4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs
摘要:
Extrusion of one of the nitrogens of the piperazine ring of potent nootropic drugs previously described gave 4-amino-piperidine analogues that maintained high cognition enhancing activity in the mouse passive avoidance test. One of the new compounds (9. active at 0.01 mg/kg ip) may represent a new lead for the development of cognition enhancers useful to treat the cognitive deficit produced by neurodegenerative pathologies like Alzheimer's disease. (C) 2003 Elsevier Science Ltd. All rights reserved.
4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs
摘要:
Extrusion of one of the nitrogens of the piperazine ring of potent nootropic drugs previously described gave 4-amino-piperidine analogues that maintained high cognition enhancing activity in the mouse passive avoidance test. One of the new compounds (9. active at 0.01 mg/kg ip) may represent a new lead for the development of cognition enhancers useful to treat the cognitive deficit produced by neurodegenerative pathologies like Alzheimer's disease. (C) 2003 Elsevier Science Ltd. All rights reserved.
[EN] OXASPIRO [2.5] OCTANE DERIVATIVES AND ANALOGS<br/>[FR] DÉRIVÉS D'OXASPIRO[2.5]OCTANE ET ANALOGUES
申请人:ZAFGEN CORP
公开号:WO2012122264A1
公开(公告)日:2012-09-13
The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.
[EN] SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS<br/>[FR] DÉRIVÉS SPIRO [CYCLOBUTANE -1,3 '-INDOLIN] -2 '-ONE UTILISÉS EN TANT QU'INHIBITEURS DE BROMODOMAINES
申请人:ORION CORP
公开号:WO2016203112A1
公开(公告)日:2016-12-22
The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy R1, R2, R4, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
Conjugates of a GLP-I moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-I polymer conjugate may include a GLP-I moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached to a water-soluble polymer, wherein the GLP-I moiety possesses an N-methyl substituent. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached at a polymer attachment site to a water-soluble polymer, wherein the GLP-I moiety is glycosylated at a site separate from the polymer attachment site.
The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity.
SULFONYL CONTAINING BENZOTHIAZOLE INHIBITORS OF ENDOTHELIAL LIPASE
申请人:Bristol-Myers Squibb Company
公开号:US20140011799A1
公开(公告)日:2014-01-09
The present invention provides compounds of Formula (I):
as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.