35028-38-7

Upstream product

• 75-44-5 phosgene 
• 100-60-7 N-methylcyclohexylamine 
• 32315-10-9 bis(trichloromethyl) carbonate 

Downstream Products

• 68721-98-2 Cyclohexyl-methyl-carbamic acid 2,5-dimethyl-4-methylsulfanyl-phenyl ester 
• 1026305-82-7 cyclohexyl-methyl-carbamic acid 3-(2-tert-butoxycarbonylamino-propyl)-phenyl ester 
• 209394-74-1 cyclohexyl-methyl-carbamic acid 3-tert-butoxycarbonylamino-indan-5-yl ester 
• 1207262-57-4 2-(5-{4-[cyclohexy(methyl)carbamoyl]piperazin-1-yl}-1,2,4-oxadiazol-3-yl)-1-methyl-1H-3,1-benzimidazol-3-ium trifluoroacetate 
• 1233855-46-3 3-(1-(cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide 
• 1233852-83-9 N-cyclohexyl-N-methyl-4-phenyl-1H-imidazole-1-carboxamide 
• 1443159-47-4 5-(biphenyl-4-ylmethyl)-N-cyclohexyl-N-methyl-1H-tetrazole-1-carboxamide 
• 1443159-51-0 5-(biphenyl-4-ylmethyl)-N-cyclohexyl-N-methyl-2H-tetrazole-2-carboxamide 
• 1548620-14-9 N-cyclohexyl-N-methylpiperidine-1-carboxamide 
• 1548620-11-6 1-benzyl-3-cyclohexyl-1,3-dimethylurea 
• 1548620-08-1 N-cyclohexyl-4-(3,5-dinitrophenyl)-N-methyl-1H-imidazole-1-carboxamide 

Relevant academic research and scientific papers

Design, synthesis and anti-inflammatory effects of novel 9-O-substituted-berberine derivatives

Berberine, an isoquinoline alkaloid in many medicinal herbs, has been found to possess broad pharmacological activities. A series of novel C-9-O-substituted-berberine derivatives have been synthesized and their anti-inflammatory effects evaluated both in vitro and in vivo. Compared to berberine, the new synthetic berberine derivatives 3i and 5e exhibit significantly improved inhibitory activities against the release of NO, TNF-α and IL-6. Furthermore, derivatives 3i and 5e were found to inhibit more effectively the migration of neutrophils and primitive macrophage in transgenic zebrafish larvae with injury-provoked inflammation. Pre-treatment with derivatives 3i or 5e could lead to a concentration-dependent decrease in nuclear factor-κB (NF-κB) p65 and NF-κB inhibitor α (IκBα) phosphorylation and inducible nitric oxide synthase (iNOS) expression in lipopolysaccharide (LPS)-induced RAW264.7 cells, which suggested that the anti-inflammatory activities of berberine derivatives 3i and 5e are related to their suppression of the NF-κB signal pathway.

Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors

At present, inhibitors of α/β-hydrolase domain 6 (ABHD6) are viewed as a promising approach to treat inflammation and metabolic disorders. This article describes the development of 1,2,5-thiadiazole carbamates as ABHD6 inhibitors. Altogether, 34 compounds were synthesized, and their inhibitory activity was tested using lysates of HEK293 cells transiently expressing human ABHD6 (hABHD6). Among the compound series, 4-morpholino-1,2,5-thiadiazol-3-yl cyclooctyl(methyl)carbamate (JZP-430) potently and irreversibly inhibited hABHD6 (IC50 = 44 nM) and showed ～ 230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL), the main off-targets of related compounds. Additionally, activity-based protein profiling indicated that JZP-430 displays good selectivity among the serine hydrolases of the mouse brain membrane proteome. JZP-430 has been identified as a highly selective, irreversible inhibitor of hABHD6, which may provide a novel approach in the treatment of obesity and type II diabetes.

PROCESS FOR THE SYNTHESIS OF SUBSTITUTED UREA COMPOUNDS

A process for preparing a substituted urea compound of Formula II or Formula I, or a pharmaceutically acceptable salt or ester thereof, Formula II, Formula I the process comprising the reaction of an intermediate of Formula II' or Formula 1', Formula II',

Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring

In the present study, we have further extended the structure-activity relationships for the tetrazolyl ureas class of compounds as potential FAAH and/or MAGL inhibitors, by replacing the dimethylamino group of the parent compounds 1 and 2 with bulkier groups or by introducing on the distal phenyl ring of 1 and 2 a selected set of substituents. Some of the new compounds (16, 20, 21, 25, and 28) inhibited FAAH potently (IC50 = 3.0-9.7 nM) and selectively (39- to more than 141-fold) over MAGL, while tetrazole 27 turned out to be a promising dual FAAH-MAGL inhibitor of potential therapeutic use. Covalent docking studies on FAAH indicated that the binding modes of tetrazoles 1-32 did not display a unique pattern. The ability of tetrazoles 1-32 to act as TRPV1 and TRPA1 modulators was also investigated.

1,2,4-OXADIAZOLE SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS SMO ANTAGONISTS

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.

Carbostyril derivatives

PCT No. PCT/JP96/02892 Sec. 371 Date May 29, 1998 Sec. 102(e) Date May 29, 1998 PCT Filed Oct. 4, 1996 PCT Pub. No. WO97/12869 PCT Pub. Date Apr. 10, 1997A carbostyril derivative of the formula (1): wherein A is lower alkylene, R is H, halogen or lower al

2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities

In order to search for anti-arteriostenotic agents, a series of 2(1H)- quinolinone derivatives was synthesized and evaluated for anti-thrombotic activity and for anti-hyperplastic activity. From this series, (-)-6-[3-[3- cyclopropyl-3-[(1R,2R)-2-hydroxycycyclohexyl]ureido]propoxy]-2(1H)- quinolinone (1p, OPC-33509) was selected as the best candidate by balancing the efficacy on anti-thrombosis and anti-hyperplasia.

CORRELATION BETWEEN THE STRUCTURE AND ACTIVITY OF AMINOSTIGMINE DERIVATIVES CONTAINING VARIOUS SUBSTITUENTS AT THE NITROGEN ATOM OF THE CARBAMOYL GROUP

Sixteen aminostigmine derivatives containing various substituents at the nitrogen atom of the carbamoyl group have been prepared, and their anticholine esterase activity in vitro, ionization constants, hydrophobicity, and toxicity have been determined.