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1. 发明专利

HU0302358A2 PIPERAZINEDIONE COMPOUNDS AND USE OF THEM FOR PRODUCING PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：HU0302358A2
公开(公告)日：2003-11-28
申请号：HU0302358
申请日：2001-05-08
申请人： ADPHARMA , THENG CHE-MING , WANG HUI-PO
发明人： CHEN HUEI-TING , CHEN YA-LAN , FAN YAN-BING , GUH JIH-HWA , LEE ON , LI ERIC I C , THENG CHE-MING , WANG HUI-PO
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Piperazinedione compounds (I) are new. Piperazinedione compounds of formula(I) are new. [Image] a and b : single or double bond; A : H, CH(RaRb) or C(RaRb); Z : R 3O-(Ar)-B or C(Rc); B : CH(Rc); Ar : heteroaryl; R 3H, alkyl, (hetero)aryl, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; R 1 and R 2H, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; Ra, Rb, Rc, Rd and Re : H, alkyl, (hetero)aryl or (hetero)cyclyl; optionally Ra+Rb, R 1+Ra and R 1+Rb : (hetero)cyclyl. provided that when b is a single bond, then A is H or CH(RaRb) or when b is a double bond, then A is C(RaRb) and when a is a single bond then Z is R 3O-(Ar)-B and when a is a double bond, Z is C(Rc). An independent claim is also included for treating tumor, involving administering a piperazinedione compound of formula (II) to a subject. [Image] Z' : CH(R cR d) or C(R cR d); R 1> and R 2>H, C(O)Re, C(O)ORe, C(O)NReRf or SO 2Re; R c, R d, Re and Rf : Ra; R 1>+Ra and R 1>+Rb : (hetero)cyclyl. When a is a single bond then Z' is CH(R cR d) and when a is a double bond, Z' is C(R cR d). Provided that if a is a single bond and b is a double bond, then one of R c and R d is H and other is heteroaryl. ACTIVITY : Cytostatic. The cytotoxic activities of (I) and taxol were tested on PC-3 cells. Cells were incubated in the presence of (I) in a serum-free medium for 24 hours. The cytotoxic activities were determined by the MTT assay. All compounds were active. The most potent (I) had an EC 5 0 value of about 0.3 micromolar, which is 30 times more potent than taxol. MECHANISM OF ACTION : Inhibitor of G 2/M progression of the cell cycle; Inhibitor of endothelial cell proliferation and angiogenesis effect; Inhibitor of polymerization of tubulin/microtubulin. Tubulin/microtubulin was incubated in the presence of (I) at a different concentrations in a solution (0.1 M MES, 1 mM EGTA, 0.5 mM MgCl 2, 0.1 mM EDTA and 2.5 M glycerol) at 37[deg]C. Then GTP was added to induce polymerization of tubulin/microtubulin. Optical density was measured at 350 nm at various time points to determine the degree of the polymerization. (I) inhibits the polymerization at 10 -> 6> - 10 -> 5> M.

2. 发明专利

AU8573598A Novel azatyrosine analogues and process of preparation thereof 未知
公开(公告)号：AU8573598A
公开(公告)日：1999-02-16
申请号：AU8573598
申请日：1998-07-23
申请人： WANG HUI PO
发明人： WANG HUI-PO , LEE ON , SHEW JIN-YUH , LEE SHUI-JANE
IPC分类号： A61K31/44 , A61K31/4418 , A61P35/00 , C07D213/65

3. 发明专利

BR0110745A 未知
公开(公告)号：BR0110745A
公开(公告)日：2003-12-30
申请号：BR0110745
申请日：2001-05-08
申请人： ADPHARMA INC , CHE MING TENG , WANG HUI-PO
发明人： CHE-MING TENG , WANG HUI-PO , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YAN-BING , CHEN CHEN YA-LAN
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Piperazinedione compounds (I) are new. Piperazinedione compounds of formula(I) are new. [Image] a and b : single or double bond; A : H, CH(RaRb) or C(RaRb); Z : R 3O-(Ar)-B or C(Rc); B : CH(Rc); Ar : heteroaryl; R 3H, alkyl, (hetero)aryl, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; R 1 and R 2H, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; Ra, Rb, Rc, Rd and Re : H, alkyl, (hetero)aryl or (hetero)cyclyl; optionally Ra+Rb, R 1+Ra and R 1+Rb : (hetero)cyclyl. provided that when b is a single bond, then A is H or CH(RaRb) or when b is a double bond, then A is C(RaRb) and when a is a single bond then Z is R 3O-(Ar)-B and when a is a double bond, Z is C(Rc). An independent claim is also included for treating tumor, involving administering a piperazinedione compound of formula (II) to a subject. [Image] Z' : CH(R cR d) or C(R cR d); R 1> and R 2>H, C(O)Re, C(O)ORe, C(O)NReRf or SO 2Re; R c, R d, Re and Rf : Ra; R 1>+Ra and R 1>+Rb : (hetero)cyclyl. When a is a single bond then Z' is CH(R cR d) and when a is a double bond, Z' is C(R cR d). Provided that if a is a single bond and b is a double bond, then one of R c and R d is H and other is heteroaryl. ACTIVITY : Cytostatic. The cytotoxic activities of (I) and taxol were tested on PC-3 cells. Cells were incubated in the presence of (I) in a serum-free medium for 24 hours. The cytotoxic activities were determined by the MTT assay. All compounds were active. The most potent (I) had an EC 5 0 value of about 0.3 micromolar, which is 30 times more potent than taxol. MECHANISM OF ACTION : Inhibitor of G 2/M progression of the cell cycle; Inhibitor of endothelial cell proliferation and angiogenesis effect; Inhibitor of polymerization of tubulin/microtubulin. Tubulin/microtubulin was incubated in the presence of (I) at a different concentrations in a solution (0.1 M MES, 1 mM EGTA, 0.5 mM MgCl 2, 0.1 mM EDTA and 2.5 M glycerol) at 37[deg]C. Then GTP was added to induce polymerization of tubulin/microtubulin. Optical density was measured at 350 nm at various time points to determine the degree of the polymerization. (I) inhibits the polymerization at 10 -> 6> - 10 -> 5> M.

4. 发明专利

GB2341857B Novel azatyrosine analogues and process of preparation thereof 未知
公开(公告)号：GB2341857B
公开(公告)日：2003-07-09
申请号：GB9813619
申请日：1998-06-25
申请人： WANG HUI-PO , TSAI HANSEN , ADVPHARMA INC
发明人： WANG HUI-PO , LEE ON , SHEW JIN-YUH , LEE SHUI-JANE
IPC分类号： A61K31/44 , A61K31/4418 , A61P35/00 , C07D213/65

5. 发明专利

NO20025373L 未知
公开(公告)号：NO20025373L
公开(公告)日：2002-12-13
申请号：NO20025373
申请日：2002-11-08
申请人： WANG HUI-PO
发明人： TENG CHE-MING , WANG HUI-PO , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YAN-BING , CHEN YA-LAN
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Piperazinedione compounds (I) are new. Piperazinedione compounds of formula(I) are new. [Image] a and b : single or double bond; A : H, CH(RaRb) or C(RaRb); Z : R 3O-(Ar)-B or C(Rc); B : CH(Rc); Ar : heteroaryl; R 3H, alkyl, (hetero)aryl, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; R 1 and R 2H, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; Ra, Rb, Rc, Rd and Re : H, alkyl, (hetero)aryl or (hetero)cyclyl; optionally Ra+Rb, R 1+Ra and R 1+Rb : (hetero)cyclyl. provided that when b is a single bond, then A is H or CH(RaRb) or when b is a double bond, then A is C(RaRb) and when a is a single bond then Z is R 3O-(Ar)-B and when a is a double bond, Z is C(Rc). An independent claim is also included for treating tumor, involving administering a piperazinedione compound of formula (II) to a subject. [Image] Z' : CH(R cR d) or C(R cR d); R 1> and R 2>H, C(O)Re, C(O)ORe, C(O)NReRf or SO 2Re; R c, R d, Re and Rf : Ra; R 1>+Ra and R 1>+Rb : (hetero)cyclyl. When a is a single bond then Z' is CH(R cR d) and when a is a double bond, Z' is C(R cR d). Provided that if a is a single bond and b is a double bond, then one of R c and R d is H and other is heteroaryl. ACTIVITY : Cytostatic. The cytotoxic activities of (I) and taxol were tested on PC-3 cells. Cells were incubated in the presence of (I) in a serum-free medium for 24 hours. The cytotoxic activities were determined by the MTT assay. All compounds were active. The most potent (I) had an EC 5 0 value of about 0.3 micromolar, which is 30 times more potent than taxol. MECHANISM OF ACTION : Inhibitor of G 2/M progression of the cell cycle; Inhibitor of endothelial cell proliferation and angiogenesis effect; Inhibitor of polymerization of tubulin/microtubulin. Tubulin/microtubulin was incubated in the presence of (I) at a different concentrations in a solution (0.1 M MES, 1 mM EGTA, 0.5 mM MgCl 2, 0.1 mM EDTA and 2.5 M glycerol) at 37[deg]C. Then GTP was added to induce polymerization of tubulin/microtubulin. Optical density was measured at 350 nm at various time points to determine the degree of the polymerization. (I) inhibits the polymerization at 10 -> 6> - 10 -> 5> M.

6. 发明专利

NO20025373A 未知
公开(公告)号：NO20025373A
公开(公告)日：2002-12-13
申请号：NO20025373
申请日：2002-11-08
申请人： WANG HUI-PO
发明人： TENG CHE-MING , WANG HUI-PO , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YAN-BING , CHEN YA-LAN
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/06 , C07D409/14

7. 发明专利

CA2408649C PIPERAZINEDIONE COMPOUNDS 未知
公开(公告)号：CA2408649C
公开(公告)日：2010-04-27
申请号：CA2408649
申请日：2001-05-08
申请人： AD PHARMA INC , TENG CHE-MING , WANG HUI-PO
发明人： LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YAN-BING , CHEN YA-LAN , TENG CHE-MING , WANG HUI-PO
IPC分类号： C07D241/18 , A61K31/4965 , A61K31/497 , C07D401/06 , C07D409/14
摘要： The use of a compound for treatment of a tumor, comprising administering to a subject in need thereof an effective amount of a compound having the following formula: (see above formula) wherein A is C(R a R b); Z is R3O-(Ar)-B, in which B is C(R c); Ar is pyridyl linked to B at position 2; and R3 is H, alkyl substituted with aryl, or aryl; in which aryl is unsubstituted or substituted with one or more substitutents selected from the group consisting of halogen, hydroxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, C1~C6 alkyl, C1~C6 alkenyl, C1~C6 alkoxy, and aryl; each of R1 and R2, independently, is H, or C(O)R d; and one of R a and R b is thienyl, furyl, pyridinyl, indolyl, 2-oxo-indolyl, aryl, alkyl, or alkyl substituted with aryl, and each of the other of R a and R b, and R c, and R d, independently, is H, alkyl, or aryl; in which alkyl and aryl are unsubstituted or substituted with one or more substitutents selected from the group consisting of halogen, hydroxyl, amino, alkylamino, arylamino, dialkylamino, diarylamino, cyano, nitro, mercapto, carbamido, carbamoyl, carboxyl, thioureido, thiocyanato, sulfonamido, C1~C6 alkyl, C2~C6 alkenyl, C1~C6 alkoxy, and aryl.

8. 发明专利

CZ20023693A3 Piperazinedione compounds, process of their preparation and antineoplastic use 未知
公开(公告)号：CZ20023693A3
公开(公告)日：2003-05-14
申请号：CZ20023693
申请日：2001-05-08
申请人： ADPHARMA , TENG CHE-MING , WANG HUI-PO
发明人： WANG HUI-PO , FAN YAN-BING , TENG CHE-MING , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , CHEN YA-LAN
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Piperazinedione compounds (I) are new. Piperazinedione compounds of formula(I) are new. [Image] a and b : single or double bond; A : H, CH(RaRb) or C(RaRb); Z : R 3O-(Ar)-B or C(Rc); B : CH(Rc); Ar : heteroaryl; R 3H, alkyl, (hetero)aryl, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; R 1 and R 2H, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; Ra, Rb, Rc, Rd and Re : H, alkyl, (hetero)aryl or (hetero)cyclyl; optionally Ra+Rb, R 1+Ra and R 1+Rb : (hetero)cyclyl. provided that when b is a single bond, then A is H or CH(RaRb) or when b is a double bond, then A is C(RaRb) and when a is a single bond then Z is R 3O-(Ar)-B and when a is a double bond, Z is C(Rc). An independent claim is also included for treating tumor, involving administering a piperazinedione compound of formula (II) to a subject. [Image] Z' : CH(R cR d) or C(R cR d); R 1> and R 2>H, C(O)Re, C(O)ORe, C(O)NReRf or SO 2Re; R c, R d, Re and Rf : Ra; R 1>+Ra and R 1>+Rb : (hetero)cyclyl. When a is a single bond then Z' is CH(R cR d) and when a is a double bond, Z' is C(R cR d). Provided that if a is a single bond and b is a double bond, then one of R c and R d is H and other is heteroaryl. ACTIVITY : Cytostatic. The cytotoxic activities of (I) and taxol were tested on PC-3 cells. Cells were incubated in the presence of (I) in a serum-free medium for 24 hours. The cytotoxic activities were determined by the MTT assay. All compounds were active. The most potent (I) had an EC 5 0 value of about 0.3 micromolar, which is 30 times more potent than taxol. MECHANISM OF ACTION : Inhibitor of G 2/M progression of the cell cycle; Inhibitor of endothelial cell proliferation and angiogenesis effect; Inhibitor of polymerization of tubulin/microtubulin. Tubulin/microtubulin was incubated in the presence of (I) at a different concentrations in a solution (0.1 M MES, 1 mM EGTA, 0.5 mM MgCl 2, 0.1 mM EDTA and 2.5 M glycerol) at 37[deg]C. Then GTP was added to induce polymerization of tubulin/microtubulin. Optical density was measured at 350 nm at various time points to determine the degree of the polymerization. (I) inhibits the polymerization at 10 -> 6> - 10 -> 5> M.

9. 发明专利

NO20025373D0 未知
公开(公告)号：NO20025373D0
公开(公告)日：2002-11-08
申请号：NO20025373
申请日：2002-11-08
申请人： WANG HUI-PO
发明人： TENG CHE-MING , WANG HUI-PO , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YAN-BING , CHEN YA-LAN
IPC分类号： C07D401/04 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , A61K
摘要： Piperazinedione compounds (I) are new. Piperazinedione compounds of formula(I) are new. [Image] a and b : single or double bond; A : H, CH(RaRb) or C(RaRb); Z : R 3O-(Ar)-B or C(Rc); B : CH(Rc); Ar : heteroaryl; R 3H, alkyl, (hetero)aryl, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; R 1 and R 2H, C(O)Rd, C(O)ORd, C(O)NRdRe or SO 2Rd; Ra, Rb, Rc, Rd and Re : H, alkyl, (hetero)aryl or (hetero)cyclyl; optionally Ra+Rb, R 1+Ra and R 1+Rb : (hetero)cyclyl. provided that when b is a single bond, then A is H or CH(RaRb) or when b is a double bond, then A is C(RaRb) and when a is a single bond then Z is R 3O-(Ar)-B and when a is a double bond, Z is C(Rc). An independent claim is also included for treating tumor, involving administering a piperazinedione compound of formula (II) to a subject. [Image] Z' : CH(R cR d) or C(R cR d); R 1> and R 2>H, C(O)Re, C(O)ORe, C(O)NReRf or SO 2Re; R c, R d, Re and Rf : Ra; R 1>+Ra and R 1>+Rb : (hetero)cyclyl. When a is a single bond then Z' is CH(R cR d) and when a is a double bond, Z' is C(R cR d). Provided that if a is a single bond and b is a double bond, then one of R c and R d is H and other is heteroaryl. ACTIVITY : Cytostatic. The cytotoxic activities of (I) and taxol were tested on PC-3 cells. Cells were incubated in the presence of (I) in a serum-free medium for 24 hours. The cytotoxic activities were determined by the MTT assay. All compounds were active. The most potent (I) had an EC 5 0 value of about 0.3 micromolar, which is 30 times more potent than taxol. MECHANISM OF ACTION : Inhibitor of G 2/M progression of the cell cycle; Inhibitor of endothelial cell proliferation and angiogenesis effect; Inhibitor of polymerization of tubulin/microtubulin. Tubulin/microtubulin was incubated in the presence of (I) at a different concentrations in a solution (0.1 M MES, 1 mM EGTA, 0.5 mM MgCl 2, 0.1 mM EDTA and 2.5 M glycerol) at 37[deg]C. Then GTP was added to induce polymerization of tubulin/microtubulin. Optical density was measured at 350 nm at various time points to determine the degree of the polymerization. (I) inhibits the polymerization at 10 -> 6> - 10 -> 5> M.

10. 发明申请

WO2012125447A3 PIPERAZINEDIONE COMPOUNDS 审中-公开
标题翻译：哌嗪二酮化合物
公开(公告)号：WO2012125447A3
公开(公告)日：2012-12-06
申请号：PCT/US2012028441
申请日：2012-03-09
申请人： UNIV TAIPEI MEDICAL , DCB USA LLC , WANG HUI-PO , TENG CHE-MING , WANG CHUN-LI , GUH JIH-HWA , PAN SHIOW-LIN , WANG YUAN-YI , LIAN JANG-FENG
发明人： WANG HUI-PO , TENG CHE-MING , WANG CHUN-LI , GUH JIH-HWA , PAN SHIOW-LIN , WANG YUAN-YI , LIAN JANG-FENG
IPC分类号： C07D401/14 , A61K31/444 , A61P35/00 , C07D401/06 , C07D401/12
CPC分类号： C07D401/06 , C07D401/14
摘要： This invention relates to piperazinedione compounds shown in the specification. These compounds are tyrosine kinase inhibitors and can be used to treat cancer.
摘要翻译：本发明涉及说明书中所示的哌嗪二酮化合物。这些化合物是酪氨酸激酶抑制剂，可用于治疗癌症。

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