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1. 发明申请

US20170334847A1 Amido Compounds And Their Use As Pharmaceuticals 有权
公开(公告)号：US20170334847A1
公开(公告)日：2017-11-23
申请号：US15602693
申请日：2017-05-23
申请人： Incyte Corporation , Incyte Holdings Corporation
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Colin Zhang , Brian W. Metcalf , Chunhong He , Ding-Quan Qian
IPC分类号： C07D207/06 , A61K31/407 , C07D495/04 , C07D493/10 , C07D491/20 , C07D491/107 , C07D491/10 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/10 , C07D471/04 , C07D417/04 , C07D413/14 , C07D413/10 , C07D405/14 , C07D405/04 , C07D403/04 , C07D401/14 , C07D401/10 , C07D401/06 , C07D401/04 , C07D333/34 , C07D295/185 , C07D221/20 , C07D217/26 , C07D217/06 , C07D213/38 , C07D211/70 , C07D211/66 , C07D211/64 , C07D211/58 , C07D211/52 , C07D211/48 , C07D211/46 , C07D211/34 , C07D211/22 , C07D211/18 , C07D211/16 , C07D209/70 , C07D209/62 , C07D209/52 , C07D209/44 , C07D209/42 , C07D209/08 , C07D207/27 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/10 , C07D207/08 , A61K31/4439 , C07D498/20 , C07D513/10
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

2. 发明申请

US20170226073A1 COMPOUNDS AND METHODS FOR TREATING CANCER 审中-公开
公开(公告)号：US20170226073A1
公开(公告)日：2017-08-10
申请号：US15502301
申请日：2015-08-07
申请人： Han W. TUN , Thomas R. CAULFIELD , Christina VON ROEMELING , Laura Ann MARLOW , Mayo Foundation for Medical Education and Research
发明人： John A. Copland, III , Han W. Tun , Thomas R. Caulfield , Christina Von Roemeling , Laura Ann Marlow
IPC分类号： C07D295/192 , C07D213/75 , A61K31/495 , C07D211/66 , A61K31/496 , A61K31/44 , C07D213/64
CPC分类号： C07D295/192 , A61K31/44 , A61K31/495 , A61K31/496 , A61K45/06 , C07D211/64 , C07D211/66 , C07D213/64 , C07D213/75 , A61K2300/00
摘要： This document provides compounds, compositions, and methods for treating cancers including renal cancer (e.g., renal cell carcinoma) as well as ovarian, breast, prostate, colon, pancreatic, bladder, liver, lung, and thyroid cancers and melanoma. For example, compounds, compositions, and methods for using one or more inhibitors of SCD1 to treat renal cell carcinoma (e.g., clear cell renal cell carcinoma (ccRCC)), thyroid cancer, or liver cancer; or to increase the efficacy of treatment for the same.

3. 发明授权

US09126927B2 Amido compounds and their use as pharmaceuticals 有权
标题翻译：酰胺化合物及其作为药物的用途
公开(公告)号：US09126927B2
公开(公告)日：2015-09-08
申请号：US13243565
申请日：2011-09-23
申请人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Brian W. Metcalf , Chunhong He , Ding-Quan Qian , Colin Zhang
IPC分类号： C07D209/96 , C07D307/94 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。

4. 发明授权

US08835654B2 Method and compositions for treating amyloid-related diseases 有权
标题翻译：治疗淀粉样蛋白相关疾病的方法和组合物
公开(公告)号：US08835654B2
公开(公告)日：2014-09-16
申请号：US13237576
申请日：2011-09-20
申请人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
发明人： Xianqi Kong , Xinfu Wu , Abderrahim Bouzide , Isabelle Valade , David Migneault , Francine Gervais , Daniel Delorme , Benoit Bachand , Mohamed Atfani , Sophie Levesque , Bita Samim
IPC分类号： A61K31/381 , C07D409/12 , C07D333/22 , C07D333/36 , C07D333/58
CPC分类号： C07C309/19 , C07C309/14 , C07C309/21 , C07C309/24 , C07C309/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/333 , C07D209/08 , C07D209/16 , C07D209/36 , C07D209/44 , C07D209/48 , C07D209/86 , C07D211/06 , C07D211/14 , C07D211/18 , C07D211/34 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/70 , C07D211/82 , C07D213/04 , C07D213/20 , C07D213/50 , C07D213/75 , C07D213/82 , C07D217/04 , C07D219/10 , C07D231/44 , C07D233/54 , C07D235/28 , C07D257/04 , C07D275/06 , C07D277/66 , C07D295/073 , C07D295/088 , C07D307/14 , C07D307/52 , C07D317/58 , C07D327/04 , C07D327/06 , C07D327/08 , C07D333/20 , C07D333/34 , C07D409/04 , C07D471/04 , C07D471/08 , C07K5/06
摘要： Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
摘要翻译：描述了治疗或预防淀粉样蛋白相关疾病的方法，化合物，药物组合物和试剂盒。

5. 发明授权

US08637576B2 Benzamide derivatives and uses related thereto 失效
标题翻译：苯甲酰胺衍生物及其用途
公开(公告)号：US08637576B2
公开(公告)日：2014-01-28
申请号：US12582535
申请日：2009-10-20
申请人： Jay P. Powers , Michael R. Degraffenreid , Xiao He , Lisa D. Julian , Dustin L. McMinn , Daqing Sun , Yosup Rew , Xuelei Yan
发明人： Jay P. Powers , Michael R. Degraffenreid , Xiao He , Lisa D. Julian , Dustin L. McMinn , Daqing Sun , Yosup Rew , Xuelei Yan
IPC分类号： A61K31/165 , A61K31/44
CPC分类号： C07D277/28 , C07C235/42 , C07C235/54 , C07C237/42 , C07C255/29 , C07C255/31 , C07C255/44 , C07C255/46 , C07C255/60 , C07C317/36 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/38 , C07D211/52 , C07D211/60 , C07D211/64 , C07D213/40 , C07D213/61 , C07D213/74 , C07D213/81 , C07D213/84 , C07D213/89 , C07D233/64 , C07D295/192 , C07D307/22 , C07D309/14 , C07D333/20
摘要： Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
摘要翻译：描述了式I和II的苯甲酰胺衍生物及其药学上可接受的盐，溶剂化物，立体异构体和前药，以及包含其的药物组合物，并具有治疗用途，特别是治疗糖尿病，肥胖症和相关病症和病症：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12如本文所提供。

6. 发明授权

US08318717B2 Compounds modifying apoptosis 有权
标题翻译：化合物修饰凋亡
公开(公告)号：US08318717B2
公开(公告)日：2012-11-27
申请号：US11914994
申请日：2006-05-23
申请人： Ole Thastrup , Jens Chr. Norrild
发明人： Ole Thastrup , Jens Chr. Norrild
IPC分类号： A61K31/397 , C07C233/00 , C07D207/16
CPC分类号： C07C237/22 , C07B2200/11 , C07D207/16 , C07D211/64
摘要： The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.
摘要翻译：本发明涉及能够抑制Smac蛋白与凋亡抑制剂（IAP）结合的化合物。这些化合物优选能够抑制IAP，从而可以促进细胞凋亡或使细胞增殖以进行细胞凋亡。该化合物可用于治疗增殖性疾病，例如癌症。

7. 发明申请

US20120015943A1 SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF 审中-公开
标题翻译：取代的羟基酸及其用途
公开(公告)号：US20120015943A1
公开(公告)日：2012-01-19
申请号：US13184600
申请日：2011-07-18
申请人： Christopher Blackburn , Emily F. Calderwood , Kenneth M. Gigstad , Alexandra E. Gould , Sean J. Harrison , He Xu
发明人： Christopher Blackburn , Emily F. Calderwood , Kenneth M. Gigstad , Alexandra E. Gould , Sean J. Harrison , He Xu
IPC分类号： A61K31/166 , A61K31/4545 , C07C259/10 , C07D239/42 , A61K31/505 , C07D213/75 , A61K31/4418 , C07D213/68 , A61K31/4409 , C07D211/62 , A61K31/4465 , C07D207/34 , A61K31/40 , C07D487/08 , A61K31/407 , A61P35/00 , C07D413/06 , A61K31/5377 , C07D401/12
CPC分类号： C07D239/26 , A61K31/166 , A61K31/40 , A61K31/407 , A61K31/4409 , A61K31/4418 , A61K31/4465 , A61K31/4545 , A61K31/505 , A61K31/5377 , C07C259/10 , C07C259/18 , C07C271/58 , C07C275/28 , C07C311/20 , C07C2601/14 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D207/34 , C07D209/42 , C07D211/62 , C07D211/64 , C07D213/40 , C07D213/56 , C07D213/68 , C07D213/75 , C07D213/81 , C07D231/12 , C07D231/14 , C07D261/18 , C07D277/62 , C07D307/68 , C07D307/85 , C07D333/70 , C07D409/06 , C07D471/04
摘要： This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
摘要翻译：本发明提供式（I）化合物：其中R1，R1b，R2a，R2b，R2c和R2d具有如本说明书中所述的值，可用作HDAC6的抑制剂。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗增殖性，炎症性，感染性，神经性或心血管疾病或病症的方法。

8. 发明授权

US08039636B2 Methods for making 4-tetrazolyl-4-phenylpiperidine compounds 有权
标题翻译：制备4-四唑基-4-苯基哌啶化合物的方法
公开(公告)号：US08039636B2
公开(公告)日：2011-10-18
申请号：US12466797
申请日：2009-05-15
申请人： Kevin Brown , Timothy J. Doyle , John W. F. Whitehead
发明人： Kevin Brown , Timothy J. Doyle , John W. F. Whitehead
IPC分类号： C07D257/04 , C07D405/00
CPC分类号： C07D211/64 , C07D257/04 , C07D307/22 , C07D401/04
摘要： Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I, where Ar1 is —C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a —(C1-C4 alkyl) group; R1 is —(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or —(C1-C4 alkyl); R2 is halogen, —C1-C3 alkyl, —O—(C1-C3 alkyl), —NH(C1-C3 alkyl) or —N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula I can be optionally substituted with one or more R2 groups.
摘要翻译：公开了可用于制备根据式I的4-四唑基-4-苯基哌啶化合物的方法，组合物和中间体，其中Ar 1是-C 3 -C 8环烷基，苯基，萘基，蒽基，菲基或 - （5-7-元））杂芳基，各自为未取代的或被一个或多个R 2基团取代; Ar 2是苯基，萘基，蒽基，菲基或 - （5-7-元）杂芳基，各自是未取代的或被一个或多个R 2基团取代; Z 1和Z 2各自独立地为 - （C 1 -C 4烷基）基团; R1是 - （CH2）nC（O）N（R3）（R4）其中R3和R4各自独立地是H或 - （C1-C4烷基）; R2是卤素，-C1-C3烷基，-O-（C1-C3烷基），-NH（C1-C3烷基）或-N（C1-C3烷基）2; n为1〜4的整数; m为0〜4的整数; 并且在某些实施方案中，连接到根据式I的化合物的哌啶环的4-位的苯基部分可以任选地被一个或多个R 2基团取代。

9. 发明申请

US20110021813A1 PHARMACEUTICAL DRUG CANDIDATES AND METHODS FOR PREPARATION THEREOF 审中-公开
标题翻译：药用药物候选药物及其制备方法
公开(公告)号：US20110021813A1
公开(公告)日：2011-01-27
申请号：US12842990
申请日：2010-07-23
申请人： Xianqi Kong , David Migneault , Xinfu Wu
发明人： Xianqi Kong , David Migneault , Xinfu Wu
IPC分类号： C07C309/05
CPC分类号： C07C309/05 , C07C309/14 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D211/32 , C07D211/52 , C07D211/64 , C07D211/70 , C07D217/04
摘要： The present invention is directed to methods of preparation of sulfonate derivatized compounds, e.g., 3-amino-1-propanesulfonic acid and 1,3-propanedisulfonic acid disodium salt with increased purity, with reduced potential for toxic by-products, and that are pharmaceutically useful, e.g., for the treatment of amyloidosis.
摘要翻译：本发明涉及制备磺酸衍生化合物的方法，例如3-氨基-1-丙磺酸和1,3-丙烷二磺酸二钠盐，其纯度提高，有毒副产物的潜力降低，且为药学上有用的，例如用于治疗淀粉样变性。

10. 发明申请

US20100069437A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 有权
标题翻译：治疗药物有用的治疗药物
公开(公告)号：US20100069437A1
公开(公告)日：2010-03-18
申请号：US12615510
申请日：2009-11-10
申请人： Zhengming Chen
发明人： Zhengming Chen
IPC分类号： A61K31/451 , C07D211/62 , A61K31/454 , A61P1/12 , A61P25/00
CPC分类号： C07D401/04 , C07D211/64 , C07D401/14
摘要： 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.
摘要翻译： 4-四唑基-4-苯基哌啶化合物，包含有效量的4-四唑基-4-苯基哌啶化合物的组合物，用于治疗或预防动物疼痛或腹泻的方法，包括向有需要的动物施用有效量的4 - 四唑基-4-苯基哌啶化合物和用于刺激细胞中阿片受体功能的方法，包括使能够表达阿片受体的细胞与有效量的4-四唑基-4-苯基哌啶化合物接触。

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