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:WO-03087036-A1 优先权日:2002-04-10 标题:Stereoselective process for the synthesis of (d)-2-amino-5-phenylpentanoic or alkyl ester thereof 发明人:COMBS TONYA LYNN 权利人:LILLY CO ELI; COMBS TONYA LYNN 摘要:The present invention provides a process for preparing a compound of formula (I); wherein R is a C1-C6 alkyl; or a salt thereof; comprising:(c) hydrolyzing (D,L)-N-acetyl-2-amino-5-phenylpentanoic acid with a suitable base in the presence of D-aminoacylase to provide (D)-2-amino-5-phenylpentanoic acid; and (d) esterifying (D)-2-amino-5-phenylpentanoic acid with an alkanol. In a further embodiment, the present invention provides a process for selectively preparing (D)-2-amino-5-phenylpentanoic acid comprising hydrolyzing (D,L)-N-acetyl-2-amino-5-phenyl pentanoic acid with a suitable base in the presence of D-aminoacylase. In a still further embodiment, the present invention provides an improved process for preparing a growth hormone secretagogue compound of formula (II) disclosed herein.
专利号:US-7763734-B2 优先权日:2006-04-19 标题 :Synthesis, structure and use of bisoxazolidines for asymmetric catalysis and synthesis 发明人:WOLF CHRISTIAN; LIU SHUANGLONG 权利人:UNIV GEORGETOWN 摘要:One aspect of the invention relates to chiral bisoxazolidines and their use in asymmetric catalysis. The chiral bisoxazolidines are a novel class of compounds that is expected to find multiple applications, for example, in asymmetric synthesis. For example, a bisoxazolidine ligand enabled the catalytic enantioselective alkynylation and alkylation of a range of aromatic and aliphatic aldehydes, generating chiral propargylic alcohols and secondary alcohols in high yields and enantiomeric excess.
专利号:WO-0010565-A1 优先权日:1998-08-18 标 题 :Growth hormone secretagogues 发明人:DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 权利人:LILLY CO ELI; DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:US-6992097-B2 优先权日:1998-08-18 标 题 :Growth hormone secretagogues 发明人:HAUSER KENNETH LEE; DODGE JEFFREY ALAN; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR III CHARLES WILLIS; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROGER LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 权利人:LILLY CO ELI 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:EP-3305900-A1 优先权日:2005-12-01 标 题 :Enzymatic encoding methods for efficient synthesis of large libraries