Claims for Patent: 8,212,033

Summary for Patent: 8,212,033

Title:	Use of substituted quinazoline compounds in treating angiogenesis-related diseases
Abstract:	Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder with one of these compounds.
Inventor(s):	Wei-guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
Assignee:	Hutchmed Ltd
Application Number:	US12/893,872
Patent Claims:	1. A method of mediating kinase insert domain receptor activity comprising administering to a subject in need thereof an effective amount of a compound of the following formula: wherein each of R1, R2, R3, R4, R5, R8, R9, and R10, independently, is H, halo, amino, hydroxy, alkyl, alkenyl, alkynyl, heterocycloalkyl, alkoxy, alkylthio, carboxy, alkoxycarbonyl, carbonylamino, or sulfonylamino; R6 is alkyl; R7 is alkoxycarbonyl, aminocarbonyl, or aminosulfonyl; X is O; and Z is N; wherein each of alkyl, alkenyl, alkynyl, heterocycloalkyl, and alkoxy is optionally substituted with at least one substituent chosen from halo, hydroxy, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamido, carbamoyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl. 2. The method of claim 1, wherein each of R3 and R4 is optionally substituted alkoxy. 3. The method of claim 1, wherein R6 is optionally substituted methyl. 4. The method of claim 3, wherein R6 is methyl. 5. The method of claim 1, wherein R7 is —C(O)NRaRb, each of Ra and Rb, independently, being H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, or Ra and Rb, together with the nitrogen atom to which they are attached, represent a 3-8 membered ring containing 1-3 heteroatoms; wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl for Ra and Rb is optionally substituted with at least one substituent chosen from halo, hydroxy, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamido, carbamoyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl. 6. The method of claim 5, wherein each of Ra and Rb, independently, is H, optionally substituted alkyl, or optionally substituted cycloalkyl. 7. The method of claim 6, wherein R6 is optionally substituted methyl. 8. The method of claim 6, wherein Ra is H and Rb is optionally substituted methyl. 9. The method of claim 6, wherein each of R3 and R4 is methoxy. 10. A method of treating a solid tumor mediated by kinase insert domain receptor activity comprising administering to a subject in need thereof an effective amount of a compound chosen from