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1. 发明申请

WO2015009977A1 AMINOMETHYL-BIARYL DERIVATIVES AS COMPLEMENT FACTOR D INHIBITORS AND USES THEREOF 审中-公开
标题翻译：氨基甲基衍生物作为补体因子D抑制剂及其用途
公开(公告)号：WO2015009977A1
公开(公告)日：2015-01-22
申请号：PCT/US2014/047106
申请日：2014-07-17
申请人： NOVARTIS AG , BELANGER, David B. , FLOHR, Stefanie , GELIN, Christine Fang , JENDZA, Keith , JI, Nan , LIU, Donglei , LORTHIOIS, Edwige Liliane Jeanne , KARKI, Rajeshri Ganesh , MAINOLFI, Nello , POWERS, James J. , RANDL, Stefan Andreas , ROGEL, Olivier , VULPETTI, Anna , YOON, Taeyoung
发明人： BELANGER, David B. , FLOHR, Stefanie , GELIN, Christine Fang , JENDZA, Keith , JI, Nan , LIU, Donglei , LORTHIOIS, Edwige Liliane Jeanne , KARKI, Rajeshri Ganesh , MAINOLFI, Nello , POWERS, James J. , RANDL, Stefan Andreas , ROGEL, Olivier , VULPETTI, Anna , YOON, Taeyoung
IPC分类号： C07D213/81 , C07C311/21 , C07C233/75 , C07C229/06
CPC分类号： C07D417/12 , C07C217/48 , C07C217/58 , C07C217/64 , C07C217/74 , C07C217/76 , C07C229/34 , C07C229/36 , C07C229/42 , C07C233/43 , C07C233/47 , C07C233/63 , C07C235/34 , C07C235/46 , C07C237/20 , C07C237/38 , C07C237/40 , C07C237/42 , C07C255/16 , C07C255/43 , C07C255/57 , C07C255/59 , C07C257/18 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/12 , C07D231/12 , C07D231/56 , C07D233/90 , C07D239/26 , C07D257/04 , C07D263/32 , C07D265/30 , C07D267/10 , C07D277/56 , C07D305/06 , C07D307/16 , C07D309/06 , C07D309/14 , C07D311/42 , C07D317/60 , C07D405/12
摘要： The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了式（I）化合物，本发明化合物的制备方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

2. 发明申请

WO2008048991A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2008048991A2
公开(公告)日：2008-04-24
申请号：PCT/US2007/081607
申请日：2007-10-17
申请人： NOVARTIS AG , SUNG, Moo Je , COPPOLA, Gary Mark , YOON, Taeyoung , GILMORE, Thomas A.
发明人： SUNG, Moo Je , COPPOLA, Gary Mark , YOON, Taeyoung , GILMORE, Thomas A.
CPC分类号： C07D235/18 , C07D209/08 , C07D209/10 , C07D209/48 , C07D263/57 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of the following structure; A-L1-B-C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
摘要翻译：本发明提供了以下结构的化合物： A-L1-B-C-D，其用于治疗或预防动物，特别是人类中与DGAT1活性相关的病症或障碍。

3. 发明申请

WO2006004589A2 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES 审中-公开
标题翻译： 3-芳基-5,6-二取代的哒嗪
公开(公告)号：WO2006004589A2
公开(公告)日：2006-01-12
申请号：PCT/US2005/016139
申请日：2005-05-06
申请人： NEUROGEN CORPORATION , YOON, Taeyoung , YUAN, Jun , LEE, Kyungae , MAYNARD, George, D. , LIU, Nian
发明人： YOON, Taeyoung , YUAN, Jun , LEE, Kyungae , MAYNARD, George, D. , LIU, Nian
IPC分类号： C07D403/02
CPC分类号： C07D237/20 , C07D237/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/04
摘要： The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
摘要翻译：本发明提供式（I）或（II）盐形式的化合物或其盐或其前药，其中变量在本文中定义为金属蛋白酶如基质金属蛋白酶（MMP）和ADAM的调节剂。本文所述的化合物或组合物可用于治疗与金属蛋白酶活性相关的疾病，包括例如关节炎，癌症，心血管病症，皮肤病症，炎症或过敏性病症。

4. 发明申请

WO2004056774A2 SUBSTITUTED BIPHENYL-4-CARBOXYLIC ACID ARYLAMIDE ANALOGUES 审中-公开
标题翻译：取代的联苯-4-羧酸酰亚胺类似物
公开(公告)号：WO2004056774A2
公开(公告)日：2004-07-08
申请号：PCT/US2003/040878
申请日：2003-12-19
申请人： NEUROGEN CORPORATION , BAKTHAVATCHALAM, Rajagopal , BLUM, Charles, A. , BRIELMANN, Harry , DARROW, James, W. , DE LOMBAERT, Stephane , YOON, Taeyoung , ZHENG, Xiaozhang
发明人： BAKTHAVATCHALAM, Rajagopal , BLUM, Charles, A. , BRIELMANN, Harry , DARROW, James, W. , DE LOMBAERT, Stephane , YOON, Taeyoung , ZHENG, Xiaozhang
IPC分类号： C07D213/00
CPC分类号： C07D213/76 , C07C233/65 , C07C233/66 , C07C233/75 , C07C235/64 , C07D211/34 , C07D213/26 , C07D213/48 , C07D213/61 , C07D213/73 , C07D213/82 , C07D213/85 , C07D241/16 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/12
摘要： Substituted bipheny1-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in viva or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供能够调节受体活性的取代的联苯-4-羧酸芳酰胺类似物。这样的配体可以用于调节viva或体外的受体活性，并且特别可用于治疗与人类，家养伴侣动物和家畜中的受体激活相关的疼痛和其它病症。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

5. 发明申请

WO2004018437A1 5-SUBSTITUTED-2-ARYLPYRAZINES AS MODULATORS OF CRF RECEPTORS 审中-公开
标题翻译：作为CRF受体调节剂的5-取代-2-亚氨基
公开(公告)号：WO2004018437A1
公开(公告)日：2004-03-04
申请号：PCT/US2003/026141
申请日：2003-08-20
申请人： NEUROGEN CORPORATION , YOON, Taeyoung , GE, Ping , DELOMBAERT, Stephane , HORVATH, Raymond
发明人： YOON, Taeyoung , GE, Ping , DELOMBAERT, Stephane , HORVATH, Raymond
IPC分类号： C07D241/20
CPC分类号： C07D241/12 , C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and peripheral disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供新的5-取代-2-芳基吡嗪化合物。这些化合物可以作为CRF受体的选择性调节剂。本文提供的5-取代-2-芳基吡嗪化合物可用于治疗许多CNS和外周疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。提供的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

6. 发明申请

WO2009150230A1 2,4'-BIPYRIDINYL COMPOUNDS AS PROTEIN KINASE D INHIBITORS USEFUL FOR THE TREATMENT OF IA HEART FAILURE AND CANCER 审中-公开
标题翻译：作为蛋白激酶D抑制剂用于治疗心脏失败和癌症的2,4'-二吡啶基化合物
公开(公告)号：WO2009150230A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/057298
申请日：2009-06-12
申请人： NOVARTIS AG , BURGIS, Robin , CAPPARELLI, Michael, Paul , DIPIETRO, Lucian , GAMBER, Gabriel, G. , JEWELL, JR., Charles, Francis , MEREDITH, Erik , MIRANDA, Karl , MONOVICH, Lauren, G. , RAO, Chang , SOLDERMANN, Nicolas , YOON, Taeyoung , ZHU, Qingming
发明人： BURGIS, Robin , CAPPARELLI, Michael, Paul , DIPIETRO, Lucian , GAMBER, Gabriel, G. , JEWELL, JR., Charles, Francis , MEREDITH, Erik , MIRANDA, Karl , MONOVICH, Lauren, G. , RAO, Chang , SOLDERMANN, Nicolas , YOON, Taeyoung , ZHU, Qingming
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D519/00 , A61K31/496 , A61P9/04 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
摘要翻译：本发明提供式I的新型有机化合物：使用方法及其药物组合物。

7. 发明申请

WO2004056774A3 SUBSTITUTED BIPHENYL-4-CARBOXYLIC ACID ARYLAMIDE ANALOGUES AS CAPSAICIN RECEPTOR MODULATORS 审中-公开
标题翻译：作为CAPSAICIN受体调节剂的取代的联苯酰基-4-羧酸亚胺酰胺类似物
公开(公告)号：WO2004056774A3
公开(公告)日：2004-11-04
申请号：PCT/US0340878
申请日：2003-12-19
申请人： NEUROGEN CORP , BAKTHAVATCHALAM RAJAGOPAL , BLUM CHARLES A , BRIELMANN HARRY , DARROW JAMES W , DE LOMBAERT STEPHANE , YOON TAEYOUNG , ZHENG XIAOZHANG
发明人： BAKTHAVATCHALAM RAJAGOPAL , BLUM CHARLES A , BRIELMANN HARRY , DARROW JAMES W , DE LOMBAERT STEPHANE , YOON TAEYOUNG , ZHENG XIAOZHANG
IPC分类号： A61P25/00 , C07D211/34 , C07D213/26 , C07D213/48 , C07D213/61 , C07D213/73 , C07D213/76 , C07D213/82 , C07D213/85 , C07D241/16 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/12 , A61K31/44 , C07C235/64
CPC分类号： C07D213/76 , C07C233/65 , C07C233/66 , C07C233/75 , C07C235/64 , C07D211/34 , C07D213/26 , C07D213/48 , C07D213/61 , C07D213/73 , C07D213/82 , C07D213/85 , C07D241/16 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/12
摘要： Substituted biphenyl-4-carboxylic acid arylamide analogues of the formula (I) capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for receptor localization studies.

8. 发明申请

WO0160806A3 SUBSTITUTED ARYLPYRAZINES 审中-公开
标题翻译：取代的芳基
公开(公告)号：WO0160806A3
公开(公告)日：2002-02-07
申请号：PCT/US0105264
申请日：2001-02-16
申请人： NEUROGEN CORP , YOON TAEYOUNG , GE PING , HORVATH RAYMOND F , LOMBAERT STEPHANE DE , HODGETTS KEVIN J , DOLLER DARIO , ZHANG CUNYU
发明人： YOON TAEYOUNG , GE PING , HORVATH RAYMOND F , DE LOMBAERT STEPHANE , HODGETTS KEVIN J , DOLLER DARIO , ZHANG CUNYU
IPC分类号： A61K31/4965 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P9/10 , A61P9/12 , A61P15/00 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D241/00 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/04 , C07D241/52
CPC分类号： C07D401/04 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/5355 , C07D241/12 , C07D241/18 , C07D241/20 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/04
摘要： Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affiity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
摘要翻译：提供了芳基吡嗪化合物，包括可以以高亲和力和对CRF1受体（包括人类CRF1受体）的高选择性结合的芳基吡嗪。因此，本发明包括用于治疗与CRF1受体相关的疾病和疾病的方法，所述疾病和疾病包括CNS相关疾病和疾病，特别是情感障碍和疾病，以及急性和慢性神经障碍和疾病。

9. 发明申请

WO1996016655A1 NOVEL ENEDIYNE QUINONE IMINES AND METHODS OF PREPARATION AND USE THEREOF 审中-公开
标题翻译：新型ENEDIYNE QUINONE IMINES及其制备和使用方法
公开(公告)号：WO1996016655A1
公开(公告)日：1996-06-06
申请号：PCT/US1995015678
申请日：1995-12-01
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , SHAIR, Matthew, D. , YOON, Taeyoung , CHOU, Ting-Chao , MOSNY, Karoline, K.
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
IPC分类号： A61K31/47
CPC分类号： C07D491/08 , A61K47/6803 , A61K47/6809
摘要： A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R1, R2 and R3 are independently the same or different and are H, Br, Cl, F, NH2, CO2H, OH, linear or branched alkyl, etc.; wherein R4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R5 is H, Br, Cl, F, O=, OH or S-SR, or linear or branched alkyl, etc.; wherein R6 is H, Br, Cl, F, CO2H, OH or S-SR', or linear or branched alkyl, etc.; wherein R7 is H, OH or S-SR", or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R" are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumors.
摘要翻译：对具有通式（I）的具有通式结构（I）的癌细胞具有细胞毒性活性的醌亚胺enediyne，其中R 1，R 2和R 3独立地相同或不同，为H，Br，Cl，F，NH 2，CO 2 H，OH，直链或支链烷基等。其中R4是H，OH或直链或支链烷氧基，直链或支链烷氧基羰基等; 其中R 5为H，Br，Cl，F，O =，OH或S-SR，或直链或支链烷基等; 其中R6是H，Br，Cl，F，CO2H，OH或S-SR'，或直链或支链烷基等; 其中R 7是H，OH或S-SR“，或直链或支链烷基，直链或支链烷氧基羰基，直链或支链烷氧基或直链或支链羟烷基;其中R，R'和R”独立地相同或不同，直链或支链烷基，直链或支链酰基或直链或支链烷氧基烷基。还提供了化合物与可切割肽，酶，碳水化合物和与癌细胞免疫反应的单克隆抗体的缀合物，以及包含类似物和缀合物的组合物，以及合成和治疗肿瘤的方法。

10. 发明申请

WO2006004589A3 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES 审中-公开
标题翻译： 3-ARY-5,6-取代的吡咯烷
公开(公告)号：WO2006004589A3
公开(公告)日：2006-04-06
申请号：PCT/US2005016139
申请日：2005-05-06
申请人： NEUROGEN CORP , YOON TAEYOUNG , YUAN JUN , LEE KYUNGAE , MAYNARD GEORGE D , LIU NIAN
发明人： YOON TAEYOUNG , YUAN JUN , LEE KYUNGAE , MAYNARD GEORGE D , LIU NIAN
IPC分类号： C07D403/04 , A61K31/501 , A61K31/502 , A61K31/5377 , A61K31/55 , C07D403/14 , C07D405/04 , C07D405/14
CPC分类号： C07D237/20 , C07D237/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/04
摘要： The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
摘要翻译：本发明提供式（I）或（II）的盐形式或前药的化合物，其中变量在本文中定义，其是金属蛋白酶例如基质金属蛋白酶（MMP）和ADAM的调节剂。本文所述的化合物或组合物可用于治疗与金属蛋白酶活性相关的疾病，包括例如关节炎，癌症，心血管疾病，皮肤病症，炎症或过敏性疾病。

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