Claims for Patent: 7,829,574

Summary for Patent: 7,829,574

Title:	Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
Abstract:	Substituted quinazoline compounds of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and X are defined herein. It also discloses a pharmaceutical composition containing one of these compounds.
Inventor(s):	Wei-guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
Assignee:	Hutchmed Ltd
Application Number:	US12/118,019
Patent Claims:	1. A compound of the following formula: in which 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, or R3 and R4, together with the carbon atoms to which they are attached, form a 4- to 7-membered saturated, unsaturated, or aromatic ring, optionally containing 1-3 hetero atoms selected from N, O and S; 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, hydroxyl, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl. 2. 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, or R3 and R4, together with the carbon atoms to which they are attached, form a 4- to 7-membered saturated, unsaturated, or aromatic ring, optionally containing 1-3 hetero atoms selected from N, O and S; R6 is alkyl; R7 is —C(O)NRaRb, each of Ra and Rb, independently, being H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, 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; X is O; and Z is N; wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, and alkoxy is optionally substituted with at least one substituent chosen from halo, hydroxyl, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl. 3. The compound of claim 1, wherein R6 is optionally substituted methyl. 4. The compound of claim 3, wherein R6 is methyl. 5. The compound of claim 1, wherein each of R3 and R4 is optionally substituted alkoxy. 6. The compound of claim 2, wherein each of R3 and R4 is optionally substituted alkoxy. 7. The compound of claim 2, wherein each of Ra and Rb, independently, is H, optionally substituted alkyl, or optionally substituted cycloalkyl. 8. The compound of claim 7, wherein Ra is H and Rb is optionally substituted methyl. 9. The compound of claim 7, wherein each of R3 and R4 is methoxy. 10. A compound of the formula: 11. A pharmaceutical composition comprising 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, or R3 and R4, together with the carbon atoms to which they are attached, form a 4- to 7-membered saturated, unsaturated, or aromatic ring, optionally containing 1-3 hetero atoms selected from N, O and S; 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, hydroxyl, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamide, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkyloxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; and a pharmaceutically acceptable carrier. 12. A pharmaceutical composition comprising a compound of the formula: and a pharmaceutically acceptable carrier. 13. A pharmaceutical composition comprising 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, or R3 and R4, together with the carbon atoms to which they are attached, form a 4- to 7-membered saturated, unsaturated, or aromatic ring, optionally containing 1-3 hetero atoms selected from N, O and S; R6 is alkyl; R7 is —C(O)NRaRb, each of Ra and Rb, independently, being H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, 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; X is O; and Z is N; wherein each of alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl and alkoxy is optionally substituted with at least one substituent chosen from halo, hydroxyl, amino, cyano, nitro, mercapto, alkoxycarbonyl, amido, carboxy, alkanesulfonyl, alkylcarbonyl, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; and a pharmaceutically acceptable carrier. 14. The compound of claim 2, wherein R6 is optionally substituted methyl. 15. The compound of claim 14, wherein R6 is methyl. 16. The compound of claim 7, wherein R6 is optionally substituted methyl. 17. The compound of claim 16, wherein R6 is methyl.