CAS: 37566-39-5; 5-Bromo-1,3,4-Thiadiazol-2-Amine

上下游产品

[1,3,4]Thiadiazol-2-ylamin formic acid thiosemicarbazide 1-[5-(4-nitro-benzenesulfonylamino)-[1,3,4]thiadiazol-2-yl]-pyridinium betaine 4-(5-bromo-[1,3,4]thiadiazol-2-yl)-3-thio-allophanic acid methyl ester H-[1,3,4]thiadiazol-2-ylideneamine5-bromo-3-methyl-3H-[1,3,4]thiadiazol-2-ylideneamine 2-bromo-5-nitro-[1,3,4]thiadiazole

2-氨基-1,3,4-噻二唑置于溴,Sodium Acetate,溶剂黄146体系中,化学反应 14.0H,以91%的收率获得2-氨基-5-溴-1,3,4-噻二唑
参考文献:Pparγ靶向分子对接和合成一些新的酰胺和脲取代的1,3,4-噻二唑衍生物作为抗糖尿病化合物
标题:Pparγ靶向分子对接和合成一些新的酰胺和脲取代的1,3,4-噻二唑衍生物作为抗糖尿病化合物
摘要:Ppar-γ激动剂通过促进胰岛素引导的细胞对血糖的吸收,提高了胰岛素敏感性,并避免了血糖紊乱.因此,在目前的工作中,Ppar-γ已被选作分子对接研究的目标,以设计有效的激动剂.通过这项研究工作,已努力制备1,4-,3-噻二唑衍生物的酰胺和脲系列,即4-取代-N-(5-(4-(1-(哌啶子基)1-哌啶基)-1,3],4-(2-噻二唑基)苯甲酰胺(4A-F)和1-(4-取代苯基)-3-(5-(4-(1-哌啶基)1-哌啶基)-1,3,4-(2-噻二唑基)脲(6A-F)对接评分和药理动物研究数据均提示含电子给体的化合物4F和6F是最有效的抗糖尿病活性分子,接近标准药物吡格列酮.进一步观测到,与含吸电子衍生物相比,含未取代芳环的衍生物也具有相当大的作用(4A和6A).在比较了酰胺和尿素系列的生物学数据后,得出的结论是,尿素(6A-F)系列比酰胺系列更有效.
Doi:10.1002/jhet.3941

专利信息

专利号:US-5847149-A
优先权日:1994-01-27
标 题 :Thiadiazole derivatives, process for their preparation, and their use as precursors for the production of liquid crystals
发明人：FUSS ROBERT WALTER; MANERO JAVIER; SCHLOSSER HUBERT; WINGEN RAINER
权利人:HOECHST AG
摘要:Thiadiazole derivatives of the formula (I) n n X-B-A.sup.1 -(M.sup.1 -A.sup.2 -).sub.m (M.sup.2 -A.sup.3).sub.n -R.sup.1(I n n ) n in which the symbols and indices have the following meanings: n X is Cl, Br or I; n B is 1,3,4-thiadiazole-2,5-diyl; n A 1 , A 2 and A 3 are identical or different and are substituted or unsubstituted 1,4-phenylene, pyrazine-2,5-diyl, pyridazine-3,6-diyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene, 1,3,4-thiadiazole-2,5-diyl, 1,3-dioxane-2,5-diyl, 1,3-dithiane-2,5-diyl, 1,3-thiazole-2,4-diyl, 1,3-thiazole-2,5-diyl, thiophene-2,4-diyl, thiophene-2,5-diyl, piperazine-1,4-diyl, piperazine-2,5-diyl, naphthalene-2,6-diyl, bicyclo 2.2.2!octane-1,4-diyl, or 1,3-dioxaborinane-2,5-diyl; n M 1 and M 2 are identical or different and are --CO--O--, --O--CO--, --O--CO--O--, --O--CS--O--, --CH 2 --O--, --O--CH 2 --, --CHâ•?CH--, --C.tbd.C-- or a single bond; n R 1 is --O-benzyl, H, an alkyl group having 1 to 12 carbon atoms or an alkoxy group having 1 to 12 carbon atoms; n m and n are 0 or 1. n The novel compounds allow the synthesis of a wide range of 1,3,4-thiadiazole derivatives, as employed, for example, as components of liquid-crystal mixtures, in a significantly reduced number of synthesis stes.

专利号:US-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2009099200-A1
优先权日:2005-06-09
标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-8653082-B2
优先权日:2009-02-25
标题:6-phenyl-2-[((piperidin-4-ylmethyl)-piperazin-1YL) or piperazin 1-ylmethyl)-piperidin-1-yl)]-imidazo[2,1-B][1,3,4]thiadiazole derivatives and their use
发明人：NIR URI; SHPUNGIN SALLY; YAFFE ETAI; COHEN MOSHE
权利人:NIR URI; SHPUNGIN SALLY; YAFFE ETAI; COHEN MOSHE; URIFER LTD
摘要:Heterocyclic compounds of formula (I), (II), (III) or a pharmaceutically acceptable salt thereof: n nwherein R 1 , R 2 and R 3 are each independently selected from hydrogen, halogen, C 1-6 alkyl, C 2-6 alkenyl, N—(C 1-6 alkyl) 2 , and N—(C 2-6 alkenyl) 2 , the C 1-6 alkyl and C 2-6 alkenyl being straight or branched; and Y 1 and Y 2 are selected from N and CH where one of Y 1 and Y 2 is N and the other is CH, are provided. Also provided are the synthesis of and pharmaceutical compositions including these compounds. These compounds and pharmaceutical compositions thereof can be used for the treatment of disorders, and in particular, cancer.

专利号:US-2011301143-A1
优先权日:2009-02-23
标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.

专利号:US-2012010186-A1
优先权日:2009-03-23
标题:Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES
权利人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES; MERCK FROSST CANADA LTD
摘要:Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.