专利号:US-10768157-B2 优先权日:2015-10-20 标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples 发明人:KABIR ABUZAR; FURTON KENNETH G 权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.
专利号:US-9382288-B2 优先权日:2010-10-06 标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action 发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO 权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG 摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
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-11306343-B2 优先权日:2014-08-12 标 题:3α-hydroxysteroid dehydrogenase mutants and process for the preparation of ursodeoxycholic acid 发明人:HUMMEL WERNER; BAKONYI DANIEL 权利人:PHARMAZELL GMBH 摘要:The invention provides novel 3α-hydroxysteroid dehydrogenase mutants, sequences that code for these enzyme mutants, methods for producing the enzyme mutants, and the use thereof in enzymatic reactions of cholic acid compounds, and in particular in the production of ursodeoxycholic acid (UDCA). The invention further provides processes for the synthesis of UDCA using the enzyme mutants and the production of UDCA using recombinant microorganisms that have been subjected to multiple modifications.
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-9295679-B2 优先权日:2008-03-25 标 题:Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity 发明人:NJAR VINCENT; BRODIE ANGELA; GEDIYA LALJI K 权利人:UNIV MARYLAND 摘要:Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.
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