4792-70-5Relevant academic research and scientific papers
SPIROCYCLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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, (2019/03/17)
Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
PYRAZOLE MAGL INHIBITORS
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, (2018/12/13)
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
Synthesis and biological activity of functionalized indole-2-carboxylates, triazino- and pyridazino-indoles
El-Gendy, Adel A.,Said, Mohamed M.,Ghareb, Nagat,Mostafa, Yasser M.,El-Ashry, El Sayed H.
experimental part, p. 294 - 300 (2009/04/11)
Condensation of aryl hydrazines with ethyl pyruvate gave the respective hydrazones 4-6; Fischer indolization led to substituted-1H-indole-2-carboxylic acid ethyl esters 7-9. The Mannich reaction of these compounds with formaldehyde and morpholine yielded ethyl 3-(morpholinomethyl)-substituted-1H-indole-2- carboxylates 10-12. The 5,7-dichloro-1H-indole-2-carbohydrazide 13 was cyclized with methyl orthoformate in DMF to give 6,8-dichloro[1,2,4]triazino[4,5-a]indol- 1(2H)-one 14. Vilsmeier-Haack formylation of 7-9 gave ethyl 3-formyl- substituted-1H-indole-2-carboxylates 15-17 whose 2,2′-((5-chloro-2- (ethoxycarbonyl)-1H-indol-3-yl)methylene)bis-(sulfanediyl) diacetic acid 18 was prepared. The reaction of 15 and 16 with substituted anilines by conventional and microwave methods gave ethyl 3-(N-aryliminomethyl)-5-halo-1H-indole-2- carboxylates 19-29. In a cyclocondensation reaction of 19-25 with thiolactic acid or thioglycolic acid substituted indolylthiazolidinones 30-33 were prepared. Reaction of hydrazine hydrate with 15-17 did not give the respective hydrazones but directly led to the cyclized products substituted-3H- pyridazino[4,5-b]indol-4(5H)-ones 34-36, while a reaction with 2,4-dichlorophenylhydrazine yielded the uncyclized hydrazones. The chlorination of 35 and 36 with POCl3 gave pyridazino[ 4,5-b]indoles 39 and 40, respectively; reaction of the latter compounds with morpholine gave 4-(substituted-5H-pyridazino[4,5-b]indol-4-yl)morpholine 41 and 42. Mannich reaction of 34 with formaldehyde and N-ethylpiperazine gave 8-chloro-3-((4- ethylpiperazin-1-yl)methyl)-3H-pyridazino[ 4,5-b]indol-4(5H)-one 43. The microwave assistance of selected reactions has a profound effect on the reaction speed. The structures of the new compounds were confirmed by both analytical and spectral data. Some compounds were subjected to investigations concerning their antimicrobial, tranquilizing, and anticonvulsant activities.
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: Role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity
La Regina, Giuseppe,Coluccia, Antonio,Piscitelli, Francesco,Bergamini, Alberto,Sinistra, Anna,Cavazza, Antonella,Maga, Giovanni,Samuele, Alberta,Zanoli, Samantha,Novellino, Ettore,Artico, Marino,Silvestri, Romano
, p. 5034 - 5038 (2008/03/14)
Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C. These compounds were highly effective against t
The first potent and selective non-imidazole human histamine H4 receptor antagonists
Jablonowski, Jill A.,Grice, Cheryl A.,Chai, Wenying,Dvorak, Curt A.,Venable, Jennifer D.,Kwok, Annette K.,Ly, Kiev S.,Wei, Jianmei,Baker, Sherry M.,Desai, Pragnya J.,Jiang, Wen,Wilson, Sandy J.,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 3957 - 3960 (2007/10/03)
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
Process for the preparation of substituted N-(indole-2-carbonyl)- glycinamides
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, (2008/06/13)
Processes and intermediates for preparing compounds of Formula (I).
Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
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, (2008/06/13)
PCT No. PCT/IB95/00442 Sec. 371 Date Dec. 2, 1997 Sec. 102(e) Date Dec. 2, 1997 PCT Filed Jun. 6, 1995 PCT Pub. No. WO96/39384 PCT Pub. Date Dec. 12, 1996Compounds of Formula (1) wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR8R9 or C(O)R12 as glucogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.
