专利号:WO-0029400-A3 优先权日:1998-11-19 标题 :Procedure for synthesis of n-[2[[[5- [(dialkilamino) methyl]-2- furanyl] methyl]thyo] ethyl]-n'- alkyl-2-nitro1,1 alkenediamines and their hydrochlorides 发明人:STANKOVI SLOBODAN; STOJANOVIC NEBOJSA; STOJICIC STANISLAVA; MILENOVIC DRAGAN 权利人:DD ZDRAVLJE FARMACEUTSKO HEMIJ; STANKOVI SLOBODAN; STOJANOVIC NEBOJSA; STOJICIC STANISLAVA; MILENOVIC DRAGANE 摘要:This invention is related to the procedure for obtaining of the therapeutically active N-[2[[[5-[(dialkylamino methyl]-2-furanyl] methyl] thio] ethyl]-N'-alky-2-nitro1,1 alkenediamines) of formula (I) and their hydrochlorides of formula (II), where R1, R2 and R3 are alkyl groups (C1-C4), and X is nitro-alkenic group by reaction of 2[[[5-[(dimethylamino-methyl-2-furanyl]methyl]thio]-ethanamine-hydrochloride) and N-methyl-1(methylthio-2-nitroethenamine) in the aqueous environment at the mild temperature.
专利号:US-4967007-A 优先权日:1989-05-10 标 题 :Improved process for the preparation of 1-substituted amino-1-substituted thio-2-nitro alkenes 发明人:DESHMUKH ABDUL R A S; BHAWAL BABURAO M; SHIRALKAR VASUDEO P; RAJAPPA SRINIVASACHARI 权利人:COUNCIL SCIENT IND RES 摘要:A process is disclosed for the manufacture of 1-substituted amino-1-substituted thio-2 nitro alkenes of the general formula: (R1NH) (R2S) Câ•?CR3 (NO2) wherein R1, R2, R3, may be same or different and may consist of hydrogen, alkyl, aryl or arylalkyl groups or combinations thereof. These alkenes are prepared by reacting a primary amine with a compound of sulfur in the presence of a primary catalyst to obtain a carbonimidodithioic acid salt which is converted to a corresponding ester which is thereafter reacted with a nitro compound in the presence of a secondary catalyst. 1-methylamino-1-methylthio-2-nitroethene is an important intermediate in the synthesis of Rantitidine and Nizatidine which are used as effective drugs in the treatment of peptic ulcers and associated gastrointestinal disorders.
专利号:WO-0029400-A2 优先权日:1998-11-19 标 题 :Procedure for synthesis of n-[2[[[5- [(dialkilamino) methyl]-2- furanyl] methyl]thyo] ethyl]-n'- alkyl-2-nitro1,1 alkenediamines and their hydrochlorides
专利号:US-9861636-B2 优先权日:2014-04-29 标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors 发明人:HE WEI 权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD 摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.