Combination of FBPase inhibitors and insulin sensitizers for the treatment of diabetes
申请人:Metabasis Therapeutics, Inc.
公开号:US06756360B1
公开(公告)日:2004-06-29
Pharmaceutical compositions containing an FBPase inhibitor and an insulin sensitizer are provided as well as methods for treating diabetes and diseases responding to increased glycemic control, an improvement in insulin sensitivity, a reduction in insulin levels, or an enhancement of insulin secretion.
Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors
作者:Robert H. Springer、M. B. Scholten、Darrell E. O'Brien、Thomas Novinson、Jon P. Miller、Roland K. Robins
DOI:10.1021/jm00345a009
日期:1982.3
3,7-disubstituted 6-carbethoxypyrazolo [1,5-a] pyrimidines and 3,7-disubstituted 6-ethoxypyrazolo-[1,5-a]pyrimidines have been prepared and evaluated as adenosine cyclic 3',5'-phosphate (cAMP) phosphodiesterase (PDE) inhibitors vs. the low Km enzyme isolated from beef heart, rabbit lung, and kidney preparations. The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors
The methods for the preparation of O- and N-functional orthocarbonic acid derivatives are reviewed, and a survey of the reactions of these compounds with electrophilic and nucleophilic reagents is given. 1. Synthesis of Orthocarbonic Acid Esters 1.1 Reaction of Substituted Trichloromethanes with Alcohols, Alkoxides, Phenols, or Phenoxides 1.2. Reaction of Substituted Dichloromethanes with Alcohols or Phenols 1.3. Reaction of Trialkoxycarbenium Salts with Alkoxides 1.4. Reaction of Cyanic Acid Esters with Alcohols 1.5. Thermolysis of Cyclic Carbonic Acid Derivatives 1.6. Reaction of Carbon Disulfide with Thallium(I) Alkoxides 1.7. Reaction of Carbon Disulfide with Organotin Compounds 1.8. Reaction of Zinc Xanthates with Alcohols 1.9. Transesterification of Orthocarbonic Acid Esters 2. Synthesis of Orthocarbamic Acid Esters 2.1. Reaction of Trihetero-substituted Carbenium Ions with Alkoxides 2.2. Alcoholysis of Tetramethylurea Diethyl Acetal 2.3. Transesterification of Orthocarbamic Acid Esters 2.4. Spirocyclic Orthocarbamic Acid Esters from Organotin Compounds 3. Synthesis of Bis[dialkylamino]-dialkoxymethanes (Tetraalkylurea Dialkyl Acetals) 3.1. Reaction of Bis[dialkylamino]-ethoxycarbenium Tetrafluoroborates with Alkoxides 3.2. Reaction of Tetraalkylurea Dichlorides (Chloroformamidinium Chlorides) with Alcohols or Alkoxides 3.3. Reaction of 2,2-Dichloro-1,3-benzodioxole with Amines 3.4. Spirocyclic Urea Acetals from Organotin Compounds 4. Synthesis of Alkoxytris[dialkylamino]methanes 5. Synthesis of Tetrakis[dialkylamino]methanes 6. Reactions of O- and N-Functional Orthocarbonic Acid Derivatives 6.1. Reactions with Electrophilic Agents 6.2. Reactions with Nucleophilic Agents 6.3. Miscellaneous Reactions of Orthocarbonic Acid Derivatives
Azabicyclic compounds for the treatment of disease
申请人:——
公开号:US20030232853A1
公开(公告)日:2003-12-18
The invention provides compounds of Formula I:
1
wherein Azabicyclo is
2
These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which &agr;7 is known to be involved.
Regiospecific synthesis of α-ketoacetals by rearrangement of α-bromo-α-fluoroketones
作者:Norbert De Kimpe、Roland Verhé、Laurent De Buyck、N. Schamp
DOI:10.1016/0040-4039(80)80018-9
日期:1980.1
α-Ketoacetals, derived from alkylaryl-α-diones and with acetalized benzoyl moiety, were synthesized by alkoxide induced rearrangement of α-bromo-α-fluoroalkylarylketones.