CAS: 298-93-1; 2-(4,5-Dimethylthiazol-2-yl)-3,5-Diphenyl-2H-Tetrazol-3-Ium Bromide

Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于n-溴代丁二酰亚胺(Nbs),乙酸乙酯体系中,化学反应生成噻唑兰
参考文献:Beyer; Pyl,Chemische Berichte,1954,Vol. 87,P. 1505,1510
标题:Beyer; Pyl,Chemische Berichte,1954,Vol. 87,P. 1505,1510

专利信息

专利号:US-9783519-B2
优先权日:2015-06-18
标 题:Palladium/silver co-catalyzed tandem reactions synthesis of phenylacetophenone derivatives by oxabenzonorbornadienes with terminal alkynes and their anti-tumor or anti-cancer activities
发明人：BIAN ZHAOXIANG; LIN CHENGYUAN; MU HUAIXUE; FAN BAOMIN; ZHOU YONGYUN; CHEN JINGCHAO; LU AIPING; CHAN ALBERT SUN-CHI
权利人:UNIV HONG KONG BAPTIST UNIV; UNIV YUNNAN MINZU
摘要:This invention relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds. More particularly, it relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds comprising phenylacetophenone derivatives using oxabenzonorbornadienes with terminal alkynes.

专利号:US-7173021-B2
优先权日:2004-09-02
标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers
发明人：WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA
权利人:TIANJIN NORTH PHARM SCI TECH C
摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent

专利号:US-8278483-B2
优先权日:2006-02-07
标题:Process for synthesis of glycomimicking cationic amphiphiles
发明人：MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA
权利人:MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA; COUNCIL SCIENT IND RES
摘要:The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.

专利号:US-8450456-B2
优先权日:2007-12-21
标题:Activating peptide of the synthesis of aquaporins and cosmetic and/or pharmaceutical composition containing it
发明人：DAL FARRA CLAUDE; DOMLOGE NOUHA; BOTTO JEAN-MARIE
权利人:DAL FARRA CLAUDE; DOMLOGE NOUHA; BOTTO JEAN-MARIE; ISP INVESTMENTS INC
摘要:The present invention concerns a peptide of the general formula (I): n R 1 -(AA) n -X 1 —X 2 —X 3 -Pro-X 4 —X 5 —X 7 -(AA) p -R 2 , capable of activating the synthesis of proteins of the family of aquaporins. n The present invention also concerns a cosmetic, nutraceutical or pharmaceutical composition, comprising a peptide of general formula (I) as active principle. The invention also relates to the use of this new active principle in a cosmetic or nutraceutical composition, intended to improve the moisturizing and the barrier function of the epidermis and intended to stimulate cutaneous regeneration. The invention also relates to the use of this new active principle to realize a pharmaceutical composition, and in particular a dermatological composition, intended to regulate and/or stimulate the activity of the aquaporins and to thus treat the pathological dryness of the skin or mucosa. The invention also relates to a method of cosmetic treatment intended to prevent or combat against dryness of the skin and mucosa, and the manifestations of cutaneous ageing.

专利号:US-9623125-B2
优先权日:2011-10-24
标 题:Controlled synthesis of polyglutamates with low polydispersity and versatile architectures
发明人：VICENT DOCON MARIA JESUS; BARZ MATTHIAS; CANAL FABIANA; CONEJOS SANCHEZ INMACULADA; DURO CASTANO AROA; ENGLAND RICHARD MARK
权利人:FUND DE LA COMUNIDAD VALENCIANA “CENTRO DE INVESTIG PRINCIPE FELIPEâ€?
摘要:Polyglutamates are well known to be highly biocompatible, biodegradable and multifunctional polymers, which have been already used as building blocks in polymer drug conjugates and polymeric micelles. Those systems have been applied to various medical applications ranging from therapy to molecular imaging. Furthermore a polyglutamic acid (PGA) paclitaxel conjugate has already entered clinical studies (Opaxioâ„¢ PGA-PTX conjugate currently in phase III of Clinical trials). n In this context, a synthetic pathway to a plethora functional polyglutamates (homopolymers, block-co-polymers, tribocks) with well-defined structure, adjustable molecular weight (Mw) and low dispersity (D=Mw/Mn<1.2) applying the ring opening polymerization (ROP) of N-carboxyanhydrides (NCA) has been developed. Additionally, the acid moieties of the polyglutamates can be activated with 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) and various functionalities can be easily introduced by “post-polymerization modificationâ€? yielding a set orthogonal reactive attachment sides. The reactive moieties, such as azides, maleimides, thiols, akynes (linear or cyclic) offer the opportunity of specific conjugation of the drugs, targeting moieties or markers. Besides introducing reactive groups the functionalization strategy was also used for PEGylation of PGA reducing charge induced interactions and therefore pharmacological properties, such as blood circulation time may be adjusted. n In summary, a tool kit of various polyglutamates has been developed enabling the synthesis of a variety of polymer drug conjugates or polymer based imaging agents. The functional polymeric precursors developed will allow us to functionalize and therefore adjust the polymer properties to a desired aplication.

专利号:US-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.