公开(公告)号：WO2022173805A1

公开(公告)日：2022-08-18

申请号：PCT/US2022/015786

申请日：2022-02-09

Applicant: TRIANA BIOMEDICINES, INC.

Inventor： GREENLEE, William, J. ,  CALANDRA, Nicholas ,  RAY, Soumya ,  KLUGE, Arthur, F.

IPC: C07D209/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D491/10 ,  A61P35/00 ,  A61K31/404

Abstract: The present application discloses novel compounds, pharmaceutical compositions containing these compounds and methods of inducing degradation of a protein, comprising contacting the protein with an effective amount of a compound of the disclosure. Methods of treating disease and disorders that results from abnormal activity of a target protein in a subject, are also disclosed.

公开(公告)号：WO2022063212A1

公开(公告)日：2022-03-31

申请号：PCT/CN2021/120199

申请日：2021-09-24

Applicant: 广州费米子科技有限责任公司

Inventor： 邱关鹏 ,  王永钢 ,  邓代国 ,  雷曾荣

IPC: C07D209/30 ,  C07D247/02 ,  C07D403/04 ,  A61K31/404 ,  A61K31/506 ,  A61K31/66 ,  A61P35/00

Abstract: 一种嘧啶基衍生物、其制备方法及其用途。所述嘧啶基衍生物具有通式(I)所示结构。该嘧啶基衍生物可以作为具有选择性的CDK7抑制剂，解决多种癌症的有效治疗需求，尤其是转录失调的癌症。

公开(公告)号：WO2021203023A1

公开(公告)日：2021-10-07

申请号：PCT/US2021/025614

申请日：2021-04-02

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： GIROUX, Simon ,  CLARK, Michael Philip ,  BRODNEY, Michael Aaron ,  NUHANT, Philippe Marcel ,  ALLEN, Emily Elizabeth ,  FIMOGNARI, JR., Robert Francis ,  ZAKY, Mariam ,  BOYD, Michael John ,  DEININGER, David D. ,  ZHANG, Hu ,  DENG, Hongbo ,  COLLIER, Philip Noel ,  MAXWELL, Brad ,  WAAL, Nathan D. ,  RONKIN, Steven M. ,  WANG, Jian ,  TANG, Qing ,  FLEMING, Gabrielle Simone ,  JONES, Peter ,  BOUCHER, Diane Marie ,  FANNING, Lev T.D. ,  HALL, Amy B. ,  HURLEY, Dennis James ,  JOHNSON, JR., Mac Arthur ,  MAXWELL, John Patrick ,  SWETT, Rebecca Jane ,  TAPLEY, Timothy Lewis ,  THOMSON, Stephen A. ,  DAMAGNEZ, Veronique ,  COTTRELL, Kevin Michael

IPC: C07D209/08 ,  C07D209/18 ,  C07D209/20 ,  C07D209/30 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D493/08 ,  A61K31/404 ,  A61K31/35 ,  A61K31/381 ,  A61P1/00 ,  A61P1/14 ,  A61P1/16 ,  A61P11/00 ,  A61P11/08 ,  A61P11/10 ,  A61P17/00 ,  A61P31/00 ,  A61P31/02 ,  A61P35/00

Abstract: Indole derivatives as alpha-l-antitrypsin modulators for treating alpha-l-antitrypsin deficiency (AATD).

公开(公告)号：WO2021173721A1

公开(公告)日：2021-09-02

申请号：PCT/US2021/019477

申请日：2021-02-24

Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

Inventor： NARAYANAN, Ramesh ,  PONNUSAMY, Thamarai ,  MILLER, Duane D. ,  HE, Yali ,  HWANG, Dong-Jin

IPC: A61K31/404 ,  C07D209/30 ,  A61P35/00

Abstract: This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：WO2020256437A1

公开(公告)日：2020-12-24

申请号：PCT/KR2020/007910

申请日：2020-06-18

Applicant: 주식회사 엘지화학

Inventor： 이상대 ,  김상훈 ,  황교현 ,  박애리 ,  김봉찬

IPC: C07D417/14 ,  C07D209/30 ,  C07D231/56 ,  A61K31/541

Abstract: 본 발명은 의약적으로 유용한 인돌 또는 인다졸 화합물을 제조하는데 있어서, 안전성(safety)을 확보하며, 공정의 단순화를 통해 수율을 향상시키고, 종래의 철(Fe) 촉매를 사용하는 방법의 문제점을 해소할 수 있는 신규한 제조방법에 관한 것이다.

公开(公告)号：WO2020254289A1

公开(公告)日：2020-12-24

申请号：PCT/EP2020/066560

申请日：2020-06-16

Applicant: UCB PHARMA GMBH

Inventor： PEGURIER, Cécile ,  LOVERA, Silvia ,  MUELLER, Christa E. ,  HOCKEMEYER, Joerg ,  RASHED, Mahmoud ,  EL-TAYEB, Ali ,  ZHANG, Yong-Qiang

IPC: C07D209/30 ,  C07D471/04 ,  C07D401/12 ,  A61K31/404 ,  A61K31/4745 ,  A61K31/444 ,  A61P25/28

Abstract: Disclosed are N-(phenyl)-lH-indole-3-sulfonamide and N-(phenyl) -1 H-pyrrolo[2,3-b]pyridine-3-sulfonamide derivatives of formula I substituted at the 1- and 6-positions of the 1H-indole or 1H-pyrrolo[2,3-b]pyridine moiety, as well as structurally related compounds (e.g. the N-pyridin-2-yl and the N-pyridin-3-yl analogues thereof). The present compounds have GPR17 modulating properties which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating disorders such as multiple sclerosis.

公开(公告)号：WO2020055725A1

公开(公告)日：2020-03-19

申请号：PCT/US2019/050165

申请日：2019-09-09

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

Inventor： NEWMAN, Amy Hauck ,  KUMAR, Vivek ,  SHAIK, Anver Basha

IPC: C07D209/30 ,  C07D307/85 ,  C07D317/68 ,  A61K31/40 ,  A61P25/36 ,  C07D471/04 ,  C07D513/04 ,  C07D209/42 ,  C07D233/90 ,  C07D405/12 ,  C07D407/12

Abstract: Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.

公开(公告)号：WO2020003119A1

公开(公告)日：2020-01-02

申请号：PCT/IB2019/055338

申请日：2019-06-25

Applicant: SUZHOU MEDNES PHARMA TECH CO., LTD.

Inventor： DU, Fang ,  HU, Xiaowei ,  LIANG, Yugang

IPC: C07D209/30 ,  C07D235/04 ,  A61K31/405 ,  A61K31/4184 ,  A61P35/00

Abstract: Provided herein is novel compounds of formula (I), (II), (III), (IV), and (V) as described in the specification, and pharmaceutically acceptable salts, solvates, and prodrugs and compositions thereof, and methods of measuring hedgehog pathway activation in tumor cells, examining tumor cell proliferation, differentiation and apoptosis and using the compounds and pharmaceutical compositions disclosed for treatment of diseases and disorders associated with the hedgehog signaling pathway.

公开(公告)号：WO2015128088A1

公开(公告)日：2015-09-03

申请号：PCT/EP2015/000441

申请日：2015-02-26

Applicant: GRÜNENTHAL GMBH

Inventor： PRÜHS, Stefan ,  SCHÄFER, Olaf

IPC: C07D209/30

CPC classification number: C07D491/107 ,  C07D209/12 ,  C07D209/30

Abstract: The present invention relates to a process for the preparation of 5-fluorotryptophol as well as a process for the preparation of (1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1 '- pyrano-[3,4b]-indol]-4-amine using the 5-fluorotryptophol obtained by said first process. The process according to the invention provides 5-fluorotryptophol in improved yield and purity without the need for chromatographic purification of the product.

Abstract translation: 本发明涉及制备5-氟异丙基苯的方法，以及制备（1r，4r）-6'-氟-N，N-二甲基-4-苯基-4'，9'- 二氢-3'H-螺[环己烷-1,1'-吡喃 - [3,4b] - 吲哚] -4-胺，使用所述第一种方法得到的5-氟肉豆蔻醇。 根据本发明的方法提供5-氟肉豆蔻醇，其产率和纯度提高，而不需要色谱纯化产物。

公开(公告)号：WO2015049351A1

公开(公告)日：2015-04-09

申请号：PCT/EP2014/071195

申请日：2014-10-02

Applicant: BAYER CROPSCIENCE AG

Inventor： FRACKENPOHL, Jens ,  BOJACK, Guido ,  HELMKE, Hendrik ,  LEHR, Stefan ,  MÜLLER, Thomas ,  WILLMS, Lothar ,  DITTGEN, Jan ,  SCHMUTZLER, Dirk ,  BICKERS, Udo ,  STREK, Harry ,  BALTZ, Rachel

IPC: A01N43/38 ,  C07D209/30 ,  C07D209/34 ,  A01P15/00

CPC classification number: C07D209/96 ,  A01N43/38 ,  A01N43/90 ,  A01N47/16 ,  C07D209/30 ,  C07D209/34 ,  C07D471/10 ,  C07D491/107

Abstract: Die Erfindung betrifft die Verwendung substituierter Dihydrooxindolylsulfonamide oder deren Salze Formel (I) wobei die Reste in der allgemeinen Formel (I) den in der Beschreibung gegebenen Definitionen entsprechen, zur Steigerung der Stresstoleranz in Pflanzen gegenüber abiotischem Stress und/oder zur Erhöhung des Pflanzenertrags.

Abstract translation: 本发明涉及使用取代的Dihydrooxindolylsulfonamide的或它们的盐的式（I），其中在说明书中给出的通式（I）中的基团，定义为在植物中增加的胁迫耐受性对非生物胁迫和/或用于增加植物产量。