CAS: 2465-59-0; 1H-Pyrazolo[3,4-D]Pyrimidine-4,6-Diol

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📜别嘌醇置于bovine Xanthine Oxidase体系中,化学反应 0.08H,反应生成羟基嘌呤
参考文献:Fyx-051: A Novel And Potent Hybrid-Type Inhibitor Of Xanthine Oxidoreductase
标题:Fyx-051: A Novel And Potent Hybrid-Type Inhibitor Of Xanthine Oxidoreductase
摘要:4-[5-(吡啶-4-基)-1 H-1,2,4-三唑-3-基]吡啶-2-甲腈(fyx-051)是牛乳黄嘌呤氧化还原酶(xor)的一种强效抑制剂.稳态动力学研究表明,它最初表现为一种竞争型抑制剂,K I 值为 5.7 x 10-9 M,几分钟后,它通过莫氧碳原子共价连接与 Xor 形成紧密复合物,这与之前的报道一致(proc Natl Acad Sci Usa 101: 7931-7936,2004).因此,Fyx-051 是一种混合型抑制剂,同时具有基于结构和机制的抑制作用.Fyx-051-Xor 复合物的分解半衰期为 20.4 小时,但酶活性并未完全恢复.研究发现,这是由于 Xor 介导 Fyx-051 转化为 4-[5-(2-羟基吡啶-4-基)-1 H-1,2,4-三唑-3-基]吡啶-2-甲腈(2-羟基-Fyx-051),以及形成 6-羟基-4-[5-(2-羟基吡啶-4-基)-1 H-1,2,4-三唑-3-基]吡啶-2-甲腈(2-羟基-Fyx-051),2,4-三唑-3-基]吡啶-2-甲腈(二羟基-Fyx-051)和 4-[5-(2,6-二羟基吡啶-4-基)-1 H-1,2,4-三唑-3-基]-6-羟基吡啶-2-甲腈(三羟基-Fyx-051).在形成三羟基-Fyx-051-Xor 复合物的同时,观测到一条明显的电荷转移带.电荷转移复合物的晶体学分析表明,Xor 的钼与三羟基-Fyx-051 的腈基之间形成了钼-氮-碳键.在氧化钾诱导的高尿酸血症大鼠模型中,Fyx-051 表现出强效,持久的降尿酸作用,似乎有望成为临床治疗高尿酸血症的候选药物.
Doi:10.1124/jpet.110.174540

专利信息

专利号:US-2002022022-A1
优先权日:2000-05-19
标题 :Inhibition of cell proliferation and matrix synthesis by antioxidants and NAD(P)H oxidase inhibitors
发明人：SHI YI; ZALEWSKI ANDREW
摘要:The present invention is directed to a method for the prophylactic and therapeutic treatment of diseases or disorders associated with the abnormal proliferation and extracellular matrix synthesis of smooth muscle cells (SMC) and fibroblasts due to activation of NAD(P)H and/or increased ROS generation. The method involves the administration of an NAD(P)H oxidase inhibitor(s) and/or antioxidant(s) to a mammal in an amount sufficient to treat the disease or disorder prophylactically or therapeutically. The NAD(P)H oxidase inhibitor inhibits the synthesis or translocation of NAD(P)H subunits, thereby blocking the generation of intracellular reactive oxygen species (ROS) and thus the proliferation and extracellular matrix synthesis of SMC and fibroblasts. Similarly, the administration of antioxidants blocks the generation of intracellular ROS, thereby inhibiting SMC and fibroblast proliferation and extracellular matrix synthesis. In addition to the prevention and treatment of vascular disease, such as atherosclerosis, graft disease, and restenosis, NAD(P)H oxidase inhibitors and antioxidants may be useful for the prevention and treatment of other conditions by decreasing cell proliferation and extracellular matrix synthesis associated therewith. These conditions include arthritis, keloid formation, cancer, tissue and organ fibrosis, and complications related to organ transplantation, metabolic syndrome, and radiation therapy.

专利号:US-11897914-B2
优先权日:2021-11-29
标题 :Synthesis of 2′ protected nucleosides
发明人：POON WING C; ZOU RUIMING; LAU ALDRICH N K; YU DAVID; Du Gengyu; YAO YUN-CHIAO; ZHAO GANG
权利人:HONGENE BIOTECH CORP
摘要:Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-12065460-B2
优先权日:2021-12-30
标 题 :Compositions and methods for liquid phase oligonucleotide synthesis
发明人：YANG GAOMAI; YAO YUN-CHIAO; YU DAVID; LAU ALDRICH N K
权利人:HONGENE BIOTECH CORP
摘要:Embodiments of the present application relate to polymers used as polymeric polyvalent hub for liquid phase oligonucleotide synthesis. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the polyvalent hub are also provided.

专利号:US-12180140-B2
优先权日:2022-12-23
标 题 :Compounds and methods for liquid phase oligonucleotide synthesis
发明人：YANG GAOMAI; XIE MIN; YANG HONGRONG; WANG SHENGDONG; LAU ALDRICH N K; ZOU RUIMING; YU DAVID
权利人:HONGENE BIOTECH CORP
摘要:The present disclosure relates to methods and compounds for liquid phase oligonucleotide synthesis employing the use of small molecules with lipophilic groups. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the compounds described herein are also provided.