发明名称 Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
摘要 The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
申请公布号 US8871776(B2) 申请公布日期 2014.10.28
申请号 US201213648494 申请日期 2012.10.10
申请人 Duquesne University of the Holy Ghost 发明人 Gangjee Aleem
分类号 C07D239/70;C07D487/04 主分类号 C07D239/70
代理机构 Buchanan Ingersoll & Rooney PC 代理人 Buchanan Ingersoll & Rooney PC ;Cochenour Craig G.
主权项 1. A compound of formula I: wherein both B and C rings may be completely or partially saturated or unsaturated with respect to bond 4b-8a, 5-6 and 7-8; the C ring may have an N or substituted N depending on the saturation level of the C ring, and the substitution may be all of R1, R2 and R3; X and Y=NH; P=NH; R1=H; and R2=H; Z=S; wherein Z may be attached to the C ring at positions 5, 6, 7 or 8 and may be attached to more than one of said positions 5, 6, 7, or 8 on the ring; wherein when the C-ring is saturated or partially saturated the Z or R3 creates chirality, then all stereoisomers thereof both separately and as racemic and/or diastereoisomeric mixtures are included; R3=aryl, alkylaryl, and substituted saturated or unsaturated alkylaryl wherein said substitution may be at either the alkyl or the aryl portion of the alkylaryl group and may be one or more substituents independently selected from (i) an alkoxy group, (ii) halogen atoms including chlorine, bromine, iodine, and fluorine, (iii) alkyl groups including straight or branched chains having from one to six carbon atoms, (iv) an aryl group, (v) a heteroaryl group having at least one atom in the aryl ring that is not carbon selected from oxygen, nitrogen or sulfur, and (vi) a carboxylic acid having up to seven carbon atoms.
地址 Pittsburgh PA US