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1. 发明申请

US20180127368A1 TRICYCLIC SULFONES AS ROR GAMMA MODULATORS 审中-公开
公开(公告)号：US20180127368A1
公开(公告)日：2018-05-10
申请号：US15806554
申请日：2017-11-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： David Marcoux , Myra Beaudoin Bertrand , T.G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G Batt
IPC分类号： C07D211/48 , C07D213/40 , C07D295/195 , C07D213/75 , C07D333/48 , C07C317/44 , C07D335/02 , C07D471/04 , C07D307/22 , C07D241/08 , C07D207/10 , C07D207/16 , C07D231/08 , C07D309/10 , C07D211/96 , C07D471/10 , C07D205/04 , C07D207/277 , C07D257/04 , C07D205/08 , A61P37/00
CPC分类号： C07D211/48 , A61P37/00 , C07B2200/05 , C07B2200/07 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/38 , C07C2602/44 , C07C2602/50 , C07C2603/08 , C07C2603/12 , C07C2603/16 , C07C2603/90 , C07D205/04 , C07D205/08 , C07D207/09 , C07D207/10 , C07D207/16 , C07D207/277 , C07D207/28 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/08 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/18 , C07D263/20 , C07D285/06 , C07D295/16 , C07D295/195 , C07D305/08 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D471/04 , C07D471/10 , C07F9/091
摘要： There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

2. 发明授权

US09862680B2 Peripherally substituted monocyclic beta-lactams 有权
公开(公告)号：US09862680B2
公开(公告)日：2018-01-09
申请号：US15181303
申请日：2016-06-13
申请人： University of Notre Dame du Lac
发明人： Marvin Miller , Serena Carosso
IPC分类号： C07D205/08 , A61K31/397 , C07D417/12
CPC分类号： C07D205/08 , C07D417/12
摘要： The invention provides monobactams that can be used as antibacterial agents or intermediates for the preparation of other useful compounds such as antibacterial agents.

3. 发明授权

US09850277B2 Therapeutically active compositions and their methods of use 有权
公开(公告)号：US09850277B2
公开(公告)日：2017-12-26
申请号：US15279146
申请日：2016-09-28
申请人： AGIOS PHARMACEUTICALS, INC
发明人： Janeta Popovici-Muller , Rene M. Lemieux , Jeremy Travins , Zhenwei Cai , Dawei Cui , Ding Zhou
IPC分类号： C07D207/26 , C07D401/04 , C07D403/04 , C07K5/065 , C07D205/08 , A61K38/05 , A61K45/06 , C07D401/14 , C07D413/04 , C07D417/04 , A61K38/00 , C07K5/06
CPC分类号： C07K5/06078 , A61K38/005 , A61K38/05 , A61K45/06 , C07D205/08 , C07D207/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D417/04 , C07K5/06191
摘要： Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

4. 发明申请

US20170355671A1 PERIPHERALLY SUBSTITUTED MONOCYCLIC BETA-LACTAMS 有权
公开(公告)号：US20170355671A1
公开(公告)日：2017-12-14
申请号：US15181303
申请日：2016-06-13
申请人： University of Notre Dame du Lac
发明人： Marvin Miller , Serena Carosso
IPC分类号： C07D205/08 , C07D417/12
CPC分类号： C07D205/08 , C07D417/12
摘要： The invention provides monobactams that can be used as antibacterial agents or intermediates for the preparation of other useful compounds such as antibacterial agents.

5. 发明申请

US20160257688A1 Process for Synthesis of Lactams 审中-公开
标题翻译：内酰胺合成方法
公开(公告)号：US20160257688A1
公开(公告)日：2016-09-08
申请号：US15031326
申请日：2014-10-22
申请人： Francis Xavier TAVARES
发明人： Francis Xavier Tavares
IPC分类号： C07D487/04 , C07D487/10
CPC分类号： C07D487/04 , C07D201/08 , C07D205/08 , C07D207/24 , C07D487/10
摘要： Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC—OR—NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam such as that of the formula (a), provided herein, wherein G represents the atom(s) needed to form a closed ring.
摘要翻译：提出了合成内酰胺的方法，其中式HOOC-OR-NH-LG的羧酸（其中OR为有机部分，LG为离去基团）与酸例如有机酸反应强酸和脱水剂，其可以是相同的酸，例如强酸酐，使得添加的酸的量允许进行所需的转化而不会在离开基团（LG）之前损失，环化和回收如本文所提供的式（a）的内酰胺，其中G表示形成封闭环所需的原子。

6. 发明授权

US09434740B2 Taxane compounds, compositions and methods 有权
标题翻译：紫杉烷化合物，组合物和方法
公开(公告)号：US09434740B2
公开(公告)日：2016-09-06
申请号：US14325960
申请日：2014-07-08
申请人： GFV, LLC
发明人： John K. Thottathil , Raymond P. Warrell
IPC分类号： C07D493/08 , C07D205/08 , C07D305/14 , C07D407/02 , C07D401/04
CPC分类号： C07D493/08 , C07D205/08 , C07D305/14 , C07D401/04 , C07D407/02
摘要： The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
摘要翻译：本发明提供了一种制备口服可用的五环紫杉烷化合物的方法，以及可用于其制备的中间体。

7. 发明申请

US20150225389A1 THERAPEUTIC COMPOUNDS AND COMPOSITIONS 有权
标题翻译：治疗化合物和组合物
公开(公告)号：US20150225389A1
公开(公告)日：2015-08-13
申请号：US14614169
申请日：2015-02-04
申请人： eXIthera Pharmaceuticals Inc.
发明人： Robert A. Chrusciel , Robert C. Gadwood , Neil J. Hayward , Michael J. Melnick , Manuel A. Navia , Toni J. Poel , Frans L. Stassen , Catherine A. Stewart
IPC分类号： C07D417/06 , C07D405/14 , C07D401/06
CPC分类号： C07D205/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/06 , C07D417/06 , C07D417/14
摘要： The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.
摘要翻译：本发明提供抑制因子XIa或激肽释放酶的化合物和组合物以及使用这些化合物和组合物的方法。

8. 发明授权

US09010853B2 Securing element, particularly suitable for use with tablet-arm chairs 有权
标题翻译：固定元件，特别适用于平板扶手椅
公开(公告)号：US09010853B2
公开(公告)日：2015-04-21
申请号：US13880750
申请日：2011-10-19
申请人： Alberto Lievore Motta
发明人： Alberto Lievore Motta
IPC分类号： A47C7/70 , C07D205/08 , C07D263/20 , A47B83/02
CPC分类号： A47C7/70 , A47B83/02 , C07D205/08 , C07D263/20
摘要： The invention can be used to secure writing tablets to different types of chairs with legs of different thicknesses and diameters, such that writing tablets can be installed on simple chairs with no armrests. The invention is essentially characterized in that it comprises: a main part having two through-holes therein, namely a first hole for receiving and housing the tubular support of the writing tablet and a second hole dimensioned to be coupled to one of the legs of the chair, and a vertical rod; and a pivoting part connected to the main part by means of the rod, aligned with the second hole and adapted to open and close such that the securing element can be released from the leg of the chair.
摘要翻译：本发明可用于将书写片固定到具有不同厚度和直径的腿的不同类型的椅子上，使得书写片剂可以安装在没有扶手的简单椅子上。本发明的特征在于其包括：主要部分，其中具有两个通孔，即用于接收和容纳书写片剂的管状支撑件的第一孔和第二孔，该第二孔的尺寸适于与椅子和垂直杆; 以及通过所述杆与所述杆部连接的枢转部件，所述枢转部件与所述第二孔对准并且适于打开和关闭，使得所述固定元件能够从所述椅子的腿部释放。

9. 发明授权

US08816079B2 Amide derivative and use thereof as medicine 有权
标题翻译：酰胺衍生物及其用作药物
公开(公告)号：US08816079B2
公开(公告)日：2014-08-26
申请号：US13643790
申请日：2011-04-27
申请人： Kazuhiro Maeda , Jun-ichi Endoh , Akiko Tarao , Kaoru Tashiro , Seigo Ishibuchi , Hidemasa Hikawa
发明人： Kazuhiro Maeda , Jun-ichi Endoh , Akiko Tarao , Kaoru Tashiro , Seigo Ishibuchi , Hidemasa Hikawa
IPC分类号： C07D251/00 , C07D253/00 , C07D241/02 , C07D403/00 , C07D413/00 , C07D211/68 , C07D401/00 , A61K31/55 , A61K31/497 , A61K31/445 , A61K31/41
CPC分类号： C07D205/08 , A61K31/437 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , C07D207/273 , C07D207/277 , C07D209/54 , C07D211/32 , C07D211/76 , C07D213/74 , C07D275/02 , C07D295/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08
摘要： Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
摘要翻译：提供了抑制诱导型MMP（特别是MMP-9）的生产的新型低分子量化合物，而不是止血型MMP-2的产生，以及用于自身免疫性疾病或骨关节炎的预防/治疗药物。由下式（I）表示的酰胺衍生物，其中每个符号如说明书中所定义，或其药理学上可接受的盐。

10. 发明授权

US08420628B2 Substituted beta-lactams 有权
标题翻译：取代的β-内酰胺
公开(公告)号：US08420628B2
公开(公告)日：2013-04-16
申请号：US10599619
申请日：2006-05-02
申请人： David W. Old
发明人： David W. Old
IPC分类号： C07D205/08 , C07D409/06 , A61K31/397 , A61P27/06 , C07D407/06 , C07D401/06 , A61P1/00
CPC分类号： C07D205/08 , A61K31/397
摘要： Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug or a metabolite thereof; wherein Y is an organic acid functional group, or an amide or ester thereof comprising up to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising up to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH═CH—(CH2)3—, or —CH2C≡C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be substituted with S or O; and D is aryl or heteroaryl.
摘要翻译：本文公开了包含其药学上可接受的盐或其前药或代谢物的化合物; 其中Y为有机酸官能团，或其中含有最多12个碳原子的酰胺或酯; 或Y是含有至多12个碳原子的羟甲基或其醚; 或Y为四唑基官能团; A是 - （CH2）6-，顺式-CH2CH = CH-（CH2）3-或-CH2C≡C-（CH2）3-，其中1或2个碳原子可以被S或O取代; 或A是 - （CH 2）m -Ar-（CH 2）o-，其中Ar是亚芳基或杂亚环烷基，m和o之和为1至4，并且其中一个CH 2可以被S或O取代; D是芳基或杂芳基。

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