 s are alkyl radicals; 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 thereapeutic effects, such as alternation in the rate of fluid transport in the gastrointestianl tract, reduction in intraocular pressure, and increase in renal fluid flow.
摘要翻译：选自具有下式的那些的化合物及其药学上可接受的酸加成盐，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各自为H或具有1至4个碳原子的烷基，或者一起为氧代; R 3各自为H或具有1至4个碳原子的烷基，或者一起是氧代，条件是R 2或R 3是烷基; 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，例如胃肠道内液体输送速率的变化，眼内压降低和肾液流量增加。

52. 发明授权

US5112822A (2-imidazolin-2-ylamino) quinoxaline derivatives and methods for using same 失效
标题翻译：（2-咪唑啉-2-基氨基）喹喔啉衍生物及其使用方法
公开(公告)号：US5112822A
公开(公告)日：1992-05-12
申请号：US560776
申请日：1990-07-31
申请人： Charles Gluchowski
发明人： Charles Gluchowski
IPC分类号： A61K31/495 , A61K31/395 , A61K31/498 , A61P1/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P27/02 , A61P43/00 , C07D20060101 , C07D403/12
CPC分类号： C07D403/12
摘要： A compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts 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 each H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are each H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo, provided that the R.sub.2 s or the R.sub.3 s are alkyl radicals; 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 alteration in the rate of fluid transport in the gastrointestinal tract, reduction in intraocular pressure, and increase in renal fluid flow.
摘要翻译：选自下列化合物的化合物：具有下式的化合物及其药学上可接受的酸加成盐，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; R2各自为H或具有1至4个碳原子的烷基，或者一起是氧代; R 3各自为H或具有1至4个碳原子的烷基，或者一起是氧代，条件是R 2或R 3是烷基; 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，这些化合物提供所需的治疗效果，例如胃肠道中流体转运速率的改变，眼内压降低和肾液流量增加。

53. 发明授权

US5034406A Method for reducing or maintaining intraocular pressure 失效
标题翻译：降低或维持眼压的方法
公开(公告)号：US5034406A
公开(公告)日：1991-07-23
申请号：US412528
申请日：1989-09-26
申请人： Charles Gluchowski
发明人： Charles Gluchowski
IPC分类号： C07D263/28 , A61K31/42 , A61K31/421 , A61P27/02 , A61P27/06
CPC分类号： A61K31/42 , Y10S514/913
摘要： A method of reducing or maintaining intraocular pressure in a mammalian eye, e.g., affected with glaucoma, is disclosed. This method comprises administering directly to the mammalian eye an effective amount of one or more 2-cycloalkylamino oxazolines, salts thereof, bases thereof and mixtures thereof.

54. 发明授权

US07208502B2 Methods of treating conditions associated with an Edg-3 receptor 失效
标题翻译：治疗与Edg-3受体相关的病症的方法
公开(公告)号：US07208502B2
公开(公告)日：2007-04-24
申请号：US10390426
申请日：2003-03-14
申请人： David Solow-Cordero , Geetha Shankar , Juliet V. Spencer , Charles Gluchowski
发明人： David Solow-Cordero , Geetha Shankar , Juliet V. Spencer , Charles Gluchowski
IPC分类号： A61K31/47
CPC分类号： A61K31/353 , A61K31/4245 , A61K31/445 , A61K31/47 , A61K31/4745 , A61K31/513 , A61K31/655
摘要： In one aspect, the present invention provides a method of modulating an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with a modulator of the Edg-3 receptor sufficient to modulate the Edg-3 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating an Edg-3 receptor mediated biological activity in a subject. A therapeutically effective amount of a modulator of the Edg-3 receptor is administered to the subject. In yet another aspect, compounds and composition useful for modulation of the Edg-3 receptor are presented.
摘要翻译：一方面，本发明提供调节细胞中Edg-3受体介导的生物活性的方法。将表达Edg-3受体的细胞与Edg-3受体的调节剂接触，足以调节Edg-3受体介导的生物活性。另一方面，本发明提供了调节受试者中Edg-3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-3受体的调节剂。在另一方面，提供了可用于调节Edg-3受体的化合物和组合物。

55. 发明申请

US20050101518A1 Methods of treating conditions associated with an EDG-2 receptor 审中-公开
标题翻译：治疗与EDG-2受体相关的病症的方法
公开(公告)号：US20050101518A1
公开(公告)日：2005-05-12
申请号：US10390427
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： A61K31/00 , A61K31/137 , A61K31/17 , A61K31/381 , A61K31/4015 , A61K31/403 , A61K31/4045 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4418 , A61K31/472 , A61K31/495 , A61K31/513 , A61K31/53
CPC分类号： A61K31/17 , A61K31/00 , A61K31/137 , A61K31/381 , A61K31/4015 , A61K31/403 , A61K31/4045 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4418 , A61K31/472 , A61K31/495 , A61K31/513 , A61K31/53
摘要： In one aspect, the present invention provides a method for modulating an Edg-2 receptor mediated biological activity in a cell. A cell expressing the Edg-2 receptor is contacted with an modulator of the Edg-2 receptor, which modulates the Edg-2 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating Edg-2 receptor mediated biological activity in a subject. A therapeutically effective amount of an modulator of the Edg-2 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-2受体介导的生物活性的方法。表达Edg-2受体的细胞与调节Edg-2受体介导的生物活性的Edg-2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-2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-2受体的调节剂。

56. 发明申请

US20050065194A1 Methods of treating conditions associated with an Edg-2 receptor 审中-公开
标题翻译：治疗与Edg-2受体相关的病症的方法
公开(公告)号：US20050065194A1
公开(公告)日：2005-03-24
申请号：US10760061
申请日：2004-01-16
申请人： Geetha Shankar , David Solow-Cordero , Juliet Spencer , Charles Gluchowski
发明人： Geetha Shankar , David Solow-Cordero , Juliet Spencer , Charles Gluchowski
IPC分类号： A61K31/433 , C07D285/14
CPC分类号： A61K31/433
摘要： In one aspect, the present invention provides a method for modulating an Edg-2 receptor mediated biological activity in a cell. A cell expressing the Edg-2 receptor is contacted with an modulator of the Edg-2 receptor, which modulates the Edg-2 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating Edg-2 receptor mediated biological activity in a subject. A therapeutically effective amount of an modulator of the Edg-2 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-2受体介导的生物活性的方法。表达Edg-2受体的细胞与调节Edg-2受体介导的生物活性的Edg-2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-2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-2受体的调节剂。

57. 发明授权

US06777426B2 Imidazole and imidazoline derivatives and uses thereof 失效
标题翻译：咪唑和咪唑啉衍生物及其用途
公开(公告)号：US06777426B2
公开(公告)日：2004-08-17
申请号：US09933106
申请日：2001-08-20
申请人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
发明人： Wai C. Wong , Yoon T. Jeon , T. G. Murali Dhar , Charles Gluchowski
IPC分类号： C07D23324
CPC分类号： C07D401/06 , C07D233/50 , C07D401/12 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及新的咪唑和咪唑啉衍生物，其是用于克隆的人α2肾上腺素能受体的选择性激动剂。本发明还涉及这些化合物用于治疗其中α2受体调节可能有用的任何疾病的用途。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。

58. 发明授权

US06734182B2 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：US06734182B2
公开(公告)日：2004-05-11
申请号：US10114597
申请日：2002-04-02
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。

59. 发明授权

US06723741B2 Benzimidazoles and benzothiazoles and uses thereof 失效
标题翻译：苯并咪唑和苯并噻唑及其用途
公开(公告)号：US06723741B2
公开(公告)日：2004-04-20
申请号：US10278608
申请日：2002-10-22
申请人： Yoon T. Jeon , Charles Gluchowski
发明人： Yoon T. Jeon , Charles Gluchowski
IPC分类号： A61K31428
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。

60. 发明授权

US06720324B2 Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof 失效
标题翻译：选择性黑色素浓缩激素-1（MCH1）受体拮抗剂及其用途
公开(公告)号：US06720324B2
公开(公告)日：2004-04-13
申请号：US09899635
申请日：2001-07-05
申请人： Mohammad R. Marzabadi , John Wetzel , John E. DeLeon , Bharat Lagu , Charles Gluchowski , Stewart Noble , Dhanapalan Nagarathnam
发明人： Mohammad R. Marzabadi , John Wetzel , John E. DeLeon , Bharat Lagu , Charles Gluchowski , Stewart Noble , Dhanapalan Nagarathnam
IPC分类号： C07D23932
CPC分类号： C07D211/58 , C07C233/79 , C07C2601/14 , C07D211/52 , C07D295/073 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/06 , C07D471/04 , C07D471/10 , C07D491/04 , C07D491/10
摘要： This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.
摘要翻译：本发明涉及作为黑色素浓缩激素-1（MCH1）受体的选择性拮抗剂的化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了改变受试者进食行为的方法，其包括向受试者施用量的有效减少受试者食物消耗的本发明化合物。本发明进一步提供了治疗受试者进食障碍的方法，其包括向受试者施用一定量的有效降低受试者食物消耗的本发明化合物。在本发明的一个实施方案中，喂食障碍是贪食症，神经性贪食症或肥胖症。

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