甲磺酸雷沙吉兰 以 水 用作溶剂,化学反应 0.6H,反应生成雷沙吉兰 参考文献:Dosage Forms With An Enterically Coated Core Tablet 标题:Dosage Forms With An Enterically Coated Core Tablet 摘要:本发明提供了一种口服制剂给患者使用,包括一种经肠包被的核心片剂,套在压缩粉末或颗粒材料的环状体内.本发明还提供了一种联合使用两种或多种活性药物成分的药物剂型.本发明还提供了一种方法,包括将本发明的药物剂型用于患有胃动力障碍的患者,例如帕金森病患者.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
专利号:US-2006194971-A1 优先权日:2005-02-24 标 题 :Anethole dithiolethione and other dithiolethiones for the treatment of conditions associated with dysfunction of monoamine neruotransmission 发明人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T 权利人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T 摘要:The present disclosure relates to dithiolethione derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The present disclosure also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the present disclosure specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) n nwherein the symbols have the meanings given in the specification.
专利号:US-2008125354-A1 优先权日:2005-11-21 标题 :Selective inhibition of matrix metalloproteinases 发明人:FIELDS GREGG B; HAMMER ROBERT 权利人:UNIV FLORIDA ATLANTIC; UNIV LOUISIANA STATE 摘要:Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.
专利号:US-8461388-B2 优先权日:2007-12-24 标题 :Process for the synthesis of propargylated aminoindan derivatives 发明人:PHULL MANJINDER SINGH; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO 权利人:PHULL MANJINDER SINGH; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CIPLA LTD 摘要:A process for preparing a compound of formula (V) or its enantiomer, which comprises:n (a) reacting racemic aminoindan of formula (II) or its enantiomer with allylhalide in presence of a base and an organic solvent at a temperature ranging from 25 C to the reflux temperature of the solvent to give compound of formula (III); nn n n n n n n n n n n n Where R is n H or n n n n n n n n n n n n n n n n (b) reacting the compound (III) with halogenating agent in a suitable organic solvent to give a dihalo compound of formula (IV). n n n n n n n n n n n n n n n n (c) treating the dihalo compound (IV) with a suitable base to give compound (V).
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.