专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-4613610-A 优先权日:1984-06-22 标题 :Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives 发明人:WAREING JAMES R 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, each of R2 and R5 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenyl, phenoxy or benzyloxy, each of R3 and R6 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R4 and R7 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, not more than one of R2 and R3 is benzyloxy, not more than one of R5 and R6 is trifluoromethyl, not more than one of R5 and R6 is phenoxy, and not more than one of R5 and R6 is benzyloxy, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2- or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R10 is hydrogen or C1-3alkyl, wherein R12 is a physiologically acceptable and hydrolyzable ester group, and M is a pharmaceutically acceptable cation, with the provisos that (i) the-X-Z group is in the 4- or 5-position of the pyrazole ring, and (ii) the R1 group and the -X-Z group are ortho to each other, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-5064953-A 优先权日:1983-12-29 标 题:Intermediates cephalosporin derivatives 发明人:OHNISHI HARUO; KOSUZUME HIROSHI; MIZOTA MASAHIRO; SUZUKI YASUO; MOCHIDA EI 权利人:MOCHIDA PHARM CO LTD 摘要:The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof. The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton. The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
专利号:US-2014051854-A1 优先权日:2010-07-26 标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
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