Bocdene and Mocdene Derivatives of Catechols and Catecholamines
摘要:
[GRAPHICS]Catechols react chemoselectively, in the presence of either alcohols, 1,2-diols, or simple phenols, with tert-butyl propynoate and with methyl propynoate to give 2-Boc-ethylidene (Bocdene) and 2-Moc-ethylidene (Mocdene) acetals, respectively, in 96-100% yields within 30 min at room temperature, provided that 150 mol % of DMAP is added. Cleavage of these acetals with pyrrolidine readily takes place (at room temperature!) in 95-100% yields, By taking advantage of the features of Bocdene acetals, novel catecholamine-related phosphate mimetics have been prepared.
Bocdene and Mocdene Derivatives of Catechols and Catecholamines
摘要:
[GRAPHICS]Catechols react chemoselectively, in the presence of either alcohols, 1,2-diols, or simple phenols, with tert-butyl propynoate and with methyl propynoate to give 2-Boc-ethylidene (Bocdene) and 2-Moc-ethylidene (Mocdene) acetals, respectively, in 96-100% yields within 30 min at room temperature, provided that 150 mol % of DMAP is added. Cleavage of these acetals with pyrrolidine readily takes place (at room temperature!) in 95-100% yields, By taking advantage of the features of Bocdene acetals, novel catecholamine-related phosphate mimetics have been prepared.
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR LOWERING LIPIDS AND LOWERING BLOOD GLUCOSE LEVELS
申请人:Smith-Swintosky L. Virginia
公开号:US20070155821A1
公开(公告)日:2007-07-05
The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) or formula (II) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and/or an anti-obesity agent.
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
申请人:Smith-Swintosky L. Virginia
公开号:US20070155827A1
公开(公告)日:2007-07-05
The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one antidepressant.
Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
申请人:Bourrie Bernard
公开号:US20070167469A1
公开(公告)日:2007-07-19
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I)
and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF PAIN
申请人:Smith-Swintosky L. Virginia
公开号:US20070155822A1
公开(公告)日:2007-07-05
The present invention is a method for the treatment of pain comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as described herein. The present invention is further directed to methods for the treatment of pain comprising co-therapy with analgesic agent(s) and a compound of formula (I) or formula (II) as described herein.
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES AS NEUROPROTECTIVE AGENTS
申请人:Smith-Swintosky L. Virginia
公开号:US20070155823A1
公开(公告)日:2007-07-05
The present invention is a methods for neuroprotection, for treating an acute neurodegenerative disorder, for treating a chronic neurodegenerative disorder and/or for preventing neuron death or damage following brain, head and/or spinal cord trauma or injury comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.