CAS: 65733-15-5; H-D-Tyr(Bzl)-Oh

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CAS号556-02-5 D-酪氨酸 | CAS号100-44-7 氯化苄 | CAS号100-39-0 溴化苄

📜D-酪氨酸置于三乙胺,氯仿体系中,用 Trifluoracetic Acid-Dichloromethane 作为反应溶剂,化学反应 1.0H,反应生成 O-苄基-D-酪氨酸
参考文献:Pharmacologically Active Peptide Derivatives And Pharmaceutical
标题:Pharmacologically Active Peptide Derivatives And Pharmaceutical
摘要:肽衍生物及其与药学上可接受的酸或碱盐,具有一般式(I),其中r=-H,C1-C3烷基,C1-C3酰基,C1-C4烷基的烷氧羰基; R1 =-H,C1-C3烷基; R2 =-H,-Oh,-Or'2,其中r'2 = C1-C3烷基,C1-C3酰基,苄基; R3 =-H,-Ch3; N = 1,2 R4 =-H,-Cooh,-Conh2,-Coor'4,其中r'4 = C1-C3烷基,苄基; R5 =-H,4-Oh,3,4-Oh,-Or'5,其中r'5 = C1-C3烷基,C1-C3酰基,苄基; R6 =-Oh,-Nh2,-Or'6,其中r'6 = C1-C3烷基,苄基; 具有镇痛,抗病毒,免疫调节药理学性质,并且含有它们作为活性成分的药物制剂.

专利信息

专利号:US-7067554-B2
优先权日:2000-05-30
标 题 :Method for the synthesis of compounds of formula I and their uses thereof
发明人：MJALLI ADNAN M M; GOPALASWAMY RAMESH; AVOR KWASI A; WYSONG CHRISTOPHER L; ANDREW PATRON
权利人:TRANSTECH PHARMA INC
摘要:This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

专利号:AU-2005200425-A1
优先权日:2000-05-30
标题 :A method for the synthesis of compounds of formula 1 and their uses thereof

专利号:US-2006189578-A1
优先权日:2000-05-30
标题:Method for the synthesis of compounds of formula I and their uses thereof

专利号:US-2004097407-A1
优先权日:2000-05-30
标题:Method for the synthesis of compounds of formula I and their uses thereof

专利号:US-2002006957-A1
优先权日:2000-05-30
标题 :Method for the synthesis of compounds of formula I and their uses thereof

专利号:US-9695191-B2
优先权日:2009-08-05
标题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN
权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG
摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.