CAS: 16610-63-2; (1-Hydroxydodecane-1,1-Diyl)Diphosphonic Acid

📜月桂酸置于甲烷磺酸,亚磷酸,三氯化磷体系中,化学反应 16.0H,反应生成(1-羟基十二烷-1,1-二基)二膦酸
参考文献:双膦酸酯对酸性鞘磷脂酶的强效和选择性抑制作用
标题:双膦酸酯对酸性鞘磷脂酶的强效和选择性抑制作用
摘要:不仅仅是修补骨头:简单的双氨基双膦酸酯(参见图片)是迄今为止已知的最有效的酸性鞘磷脂酶抑制剂.它可以一步一步合成,并在体外抑制细胞死亡.由于酸性鞘磷脂酶是炎性肺部疾病的推定药物靶标,因此双膦酸盐可用于治疗肺部疾病.
Doi:10.1002/anie.200903288

专利信息

专利号:US-4964846-A
优先权日:1986-05-16
标 题 :Process for the E/Z stereoselective synthesis of homochiral five and six ring intermediate products
发明人：GAIS HANS-JOACHIM; ERDELMEIER IRENE; BIRK ROLF
权利人:SCHERING AG
摘要:This invention comprises a process for the production of unsymmetrical olefins from prochiral symmetrical ketones by addition of lithiosulfoximine from n-butyllithium and N-substituted S-methyl-S-phenyl-sulfoximine derivatives and then reaction with n-butyllithium/trimethychlorosilane.

专利号:US-5877296-A
优先权日:1994-06-03
标题:Process for preparing conjugates of methyltrithio antitumor agents
发明人：HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN
权利人:AMERICAN CYANAMID CO
摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

专利号:US-5342947-A
优先权日:1992-10-09
标 题:Preparation of water soluble camptothecin derivatives
发明人：LACKEY Karen; STERNBACH DANIEL D
权利人:GLAXO INC
摘要:The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), (I) wherein: n represents the integer 1 or 2; R1 represents independently, hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; and R2 represents hydrogen and the pharmaceutically acceptable salts thereof.

专利号:US-5877207-A
优先权日:1996-03-11
标 题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
发明人：KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A
权利人:ALLERGAN SALES INC
摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

专利号:US-5739116-A
优先权日:1994-06-03
标题:Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents

专利号:US-5126351-A
优先权日:1991-01-24
标 题:Antitumor compounds
发明人：LUZZIO MICHAEL J; BESTERMAN JEFFREY M; EVANS MICHAEL G; JOHNSON M ROSS
权利人:GLAXO INC
摘要:The present invention relates to the compounds of formula (I), ##STR1## wherein: R 1 is hydrogen, hydroxy or amino; n R 2 is hydrogen, hydroxy, methoxy or methoxymethoxy; n R 3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R 2 , methylenedioxy (also known as 1,3-dioxolo); n R 4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C 1-4 )alkylaminomethyl or, taken together with R 3 , methylenedioxy; n R 5 is hydrogen or hydroxy; provided that at least one of R 1 through R 5 is other than hydrogen; and n i) X 2 is hydroxy or methoxy with X 1 , X 3 and X 4 being hydrogen; or n ii) X 1 taken together with X 2 , n X 2 taken together with X 3 or X 3 taken together with X 4 , is methylenedioxy, provided that each of the remaining respective X 1 , X 2 , X 3 and X 4 substituents are hydrogen, n intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.