CAS: 119169-78-7; Epristeride

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CAS号201230-82-2 carbon monoxide | CAS号131267-80-6 N-皮丁基-4-雄烯-3-酮-... | CAS号2681-55-2 雄甾-3-酮-4-烯-17ba... | CAS号302-97-6 3-氧代-雄甾-4-烯-17β-羧酸

3-Carbomethoxy-N-T-Butyl-Androst-3,5-Diene-17β-Carboxamide置于水,Potassium Carbonate体系中,用 甲醇 用作溶剂,化学反应生成爱普列特
参考文献:不饱和3-羧基类固醇抑制类固醇5α-还原酶.
标题:不饱和3-羧基类固醇抑制类固醇5α-还原酶.
摘要:已经制备了一系列带有3-羧基取代基的不饱和类固醇,并在体外进行了测定,作为人和大鼠前列腺类固醇5α-还原酶的抑制剂(ec 1.3.1.30).有人提出,观测到的3-雄烯基-3-羧酸的紧密结合是由于模拟的类固醇5α-在nadph依赖性的睾丸激素的nadph依赖性共轭还原过程中形成的一种推定的高能酶结合的烯醇式中间体.还原酶.这些化合物是通过钯(0)催化衍生自3-酮前体的烯醇(三氟甲基)磺酸盐的羰基甲氧基化反应制得的.探索了a和b环的不饱和修饰以及在c-3,-4,-6和-11处的取代.单和二烷基甲酰胺被用作17个β侧链,以增强人类酶的抑制活性.
Doi:10.1021/jm00165A010

专利信息

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

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 (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人：SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

专利号:US-2012295932-A1
优先权日:2011-05-17
标 题 :Method for the treatment of cancer
发明人：FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH
权利人:FERLINI CRISTIANO; MARIANI MARISA; SHAHABI SHOHREH; WESTERN CONNECTICUT HEALTH NETWORK INC
摘要:Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. Also provided is a method of sensitizing a cancer cell from a solid tumor from a male patient other than a prostate cancer cell to treatment with a chemotherapeutic agent comprising administering an effective amount ofn (a)n (i) at least one antiandrogen; (ii) at least one inhibitor of androgen synthesis; or (iii) a combination of at least one antiandrogen and at least one inhibitor of androgen synthesis; and n (b) at least one chemotherapeutic agent other than an antiandrogen or an inhibitor of androgen synthesis for the treatment of cancer characterized by a solid tumor, other than prostate cancer, in a male patient. The antiandrogen, the inhibitor of androgen synthesis, or the combination of both may be administered before, after, or at the same time as the chemotherapeutic agent.

专利号:US-2024382626-A1
优先权日:2023-05-16
标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof
发明人：PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA
权利人:UNIV TEXAS
摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.