202797-02-2

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• 56888-56-3 cyclononanone p-toluenesulfonyl hydrazone 
• 68-12-2 N,N-dimethyl-formamide 
• 3350-30-9 cyclononanone 

Relevant academic research and scientific papers

Discovery of 2-aminothiazole-4-carboxamides, a novel class of muscarinic M3 selective antagonists, through solution-phase parallel synthesis

Synthesis and structure-activity relationship of a new class of muscarinic M3 selective antagonists were described. In the course of searching for a muscarinic M3 antagonist with a structure distinct from those of the 2-(4,4-difluorocyclopentyl)-2-phenylacetamide derivatives, we identified a thiazole-4-carboxamide derivative (1) as a lead compound in our in-house chemical collection. Since this compound (1) showed relatively low binding affinity (K1 = 140 nM) for M3 receptors in the human binding assays, we tried to improve its potency and selectivity for M 3 over M1 and M2 receptors by derivatization of 1 through a combinatorial approach. A solution-phase parallel synthesis effectively contributed to the optimization of each segment of 1. Thus, we have identified a cyclooctenylmethyl derivative (3e) and a cyclononenylmethyl derivative (3f) as representative M3 selective antagonists in this class.

Cyclic compounds and uses thereof

Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1is an optionally substituted five- or six-membered ring group; X1is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1and E4are each optionally substituted carbon or the like; E2and E3are each oxygen or the like; and a and b are each a single bond or a double bond); X2is a divalent group constituting a straight chain moiety; Z1is a divalent cyclic group or the like; Z2is a free valency or the like; and R2is optionally substituted amino or the like.

Structure-activity relationships of xanthene carboxamides, novel CCR1 receptor antagonists

The structure-activity relationships of xanthene carboxamide derivatives on the CCR1 receptor binding affinity and the functional antagonist activity were described. Previously, we reported a quaternarized xanthen-9-carboxamide 1 as a potent human CCR1 receptor antagonist that was derived from a xanthen-9-carboxamide lead 2a. Further derivatization of 2a focusing on installing an additional substituent into the xanthene ring resulted in the identification of 2b-1 with IC50 values of 1.8 nM and 13 nM in the binding assay using human CCR1 receptors transfected CHO cells and in the functional assay using U937 cells expressing human CCR1 receptors, respectively.

CYCLIC COMPOUNDS AND USES THEREOF

Compounds of general formula (1) or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five-to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.

Chemokine receptor antagonists

PCT No. PCT/JP97/02548 Sec. 371 Date Jan. 29, 1999 Sec. 102(e) Date Jan. 29, 1999 PCT Filed Jul. 23, 1997 PCT Pub. No. WO98/04554 PCT Pub. Date Feb. 5, 1998The present invention relates to a compound of the general formula: wherein each of R1 and R2 which