专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2022356139-A1 优先权日:2019-09-03 标 题:Synthesis of deuterated aldehydes 发明人:WANG WEI 权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA 摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:US-2011105751-A1 优先权日:2008-03-31 标题:Conversion of tryptophan into beta-carboline derivatives 发明人:PIRC SAMO 权利人:LEAK PHARMACEUTICALS D D 摘要:The invention belongs in the field of organic chemistry and relates to a new shortened Pictet-Spengler type reaction for preparing isomerically pure β-carboline compounds useful for the synthesis of tadalafil.
专利号:US-9422321-B2 优先权日:2010-09-07 标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments 发明人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE 权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU 摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
专利号:US-6933303-B2 优先权日:2001-10-19 标 题:Heteroaryl-fused nitrogen heterocycles as therapeutic agents 发明人:MJALLI ADNAN M M; ANDREWS ROBERT C; XIE RONGYUAN; YARRAGUNTA RAVINDRA R; REN TAN 权利人:TRANSTECH PHARMA INC 摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
参考标题:Versatile Synthesis Of Malonamic Acid Derivatives From A β-Ketothioester 作者:Pilar López-Alvarado,Carmen Avendaño,J Carlos Menéndez |发布日期:2001.7 摘要:An Efficient Synthetic Route Is Described That Allows The Preparation Under Mild Conditions Of Several Types Of Malonamic Acid Derivatives. The S-Tert-Butyl Acetothioacetate Monoanion Reacted With Aryl Or Alkyl Isocyanates To Give β-Amidothioesters In One Step And 73-87% Yield, After Spontaneous Deacetylation Of Tricarbonyl Intermediates. Treatment Of These Thioesters With Several Aliphatic Or Aromatic