107618-33-7

Upstream product

• 107618-21-3 4-(2-amino-4-fluoro-phenylamino)-piperidine-1-carboxylic acid ethyl ester 
• 57-13-6 urea 
• 530-62-1 1,1'-carbonyldiimidazole 
• 503-38-8 trichloromethyl chloroformate 
• 75-44-5 phosgene 
• 345-17-5 1-chloro-4-fluoro-2-nitrobenzene 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 58859-46-4 ethyl 4-aminopiperidine-1-carboxylate 
• 364-74-9 1,4-difluoro-2-nitrobenzene 
• 107618-14-4 4-(4-fluoro-2-nitro-phenylamino)-piperidine-1-carboxylic acid ethyl ester 

Downstream Products

• 58859-77-1 5-fluoro-1,3-dihydro-1-(4-piperidinyl)-2H-benzimidazol-2-one 
• 1469924-46-6 C₂₁H₂₀F₃N₃O₃ 
• 1469924-47-7 C₂₁H₂₀F₃N₃O₃ 
• 633310-95-9 C₃₁H₄₁FN₆O₂ 
• 633311-57-6 C₃₀H₃₁F₃N₆O₂ 
• 633311-66-7 C₃₀H₃₁F₃N₆O₂ 
• 1469924-76-2 C₄₁H₅₇FN₆O₆ 
• 1469924-77-3 C₄₀H₄₇F₃N₆O₆ 
• 1469924-78-4 C₄₀H₄₇F₃N₆O₆ 
• 1469924-58-0 C₁₉H₂₆FN₃O 
• 1469924-59-1 C₁₈H₁₆F₃N₃O 
• 1469924-60-4 C₁₈H₁₆F₃N₃O 
• 618900-33-7 C₁₆H₂₀FN₃O₂S 

Relevant academic research and scientific papers

Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists

A novel series of benzimidazolone-containing histamine H 3-receptor antagonists were prepared and their structure-activity relationship was explored. These benzimidazolone analogs demonstrate potent H3-receptor binding affinities, no P450 enzyme inhibition, and strong H3 functional activity. Compound 1o exhibits the best overall profile with H3Ki = 0.95 nM and rat AUC = 12.9 μM h.

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

This Letter describes the first account of the synthesis and SAR, developed through an iterative analogue library approach, of analogues of the highly selective M1 allosteric agonist TBPB. With slight structural changes, mAChR selectivity was maintained, but the degree of partial M1 agonism varied considerably.

BENZIMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose

Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine

In our continuing effort to identify CGRP receptor antagonists for the acute treatment of migraine, we have undertaken a study to evaluate alternative 4-substituted piperidines to the lead dihydroquinazolinone 1. In this regard, we have identified the piperidinyl-azabenzimidazolone and phenylimidazolinone structures which, when incorporated into the benzodiazepine core, afford potent CGRP receptor antagonists (e.g., 18 and 29). These studies produced a potent analog (18) which overcomes the instability issues associated with the lead structure 1. A general pharmacophore for the 4-substituted piperidine component of these CGRP receptor antagonists is also presented.

TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2/

1-(4-PIPERIDINYL) BENZIMIDAZOLONES AS HISTAMINE H3 ANTAGONISTS

Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined

Piperidines

Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.

alpha 1a adrenergic receptor antagonists

This invention relates to novel compounds, their synthesis and use as selective alpha 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Alpha 1a adrenergic receptor antagonists

This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.