361345-36-0

Upstream product

• 455-88-9 5-nitro-2-fluorotoluene 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 7149-70-4 2-bromo-5-nitrotoluene 
• 446-33-3 5-Fluoro-2-nitrotoluene 

Downstream Products

• 1390656-67-3 tert-butyl 4-(4-(7-chloro-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-2-methylphenyl)piperazine-1-carboxylate 
• 1390656-68-4 tert-butyl 4-(4-(7-(2,6-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[3,4-d]pyridazin-5-ylamino)-2-methylphenyl)piperazine-1-carboxylate 
• 808196-28-3 tert-butyl 4-(4-iodo-2-methylphenyl)piperazine-1-carboxylate 
• 1048664-05-6 1-(2-methyl-4-nitrophenyl)piperazine dihydrochloride 
• 361345-37-1 1-(t-butoxycarbonyl)-4-(4-amino-3-methylbenzene)sulphonylpiperazinide 

Relevant academic research and scientific papers

Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors

Fms-like tyrosine kinase 3 (FLT3) has been considered as a potential drug target for the treatment of acute myeloid leukemia (AML), because of its high and aberrant expression in AML patients, especially the patients with FLT3-ITD mutation. Initiating from a hit compound (IC50: 500 nM against FLT3-ITD), a series of compounds were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent FLT3-ITD inhibitors. During the medicinal chemistry works, flexible molecular docking was used to provide design rationale and study the binding modes of the target compounds. Through the mixed SAR exploration based on the enzymatic and cellular activities, compound T24 was identified with potent FLT3-ITD inhibitory (IC50: 0.41 nM) and anti-proliferative (IC50: 0.037 μM against MV4-11 cells) activities. And the binding mode of T24 with “DFG-in” FLT3 was simulated by a 20-ns molecular dynamics run, providing some insights into further medicinal chemistry efforts toward novel FLT3 inhibitors in AML therapy.

Thiazolidine derivatives or salts thereof as an active ingredient an inhibitor Pim

PROBLEM TO BE SOLVED: To provide compounds which have excellent Pim inhibitory action and are useful as pharmaceuticals.SOLUTION: A compound is a thiazolidine derivative represented by the general formula (1) in the figure, or a salt thereof. (In the formula, X represents O or S; Rrepresents a hydrogen atom or a Calkyl group; Z, Z, Z, Z, Zand Zeach independently represent CH or N; Y represents an optionally substituted, divalent Caromatic hydrocarbon group or the like; Am represents a disubstituted amino group, or an optionally substituted, nitrogen-containing saturated heterocyclic group; and Rand Reach independently represent a hydrogen atom, a halogen atom, an alkyl group or the like.)

PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS

The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

BICYCLIC INHIBITORS OF ALK

The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES

Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1~X5, R1~R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.

The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide y Y2 receptor

A series of small molecules based on a chemotype identified from our compound collection were synthesized and tested for binding affinity (IC 50) at the human Neuropeptide Y Y2 receptor (NPY Y 2). Six of the 23 analogs tes

PYRIDONE-SUBSTITUTED-DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVE

The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom. The compound of the invention has, based on its excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.

PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

4-ARYL-2-AMINO-PYRIMIDINES OR 4-ARYL-2-AMINOALKYL-PYRIMIDINES AS JAK-2 MODULATORS AND METHODS OF USE

This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.

Dihydropyrazolopyrimidinone derivatives

The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.