公开(公告)号：WO2018215070A1

公开(公告)日：2018-11-29

申请号：PCT/EP2017/062692

申请日：2017-05-24

申请人： JOHANN WOLFGANG GOETHE-UNIVERSITÄT FRANKFURT AM MAIN

发明人： MERK, Daniel ,  SCHMIDT, Jurema ,  PROSCHAK, Ewgenij ,  SCHUBERT-ZSILAVECZ, Manfred

IPC分类号： A61K31/192 ,  C07C255/60 ,  C07C311/08 ,  C07C311/46 ,  C07C311/51 ,  C07C317/32 ,  C07C321/28 ,  C07D257/04 ,  C07C233/73 ,  C07C233/76 ,  C07C233/78 ,  C07C233/87 ,  C07C235/52 ,  C07C237/30 ,  C07C237/36 ,  A61P3/06 ,  A61K31/166 ,  A61K31/18 ,  A61K31/277 ,  A61K31/41

摘要： The present invention pertains to novel dual modulators of farnesoid X receptor (FXR) and soluble epoxide hydrolase (sEH). The modulators of the invention were designed to provide compounds which harbor a dual activity as agonists of FXR and inhibitors (antagonists) of sEH. The invention also provides methods for treating subjects suffering from diseases associated with FXR and sEH, such as metabolic disorders, in particular non-alcoholic fatty liver or non-alcoholic steatohepatitis (NASH).

公开(公告)号：WO2018213699A1

公开(公告)日：2018-11-22

申请号：PCT/US2018/033382

申请日：2018-05-18

申请人： MEMORIAL SLOAN KETTERING CANCER CENTER

发明人： GOLDBERG, Jonathan ,  GOLDBERG, Elena ,  MA, Wenfu

IPC分类号： A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/185

摘要： The present disclosure provides compositions and methods for modifying endoplasmic reticulum trafficking of proteins. Also disclosed herein are methods for treating cancer and/or enhancing cancer or viral immunotherapy in a subject by increasing the extracellular secretion levels of GRP94 in the subject. Such methods comprise administering to the subject an effective amount of 4-PBA and/or a 4-PBA analog selected from among methoxy- PBA, 3-PPA, 5-PVA, hydroxy-PPA, hydroxy-PBA, and tolyl-BA.

公开(公告)号：WO2018212368A1

公开(公告)日：2018-11-22

申请号：PCT/KR2017/005061

申请日：2017-05-16

申请人： 연세대학교 산학협력단 ,  이화여자대학교 산학협력단

发明人： 김어수 ,  남궁기 ,  정지현 ,  장수아 ,  권영주 ,  전규연 ,  전경화

IPC分类号： C07C225/22 ,  C07C311/21 ,  C07D211/14 ,  C07D241/04 ,  A61K31/136 ,  A61K31/18 ,  A61K31/496

摘要： 본 발명은 신규 화합물 및 상기 화합물을 유효성분으로 포함하는 퇴행성 신경질환의 예방 또는 치료용 약학 조성물에 관한 것으로, 에이엠피-활성 단백질 키나아제 활성 효능 및 인 실리코상 결합능이 좋은 모체 구조에서 화학적 변형(chemical modification)을 진행하여 얻어진 신규 화합물은 에이엠피-활성 단백질 키나아제(AMP-activated protein kinase;AMPK) 효소 활성화를 효과적으로 유도하여 퇴행성 신경질환을 효과적으로 예방 또는 치료할 수 있다.

公开(公告)号：WO2018201146A1

公开(公告)日：2018-11-01

申请号：PCT/US2018/030251

申请日：2018-04-30

申请人： CASE WESTERN RESERVE UNIVERSITY ,  UNIVERSITY OF PITTSBURGH

发明人： PALCZEWSKI, Krzysztof ,  CHEN, Yuanyuan ,  LIPKOVICH, Holly

IPC分类号： A61K31/18 ,  A61K31/34 ,  A61K31/341 ,  A61K31/40 ,  A61K31/495 ,  A61P29/00

摘要： This application relates to compounds and methods of treating retinal degeneration associated with inherited rhodopsin mutations in the ocular tissue of a subject. The retinal degeneration, can include, for example, macular degeneration, including age-related macular degeneration, Stargardt disease, and retinitis pigmentosa. The retinitis pigmentosa can include autosomal dominate retinitis pigmentosa associated with a P23H RHO mutation. A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I), wherein the compound of formula (I) acts as a chaperone of rhodopsin.

公开(公告)号：WO2018188536A1

公开(公告)日：2018-10-18

申请号：PCT/CN2018/082188

申请日：2018-04-08

申请人： 成军

发明人： 成军

IPC分类号： A61K31/7084 ,  A61K31/675 ,  A61K31/18 ,  A61K31/20 ,  A61P1/16 ,  C12N15/85 ,  C12N15/12

CPC分类号： A01K67/02 ,  A61K31/18 ,  A61K31/20 ,  A61K31/675 ,  A61K31/7084 ,  A61K45/00 ,  A61K49/00 ,  A61P1/16 ,  C12N15/85 ,  C12N15/90

摘要： 提供了靶向NS5ATP9（HCV NS5A-transactivated protein 9）预防或治疗组织纤维化、组织硬化的药物的筛选方法，及使用上述方法筛选获得的药物。还提供了替诺福韦酯（TDF）、替诺福韦艾拉酚胺富马酸（TAF）或二者的衍生物在制备预防和/或治疗肝纤维化疾病药物中的用途。

公开(公告)号：WO2018161892A1

公开(公告)日：2018-09-13

申请号：PCT/CN2018/078136

申请日：2018-03-06

申请人： 中国药科大学 ,  南京大学

发明人： 赖宜生 ,  葛书山 ,  郑英博 ,  邹毅 ,  王芳 ,  徐强 ,  郭文洁 ,  王燕 ,  胡月

IPC分类号： C07C311/46 ,  C07C303/38 ,  C07C311/19 ,  C07C311/39 ,  C07C311/16 ,  C07C311/17 ,  A61K31/18 ,  A61K31/63 ,  A61P35/00 ,  A61P31/12 ,  A61P25/28

CPC分类号： C07C303/38 ,  C07C303/40 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/39 ,  C07C311/40 ,  C07C311/46 ,  C07D317/58 ,  Y02A50/465

摘要： 一种具有式(I)结构特征的苯磺酰胺类化合物或其药学上可接受的盐、其制备方法、以及它们作为吲哚胺2,3-双加氧酶1(IDO1)抑制剂的用途。实验结果表明，化合物对IDO1的活性具有显著抑制作用，能够有效地促进T细胞增殖，抑制初始T细胞分化成调节性T细胞，逆转IDO1介导的免疫抑制，可以用于治疗具有IDO1介导的犬尿氨酸代谢途径的病理学特征的相关疾病，包括癌症、病毒感染、神经变性疾病、白内障、器官移植排斥、抑郁症和自身免疫性疾病等。

公开(公告)号：WO2018144570A1

公开(公告)日：2018-08-09

申请号：PCT/US2018/016184

申请日：2018-01-31

申请人： EMORY UNIVERSITY ,  NEUROPN THERAPEUTICS

发明人： SANDS, Jeff ,  KLEIN, Janet ,  KHANNA, Ish ,  PILLARISETTI, Sivaram

IPC分类号： A61K31/155 ,  A61K31/167 ,  A61K31/17 ,  A61K31/18 ,  A61K31/198 ,  A61K31/216

摘要： In certain embodiments, this disclosure relates to methods of treating or preventing nephrogenic diabetes insipidus comprising administering an effective amount of a compound of Formula (I) or derivatives thereof, as described herein, to a subject in need thereof. In certain embodiments, the subject has been diagnosed with nephrogenic diabetes insipidus.

公开(公告)号：WO2018118711A1

公开(公告)日：2018-06-28

申请号：PCT/US2017/066822

申请日：2017-12-15

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： STOCKWELL, Brent R.

IPC分类号： A61K31/15 ,  A61K31/18 ,  C07C13/567

摘要： The present invention provides, inter alia , a compound according to formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for regulating GPX4 in a cell and methods for inducing ferroptosis in a cell.

公开(公告)号：WO2018111619A1

公开(公告)日：2018-06-21

申请号：PCT/US2017/064654

申请日：2017-12-05

申请人： IMPRIMIS PHARMACEUTICALS, INC.

发明人： SAADEH, Dennis, Elias ,  BAUM, Mark, L.

IPC分类号： A61K31/015 ,  A61K31/047 ,  A61K31/18 ,  A61K31/21 ,  A61K31/381 ,  A61K31/4168 ,  C07D233/20 ,  C07D265/30 ,  C07D285/06

摘要： Pharmaceutical compositions for treating or mitigating glaucoma are described, the compositions comprising several separate components for an improved effect. Methods for fabricating the compositions and using them are also described.

公开(公告)号：WO2018098353A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/063120

申请日：2017-11-22

申请人： CHEMOCENTRYX, INC.

发明人： MIAO, Zhenhua ,  SCHALL, Thomas ,  SINGH, Rajinder

IPC分类号： A61K31/18 ,  A61K31/44 ,  A61K31/437 ,  C07D213/24 ,  C07D213/30 ,  C07D213/44

摘要： A method of treating focal segmental glomerulosclerosis with a compound of Formula I is provided. FSGS may be primary (no known cause) or secondary. The secondary FSGS may be associated with infections or viruses such as HIV, diseases such as sickle cell disease or lupus, toxins or drugs such as anabolic steroids, heroin or pamidronate, nephron loss and hyperfiltration, such as with chronic pyelonephritis and reflux, morbid obesity, or diabetes mellitus.