2-乙酰氨基-5-苯甲硫基-1,3,4-噻二唑置于水,氯,溶剂黄146,氨体系中,化学反应 0.5H,反应生成 乙酰唑胺 参考文献:Compositions And Methods For The Suppression Of Carbonic Anhydrase Activity 标题:Compositions And Methods For The Suppression Of Carbonic Anhydrase Activity 摘要:该发明涉及公式i的化合物或其药用可接受盐,以及其多晶型,溶剂合物,对映体,立体异构体和水合物.包括有效量的公式i化合物的药物组合物,以及用于治疗,预防或调节疾病中的碳酸酐酶活性的方法可以制成口服,颊内,直肠,局部,经皮,经粘膜,静脉,肠道给药,糖浆或注射剂.这些组合物可用于治疗青光眼,癫痫发作,特发性颅内高压(假性脑膜炎),高原反应,胱氨酸尿症,周期性麻痹和硬膜扩张,充血性心力衰竭,药物诱导性水肿,利尿剂,因肢体动脉阻塞而导致的间歇性跛行以及血管性痴呆的治疗.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:WO-2022055467-A1 优先权日:2020-09-08 标题:Certain new 4-(2-((5-(substitutedamino)-1,3,4-thiadiazole-2-yl)thio)acetyl)benzenesulphoneamide derivatives and a method for the synthesis of said derivatives 发明人:KAPLANCIKLI ZAFER ASIM; ÖZKAY YUSUF; BEYDEMİR ŞÜKRÜ; ILGIN SINEM; ATLI EKLİOÄžLU ÖZLEM; OSMANİYE DERYA; LEVENT SERKAN; ACAR ÇEVİK ULVIYE; SAÄžLIK BEGÜM NURPELIN; KAYA ÇAVUÅžOÄžLU BETÜL; KORKUT ÇELİKATEÅž BÜŞRA; NEZİR DENIZ; BÜYÜKEMİR OYA; DEMİR YELIZ; KARADUMAN ABDULLAH BURAK 权利人:ANADOLU UENIVERSITESI 摘要:The invention relates to a certain new 4-(2-((5-(substitutedamino)-1,3,4-thiadiazole-2-yl)thio)acetyl)benzenesulphonamide derivatives for use in pharmaceutics, chemical and pharmaceutical industry, and to a method for the synthesis of said derivatives.
专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:EP-2054420-B1 优先权日:2006-08-02 标题:Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof 发明人:MATULIS DAUMANTAS; DUDUTIENE VIRGINIJA; MATULIENE JURGITA; MISTINAITE LINA 权利人:BIOTECHNOLOGIJOS INST 摘要:The invention is related to novel compounds - benzimidazo[1,2-c][1,2,3]thiadiazole sulfonamides, corresponding to the general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression such as glaucome. The compounds of formula (I) inhibits enzymes such as carbonic anhydrases and metallo proteinases. This invention is also related to new intermediate compounds which are used for the synthesis of sulfonamides of formula (I).
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合成参考文献
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