专利号:US-12098115-B2 优先权日:2016-09-15 标 题:Methods and compositions for terpenoid synthesis 发明人:GRENNING ALEXANDER JAMES 权利人:UNIV FLORIDA 摘要:In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are γ-allyl Knoevenagel adducts or quasi γ-allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise α-alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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-4460786-A 优先权日:1980-07-10 标题 :Process for the selective addition of a compound having an activated carbon atom onto a substituted conjugated diene 发明人:MOREL DIDIER 权利人:RHONE POULENC IND 摘要:The selective addition of a compound having an activated carbon atom onto the carbon atom in the 4-position of a buta-1,3-diene carrying a hydrocarbon substituent on the carbon atom in the 2-position is achieved by reacting the compound having the activated carbon atom with the buta-1,3-diene carrying the hydrocarbon substituent in water or in an aqueous-alcoholic mixture in the presence of a catalyst which consists of at least one water-soluble phosphine and at least one rhodium compound, the catalyst being in solution in the water or aqueous alcoholic mixture. The products obtained are useful as precursors of intermediates for the synthesis of vitamins and perfumes.
专利号:US-8288565-B2 优先权日:2009-07-16 标题 :Process for the synthesis of (2S,3AR,7AS)-octahydro-1H-indole carboxylic acid as an intermediate for trandolapril 发明人:CHEMBURKAR SANJAY R; REDDY RAJARATHNAM E; REAMER DOUGLAS M; PAVLINA JOHN T; ULREY STEPHEN S; KOTECKI BRIAN J 权利人:CHEMBURKAR SANJAY R; REDDY RAJARATHNAM E; REAMER DOUGLAS M; PAVLINA JOHN T; ULREY STEPHEN S; KOTECKI BRIAN J; ABBOTT LAB 摘要:A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.
专利号:US-5233044-A 优先权日:1989-06-08 标题:Active esters for solid phase peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectrophotometric monitoring and automation of peptide synthesis.
专利号:US-9951011-B2 优先权日:2013-09-20 标题 :Carbazole compounds for in vivo imaging 发明人:TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER 权利人:GE HEALTHCARE LTD 摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
参考文献:10.1007/s10895-011-0915-2 摘要:Patil SR, Shelar DP, Rote RV, Jachak MN. A fluorescence study of new angular polycyclic blue light-emitting pyrazolo[3,4-h][1,6]naphthyridine and their interaction with bovine serum albumin (BSA). J Fluoresc. 2011 Nov;21(6):2037–52. doi: 10.1007/s10895-011-0915-2.