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1. 发明公开

EP3337466A1 NOVEL POLYGODIAL ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES 审中-公开
公开(公告)号：EP3337466A1
公开(公告)日：2018-06-27
申请号：EP16839838.6
申请日：2016-08-17
申请人： The Board of Regents of The University of Texas System , Texas State University - San Marcos
发明人： GONZALES, Cara, B , KORNIENKO, Alexander , DASARI, Ramesh
IPC分类号： A61K31/01 , A61K31/015 , C07C13/47 , C07C13/48 , C07C13/50
CPC分类号： C07C13/48 , A61P35/02 , C07C67/343 , C07C69/738 , C07C255/00 , C07C255/31 , C07C2602/28 , C07D209/00 , C07D209/62 , C07F9/00 , C07F9/4018
摘要： The present disclosure relates generally to derivatives of polygodial and methods of use thereof. In some aspects, the present disclosure relates to using polygodial derivatives to treat cancer or other hyperproliferative diseases.

2. 发明公开

EP3099296A4 ISOINDOLINE COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE 有权
标题翻译： ISOINDOLINZUSAMMENSETZUNGEN UND VERFAHREN ZUR BEHANDLUNG NEURODEGENERATIVER ERKRANKUNGEN
公开(公告)号：EP3099296A4
公开(公告)日：2017-07-19
申请号：EP15743281
申请日：2015-01-30
申请人： COGNITION THERAPEUTICS INC
发明人： RISHTON GILBERT , CATALANO SUSAN M , LOOK GARY C
IPC分类号： A61K31/404 , A61K31/405 , A61P25/00 , A61P25/28 , C07D209/44 , C07D491/048
CPC分类号： C07D209/44 , C07D209/62 , C07D403/06 , C07D491/048 , C07D491/056
摘要： Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
摘要翻译：异吲哚啉σ-2受体拮抗剂化合物，包含此类化合物的药物组合物，以及用于抑制神经元细胞中Abeta相关突触丢失或突触功能障碍，调节神经元细胞中Aβ相关膜运输变化以及治疗与Abeta病理学相关的认知减退的方法被提供。

3. 发明公开

EP2963021A1 AMIDO COMPOUNDS AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： AMIDOVERBINDUNGEN UND DEREN VERWENDUNG ALS ARZNEIMITTEL
公开(公告)号：EP2963021A1
公开(公告)日：2016-01-06
申请号：EP15168750.6
申请日：2005-05-04
申请人： Incyte Holdings Corporation
发明人： YAO, Wenqing , ZHUO, Jincong , XU, Meizhong , ZHANG, Colin , METCALF, Brian , HE, Chunhong , QIAN, Ding-Quan
IPC分类号： C07D221/00 , C07D223/02 , C07D223/04 , C07D231/04
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
摘要翻译：本发明涉及11型羟基类固醇脱氢酶1型抑制剂，盐皮质激素受体（MR）的拮抗剂及其药物组合物。本发明的化合物可用于治疗与11-²羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病的表达或活性相关的各种疾病。

4. 发明公开

EP2588104A4 ISOINDOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS 有权转让
标题翻译：正变构异吲哚酮M1受体调节剂
公开(公告)号：EP2588104A4
公开(公告)日：2013-12-11
申请号：EP11801342
申请日：2011-06-27
申请人： MERCK SHARP & DOHME
发明人： KUDUK SCOTT D , BESHORE DOUGLAS C , YANG ZHIQIANG , SHU YOUHENG
IPC分类号： A61K31/4035 , A61P29/00 , C07D209/62 , C07D209/64 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/14 , C07D471/04
CPC分类号： C07D209/62 , C07D209/64 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/04 , C07D405/14 , C07D471/04

5. 发明公开

EP1343796A4 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：EP1343796A4
公开(公告)日：2005-01-12
申请号：EP01985647
申请日：2001-10-23
申请人： SMITHKLINE BEECHAM CORP
发明人： BONDINELL WILLIAM E , NEEB MICHAEL J
IPC分类号： C07D209/44 , C07D209/62 , C07D215/08 , C07D217/06 , C07D223/16 , C07D223/32 , C07D401/12 , C07D413/04 , C07D491/10 , C07H1/00
CPC分类号： C07D401/12 , C07D209/44 , C07D209/62 , C07D215/08 , C07D217/06 , C07D223/16 , C07D223/32 , C07D413/04 , C07D491/10

6. 发明公开

EP0095666A3 Tetrahydro-benzo(e) isoindolines 失效
标题翻译：四氢 - 苯并（e）异吲哚啉
公开(公告)号：EP0095666A3
公开(公告)日：1985-01-16
申请号：EP83104932
申请日：1983-05-19
申请人： ABBOTT LABORATORIES
发明人： DeBernardis, John Francis , Kerkman, Daniel Joseph , McClellan, William John
IPC分类号： C07D209/62 , C07D405/06 , C07D209/66 , C07C121/48 , A61K31/40 , C07C121/75
CPC分类号： C07D405/06 , C07C255/00 , C07D209/62 , C07D209/66
摘要： DisGosed herein are tetrahydro-benzo [e] isoindolines useful in the treatment of hypertension, which are represented by the formula
wherein R, R,, and R 2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, benzyloxy, benzoyloxy, thiomethyl, halo, or
wherein R. and R 5 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula
wherein R 6 is loweralkyl of 1 to 4 carbon atoms; or R and R,, or R, and R 2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R, or R 2 must be other than hydrogen; and R 3 is hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula
wherein m is 0, 1 or 2, p is 0 or 1, R 7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R 8 and R 9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1. to 4 carbon atoms, or halo, or R, and R 9 can be taken together to form a methylendioxy or ethylenedioxy bridge; or 1,4-benzodioxan.
摘要翻译：本发明公开了用于治疗高血压的四氢 - 苯并[e]异吲哚啉，其由下式表示：其中R 1，R 2和R 2独立地选自氢，羟基，1至3个碳原子的低级烷氧基，1的低级链烯氧基苄氧基，苯甲酰氧基，硫代甲基，卤素，或者其中R和R 5独立地选自氢，1-4个碳原子的低级π-酰氨基或下式的磺酰基：其中R 6为1-4个碳原子的低级烷基; 或R 1和R 2或R 1和R 2可一起形成亚甲二氧基或亚乙二氧基桥; 条件是R 1，R 2或R 2中的至少一个必须不是氢; 和R3是氢; 具有1至4个碳原子的低级烷基; 卤素取代的1至4个碳原子的低级烷基; 其中m为0,1或2，p为0或1，R 7为氢或1-4个碳原子的低级烷基，R 8和R 9独立地选自氢，羟基，甲氧基，1-4低级烷基碳原子或卤素，或R 1和R 9可一起形成亚甲基二氧基或亚乙基二氧桥; 或1,4-苯并二恶烷。

7. 发明公开

EP0065658A2 Verwendung von Sulfenamiden als Lipoxygenasehemmer und diese enthaltende Arzneimittel 失效
标题翻译：使用亚磺酰胺作为脂氧合酶抑制剂和包含它们的药物组合物。
公开(公告)号：EP0065658A2
公开(公告)日：1982-12-01
申请号：EP82103517.7
申请日：1982-04-26
申请人： BAYER AG
发明人： Busse, Wolf-Dieter, Dr. , Krauthausen, Edmund, Dr. , Mardin, Mithat, Dr.
IPC分类号： C07D239/42 , C07C145/00 , C07C145/04 , C07D249/14 , C07D285/12 , C07D263/26 , C07D263/58 , C07D263/18 , C07D265/18 , C07D295/22 , C07D279/06
CPC分类号： C07D209/48 , C07C313/34 , C07D209/38 , C07D209/50 , C07D209/62 , C07D223/10 , C07D225/02 , C07D231/08 , C07D231/12 , C07D233/56 , C07D233/80 , C07D235/22 , C07D239/42 , C07D249/08 , C07D249/14 , C07D257/06 , C07D263/18 , C07D263/26 , C07D263/58 , C07D265/18 , C07D265/26 , C07D277/82 , C07D279/06 , C07D285/08 , C07D285/135 , C07D295/26
摘要： Die vorliegende Erfindung betrifft die Verwendung von teilweise bekannten Sulfenamiden der allgemeinen Formel I
worin R 1 , R 2 und R 3 die in der Beschreibung angegebene Bedeutung haben, als Arzneimittel, insbesondere ihre Verwendung als Lipoxygenasehemmer, diese enthaltende Arzneimittel und deren Herstellung.
摘要翻译：本发明涉及通式I 其中R 1，R 2和R 3具有说明书中给出的含义，作为药物，特别是它们作为脂氧合酶抑制剂，含有它们的药物及其制备药物组合物中的部分已知的亚磺酰胺的。

8. 发明授权

EP2989102B1 CARBAZOLE DIOXAZINE PIGMENTS 有权
公开(公告)号：EP2989102B1
公开(公告)日：2018-11-28
申请号：EP14794345.0
申请日：2014-04-25
申请人： Gharda, Keki Hormusji
发明人： Gharda, Keki Hormusji
IPC分类号： C07D498/22 , C07D209/88 , C09B19/02 , C09B67/04 , C09B67/14 , C08K5/3417 , C08K5/3437
CPC分类号： C07D498/22 , C07D209/62 , C07D209/88 , C08K5/3417 , C08K5/3437 , C09B19/02 , C09B67/0002 , C09B67/0017
摘要： The present disclosure relates to a benzoyl substituted carbazole-dioxazine pigment and its preparation. The process involves benzoylation of 3-nitro-N-ethylcarbazole in monochlorobenzene using benzoylchloride and ferric chloride to yield 3-nitro-6-benzoyl-N-ethyl carbazole, which on catalytic hydrogenation and subsequent condensation with chloranil and cyclization yields benzoyl substituted carbazole-dioxazine pigment.

9. 发明公开

EP2830614A4 CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 失效
标题翻译：来自DUOCARMYIN类似物的环状前药
公开(公告)号：EP2830614A4
公开(公告)日：2015-09-23
申请号：EP13769317
申请日：2013-03-26
申请人： SCRIPPS RESEARCH INST
发明人： BOGER DALE L
IPC分类号： A61K31/27 , A61P35/00
CPC分类号： C07D498/06 , A61K45/06 , C07D209/62

10. 发明公开

EP2830614A1 CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 失效
标题翻译：循环前体药物OFF卡霉素类似物
公开(公告)号：EP2830614A1
公开(公告)日：2015-02-04
申请号：EP13769317.2
申请日：2013-03-26
申请人： The Scripps Research Institute
发明人： BOGER, Dale L.
IPC分类号： A61K31/27
CPC分类号： C07D498/06 , A61K45/06 , C07D209/62
摘要： The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient
in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spirocyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation
in vivo . Methods of synthesis and biological methods and data are also provided.

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