CAS: 446-86-6; 6-((1-Methyl-4-Nitro-1H-Imidazol-5-yl)Thio)-9H-Purine

上下游产品

5-chloro-1-methyl-4-nitroimidazole 6-Mercaptopurine 9-acetyl-6-[(1-methyl-4-nitro-5-imidazolyl)thio]purineBenzoic acid 2-[6-(3-methyl-5-nitro-3H-imidazol-4-ylsulfanyl)-purin-9-ylmethoxy]-ethyl ester 28H21N9O11SC28H21N9O11S 35H27N7O9SC35H27N7O9S hypoxanthine

9-Acetyl-6-[(1-Methyl-4-Nitro-5-Imidazolyl)Thio]Purine 以 甲醇 作为反应溶剂,化学反应 0.17H,反应生成 硫唑嘌呤
参考文献:Chemical Transformations Of 6-[(1-Methyl-4-Nitro-5-Imidazolyl)-Thio]Purine (Azathioprine)
标题:Chemical Transformations Of 6-[(1-Methyl-4-Nitro-5-Imidazolyl)-Thio]Purine (Azathioprine)
摘要:
DOI:10.1007/bf02256869

专利信息

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:US-2007172520-A1
优先权日:2005-11-18
标题:Immunotargeting of Nonionic Surfactant Vesicles
发明人：VANAUKER MICHAEL; PLAAS ANNA; HOOD ELIZABETH
权利人:UNIV SOUTH FLORIDA
摘要:An immunoniosmes for targeted delivery of therapeutic agents to specific tissues in a host and methods of synthesis of those niosomes. An antibody molecule having specificity for a target antigen, such as a cell surface marker or other marker differentially expressed on a target cell, is covalently coupled to a functionalized membrane constituent. In a particular embodiment the functionalized membrane constituent is polyoxyethylene sorbitan monostearate functionalized with cyanuric chloride. The niosomes of this invention thus provide a composition that enhances internalization or retention of the bioactive agent of the niosome into the cytoplasm of the cells of the target tissue by providing a high degree of target specificity. Furthermore, the membrane vesicle enhances the life of the therapeutic agent by preventing its degradation in the extracellular environment, while exhibiting lower toxicity than can occur with some liposomes. The niosomes of the present invention are thus particularly useful as vehicles for the delivery of therapeutics to specific target cells.

专利号:US-8710261-B2
优先权日:2005-02-22
标 题:5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases
发明人：PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G
权利人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G; RANBAXY LAB LTD
摘要:The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R 1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R 2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R χ , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , C(â•?Y)NR 4 R 5 , C(â•?O)OR 6 [wherein Y is oxygen or sulphur], OR 5 , —O(Câ•?O)NR 4 R 5 , O-acyl, S(O) m R 4 , —SO 2 N(R 4 ) 2 , cyano, amidino or guanidino [wherein R 4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R 5 is hydrogen or R 4 ; R x is R 4 or —SO 2 N(R 4 ) 2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R 3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR 4 , —OC(â•?O)NR 4 R 5 , O-acyl, NH 2 , NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R x , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterize by over-expression and over-activation of an matrix metalloproteinase, using the compounds.

专利号:US-8207221-B2
优先权日:2004-01-30
标 题:Crystalline polymorphs of a CXC-chemokine receptor ligand
发明人：HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN
权利人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN; SCHERING CORP
摘要:The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: n n n n n n n n n n These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.

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-6187756-B1
优先权日:1996-09-05
标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.