专利号:US-8476426-B2 优先权日:2011-02-14 标题 :Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:PEGLION JEAN-LOUIS; DESSINGES AIMEE 权利人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERVIER LAB 摘要:Process for the synthesis of ivabradine of formula (I): n nand addition salts thereof with a pharmaceutically acceptable acid.
专利号:US-6642367-B2 优先权日:1995-03-06 标 题:Process for the synthesis of 2′-O-substituted pyrimidines and oligomeric compounds therefrom 发明人:COOK PHILLIP DAN; SANGHVI YOGESH S; SPRANKLE KELLY G; ROSS BRUCE S; GRIFFEY RICH H; SPRINGER ROBERT H 权利人:ISIS PHARMACEUTICALS INC 摘要:Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5′ positions. Monomeric sub-units having these modifications may be further modified at the 2′ position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-6753449-B2 优先权日:2001-10-09 标题 :Cleavable linker for solid phase synthesis 发明人:GUO MAOJUN 权利人:ARQULE INC 摘要:Cleavable alkene-containing linkers and supports useful for the solid phase synthesis of chemical compounds, and combinatorial libraries of compounds, are disclosed. Also disclosed are methods of making and using the linkers and supports.
专利号:US-6001991-A 优先权日:1996-10-04 标题 :Antisense oligonucleotide modulation of MDR P-glycoprotein gene expression 发明人:DEAN NICHOLAS M; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:Oligonucleotides are provided which are specifically hybridizable with nucleic acids encoding the human MDR1 P-glycoprotein. Also disclosed are methods of using the oligonucleotides of the invention in methods of modulating the expression of MDR genes, inhibition of which leads to inhibition of the synthesis of MDR P-glycoproteins and thereby inhibits cellular multidrug resistance. Such inhibition is desirable for treating various hyperproliferative disorders or diseases, such as various cancers, in conjunction with chemotherapy utilizing one or more chemotherapeutic agents, for preventing or modulating the development of multidrug resistance during the chemotherapeutic treatment of an animal, and for resensitizing hyperproliferative MDR cells in an animal having such diseases or disorders that has been previously exposed to chemotherapeutic agents. Modified derivatives of the oligonucleotides of the invention, such as chimeras and conjugates (e.g., of an oligonucleotide and a lipophilic moiety, such as cholesterol), are also disclosed. The biological activity and cellular uptake of oligonucleotides is enhanced by such modifications.
专利号:US-5948903-A 优先权日:1991-01-11 标题:Synthesis of 3-deazapurines 发明人:COOK P DAN; ACEVEDO OSCAR L; ANDREWS ROBERT S 权利人:ISIS PHARMACEUTICALS INC 摘要:This invention relates to compounds based on the 3-deazapurines ring system and to methods for making such compounds. The invention also generally relates to the field of 'antisense' agents, agents that are capable of specific hybridization with a nucleotide sequence of an RNA. The 3-deazapurine-containing compounds of this invention can be useful for modulating the activity of RNA when incorporated into oligonucleotides. Oligonucleotides and their analogs are used for a variety of therapeutic and diagnostic purposes, such as treating diseases, regulating gene expression in experimental systems, assaying for RNA and for RNA products through the employment of antisense interactions with such RNA, diagnosing diseases, modulating the production of proteins and cleaving RNA in site specific fashions.