502434-61-9

Upstream product

• 502607-38-7 (2S)-2-mesyloxymethyl-4-methyl-3,4-dihydro-2H-1,4-benzoxazine 
• 99-76-3 methyl 4-hydroxylbenzoate 
• 1978-38-7 2-fluoro-N-methylaniline 
• 824-48-6 N-(2-fluorophenyl)formamide 
• 348-54-9 2-Fluoroaniline 
• 502434-54-0 (2S)-3-(N-(2-fluorophenyl)-N-methylamino)-1, 2-propanediol 
• 502434-59-5 [(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methyl 4-methylbenzenesulfonate 
• 386702-75-6 (S)-2-hydroxymethyl-4-methyl-3,4-dihydro-2H-benzo[1,4]oxazine 

Downstream Products

• 502606-10-2 benzyl [2,5-dimethyl-1-(4-{[(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methoxy}benzoyl)-1H-indol-3-yl]acetate 
• 502606-12-4 benzyl [5-chloro-2-methyl-1-(4-{[(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methoxy}benzoyl)-1H-indol-3-yl]acetate 
• 502606-11-3 benzyl [5-fluoro-2-methyl-1-(4-{[(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methoxy}benzoyl)-1H-indol-3-yl]acetate 
• 1321938-57-1 benzyl [5-methoxy-2-methyl-1-(4-{[(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methoxy}benzoyl)-1H-indol-3-yl]acetate 
• 502607-40-1 4-{[(2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl]methoxy}benzoyl chloride 

Relevant academic research and scientific papers

Discovery of selective indole-based prostaglandin D2 receptor antagonist

A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D2 receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure-activity relationship study is presented.

CARBOXYOIC ACID COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT

A carboxylic acid compound represented by formula (I): (meanings of the symbols in the formula are as mentioned in the specification) and a pharmaceutical agent comprising the compound. Since the compound represented by formula (I) binds to a DP receptor and shows antagonistic activity for the DP receptor, it is useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

INDOLE DERIVATIVES

Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification. and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.

INDOLE DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

Indole derivatives represented by formula (I) ???wherein all symbols represent the same as that in specification), production methods thereof, and DP receptor antagonist comprising them as active ingredients. Since the compounds of formula (I) binds and antagonizes to DP receptor, they are useful for the prevention and/or treatment against allergic diseases, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, cerebrovascular disorder, pleuritis complicated by rheumatoid arthritis, ulcerative colitis.