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21. 发明申请

US20150150849A1 CANCER TARGETING USING CARBONIC ANHYDRASE ISOFORM IX INHIBITORS 审中-公开
标题翻译：使用碳氢化合物ISOFORM IX抑制剂进行癌症定位
公开(公告)号：US20150150849A1
公开(公告)日：2015-06-04
申请号：US14613881
申请日：2015-02-04
申请人： Claudiu Supuran , STICHTING MAASTRICHT RADIATION ONCOLOGY "MAASTRO- CLINIC" , UNIVERSITÉ MONTPELLIER 2 Sciences et Techniques
发明人： Philippe Lambin , Jean-Yves Winum , Claudiu Supuran
IPC分类号： A61K31/4164 , A61K31/635
CPC分类号： A61K31/4164 , A61K31/635 , C07D233/88 , C07D233/91 , C07D233/95
摘要： The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1), wherein R1, R2, and Z are as defined herein:
摘要翻译：本发明涉及包含硝基咪唑部分的新型碳酸酐酶IX抑制剂及其在治疗缺氧条件，特别是癌症治疗，特别是化疗和放疗中的用途。与本领域相比，本发明的化合物对碳酸酐酶IX酶的特异性增加。本发明涉及由式（1）表示的新型硝基咪唑衍生物，其中R1，R2和Z如本文所定义：

22. 发明授权

US08999989B2 Benzene or thiophene derivative and use thereof as VAP-1 inhibitor 有权
标题翻译：苯或噻吩衍生物及其作为VAP-1抑制剂的用途
公开(公告)号：US08999989B2
公开(公告)日：2015-04-07
申请号：US12991035
申请日：2009-05-29
申请人： Tatsuya Matsukawa , Kazuhiro Masuzaki , Akiko Kawasaki , Akiko Akasaka , Yosuke Kawai
发明人： Tatsuya Matsukawa , Kazuhiro Masuzaki , Akiko Kawasaki , Akiko Akasaka , Yosuke Kawai
IPC分类号： A61K31/496 , C07D241/04 , C07D213/74 , C07C243/32 , C07C243/34 , C07C281/02 , C07C281/06 , C07D233/88 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/24 , C07D265/36 , C07D333/36 , C07D401/04 , C07D409/06 , C07D417/04 , C07D487/08
CPC分类号： A61K31/381 , A61K31/4025 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/497 , A61K31/505 , A61K31/506 , C07C243/32 , C07C243/34 , C07C281/02 , C07C281/06 , C07D213/72 , C07D213/74 , C07D213/75 , C07D233/64 , C07D233/88 , C07D237/20 , C07D239/42 , C07D241/20 , C07D241/24 , C07D265/36 , C07D333/10 , C07D333/36 , C07D401/04 , C07D409/06 , C07D417/04 , C07D487/08
摘要： The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供可用作VAP-1抑制剂的新型苯衍生物或噻吩衍生物，或用于预防或治疗VAP-1相关疾病等的药物，即由式（I）表示的化合物：其中每个符号如本说明书中所定义，或其药学上可接受的盐。

23. 发明申请

US20150025094A1 COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE 有权
标题翻译：用于补充葡萄糖的化合物和组合物
公开(公告)号：US20150025094A1
公开(公告)日：2015-01-22
申请号：US14236224
申请日：2012-08-01
申请人： Shlomo Sasson , Erol Cerasi , Arie Lev Gruzman , Ella Meltzer-Mats
发明人： Shlomo Sasson , Erol Cerasi , Arie Lev Gruzman , Ella Meltzer-Mats
IPC分类号： C07D471/04 , C07D285/135 , C07D233/88 , C07D277/54 , C07D249/12 , C07D239/38 , C07D277/82
CPC分类号： C07D471/04 , C07D233/88 , C07D235/28 , C07D239/38 , C07D249/12 , C07D277/54 , C07D277/74 , C07D277/78 , C07D277/82 , C07D285/135 , C07D311/58 , C07D339/02 , C07D339/08 , C07D417/12
摘要： The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related disorders.
摘要翻译：本发明涉及以下化合物：其中连接体独立地选自-S-，-S-S-，-S-（CH 2）n - ， - NH - ， - NH（CH 2）正，-O - ， - SO 2 - ，亚芳基，亚杂芳基; R 1选自直链或支链C 4 -C 20烷基，直链或支链C 4 -C 20烯基，直链或支链C 4 -C 20炔基，每个任选被至少一个NH，C 5 -C 7饱和环烷基或杂烷基环中断， C 5 -C 12芳族或杂芳环，各自任选被至少一个选自-COOH，-NH 2，C 1 -C 8烷氧基，C 1 -C 5脒基，C 1 -C 5羧基，卤素基团取代; R 2独立地选自H，OH，SH，NH 2，NO 2，卤素，CN，C 1 -C 8烷氧基，C 1 -C 5羧酸，直链或支链C 1 -C 8烷基，直链或支链C 2 -C 10烯基各自任选被至少一个选自C 1 -C 5烷氧基，C 1 -C 5羧酸，OH，SH，NH 2，卤素的取代基取代的直链或支链C 2 -C 12炔基; 和用于治疗糖尿病和相关疾病的组合物。

24. 发明申请

US20140371283A1 HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING 审中-公开
标题翻译：调制面媒介应用程序处理的HYDANTOINS
公开(公告)号：US20140371283A1
公开(公告)日：2014-12-18
申请号：US14179310
申请日：2014-02-12
申请人： Buck Institute for Research on Aging
发明人： VARGHESE JOHN , Dale E. BREDESEN
IPC分类号： C07D233/88 , C07D233/76
CPC分类号： C07D233/76 , A61K31/4166 , A61K31/4168 , A61K31/4439 , A61K31/46 , A61K31/506 , A61K45/06 , C07D233/70 , C07D233/88 , C07D401/04 , C07D401/10 , C07D403/10 , A61K2300/00
摘要： In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
摘要翻译：在某些实施方案中，本文提供了有效抑制针对APP的BACE活性的乙内酰脲化合物。不受特定理论的约束，据信本文鉴定的乙内酰脲的活性似乎与结合BACE和/或APP有关，特别是当这些部分形成BACE / APP复合物时。因此，据信本文所述的化合物代表本文中称为APP-结合-BACE抑制剂（ABBI）的新一类化合物，并提供调节APP处理的新机制。本文所述的乙内酰脲似乎显示改善的脑渗透性和功能性BACE抑制。

25. 发明授权

US08906915B2 Compounds, compositions, and methods for controlling biofilms 有权
标题翻译：用于控制生物膜的化合物，组合物和方法
公开(公告)号：US08906915B2
公开(公告)日：2014-12-09
申请号：US13526235
申请日：2012-06-18
申请人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
发明人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
IPC分类号： A61K31/535 , C07D487/04 , C07D405/12 , C07D233/88 , C07D409/04
CPC分类号： C07D233/88 , C07D405/12 , C07D409/04 , C07D487/04
摘要： The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
摘要翻译：本发明涉及取代的2-氨基咪唑及其对生物膜形成有活性的咪唑并[1,2-a]嘧啶鎓盐前体。本发明还涉及带有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐以及取代的2-氨基咪唑，其中氨基具有通过叠氮基炔代Huisgen环加成反应形成的末端杂环基，例如三唑基由具有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐制得。本发明还涉及可用作合成具有叠氮基烷基取代基的所述咪唑并[1,2-a]嘧啶鎓盐的起始原料的一类N-（叠氮基烷基）嘧啶-2-胺。本发明还涉及抗微生物组合物，其包括微生物生物膜形成抑制量的这种取代的2-氨基咪唑或咪唑并[1,2-a]嘧啶鎓盐与赋形剂的组合。还公开了抑制或控制植物，人或动物的身体部位或人或动物可能接触的表面的微生物生物膜形成的方法。

26. 发明授权

US08778980B2 Heterocyclic aspartyl protease inhibitors 有权
公开(公告)号：US08778980B2
公开(公告)日：2014-07-15
申请号：US13551315
申请日：2012-07-17
申请人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A01N43/82 , A61K31/41 , C07D271/06
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

27. 发明授权

US08759344B2 Imidazopyridine derivatives, process for preparation thereof and therapeutic use thereof 有权
标题翻译：咪唑并吡啶衍生物，其制备方法及其治疗用途
公开(公告)号：US08759344B2
公开(公告)日：2014-06-24
申请号：US13808503
申请日：2011-07-04
申请人： Chantal Alcouffe , Reinhard Kirsch , Corentin Herbert , Gilbert Lassalle
发明人： Chantal Alcouffe , Reinhard Kirsch , Corentin Herbert , Gilbert Lassalle
IPC分类号： A61K31/53 , C07D401/00 , C07D413/00 , A61K31/517 , A61K9/20 , C07D211/82 , C07D471/04 , C07D233/88 , C07D211/90 , C07D233/64 , A61K45/06 , A61K31/5377 , C07D233/90
CPC分类号： A61K31/517 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/437 , A61K31/5377 , A61K45/06 , C07D211/82 , C07D211/90 , C07D233/64 , C07D233/88 , C07D233/90 , C07D471/04
摘要： The invention relates to compounds corresponding to formula (I): in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.
摘要翻译：本发明涉及对应于式（I）的化合物：其中R 2和R 3一起与它们所连接的苯基的碳原子一起形成对应于式（A），（A）中的一个的6-元含氮杂环， B）或（C）：其中波浪线表示R2和R3所连接的苯基核。制备过程和治疗用途。

28. 发明申请

US20140094436A1 IMIDAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
标题翻译：调节HSP90活性的咪唑化合物
公开(公告)号：US20140094436A1
公开(公告)日：2014-04-03
申请号：US14103420
申请日：2013-12-11
申请人： Weiwen Ying , Zhenjian Du , Kevin Foley
发明人： Weiwen Ying , Zhenjian Du , Kevin Foley
IPC分类号： C07D233/84 , C07F9/6506 , C07D233/88 , C07D403/10
CPC分类号： A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/428 , A61K31/4709 , A61K31/52 , A61K31/5377 , A61K31/675 , C07D233/70 , C07D233/84 , C07D233/88 , C07D403/02 , C07D403/04 , C07D403/10 , C07F9/6506
摘要： Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
摘要翻译：式（I）化合物，包含式（I）化合物的药物组合物和抑制细胞中Hsp90的方法，治疗或预防哺乳动物中的增殖病症并治疗哺乳动物的癌症，其包括给予式（I）化合物至患者或细胞。变量R5是任选取代的杂芳基; 任选取代的6至14元芳基; 任选在任何可取代的氮或碳原子上取代的双环9元杂环; 或本文定义的取代基R18。环A是除了R3之外任选进一步被一个或多个取代基取代的芳基或杂芳基。取代基R 3在本文中定义。

29. 发明申请

US20140080825A1 Modulators of ATP-binding cassette transporters 有权
公开(公告)号：US20140080825A1
公开(公告)日：2014-03-20
申请号：US13972151
申请日：2013-08-21
申请人： Vertex Pharmaceuticals Incorporated
发明人： Sara Sabina Hadida-Ruah , Peter Diederik Jan Grootenhuis , Mark Thomas Miller , Matthew Hamilton
IPC分类号： C07D417/12 , C07D417/06 , C07D413/12
CPC分类号： C07D417/12 , C07D231/40 , C07D233/88 , C07D263/48 , C07D271/113 , C07D277/46 , C07D277/54 , C07D277/82 , C07D285/135 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/14 , C07D493/10
摘要： The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

30. 发明授权

US08653124B2 Inhibition of bacterial biofilms with imidazole derivatives 有权
标题翻译：用咪唑衍生物抑制细菌生物膜
公开(公告)号：US08653124B2
公开(公告)日：2014-02-18
申请号：US13019450
申请日：2011-02-02
申请人： Christian Melander , John Cavanagh , Robert W. Huigens, III , T. Eric Ballard , Justin J. Richards
发明人： Christian Melander , John Cavanagh , Robert W. Huigens, III , T. Eric Ballard , Justin J. Richards
IPC分类号： C07D233/64 , A61K31/4168
CPC分类号： A01N43/52 , A01N43/50 , A61K8/4946 , A61L27/54 , A61L29/16 , A61L31/16 , A61L2300/204 , A61L2300/404 , A61Q11/00 , A61Q17/005 , C07D233/88 , C07D235/30 , C07D401/14 , C07D403/12
摘要： Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
摘要翻译：提供了用于预防，去除和/或抑制生物膜形成的咪唑衍生物化合物的公开，包含这些化合物的组合物，包含这些化合物的装置及其使用方法。

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