- Memantine urea derivative as well as preparation method and application thereof
-
The invention provides a memantine urea derivative as well as a preparation method and application thereof, and relates to the technical field of medicines. The memantine urea derivative provided by the invention has a typical urea structure as a primary
- -
-
-
- CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
-
This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
- -
-
Page/Page column 172; 207
(2021/11/26)
-
- Aminodithioformate compound used as FAK inhibitor
-
A purpose of the invention is to provide an aminodithioformate compound serving as an FAK inhibitor, a pharmaceutical composition, a preparation method and applications thereof, wherein the compound has a structure represented by the following general formula (I).
- -
-
Paragraph 0092-0094; 0113-0115
(2020/05/09)
-
- SMALL MOLECULE PROTEOLYSIS-TARGETING CHIMERAS AND METHODS OF USE THEREOF
-
Novel small molecule proteolysis-targeting chimeras (PROTACs) are provided, along with methods for their use as Bruton's tyrosine kinase (BTK) degraders. The small molecule PROTACs described herein are useful in treating and/or preventing BTK-related diseases, such as cancer, neurodegenerative disorders, inflammatory diseases, and metabolic disorders. Also provided are methods for inducing BTK degradation in a cell using the compounds and compositions described herein. Exemplary compounds include: (I).
- -
-
Page/Page column 66; 67-68
(2020/12/30)
-
- Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities
-
A series of 2,4-diarylaminopyrimidine derivatives containing dithiocarbamate moiety were designed by molecular hybridization strategy and synthesized for screening as inhibitors of focal adhesion kinase (FAK). Most of these compounds exhibit significant a
- Su, Yue,Li, Ridong,Ning, Xianling,Lin, Zhiqiang,Zhao, Xuyang,Zhou, Juntuo,Liu, Jia,Jin, Yan,Yin, Yuxin
-
-
- DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
-
The present application provides bifunctional compounds of Formula X or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
- -
-
Page/Page column 185; 186
(2019/08/12)
-
- DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
-
The present application provides bifunctional compounds of Formula (I), or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
- -
-
Page/Page column 126
(2018/06/12)
-
- DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
-
The present application provides bifunctional compounds of Formula (X), or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
- -
-
Page/Page column 154; 155
(2018/06/12)
-
- Piperazine substituted 1, 3 - di-substituted urea compound and piperazine substituted amide compounds and a method for its preparation and use
-
The present invention relates to a class of piperazine substituted 1,3-disubstitued urea compounds and piperazine substituted amide compounds, or pharmaceutically acceptable salts of the piperazine substituted 1,3-disubstitued urea compounds and the piper
- -
-
Paragraph 0094-0096
(2017/04/22)
-
- VEGFR3 INHIBITORS
-
This invention relates to compounds of the formula (I). The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphanglogenesis.
- -
-
Page/Page column 95
(2014/03/22)
-
- METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
-
The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
- -
-
-
- CARBAZOLE AND CARBOLINE KINASE INHIBITORS
-
The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
- -
-
Page/Page column 141
(2010/08/04)
-
- N- (1, 1, 1, 3, 3, 3-HEXAFLUORO-2-HYDROXYPROPAN-2-YL) BENZYL-N' -ARYLCARBONYLPIPERAZ INE DERIVATIVES
-
101 Abstract. The present invention relates tohexafluoroisopropanol derivativeshaving the general formula I X O N N Y OH F 3 C CF 3 A R 1 R 2 R 3 ( ) n W Z B R 6 5 Formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives inthe treatment of atherosclerosis
- -
-
Page/Page column 26
(2009/12/23)
-
- OXAZOLE TYROSINE KINASE INHIBITORS
-
The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1 : provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
- -
-
-
- DIAMINOPYRIMIDINECARBOXA MIDE DERIVATIVE
-
A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
- -
-
Page/Page column 22
(2008/06/13)
-
- HETEROCYCLICALLY SUBSTITUTED INDOLINONES, THEIR PRODUCTION AND USE AS MEDICAMENTS
-
The invention relates to heterocyclically substituted indolinones of general formula (I), in which R1 to R5 and X are defined as cited in claim 1, to their tautomers, diastereomers, enantiomers and to their mixtures, prodrugs and salts, in particular their physiologically compatible salts. Said compounds exhibit valuable pharmacological characteristics, in particular an inhibiting action on various receptor tyrosine kinases and cyclin-CDK complexes and on the proliferation of endothelial cells and various tumour cells. The invention also relates to medicaments containing said compounds, to the use of the latter and to a method for producing the same.
- -
-
Page/Page column 98
(2008/06/13)
-
