公开(公告)号：US20240360146A1

公开(公告)日：2024-10-31

申请号：US18574511

申请日：2022-06-30

申请人： HANGZHOU HEALZEN THERAPEUTICS CO., LTD. ,  SHANGHAI INSTITTUTE OF MATERIA, CHINESE ACADEMY OF SCCIENCES

发明人： Xinglu ZHOU ,  Jia LI ,  Xingguo LIU ,  Yubo ZHOU ,  Miao HU ,  Xiaomin LUO ,  Jiangfeng XIE ,  Weijuan KAN ,  Mingbo SU ,  Yizhe WU

IPC分类号： C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6558

CPC分类号： C07D491/048 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/675 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07F9/65583

摘要： Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof; or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

公开(公告)号：US20240352024A1

公开(公告)日：2024-10-24

申请号：US18650142

申请日：2024-04-30

申请人： TENACIA BIOTECHNOLOGY (HONG KONG) CO., LIMITED

发明人： Torsten M. Madsen ,  M. Amin Khan ,  Mohsen Arghavani ,  Phil Bauer ,  Eduardo Mar

IPC分类号： C07D487/10 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  A61P25/02

CPC分类号： C07D487/10 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/4866 ,  A61P25/02 ,  C07B2200/13

摘要： Provided herein are methods of treating painful diabetic peripheral neuropathy, such as advanced painful DPN, in a patient by administering to the patient an effective amount of NYX-2925 or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of 3-hydroxy-2-(5-isobutyryl-1-oxo-2,5-diazaspiro [3,4] octan-2-yl) butanamide.

公开(公告)号：US20240343704A1

公开(公告)日：2024-10-17

申请号：US18288213

申请日：2022-05-02

申请人： Ontario Institute for Cancer Research (OICR)

发明人： Anh Chau ,  Methvin Isaac ,  Babu Joseph ,  Radek Laufer ,  Gennady Poda ,  Michael Prakesch ,  Pandiaraju Subramanian ,  David Uehling ,  Iain Watson ,  Brian Wilson ,  Tao Xin

IPC分类号： C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/08

CPC分类号： C07D401/04 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/695 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/113 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07F7/0836

摘要： The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

公开(公告)号：US12116375B2

公开(公告)日：2024-10-15

申请号：US18490700

申请日：2023-10-19

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D409/04 ,  A61K38/17 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D495/04 ,  C12N9/14 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/185 ,  C07D295/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US20240336611A1

公开(公告)日：2024-10-10

申请号：US18547190

申请日：2022-02-23

申请人： Insilico Medicine IP Limited

发明人： Aleksandrs ZAVORONKOVS ,  Aleksandr ALIPER ,  Vladimir ALADINSKIY ,  Andrey KUKHARENKO ,  Luoheng QUIN ,  Xin CHENG

IPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

摘要： Provided are TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formulas (A), (A*), (I), (II), (AA), (B), (C), (D), (B*), (C*) and (D*). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.

公开(公告)号：US20240316022A1

公开(公告)日：2024-09-26

申请号：US18573731

申请日：2022-06-30

申请人： TYRA BIOSCIENCES, INC.

发明人： Robert L. HUDKINS ,  Daniel C. BENSEN

IPC分类号： A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5383 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04

CPC分类号： A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5383 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04

摘要： Disclosed herein are compounds and methods of treating diseases and/or conditions associated with FGFR inhibition.

公开(公告)号：US20240309002A1

公开(公告)日：2024-09-19

申请号：US18665923

申请日：2024-05-16

申请人： Shionogi & Co., Ltd.

发明人： Kouhei NODU ,  Yusuke Tateno ,  Kengo Masuda ,  Yuji Nishiura ,  Yoshikazu Sasaki ,  Yu Hinata

IPC分类号： C07D471/20 ,  A61K31/438 ,  A61K31/444 ,  C07D471/10 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

CPC分类号： C07D471/20 ,  A61K31/438 ,  A61K31/444 ,  C07D471/10 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

摘要： The present invention provides the compound represented by the following formula (I):






wherein a moiety represented by formula:








or the like;

y is 0 or 1; R1 is hydrogen or the like; R2a and R2b are taken together with an adjacent carbon atom to form ring B; ring B is a substituted or unsubstituted non-aromatic carbocycle or the like; R3a is hydrogen or the like; R3b is hydrogen or the like; R4a is represented by formula:





L1 is a single bond or the like; L2 is —C(═O)— or the like; La is a single bond or the like; R7 is substituted or unsubstituted alkyl or the like; R4b is substituted or unsubstituted alkyl or the like; R4c is each independently halogen or the like.

公开(公告)号：US12084407B2

公开(公告)日：2024-09-10

申请号：US17780047

申请日：2020-11-25

申请人： CANOPY GROWTH CORPORATION

发明人： Siawash Ahmar ,  Krishna Kumar Gnanasekaran ,  Jeffrey Alan Omeara

IPC分类号： C07C311/29 ,  A61P3/00 ,  C07C309/75 ,  C07C311/51 ,  C07C317/22 ,  C07D205/06 ,  C07D205/12 ,  C07D207/408 ,  C07D211/54 ,  C07D213/71 ,  C07D233/84 ,  C07D235/16 ,  C07D235/28 ,  C07D239/40 ,  C07D249/08 ,  C07D249/10 ,  C07D263/32 ,  C07D277/30 ,  C07D295/15 ,  C07D295/26 ,  C07D305/08 ,  C07D307/64 ,  C07D487/10

CPC分类号： C07C311/29 ,  A61P3/00 ,  C07C309/75 ,  C07C311/51 ,  C07C317/22 ,  C07D205/06 ,  C07D205/12 ,  C07D207/408 ,  C07D211/54 ,  C07D213/71 ,  C07D233/84 ,  C07D235/16 ,  C07D235/28 ,  C07D239/40 ,  C07D249/08 ,  C07D249/10 ,  C07D263/32 ,  C07D277/30 ,  C07D295/15 ,  C07D295/26 ,  C07D305/08 ,  C07D307/64 ,  C07D487/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14

摘要： The synthesis of a range of pentylbezene-1,3-diol compounds of formula I is disclosed. These compounds bind to cannabinoid 1 and 2 receptors (CB1 and CB2), and are thus presumed to be useful in modulating the activity of such receptors. Accordingly, the use of such synthetic cannabinoids in the treatment of various disorders mediated by CB1 and CB2 is contemplated.

公开(公告)号：US12077533B2

公开(公告)日：2024-09-03

申请号：US17393463

申请日：2021-08-04

申请人： Pfizer Inc.

发明人： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I Trujillo

IPC分类号： A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC分类号： C07D471/04 ,  A61K31/4523 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

摘要： The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure:




or a pharmaceutically acceptable salt thereof, as set forth in the Description.

公开(公告)号：US20240279218A1

公开(公告)日：2024-08-22

申请号：US18590606

申请日：2024-02-28

申请人： Hoffmann-La Roche Inc.

发明人： Bernd BUETTELMANN ,  Giuseppe CECERE ,  Bernhard FASCHING ,  Katrin GROEBKE ZBINDEN ,  Maria-Clemencia HERNANDEZ ,  Henner KNUST ,  Andreas KOBLET ,  Emmanuel PINARD ,  Andrew THOMAS

IPC分类号： C07D413/14 ,  A61P25/28 ,  C07D471/04 ,  C07D487/10

CPC分类号： C07D413/14 ,  A61P25/28 ,  C07D471/04 ,  C07D487/10

摘要： Compounds having the formula (I)






wherein R1, R2, R3, R4, R5, R6, X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.