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1. 发明授权

EP2606031B1 AUTOTAXIN INHIBITORS AND USES THEREOF 失效转让
标题翻译：自杀毒素抑制剂及其用途
公开(公告)号：EP2606031B1
公开(公告)日：2017-09-27
申请号：EP11818851.5
申请日：2011-08-19
申请人： Amira Pharmaceuticals, Inc.
发明人： ROPPE, Jeffrey, Roger , PARR, Timothy, Andrew , STOCK, Nicholas, Simon , VOLKOTS, Deborah , HUTCHINSON, John, Howard
IPC分类号： C07D209/30 , C07D401/04 , C07D401/06 , A61K31/404 , A61K31/4439 , A61P11/00 , A61P35/00
CPC分类号： A61K31/404 , A61K31/41 , A61K31/4155 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/506 , A61K31/69 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/32 , C07D209/36 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/04 , C07F5/025
摘要： Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.
摘要翻译：本文描述的是作为autotaxin抑制剂的化合物。还描述了包含本文所述化合物的药物组合物和药物，以及单独或与其他化合物组合使用此类抑制剂用于治疗自体染色质依赖性或autotaxin介导的病症或疾病的方法。

2. 发明公开

EP3186267A1 AMPHIPHILIC COMPOUNDS WITH NEUROPROTECTIVE PROPERTIES 有权
标题翻译：具有神经保护性质的两性化合物
公开(公告)号：EP3186267A1
公开(公告)日：2017-07-05
申请号：EP15763482.5
申请日：2015-08-25
申请人： Ustav Organicke Chemie a Biochemie AV CR, v.v.i. , Fyziologicky Ustav AV CR, v.v.i.
发明人： KUDOVA, Eva , CHODOUNSKA, Hana , KAPRAS, Vojtech , VYKLICKY, Ladislav , VALES, Karel , JAHN, Ullrich
IPC分类号： C07J1/00 , C07J9/00 , C07J13/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J63/00 , C07J71/00 , A61K31/56 , A61P25/00 , A61P25/08 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/30 , C07C279/14 , C07C305/20 , C07C211/63 , C07C13/60 , C07C55/00
CPC分类号： C07J43/003 , C07C59/80 , C07C305/20 , C07C2603/26 , C07D209/36 , C07D213/18 , C07D317/72 , C07J1/0007 , C07J1/0011 , C07J9/00 , C07J9/005 , C07J13/007 , C07J31/006 , C07J41/0005 , C07J41/0033 , C07J41/0038 , C07J53/001 , C07J63/008 , C07J71/0005
摘要： The present invention provides amphiphilic compounds with a tetradecahydrophenanthrene skeleton of formula (I), wherein R1-R5 are as defined herein, and their enantiomers, exhibiting neuroprotective effects, for use as medicaments for treating neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain , addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing said compound.
摘要翻译：本发明提供了具有十四氢菲构架的两亲化合物及其对映异构体，表现出神经保护作用，其作为药物用于治疗与谷氨酸能神经递质系统失衡相关的神经精神病症，例如CNS的缺血性损伤，CNS的神经退行性改变和病症，情感障碍，抑郁症，创伤后应激障碍以及与压力，焦虑，精神分裂症和精神障碍有关的疾病，疼痛，成瘾，多发性硬化症，癫痫症，神经胶质瘤和含有所述化合物的药物组合物。

3. 发明授权

EP2276732B1 NOVEL ESTROGEN RECEPTOR LIGANDS 有权
标题翻译：新的配基对雌激素受体
公开(公告)号：EP2276732B1
公开(公告)日：2015-05-20
申请号：EP09731606.1
申请日：2009-04-16
申请人： KARO BIO AB
发明人： RHÖNNSTAD, Patrik , KALLIN, Elisabet , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping
IPC分类号： C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , A61K31/404 , A61P5/24 , A61P3/06 , A61P13/00
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04

4. 发明授权

EP1567492B1 N-ARYLSULFONYL-3-AMINOALKOXYINDOLES 失效
标题翻译：的N-芳基磺酰基-3- AMINOALKOXYINDOLE
公开(公告)号：EP1567492B1
公开(公告)日：2013-05-22
申请号：EP03778739.7
申请日：2003-11-25
申请人： Suven Life Sciences Limited
发明人： Ramakrishna, Venkata Satya Nirogi , Shirsath, Vikas Shreekrishna , Kambhampati, Rama Sastri , Rao, Venkata Satya Veerabhadra Vadlamudi , Jasti, Venkateswarlu
IPC分类号： C07D209/08 , C07D209/36 , A61K31/404
CPC分类号： C07D209/36 , C07D209/08

5. 发明公开

EP1981534A4 INDOLEAMINE 2,3-DIOXYGENASE PATHWAYS IN THE GENERATION OF REGULATORY T CELLS 审中-公开
标题翻译：吲哚胺2,3-双加氧酶-WAY在生产调节性T细胞
公开(公告)号：EP1981534A4
公开(公告)日：2012-04-04
申请号：EP07717763
申请日：2007-01-05
申请人： MED COLLEGE GEORGIA RES INST , UNIV MINNESOTA
发明人： CHEN WEI , BLAZAR BRUCE R , MUNN DAVID , MELLOR ANDREW
IPC分类号： A01N43/38 , C07D209/14
CPC分类号： C07D471/04 , A61K31/405 , C07D209/12 , C07D209/14 , C07D209/20 , C07D209/36 , C07D209/40 , C07D209/94 , C07D213/74 , C07D215/26 , C07D233/56 , C07D307/77 , C07D307/92 , C07D311/92 , C07D333/58 , C07D403/06 , C07D417/04 , C07D491/04 , C07D513/04

6. 发明授权

EP2114878B1 5-(HETEROCYCLYL)ALKYL-N-(ARYLSULFONYL)INDOLE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS 有权
标题翻译： 5-（杂环基）烷基-N-（芳基磺酰基）吲哚类化合物及其作为5-HT 6配体的
公开(公告)号：EP2114878B1
公开(公告)日：2010-12-15
申请号：EP07827525.2
申请日：2007-07-26
申请人： Suven Life Sciences Limited
发明人： RAMAKRISHNA, Nirogi, Venkata, Satya , KAMBHAMPATI, Rama, Sastri , KONDA, Jagadishbabu , KOTHMIRKAR, Prabhakar , JASTI, Venkateswarlu
IPC分类号： C07D209/08 , A61K31/404 , A61P25/00
CPC分类号： C07D209/08 , C07D209/36
摘要： The present invention relates to novel 5-(Heterocyclyl)alkyl-N- (arylsulfonyl)indole compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.

7. 发明授权

EP1537078B1 INDOLES HAVING ANTI-DIABETIC ACTIVITY 有权
标题翻译： WITH影响降糖吲哚
公开(公告)号：EP1537078B1
公开(公告)日：2010-04-14
申请号：EP03791952.9
申请日：2003-08-27
申请人： Merck Sharp & Dohme Corp.
发明人： ACTON, John, J., III , DEBENHAM, Sheryl, D. , LIU, Kun , MEINKE, Peter, T. , WOOD, Harold, B. , BLACK, Regina, M.
IPC分类号： C07D209/12 , A61K31/404 , A61P3/10 , C07D401/04 , C07D209/36 , C07D413/04 , C07D209/30 , C07D401/06 , C07D405/06 , C07D403/12 , C07D209/10
CPC分类号： C07D209/10 , C07D209/12 , C07D209/14 , C07D209/30 , C07D209/36 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/04
摘要： Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

8. 发明公开

EP2113258A1 AURONE DERIVATIVE-CONTAINING COMPOSITION FOR DIAGNOSIS 审中-公开
标题翻译： EIN AURONDERIVAT ENTHALTENDE ZUSAMMENSETZUNG ZUR DIAGNOSE
公开(公告)号：EP2113258A1
公开(公告)日：2009-11-04
申请号：EP07830664.4
申请日：2007-10-26
申请人： Nagasaki University
发明人： ONO, Masahiro
IPC分类号： A61K51/00 , C07D307/83
CPC分类号： C07D307/83 , A61K51/0419 , C07D209/36
摘要： The present invention provides a composition for diagnosing amyloid-related diseases, comprising a compound represented by general formula (I):

wherein X represents O or the like; R 1 , R 3 , R 4 , R 5 , R 6 , R 8 and R 9 represent a hydrogen atom or the like; R 2 represents a halogen atom or the like; and R 7 represents a dimethylamino group or the like;
or the compound labeled with a radionuclide, or a pharmaceutically acceptable salt of the compound or the labeled compound. The compound represented by general formula (I) has all of the following properties: high binding specificity to amyloid β protein, high permeability through the blood-brain barrier, and rapid clearance from sites without senile plaques in the brain.
摘要翻译：本发明提供了用于诊断淀粉样蛋白相关疾病的组合物，其包含通式（I）表示的化合物：其中X表示O等; R 1，R 3，R 4，R 5，R 6，R 8和R 9表示氢原子等; R 2表示卤素原子等; R 7表示二甲基氨基等; 或用放射性核素标记的化合物或化合物或标记化合物的药学上可接受的盐。由通式（I）表示的化合物具有以下特性：对淀粉样蛋白2蛋白的高结合特异性，通过血脑屏障的高通透性，以及从脑中没有老年斑的位置的快速清除。

9. 发明公开

EP1947085A1 Substituted indole sulfonamide compounds, their preparation and use as medicaments 审中-公开
标题翻译： Substituierte Indolsulfonamidverbindungen，ihre Herstellung und ihre Verwendung als Medikamente
公开(公告)号：EP1947085A1
公开(公告)日：2008-07-23
申请号：EP07384011.8
申请日：2007-01-19
申请人： Laboratorios del Dr. Esteve S.A.
发明人： Beller, Matthias , Alex, Karolin , Díaz Fernández, José Luis
IPC分类号： C07D209/36 , C07D409/12 , A61K31/404 , A61P3/04
CPC分类号： C07D209/36 , C07D409/12
摘要： The present invention relates to substituted indole sulfonamide compounds of general formula(I),

a process for their preparation, a medicament comprising these compounds and the use of substituted indole sulfonamide compounds for the preparation of medicaments for 5-HT 6 receptor regulation as well as for the treatment of disorders related thereto.
摘要翻译：本发明涉及通式（I）的取代的吲哚磺酰胺化合物，其制备方法，包含这些化合物的药物和使用取代的吲哚磺酰胺化合物制备用于5-HT 6受体调节的药物以及用于治疗与其相关的疾病。

10. 发明公开

EP1656347A1 SUBSTITUTED INDOLE DERIVATIVES FOR PHARMACEUTICAL COMPOSITION FOR TREATING RESPIRATORY DISEASES 有权
标题翻译：取代的吲哚衍生物的药物组合物用于呼吸系统疾病的治疗
公开(公告)号：EP1656347A1
公开(公告)日：2006-05-17
申请号：EP04768065.7
申请日：2004-08-16
申请人： AstraZeneca AB
发明人： BONNERT, Roger Victor, AstraZeneca R & D Charnwood , COOK, Anthony Ronald, AstraZeneca R & D Charnwood , LUKER, Timothy Jon, AstraZeneca R D Charnwood , MOHAMMED, Rukhsana T., AstraZeneca R & D Charnwood , THOM, Stephen, AstraZeneca R & D Charnwood
IPC分类号： C07D209/36
CPC分类号： C07D209/36
摘要： The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders.

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