CAS: 112568-12-4; N-((4R,7R,10R,13S,16S,19R)-19-(((S)-1-(((S)-1-((S)-2-(((R)-1-Amino-1-Oxopropan-2-yl)Carbamoyl)Pyrrolidin-1-yl)-6-(Isopropylamino)-1-Oxohexan-2-yl)Amino)-4-Methyl-1-Oxopentan-2-yl)Carbamoyl)-7-(4-Chlorobenzyl)-13-(Hydroxymethyl)-4-(Naphthalen-2-Ylmethyl)-16-(4-(Nicotinamido)Butyl)-2,5,8,11,14,17-Hexaoxo-10-(Pyridin-3-Ylmethyl)-3,6,9,12,15,18-Hexaazatricosan-23-yl)Nicotinamide

上下游产品

CAS号98266-33-2 B°C-D-3-(3-吡啶基)-丙氨酸 | CAS号57292-44-1 B°C-D-4-氯苯丙氨酸 | CAS号76985-10-9 B°C-3-(2-萘基)-D-丙氨酸 | CAS号78545-07-0 O-benzoyl-N-(te...

Boc-3-(3-吡啶基)-D-丙氨酸,N-叔丁氧羰基-D-4-氯苯丙氨酸,Boc-3-(2-萘基)-D-丙氨酸,Boc-Ser(Bzl)-Oh,Alkaline Earth Salt Of/the/ Methylsulfuric Acid 反应生成安替肽
参考文献:释放促性腺激素的激素拮抗剂,在5和6位具有nω三唑基鸟氨酸,-赖氨酸或-P-氨基苯丙氨酸残基.
标题:释放促性腺激素的激素拮抗剂,在5和6位具有nω三唑基鸟氨酸,-赖氨酸或-P-氨基苯丙氨酸残基.
摘要:为了用作人类的生育调节剂,促性腺激素释放激素(gnrh)拮抗剂必须具有极强的作用力和长效作用,并且必须表现出微不足道的副作用,例如刺激组胺释放.为此,我们最近合成了一系列具有标准ac-Dnal1-Dcpa2-Dpal3取代基的类似物,其中鸟氨酸,赖氨酸或对氨基苯丙氨酸(aph)的n氨基氨基官能团被转化为氨基三唑基(atz )在5和6位的衍生物,并在7和10位进一步修饰.测试了类似物与垂体细胞膜结合,在肥大细胞测定中释放组胺,抑制cast割的雄性小鼠促黄体生成激素(lh)分泌的能力.大鼠或培养的垂体细胞,并干扰完整雌性大鼠的排卵.皮下注射(sc)50毫克的azaline A(7,[ac-Dnal1,Dcpa2,Dpal3,Lys5(atz),Dlys6 ++ +(atz),Ilys8,Dala10] Gnrh)溶于0.2 Ml水性介质中显着抑制去势雄性大鼠的lh释放达24 H,相同剂量的azaline
Doi:10.1021/jm00101A003

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:US-2004259801-A1
优先权日:2000-08-17
标 题 :Method for the synthesis of peptide salts, their use and pharmaceutical preparations containing the peptide salts

专利号:US-11440881-B2
优先权日:2019-05-09
标题 :Thiosemicarbazates and uses thereof
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

专利号:US-5169935-A
优先权日:1990-06-20
标 题:Method of making peptides
发明人：HOEGER CARL A; THEOBALD PAULA G; PORTER JOHN S; RIVIER JEAN E F
权利人:SALK INST FOR BIOLOGICAL STUDI
摘要:Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the alpha -amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone. Following cleavage from the resin and removal of any protecting groups still remaining, the peptide is appropriately purified, thus requiring only a single purification to be carried out while forming a synthetic peptide including residues for which the modified amino acids are not readily commercially available.