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81. 发明申请

WO2019148471A1 FG-4592或其盐的新用途以及药品和保健品审中-公开
公开(公告)号：WO2019148471A1
公开(公告)日：2019-08-08
申请号：PCT/CN2018/075174
申请日：2018-02-02
申请人：中国人民解放军军事科学院军事医学研究院
发明人：朱玲玲 , 周延召 , 赵彤 , 赵名 , 范明 , 吴海涛
IPC分类号： A61K31/472 , A61P25/00 , A61P25/28 , A61P25/16 , A61P9/00 , C07D217/16 , A23L33/00
摘要：本发明涉及本发明涉及FG-4592的新用途以及药品和保健品。所述新用途是FG-4592或其药学上可接受的盐在制备治疗和/或预防神经损伤疾病或神经退行性疾病产品中的用途。所述产品可为药品和/或保健品。克服了目前FG-4592只用于治疗贫血的应用中的局限性，所述FG-4592能够明显提高APP/PS1转基因小鼠的空间记忆功能，改善其认知功能的下降的情况，可用于治疗早期认知功能损伤、中风、阿尔茨海默病、认知功能障碍、血管性痴呆、帕金森氏病等。

82. 发明申请

WO2019069973A1 含窒素ヘテロアリール化合物およびその医薬用途审中-公开
公开(公告)号：WO2019069973A1
公开(公告)日：2019-04-11
申请号：PCT/JP2018/037007
申请日：2018-10-03
申请人：日本たばこ産業株式会社
发明人：長森　弘将 , 西丸　達也 , ▲高▼木　正樹 , 三谷　育生 , 中川　祐一
IPC分类号： C07D213/55 , A61K31/4418 , A61K31/4433 , A61K31/472 , A61K31/4965 , A61K31/497 , A61P19/06 , A61P43/00 , C07D213/61 , C07D217/16 , C07D241/12 , C07D405/04
摘要：本発明は、GLUT9阻害活性を有する化合物を提供する。　本発明は、式[I]の化合物またはその製薬上許容される塩を提供する。（式中の記号は明細書における定義と同義である）

83. 发明申请

WO2017153519A1 3-OXA-8-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AND THIER USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES 审中-公开
标题翻译： 3-氧杂-8-氮杂环庚烯[3.2.1]辛烷衍生物及其在治疗癌症和血红蛋白病中的用途
公开(公告)号：WO2017153519A1
公开(公告)日：2017-09-14
申请号：PCT/EP2017/055536
申请日：2017-03-09
申请人： CTXT PTY LIMITED
发明人： STUPPLE, Paul Anthony
IPC分类号： C07D217/16 , A61K31/4725 , A61K31/5386 , C07D498/08 , A61P35/00 , A61P7/06
摘要： A compound of formula Ia, Ib, Ic or Id: wherein: n is 1 or 2;R N is H or Me; R 1 is optionally one or more halo or methyl groups;R 2a and R 2b are independently selected from the group consisting of: (i) F; (ii) H;(iii) Me; and (iv) CH 2 OH; R 2c and R 2d (if present) are independently selected from the group consisting of: (i) F; (ii) H;(iii) Me; and(iv) CH 2 OH;R 3a and R 3b are independently selected from H and Me; R 4a is selected from OH,-NH 2 , -C(=O)NH 2 , and -CH 2 OH; R 4b is either H or Me; R 5 is either H or Me; m is 1 or 2; q is 0 or 1;R 11a , R 11b , R 11c and R 11d are independently selected from H, halo, C 1-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, C 1-4 alkyloxy, NH-C 1-4 alkyl and cyano; R 12a and R 12b are independently selected from the group consisting of: (i) F; (ii) H;(iii) Me; and (iv) CH 2 OH; R 12c and R 12d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH;R 12e is H or Me; R 13a and R 13b are independently selected from H and Me; R 14 is either H or Me; R 16a and R 16b are independently selected from H and Me; R 6 is selected from H, OMe, and OEt.
摘要翻译：式Ia，Ib，Ic或Id的化合物：其中：n是1或2; R N是H或Me; R 1任选地为一个或多个卤素或甲基; R 2a和R 2b独立地选自：（i） F; （ii）H;（iii）我; 和（iv）CH 2 OH; R 2c和R 2d（如果存在）独立地选自：（i）F; （ii）H;（iii）我; 和（iv）CH 2 OH：R 3a和R 3b独立地选自H和Me; R 4a选自OH，-NH 2 2，-C（= O）NH 2和-CH 2， OH; R 4b是H或Me; R 5是H或Me; m是1或2; q是0或1; R 11a，R 11b，R 11c和R 11d独立地选自H ，卤素，C 1-4烷基，C 1-4氟代烷基，C 3-4环烷基，C 1-4芳基，烷氧基，NH-C 1-4烷基和氰基; R 12a和R 12b独立地选自：（i）F; （ii）H;（iii）我; 和（iv）CH 2 OH; R 12c和R 12d独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH：R 12e是H或Me; R 13a和R 13b独立地选自H和Me; R 14是H或Me; R 16a和R 16b独立地选自H和Me; R 6选自H，OMe和OEt。

84. 发明申请

WO2017153513A1 TETRAHYDROISOQUINOLINES AS PRMT5 INHIBITORS 审中-公开
标题翻译：四氢异喹啉作为PRMT5抑制剂
公开(公告)号：WO2017153513A1
公开(公告)日：2017-09-14
申请号：PCT/EP2017/055529
申请日：2017-03-09
申请人： CTxT PTY LIMITED
发明人： BERGMAN, Ylva Elisabet , CAMERINO, Michelle Ang , WALKER, Scott Raymond , STUPPLE, Paul Anthony
IPC分类号： C07D401/14 , C07D405/14 , C07D217/16 , C07D401/12 , C07D413/12 , C07D471/04 , C07D498/08 , A61K31/4725 , A61K31/437 , A61P7/00 , A61P35/00
摘要： A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R 1a , R 1b , R 1c and R 1d are independently selected from the group consisiting of H, halo, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, NH-C 1-4 alkyl and cyano; R 2a and R 2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2c and R 2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH 2 OH; R 2e is H or Me; R 3a and R 3b are independently selected from H and Me; R 4 is either H or Me; R 5 is either H or Me; R 6a and R 6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C 5-12 heteroaryl; wherein when R 2e is H, at least one of R 1a , R 1b , R 1c and R 1d is selected from C 1-4 alkoxy, C 2-4 alkyl, C 1-4 fluoroalkyl, C 3-4 cycloalkyl, NH-C 1-4 alkyl and cyano.
摘要翻译：式（I）的化合物，其中：n是1或2; p是0或1; R 1a，R 1b，R 1c和R 1d独立地选自H，卤素，C 1-4烷氧基，C 1-4烷基，C 1-4氟代烷基，C 3-4 - / - 亚烷基 NH 2 -C 1-4烷基和氰基; R 2a和R 2b独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2c和R 2d独立地选自：（i）F; （ii）H; （iii）我; 和（iv）CH 2 OH; R 2e是H或Me; R 3a和R 3b独立地选自H和Me; R 4是H或Me; R 5是H或Me; R 6a和R 6b独立地选自H和Me; A是（i）任选取代的苯基; （ii）任选取代的萘基; 或（iii）任选取代的C 5-12杂芳基; 其中当R 2ee为H时，R 1a，R 1b，R 1c和R 1b中至少一个为氢，其中1d选自C 1-4烷氧基，C 2-4烷基，C 1-4氟代烷基，C 3-4环烷基，NH-C 1-4烷基和氰基

85. 发明申请

WO2017087608A8 MODULATORS OF ROR-GAMMA 审中-公开
标题翻译： ROR-GAMMA调制器
公开(公告)号：WO2017087608A8
公开(公告)日：2017-05-26
申请号：PCT/US2016/062422
申请日：2016-11-17
申请人： VITAE PHARMACEUTICALS, INC.
发明人： CLAREMON, David, A. , DILLARD, Lawrence, Wayne , FAN, Yi , JIA, Lanqi , SINGH, Suresh, B. , TICE, Colin, M. , XU, Zhenrong , YUAN, Jing , ZHUANG, Linghang
IPC分类号： C07D401/14 , C07D217/04 , C07D217/16 , C07D217/24 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D239/88 , C07D471/04 , C07D495/04
摘要： Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
摘要翻译：所提供的是式I的新化合物：其药学上可接受的盐及其药物组合物，其可用于治疗由RORγ介导的疾病和病症。还提供了包含式I的新化合物的药物组合物及其用于治疗一种或多种炎性，代谢性，自身免疫性和其他疾病或病症的方法。

86. 发明申请

WO2017035288A1 COMPOSITION AND METHOD FOR PREVENTION, MITIGATION OR TREATMENT OF AN ENTEROPATHOGENIC BACTERIAL INFECTION 审中-公开
标题翻译：预防，减轻或治疗肠道致病菌感染的组合物和方法
公开(公告)号：WO2017035288A1
公开(公告)日：2017-03-02
申请号：PCT/US2016/048517
申请日：2016-08-25
申请人： TRUSTEES OF DARTMOUTH COLLEGE
发明人： KULL, F., Jon , TAYLOR, Ronald, K. , GRIBBLE, Gordon, W. , ONYANGO, Evans, O. , KELLEY, Anne, R.
IPC分类号： C07D209/18 , C07D215/14 , C07D217/16 , C07C57/50 , C07C57/40 , A61K31/405 , A61K31/47 , A61K31/192 , A61P31/04
CPC分类号： A61K31/192 , A61K31/405 , A61K31/47 , C07C53/136 , C07C57/40 , C07C57/42 , C07C57/50 , C07C2602/10 , C07C2602/28 , C07D209/12 , C07D217/16
摘要： Provided herein are bicyclic compounds for decreasing the expression of bacterial virulence factors thereby preventing, mitigating, or treating bacterial infection,
摘要翻译：本文提供的是用于减少细菌毒力因子的表达从而预防，缓解或治疗细菌感染的双环化合物，

87. 发明申请

WO2014193781A1 3,4-DIHYDROISOQUINOLIN-2(1H)-YL COMPOUNDS 审中-公开
标题翻译： 3,4-二氢喹啉-2（1H） - 甲基化合物
公开(公告)号：WO2014193781A1
公开(公告)日：2014-12-04
申请号：PCT/US2014/039494
申请日：2014-05-27
申请人： ELI LILLY AND COMPANY
发明人： BEADLE, Christopher David , COATES, David Andrew , HAO, Junliang , KRUSHINSKI JR., Joseph Herman , REINHARD, Matthew Robert , SCHAUS, John Mehnert , WOLFANGEL, Craig Daniel
IPC分类号： C07D217/16 , A61K31/472 , A61P25/16 , A61P25/18
CPC分类号： C07D217/16
摘要： The invention provides certain 3,4-dihydroisoquinolin-2(1H)-yl compounds, particularly compounds of formula (I), and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula (I) to treat cognitive impairment associated with Parkinson's disease or schizophrenia.
摘要翻译：本发明提供某些3,4-二氢异喹啉-2（1H） - 基化合物，特别是式（I）化合物及其药物组合物。本发明还提供使用式（I）化合物治疗与帕金森病或精神分裂症相关的认知障碍的方法。

88. 发明申请

WO2014100730A1 PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE AND USES THEREOF 审中-公开
标题翻译：含有二氢或四氢喹啉的PRMT5抑制剂及其用途
公开(公告)号：WO2014100730A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/077250
申请日：2013-12-20
申请人： EPIZYME, INC.
发明人： DUNCAN, Kenneth, W. , CHESWORTH, Richard , BORIACK-SJODIN, Paula, Ann , MUNCHHOF, Michael, John , JIN, Lei
IPC分类号： C07D401/14 , C07D405/14 , C07D217/16 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/502 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/497 , A61K31/498 , A61K31/472 , A61K31/4725
CPC分类号： C07D413/12 , A61K31/472 , A61K31/4725 , A61K31/497 , A61K31/498 , A61K31/502 , A61K31/517 , A61K31/5377 , A61K31/538 , C07D217/04 , C07D217/08 , C07D217/16 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D417/12
摘要： Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5- mediated disorders are also described.
摘要翻译：本文描述了式（A）的化合物，其药学上可接受的盐及其药物组合物。本发明的化合物可用于抑制PRMT5活性。还描述了使用该化合物治疗PRMT5介导的病症的方法。

89. 发明申请

WO2014074775A1 HETEROARYL DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： HETEROARYL衍生物及其用途
公开(公告)号：WO2014074775A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/069056
申请日：2013-11-08
申请人： JACOBUS PHARMACEUTICAL COMPANY, INC.
发明人： HEFFERNAN, Gavin, David , JACOBUS, David, Penman , SAIONZ, Kurt, William , SCHIEHSER, Guy, Alan , SHIEH, Hong-Ming , ZHAO, Wenyi
IPC分类号： C07D213/73 , C07D213/84 , C07D213/38 , C07D213/65 , C07D333/58 , C07D215/14 , C07D333/28 , C07D401/10 , C07D239/26 , C07D413/04 , C07D241/12 , C07D213/12 , C07D213/61 , C07D307/80 , C07D213/36 , A61K31/343 , A61K31/381 , A61K31/44 , A61K31/47 , A61K31/505 , C07D217/16
CPC分类号： C07D413/04 , A61K31/343 , A61K31/381 , A61K31/415 , A61K31/4418 , A61K31/4439 , A61K31/47 , A61K31/496 , A61K31/505 , A61K31/536 , A61K31/5377 , A61K45/06 , C07D213/36 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/84 , C07D215/14 , C07D217/16 , C07D231/12 , C07D239/26 , C07D241/12 , C07D307/80 , C07D307/81 , C07D333/28 , C07D333/58 , C07D401/10 , Y02A50/411
摘要： The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium , including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
摘要翻译：本发明涉及抗疟疾化合物及其抗疟原虫原生动物的用途，包括耐药性Plasmodia菌株。本发明还涉及含有这些化合物的组合物和制备该化合物的方法。

90. 发明申请

WO2013132253A1 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 3-氨基-5-取代的异喹啉-1-酮化合物及其治疗用途
公开(公告)号：WO2013132253A1
公开(公告)日：2013-09-12
申请号：PCT/GB2013/050561
申请日：2013-03-07
申请人： INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： ASHWORTH, Alan , LORD, Christopher James , ELLIOTT, Richard James Rowland , NICULESCU-DUVAZ, Dan , PORTER, Roderick , BOFFEY, Raymond John , BAYFORD, Melanie Jayne , FIRTH-CLARK, Stuart , JARVIS, Ashley Nicholas , PERRIOR, Trevor Robert , KEY, Rebekah Elisabeth
IPC分类号： A61P35/00 , A61K31/472 , C07D401/14 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/12 , C07D487/04 , C07D487/08 , C07D487/10 , A61K31/4725 , A61K31/496 , A61K31/506
CPC分类号： C07D217/24 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/04 , C07D487/08 , C07D487/10
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及特别是抑制PARP（例如PARP1，TNKS1，TNKS2等）和/或Wnt信号传导的某些3-芳基-5-取代-2H-异喹啉-1-酮化合物。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制PARP（例如PARP1，TNKS1，TNKS2等）的用途; 抑制Wnt信号; 治疗通过抑制PARP而改善的疾病（例如PARP1，TNKS1，TNKS2等）; 治疗通过抑制Wnt信号传导而改善的病症; 治疗癌症等增殖性疾病

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