CAS: 147098-20-2; Calcium (3R,5S,E)-7-(4-(4-Fluorophenyl)-6-Isopropyl-2-(N-Methylmethylsulfonamido)Pyrimidin-5-yl)-3,5-Dihydroxyhept-6-Enoate

专利信息

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-9932361-B2
优先权日:2013-02-20
标题:Convenient process for the preparation of statins
发明人：DE LUCCHI OTTORINO; TARTAGGIA STEFANO; FERRARI CLARK; GALVAGNI MARCO; PONTINI MARTA; FOGAL STEFANO; MOTTERLE RICCARDO; MORENO ROSA MARIA; COMELY ALEX
权利人:F I S —FABBRICA ITALIANA SINTETICI S P A
摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.

专利号:US-10022366-B2
优先权日:2013-04-23
标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
发明人：STINCHCOMB AUDRA L; GHOSH PRIYANKA
权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

专利号:WO-2014045294-A1
优先权日:2012-09-20
标题:A novel process for the preparation of rosuvastatin calcium using novel intermediates
发明人：KIRAN KUMAR RAMPALLY; MADHUSUDHAN GUTTA; SANKAR ARJUNAN; NAGENDER DINDIGALA; VENU KONDA; CHANDRA SHEKHAR KATKHAM
权利人:INOGENT LAB PRIVATE LTD
摘要:The present invention relates to novel process for the preparation of [(E)-7-[4-(4-fluorophenyl)-6-isopropy 1-2-isopropyl-2-[methyl (methyllsulfonyl)amino] pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] calcium salt using novel intermediates. Novel intermediate compounds and processes for the selective synthesis of Rosuvastatin calcium of the formula (I) using these novel intermediate compounds are disclosed. In one aspect, the present invention relates to a process for the preparation of Rosuvastatin or a pharmaceutically acceptable salt thereof of Formula I.

专利号:US-9376397-B2
优先权日:2009-02-02
标 题 :Key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; KOSMRLJ JANEZ
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.

专利号:US-9067895-B2
优先权日:2009-12-16
标题 :Processes for the preparation of key intermediate for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof
发明人：ANDRENSEK SAMO; ANZEL JOLANDA; HOCEVAR MARJETA; CASAR ZDENKO
权利人:ANDRENSEK SAMO; ANZEL JOLANDA; HOCEVAR MARJETA; CASAR ZDENKO; LEK PHARMACEUTICALS
摘要:The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.