CAS: 914471-09-3; 4-Amino-N'-(3-Chloro-4-Fluorophenyl)-N-Hydroxy-1,2,5-Oxadiazole-3-Carboximidamide

上下游产品

3-chloro-4-fluorophenylamine 4-amino-N-hydroxy-1,2,5-oxadiazole-3-carboximidamidoyl chloride meta-fluoroaniline3-(4-amino-1,2,5-oxadiazol-3-yl)-4-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5(4H)-one 3-(4-amino-1,2,5-oxadiazol-3-yl)-4-(3-chlorophenyl)-1,2,4-oxadiazol-5(4H)-one

📜3-氯-4-氟苯胺,4-氨基-1,2,5-恶二唑-3-氯化甲醛肟 以 乙醇 作为反应溶剂,化学反应 2.0H,反应生成 4-氨基-N-(3-氯-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒
参考文献:在小鼠黑素瘤模型中发现具有吲哚胺2,3-双加氧酶的强效竞争性抑制剂的体内药效学活性和功效
标题:在小鼠黑素瘤模型中发现具有吲哚胺2,3-双加氧酶的强效竞争性抑制剂的体内药效学活性和功效
摘要:在吲哚胺2,3-二加氧酶(ido)的新型抑制剂中,已发现羟am的化学型是关键药效团.优化导致鉴定出5L,这是ido的一种有力(hela Ic 50 = 19 Nm)竞争性抑制剂.小鼠中5L的测试证明ido具有药效学抑制作用,这是通过血浆中犬尿氨酸水平降低(> 50%)和携带分泌gm-Csf的b16黑色素瘤肿瘤的小鼠的剂量依赖性功效来衡量的.
DOI:10.1021/jm900518F

专利信息

专利号:US-2024350669-A1
优先权日:2022-01-07
标题 :Inhibition of kynurenine synthesis and/or signaling to treat leukemia and myelodysplasia
发明人：KOUSTENI STAVROULA; GALÃ?N-DÃ?EZ MARTA
权利人:UNIV COLUMBIA
摘要:Methods and compositions for treating leukemia involving administering a therapeutically effective amount of an inhibitor of indoleamine 2,3 dioxygenase (IDO1). The leukemia may be is acute myeloid leukemia or acute lymphoid leukemia. The inhibitor can be a small molecule such as indiximod, epacadostat, BMS-986205, navoximod, PF-0684003, KHK2455 or LY3381916 or epacadostat. The inhibitor can be used alone or in conjunctions with other chemotherapeutic agents. IDO1 can also be inhibited using a CRISP-CAS system. The inhibitor can be administered orally, intravenously, intramuscularly, topically, arterially, or subcutaneously.

专利号:WO-2024231384-A1
优先权日:2023-05-10
标题:Compositions for treating senescence related disease
发明人：PENDE MARIO; FUMAGALLI STEFANO
权利人:INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT; UNIV PARIS CITE
摘要:Inventors have identified glycerol-3-phosphate (G3P) and phosphoethanolamine (PEtn) metabolism as potent regulators of the senescent program at the nexus of TAG and PL metabolism. They show that Glycerol kinase (GK) and Phosphate Cytidylyltransferase 2 Ethanolamine (Pcyt2) activities, which catalyse regulatory steps in TAG and PL synthesis impact G3P and PEtn levels in a homeostatic fashion controlling the senescence program. Finally, they provide evidence that pharmacological inhibitors of GK activity act senomorphic, thus suggesting a novel therapeutic target for interventions in age-related diseases and cancer. The present invention relates to a method for treating senescence related disease in a subject in need thereof comprising administering said subject with a therapeutically effective amount of a modulator of Glycerol kinase (GK), Glycerol 3 phosphate phosphatase (G3PP), Ethanolamine-Phosphate Phospho-Lyase (ETNPPL) and/or Phosphate Cytidylyltransferase 2 (PCYT2).

专利号:US-2022259202-A1
优先权日:2019-06-17
标题:1-(4-(aminomethyl)benzyl)-2-butyl-2h-pyrazolo[3,4-c]quinolin-4-amine derivatives and related compounds as toll-like receptor (tlr) 7/8 agonists, as well as antibody drug conjugates thereof for use in cancer therapy and diagnosis
发明人：MEIMETIS LABROS
权利人:SUTRO BIOPHARMA INC
摘要:1-(4-(aminomethyl)benzyl)-2-butyl-2H-pyrazolo[3,4-c]quinolin-4-amine derivatives thereof and related compounds of formula (I) as toll-like receptor (TLR) 7/8 agonists for cancer therapy. Linker payload compounds thereof, and antibody conjugates thereof for cancer diagnosis. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 145 to 156; examples 1 to 3; biological examples 1 to 6; tables 1 and 2).