Amide compounds of amino acid 3 - thieno 2,3 pyridin - 2 - substituted carboxylic acid, processes for their preparation, Pharmaceutical compositions containing them and their use in the treatment of diseases mediated by the IKB Kinase (IKK) Complex.

摘要

1. Useful compounds in the quinase inhibitors of IKB quinasa (IKK) complex. These compounds can be used to treat IKK treated diseases, including autoimmune diseases, inflammation and cancer. In addition, this document describes the synthesis of drugs containing these compounds and the procedures for their manufacture. Item 1: a formula compound (1), wherein: R1 is (a) a phenyl or non phenyl compound selected from furanio, tienilo, piridio, pirrolilo, imidazolinlo and benzofuranilo, which can be replaced by 1-2r4; (b) an isocyclohexane selected from 1-piperidinilo, 1-piperazinilo, 1-pirrolidinium and 4-morpholinil,Alternative 1 to 2 groups of c1-6-c1-5 co2quette C1-5, phenyl, benzene-oh and - C (o) isomerized asphalt were substituted, endosulfan, smallpox, pyridine and pyridine (c) R7 (CH2) Mo -,(D) R7OCH2-(E) R7 (CH2) mNH-(F) R7 (CH2) p (CH 3DCH) m-(g) C1-6, one or two R8 (H) alcoxi c1-8, one or two R8 (I) c1-8s (o) n -, optional, partially or completely halogenated and optional;Optionally, partially or completely halogenated and optionally replaced with one or two R8 (J) - n (R5) (R6),This is life. This is life. notesin which R ?? it is R7, pyridyl or -CH3; R 2 is heteroaryl selected from the group consisting of furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, indolizyl, pyrazinyl, indolizyl benzothienyl, indazolyl, benzimidazolyl, benzothiazolyl, benzoxazolyl, purinyl, quinolizinyl, quinolinyl, isoquinolinyl, cinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, naftirininyl, pteridinyl, carbazolyl, acridinyl, fenazinyl, fenazinyl, fenazinyl, fenazinyl, fenazinyl, phenozinyl, phenozinyl, fenazinyl, phenozinyl, phenozinyl, phenozinyl, phenozinyl, phenozinyl, phenozinyl, phenozinyl, phenozinyl, phenyl. R3 is -OH or -H;R4 is selected from C1-6, alcox C1-6, hydroxy C1-6, octanol-hc-6, halide-cn, CO2H, co2coquilo C1-6, s (o) C1-6, s (o) n-p-tolilo, NO2, oh, CF3, and-n (R5) (R6).- NHC (O) NHalquilo C1-6 -C (O) N (R5) (R6)phenyl optionally substituted with halogen, C1-6 alkyl, -CN or C1-6 alkoxy, and heteroaryl selected from R2; R5 and R6 are independently selected from H, C1-6alkyl, -C (O) C1-6alkyl, -SO2C1-6alkyl, phenyl, pyridyl, benzyl, piperidinyl, phenylethyl and (CH3) 3COC (O) -;XY oxy; C10 oxy; C1 oxy oxy oxy; R6; This is 0, 1 or 2; P is 0, 1, 2, or 3; Z is an o-o-ch2 link;And a mixture of salts, esters, polyphosphate esters, isomers and pharmaceutically acceptable isomers thereof. ILO Convention No. 14: preparation of a formula compound (1): wherein R1, R2, R3 and Z are as defined in ILO Convention No. 1, including the procedure of reacting a formula compound (2) with a formula amine (3) under reduced conditions to provide an ideal formula compound (1). ILO Convention No. 15: procedures for developing a formula compound (1), wherein R1, R2, R3 and Z are defined in ILO Convention No. 1, including procedures for making a formula compound react (4),Where x is a laser group with a formula compound (5),If there is enough base to provide the ideal formula compound (1).