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1. 发明公开

EP3233794A1 INDENYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND MEDICAL USES THEREOF 审中-公开
标题翻译：茚基化合物，药物组合物及其医学用途
公开(公告)号：EP3233794A1
公开(公告)日：2017-10-25
申请号：EP15823453.4
申请日：2015-12-16
申请人： ADT Pharmaceuticals, Inc.
发明人： PIAZZA, Gary A. , CHEN, Xi , KEETON, Adam B. , BOYD, Michael R.
IPC分类号： C07D207/14 , C07D213/24 , C07D235/30 , C07D307/38 , C07D307/52 , C07D405/12 , C07C43/205 , C07C233/58 , A61K31/075 , A61K31/166 , A61K31/443 , A61K31/506 , A61K31/341 , A61K31/44 , A61K31/505 , A61K31/40 , A61P35/00
CPC分类号： C07D317/64 , A61K31/341 , A61K31/36 , A61K31/40 , A61K31/401 , A61K31/44 , A61K31/445 , A61K45/06 , A61K2300/00 , C07C233/58 , C07C235/32 , C07C237/20 , C07C2601/02 , C07C2602/08 , C07D207/14 , C07D207/337 , C07D211/56 , C07D213/24 , C07D213/75 , C07D235/30 , C07D307/38 , C07D307/52 , C07D307/54 , C07D405/12
摘要： Disclosed are compounds, for example, compounds of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.
摘要翻译：公开了化合物，例如其中R，R 0，R 1 -R 8，n，X，Y，Y'和E如本文所述的式（I）化合物，含有这样的化合物以及治疗或预防疾病或病症例如癌症的方法。

2. 发明公开

EP2861572A1 IMPROVED PROCESS FOR THE PREPARATION OF 2-SUBSTITUTED-2-(6-(SUBSTITUTED)-7-METHYLBENZO[D][1,3]DIOXOL-4-YL)ACETIC ACID DERIVATIVES 有权
标题翻译： VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 2-SUBSTITUT-2-（6-（SUBSTITUT-）7-甲基苯并[D] [1,3]二氧杂环戊烯-4-基） - 苯甲酰胺
公开(公告)号：EP2861572A1
公开(公告)日：2015-04-22
申请号：EP13750150.8
申请日：2013-06-19
申请人： Natco Pharma Limited
发明人： MUDDASANI, Pulla Reddy , CHINTALAPUDI, Manikumar , NANNAPANENI, Venkaiah Chowdary
IPC分类号： C07D317/64 , C07C15/02
CPC分类号： C07D317/64 , C07C43/23 , C07C59/64 , C07C69/734 , C07D309/12 , C07F7/1804 , Y02P20/55
摘要： Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I the above Formula I, XII, XIII, XV, wherein R1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R2 is C1-C6 alkyl. 2,4-Dihydroxy-3-methylbenzaldehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin.
摘要翻译：本发明涉及制备式I的2-取代-2-（6-（取代的）-7-甲基苯并[d] [1,3]二氧杂环戊烯-4-基）乙酸衍生物的改进和商业化方法上述式I，XII，XIII，XV，其中R 1是O-保护基如甲氧基甲基，乙氧基甲基，三烷基甲硅烷基，芳基甲基，四氢吡喃-2-基，烯丙基; X是羟基，卤素，甲磺酸酯，三氟甲磺酸酯，甲苯磺酸酯，乙酸酯; Y是氧原子，NH或硫原子; R2是C1-C6烷基。 2,4-二羟基-3-甲基苯甲醛在C-4位选择性保护为式-IIII的醚化合物的形式，氧化醛官能团以获得式-IIIIII的二醇，并在卡西拉希反应下与乙醛酸乙酯缩合得到式XV化合物的条件。通过常规化学方法将式XV的化合物转化为式I的化合物。式I的化合物是合成类似于trabectinin的ecteinascidine的关键中间体。

3. 发明公开

EP2785178A1 OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： OPSIN结合配体，组合物和使用方法
公开(公告)号：EP2785178A1
公开(公告)日：2014-10-08
申请号：EP12852566.4
申请日：2012-11-29
申请人： Bikam Pharmaceuticals, Inc.
发明人： QUACH, Tan , BERMAN, Judd , GARVEY, David, S.
IPC分类号： A01N35/00
CPC分类号： C07C211/52 , C07C33/50 , C07C43/215 , C07C43/225 , C07C49/237 , C07C49/813 , C07C211/45 , C07C211/46 , C07C217/84 , C07C237/30 , C07C255/54 , C07C255/58 , C07C255/59 , C07C323/09 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D317/46 , C07D317/64 , C07D317/66
摘要： Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
摘要翻译：公开了化合物和组合物，所述化合物和组合物用于治疗由眼部积聚的毒性视觉周期产物（例如干性成人黄斑变性）引起的或与眼部疾病有关的眼科疾病，以及由突变视蛋白错误折叠引起的或与错误折叠有关的疾病蛋白质和/或视蛋白蛋白质的错误定位。还描述了单独或与其他治疗剂组合的这些化合物的组合物以及使用这些化合物和/或组合物的治疗方法。还公开了合成这些试剂的方法。

4. 发明公开

EP2725018A1 SUBSTITUTED CINNAMAMIDE DERIVATIVE, PREPARATION METHOD AND USE THEREOF 有权
标题翻译：替代品CINNAMAMIDDERIVAT，HERSTELLUNGSVERFAHRENDAFÜRUND VERWENDUNG DAVON
公开(公告)号：EP2725018A1
公开(公告)日：2014-04-30
申请号：EP12803864.3
申请日：2012-06-26
申请人： Tasly Pharmaceutical Group Co., Ltd.
发明人： MA, Xiaohui , JIN, Yuanpeng , HAN, Min , ZHOU, Shuiping , ZHOU, Wangyi , LUO, Xuejun , WANG, Guocheng , YAN, Lulu , ZHANG, Lanlan , ZHU, Yonghong
IPC分类号： C07D317/64 , C07D317/62 , C07D317/60 , A61K31/36 , A61P25/24
CPC分类号： C07D405/06 , C07D317/50 , C07D317/52 , C07D317/60 , C07D317/62 , C07D317/64
摘要： The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.
摘要翻译：本发明涉及取代的肉桂酰胺衍生物，其制备方法及其用途。所述衍生物中的每一个都具有式（I）的结构。还公开了制备本发明的取代肉桂酰胺及其衍生物的方法。选择取代的胡椒醛衍生物作为原料，通过Wittig反应和酸 - 胺缩合反应制备本发明的取代的肉桂酰胺衍生物。此外，公开了本发明化合物在预防和治疗抑郁型精神疾病中的用途。

5. 发明授权

EP1701950B1 ECSTASY HAPTENS AND IMMUNOGENS 有权
标题翻译：狂喜和半抗原免疫原
公开(公告)号：EP1701950B1
公开(公告)日：2014-02-12
申请号：EP04818007.9
申请日：2004-12-13
申请人： Siemens Healthcare Diagnostics Inc.
发明人： ZHENG, Yi, Feng , YANG, Yali
IPC分类号： C07D403/12 , C07D317/64 , C07D405/12 , C07K16/44 , G01N33/94 , C07D317/60
CPC分类号： C07D405/12 , C07D317/60 , C07D317/64 , C07D403/12 , C07K16/44 , G01N33/946 , Y10S435/961 , Y10S435/975

6. 发明公开

EP2248796A4 2-METHYLENE-5-SUBSTITUTED METHYLENE CYCLOPENTANONE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译： 2-亚甲基-5-取代METHYLENCYCLOPENTANONDERIVATE及其用途
公开(公告)号：EP2248796A4
公开(公告)日：2012-04-25
申请号：EP09710520
申请日：2009-02-10
申请人： UNIV SHENYANG PHARMACEUTICAL
发明人： ZHAO LINXIANG , WANG JINGLI , BIAN ZHENJUN , WANG RUI , LIU DAN , JING YONGKUI
IPC分类号： C07C49/687 , A61K31/122 , A61P35/00 , C07C49/653 , C07C49/683 , C07C49/753 , C07D317/54
CPC分类号： C07C49/683 , C07C45/59 , C07C45/673 , C07C49/697 , C07C49/753 , C07C225/22 , C07C317/24 , C07C2601/08 , C07D317/64

7. 发明公开

EP2201944A3 Use of substituted 2-aminoacetamides for treating, preventing or ameliorating manic depression 有权
标题翻译：使用取代的2- Aminoacetamiden的躁狂抑郁症的治疗，预防或改善
公开(公告)号：EP2201944A3
公开(公告)日：2010-07-28
申请号：EP10160059.1
申请日：1998-11-20
申请人： Purdue Neuroscience Company
发明人： Lan, Nancy, C , Wang, Yan , Cai, Sui, Xiong
IPC分类号： A61K31/165 , A61P25/18 , A61P25/24
CPC分类号： C07C233/05 , A61K31/165 , C07C237/06 , C07C237/08 , C07C2601/14 , C07D211/46 , C07D213/65 , C07D213/68 , C07D215/20 , C07D239/34 , C07D241/08 , C07D309/12 , C07D317/64
摘要： This invention relates to a compound having the Formula (II):

or a pharmaceutically acceptable salt thereof, wherein the substituents are defined herein, for use in a method of treating, preventing or ameliorating manic depression.

8. 发明公开

EP1981837A2 METHODS AND COMPOSITIONS FOR MODULATING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ACTIVITY 审中-公开
标题翻译：方法和组合物控制调节鞘氨醇-1-磷酸受体活性
公开(公告)号：EP1981837A2
公开(公告)日：2008-10-22
申请号：EP07763628.0
申请日：2007-01-30
申请人： Praecis Pharmaceuticals Incorporated
发明人： DENG, Hongfeng , EVINDAR, Ghotas , KAVARANA, Malcolm, J. , MORGAN, Barry , SAHA, Ashis, K. , SATZ, Alexander, L.
IPC分类号： C07C235/00 , C07D231/12 , C07D233/54 , C07D239/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/28 , C07D285/12 , C07D307/42 , C07D317/58 , C07D317/64 , C07D471/04 , C07F9/00
CPC分类号： C07F9/65062 , C07B2200/07 , C07C237/04 , C07C237/42 , C07C255/60 , C07C271/22 , C07C317/40 , C07C323/41 , C07C2601/14 , C07D207/12 , C07D209/88 , C07D213/30 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/26 , C07D249/06 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/28 , C07D285/12 , C07D307/42 , C07D317/58 , C07D317/64 , C07D333/16 , C07D417/10 , C07D471/04 , C07F9/091 , C07F9/65033 , C07F9/65037 , C07F9/65122 , C07F9/65181 , C07F9/65182 , C07F9/653 , C07F9/65312 , C07F9/6539 , C07F9/65395 , C07F9/65517 , C07F9/6561
摘要： The present invention relates to compounds which modulate the activity of the SlPl receptor, the use of these compounds for treating conditions associated with signaling through the SlPl receptor, and pharmaceutical compositions comprising these compounds.

9. 发明公开

EP1893568A2 MONOAMINE RE-UPTAKE INHIBITORS AND METHODS RELATING THERETO 审中-公开
标题翻译：蒙大拿 - 威尼斯美国饥饿人士（DAMITZUSAMMENHÄNGENDEVERFAHREN）
公开(公告)号：EP1893568A2
公开(公告)日：2008-03-05
申请号：EP06772503.6
申请日：2006-06-07
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： PONTILLO, Joseph , GAO, Yinghong , WADE, Warren, S. , WU, Dongpei , ECCLES, Wendy, K.
IPC分类号： C07C323/32 , C07C217/74 , C07D333/54 , C07D317/64
CPC分类号： C07C215/42 , C07C217/74 , C07C323/32 , C07C2602/08 , C07D265/34 , C07D317/64 , C07D333/54
摘要： Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure (I) wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting monoamine re-uptake in a subject in need thereof.
摘要翻译：公开了单胺再吸收抑制剂，更具体地说，可用于治疗男性和女性中枢性或周围神经系统疾病的5-羟色胺和去甲肾上腺素再摄取抑制剂。本发明的化合物具有以下结构：其中R 1，R 2，R 3，R 4， R 5，R 6，m，n，W，X，Y和Z如本文所定义，包括立体异构体，前药和药学上可接受的盐，酯和溶剂合物。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中抑制单胺再摄取的方法。

10. 发明公开

EP1850855A2 COMPOUNDS AND USES THEREOF 审中-公开
标题翻译： VERBINDUNGEN UND IHRE VERWENDUNGEN
公开(公告)号：EP1850855A2
公开(公告)日：2007-11-07
申请号：EP06734920.9
申请日：2006-02-13
申请人： CombinatoRx, Incorporated
发明人： FOLEY, Michael, A. , KEITH, Curtis , BORCHARDT, Ronald, T.
IPC分类号： A61K31/554
CPC分类号： C07D317/64 , C07C229/12 , C07C279/04 , C07C2603/32 , C07D267/16 , C07D267/20
摘要： The invention features charge-modified antidepressants and compounds conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a compound of the invention.
摘要翻译：本发明的特征在于电荷修饰的抗抑郁剂和化合物以与抗体在体内裂解的方式缀合于带电荷的基团或大体积基团。本发明提供了通过向患者施用本发明化合物来治疗患有炎性疾病的患者的方法。

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