abstract |
5-PHENYL-PENTANOIC ACID DERIVATIVES, THEIR PREPARATION PROCESSES, PHARMACEUTICAL COMPOSITION UNDERSTANDING THE SAME AND SEPARATION PROCESS OF THESE DERIVATIVES. The present invention relates to compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R1 is optionally alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or substituted alkynyloxy; R 2 - is alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 - R 5 -, -NHC (= Y) R 4 -, -NHC (= Y) NR 5 - R ~ x ~, -NHC (= 0) OR ~ 4 ~, -NHSO ~ 2 ~ R ~ 4 ~, C (= Y) NR ~ 4 ~ R ~ 5 ~, C (= O) OR ~ 6 ~ (where Y is oxygen or sulfur), OR ~ 5 ~, -O (C = O) NR ~ 4 ~ R ~ 5 ~, O-acyl, S (O) ~ m ~ R ~ 4 ~, -SO ~ 2 ~ N ( R 4 -) - 2 -, cyano, amidino or guanidino (where R 4 - is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl in is an integer of 0 R 2 is hydrogen or R 4, R 4 is R 4 or -SO 2 N (R 4) -2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl heterocyclylalkyl or cycloalkylalkyl; R3 is hydrogen, fluoro, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4-, -OC (= O) NR4-5 R5, O-acyl, NH4. 2 ~, NR ~ 4 ~ R ~ 5 ~, -NHC (= Y) R ~ 4 ~, -NHC (= Y) NR ~ 5 ~ R ~ x ~, -NHC (= O) OR ~ 4 ~, - NHSO ~ 2 ~ R ~ 4 ~, and to synthetic processes thereof. are further directed to pharmaceutical compositions comprising the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, kidney disease, tumor metastases, and other inflammatory disorders characterized by overexpression and overactivation of matrix metalloproteinase using the compounds. |