78358-08-4

Upstream product

• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 3840-31-1 (3,4,5-trimethoxyphenyl)methanol 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 178371-55-6 1-(3,4,5-trimethoxy-benzyl)-2-oxo-pyrrolidine 
• 1393734-47-8 2-(3,4-dimethoxyphenyl)-5,7-dimethoxy-3-((3,4,5-trimethoxybenzyl)oxy)-4H-chromen-4-one 
• 57944-75-9 2-(3,4,5-trimethoxybenzyl)isoindoline-1,3-dione 
• 133992-56-0 5-(azidomethyl)-1,2,3-trimethoxybenzene 
• 178371-69-2 1-(3,4,5-trimethoxy-benzyl)-3-(3,4-dimethoxy-phenylmethyl)-3-(2-t-butyldimethylsilyloxy-ethyl)-2-oxo-pyrrolidine 
• 178371-74-9 1-(3,4,5-trimethoxy-benzyl)-3-(4-fluoro-phenylmethyl)-2-oxo-pyrrolidine 
• 204510-62-3 (R,S)-1-methoxy-2-cyano-3-(3,4,5-trimethoxybenzyl)cyclopentene 
• 204510-61-2 2-Oxo-5-(3,4,5-trimethoxy-benzyl)-cyclopentanecarbonitrile 
• 18111-18-7 5-(iodomethyl)-1,2,3-trimethoxybenzene 

Relevant academic research and scientific papers

Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry

The over-expression of aminopeptidase N on diverse malignant cells is associated with the tumor angiogenesis and metastasis. In this report, one new series of leucine ureido derivatives containing the triazole moiety was designed, synthesized and evaluated as APN inhibitors. Among them, compound 13v showed the best APN inhibition with an IC50 value of 0.089 ± 0.007 μM, which was two orders of magnitude lower than that of bestatin (IC50 = 9.4 ± 0.5 μM). Compound 13v also showed dose-dependent anti-angiogenesis activities. Even at the lower concentration (10 μM), compound 13v presented similar anti-angiogenesis activity compared with bestatin at 100 μM in both the human umbilical vein endothelial cells (HUVECs) capillary tube formation assay and the rat thoracic aorta rings test. Moreover, compared with bestatin, 13v exhibited comparable, if not better in vivo anti-metastasis activity in a mouse H22 pulmonary metastasis model.

SUBSTITUTED 4-(1H-BENZIMIDAZOL-2-YL)[1,4]DIAZEPANES USEFUL FOR THE TREATMENT ALLERGIC DISEASES

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4] diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. 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.

Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. 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.

Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease

The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. 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.

Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases

The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. 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.

Substituted piperidines useful for the treatment of allergic diseases

The present invention relates to novel substituted piperidine derivatives of the formula STR1stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic diseases including: seasonal rhinitis, allergic rhinitis, and sinusitis.

2,4-diamino-6,7-dihydro-5?-cyclopentacf|pyrimidine analogues of trimethoprim as inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase

Three previously unreported (R,S)-2,4-diamino-5-[(3,4,5-trimethoxyphenyl)alkyl]-6,7-dihydro5.ff- cyclopenta[rf]pyrimidines 15a-c were synthesized as analogues of trimethoprim (TMP) and were tested as inhibitors of Pneumocystis carinii, Toxoplasma gondii,