235097-95-7

Upstream product

• 459-04-1 4-Fluorophenylacetyl chloride 
• 159707-16-1 (4S)-benzyl-3-[2'-(4-fluorophenyl)acetyl]-2-oxazolidinone 
• 810680-77-4 (S)-2-(4-fluorophenyl)pent-4-enoyl chloride 
• 494802-92-5 (S)-2-(4-fluorophenyl)-4-pentenoic acid 
• 235097-94-6 (S)-2-(4-fluorophenyl)pent-4-enoic acid,N-methyl amide 

Downstream Products

• 334824-79-2 N-[2-(4-fluoro-phenyl)-pent-4-enyl]-N-methyl-benzenesulfonamide 
• 334824-88-3 N-[2-(4-fluoro-phenyl)-4-oxo-butyl]-N-methyl-benzenesulfonamide 
• 209349-07-5 1'-(3-((S)-(4-Fluorophenyl))-4-(N-(phenylsulfonyl)(methylamino))butyl)-spiro(2,3-dihydrobenzothiophene-3,4'-piperidine) 
• 917572-26-0 3-bromo-N-[(2S)-2-(4-fluorophenyl)penta-4-en-1-yl]-N-methyl-5-(trifluoromethyl)benzamide 
• 930783-06-5 3-bromo-N-{(2S)-2-(4-fluorophenyl)-4-[3-(4-acetylpiperazin-1-yl)azetidin-1-yl]butyl}-N-methyl-5-(trifluoromethyl)benzamide 
• 917572-25-9 3-bromo-N-[(2S)-2-(4-fluorophenyl)-4-oxobutyl]-N-methyl-5-(trifluoromethyl)benzamide 

Relevant academic research and scientific papers

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement for and optimization of the C-2 phenyl fragment. The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X = H, 3-F, 3-Cl, 3-Me).

Carboxy substituted acylic carboxamide derivatives

The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): STR1and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.

SUBSTITUTED N-METHYL-N-(4-(4-(1H-BENZIMIDAZOL-2-YL) {1,4}DIAZEPAN-1-YL)-2-(ARYL)BUTYL) BENZAMIDES USEFUL FOR THE TREATMENT OF ALLERGIC DISEASES

The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)[1,4]diazepan-1-yl)-2-(aryl)butyl)benzamide derivatives of the formula: STR1 stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.