CAS: 888216-25-9; 3-(2,4-Dihydroxy-5-Isopropylphenyl)-4-(1-Methyl-1H-Indol-5-yl)-1H-1,2,4-Triazol-5(4H)-One

上下游产品

34H32N4O3C34H32N4O3 5-nitroindole 1-methyl-5-nitro-1H-indole 1-methyl-1H-indol-5-amine

📜1-甲基-1H-吲哚-5-胺置于palladium On Activated Charcoal,氢气,一水合肼,溶剂黄146,三乙胺,Sodium Hydroxide,Potassium Hexacyanoferrate(Iii)体系中,用 1,4-二氧六环,甲醇,乙醇,二氯甲烷 作为反应溶剂,化学反应 12.42H,反应生成 3-(2,4-二羟基-5-异丙基苯基)-4-(1-甲基吲哚-5-基)-5-羟基-4H-1,2,4-噻唑
参考文献:一种改进的hsp90抑制剂ganetespib的制备方法
标题:一种改进的hsp90抑制剂ganetespib的制备方法
摘要:本发明本发明公开了一种改进的hsp90抑制剂ganetespib的制备方法,通过改进合成方法中的原料,将较贵的几种原料进行了设计合成,降低了成本,还能有效提高产率;对原有的几种毒性大活性低的原料进行了替换;对反应过程中的温度,压强以及时间进行了更为精确的改进,使得产率大大提高.本发明注重于工艺改进,过程更加的容易进行,毒性更低,成本更加便宜,最重要的是大大提高了各步骤以及最终产物的产率.

专利信息

专利号:US-2008125587-A1
优先权日:2006-05-25
标 题 :Synthesis of triazole compounds that modulate HSP90 activity
发明人：CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA
权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA
摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2015217006-A1
优先权日:2014-02-06
标题:Al-f-18-labeled, al-f-19-labeled and ga-68-labeled gastrin-releasing peptide receptor (grpr)-antagonists for imaging of prostate cancer
发明人：MCBRIDE WILLIAM J; CHATALIC KRISTELL L S; HENDRIKS-DE JONG MARION; BOERMAN OTTO C; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F-, 19 F- or 68 Ga-labeled molecules of use in PET, SPECT and/or MRI imaging of prostate cancer. Preferably, the 18 F, 19 F or 68 Ga is attached to a chelator moiety on a prostate cancer targeting molecule, more preferably a bombesin analog, more preferably a GRPR antagonist, most preferably JMV5132 or JMV4168. The 18 F or 19 F may form a complex with a group IIIA metal to promote binding to the chelators. The labeled molecules may be used to detect, diagnose and/or image prostate cancer, including metastatic prostate cancer, in vivo.

专利号:WO-2014018862-A1
优先权日:2012-07-27
标 题 :Pharmaceutical compositions comprising a heat shock protein inhibitor and a; purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer
发明人：FANG YE
权利人:CORNING INC; FANG YE
摘要:A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.

专利号:US-2017107577-A1
优先权日:2014-03-11
标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
发明人：AL-EJEH FARES
权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

专利号:US-2016045626-A1
优先权日:2007-01-11
标题 :Methods and Compositions for Improved Labeling of Targeting Peptides
发明人：MCBRIDE WILLIAM J; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a therapeutic or diagnostic isotope, such as 61 Cu, 62 Cu, 64 Cu, 67 Cu, 18 F, 19 F, 66 Ga, 67 Ga, 68 Ga, 72 Ga, 111 In, 177 Lu, 44 Sc, 47 Sc, 86 Y, 88 Y, 90 Y, 45 Ti or 89 Zr, preferably 18 F or 19 F. More preferably, the targeting peptide is NOTA-octreotate, NOTA-MPAA-octreotate, pyridine-NOTA-octreotate or triazole-NOTA-octreotate. The labeled targeting peptides may be used for detection, diagnosis, imaging and/or treatment of sst 2 + tumors, such as neuroendocrine tumors.