公开(公告)号：US20240158397A1

公开(公告)日：2024-05-16

申请号：US18202704

申请日：2023-05-26

申请人： Sloan-Kettering Institute for Cancer Research

发明人： Gabriela Chiosis ,  Huazhong He ,  Danuta Zatorska

IPC分类号： C07D473/40 ,  A61K31/52

CPC分类号： C07D473/40 ,  A61K31/52

摘要： Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are otherwise delivered to the brain.

公开(公告)号：US20230339916A1

公开(公告)日：2023-10-26

申请号：US18043752

申请日：2021-08-26

申请人： SYNGENTA CROP PROTECTION AG

发明人： Mathilde Denise LACHIA ,  Alain DE MESMAEKER ,  Alexandre Franco Jean Camille LUMBROSO ,  Roman STAIGER

IPC分类号： C07D405/12 ,  C07D473/40 ,  C07D413/12 ,  C07D417/12 ,  A01P21/00 ,  A01N43/38 ,  A01N43/56 ,  A01N43/647 ,  A01N43/90 ,  A01N43/52 ,  A01N43/42 ,  A01N43/76 ,  A01N43/78 ,  A01N43/84 ,  C07D487/04

CPC分类号： C07D405/12 ,  C07D473/40 ,  C07D413/12 ,  C07D417/12 ,  A01P21/00 ,  A01N43/38 ,  A01N43/56 ,  A01N43/647 ,  A01N43/90 ,  A01N43/52 ,  A01N43/42 ,  A01N43/76 ,  A01N43/78 ,  A01N43/84 ,  C07D487/04

摘要： Compounds of formula (I) wherein the substituents are as defined in claim 1, useful as plant growth regulators and/or seed germination promoters.

公开(公告)号：US11724982B2

公开(公告)日：2023-08-15

申请号：US16868343

申请日：2020-05-06

申请人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

发明人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

IPC分类号： C07C233/25 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C273/18 ,  C07C231/14 ,  C07C253/30 ,  C07D213/75 ,  C07D213/76 ,  C07D347/00 ,  C07D239/47 ,  C07D239/91 ,  C07D473/40 ,  C07D263/57 ,  C07D209/08 ,  C07D215/40 ,  C07D401/04 ,  C07D471/04 ,  C07J43/00 ,  C07D417/04 ,  C07D405/04 ,  C07C231/12 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C255/60 ,  C07C255/58 ,  C07C271/38 ,  C07C275/34

CPC分类号： C07C233/25 ,  C07C231/12 ,  C07C231/14 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C253/30 ,  C07C255/58 ,  C07C255/60 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C271/38 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/34 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D215/40 ,  C07D239/47 ,  C07D239/91 ,  C07D263/57 ,  C07D347/00 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/40 ,  C07J43/003 ,  C07C273/1854 ,  C07C275/64 ,  C07C269/06 ,  C07C271/38 ,  C07C231/14 ,  C07C233/25 ,  C07C253/30 ,  C07C255/60 ,  C07C253/30 ,  C07C255/58 ,  C07C273/1809 ,  C07C275/34

摘要： The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure:




wherein

A is an aryl or heteroaryl, each with or without substitution; and

R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising:

(a) reacting a compound having the structure:





with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:





and

(b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

公开(公告)号：US20180360832A1

公开(公告)日：2018-12-20

申请号：US15993299

申请日：2018-05-30

申请人： ICOS CORPORATION

发明人： Chanchal SADHU ,  Ken DICK ,  Jennifer TREIBERG ,  C. Gregory SOWELL ,  Edward A. KESICKI ,  Amy OLIVER

IPC分类号： A61K31/506 ,  C07D473/32 ,  C07D473/24 ,  C07D473/38 ,  C07D473/40 ,  C07D473/34 ,  C12N9/12 ,  C12N9/99 ,  C07D473/16 ,  C07D473/00 ,  C07D473/30 ,  C07D403/12 ,  C07D487/04

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

公开(公告)号：US10010550B2

公开(公告)日：2018-07-03

申请号：US15589910

申请日：2017-05-08

申请人： ICOS CORPORATION

发明人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

IPC分类号： A61K31/513 ,  A61K31/506 ,  C07D473/32 ,  C12N9/12 ,  C07D487/04 ,  C07D473/40 ,  C12N9/99 ,  C07D473/34 ,  C07D473/30 ,  C07D473/24 ,  C07D473/16 ,  C07D473/00 ,  C07D403/12 ,  C07D473/38

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

公开(公告)号：US20180161336A1

公开(公告)日：2018-06-14

申请号：US15659306

申请日：2017-07-25

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin Michael Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC分类号： A61K31/5377 ,  C07D403/12 ,  C07D241/42 ,  A61K31/506 ,  C07D513/04 ,  C07D498/08 ,  C07D491/048 ,  C07D487/04 ,  C07D475/00 ,  C07D473/40 ,  C07D471/04 ,  C07D417/12 ,  C07D413/12 ,  C07D405/14 ,  C07D405/12 ,  C07D403/14 ,  C07D401/14 ,  C07D241/40 ,  C07D491/08 ,  C07D271/12 ,  C07D401/12 ,  C07D413/14 ,  C07D491/056 ,  C07D491/052 ,  C07D241/44 ,  C07D413/04 ,  A61K31/5386

CPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D241/42 ,  C07D241/44 ,  C07D271/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

摘要： The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US09957270B2

公开(公告)日：2018-05-01

申请号：US15124654

申请日：2015-03-13

申请人： Agency for Science, Technology and Research

发明人： Haishan Wang ,  Dizhong Chen ,  Chang Kai Soh

IPC分类号： A01N43/90 ,  A61K31/52 ,  A61K31/519 ,  C07D473/00 ,  C07D487/00 ,  C07D473/34 ,  C07D473/32 ,  A61K45/06 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/40

CPC分类号： C07D473/34 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/16 ,  C07D473/32 ,  C07D473/40 ,  A61K2300/00

摘要： The present invention relates to fused pyrimidine-based hydroxamate compounds of formula (I), comprising a hydroxamate group, that are inhibitors of histone deacetylase (HDAC) and kinases. More particularly, the present invention relates to hydroxamate substituted purine or 5H-pyrrolo[3,2-d]pyrimidine derivatives, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having histone deacetylase, non-histone deacetylase and kinase activities/functions and/or via unspecified/multi-targeted mechanisms.

公开(公告)号：US09926321B2

公开(公告)日：2018-03-27

申请号：US15160293

申请日：2016-05-20

申请人： Sloan-Kettering Institute for Cancer Research

发明人： Weilin Sun ,  Tony Taldone ,  Pallav Patel ,  Gabriela Chiosis

IPC分类号： C07D473/34 ,  C07D473/40 ,  A61K31/52

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D473/40

摘要： The disclosure relates to Compounds of Formulae (IA) and (IB), and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and (IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.

公开(公告)号：US20170298008A1

公开(公告)日：2017-10-19

申请号：US15516610

申请日：2015-10-09

申请人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

发明人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

IPC分类号： C07C233/25 ,  C07C231/12 ,  C07D239/91 ,  C07D215/40 ,  C07D213/76 ,  C07D213/75 ,  C07D209/08 ,  C07C259/10 ,  C07C259/06 ,  C07C255/60 ,  C07C253/30 ,  C07C233/81 ,  C07C233/80 ,  C07C233/54 ,  C07C233/33 ,  C07D401/04 ,  C07D473/40

CPC分类号： C07C233/25 ,  C07C231/12 ,  C07C231/14 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C253/30 ,  C07C255/60 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C273/1809 ,  C07C273/1854 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D215/40 ,  C07D239/47 ,  C07D239/91 ,  C07D263/57 ,  C07D347/00 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/40 ,  C07J43/003 ,  C07C275/64 ,  C07C271/38 ,  C07C255/58 ,  C07C275/34

摘要： The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without subsutitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)7, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

公开(公告)号：US20170049772A1

公开(公告)日：2017-02-23

申请号：US15281702

申请日：2016-09-30

申请人： ICOS CORPORATION

发明人： Chanchal SADHU ,  Ken DICK ,  Jennifer TREIBERG ,  C. Gregory SOWELL ,  Edward A. KESICKI ,  Amy OLIVER

IPC分类号： A61K31/506 ,  C12N9/99 ,  C12N9/12

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphotidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating disease, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kδ）活性的方法，以及治疗PI3Kδ在白细胞功能中起作用的疾病如免疫和炎症病症的方法。 优选地，所述方法使用选择性抑制PI3Kδ的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。 还提供了使用PI3Kδ抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了在体外和体内使用PI3Kδ抑制化合物抑制PI3Kδ介导的过程的方法。