公开(公告)号：US07288545B2

公开(公告)日：2007-10-30

申请号：US10689865

申请日：2003-10-20

Applicant: Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

Inventor： Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

IPC: A61K31/496 ,  C07D405/14

CPC classification number: C07D401/06 ,  C07D409/14

Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.

公开(公告)号：US06635649B2

公开(公告)日：2003-10-21

申请号：US09851077

申请日：2001-05-08

Applicant: Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

Inventor： Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

IPC: A61K31496

CPC classification number: C07D401/06 ,  C07D409/14

Abstract: Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.

Abstract translation: 哌嗪二酮化合物，分别为：＆lt; CUSTOM-CHARACTER FILE =“US06635649-20031021-P00900.TIF”ALT =“custom character”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/ >和 或双键; 当是单键，或C（R a R b）当为双键时; 当是单键或C（R ）”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00005”/>是双键; Ar是杂芳基; 且R 3为H，烷基，芳基，杂芳基，C（O）R d，C（O）OR d，C（O）NR d R e或SO 2 R d; R 1和R 2各自独立地是H，C（O）R d，C（O）OR d，C（O）NR d R e或SO 2 R ; R a，R b，R c，R d和R e各自独立地是H，烷基，芳基，杂芳基，环基或杂环基。 任选地，R 5和R b一起是环基或杂环基; 并且还可任选地，R 1和R 5'或R 1和R b一起是环基或杂环基。 还公开了用上述哌嗪二酮化合物治疗肿瘤的方法。