LEUCOTRIENE ANTAGONIST

Japanese Patent JPS59205339

A

Compounds of the formula: and their pharmaceutically acceptable salts, which are novel, are antagonists of leukotrienes of C4, D4 and E4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents and are made into pharmaceutical compositions. In the formula, R1 is a radical of formula COOR3, where R3 is hydrogen or an alkyl or cycloalkyl group containing not more than six carbon atoms; CH2OH; CHO; CH2NHSO2R4, where R4 is OH; C1-6 alkyl, C1-6 alkoxy phenyl, phenyl substituted by C1-3 alkyl or C1-3 alkoxy, halogen, hydroxy, haloalkyl, COOH, CN, formyl, C1-6 acyl or C1-4 peRfluoroalkyl; CN; or CON(R5)2, where each R5, independently of the other, is H, OH or C1-4 alkyl; a tetrazolyl radical, a monocyclic or bicyclic heterocyclic ring containing an acidic @hydroxyl@ group; or a radical of formula where each s, independently of the other, is 0, 1, 2 or 3; R2 is (A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms, one being N, and the other (if any) being N or S, each ring in the heterocyclic radical having 5 or 6 atoms, or (B) a radical X-R8 where X is O, S or NH and R8 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical derived from an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom that is N, O or S in the ring; and each R10, independently of the other is H or C1-4 alkyl; R6 is H or C1-4 alkyl; R2 is a halogen atom; and R9 is a hydrogen atom or hydroxyl group.

WO/2001/055086	ALKYNYLSUBSTITUTED PROPIONIC ACID DERIVATIVES AND THEIR USE AGAINST DIABETES AND OBESITY
JPS52153932	PRODUCTION OF 22 ARYLALKANE
WO/2003/051821	SUBSTITUTED PHENYLPROPIONIC ACID DERIVATIVES AS AGONISTS TO HUMAN PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR ALPHA (PPAR)

PATORISU BERANJIYAA
IBUAN GIYUINDON
REJIYAN FUOOTEIN
KURISUCHIYAN YOAKIMU
JIYOSHIYUA ROKATSUCHI

JP7878084A

November 20, 1984

April 20, 1984

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MERCK FROSST CANADA INC

C07C69/734; A61K31/12; A61K31/165; A61K31/18; A61K31/19; A61K31/215; A61K31/275; A61K31/41; A61K31/433; A61P11/00; A61P27/16; A61P29/00; A61P37/08; C07C45/00; C07C45/71; C07C49/84; C07C49/86; C07C51/00; C07C59/64; C07C59/90; C07C67/00; C07C69/003; C07C231/00; C07C231/12; C07C233/18; C07C235/34; C07C239/00; C07C253/00; C07C255/37; C07C259/06; C07C301/00; C07C303/40; C07C307/02; C07C311/00; C07C325/00; C07C327/20; C07C327/28; C07D257/04; C07D285/10; C07D303/18; (IPC1-7): A61K31/12; A61K31/165; A61K31/18; A61K31/19; A61K31/215; A61K31/275; A61K31/41; C07C49/84; C07C49/86; C07C59/64; C07C69/003; C07C69/734; C07C83/10; C07C103/26; C07C103/30; C07C103/76; C07C121/75; C07C143/72; C07C143/86; C07C153/07; C07D257/04; C07D285/10

Masao Okabe

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