1201916-87-1

Upstream product

• 2075-46-9 4-nitro-1H-pyrazole 
• 118811-07-7 tert-butyl 4-(tosyloxy)piperidin-1-carboxylate 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 34619-03-9 tert-butyldicarbonate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 141699-59-4 1-(tert-butoxycarbonyl)piperidin-4-yl methanesulfonate 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 3994-50-1 1-methyl-4-nitropyrazole 

Downstream Products

• 1029413-55-5 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylic acid tert-butyl ester 
• 1201933-98-3 2-((5-chloro-2-((1-(4-piperidyl)pyrazol-4-yl)amino)-4-pyridyl)amino)-N-methyl-benzamide 

Relevant academic research and scientific papers

Thienopyrimidine derivatives and preparation method thereof

Disclosed are a thienopyrimidine derivative and a preparation method therefor. Provided is a method for preparing a compound as shown in formula B, which method is characterized by comprising the following steps: subjecting a compound as shown in formula

HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS

Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.

AZAINDOLE DERIVATIVE AND USE THEREOF AS FGFR AND C-MET INHIBITOR

A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said che

Preparation method of FLT3 and FGFR kinase inhibitor

The invention discloses a preparation method of an FLT3 and FGFR kinase inhibitor. The preparation method comprises the following steps: S1, performing reacting of 4-nitropyrazole with N-BOC-4-hydroxypyridine to obtain an intermediate 1, and carrying out

HETEROARYLAMINOPYRIMIDINE AMIDE AUTOPHAGY INHIBITORS AND METHODS OF USE THEREOF

Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers. (I)

Discovery of 7H-pyrrolo[2,3-d]pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study

Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy. Biological evaluation indicated that most of these new compounds could potently inhibit FAK kinase, leading to the promising inhibitors against the proliferation of U-87MG, A-549, and MDA-MB-231 cancer cell lines. Among them, the optimized compound 18h potently inhibited the enzyme (IC50 = 19.1 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC50 values of 0.35, 0.24, and 0.34 μM, respectively. Compound 18h is a multi-target kinase inhibitor. Furthermore, compound 18h also exhibited relatively less cytotoxicity (IC50 = 3.72 μM) toward a normal human cell line, HK2. According to the flow cytometry and wound healing assay results, compound 18h effectively induced apoptosis and G0/G1 phase arrest of MDA-MB-231 cells and suppressed the migration of U-87MG, A-549 and MDA-MB-231 cells. The docking study of compound 18h was performed to elucidate its possible binding modes and to provide a structural basis for the further structural guidance design of FAK inhibitors. Collectively, these data support the further development of compound 18h as a lead compound for FAK-targeted anticancer drug discovery.

PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR

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.

1,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDINE-3-ONE COMPOUNDS AS INHIBITORS OF WEE-1 KINASE

The disclosure includes compounds of Formula (I) wherein Q, R1, R2, and m are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.

N-heteroarylsulfonamide derivative, and preparation and application of same

The invention provides an N-heteroarylsulfonamide derivative, and preparation and an application of same. The derivative includes pharmaceutically acceptable salts and solvates thereof; a test provesthat the N-heteroarylsulfonamide derivative allows specific combination and inhibit or reduce the activity of potassium pathway Kv1.3, so that the derivative can be used for treating autoimmune diseases, caused by abnormal activation of the potassium pathway Kv1.3, of human or animal. An inhibitor in the invention also includes a medicinal composition of the compound. The invention also provides amethod for preparing the compound. The derivative has the general formula as the specification.