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1. 发明公开

US20240067616A1 PEPTIDE CONJUGATES OF MICROTUBULE-TARGETING AGENTS AS THERAPEUTICS 审中-公开
公开(公告)号：US20240067616A1
公开(公告)日：2024-02-29
申请号：US18152987
申请日：2023-01-11
申请人： Cybrexa 3, Inc.
发明人： Daniel Richard Marshall , Johanna Marie Csengery , Robert John Maguire , Robert A. Volkmann
IPC分类号： C07D265/12 , A61K47/64
CPC分类号： C07D265/12 , A61K47/64
摘要： The present invention relates to peptide conjugates of microtubule-targeting agents such as maytansinoid derivatives which are useful for the treatment of diseases such as cancer.

2. 发明授权

US10994019B2 Bicyclic peptide-toxin conjugates specific for MT1-MMP 有权
公开(公告)号：US10994019B2
公开(公告)日：2021-05-04
申请号：US16097305
申请日：2017-05-04
申请人： BicycleRD Limited
发明人： Daniel Teufel , Silvia Pavan , Leonardo Baldassarre
IPC分类号： A61K31/5365 , A61K47/64 , C07D265/04 , C07D265/12 , C07K7/08 , C07K14/00 , A61P35/00
摘要： The present invention relates to drug conjugates comprising bicyclic peptides specific for MT1-MMP conjugated to one or more effector and/or functional groups which have utility in targeted cancer therapy.

3. 发明申请

US20160347725A1 INHIBITORS OF PAXILLIN FUNCTION AND RELATED COMPOSITIONS AND METHODS 有权
标题翻译： PAXILLIN功能抑制剂及相关成分及方法
公开(公告)号：US20160347725A1
公开(公告)日：2016-12-01
申请号：US15116764
申请日：2015-02-04
申请人： Bialal Abou ALEIWI , UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： Charles Ryan Yates , Duane D. Miller , Frank Park , Jordan J. Toutounchian , Vanessa Moraies-Tirado , Shivaputra Patil , Jayaprakash Pagadala , Bial Abou Aleiwi
IPC分类号： C07D265/18 , C07D211/84 , C07D265/12
CPC分类号： C07D265/18 , A61K9/0048 , A61K9/1075 , A61K47/14 , C07D211/84 , C07D215/36 , C07D221/10 , C07D239/82 , C07D265/12 , C07D498/04
摘要： This disclosure relates to small molecule inhibitors of paxillin and paxillin binding, and related compositions and methods of treatment.
摘要翻译：本公开涉及桩蛋白和桩蛋白结合的小分子抑制剂，以及相关组合物和治疗方法。

4. 发明授权

US08801976B2 Photochromic material 有权
标题翻译：光致变色材料
公开(公告)号：US08801976B2
公开(公告)日：2014-08-12
申请号：US13629975
申请日：2012-09-28
申请人： Korea University Research and Business Foundation
发明人： Dong Hoon Choi
IPC分类号： G02B5/23 , C07D265/12 , C07D265/00
CPC分类号： C09B19/00 , C09B57/00 , C09K9/02 , G02B5/23
摘要： Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first wavelength, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second wavelength.
摘要翻译：公开了光致变色染料。光致变色染料可以包括第一光反应性基团和第二光反应性基团。可以通过具有第一波长的辐射在光致变色染料的第一光反应性基团中诱导第一光致变色反应，并且可以通过具有第二波长的辐射在光致变色染料的第二光反应性基团中诱导第二光致变色反应。

5. 发明授权

US08772271B2 Micronized tanaproget, compositions, and methods of preparing the same 失效
标题翻译：微粉化钠盐，组合物及其制备方法
公开(公告)号：US08772271B2
公开(公告)日：2014-07-08
申请号：US13890523
申请日：2013-05-09
申请人： Wyeth LLC
发明人： Arwinder S. Nagi , Ramarao Chatlapalli , Shamim Hasan , Mohamed Ghorab , Dhaval Gaglani
IPC分类号： A61K31/335 , A61K31/56 , C07D295/00 , C07D265/12
CPC分类号： A61K9/16 , A61K9/0002 , A61K9/167 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K31/536
摘要： The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.
摘要翻译：本发明提供了组合物，理想的药物组合物，其含有微粉化的tanaproget。组合物还可以含有微晶纤维素，交联羧甲基纤维素钠，无水乳糖，硬脂酸镁，微粒化的乙二胺四乙酸钙二水合钙和微粉化硫代硫酸钠五水合物。该组合物可用于避孕和激素替代治疗以及治疗和/或预防子宫肌层肌瘤，良性前列腺肥大，良性和恶性肿瘤性疾病，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症，多囊卵巢综合征，以及癌和腺癌垂体，子宫内膜，肾，卵巢，乳腺，结肠，前列腺和其他激素依赖性肿瘤，以及制备有用的药物。额外的用途包括刺激食物摄入。

6. 发明授权

US08420808B2 Process for the preparation of Efavirenz 有权
标题翻译：制备依法韦仑的方法
公开(公告)号：US08420808B2
公开(公告)日：2013-04-16
申请号：US13060839
申请日：2009-01-30
申请人： Alessandro Leganza , Marco Galvagni
发明人： Alessandro Leganza , Marco Galvagni
IPC分类号： C07D265/12
CPC分类号： C07D265/18
摘要： The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.
摘要翻译：本发明涉及制备依法韦仑，（4S）-6-氯-4-（环丙基乙炔基）-4-（三氟甲基）-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的方法，一种式（I）包括使式（II）的中间体作为游离碱或其盐与二光气（TCMCF，氯甲酸三氯甲酯）Cl 3 CO-COCl在有机溶剂中或在包含有机溶剂和水，优选但不强制地在弱碱存在下以足以中和反应混合物的量或高达30％摩尔过量的这种量。

7. 发明申请

US20130072478A1 N-(3-(2-AMINO-6,6-DIFLUORO-4,4A,5,6,7,7A-HEXAHYDRO-CYCLOPENTA[E][1,3]OXAZIN-4-YL)-PHENYL-AMIDES AS BACE1 INHIBITORS 有权
标题翻译： N-（3-（2-氨基 - 6,6-二氟-4,4A，5,6,7,7a-十六氢 - 环戊二烯并[E] [1,3]氧杂-4-基） - 苯甲酰胺 BACE1抑制剂
公开(公告)号：US20130072478A1
公开(公告)日：2013-03-21
申请号：US13609304
申请日：2012-09-11
申请人： Hans Hilpert , Emmanuel Pinard , Thomas Woltering
发明人： Hans Hilpert , Emmanuel Pinard , Thomas Woltering
IPC分类号： C07D413/12 , C07D265/12 , A61P25/28 , A61K31/536
CPC分类号： C07D413/12
摘要： The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
摘要翻译：本发明提供N-（3-（2-氨基-6,6-二氟-4,4a，5,6,7,7a-六氢 - 环戊二烯并[e] [1,3]恶嗪-4-基） - 苯基） - 具有BACE1抑制活性的式I的酰胺，其制备，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默氏病。

8. 发明授权

US08304537B2 Use of oxazine compounds for making chromogenic materials 失效
标题翻译：使用恶嗪化合物制造显色材料
公开(公告)号：US08304537B2
公开(公告)日：2012-11-06
申请号：US12733887
申请日：2008-10-17
申请人： Massimiliano Tomasulo , Francisco M. Raymo
发明人： Massimiliano Tomasulo , Francisco M. Raymo
IPC分类号： C07D265/12 , G02B5/23 , C07D265/00
CPC分类号： C09K9/02 , C07D498/04 , C09K2211/1033
摘要： Heterocyclic compounds incorporating a [1,3]oxazine ring may be used to make chromogenic materials. These molecules switch from a colorless state to a colored form upon addition of either acid or base. In both instances, the [1,3]oxazine ring opens in response to the pH change forming an indolium cation, after the addition of acid, or a phenolate anion, after the addition of base. Alternatively, the switch may occur in response to a change in electrical current or potential or a change in temperature. Chromophores absorb in the visible region of the electromagnetic spectrum. Hence, their formation translates into the appearance of color. These processes are fully reversible and the original colorless state can be regenerated by switching the pH back to neutral. Thus, these halochromic compounds can be used to develop displays, filters, indicators, lenses, sensors, switches, or windows able to switch their color in response to pH changes.
摘要翻译：掺入[1,3]恶嗪环的杂环化合物可用于制备显色材料。这些分子在加入酸或碱时，从无色状态转变为有色形式。在这两种情况下，加入碱后，[1,3]恶嗪环响应于pH变化而形成吲哚鎓阳离子，在加入酸或酚盐阴离子之后打开。或者，开关可以响应于电流或电位的变化或温度变化而发生。发色团在电磁谱的可见区域吸收。因此，它们的形成转化为颜色的外观。这些过程是完全可逆的，原始的无色状态可以通过将pH转换回中性来再生。因此，这些卤化铬化合物可用于开发显示器，过滤器，指示剂，透镜，传感器，开关或能够响应于pH变化而转换其颜色的窗户。

9. 发明申请

US20120190675A1 Azaspirohexanones 有权
标题翻译：阿扎苯甲酮
公开(公告)号：US20120190675A1
公开(公告)日：2012-07-26
申请号：US13166895
申请日：2011-06-23
申请人： Frank HIMMELSBACH
发明人： Frank HIMMELSBACH
IPC分类号： A61K31/537 , C07D265/18 , C07D413/10 , C07D498/10 , C07D221/20 , A61P3/06 , C07D239/70 , A61K31/527 , A61P3/00 , A61P3/10 , A61P3/04 , C07D265/12 , A61K31/438
CPC分类号： C07D221/20 , C07D265/12 , C07D265/18 , C07D413/10
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要翻译：本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4，R7，A，Z和m如本文所定义。式（I）化合物是11-β-羟基类固醇脱氢酶1（11beta-HSD1）的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是糖尿病 2型，肥胖症和血脂异常。

10. 发明授权

US08129524B2 Cyanopyrrole containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same 失效
标题翻译：含有环状氨基甲酸酯和硫代氨基甲酸酯联芳基的氰基吡咯及其制备方法
公开(公告)号：US08129524B2
公开(公告)日：2012-03-06
申请号：US13179730
申请日：2011-07-11
申请人： Bogdan Kazimierz Wilk
发明人： Bogdan Kazimierz Wilk
IPC分类号： C07D265/12 , C07D207/30
CPC分类号： C07D413/04 , C07D207/34
摘要： Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl) benzoicacid methyl ester, 5-[4-amino-3-(1-hydroxy-1-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-1H-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.
摘要翻译：提供了含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法：Z相同或不同，为H，任选取代的C 1 -C 6烷基或CORA; RA为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基，或任选取代的C 1至C 6氨基烷基; Q相同或不同，为H，OH，NH 2，CN，卤素，任选取代的C 1至C 6烷基，任选取代的C 2至C 6烯基，任选取代的C 1至C 6炔基，任选取代的C 1至C 6烷氧基，任选取代的C 1至 C6氨基烷基或CORB; 且R B为H，任选取代的C 1至C 6烷基，任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基。包括2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基）苯甲酸甲酯，5- [4-氨基-3-（1-羟基-1-甲基 - 乙基） - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-（5-氰基-1-甲基-1H-吡咯-2-基） - 苯基 - 乙酮或其药学上可接受的盐，并提供其用途。

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