专利号:US-3682895-A 优先权日:1970-07-17 标题 :Synthesis of 3-hydroxy-5-bufa-20,22-dienolide 发明人:PETTIT GEORGE R; FESSIER DYRAL C; PAUIL KENNETH D 权利人:GEORGE R PETTIT; DYRAL C FESSIER; KENNETH D PAUIL 摘要:THERE IS PROVIDED A NOVEL METHOD OF SYNTHEESIZING 5ABUFADIENOLIDES, WHICH ARE USEFUL INTERMEDIATES IN THE TOTAL SYNTHESIS OF BUFALIN, A CARDIAC ACTIVE COMPOUND. EPIANDROSTERONE ACETATE IS CONVERTED INTO 3B - ACETOXYL-5APREGNANE-21-AL WHICH UNDERGOES CHAIN EXTENSION TO METHYL 3B-ACETOXYL-20-FORMYL-21-NOR-5A-CHOLANATE WHICH IS RING CLOSED TO FORM THE 3B - ACETOXY-5-A-BUF-20(21)-ENOLIDE WHICH IS DEHYDROGENATED TO THE CORRESPONDING BUFADIENOLIDE.
专利号:EP-2097079-B1 优先权日:2006-11-30 标题:Modulation of prostaglandin/cyclooxygenase metabolic pathways 发明人:WUELFERT ERNST 权利人:HUNTER FLEMING LTD 摘要:A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2. The compounds are 7-hydroxy-steroids or condensed indoles.
专利号:US-4215044-A 优先权日:1979-04-23 标题:Synthesis of α-fluorocarbonyl compounds 发明人:MIDDLETON WILLIAM J 权利人:DU PONT 摘要:Process for preparing an organic compound of the formula R 2 R 2 CFC(O)R 3 , which process comprises contacting and reacting in a reaction mixture which includes an inert solvent, at a temperature of -40° C. to -100° C., ROF and ##STR1## R is polyfluoroperhaloalkyl of 1-6 carbon atoms or FOCF 2 ; R 1 is hydrocarbyl of 1-6 carbon atoms; n each R 2 is selected from H, alkyl of 1-17 carbon atoms, cycloalkyl of 3-6 carbon atoms, aryl, heteroaryl and such alkyl, cycloalkyl, aryl and heteroaryl substituted by halogen or alkoxy of 1-6 carbon atoms; n R 3 is selected from H, alkyl and haloalkyl of 1-16 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl and haloaryl, OSi(R 1 ) 3 , OH, NH 2 , alkoxy of 1-6 carbon atoms, aryloxy, NHR 1 and NR 1 2 wherein R 1 is alkyl of 1-6 carbon atoms, N-arylamino and nitrogen or sulfur heterocyclic of 4-5 carbon atoms; n R 3 and one R 2 taken together is a diradical which with the Câ• C group is carbocyclic, heterocyclic or haloheterocyclic, and recovering from the reaction mixture the compound of the formula R 2 R 2 CFC()R 3 .
专利号:US-6147159-A 优先权日:1998-09-30 标 题 :Compositions for organic synthesis on solid phase and methods of using the same 发明人:HU YONGHAN; LABADIE JEFFREY W; PORCO JR JOHN ANTHONY; TROST BARRY MARTIN 权利人:ARGONAUT TECHNOLOGIES 摘要:A modified solid support for use in solid phase synthesis which comprises: a solid support having a linker group extending therefrom having the general formula: wherein R1 and R2 are each independently selected from the group consisting of alkyl, cycloalkyl, aryl, alkoxy, aryloxy, fluorine, chlorine, iodine and bromine.
专利号:US-6333317-B1 优先权日:1997-03-28 标 题:Regulation of amyloid precursor protein (APP) expression by administration of an estrogenic compound 发明人:LEE ROBERT K K; WURTMAN RICHARD J 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:It has been discovered that lipophilic hormones that interact with cytosolic or nuclear receptors regulate APP expression and synthesis, through modification of APP mRNA stability and/or regulation of APP gene transcription and translation activities. These studies demonstrate that the treatment of brain cells with estrone or 17β-estradiol results in a reduction in the level of APP holoprotein expression, without a concomitant change in the total level of cell protein. The reduction in the level of APP holoprotein caused by estrone or 17β-estradiol is also expected to reduce the production of neurotoxic APP fragments. In as much as estrogen deficiency in postmenopausal women is associated with a higher incidence of Alzheimer's disease, this discovery opens the possibility that estrogen therapy may prevent some of the neurodegenerative and cognitive changes associated with Alzheimer's disease, aging and other disease conditions associated with such neurodegenerative and cognitive decline.
专利号:US-4267376-A 优先权日:1978-09-08 标 题 :Steroid synthesis 发明人:TSUJI JIRO 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:A compound having the general formula ##STR1## wherein R 1 is a lower alkyl group, R 2 is hydrogen or a lower alkyl group and Y is a protected hydroxyl group, for example, (±)-3β-tert.butoxy-2,3,3a,4,5,7,8,9,9aβ,9bα-decahydro-3aβ-methyl-6-(3-butenyl)-1H-benz(e)inden-7-one, which is an intermediate for steroids, is prepared by dehydrative cyclization of a compound of the general formula ##STR2## wherein the symbols of R 1 , Y and R 2 are same as defined above.