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1. 发明申请

WO2018026371A1 DUAL NAV1.2/5HT2A INHIBITORS FOR TREATING CNS DISORDERS 审中-公开
标题翻译：双NAV1.2 / 5HT2A抑制剂治疗中枢神经系统病症
公开(公告)号：WO2018026371A1
公开(公告)日：2018-02-08
申请号：PCT/US2016/045559
申请日：2016-08-04
申请人： SUNOVION PHARMACEUTICALS INC.
发明人： HEFFERNAN, Michele L.R. , HARDY, Larry Wendell , BROWN, Scott P. , HERMAN, Lee W.
IPC分类号： C07D207/12 , C07D211/22 , C07D241/38 , C07D295/08 , C07D295/092 , C07D401/06 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D417/04 , C07D417/06 , C07D471/04 , C07D471/10 , C07D487/10 , C07D491/107 , C07D491/12 , A61K31/40 , A61K31/4025 , A61K31/428 , A61K31/4427 , A61K31/4523 , A61K31/4725 , A61K31/496 , A61K31/4995 , A61K31/5513 , A61P25/18 , A61P25/28
CPC分类号： C07D401/08 , A61P25/18 , A61P25/28 , C07D207/12 , C07D207/36 , C07D211/42 , C07D211/44 , C07D211/58 , C07D213/81 , C07D217/24 , C07D221/20 , C07D223/08 , C07D235/12 , C07D237/14 , C07D241/04 , C07D243/08 , C07D249/12 , C07D265/30 , C07D267/10 , C07D275/04 , C07D277/66 , C07D295/027 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/104 , C07D295/108 , C07D307/83 , C07D311/08 , C07D311/22 , C07D311/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06 , C07D413/08 , C07D417/04 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/10 , C07D491/048 , C07D491/107 , C07D491/20 , C07D513/04
摘要： Compounds of formula I: I are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
摘要翻译：公开了式I的化合物：以及含有这些化合物的药物组合物。还公开了治疗有需要的患者的神经或精神障碍的方法。这些障碍包括抑郁症，双相障碍，疼痛，精神分裂症，强迫症，成瘾，社交障碍，注意力缺陷多动障碍，焦虑症，孤独症，认知障碍或神经精神症状，例如冷漠，抑郁，焦虑，精神病，侵略，激动，冲动控制障碍和神经疾病如阿尔茨海默氏病和帕金森病的睡眠障碍。

2. 发明申请

WO2012074757A1 ALANINYL MAYTANSINOL ANTIBODY CONJUGATES 审中-公开
标题翻译： ALANINYL MAYTANSINOL抗体结合
公开(公告)号：WO2012074757A1
公开(公告)日：2012-06-07
申请号：PCT/US2011/061031
申请日：2011-11-16
申请人： GENENTECH, INC. , FLYGARE, John , JUNUTULA, Jagath Reddy , PILLOW, Thomas
发明人： FLYGARE, John , JUNUTULA, Jagath Reddy , PILLOW, Thomas
IPC分类号： C07D491/12 , A61K31/535 , A61K39/00
CPC分类号： C07D491/12
摘要： Linker-drug intermediates of Formula I are conjugated to antibodies to form antibody-drug conjugates where the drug moiety is an N-methylalaninyl-maytansinoid. L is Formula IA; E is Formula IB or Formula IC; n is 2, 3, 4, 5, or 6; m is 2, 3 or 4; and q is 0 or 1.
摘要翻译：式I的接头 - 药物中间体与抗体缀合以形成抗体 - 药物偶联物，其中药物部分是N-甲基丙酰氨基 - 美登木素生物碱。 L是式IA; E为式IB或式IC; n为2,3,4,5或6; m为2,3或4; q为0或1。

3. 发明申请

WO2007120752A3 4, 5-DIHYDRO- [1, 2, 4] TRIAZOLO [4, 3-F] PTERIDINES AS PROTEIN KINASE PLK1 INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译： 4,5-二氢 - [1,2,4]三唑[4,3-F]脯氨酸作为蛋白激酶PLK1抑制剂治疗增殖性疾病
公开(公告)号：WO2007120752A3
公开(公告)日：2008-05-08
申请号：PCT/US2007009006
申请日：2007-04-12
申请人： VERTEX PHARMA , CHARRIER JEAN-DAMIEN , KAY DAVID , KNEGTEL RONALD
发明人： CHARRIER JEAN-DAMIEN , KAY DAVID , KNEGTEL RONALD
IPC分类号： C07D491/12 , A61K31/519 , A61P35/00
CPC分类号： C07D487/14
摘要： The present invention relates to compounds of formula (I) useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的式（I）化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

4. 发明申请

WO2004103272A3 IMPROVED CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS 审中-公开
公开(公告)号：WO2004103272A3
公开(公告)日：2004-12-02
申请号：PCT/US2004/013314
申请日：2004-05-20
申请人： IMMUNOGEN, INC. , WIDDISON, Wayne, C. , CHARI, Ravi, V., J.
发明人： WIDDISON, Wayne, C. , CHARI, Ravi, V., J.
IPC分类号： A61K31/5365 , A61K47/48 , C07D491/12 , C07D498/16
摘要： New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.

5. 发明申请

WO0204457A8 AZEPINO[4,5-B]PYRANO[3,2-E]INDOLES 审中-公开
标题翻译：氮杂并[4,5-B]吡喃并[3,2-E]吲哚
公开(公告)号：WO0204457A8
公开(公告)日：2002-03-21
申请号：PCT/US0121423
申请日：2001-07-06
申请人： UPJOHN CO , FU JIAN MIN
发明人： FU JIAN-MIN
IPC分类号： A61K31/55 , A61P25/00 , C07D491/14 , C07D491/147 , C07D491/12
CPC分类号： C07D491/14 , A61K31/55
摘要： The invetion provides a compound of formula (1), wherein: R -R , m, m, p, and the bonds a and b represented by --- have any of the values, specific values, or preferred values described in the specification; or a salt or solvate thereof. The invention also provides pharmaceutical compositions comprising such a compound, as well as intermediates and processes useful for preparing such a compound, and therapeutic methods including the administration of such a compound.
摘要翻译：该发明提供了式（1）的化合物，其中：R 1 -R 5，m，m，p和由---表示的键a和b具有任何值，具体值或说明书中描述的优选值; 或其盐或溶剂化物。本发明还提供了包含这种化合物的药物组合物，以及可用于制备该化合物的中间体和方法，以及治疗方法，包括给予这种化合物。

6. 发明申请

WO02020484A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO02020484A1
公开(公告)日：2002-03-14
申请号：PCT/SE2001/001869
申请日：2001-08-30
IPC分类号： C07D473/06 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/522 , A61K31/5415 , A61P11/06 , A61P27/16 , A61P29/00 , A61P31/18 , A61P37/02 , A61P43/00 , C07D211/46 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/04 , C07D473/08 , C07D487/04 , C07D491/12
CPC分类号： C07D401/12 , C07D211/46 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/04 , C07D487/04 , C07D491/12
摘要： The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.
摘要翻译：本发明提供式（I）化合物：作为趋化因子和H1受体活性的调节剂。这些化合物特别适用于治疗哮喘和鼻炎。

7. 发明申请

WO98042714A1 NEW SESQUITERPENE DERIVATIVES 审中-公开
标题翻译：新的SESQUITERPENE衍生物
公开(公告)号：WO98042714A1
公开(公告)日：1998-10-01
申请号：PCT/JP1998/000992
申请日：1998-03-11
IPC分类号： C07D491/052 , C07D491/10 , C07D491/12 , C07D491/153 , C07F9/6561 , A61K31/40
CPC分类号： C07D491/10 , C07D491/12 , C07F9/6561
摘要： Sesquiterpene derivatives useful as antiviral agents, which are represented by general formula (I), wherein R represents hydrogen or halogen; R represents hydrogen, halogen, -OR (in which R is hydrogen or the like) or -NHR (in which R is hydrogen or the like); or R and R together form oxo or =NR (in which R is hydroxyl or the like); R represents hydrogen or halogen; R represents hydrogen, halogen, -OR (in which R is hydrogen or the like) or -NHR (in which R is hydrogen or the like); or R and R together form oxo or =NR (in which R is hydroxyl or the like); or R and R together form an unsaturated bond or -O-; A represents =NR (in which R is hydrogen, lower alkyl or the like); R represents hydrogen, cyano or the like; X represents hydrogen, cyano or the like; Y and Y are each hydrogen or they together form oxo; and Z and Z are each hydrogen or they together form oxo, or Z is hydrogen and Z is hydroxyl.
摘要翻译：用作抗病毒剂的倍半萜衍生物，其由通式（I）表示，其中R 1表示氢或卤素; R 2表示氢，卤素，-OR 7（其中R 7为氢等）或-NHR 8（其中R 8为氢等）; 或R 1和R 2一起形成氧代或= NR 9（其中R 9是羟基等）; R 3表示氢或卤素; R 4表示氢，卤素-OR 10（其中R 10为氢等）或-NHR 11（其中R 11为氢等）; 或R 3和R 4一起形成氧代或= NR 12（其中R 12是羟基等）; 或R 2和R 4一起形成不饱和键或-O-; A表示= NR 5（其中R 5是氢，低级烷基等）; R 6表示氢，氰基等; X表示氢，氰基等; Y 1和Y 2各自为氢或它们一起形成氧代; Z 1和Z 2各自为氢或它们一起形成氧代，或Z 1为氢，Z 2为羟基。

8. 发明申请

WO2015048365A1 NOVEL 20(S)-SULFONYLAMIDINE DERIVATIVES OF CAMPTOTHECIN AND THE USE THEREOF AS A POTENT ANTITUMOR AGENT 审中-公开
标题翻译：氨茶碱的新二十（S） - 磺酰胺衍生物及其作为抗肿瘤剂的用途
公开(公告)号：WO2015048365A1
公开(公告)日：2015-04-02
申请号：PCT/US2014/057575
申请日：2014-09-26
申请人： LEE, Kuo-Hsiung , QIAN, Keduo , YANG, Xiaoming , GOTO, Masuo , LIU, Ying-Qian , ZHAO, Yong-Long , YANG, Liu , WANG, Mei-Juan , ZHANG, Zhi-Jun , WU, Tian-Shung , TENG, Che-Ming , WANG, Chih-Ya , PAN, Shiow-Lin , KUO, Sheng-Chu , HUNG, Hsin-Yi , CHANG, Ling-Chu , WU, Yang-Chang , HSIEH, Min-Tsang , HSU, Chung Y. , SHYU, Woei-Cherng , LIN, Chen-Huan
发明人： LEE, Kuo-Hsiung , QIAN, Keduo , YANG, Xiaoming , GOTO, Masuo , LIU, Ying-Qian , ZHAO, Yong-Long , YANG, Liu , WANG, Mei-Juan , ZHANG, Zhi-Jun , WU, Tian-Shung , TENG, Che-Ming , WANG, Chih-Ya , PAN, Shiow-Lin , KUO, Sheng-Chu , HUNG, Hsin-Yi , CHANG, Ling-Chu , WU, Yang-Chang , HSIEH, Min-Tsang , HSU, Chung Y. , SHYU, Woei-Cherng , LIN, Chen-Huan
IPC分类号： C07D491/12 , C07D471/04 , A61K31/4745 , A61K35/00
CPC分类号： C07D491/22 , C07F7/0812 , C07F9/6561
摘要： The present invention is related to novel 20-sulfonylamidine derivatives of camptothecin (1), method of synthesizing the same, and use thereof as an antitumor agent, for examples an antitumor agent for treating nasopharyngeal, lung, breast or prostate cancer.
摘要翻译：本发明涉及喜树碱（1）的新型20-磺酰脒衍生物，其合成方法及其作为抗肿瘤剂的用途，例如用于治疗鼻咽癌，肺癌，乳腺癌或前列腺癌的抗肿瘤剂。

9. 发明申请

WO2009134616A8 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译：新型丙型肝炎病毒复制抑制剂
公开(公告)号：WO2009134616A8
公开(公告)日：2010-05-14
申请号：PCT/US2009040567
申请日：2009-04-14
申请人： INTERMUNE INC , BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
发明人： BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
IPC分类号： C07D285/30 , A61K31/5415 , A61P31/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/12
CPC分类号： C07D471/04 , C07D285/30 , C07D417/04 , C07D487/04
摘要： The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译：实施方案提供通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。该实施方案进一步提供了治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常包括向有需要的个体施用有效量的主题化合物或组合物。

10. 发明申请

WO2005003086A3 SULFONIC ACID DERIVATIVES OF POLYCYCLIC DYES USED FOR ANALYTICAL APPLICATIONS 审中-公开
标题翻译：磺酸多环染料分析应用
公开(公告)号：WO2005003086A3
公开(公告)日：2006-02-23
申请号：PCT/EP2004007248
申请日：2004-07-02
申请人： ATTO TEC GMBH , ZILLES ALEXANDER , ARDEN-JACOB JUTTA , DREXHAGE KARL-HEINZ , KEMNITZER NORBERT UWE , HAMERS-SCHNEIDER MONIKA
发明人： ZILLES ALEXANDER , ARDEN-JACOB JUTTA , DREXHAGE KARL-HEINZ , KEMNITZER NORBERT UWE , HAMERS-SCHNEIDER MONIKA
IPC分类号： C07D20060101 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D221/18 , C07D401/12 , C07D405/12 , C07D471/04 , C07D471/22 , C07D491/04 , C07D491/12 , C07D491/14 , C07D491/22 , C07D498/22 , C09B67/18 , G01N33/58
CPC分类号： C07D401/12 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D221/18 , C07D405/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D491/14 , C07D491/22 , C07D498/04 , C07D498/14 , C09B11/24 , C09B11/28 , C09B19/00 , C09B21/00 , C09B57/02
摘要： The invention relates to the production of quinoline compounds containing sulfonic acid groups, said quinoline compounds, and the conversion thereof into dyes containing sulfonic acid groups. The inventive dyes are used especially for marking analytes, e.g. for marking biomolecules.
摘要翻译：本发明涉及含有磺酸基的喹啉化合物的制备中，喹啉化合物本身及其转化成含磺酸的染料。本发明的染料特别地用于标记分析物，例如用于标记的生物分子。

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