CAS: 606-58-6; 4-Amino-7-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-yl)-7H-Pyrrolo[2,3-D]Pyrimidine-5-Carbonitrile

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CAS号52443-16-0 5-chloro-9-[3,4...

专利信息

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-6645513-B2
优先权日:1998-10-26
标题 :Treatment of skin with adenosine or adenosine analog
发明人：DOBSON JR JAMES G; ETHIER MICHAEL F
权利人:UNIV MASSACHUSETTS
摘要:Methods for enhancing the condition of non-diseased skin by application of compositions containing adenosine or an adenosine analog are disclosed. Also disclosed are methods for increasing DNA synthesis or protein synthesis in dermal cells, and methods for increasing dermal cell size, by application of compositions containing adenosine.

专利号:US-4140851-A
优先权日:1977-11-21
标题:Synthesis and antitumor activity of 2,4,5-trisubstituted-pyrrolo2,3-d]-pyrimidine nucleosides
发明人：TOWNSEND LEROY B
权利人:US HEALTH EDUCATION & WELFARE
摘要:Certain trisubstituted pyrrolopyrimidine nucleosides are prepared from toyocamycin and have shown antitumor activity against L1210 and P388 murine leukemia. The particular compounds of interest are selected from the following structural formula: ##STR1## where X is halo n Y is halo; --NH 2 ; --SH, --SR (where R is lower alkyl, benzyl); --OR (where OR is methoxy or alkoxy or where alk is C1-C6); amino (where the amino is --NH 2 , -alkyl amino or -dialkyl amino and alkyl is C1-C6); gamma gamma dimethyl allyl amino; benzyl amino; phenyl amino; seleno n Z is CN; CXNH 2 where X is â•?0, â•?S, or â•?Se, â•?NH, â•?NHNH 2 , â•?NOH. OR Z is = --CH 2 NH 2 , --CORâ•?NH n Ribâ•?β-D-ribofuranosyl n Preferred members of this group of compounds are shown by the following structural formula: ##STR2## where X is Cl n Y is Cl or NH 2 n Z is CN, CONH 2 , or Câ•?NOH--NH 2 n These compounds are further identified as NSC #145387 (Compound 5) ##STR3## NSC #177369 (Compound 6) ##STR4## NSC #182864 (Compound 8) ##STR5## NSC #180526 (Compound 10) ##STR6## These compounds at dosages of 13 - 200 mg/kg of body weight administered every other day on the standard six-day schedule showed activity against both L1210 and P388 murine leukemia (Protocol 11, National Institutes o Health, November 11, 1972).

专利号:US-12036300-B2
优先权日:2021-03-31
标题:Methods and compositions for improving skin
发明人：LIAO I-CHIEN; BRIEVA PATRICIA; JUCHAUX FRANCK; BOUEZ CHARBEL; ZHENG QIAN; QIAN KUN
权利人:OREAL
摘要:A method for managing skin tone comprising reducing the synthesis of melanin by applying a skin treatment composition to skin. The skin treatment composition may include about 0.1 to about 25 wt. % of acetyl trifluoromethylphenyl valylglycine; about 0.5 to about 30 wt. % of a polyol; about 0.1 to about 30 wt. % of a silicone, fatty compound, or a mixtures thereof, wherein the skin treatment composition is an emulsion, and all weight percentages are based on the total weight of the skin treatment composition.

专利号:CN-104404111-A
优先权日:2014-12-18
标题 :A method for improving the synthesis of toyocamycin by amylase streptomyces chromogenes