公开(公告)号：WO2022056238A1

公开(公告)日：2022-03-17

申请号：PCT/US2021/049826

申请日：2021-09-10

Applicant: TERNS PHARMACEUTICALS, INC.

Inventor： WANG, Yujin ,  SHU, Chutian ,  GUO, Sheng ,  DUAN, Matt ,  BIAN, Jianwei ,  DENG, Jiaxin ,  SI, Aiyong

IPC: A61K31/55 ,  C07D405/00

Abstract: Provided herein are pharmaceutical compositions comprising a substantially amorphous form of 6-(4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)piperi din-1-yl)-1- methyl-1H-indole-3-carboxylic acid, such as solid dispersions of 6-(4-((5-cyclopropyl-3-(2,6- dichlorophenyl)isoxazol-4-yl)methoxy)piperidin-1 -yl)-1-methyl-1H-indole-3-carboxylic acid; methods of preparation thereof, and methods of use thereof.

公开(公告)号：WO2021092172A

公开(公告)日：2021-05-14

申请号：PCT/US2020/059109

申请日：2020-11-05

Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. [US]/[US] ,  UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL [US]/[US]

Inventor： XIE, Jin ,  KUMAR, Anil ,  LI, Zibo

IPC: A61K31/33 ,  A61K31/395 ,  A61K47/50 ,  C07D401/00 ,  C07D405/00 ,  C07D471/04

Abstract: Radiosensitizer prodrugs and formulations and methods of use thereof are provided. Typically, the radiosensitizer prodrug is an analog of a radiosensitizer parent compound having one or more S-nitrosothiol moieties. Typically, the S-N bond of the S-nitrosothiol moiety can be cleaved by radiation during radiotherapy, releasing the parent compound and nitric oxide. One or preferably both the parent compound and the nitric oxide can contribute to death of tumor cells exposed to radiotherapy. Nanoparticle formulations for delivery of the prodrug, and methods of using them in combination with radiotherapy to treat tumors and cancer are also provided.

公开(公告)号：WO2021057890A1

公开(公告)日：2021-04-01

申请号：PCT/CN2020/117670

申请日：2020-09-25

Applicant: 南京明德新药研发有限公司

Inventor： 杨亚讯 ,  江志赶 ,  夏建华 ,  魏巍 ,  贺海鹰 ,  陈曙辉

IPC: C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D413/14 ,  C07D471/04 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505

Abstract: 一类带有吡嗪结构的化合物，具体公开了式(VII)所示化合物、其异构体或其药学上可接受的盐，及其在制备CRAC抑制剂中的应用。

公开(公告)号：WO2019232449A9

公开(公告)日：2019-12-05

申请号：PCT/US2019/035015

申请日：2019-05-31

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： PAZOLLI, Ermira ,  BUONAMICI, Silvia ,  SAMARAKOON, Thiwanka ,  PRAJAPATI, Sudeep ,  FISHKIN, Nathan ,  PALACINO, James ,  SEILER, Michael ,  ZHU, Ping ,  COOK, Andrew ,  SMITH, Peter ,  LIU, Xiang ,  ELLERY, Shelby ,  REYNOLDS, Dominic ,  YU, Lihua ,  WU, Zhenhua ,  PENG, Shouyong ,  CALANDRA, Nicholas ,  SHEEHAN, Megan ,  XIAO, Yonghong

IPC: A61K47/68 ,  A61P35/00 ,  C07D405/00 ,  A61K39/00 ,  C07K7/00 ,  C07K14/00

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

公开(公告)号：WO2018127846A1

公开(公告)日：2018-07-12

申请号：PCT/IB2018/050095

申请日：2018-01-06

Applicant: LAURUS LABS LIMITED

Inventor： BOLLU, Ravindra Babu ,  DALASINGH, Prasanta Kumar ,  DWARAMPUDI, Sushmita ,  ANNEM, Chandrahasa Reddy ,  VASIREDDI, Uma Maheswer Rao

IPC: C07D405/00 ,  A61K31/00

Abstract: The present invention generally relates to crystalline forms of Lumacaftor, processes for its preparation and pharmaceutical compositions thereof. The present invention also relates to an improved process for preparation of Lumacaftor.

公开(公告)号：WO2014085545A1

公开(公告)日：2014-06-05

申请号：PCT/US2013/072172

申请日：2013-11-27

Applicant: THE UNIVERSITY OF CHICAGO

Inventor： BUDKE, Brian ,  KALIM, Jay, H. ,  PAWLOKSKI, Michal ,  KOZIKOWSKI, Alan, P. ,  CONNELL, Philip, P.

IPC: C07D209/02 ,  C07D405/00 ,  A61K31/496

CPC classification number: A61K31/402 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/456

Abstract: The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation.

Abstract translation: 本发明涉及涉及抑制剂和参与同源重组的蛋白质RAD51的方法和组合物。 在一些实施方案中，存在使细胞对DNA损伤剂的作用敏感的方法，其可以具有癌症患者的特殊应用。 在本发明的一些实施方案中，RAD51抑制剂是直接影响RAD51活性的小分子，例如其促进丝状细胞形成的能力。

公开(公告)号：WO2014018748A1

公开(公告)日：2014-01-30

申请号：PCT/US2013/052044

申请日：2013-07-25

Applicant: SARCODE BIOSCIENCE INC.

Inventor： ZELLER, James, Robert ,  VENKATRAMAN, Sripathy ,  BROT, Elisabeth, C.A. ,  IYER, Subashree ,  HALL, Michael

IPC: C07D405/00 ,  C07D405/02 ,  C07D405/10

CPC classification number: C07D407/06 ,  C07B2200/13 ,  C07D405/06

Abstract: Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.

Abstract translation: 公开了化合物的制备和纯化方法，其中间体，其多晶型物和相关化合物。 还公开了其在治疗LFA-1介导的疾病中的制剂及其用途。

公开(公告)号：WO2012069989A1

公开(公告)日：2012-05-31

申请号：PCT/IB2011/055229

申请日：2011-11-22

Applicant: CADILA PHARMACEUTICALS LIMITED ,  KHAMAR, Bakulesh Mafatlal ,  SHARMA, Arun Omprakash ,  PARIKH, Sanjay Natvarlal ,  BHATT, Achyut Pravinbhai ,  PANSURIYA, Akshay Madhubhai ,  JADEJA, Krunal Aniruddhbhai ,  BAPAT, Uday Rajaram ,  MODI, Indravadan Ambalal

Inventor： KHAMAR, Bakulesh Mafatlal ,  SHARMA, Arun Omprakash ,  PARIKH, Sanjay Natvarlal ,  BHATT, Achyut Pravinbhai ,  PANSURIYA, Akshay Madhubhai ,  JADEJA, Krunal Aniruddhbhai ,  BAPAT, Uday Rajaram ,  MODI, Indravadan Ambalal

IPC: C07D405/14 ,  C07D405/00 ,  C07D405/04

CPC classification number: C07D211/90

Abstract: The present invention relates to a process for the removal of t-butyl group from t-butyl methyl 4-(2',3'-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate to provide-1,4-dihydro-2,6-dimethyl-4-(2',3'-dichorophenyl)-5-methoxycarbonyl-3-pyridine- carboxylic acid, which is further converted to to yield clevidipine having HPLC purity over 6 99%.

Abstract translation: 本发明涉及从叔丁基4-（2'，3'-二氯苯基）-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸甲酯除去叔丁基的方法， 提供-1,4-二氢-2,6-二甲基-4-（2'，3'-二氯苯基）-5-甲氧基羰基-3-吡啶羧酸，其进一步转化为具有HPLC纯度超过6的氯维地平 99％。

公开(公告)号：WO2010091411A1

公开(公告)日：2010-08-12

申请号：PCT/US2010/023642

申请日：2010-02-09

Applicant: GLAXOSMITHKLINE LLC ,  BANKA, Anna ,  BASKARAN, Subramanian ,  CATALANO, John ,  CHONG, Pek ,  DICKSON, Hamilton ,  FANG, Jing ,  MAUNG, Jack ,  NEITZEL, Martin, Leon ,  PEAT, Andy ,  PRICE, Daniel ,  RAI, Roopa ,  ROBERTS, Christopher, Don ,  SHOTWELL, Brad ,  TAI, Vincent ,  ZHANG, Huichang

Inventor： BANKA, Anna ,  BASKARAN, Subramanian ,  CATALANO, John ,  CHONG, Pek ,  DICKSON, Hamilton ,  FANG, Jing ,  MAUNG, Jack ,  NEITZEL, Martin, Leon ,  PEAT, Andy ,  PRICE, Daniel ,  RAI, Roopa ,  ROBERTS, Christopher, Don ,  SHOTWELL, Brad ,  TAI, Vincent ,  ZHANG, Huichang

IPC: C07D405/00

CPC classification number: C07D471/04

Abstract: Provided are compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).

Abstract translation: 提供式（I）的化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由病毒如丙型肝炎病毒（HCV）的黄病毒科家族介导的病毒感染的用途。

公开(公告)号：WO2009140164A1

公开(公告)日：2009-11-19

申请号：PCT/US2009/043302

申请日：2009-05-08

Applicant: CHIPSCREEN BIOSCIENCES LTD. ,  LU, Xian-Ping ,  LI, Zhi-Bin ,  NING, Zhi-Qiamg

Inventor： LU, Xian-Ping ,  LI, Zhi-Bin ,  NING, Zhi-Qiamg

IPC: A61K31/44 ,  C07D401/00 ,  C07D405/00

CPC classification number: C07D213/82 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention relates to certain 6-aminonicotinamide derivatives which are capable of inhibiting histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.

Abstract translation: 本发明涉及能够抑制组蛋白脱乙酰酶的某些6-氨基烟酰胺衍生物。 因此，本发明的化合物可用于治疗与异常组蛋白脱乙酰酶活性相关的疾病。 还公开了包含这些化合物的药物组合物，利用包含这些化合物的药物组合物治疗疾病的方法，以及制备这些化合物的方法。