公开(公告)号：US20240352036A1

公开(公告)日：2024-10-24

申请号：US18634034

申请日：2024-04-12

申请人： Revolution Medicines, Inc.

发明人： Shaoling LI ,  Paul Lobben ,  Kang-Jye Chou ,  Jun Huang ,  Xiaojun Huang

IPC分类号： C07D498/22 ,  A61K31/504 ,  A61K31/5386

CPC分类号： C07D498/22 ,  A61K31/504 ,  A61K31/5386

摘要： The disclosure features crystalline forms of Ras inhibitors, pharmaceutical compositions thereof, and their uses in the treatment of cancers.

公开(公告)号：US20240352015A1

公开(公告)日：2024-10-24

申请号：US18755191

申请日：2024-06-26

申请人： Shionogi & Co., Ltd.

发明人： Yoshiyuki TAODA ,  Yuto UNOH

IPC分类号： C07D471/14 ,  A61K31/53 ,  A61P31/18 ,  C07D471/18 ,  C07D487/14 ,  C07D491/22 ,  C07D498/22

CPC分类号： C07D471/14 ,  A61K31/53 ,  A61P31/18 ,  C07D471/18 ,  C07D487/14 ,  C07D491/22 ,  C07D498/22

摘要： The present invention provides a compound represented by Formula (I):




wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.

公开(公告)号：US20240287095A1

公开(公告)日：2024-08-29

申请号：US18422175

申请日：2024-01-25

申请人： BAYLOR UNIVERSITY

发明人： John L. Wood ,  Ke Kong ,  Kevin Gayler

IPC分类号： C07D498/22 ,  A61P35/00

CPC分类号： C07D498/22 ,  A61P35/00

摘要： Equipotent indolocarbazole-derived analogs of staurosporine identified herein are prepared through C—H borylation chemistry. Functionality resides at C2 and C10 of the indolocarbazole aromatic region. Introducing functionality in this previously inaccessible region does not abrogate kinase activity and is shown to change the selectivity profile.

公开(公告)号：US20240262848A1

公开(公告)日：2024-08-08

申请号：US18597844

申请日：2024-03-06

申请人： BeiGene, Ltd.

发明人： Chao YU ,  Jie CHEN ,  Yichao BIAN ,  Xiaoyu LI ,  Hanzi SUN ,  Huaqing LIU ,  Ce WANG ,  Zhiwei WANG

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/553 ,  A61P35/00 ,  C07D498/22

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/553 ,  A61P35/00 ,  C07D498/22

摘要： Provided herein are compounds having the following structure:




wherein the substituents are as defined herein, compositions comprising an effective amount of a compound, and methods for modulating activity of KRAS G12D and/or G12V.

公开(公告)号：US12054497B2

公开(公告)日：2024-08-06

申请号：US17773607

申请日：2020-10-28

申请人： GENFLEET THERAPEUTICS (SHANGHAI) INC. ,  ZHEJIANG GENFLEET THERAPEUTICS CO., LTD.

发明人： Fusheng Zhou ,  Tao Jiang ,  Chonglan Lin ,  Lijian Cai ,  Wan He ,  Jiong Lan

IPC分类号： C07D471/22 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D471/14 ,  C07D471/16 ,  C07D498/22

CPC分类号： C07D498/22 ,  C07D471/16 ,  C07D471/22

摘要： A substituted heterocyclic fused cyclic compound as represented by formula (I) or formula (IA) and having a selective inhibitory effect on KRAS gene mutation, or a pharmaceutically-acceptable salt, a stereoisomer, a solvate or a prodrug thereof, a pharmaceutical composition containing the compound, and an application thereof in preparation of cancer drugs are provided.

公开(公告)号：US20240208975A1

公开(公告)日：2024-06-27

申请号：US18497515

申请日：2023-10-30

申请人： Kumquat Biosciences Inc.

发明人： Baogen Wu ,  Pingda Ren ,  Zhiyong Chen ,  Yi Liu

IPC分类号： C07D471/22 ,  A61K45/06 ,  C07D495/22 ,  C07D498/22

CPC分类号： C07D471/22 ,  A61K45/06 ,  C07D495/22 ,  C07D498/22

摘要： The present disclosure provides compounds and pharmaceutically acceptable salt thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

公开(公告)号：US20240197726A1

公开(公告)日：2024-06-20

申请号：US18280035

申请日：2022-03-01

申请人： THE UNIVERSITY OF TOKYO

发明人： Hiroki OGURI ,  Ryo TANIFUJI

IPC分类号： A61K31/4995 ,  A61P35/00 ,  C07D471/18 ,  C07D491/22 ,  C07D498/22

CPC分类号： A61K31/4995 ,  A61P35/00 ,  C07D471/18 ,  C07D491/22 ,  C07D498/22

摘要： [Problem] To provide: a novel tetrahydroisoquinoline (THIQ) alkaloid compound having a macrocyclic structure; an intermediate of the compound; and a method for producing the compound.
[Solution] Provided is a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.




The present invention also provides: a method for synthesizing this compound; and an intermediate compound useful in this synthesis.

公开(公告)号：US20240180924A1

公开(公告)日：2024-06-06

申请号：US18526158

申请日：2023-12-01

申请人： Newave Pharmaceutical Inc.

发明人： Yi Chen

IPC分类号： A61K31/553 ,  A61K31/282 ,  A61K31/4184 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/52 ,  A61K31/635 ,  A61K31/7048 ,  A61K33/243 ,  A61K35/17 ,  A61K38/07 ,  A61K39/395 ,  A61K47/68 ,  A61P35/02 ,  C07D471/14 ,  C07D491/147 ,  C07D498/14 ,  C07D498/22 ,  C07D513/14 ,  C07D515/14 ,  C07D519/00

CPC分类号： A61K31/553 ,  A61K31/282 ,  A61K31/4184 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/52 ,  A61K31/635 ,  A61K31/7048 ,  A61K33/243 ,  A61K35/17 ,  A61K38/07 ,  A61K39/3955 ,  A61K47/6849 ,  A61P35/02 ,  C07D471/14 ,  C07D491/147 ,  C07D498/14 ,  C07D498/22 ,  C07D513/14 ,  C07D515/14 ,  C07D519/00

摘要： The disclosure includes compounds of Formula (A), (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j m, n, k, v, s, g, V, W, L, Z1, Q1, Q2, Q3, Q4, Q5, Q6 and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a nerodegenerative disease with these compounds.

公开(公告)号：US20240174691A1

公开(公告)日：2024-05-30

申请号：US18282254

申请日：2022-03-17

申请人： GENFLEET THERAPEUTICS (SHANGHAI) INC. ,  ZHEJIANG GENFLEET THERAPEUTICS CO., LTD.

发明人： Tao JIANG ,  Fusheng ZHOU ,  Leitao ZHANG ,  Lijian CAI ,  Feng YAN ,  Jichen ZHAO ,  Jiong LAN ,  Qiang LU

IPC分类号： C07D498/22 ,  A61K31/553 ,  A61P35/00 ,  C07D519/00

CPC分类号： C07D498/22 ,  A61K31/553 ,  A61P35/00 ,  C07D519/00

摘要： Disclosed are a pyrimidine-fused cyclic compound having an inhibitory effect on KRAS gene mutation, or a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, and a pharmaceutical composition containing the compound, and the use thereof in the preparation of a drug for treating cancer.

公开(公告)号：US20240139185A1

公开(公告)日：2024-05-02

申请号：US18184766

申请日：2023-03-16

申请人： Revolution Medicines, Inc.

发明人： Meizhong JIN ,  Nicholas Perl ,  Anna Kohlmann ,  Ning Yin ,  Jason T. Lowe ,  Jae Young Ahn ,  Mark Joseph Mulvihill ,  Elena S. Koltun ,  Adrian L. Gill

IPC分类号： A61K31/504 ,  A61K45/06 ,  C07D487/18 ,  C07D498/18 ,  C07D498/22

CPC分类号： A61K31/504 ,  A61K45/06 ,  C07D487/18 ,  C07D498/18 ,  C07D498/22

摘要： The disclosure features macrocyclic compounds, alone and in combination with other therapeutic agents, as well as pharmaceutical compositions and protein complexes thereof, capable of modulating biological processes including RAS and RAS-RAF inhibition, and their uses in the treatment of cancers.