127423-61-4Relevant articles and documents
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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Paragraph 0272; 0276; 0932-0933, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
NITROGEN HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Paragraph 1808; 1922, (2021/06/26)
The present disclosure relates to compounds of formula (I): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds as inhibitors of receptor tyrosine kinases, in particular oncogenic mutants of ErbB-receptors e.g. in the treatment of cancer.
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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Paragraph 00758, (2021/12/30)
Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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Paragraph 0119-0120; 0126-0127, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
Novel pyrrolidine or piperidine derivatives having activity for T-type calcium channel
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Paragraph 0379-0382, (2020/04/23)
A pyrrolidine or piperidine compound having activity for T - type calcium channel, wherein the pyrrolidine or piperidine compound of Formula 1 according to the present invention has an excellent antagonistic activity to, T-type calcium channel, and can be used as a preventive or therapeutic agent, for pain diseases, or cancer related to cancer, or cancer such as, epilepsy and,hepatic pain, angina. (by machine translation)
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00537, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00230; 00666; 00672, (2020/07/05)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
Wellaway, Christopher R.,Bamborough, Paul,Bernard, Sharon G.,Chung, Chun-Wa,Craggs, Peter D.,Cutler, Leanne,Demont, Emmanuel H.,Evans, John P.,Gordon, Laurie,Karamshi, Bhumika,Lewis, Antonia J.,Lindon, Matthew J.,Mitchell, Darren J.,Rioja, Inmaculada,Soden, Peter E.,Taylor, Simon,Watson, Robert J.,Willis, Rob,Woolven, James M.,Wyspiańska, Beata S.,Kerr, William J.,Prinjha, Rab K.
, p. 9020 - 9044 (2020/08/24)
The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of the family with similar affinity, resulting in a diverse range of biological effects. To enable further understanding of the broad phenotype characteristic of pan-BET inhibition, the development of inhibitors selective for individual, or sets of, bromodomains within the family is required. In this regard, we report the discovery of a potent probe molecule possessing up to 150-fold selectivity for the N-terminal bromodomains (BD1s) over the C-terminal bromodomains (BD2s) of the BETs. Guided by structural information, a specific amino acid difference between BD1 and BD2 domains was targeted for selective interaction with chemical functionality appended to the previously developed I-BET151 scaffold. Data presented herein demonstrate that selective inhibition of BD1 domains is sufficient to drive anti-inflammatory and antiproliferative effects.
(S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride and synthesis method therefor
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Paragraph 0026-0028; 0032-0034; 0038-0040, (2019/07/04)
The invention discloses (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride and a synthesis method therefor and belongs to the technical field of organic chemical synthesis. The synthesis methodcomprises the following procedures: subjecting (R)-3-pyridonyl-1-tert-butyl carboxylate, which serves as a raw material, to reactions of four steps, i.e., methanesulfonate synthesis, methyl amination, acetyl loading and tert-butyloxycarbonyl removing salt forming, thereby obtaining the (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride. The synthesis method for the (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride, provided by the invention, is safe, convenient and economical, the obtained (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride is stable in performance and can be conveniently stored and transported.
SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
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Paragraph 001372; 001373; 001374, (2018/04/27)
Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.