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1. 发明申请

US20130023494A1 MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译： GPR119受体的调节剂和与之相关的疾病的治疗
公开(公告)号：US20130023494A1
公开(公告)日：2013-01-24
申请号：US13639652
申请日：2011-04-05
申请人： Robert M. Jones , Sangdon Han , Daniel J. Buzard , Juerg Lehmann , Sanju Narayanan , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Daniel J. Buzard , Juerg Lehmann , Sanju Narayanan , Dawei Yue
IPC分类号： A61K31/445 , C07D413/04 , A61K31/454 , C07D401/04 , A61K31/506 , C07D401/14 , C07D401/12 , A61K31/497 , A61K31/501 , C07D417/14 , A61K31/541 , A61K31/4523 , A61P19/00 , A61P25/00 , A61P3/00 , A61P3/10 , A61P3/04 , A61K31/4985 , A61K31/69 , A61K31/4745 , A61K31/522 , A61K31/53 , A61K31/519 , C07D211/46
CPC分类号： C07D211/46 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一试剂或与一种或多种另外的药剂如DPP-IV抑制剂组合使用，双胍类，SGLT2抑制剂或α-葡糖苷酶抑制剂，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加血液肠降血糖水平来改善病情; 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

2. 发明授权

US10377718B2 Apelin receptor (APJ) agonists and uses thereof 有权
公开(公告)号：US10377718B2
公开(公告)日：2019-08-13
申请号：US15023510
申请日：2015-06-05
申请人： Research Triangle Institute , Scott P. Runyon , Rangan Maitra , Sanju Narayanan , James Barnwell Thomas
发明人： Scott P. Runyon , Rangan Maitra , Sanju Narayanan , James Barnwell Thomas
IPC分类号： C07D231/14 , A61K45/06 , A61K31/415 , C07D405/12 , A61K31/422 , A61K31/454 , A61K31/4155 , A61K31/496 , C07D413/12 , C07D403/12 , C07D403/06 , C07D407/12
摘要： This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

3. 发明申请

US20160207889A1 APELIN RECEPTOR (APJ) AGONISTS AND USES THEREOF 审中-公开
标题翻译： APELIN受体（APJ）激素及其用途
公开(公告)号：US20160207889A1
公开(公告)日：2016-07-21
申请号：US15023510
申请日：2015-06-05
申请人： Scott P. RUNYON , Rangan MAITRA , Sanju NARAYANAN , James Barnwell THOMAS , RESEARCH TRIANGLE INSTITUTE
发明人： Scott P. Runyon , Rangan Maitra , Sanju Narayanan , James Barnwell Thomas
IPC分类号： C07D231/14 , A61K45/06 , A61K31/415 , C07D405/12 , A61K31/422 , A61K31/454 , A61K31/4155 , A61K31/496 , C07D413/12
CPC分类号： C07D231/14 , A61K31/415 , A61K31/4155 , A61K31/422 , A61K31/454 , A61K31/496 , A61K45/06 , C07D403/06 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12
摘要： This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
摘要翻译：本公开涉及apelin受体（APJ）的激动剂和这种激动剂的用途。

4. 发明授权

US08809381B2 Highly selective sigma receptor ligands 有权
标题翻译：高选择性sigma受体配体
公开(公告)号：US08809381B2
公开(公告)日：2014-08-19
申请号：US12673486
申请日：2008-08-18
申请人： Christopher R. McCurdy , Christophe Mesangeau , Sanju Narayanan , Rae Reiko Matsumoto , Jacques Henri Poupaert
发明人： Christopher R. McCurdy , Christophe Mesangeau , Sanju Narayanan , Rae Reiko Matsumoto , Jacques Henri Poupaert
IPC分类号： A01N43/78 , A61K31/425 , C07D277/62 , C07D277/68 , A61K31/497 , A01N43/40 , A61K31/445 , A01N43/00 , A61K31/55 , C07D217/00 , C07D295/00 , C07D223/00 , C07D401/00 , C07D451/00 , C07D453/00 , C07D455/00 , C07D471/00 , C07D223/14 , C07D487/00 , C07D491/00 , C07D513/00
CPC分类号： C07D277/70 , A61K51/0455 , A61K51/0459 , A61K51/0468 , C07D235/26 , C07D263/58 , C07D277/68 , C07D401/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D491/10 , C07D491/107
摘要： A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be optionally substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic and heterocyclic group.
摘要翻译：可用于治疗需要治疗涉及σ受体的受试者或用于缓解由具有通式I的药物滥用引起的影响的化合物的化合物，其中R 1可以是任选取代的C-4至C-7N-杂环的基团，例如任选取代的四氢吡啶，任选取代的氮杂环庚烷，叔胺（环状或非环状），异二氢吲哚-1,3-二酮或任选取代的四氢异喹诺酮（芳族取代的）：R2， 3,4,5,6可以各自独立地为下列部分中的任何一种或组合：氰基，硝基，酰基，烷基，酰氨基，叠氮基，异硫氰酸酯，异氰酸酯任选取代的苯胺基，卤素，醚，磺酰胺，硫代酰基，硝基，芳族，杂环，烯属，乙炔，氘或氚; Y可以是CH，CH 2，O，S，OCH 2，N-R，N-Ar，C-R，C-Ar; Z可以是H，O，S，S-R或NR。 R基团可以是H，芳基，烷基或环烷基; “n”可以是长度为1至5个碳原子，立体异构体，功能类似物和其药学上可接受的盐，其中桥接R 1和N的部分可以是任选取代的亚烷基，任选取代的亚烯基或任选取代的亚炔基，并且其中亚烷基可以包括插入的C 3 -C 5环烷基，芳族和杂环基。

5. 发明申请

US20110195955A1 HIGHLY SELECTIVE SIGMA RECEPTOR LIGANDS 有权
标题翻译：高选择性SIGMA受体配体
公开(公告)号：US20110195955A1
公开(公告)日：2011-08-11
申请号：US12673486
申请日：2008-08-18
申请人： Christopher R. McCurdy , Christophe Mesangeau , Sanju Narayanan , Rae Reiko Matsumoto , Jacques Henri Poupaert
发明人： Christopher R. McCurdy , Christophe Mesangeau , Sanju Narayanan , Rae Reiko Matsumoto , Jacques Henri Poupaert
IPC分类号： A61K31/55 , C07D413/06 , C07D413/14 , A61K31/496 , A61P25/30
CPC分类号： C07D277/70 , A61K51/0455 , A61K51/0459 , A61K51/0468 , C07D235/26 , C07D263/58 , C07D277/68 , C07D401/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D491/10 , C07D491/107
摘要： A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be optionally substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic and heterocyclic group.
摘要翻译：可用于治疗需要治疗涉及σ受体的受试者或用于缓解由具有通式I的药物滥用引起的影响的化合物的化合物，其中R 1可以是任选取代的C-4至C-7N-杂环的基团，例如任选取代的四氢吡啶，任选取代的氮杂环庚烷，叔胺（环状或非环状），异二氢吲哚-1,3-二酮或任选取代的四氢异喹诺酮（芳族取代的）：R2， 3,4,5,6可以各自独立地为下列部分中的任何一种或组合：氰基，硝基，酰基，烷基，酰氨基，叠氮基，异硫氰酸酯，异氰酸酯任选取代的苯胺基，卤素，醚，磺酰胺，硫代酰基，硝基，芳族，杂环，烯属，乙炔，氘或氚; Y可以是CH，CH 2，O，S，OCH 2，N-R，N-Ar，C-R，C-Ar; Z可以是H，O，S，S-R或NR。 R基团可以是H，芳基，烷基或环烷基; “n”可以是长度为1至5个碳原子，立体异构体，功能类似物和其药学上可接受的盐，其中桥接R 1和N的部分可以是任选取代的亚烷基，任选取代的亚烯基或任选取代的亚炔基，并且其中亚烷基可以包括插入的C 3 -C 5环烷基，芳族和杂环基。

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