专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2017074833A1 MACROCYCLIC SPIROCARBAMATE DERIVATIVES AS FACTOR XIA INHIBITORS, PHARMACEUTICALLY ACCEPTABLE COMPOSITIONS AND THEIR USE 审中-公开
标题翻译：作为因子XIA抑制剂的大环磺胺衍生物，药学上可接受的组合物及其用途
公开(公告)号：WO2017074833A1
公开(公告)日：2017-05-04
申请号：PCT/US2016/058363
申请日：2016-10-24
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LIM, Yeon-Hee , XU, Jiayi , ZHOU, Wei
发明人： ALI, Amjad , LIM, Yeon-Hee , XU, Jiayi , ZHOU, Wei
IPC分类号： C07D401/06 , C07D487/04 , A61K31/4747 , C07D491/10
CPC分类号： A61K31/4747 , C07D498/10 , C07D519/00
摘要： The present invention provides a compound of Formula (I) and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds and said stereoisomers, and pharmaceutical compositions thereof, and methods for using said compounds and compositions for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
摘要翻译：本发明提供了式（I）化合物及其立体异构体，所述化合物和所述立体异构体的药学上可接受的盐及其药物组合物，以及使用所述化合物和组合物治疗或预防血栓形成，栓塞，高凝状态或纤维变性。这些化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

2. 发明申请

WO2013170191A1 METHODS OF USING ANTAGONISTS OF NAD BIOSYNTHESIS FROM NICOTINAMIDE 审中-公开
标题翻译：从NICOTINAMIDE使用NAD生物合成的拮抗剂的方法
公开(公告)号：WO2013170191A1
公开(公告)日：2013-11-14
申请号：PCT/US2013/040613
申请日：2013-05-10
申请人： GENENTECH, INC. , FORMA TM, LLC
发明人： SHAMES, David , BELMONT, Lisa
IPC分类号： A61K38/10 , A61K39/395 , A61K31/4406 , A61K31/4409 , A61K31/4425 , A61K31/451 , A61K31/455 , A61K31/4747 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/451 , A61K31/4406 , A61K31/4409 , A61K31/4425 , A61K31/455 , A61K31/4747 , A61K31/5377 , A61K2300/00
摘要： Provided herein are NAD biosynthesis from nicotinamide antagonists (e.g., Nampt antagonists and/or NMNAT antagonists) and methods of using the same.
摘要翻译：本文提供了来自烟酰胺拮抗剂（例如，Nampt拮抗剂和/或NMNAT拮抗剂）的NAD生物合成及其使用方法。

3. 发明申请

WO2013068769A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2013068769A1
公开(公告)日：2013-05-16
申请号：PCT/GB2012/052806
申请日：2012-11-12
申请人： RE:VIRAL LTD
发明人： COCKERILL, Stuart , PILKINGTON, Christopher , LUMLEY, James , ANGELL, Richard , MATHEWS, Neil
IPC分类号： C07D401/06 , C07D403/06 , C07D413/06 , C07D471/10 , A61K31/437 , A61K31/4439 , A61K31/538 , A61P31/14
CPC分类号： C07D403/06 , A61K31/4184 , A61K31/437 , A61K31/4747 , A61K31/5386 , A61K31/5513 , A61K45/06 , C07D401/06 , C07D413/06 , C07D471/10 , C07D498/10
摘要： Benzimidazoles of formula (I): wherein: A is 5-to 12-membered aryl or 5-to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, -(CH 2 ) p -, -X-, -CH 2 -X-, or -X-CH 2 -; X is -O-, -S-, -N(R 2 )-, >C=O, >S(=O), >S(=O) 2 , -O-C(=O)-, -C(=O)-O-, N(R 2 )-C(=O)-, or -C(=O)-N(R 2 )-; each L is independently a single bond, C 1-3 alkylene, C 2-3 alkenylene or C 2-3 alkynylene; R 1 is C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, each of which is unsubstituted or substituted; each Z is independently -N(R 2 ) 2 , -OR 2 , -SR 2 , -S(=O)R 2 , -S(=O) 2 R 2 ; each R 2 is independently hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
摘要翻译：式（I）的苯并咪唑：其中：A为5至12元芳基或5至12元杂芳基，其各自为未取代或取代的; Y是单键， - （CH 2）p - ， - X - ， - CH 2 -X-或-X-CH 2 - ; X是-O - ， - S - ， - N（R 2） - ，> C = O，> S（= O），> S（= O）2，-OC（= O） - ， - ）-O-，N（R 2）-C（= O） - 或-C（= O）-N（R 2） - ; 每个L独立地是单键，C1-3亚烷基，C2-3亚烯基或C2-3亚炔基; R 1为C 1-6烷基，C 2-6烯基或C 2-6炔基，其各自为未取代或取代的; 每个Z独立地是-N（R 2）2，-OR 2，-SR 2，-S（= O）R 2，-S（= O）每个R 2独立地是氢，C 1-6烷基，C 2-6烯基或C 2-6炔基，其中所述烷基，烯基和炔基是未取代的或取代的; m为0,1,2或3; n为1,2或3; 和p为1,2或3; 其药学上可接受的盐是RSV的抑制剂，因此可用于治疗或预防RSV感染。

4. 发明申请

WO2013024130A1 FURO[3,4-C]QUINOLINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： FURO [3,4-C]喹啉衍生物，含有这些化合物的药物，其使用及其制备方法
公开(公告)号：WO2013024130A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/065989
申请日：2012-08-16
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , TRIESELMANN, Thomas , HAMPRECHT, Dieter , WAGNER, Holger
发明人： TRIESELMANN, Thomas , HAMPRECHT, Dieter , WAGNER, Holger
IPC分类号： C07D491/20 , A61K31/4355 , A61P9/00
CPC分类号： C07D491/20 , A61K31/4747 , A61K45/06
摘要： The present invention relates to compounds defined by formula (I), wherein the variables R 1 -R 8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
摘要翻译：本发明涉及由式（I）定义的化合物，其中变量R1-R8如描述中所定义，具有有价值的药理学活性。特别地，化合物是胆固醇酯转移蛋白（CETP）的抑制剂，因此适用于治疗和预防可受该蛋白质抑制影响的疾病。

5. 发明申请

WO2012149236A1 NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS 审中-公开
标题翻译：新型双相含氮异氰酸酯TGR5受体调节剂
公开(公告)号：WO2012149236A1
公开(公告)日：2012-11-01
申请号：PCT/US2012/035327
申请日：2012-04-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
发明人： ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
IPC分类号： C07D215/08 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/4709 , A61K31/553 , A61K31/554 , A61P3/00 , A61P9/00 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4747 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , A61K45/06 , C07D215/08 , C07D221/16 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/60
摘要： Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R 3 , R 4 , R 4a , R 5a , R 5b , R 5c , R 5d , R 5e , R 6a , R 6b , and R 6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：式I的新型化合物或其对映体，非对映体，互变异构体，前药或其盐，其中m，Q，T，U，V，环A，X，Y，R 3，R 4，R 4a，R 5a，R 5b，R 5c，本文定义的R5e，R6a，R6b和R6c是TGR5G蛋白偶联受体调节剂。 TGR5G蛋白偶联受体调节剂可用于治疗，预防或减缓需要TGR5G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物和通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与TGR5G蛋白偶联受体的活性有关的疾病或病症的方法。

6. 发明申请

WO2012011103A2 METHODS AND COMPOSITIONS FOR INHIBITING THE NUCLEAR FACTOR kB PATHWAY 审中-公开
标题翻译：抑制核因子kB途径的方法和组合物
公开(公告)号：WO2012011103A2
公开(公告)日：2012-01-26
申请号：PCT/IL2011/000576
申请日：2011-07-19
申请人： BEN GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITY , MOR RESEARCH APPLICATIONS LTD. , GOLAN, Avi , GOPAS, Jacob , OZER, Janet , EISNER, Nadav , BACHER, Adelbert , EISENREICH, Wolfgang , OSTROZHENKOVA, Elena , WINER, Hila
发明人： GOLAN, Avi , GOPAS, Jacob , OZER, Janet , EISNER, Nadav , BACHER, Adelbert , EISENREICH, Wolfgang , OSTROZHENKOVA, Elena , WINER, Hila
IPC分类号： A61K31/4747
CPC分类号： A61K31/438 , A61K31/4747 , A61K31/7048 , A61K33/24 , A61K36/62 , A61K2300/00
摘要： The current invention provides therapeutic methods which include inhibition of nuclear factor κb pathway in a cell based on the discovery of an active fraction of a plant extract termed NUP or a composition which includes NUP. NUP is used in treating and managing different diseases such as cancer, inflammation, and virus infections.
摘要翻译：本发明提供了治疗方法，其包括基于发现名为NUP的植物提取物的活性部分或包含NUP的组合物来抑制细胞中的核因子κb途径。 NUP用于治疗和管理不同的疾病，如癌症，炎症和病毒感染。

7. 发明申请

WO2010133663A1 SEROTONIN 5-HT3 RECEPTOR ANTAGONISTS FOR USE IN THE TREATMENT OF LESIONAL VESTIBULAR DISORDERS 审中-公开
标题翻译：用于治疗淋巴结病变的SEROTONIN 5-HT3受体拮抗剂
公开(公告)号：WO2010133663A1
公开(公告)日：2010-11-25
申请号：PCT/EP2010/056953
申请日：2010-05-20
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , CHABBERT, Christian , VENAIL, Frédéric
发明人： CHABBERT, Christian , VENAIL, Frédéric
IPC分类号： A61K31/4178 , A61P1/08 , A61K31/00 , A61K31/4184 , A61K31/437 , A61K31/439 , A61K31/46 , A61K31/4747 , A61K31/496 , A61K31/538 , A61K31/7088 , A61K38/00 , A61K39/395 , A61K48/00
CPC分类号： A61K31/4178 , A61K31/4184 , A61K31/437 , A61K31/439 , A61K31/46 , A61K31/4747 , A61K31/496 , A61K31/538 , A61K31/7088
摘要： The invention relates to serotonin 5-HT3 receptor antagonists or inhibitors of serotonin 5-HT3 receptor gene expression for use in the treatment of a lesional vestibular disorder.
摘要翻译：本发明涉及5-羟色胺5-HT 3受体拮抗剂或5-羟色胺5-HT 3受体基因表达抑制剂，用于治疗损伤性前庭疾病。

8. 发明申请

WO2010117800A2 SHH REGULATION AND METHODS THEREOF 审中-公开
标题翻译： SHH法规及其方法
公开(公告)号：WO2010117800A2
公开(公告)日：2010-10-14
申请号：PCT/US2010/029229
申请日：2010-03-30
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , KOTTMANN, Andreas, Hugo
发明人： KOTTMANN, Andreas, Hugo
IPC分类号： A61K31/4747
CPC分类号： A61K31/4747
摘要： The invention provides for methods of upregulating endogenous GDNF by inhibiting Shh signaling. The invention further provides a method for increasing the production of cholinergic neurons and dopamine neurons by subventricular zone (SVZ) neurogenesis in a subject. The invention further provides methods for treating a neurodegenerative disorder in a subject.
摘要翻译：本发明提供通过抑制Shh信号上调内源性GDNF的方法。本发明还提供了通过受试者的室下区（SVZ）神经发生来增加胆碱能神经元和多巴胺神经元的产生的方法。本发明还提供了治疗受试者中的神经变性疾病的方法。

9. 发明申请

WO2009120277A1 USE AND COMPOSITION FOR TREATING DEMENTIA 审中-公开
标题翻译：用于治疗DEMENTIA的使用和组合
公开(公告)号：WO2009120277A1
公开(公告)日：2009-10-01
申请号：PCT/US2009/001662
申请日：2009-03-17
申请人： CHASE PHARMACEUTICALS CORPORATION , CHASE, Thomas, N. , CLARENCE-SMITH, Kathleen, E.
发明人： CHASE, Thomas, N. , CLARENCE-SMITH, Kathleen, E.
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/46 , A61K31/27 , A61K31/325 , A61K31/445 , A61K31/473 , A61K31/4747 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-selective, peripheral anticholinergic agent (nsPAChA) for the preparation of a pharmaceutical composition for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia and pharmaceutical compositions comprising a non-selective peripheral anticholinergic agent of formula II as illustrated in the description and an acetylcholine esterase inhibitor are also described.
摘要翻译：描述了通过与非选择性组合施用所述AChEI降低伴随的副作用来增加最大耐受剂量以及因此乙酰胆碱酯酶抑制剂（AChEI）在患有阿尔茨海默型痴呆症的患者中的功效的方法的外周抗胆碱能药物，由此实现所述患者的CNS中乙酰胆碱酯酶增强的抑制，从而在所述患者体内减轻阿尔茨海默氏型痴呆的症状得到更大程度的改善。使用非选择性的外周抗胆碱能药物（nsPAChA）来制备药物组合物，用于增加患有阿尔茨海默型痴呆的患者中乙酰胆碱酯酶抑制剂（AChEI）的最大耐受剂量和功效，还描述了包含如说明书中所述的式II的非选择性外周抗胆碱能药物和乙酰胆碱酯酶抑制剂的药物组合物。

10. 发明申请

WO2006101954A3 INTERSTITIAL CYSTITIS TREATMENT 审中-公开
标题翻译：间歇性CYCTITIS治疗
公开(公告)号：WO2006101954A3
公开(公告)日：2007-01-11
申请号：PCT/US2006009459
申请日：2006-03-16
申请人： INDEVUS PHARMACEUTICALS INC , SANDAGE BOBBY W JR , COOPER GLENN L
发明人： SANDAGE BOBBY W JR , COOPER GLENN L
IPC分类号： A61K31/045 , A61K31/131
CPC分类号： A61K31/4747
摘要： An anti-muscarinic agent exemplified by trospium is administered by intravesicular instillation into the bladder and used to treat interstitial cystitis. The instilled medication does not interact systemically with the patient; the localized effect of the medication avoids any question of systemic side effects or untoward reactions with body organs or systems.
摘要翻译：通过脉管内滴注给予膀胱中的以毒蛾为例的抗毒蕈碱药，并用于治疗间质性膀胱炎。滴注的药物不会与患者系统地相互作用; 药物的局部效应避免了与身体器官或系统的全身副作用或不良反应的任何问题。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式