258503-85-4

Upstream product

• 119-32-4 4-Methyl-3-nitroanilin 
• 295349-76-7 2-morpholinopyridine-4-carbonyl chloride 
• 65287-34-5 2-chloropyridine-4-carbonyl chloride 
• 258503-84-3 2-chloro-N-(4-methyl-3-nitrophenyl) pyridine-4-carboxamide 
• 110-91-8 morpholine 
• 295349-64-3 2-morpholin-4-ylisonicotinic acid 

Downstream Products

• 623155-40-8 C₂₅H₂₅N₇O₄ 
• 623153-27-5 C₂₇H₃₀N₈O₃ 
• 687995-79-5 acetic acid 7-methoxy-4-{2-methyl-5-[(2-morpholin-4-yl-pyridine-4-carbonyl)-amino]-phenylamino}-quinazolin-6-yl ester 
• 263400-18-6 6-hydroxy-7-methoxy-4-[2-methyl-5-(2-morpholinopyridine-4-carboxamido)anilino]quinazoline 
• 334893-17-3 6-chloro-4-[2-methyl-5-(2-morpholinopyrid-4-ylcarbonylamino)anilino]pyrimidine 
• 334893-16-2 2-chloro-4-[2-methyl-5-(2-morpholinopyrid-4-ylcarbonylamino)anilino]pyrimidine 

Relevant academic research and scientific papers

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.

Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase

SAR studies led to the identification of 4-(3-benzoylamino-6-methyl- anilino)quinazolines as potent and selective inhibitors of p38 MAP kinase. Further optimisation led to the identification of a series of 4-(3-benzoylamino-6-methyl-anilino)pyrimidines as potent inhibitors of the p38 MAP kinase signalling pathway in vitro and in vivo. SAR studies led to the identification of 4-(3-benzoylamino-6-methyl-anilino)quinazolines as potent and selective inhibitors of p38 MAP kinase. Further optimisation led to the identification of a series of 4-(3-benzoylamino-6-methyl-anilino)pyrimidines as potent inhibitors of the p38 MAP kinase signalling pathway in vitro and in vivo.

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.

PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE AS INHIBITORS OF CYTOKINE MEDIATED DISEASE

This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0-2; Ris a group such a

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 AND THEIR USE AS CYTOKINE INHIBITORS

The invention concerns amide derivatives of formula (I) wherein R 3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R 1 and R 2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R 4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q 2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; 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.