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1. 发明授权

US10590117B2 Spring retaining pin for valve stem retention 有权
公开(公告)号：US10590117B2
公开(公告)日：2020-03-17
申请号：US15320970
申请日：2015-06-26
申请人： HUSKY INJECTION MOLDING SYSTEMS LTD.
发明人： Douglas Oliver Hall , Patrice Fabien Dezon-Gaillard , Manon Danielle Belzile , Edward Joseph Jenko , John Knapp
IPC分类号： C07D413/04 , C07D213/62 , C07D213/78 , C07D213/81 , B29C45/28
摘要： An apparatus and method of coupling and decoupling a valve stem to an actuator are disclosed. In one embodiment, the actuator includes a moveable member that is coupled to the valve stem. One of the valve stem and the moveable member is a male coupling portion and the other of the valve stem and moveable member is the female coupling portion. The male coupling portion is nested within the female coupling portion. A retaining pin retains the male coupling portion with respect to the female coupling portion.

2. 发明授权

US09409865B2 Modulators of methyl modifying enzymes, compositions and uses thereof 有权
公开(公告)号：US09409865B2
公开(公告)日：2016-08-09
申请号：US14707874
申请日：2015-05-08
申请人： Constellation Pharmaceuticals, Inc.
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Gagnon , Jean-Christophe Harmange , Christopher G. Nasveschuk
IPC分类号： C07D213/62 , C07D213/64 , C07D213/81 , C07D405/12 , C07D401/12
CPC分类号： C07D213/64 , C07D213/81 , C07D401/12 , C07D405/12
摘要： Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

3. 发明授权

US09346794B1 Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity 有权
公开(公告)号：US09346794B1
公开(公告)日：2016-05-24
申请号：US14981999
申请日：2015-12-29
申请人： Boehringer Ingelheim International GmbH
发明人： Thorsten Oost , Dennis Fiegen , Christian Gnamm
IPC分类号： A61K31/54 , A61K31/50 , A61K31/501 , A61K38/00 , A61P11/06 , A61P17/00 , A61P29/00 , C07D215/00 , C07D213/62 , C07D417/04 , C07D213/82 , C07D401/04 , C07D413/04 , C07D405/04
CPC分类号： C07D417/04 , C07D213/82 , C07D401/04 , C07D405/04 , C07D413/04
摘要： This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.

4. 发明授权

US09073855B2 BCL-2 selective apoptosis-inducing agents for the treatment of cancer and immune diseases 有权
标题翻译： BCL-2选择性细胞凋亡诱导剂用于治疗癌症和免疫疾病
公开(公告)号：US09073855B2
公开(公告)日：2015-07-07
申请号：US13839060
申请日：2013-03-15
申请人： AbbVie Inc.
发明人： George A. Doherty , Steven W. Elmore , Lisa Hasvold , Laura Hexamer , Robert A. Mantei , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Gary T. Wang , Le Wang , Xilu Wang , Michael D. Wendt , Todd M. Hansen
IPC分类号： C07D401/10 , C07D213/62 , C07D307/02 , C07D215/14 , C07D209/32 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D231/56 , C07D235/26 , C07D249/04 , C07D295/125 , C07D295/14 , C07D309/14 , C07D401/12 , C07D405/12 , C07D417/12 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D295/13 , C07D309/08 , C07D487/04 , C07D209/20 , C07D295/155 , C07D309/32
CPC分类号： C07D215/14 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D209/20 , C07D209/32 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D231/56 , C07D235/26 , C07D249/04 , C07D295/125 , C07D295/13 , C07D295/14 , C07D295/155 , C07D309/08 , C07D309/14 , C07D309/32 , C07D401/12 , C07D405/12 , C07D417/12 , C07D487/04
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
摘要翻译：公开了抑制抗凋亡Bcl-2或Bcl-xL蛋白的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达抗凋亡Bcl-2蛋白。

5. 发明授权

US09072796B2 Method for preparing deuterated diphenylurea 有权
标题翻译：氘化二苯脲的制备方法
公开(公告)号：US09072796B2
公开(公告)日：2015-07-07
申请号：US14092253
申请日：2013-11-27
申请人： SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.
发明人： Weidong Feng , Xiaoyong Gao , Xiaojun Dai
IPC分类号： C07D213/62 , A61K51/04 , C07D213/81 , C07C209/24 , C07D209/48 , C07D213/68 , C07B59/00
CPC分类号： A61K51/0455 , C07B59/002 , C07C209/24 , C07D209/48 , C07D213/68 , C07D213/81
摘要： Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.
摘要翻译：公开了N-（1,1,1-三氘代甲基）邻苯二甲酰亚胺的中间体化合物及其在制备氘代二苯基脲衍生物中的用途。

6. 发明授权

US08829003B2 Compounds for treating proliferative disorders 有权
公开(公告)号：US08829003B2
公开(公告)日：2014-09-09
申请号：US13806602
申请日：2011-06-21
申请人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
发明人： Shudong Wang , Osama Chahrour , Tiangong Lu , Anran Hu
IPC分类号： A61K31/497 , C07D213/62
CPC分类号： C07D213/74 , C07D213/73 , C07D213/75 , C07D213/76 , C07D239/47 , C07D401/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilizing or immobilizable derivative thereof; wherein: any one or two of X., X2 and X3 is a N atom and the remaining two or one of X1, X2 and X3 are independently CR13; Y is selected from SO2 and SO; R1, R2, R3, and R7 and the one or two R13 groups are each independently selected from H and R10, R10 is selected from R8, alkyl, aryl, heteroaryl and combinations of two or more thereof and combinations with one or more R9, or R10 is one or more moieties R11 Sinking one or more alkyl, alkoxy, aryl, heteroaryl or R8 or R9 groups or combinations thereof, directly or via a moiety selected from alkylene, arylene, heteroarylene or combinations thereof, wherein alkyl, aryl, heteroaryl groups or moieties thereof may be substituted with one or more groups R12, or R10 is selected from a group R12; R11 is selected from 0-, N—, NH—, N═C, CO—, C00-, CON—, CONH—, S02-, S02N—, S02NH—; R12 is selected from halogen, NH2, N02, CN, OH, COOH, CONH2, C(═NH)NH2, S03H, S02NH2, S02CH3, OCH3, OCH2CH3, CF3; R8 and R9 comprise one or more solubilizing moieties independently chosen from i) neutral hydrophilic groups, ii) ionisable organic acids, iii) ionisable organic bases, iv} chemical functions or moieties providing covalent or non-covalent attachment or binding to a solid phase or an immobile receptor and combinations thereof; R4, R5 and R6 are each independently selected from H and R10, or two of R4 to R6 are linked to form a cyclic ether or amine containing one or more additional oxygen or nitrogen atoms. The compound may be used for treating a condition mediated by one or more enzymes selected from AKT, Aurora kinase, BCR-ABL, CDK, FLT, GSK3, IKK, JAK, MAPK, PDGF, PI3K, PKA, PKB, PKC, PLK, Src and VEGF family enzymes, or for treating cancer or other proliferative disorder, or for inhibiting growth of cancer cells, or for inducing apoptosis of cancer cells, in a human or animal subject.

7. 发明授权

US08791147B2 Calcium receptor modulating agents 有权
标题翻译：钙受体调节剂
公开(公告)号：US08791147B2
公开(公告)日：2014-07-29
申请号：US13123468
申请日：2009-10-07
申请人： Christopher Fotsch , Paul Harrington
发明人： Christopher Fotsch , Paul Harrington
IPC分类号： A61K31/44 , C07D211/72 , C07D211/84 , C07D213/62 , C07D213/78 , C07D211/70 , C07D211/82 , C07D213/24
CPC分类号： A61K31/44 , A61K31/437 , A61K31/4412
摘要： The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.
摘要翻译：本发明一般涉及新型的拟钙化合物和包含它们的药物组合物。本发明还涉及使用式（I）表示的化合物治疗与钙感受受体的功能有关的疾病或病症的方法。其中Cy1是吡啶基，吡啶基，喹啉基或9-乙基-9H-咔啉基，其各自任选被取代，Cy2是苯基萘基。

8. 发明授权

US08748462B2 Spirocyclic GPR40 modulators 有权
标题翻译：螺环GPR40调节剂
公开(公告)号：US08748462B2
公开(公告)日：2014-06-10
申请号：US13119951
申请日：2009-10-13
申请人： Sean P. Brown , Paul Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , XianYun Jiao , Sujen Lai , An-Rong Li , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang , Ming Yu , Liusheng Zhu
发明人： Sean P. Brown , Paul Dransfield , Xiaohui Du , Zice Fu , Jonathan Houze , XianYun Jiao , Sujen Lai , An-Rong Li , Jiwen Liu , Zhihua Ma , Julio C. Medina , Vatee Pattaropong , Wang Shen , Marc Vimolratana , Yingcai Wang , Zhongyu Wang , Ming Yu , Liusheng Zhu
IPC分类号： A61K31/19 , C07C69/76 , C07D211/72 , C07D211/84 , C07D213/62 , A61K31/44
CPC分类号： C07C62/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/643 , C07D217/24 , C07D253/065 , C07D277/22 , C07D311/04 , C07D401/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I′A or I′B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式IA，IB，I'A或I'B：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

9. 发明授权

US08501757B2 Substituted phenylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same 失效
标题翻译：取代的苯胺甲酰胺类似物作为mGluR5负变构调节剂及其制备和使用方法
公开(公告)号：US08501757B2
公开(公告)日：2013-08-06
申请号：US12885420
申请日：2010-09-17
申请人： P. Jeffrey Conn , Craig W. Lindsley , Kyle A. Emmitte , Charles David Weaver , Alice L. Rodriguez , Andrew S. Felts , Carrie K. Jones , Brittney S. Bates , Brian A. Chauder
发明人： P. Jeffrey Conn , Craig W. Lindsley , Kyle A. Emmitte , Charles David Weaver , Alice L. Rodriguez , Andrew S. Felts , Carrie K. Jones , Brittney S. Bates , Brian A. Chauder
IPC分类号： A61K31/505 , A61K31/44 , C07D239/02 , C07D403/12 , C07D401/12 , C07D213/62 , A61K31/4965
CPC分类号： A61K31/4406 , A61K31/497 , C07D401/12 , C07D401/14
摘要： Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：公开了代谢型谷氨酸受体亚型5（mGluR5）的负变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

10. 发明授权

US08314240B2 Sulfonamide compounds or salts thereof 失效
标题翻译：磺酰胺化合物或其盐
公开(公告)号：US08314240B2
公开(公告)日：2012-11-20
申请号：US13000677
申请日：2009-06-22
申请人： Hideki Kubota , Issei Tsukamoto , Kazunori Kamijo , Koji Kato , Yuta Fukuda , Hidenori Azami
发明人： Hideki Kubota , Issei Tsukamoto , Kazunori Kamijo , Koji Kato , Yuta Fukuda , Hidenori Azami
IPC分类号： A61K31/44 , C07D213/62
CPC分类号： C07C311/21 , A61K31/341 , A61K31/426 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/443 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , C07C2602/08 , C07D213/71 , C07D213/80 , C07D277/20 , C07D277/36 , C07D277/56 , C07D307/64 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： [Object] A compound which is useful as an EP1 receptor antagonist is provided.[Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
摘要翻译：提供了可用作EP1受体拮抗剂的化合物。 [解决方案]本发明人研究了EP1受体拮抗剂，并证实了具有磺酰胺结构的化合物，其中磺酰胺结构的氮原子被2-氟丙基取代，3-氟-2-甲基丙基或具有有效的EP1受体拮抗作用，从而完成本发明。本发明的磺酰胺化合物具有有效的EP1受体拮抗作用，可用作预防和/或治疗下尿路症状等的药剂。

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