CAS: 31430-18-9; Methyl (6-(Thiophene-2-Carbonyl)-1H-Benzo[d]Imidazol-2-yl)Carbamate

上下游产品

(R)-((S)-2-Amino-propionylamino)-[2-methoxycarbonylamino-5-(thiophene-2-carbonyl)-benzoimidazol-1-yl]-acetic acid((S)-2-Benzyloxycarbonylamino-propionylamino)-[2-methoxycarbonylamino-6-(thiophene-2-carbonyl)-benzoimidazol-1-yl]-acetic acid benzyl ester ((S)-2-Benzyloxycarbonylamino-propionylamino)-[2-methoxycarbonylamino-5-(thiophene-2-carbonyl)-benzoimidazol-1-yl]-acetic acid benzyl ester

(2R)-2-[[(2S)-2-Aminopropanoyl]Amino]-2-[2-(Methoxycarbonylamino)-5-(Thiophene-2-Carbonyl)Benzimidazol-1-Yl]Acetic Acid置于n-羟基丁二酰亚胺,N,N'-二环己基碳二亚胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,以22%的收率获得产物诺考达唑
参考文献:Synthèse Et Activité Antinéoplastique De Dérivés Alanyl-2-Glycyl Peptide De Nocodazole
标题:Synthèse Et Activité Antinéoplastique De Dérivés Alanyl-2-Glycyl Peptide De Nocodazole
摘要:
DOI:10.1016/0223-5234(89)90079-2

专利信息

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-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-12146136-B2
优先权日:2020-03-26
标题:Synthesis of modified oligonucleotides with increased stability
发明人：KHVOROVA ANASTASIA; ROUX LOÃ?C MAURICE RENÉ JEAN; YAMADA KEN
权利人:UNIV MASSACHUSETTS
摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.

专利号:US-10266565-B2
优先权日:2011-04-12
标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN
权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人：CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

专利号:US-10047122-B2
优先权日:2013-03-14
标 题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：QIAN WENJIAN; PARK JUNG EUN; LAI CHRISTOPHER C; KELLEY JAMES A; LEE KYUNG S; BURKE JR TERRENCE R
权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.