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公开(公告)号：EP4112616A1
公开(公告)日：2023-01-04
申请号：EP22175891.5
申请日：2018-09-11
IPC分类号： C07D417/04 , C07D417/14 , C07D277/42 , C07D277/28 , C07D417/12 , A61P25/28 , A61P35/00 , A61P37/00 , A61K31/427
摘要： This application is directed to inhibitors of RAD51 represented by the following structural formula,
and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.-
公开(公告)号：EP3481810A1
公开(公告)日：2019-05-15
申请号：EP17828262.0
申请日：2017-07-11
IPC分类号： C07D277/42 , C07D495/04
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公开(公告)号：EP2594555B1
公开(公告)日：2018-03-07
申请号：EP11800989.3
申请日：2011-07-01
IPC分类号： C07D207/34 , A61K31/341 , A61K31/415 , A61K31/4178 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/498 , A61K31/5383 , A61K31/55 , A61P3/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14
CPC分类号： C07D498/04 , C07D207/34 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/052 , C07F5/025
摘要： A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27 kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.
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4.发明公开DISUBSTITUTED PIPERIDINE DERIVATIVES AS BUTYRYLCHOLINESTERASE INHIBITORS FOR USE IN THE TREATMENT OF ALZHEIMER 审中-公开用于治疗阿尔茨海默病的丁酰胆碱酯酶抑制剂的二取代哌啶衍生物
公开(公告)号：EP3256128A1
公开(公告)日：2017-12-20
申请号：EP16720556.6
申请日：2016-03-22
申请人： Univerza v Ljubljani
发明人： BRUS, Boris , KOSAK, Urban , KNEZ, Damijan , COQUELLE, Nicolas , COLLETIER, Jacques-Philippe , GOBEC, Stanislav
IPC分类号： A61K31/445 , A61K31/4523 , A61K31/453 , A61K31/4709 , C07D311/10 , C07D215/26 , C07D277/42 , C07D295/04 , A61P25/28
CPC分类号： C07D211/28 , A61K31/445 , A61K31/4523 , A61K31/453 , A61K31/4709 , C07D211/26 , C07D401/12 , C07D405/12
摘要： This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia.
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公开(公告)号：EP2682390A4
公开(公告)日：2014-07-23
申请号：EP12752555
申请日：2012-02-01
发明人： JIANG FENGCHAO , ZHOU PING , CHEN JIANGUO , WANG YUE , CAO BAOSHUAI , YAN JIA
IPC分类号： C07D277/46 , A61K31/425 , A61P3/10 , A61P25/00 , A61P37/00 , C07D277/42 , C07D417/12
CPC分类号： C07D277/42 , C07D277/46 , C07D295/14 , C07D417/12
摘要： The present invention relates to the preparation of a 2-aminothiazole derivative having a structure as formula (I) and a therapeutic effect thereof for Alzheimer's disease (AD), and a therapeutic effect thereof against transplant rejection, autoimmune diseases, ischemia-reperfusion injury, chronic inflammation response, endotoxemia, and other diseases.
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6.发明授权(4-[4-[5-(substituted amino)-pyridin-2-yl]phenyl]-cyclohexyl)-acetic acid derivatives as DGAT inhibitors 有权（4- [4- [5-（取代的氨基） - 吡啶-2-基]苯基] - 环己基） - 乙酸衍生物，DGAT-抑制素
公开(公告)号：EP2418202B1
公开(公告)日：2014-01-29
申请号：EP11158211.0
申请日：2007-03-28
申请人： Novartis AG
IPC分类号： C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/10 , C07D413/12 , A61K31/44 , A61K31/50 , A61K31/53 , A61K31/421 , A61K31/426
CPC分类号： C07D413/10 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/76 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention provides new organic compounds of the following formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒA-L1-B-C-D-L2-E wherein A, L1, B, C, D, L2 and E are as defined in the description of the invention, that are useful for treating or preventing conditions or disorders associated with DGAT1 activity, particularly type 2 diabetes, and pharmaceutical compositions comprising such compounds.
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7.发明公开
公开(公告)号：EP2627662A1
公开(公告)日：2013-08-21
申请号：EP11773962.3
申请日：2011-10-13
IPC分类号： C07K1/113 , C07K1/107 , C07D277/42
CPC分类号： C07K7/64 , C07D277/42 , C07D417/04 , C07K1/1136 , C07K5/123 , C07K5/126
摘要： The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.
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8.发明公开HETEROCYCLIC COMPOUND, AND p27 KIP1 DEGRADATION INHIBITOR 有权P27-KIP-1-ABBAUHEMMER的HETEROZYKLISCHE VERBINDUNG
公开(公告)号：EP2594555A1
公开(公告)日：2013-05-22
申请号：EP11800989.3
申请日：2011-07-01
IPC分类号： C07D207/34 , A61K31/341 , A61K31/415 , A61K31/4178 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/498 , A61K31/5383 , A61K31/55 , A61P3/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14
CPC分类号： C07D498/04 , C07D207/34 , C07D231/40 , C07D277/20 , C07D277/42 , C07D307/68 , C07D403/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/052 , C07F5/025
摘要： A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27 kip1 is provided. The compound or the salt thereof is represented by the following formula (1):
wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.摘要翻译： 提供了可用于选择性抑制p27kip1降解的新型杂环化合物或其盐。 化合物或其盐由下式（1）表示：其中A表示烷基，环烷基，芳基或杂环基，基团A可以具有取代基; 环B表示5-8元单环杂环或含有单环杂环的稠环，环B可以具有取代基; 环C表示芳香环，环C可以具有取代基; L表示包含选自碳原子，氮原子，氧原子和硫原子的3至5个原子的主链的连接体，其中主链中的至少一个原子是选自以下的杂原子 由氮原子，氧原子和硫原子组成的基团，连接体L可以具有取代基; n为0或1。
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9.发明授权Process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazol-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine 有权[2-环丙基-1-（3-氟-4-甲基苯基）乙基 - 一种用于[4-（2-氯-4-甲氧基-5-甲基苯基）-5-甲基 - 噻唑-2-基]的制备方法 ]胺
公开(公告)号：EP2424848B1
公开(公告)日：2013-03-13
申请号：EP10718684.3
申请日：2010-04-26
申请人： SANOFI
IPC分类号： C07D277/42 , C07D327/04 , C07C331/04
CPC分类号： C07D277/42 , C07C331/04 , C07D327/04
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10.发明授权(4-(4-[6-(trifluoromethyl-pyridin-3-ylamino)-N-containing-heteroaryl]-phenyl)-cyclohexyl)-acetic acid derivatives and pharmaceutical uses thereof 有权（4-（4- [6-（三氟甲基 - 吡啶-3-基氨基）-N-含有杂芳基] - 苯基） - 环己基）乙酸衍生物及其药物应用
公开(公告)号：EP2004607B1
公开(公告)日：2011-10-19
申请号：EP07754311.4
申请日：2007-03-28
申请人： Novartis AG
IPC分类号： C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/10 , A61K31/44
CPC分类号： C07D413/10 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/76 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
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