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1. 发明授权

US6159990A Oxazolidinones as .alpha..sub.1A receptor antagonists 失效
标题翻译：恶唑烷酮作为α1A受体拮抗剂
公开(公告)号：US6159990A
公开(公告)日：2000-12-12
申请号：US99225
申请日：1998-06-17
申请人： Bharat Lagu , T.G. Murali Dhar , Dhanapalan Nagarathnam , Yoon T. Jeon , Mohammad R. Marzabadi , Wai C. Wong , Charles Gluchowski
发明人： Bharat Lagu , T.G. Murali Dhar , Dhanapalan Nagarathnam , Yoon T. Jeon , Mohammad R. Marzabadi , Wai C. Wong , Charles Gluchowski
IPC分类号： A61K31/58 , C07D263/26 , C07D263/52 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , A61K31/445
CPC分类号： C07D263/52 , A61K31/58 , C07D263/26 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , A61K31/535 , A61K31/495 , A61K31/445 , A61K2300/00
摘要： This invention is directed to oxazolidinone compounds which are selective antagonists for human .alpha..sub.1A 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, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the .alpha..sub.1A 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：本发明涉及作为人α1A受体的选择性拮抗剂的恶唑烷酮化合物。本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及用于治疗其中α1A拮抗作用的任何疾病受体可能是有用的。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。

2. 发明授权

US06620815B1 Oxazolidinones and uses thereof 失效
标题翻译：恶唑烷酮及其用途
公开(公告)号：US06620815B1
公开(公告)日：2003-09-16
申请号：US09636518
申请日：2000-08-10
申请人： Bharat Lagu , T. G. Murali Dhar , Dhanapalan Nagarathnam , Yoon T. Jeon , Mohammad R. Marzabadi , Wai C. Wong , Charles Gluchowski
发明人： Bharat Lagu , T. G. Murali Dhar , Dhanapalan Nagarathnam , Yoon T. Jeon , Mohammad R. Marzabadi , Wai C. Wong , Charles Gluchowski
IPC分类号： A61K31496
CPC分类号： C07D263/52 , A61K31/58 , C07D263/26 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , A61K31/535 , A61K31/495 , A61K31/445 , A61K2300/00
摘要： This invention is directed to oxazolidinone compounds which are selective antagonists for human &agr;1A 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, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A 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：本发明涉及作为人α1A受体的选择性拮抗剂的恶唑烷酮化合物。本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及治疗任何α1A受体拮抗作用的疾病的用途可能是有用的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。

3. 发明授权

US06294566B1 Imidazoline derivatives and uses thereof 失效
标题翻译：咪唑啉衍生物及其用途
公开(公告)号：US06294566B1
公开(公告)日：2001-09-25
申请号：US09398861
申请日：1999-09-20
申请人： Wai C. Wong , Yoon T. Jeon , Charles Gluchowski
发明人： Wai C. Wong , Yoon T. Jeon , Charles Gluchowski
IPC分类号： A61K314168
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。

4. 发明授权

US6093727A 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：US6093727A
公开(公告)日：2000-07-25
申请号：US175253
申请日：1998-10-20
申请人： Wai C. Wong , Yoon T. Jeon , Charles Gluchowski
发明人： Wai C. Wong , Yoon T. Jeon , Charles Gluchowski
IPC分类号： A61K31/415 , A61K31/47 , A61K31/505 , A61P9/12 , C07D233/48 , C07D233/50 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/44 , C07D215/38 , C07D221/04
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 a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.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：本发明涉及新颖的咪唑和咪唑啉衍生物，它们是用于克隆人a，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。

5. 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。

6. 发明授权

US5866579A 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：US5866579A
公开(公告)日：1999-02-02
申请号：US834658
申请日：1997-04-11
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： A61K31/415 , A61K31/47 , A61K31/505 , A61P9/12 , C07D233/48 , C07D233/50 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D471/04 , C07D491/04 , C07D495/04
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 .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.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：本发明涉及新颖的咪唑和咪唑啉衍生物，它们是用于克隆的人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。

7. 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.

8. 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。

9. 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。

10. 发明授权

US06403626B1 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US06403626B1
公开(公告)日：2002-06-11
申请号：US09992947
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.
摘要翻译：本发明提供具有以下结构的化合物：其中R 1，R 2，R 3和R 9各自独立地为H; 直链或支链，取代或未取代的C 1 -C 7烷基，C 2 -C 7烯基或炔基; C 3 -C 7环烷基或环烯基; 酰基，苯基，取代的苯基或杂芳基; 其中每个虚线表示单键或双键，条件是如果R1存在，则R3不存在，并且在3位的N和位置2的C之间存在双键，而在位置2与C之间存在单键 N位于1位，如果R3存在，R1不存在，并且在位置1处的N和位置2的C之间存在双键，在位置2的C与位置3的N之间具有单键; 其中R 4，R 5和R 6各自独立地为H，F，Cl，Br，I; 直链或支链，取代或未取代的C 1 -C 7烷基，C 2 -C 7烯基或炔基; C 3 -C 7环烷基或环烯基; 苯基，取代的苯基，杂芳基，-OH，-OR7，-CN，-COR7，-CO2R7，-CON（R7）2，-OCOR7，-SR7，-N（R7）2，-NR7COR7， - （CH2）， - （CH2）nN（R7）2， - （CH2）nNR7COR7，其中n是1至4的整数; 并且其中R 7和R 8各自独立地为H; 直链或支链，取代或未取代的C 1 -C 7烷基，C 2 -C 7烯基或炔基; 苯基或取代的苯基。这些化合物对克隆的人α2受体是选择性的，并且可用作止痛剂，镇静剂或麻醉剂。

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