221876-07-9

Upstream product

• 204078-31-9 3-(morpholin-4-yl)benzonitrile 
• 403-54-3 m-Fluorobenzonitrile 
• 79-37-8 oxalyl dichloride 
• 215309-00-5 3-(4-morpholinyl)benzoic acid 

Downstream Products

• 250681-52-8 N-(3-nitro-4-methylphenyl)-3-morpholinobenzamide 
• 247937-75-3 bis-m-morpholinobenzoyl trisulfide 
• 1394161-92-2 5-(3-morpholinophenyl)oxazole-4-carboxylic acid 
• 1394161-91-1 methyl 5-(3-morpholinophenyl)oxazole-4-carboxylate 
• 1327167-30-5 N-(3-(3-[(phenylsulfonyl)amino]phenyl)-1H-pyrazol-5-yl)-3-morpholinobenzamide 
• 250681-51-7 N-[2-methyl-5-(3-morpholinobenzamido)phenyl]-3-hydroxybenzamide 
• 250683-66-0 N-[2-chloro-5-(3-morpholinobenzamido)phenyl]-3,4-dimethoxybenzamide 
• 250681-56-2 N-[2-methyl-5-(3-morpholinobenzamido)phenyl]-4-benzyloxybenzamide 
• 250681-57-3 N-[2-methyl-5-(3-morpholinobenzamido)phenyl]-4-hydroxybenzamide 
• 250681-53-9 N-(3-amino-4-methylphenyl)-3-morpholinobenzamide 

Relevant academic research and scientific papers

Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors

The tropomyosin receptor kinases TRKs are responsible for different tumor types which caused by NTRK gene fusion, and have been identified as a successful target for anticancer therapeutics. Herein, we report a potent and selectivity TRKs inhibitor 19m through rational drug design strategy from a micromolar potency hit 17a. Compound 19m significantly inhibits the proliferation of TRK-dependent cell lines (Km-12), while it has no inhibitory effect on TRK-independent cell lines (A549 and THLE-2). Furthermore, kinases selectivity profiling showed that in addition to TRKs, compound 19m only displayed relatively strong inhibitory activity on ALK. These data may indicate that compound 19m has a good drug safety. Partial ADME properties were evaluated in vitro and in vivo. Compound 19m exhibited a good AUC values and volume of distribution and low clearance in the pharmacokinetics experiment of rats. Finally, a pharmacophore model guided by experimental results is proposed. We hope this theoretical model can help researchers find type I TRK inhibitors more efficiently.

Pyrrolidine integrin regulator and application thereof

Disclosed are a compound as represented by formula I, and a racemate, a stereoisomer, a tautomer, an isotopic marker, a nitrogen oxide, a solvate, a polymorph, a metabolite, an ester, and a prodrug thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, a preparation method therefor, and the medical use thereof. The structure of formula I is as follows:

NOVEL PYRAZOLE AND IMIDAZOLE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS

The present invention relates to pyrazole and imidazole derivatives of formula (I) wherein U, V, L, X, Y, R1, (R2)n and (R3)m and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

PYRIMIDINE DERIVATIVES

The invention concerns pyrimidine derivatives of Formula (I) wherein m is 0-3 and each Ris a group such as hydroxy, halogeno, trifluoromethyl and cyano; Ris hydrogen, halogeno or (1-6C)alkyl; n is 0-2 and each Ris a group such as hydroxy, halogeno, trifluoromethyl and cyano; p is 0-4; and Qis aryl or heteroaryl; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis

The discovery, rational analogue design, synthesis and SAR of a novel bisamide class of p38 MAP kinase inhibitor are reported. The activity in vitro is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues, such as 18. A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38α enzyme activity and lipopolysaccharide-induced tumour necrosis factor-α release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.

Substituted anilino-quinazoline (or quinoline) compounds and use thereof

The invention concerns amide derivatives of Formula (I), wherein: G is N or CH; R1is a group such as hydroxy, halo, trifluoromethyl, C1-6alkyl and C1-6alkoxy; each of R2and R3is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy and C3-7cycloalkyl, or R4is of the Formula (IC): —K—J, wherein J is aryl, heteroaryl or heterocyclyl and K is a bond or a group such as oxy and imino, R5is a group such as hydrogen, halo and trifluoromethyl: m is 1-3 and q is 0-4; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

BEZAMIDE DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY CYTOKINES

The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines

Amide derivatives useful as inhibitors of the production of cytokines

The invention concerns amide derivatives of formula (I) wherein R3is (1-6C)alkyl or halogeno; Q1is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2is a substituent such as hydroxy and halogeno; q is 0-4; and Q2includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Benzamide derivatives for the treatment of diseases mediated by cytokines

The invention concerns amide derivatives of Formula (I) wherein: R1and R2include hydroxy, C1-6alkoxy, mercapto, C1-6akylthio, amino and heterocyclyl; m and p are independently 0-3; R3is halo, cyano or C1-6alkoxy; q is 0-4; and R4is aryl or cycloalkyl wherein R4is optionally substituted with up to 3 substituents having any value defined for each R1group; or a pharmaceutically-acceptable salt or in-vivo-cleavable ester thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.