CAS: 119-44-8; 2-Aminopteridine-4,6-Diol

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CAS号146196-27-2 2-amino-6-chlor... | CAS号1131-35-7 4,6-Pteridinedi... | CAS号492-11-5 无色喋呤 | CAS号49653-17-0 Ethyl ethoxyhyd... | CAS号2757-91-7 2-amino-4,6-dio... | CAS号492-11-5 无色喋呤 | CAS号645-93-2 三聚氰胺一酰胺 | CAS号56-40-6 甘氨酸 | CAS号6538-79-0 pterorhodin

📜2-氨基-4-羟基蝶啶置于双氧水体系中,用 四氢呋喃 用作溶剂,化学反应 6.0H,反应生成酵母粉
参考文献:用于癌症免疫治疗的高效 Toll 样受体 7/8 双激动剂的基于结构的设计
标题:用于癌症免疫治疗的高效 Toll 样受体 7/8 双激动剂的基于结构的设计
摘要:Toll 样受体 7 和 8 的激活已成为癌症免疫治疗的一种有前途的策略.在此,我们报告了一系列基于吡啶并 [3,2-D ] 嘧啶的 Toll 样受体 7/8 双激动剂的设计和合成,这些激动剂对 Tlr7 和 Tlr8 表现出强效且接近等效的激动活性.在体外,化合物24E和25A在人外周血单核细胞测定中显着诱导 Ifn-α,Ifn-γ,Tnf-α,Il-1β,Il-12P40 和 Ip-10 的分泌.在体内,化合物24E,24M和25A通过重塑肿瘤微环境显着抑制 Ct26 荷瘤小鼠的肿瘤生长.此外,化合物24E,24M和25A显着提高了 Pd-1/pd-L1 阻断的抗肿瘤活性.特别是,化合物24E与抗 Pd-L1 抗体结合导致肿瘤完全消退.这些结果表明,Tlr7/8 激动剂(24E,24M和25A)作为单药或与 Pd-1/pd-L1 阻断剂联合用于癌症免疫治疗具有巨大潜力.
Doi:10.1021/acs.Jmedchem.1C00179

专利信息

专利号:US-6153615-A
优先权日:1991-12-26
标 题 :Blocking induction of tetrahydrobioterin to block induction of nitric oxide synthesis
发明人：GROSS STEVEN S
权利人:CORNELL RES FOUNDATION INC
摘要:Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and/or pterin salvage pathway tetrahydrobiopterin synthesis antagonists are administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylactic or curative effect for endotoxin- or cytokine-induced hypotension or for restoration of vascular contractile sensitivity to pressor agents in the treatment of such hypotension). The tetrahydrobiopterin synthesis antagonist may be administered with α 1 -adrenergic agonist or with nitric oxide synthase inhibitor. The tetrahydrobiopterin synthesis antagonists are also administered to attenuate inflammation caused by induced nitric oxide production in immune cells. Unwanted counterproductive or side effects can be eliminated or ameliorated by administration additionally of levodopa with or without carbidopa and L-5-hydroxytryptophane.

专利号:US-6274581-B1
优先权日:1991-12-26
标 题 :Blocking induction of tetrahydrobiopterin to block induction of nitric oxide synthesis
发明人：GROSS STEVEN S
权利人:CORNELL RES FOUNDATION INC
摘要:Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and/or pterin salvage pathway tetrahydrobiopterin synthesis antagonist are administered to inhibit nitric oxide synthesis from arginine in vascular smooth muscle cells in a subject in need of such inhibition (e.g. for prophylactic or curative effect for cytokine-induced hypotension or for restoration of vascular contractile sensitivity to pressor agents in the treatment of such hypotension).

专利号:US-6844343-B1
优先权日:1999-09-17
标 题 :N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent
发明人：PFLEIDERER WOLFGANG; SCHMIDT HARALD; FROEHLICH LOTHAR; KOTSONIS PETER; TAGHAVI-MOGHADAM SHAHRIYAR
权利人:VASOPHARM BIOTECH GMBH
摘要:Compounds of formula (I), where preferably: A=a bridge of partial formula (II) or (III), R<1 >and R<2>=independently (substituted) alkyl, aryl or aralkyl, or together form a heterocycle, R<3>=H, -CO-Alkyl, or -CO-Aryl, R<4>=Aryl, -CO-O-Aryl or -CO-Aryl and R<5>=H, are potent inhibitors of NO-synthase and are suitable as pharmaceutical agents of prophylaxis and treatment of disease states associates with a disturbed NO metabolism.

专利号:US-5877176-A
优先权日:1991-12-26
标题 :Blocking induction of tetrahydrobiopterin to block induction of nitric oxide synthesis

专利号:US-5880124-A
优先权日:1991-12-26
标 题:Blocking induction of tetrahydrobiopterin to block induction of nitric oxide synthesis

专利号:WO-9513803-A1
优先权日:1993-11-15
标题 :Blocking induction of tetrahydrobiopterin to block induction of nitric oxide synthesis