公开(公告)号：WO2022015974A2

公开(公告)日：2022-01-20

申请号：PCT/US2021/041816

申请日：2021-07-15

Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, INC.

Inventor： POTTS, Ryan ,  CHEN, Taosheng ,  RANKOVIC, Zoran ,  MIN, Jaeki ,  LIN, Wenwei ,  YANG, Seung Wook ,  MAYASUNDARI, Anand

IPC: A61K31/47 ,  A61K31/4706 ,  A61K38/00 ,  A61P35/00 ,  C07D215/46 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07K14/47 ,  C07K14/4748

Abstract: Testis-restricted melanoma antigen (MAGE) proteins are frequently hijacked in cancer and play a critical role in tumorigenesis. These proteins assemble with E3 ubiquitin ligases and function as substrate adaptors that direct the ubiquitination of novel targets, including key tumor suppressors. However, the development of MAGE-directed therapeutics heretofore has been extremely limited. In one aspect, the disclosure relates to compounds and peptides useful as inhibitors of MAGE-A11:substrate interaction, methods of making same, pharmaceutical compositions comprising same, and methods of treating a disorder associated with a MAGE-A11 dysfunction, e.g., a cancer, using same. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

公开(公告)号：WO2021217574A1

公开(公告)日：2021-11-04

申请号：PCT/CN2020/088241

申请日：2020-04-30

Applicant: WATERSTONE PHARMACEUTICALS (WUHAN) CO., LTD.

Inventor： CUI, Jian ,  HU, Minglong ,  LIANG, Ying ,  YU, Yao ,  MENG, Yuan ,  LI, Tongtong ,  ZHAO, Along ,  ZHANG, Faming

IPC: C07D215/46 ,  A61K31/4706 ,  A61P31/14

Abstract: A method of treating or preventing a Coronaviridae infection in a subject comprising administrating a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof to the subject in need thereof, wherein R1 is OH or H, and the Coronaviridae comprises at least one selected from 2019-nCov virus, HCov 229E virus, SARS virus, MERS virus.

公开(公告)号：WO2020193448A1

公开(公告)日：2020-10-01

申请号：PCT/EP2020/057914

申请日：2020-03-23

Applicant: UNIVERSITAT DE BARCELONA

Inventor： MUÑOZ-TORRERO LÓPEZ-IBARRA, Diego ,  VÁZQUEZ CRUZ, Santiago ,  PONT MASANET, Caterina ,  CODONY GISBERT, Sandra

IPC: A61K31/4706 ,  A61P25/28 ,  C07D215/46 ,  C07D401/12

Abstract: The invention provides compounds of formula I wherein: m is 0, 1 or 2; n is 2, 3, 4 or 5; R 0 and R 1 are both H, or they form a bridge -CH 2 -C(R 4 )=CH-, R 4 being CH 3 or CH 2 CH 3 ; R 2 and R 3 independently are H, F, Cl or (C 1 -C 4 )-alkyl; R 5 is H, F, Cl, Br, I, OCH 3 , OCF 3 , SF 5 , SO 2 F, SO 2 CH 3 , NO 2 , CF 3 or (C 1 -C 4 )-alkyl; R 6 and R 7 independently are H, F, Cl, CH 3 or CF 3 ; and optionally R 5 and R 6 form a bridge -O-CH 2 -O-, R 7 being H, in vitro assays show that compounds I are simultaneously inhibitors of acetylcholinesterase and inhibitors of soluble epoxide hydrolase, and that they have a good blood-brain barrier permeability. Thus, compounds I are multitarget active pharmaceutical ingredients for the treatment of Alzheimer's disease in humans.

公开(公告)号：WO2015192198A1

公开(公告)日：2015-12-23

申请号：PCT/CA2014/000816

申请日：2014-11-14

Applicant: THE HOSPITAL FOR SICK CHILDREN

Inventor： KIM, Peter, K.

IPC: A61K31/4706 ,  A61K31/198 ,  A61K31/352 ,  A61K31/365 ,  A61K31/55 ,  A61P25/00 ,  A61P3/00 ,  C07D215/46 ,  C07D311/58 ,  C07D407/06

CPC classification number: A61K31/7048 ,  A61K31/198 ,  A61K31/352 ,  A61K31/365 ,  A61K31/382 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/409 ,  A61K31/4706 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/58 ,  A61K31/675

Abstract: A method is described for treating a peroxisome biogenesis disorder by administering to an individual in need thereof an effective amount of an autophagy inhibitor. Uses, compositions, and commercial packages are also described. The peroxisome biogenesis disorder may be Zellweger syndrome, neonatal adrenoleukodystrophy, Refsum disease, or cerebrohepatorenal syndrome. The autophagy inhibitor may be chloroquine diphosphate; hydroxychloroquine sulfate; verteporfin; difluoromethylornithine; clarithromycin; clomipramine; desmethylclomipramine hydrochloride, anisomycin; Spautin-1; U0126; SP600125; Wortmannin; LY294002; Bafilomycin; Forskolin; Melatonin; 1-((2- (diethylamino)ethyl)amino)-4-methylthioxanthen-9-one; 1-(2-diethylaminoethylamino)-4- (hydroxymethyl)-9-thioxanthenone; or N-[[1-[[2- (diethylamino)ethyl]amino]-9-oxo-9H- thiaxanthen-4-yl]methyl]methanesulfonamide.

Abstract translation: 描述了通过向有需要的个体施用有效量的自噬抑制剂来治疗过氧化物酶体生物发生障碍的方法。 还描述了使用，组合物和商业包装。 过氧化物酶体生物发生障碍可能是泽尔韦格综合征，新生儿肾上腺脑白质营养不良，精神病或脑血管综合征。 自噬抑制剂可以是二磷酸氯喹; 硫酸羟氯喹; 维替泊芬; 二氟; 克拉霉素; 氯米帕明; 盐酸去甲基丙咪嗪，茴香霉素; Spautin-1; U0126; SP600125; 渥曼青霉素; LY294002; 洛霉素; 毛喉素; 褪黑激素; 1 - （（2-（二乙基氨基）乙基）氨基）-4-甲基噻吨-9-酮; 1-（2-二乙氨基乙氨基）-4-（羟甲基）-9-噻吨酮; 或N - [[1 - [[2-（二乙基氨基）乙基]氨基] -9-氧代-9H-噻吩-4-基]甲基]甲磺酰胺。

公开(公告)号：WO2015054572A1

公开(公告)日：2015-04-16

申请号：PCT/US2014/060036

申请日：2014-10-10

Applicant: ARAXES PHARMA LLC ,  LI, Liansheng ,  FENG, Jun ,  WU, Tao ,  REN, Pingda ,  LIU, Yi ,  LIU, Yuan ,  LONG, Yun, Oliver

Inventor： LI, Liansheng ,  FENG, Jun ,  WU, Tao ,  REN, Pingda ,  LIU, Yi ,  LIU, Yuan ,  LONG, Yun, Oliver

IPC: C07D239/94 ,  C07D403/12 ,  C07D215/46 ,  C07D215/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D237/28 ,  C07D409/04 ,  C07D409/14 ,  C07D417/10 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/94 ,  C07D215/46 ,  C07D215/54 ,  C07D231/56 ,  C07D237/28 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/10 ,  C07D417/12 ,  C07D487/04 ,  C07D495/04

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R 1 , R 2a , R 3a , R 3b , R 4a , R 4b , G 1 , G 2 , L 1 , L 2 , m 1 , m 2 , A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract translation: 提供具有作为G12C突变体KRAS蛋白质的抑制剂的活性的化合物。 化合物具有以下结构（I）：或其药学上可接受的盐，互变异构体，前药或立体异构体，其中R1，R2a，R3a，R3b，R4a，R4b，G1，G2，L1，L2，m1，m2， B，W，X，Y，Z和E如本文所定义。 还提供了与这种化合物的制备和使用相关的方法，包含这些化合物的药物组合物和调节G12C突变型KRAS蛋白质用于治疗疾病如癌症的活性的方法。

公开(公告)号：WO2009117381A3

公开(公告)日：2009-12-23

申请号：PCT/US2009037346

申请日：2009-03-17

Applicant: REDDYS LAB LTD DR ,  REDDYS LAB INC DR ,  BOLLIKONDA SATYANARAYANA ,  KANDIRELLI KIRANKUMAR VENKATA ,  MEDISETTI RAMA KRISHNA VENKATA ,  KOPPARAPU JANARDANA SARMA RAMA ,  MANUDHANE KUSHAL SURAJMAL

Inventor： BOLLIKONDA SATYANARAYANA ,  KANDIRELLI KIRANKUMAR VENKATA ,  MEDISETTI RAMA KRISHNA VENKATA ,  KOPPARAPU JANARDANA SARMA RAMACHANDRA ,  MANUDHANE KUSHAL SURAJMAL

IPC: C07D215/18 ,  C07D215/16 ,  C07D215/46

CPC classification number: C07D215/18

Abstract: Processes for preparing montelukast acid and its salts.

Abstract translation: 制备孟鲁司特酸及其盐的方法。

公开(公告)号：WO2008155468A1

公开(公告)日：2008-12-24

申请号：PCT/FI2008/050381

申请日：2008-06-19

Applicant: LAIHO, Marikki ,  PELTONEN, Karita

Inventor： LAIHO, Marikki ,  PELTONEN, Karita

IPC: C07D471/04 ,  C07D487/04 ,  C07D215/46 ,  C07D495/14 ,  C07D239/88 ,  A61K31/4162 ,  A61K31/4985 ,  A61K31/381 ,  A61K31/4196 ,  A61K31/498 ,  A61K31/4375 ,  A61P35/00

CPC classification number: C07D215/54 ,  A61K31/519

Abstract: The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules.

Abstract translation: 本发明提出鉴定作为肿瘤抑制蛋白p53途径的激活剂的小分子化合物及其相关家族成员p63和p73的功能的方法。 本发明进一步涉及杀死肿瘤细胞和治疗癌症或其他需要激活p53家族成员途径和DNA损伤应答途径的条件与小分子的方法。

公开(公告)号：WO2007109251A3

公开(公告)日：2007-12-13

申请号：PCT/US2007006874

申请日：2007-03-20

Applicant: AVANIR PHARMACEUTICALS ,  SIRCAR JAGADISH ,  KUMAR SUNIL K C ,  DAVIS TIMOTHY JAMES ,  YING WENBIN ,  NUSSBAUMER PETER ,  BILLICH ANDREAS

Inventor： SIRCAR JAGADISH ,  KUMAR SUNIL K C ,  DAVIS TIMOTHY JAMES ,  YING WENBIN ,  NUSSBAUMER PETER ,  BILLICH ANDREAS

IPC: C07D215/46 ,  A61K31/4709 ,  A61P31/00 ,  A61P35/00 ,  C07D401/06 ,  C07D409/12 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04

CPC classification number: C07D215/46 ,  C07D401/06 ,  C07D409/12 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04

Abstract: Inhibitors of tumor necrosis factor alpha are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with tumor necrosis factor alpha. The inhibitors of tumor necrosis factor alpha have the following structures: (I) including stereoisomers, pharmaceutically acceptable salts, and solvates thereof, wherein substituents are as defined herein. Compositions containing an inhibitor of tumor necrosis factor alpha in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract translation: 提供了肿瘤坏死因子α的抑制剂，其可用于治疗各种疾病，包括治疗与肿瘤坏死因子α相关的病理状况。 肿瘤坏死因子α的抑制剂具有以下结构：（I）包括其立体异构体，药学上可接受的盐和溶剂化物，其中取代基如本文所定义。 还提供了含有肿瘤坏死因子α抑制剂以及药学上可接受的载体的组合物，以及使用它们的方法。

公开(公告)号：WO2007117161A1

公开(公告)日：2007-10-18

申请号：PCT/NZ2007/000077

申请日：2007-04-04

Applicant: AUCKLAND UNISERVICES LIMITED ,  DENNY, William, Alexander ,  BAGULEY, Bruce, Charles ,  MARSHALL, Elaine, Shirley ,  SUTHERLAND, Hamish, Scott

Inventor： DENNY, William, Alexander ,  BAGULEY, Bruce, Charles ,  MARSHALL, Elaine, Shirley ,  SUTHERLAND, Hamish, Scott

IPC: C07D407/04 ,  C07D239/94 ,  C07D409/04 ,  A61K31/4706 ,  C07D401/04 ,  C07D409/06 ,  A61K31/517 ,  C07D401/06 ,  C07D413/04 ,  C07D215/44 ,  C07D403/04 ,  C07D413/06 ,  C07D215/46 ,  C07D403/06 ,  C07D417/04 ,  C07D217/22 ,  C07D405/04 ,  C07D417/06 ,  C07D239/86 ,  C07D405/06 ,  G01N33/53 ,  C07D239/91 ,  C07D407/06

CPC classification number: C07D405/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  G01N33/5011

Abstract: The present invention relates to substituted ring fused azines and methods of using said compounds in treating cancers. More specifically, the present invention relates to the preparation of 4-alkyl-2-(heterocyclic)-azines and their use as cancer agents or drugs for cancer therapy. The compounds of the invention display favourable in vivo and in vitro activity against selected cancers.

Abstract translation: 本发明涉及取代的环稠合吖嗪和使用所述化合物治疗癌症的方法。 更具体地，本发明涉及4-烷基-2-（杂环） - 嗪的制备及其作为癌症治疗剂或癌症治疗药物的用途。 本发明的化合物对选定的癌症显示有利的体内和体外活性。

公开(公告)号：WO2006008133A3

公开(公告)日：2006-03-23

申请号：PCT/EP2005007846

申请日：2005-07-19

Applicant: SIENA BIOTECH SPA ,  GAVIRAGHI GIOVANNI ,  GHIRON CHIARA ,  BOTHMANN HENDRICK ,  RONCARATI RENZA ,  TERSTAPPENN GEORG CHRISTIAN

Inventor： GAVIRAGHI GIOVANNI ,  GHIRON CHIARA ,  BOTHMANN HENDRICK ,  RONCARATI RENZA ,  TERSTAPPENN GEORG CHRISTIAN

IPC: C07D295/12 ,  A61K31/445 ,  A61P25/28 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/46 ,  C07D243/08 ,  C07D295/14 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D213/40 ,  C07D209/08 ,  C07D209/18 ,  C07D211/52 ,  C07D211/60 ,  C07D213/56 ,  C07D213/82 ,  C07D215/38 ,  C07D217/04 ,  C07D239/26 ,  C07D243/08 ,  C07D295/13 ,  C07D295/15 ,  C07D295/185 ,  C07D319/18 ,  C07D333/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12

Abstract: The present invention relates to compounds with a7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.

Abstract translation: 本发明涉及具有α7nAChR激动活性的化合物，其制备方法，含有该化合物的药物组合物及其用于治疗神经，精神，认知，免疫和炎症疾病的用途。