CAS: 34552-84-6; 4-Hydroxy-2-Methyl-N-(5-Methylisoxazol-3-yl)-2H-Benzo[e][1,2]Thiazine-3-Carboxamide 1,1-Dioxide

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📜4-(1-Pyrrolidinyl)-N-(5-Methyl-3-Isoxazolyl)-2-Methyl-2H-1,2-Benzothiazin-3-Carboxamid-1,1-Dioxid置于盐酸体系中,用 溶剂黄146 作为反应溶剂,化学反应 0.75H,以97%的收率获得产物伊索昔康
参考文献:异昔康和相关的4-羟基-N-异恶唑基-2H-1,2-苯并噻嗪-3-羧酰胺1,1-二氧化物.强效非甾体类抗炎药.
标题:异昔康和相关的4-羟基-N-异恶唑基-2H-1,2-苯并噻嗪-3-羧酰胺1,1-二氧化物.强效非甾体类抗炎药.
摘要:合成了一系列新的抗炎药,即4-羟基-2H-1,2-苯并噻嗪1,1-二氧化物的n-异恶唑基-3-羧酰胺,并作为角叉菜胶诱导的大鼠爪水肿(cirpe)的抗炎药进行了评估分析和佐剂诱发的多关节炎(aip)分析.发现几种类似物比阿司匹林和苯基丁氮酮等效或有效.讨论了构效关系.发现其中一种化合物为4-羟基-2-甲基-N-(5-甲基-3-异恶唑基)-2H-1,2-苯并噻嗪3-羧酰胺1,1-二氧化物(3A;异昔康)在cirpe和治疗性aip分析中,其效力是苯基丁a的3倍.isoxicam(3A)目前正在作为抗关节炎药物进行iii期临床试验.
DOI:10.1021/jm00343A003

专利信息

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:WO-2022226312-A1
优先权日:2021-04-22
标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
发明人：KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
权利人:CLEAR CREEK BIO INC
摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

专利号:US-8067465-B2
优先权日:2002-01-15
标题:Tricyclic-bis-enone derivatives and methods of use thereof
发明人：HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO
权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE
摘要:Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.

专利号:WO-0140208-A3
优先权日:1999-12-06
标 题:Process for synthesis of 4-hydroxy-2h-1,2-benzothiazine-3-carboxamides
发明人：STANKOVIC SLOBODAN; STOJANOVIC NEBOJSA; MILOSEVIC SNEZANA; NIKOLIC DEJAN
权利人:AD ZDRAVLJE; STANKOVIC SLOBODAN; STOJANOVIC NEBOJSA; MILOSEVIC SNEZANA; NIKOLIC DEJAN
摘要:Suggested invention is related to the field of organic chemistry technology, specifically to the process for preparation of the compound 4-hydroxy - 2 - methyl - 2 H - 1 , 2 - benzothiazine - 3 - carboxamide - 1 , 1 -dioxide, of general formula (I), wherein R denotes one of the following radicals: alkyl group (C2-C6), cycloalkyl, benzyl, phenyl, pyridyl, methyl-pyridyl, pyrimidyl, thiazole, isothiazole. Concerning clinical practice, the special interest, as non-steroidal antirheumatics characterized by anti-inflammatory and analgesic properties, belongs to: piroxicam (4-hydroxy-2-methyl-N-(2-pyridinyl-2H-1,2-benzothiazine-3-carboxamid-1,1-dioxide)), isoxicam (4-hydroxy-2-methyl-N-(5-methyl-3-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide)) and sudoxicam (4-hydroxy-2-methyl-N-2-thiazolyl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide). Individual characteristics of the present invention are: the use of ethylester and dimethyl formamide with sodium ethoxide for opening of the cycle and for work at low temperatures in the mentioned phase; afterwards, methylation and final condensation with an amine of general formula NH2-Retard tablete, wherein R denotes: 2-pyridyl, alkyl substituted 2-pyridyl, 2-thiazole, 2-thiazole substituted with one or two alkyl groups, while each alkyl has from 1 to 4 carbon atoms or 5-methyl-3- isoxazolyl, using specific catalysts and adsorbents in an inert solvent and inert atmosphere.

专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEs†). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.