专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

ZA200209917B Piperazinedione compounds. 未知
公开(公告)号：ZA200209917B
公开(公告)日：2004-04-28
申请号：ZA200209917
申请日：2002-12-06
申请人： ADPHARMA INC , TENG CHE MING , WANG HUI
发明人： CHEN HUEI-TING , CHEN YA-LAN , FAN YAN-BING , GUH JIH-HWA , LEE ON , LI ERIC I C , TENG 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 , C07D , 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.

2. 发明申请

WO0195858A3 PIPERAZINEDIONE COMPOUNDS 审中-公开
标题翻译：哌嗪化合物
公开(公告)号：WO0195858A3
公开(公告)日：2002-03-21
申请号：PCT/US0114721
申请日：2001-05-08
申请人： ADPHARMA INC , TENG CHE MING , WANG HUI PONG , LI ERIC I C , LEE ON , GUH JIH HWA , CHEN HUEI TING , FAN YA BING , CHEN YA LAN
发明人： TENG CHE-MING , WANG HUI-PONG , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YA-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
摘要： Piperazinedione compounds of the formula (I), wherein each of ---- and ---- , independently, is a single bond or a double bond; A is H or CH(R R ) when ---- is a single bond, or C(R R ) when ---- is a double bond; Z is R3O-(Ar)-B, in which B is CH(R ) when ---- is a single bond, or C(R ) when ---- is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)R , C(O)OR , C(O)NR R , or SO2R , each of R1 and R2, independently, is H C(O)R , C(O)OR , C(O)NR R , or SO2R ; and each of R , R , R , R , and R , independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, R and R taken together are cyclyl or heterocyclyl; and, also optionally, R1 and R or R1 and R taken together are cyclyl or heterocyclyl.
摘要翻译：式（I）的哌嗪二酮化合物，其中各自独立地是单键或双键; 当o-为单键时，A为H或CH（R a R b），当O - - 是双键; Z是R3O-（Ar）-B，其中当CH是单键时，B是CH（R c），或者当C（R c） ---- 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独立地是HC（O）R d，C（O）OR d，C（O）NR d R e或SO 2 R d; 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 a和R b一起是环基或杂环基; 并且还可任选地，R 1和R a或R 1和R 3一起是环基或杂环基。

3. 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.

4. 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.

5. 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.

6. 发明专利

NO326341B1 未知
公开(公告)号：NO326341B1
公开(公告)日：2008-11-10
申请号：NO20025373
申请日：2002-11-08
申请人： TENG CHE-MING
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 , C07D401/06 , A61K20060101 , A61K31/496 , A61K31/4965 , A61K31/497 , A61P35/00 , A61P35/02 , C07D20060101 , C07D241/18 , 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.

7. 发明专利

JPH11147824A NEW ANTICANCEROUS COMPOUND OF AZATYROSINES AND ITS PREPARATION 失效
公开(公告)号：JPH11147824A
公开(公告)日：1999-06-02
申请号：JP19168298
申请日：1998-07-07
申请人： WANG HUI , SAI OSHO
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
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound useful for treatment of pancreatic cancer, colonic cancer, thyroid cancer, malanotic cancer, etc. SOLUTION: This anticancerous compound is a compound of formula I [R1 is a 1-6C alkyl, benzyl or a 1-6C carbonyl; R2 is a 1-6C alkyl or a 1-6C alkoxyl; R3 is CONR4 R5 or CONHNR4 R5 (R4 and R5 are each H, a 1-6C alkyl, a 2-6C alkenyl or the like) or the like], e.g. N-propyl3-(5-benzyloxy-2-pyridyl)-2-(t- butoxycarbonyl)aminopropionamide acid. The compound of formula I is obtained by using 5-hydroxy2-hydroxymethylpyridine as a raw material, reacting an intermediate of formula II with an alcohol, an amine or an hydrazine in a same equivalent, and dicyclohexylcarbodiimide or carbonyldiimidazole in the same equivalent in a nonprotonic organic solvent such as dimethylamide and dichloromethane under a condition of 20-45 deg.C for 2-12 hr, removing the solvent therefrom and recrystallizing the product.

8. 发明专利

DE19830167B4 未知
公开(公告)号：DE19830167B4
公开(公告)日：2006-04-20
申请号：DE19830167
申请日：1998-07-06
申请人： WANG HUI , TSAI HANSEN
发明人： WANG HUI-PO , LEE ON , SHEW JIN-YUH , LEE SHUI-JANE
IPC分类号： C07D213/65 , A61K31/44 , A61K31/4418 , A61P35/00

9. 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.

10. 发明专利

AU9450501A Piperazinedione compounds 未知
公开(公告)号：AU9450501A
公开(公告)日：2001-12-24
申请号：AU9450501
申请日：2001-05-08
申请人： ADPHARMA INC
发明人： TENG CHE-MING , WANG HUI-PONG , LI ERIC I C , LEE ON , GUH JIH-HWA , CHEN HUEI-TING , FAN YA-BING , CHEN YA-LAN
IPC分类号： A61K31/4965 , A61K31/497 , C07D241/18 , C07D401/06 , C07D409/14

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式