CAS: 1254032-66-0; (S)-4-(3-Amino-1-(Isoquinolin-6-Ylamino)-1-Oxopropan-2-yl)Benzyl 2,4-Dimethylbenzoate

专利信息

专利号:US-7321046-B2
优先权日:2002-09-06
标 题 :Analogs of dictyostatin, intermediates therefor and methods of synthesis thereof
发明人：CURRAN DENNIS P; SHIN YOUSEUNG; FOURNIER JEAN-HUGUES; MANCUSO JOHN; DAY BILLY W; BRUCKNER ARNDT; FUKUI YOSHIKAZU
权利人:UNIV PITTSBURGH
摘要:Dictyostatin and its analogs show great promise as new anticancer agents. The present invention provides dictyostatin analogs, synthetic intermediates for the synthesis of dictyostatin analogs, and synthetic methods for the synthesis of such analogs and intermediates. Dictyostatin analogs can have the following structure or its enantiomer n nwherein R 1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R 2 is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiR a R b R c , CH 2 OR d , or COR e ; R a , R b and R c are independently an alkyl group or an aryl group; R d is an alkyl group, an aryl group, an alkoxylalkyl group, —R i SiR a R b R c or a benzyl group, wherein R i is an alkylene group; R e is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NR g R h , wherein R g and R h are independently H, an alkyl group or an aryl group; R 3 is (CH 2 ) n where n is and integer in the range of 0 to 5, —CH 2 CH(CH 3 )—, —CHâ•?CH—, —CHâ•?C(CH 3 )—, or —C≡C—; R 4 isn n nwherein R 23a is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiR a R b R c , CH 2 OR d , or COR e ; R 23b is H, a protecting group, an alkyl group, a benzyl group, a trityl group, —SiR a R b R c , CH 2 OR d , or COR e , or R 23a and R 23b together form a portion of six-membered acetal ring incorporating CR t R u ; R t and R u are independently H, an alkyl group, an aryl group or an alkoxyaryl group; and R 5 is H or OR 2b , wherein R 2b is H, a protecting group, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiR a R b R c , CH 2 OR d , or COR e ; provided that the compound is not dictyostatin 1.

专利号:US-2007082039-A1
优先权日:2004-10-18
标题 :Synthesis of fatty alcohol esters of alpha-hydroxy carboxylic acids, the use of the same as percutaneous permeation enhancers, and topical gels for the transdermal delivery of steroids
发明人：JONES GERALD S JR; ST LAURENT JOSEPH P; GOODRICH SCOTT A
权利人:JONES GERALD S JR; ST LAURENT JOSEPH P; GOODRICH SCOTT A
摘要:The present invention provides a novel approach for the preparation of fatty alcohol esters of α-hydroxy carboxylic acids. The present invention also provides a novel topical gel for the transdermal delivery of steroids using the fatty alcohol esters as permeation enhancers.

专利号:US-2002058286-A1
优先权日:1999-02-24
标 题 :Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; STACHEL SHAWN J; LEE CHUL BOM; CHAPPELL MARK D; CHOU TING-CHAO; WU ZHICAI
摘要:The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.

专利号:US-10550087-B2
优先权日:2015-11-17
标 题:Process for the preparation of kinase inhibitors and intermediates thereof
发明人：STURDIVANT JILL MARIE; DELONG MITCHELL A; CHAMBOURNIER GILLES; PAMMENT MICHAEL G; FEDIJ VICTOR
权利人:AERIE PHARMACEUTICALS INC
摘要:Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.

专利号:US-9643927-B1
优先权日:2015-11-17
标题:Process for the preparation of kinase inhibitors and intermediates thereof
发明人：STURDIVANT JILL M; DELONG MITCHELL A; CHAMBOURNIER GILLES; PAMMENT MICHAEL G; FEDIJ VICTOR
权利人:AERIE PHARMACEUTICALS INC
摘要:Described are processes for the synthesis of certain compounds, useful for treating diseases, e.g. eye disease, such as glaucoma and ocular hypertension, in a subject.

专利号:US-6867305-B2
优先权日:1996-12-03
标题:Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; STACHEL SHAWN J; LEE CHUL BOM; CHAPPELL MARK D; WU ZHICAL
权利人:SLOAN KETTERING INST CANCER; UNIV COLUMBIA
摘要:The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.