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1. 发明专利

DE69524154T2 未知
公开(公告)号：DE69524154T2
公开(公告)日：2002-07-18
申请号：DE69524154
申请日：1995-07-27
申请人： BRISTOL MYERS SQUIBB CO
发明人： WONG HENRY S , WITTMAN MARK D
IPC分类号： A61K31/335 , A61K31/337 , A61K36/00 , A61P35/00 , C07D305/14 , C07D407/12
摘要： The present invention concerns taxane derivatives of formula I, wherein R is hydrogen, C1-8 alkyloxy, C2-8 alkenyloxy, or C2-8 alkynyloxy, each can be optionally substituted with hydroxy; R is hydroxy, -OC(O)R or -OC(O)OR ; R and R are independently C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, or -Z-R ; p is zero or one; Z is a direct bond, C1-8 alkylene or C2-8 alkenediyl; R is aryl, substituted aryl, C3-8 cycloalkyl or heteroaryl; and R is C1-8 alkyl optionally, substituted with one to six same or different halogen atoms, C3-8 cycloalkyl or C2-8 alkenyl; or R is a radical of the formula wherein D is a bond or C1-8 alkyl; and R , R and R are independently hydrogen, amino, C1-8 alkylamino, di-C1-8alkylamino, halogen, C1-8 alkyl, or C1-8 alkyloxy, their use as antitumor agents and pharmaceutical compositions containing the novel compounds.

2. 发明专利

NO934614L 未知
公开(公告)号：NO934614L
公开(公告)日：1994-06-27
申请号：NO934614
申请日：1993-12-15
申请人： BRISTOL MYERS SQUIBB CO
发明人： GOLIK JERZY , VYAS DOLATRAI , WRIGHT JOHN J , WONG HENRY S , KADOW JOHN F , THOTATHIL JOHN K , LI WEN-SEN , KAPLAN MURRAY ARTHUR , PERRONE ROBERT KEVIN
IPC分类号： A61K31/665 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48 , C07F9/11
摘要： The present invention concerns novel water-soluble phosphonooxymethyl ethers of taxane derivatives, their use as antitumor agents, and pharmaceutical compositions containing the novel compounds.

3. 发明专利

HU201773B PROCESS FOR PRODUCING REBECCAMYCIN ANALOGS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH ACTIVE INGREDIENT 未知
公开(公告)号：HU201773B
公开(公告)日：1990-12-28
申请号：HU516487
申请日：1987-11-20
申请人： BRISTOL MYERS SQUIBB CO
发明人： KANEKO TAKUSHI , WONG HENRY S , UTZIG JACOB J
IPC分类号： C07H19/23 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61P35/00 , C07H19/044
摘要： There are disclosed analogs of the antitumor agent, rebeccamycin, having the formula wherein: n is an integer from 1 to 6; A and A are selected from H and -(CH2)nNR R and at least one of A and A is -(CH2)n-NR R ; R and R , independently, are selected from hydrogen, unsubstituted and substituted C1-C6 alkyl, aralkyl having 1 to 3 carbons in the alkyl moiety and unsubstituted phenyl or phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, carboxyl, alkoxycarbonyl, and amino and mono- and di-lower-alkylamino groups in the aryl moiety, and aryl selected from unsubstituted phenyl and phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, amino, mono- and dialkylamino, nitro, carboxyl, alkoxycarbonyl, and cyano groups provided that both R and R are not each aryl and, when taken together, R and R may be selected from -(CH2)4- and (CH2)2-R -(CH2)2- to form a 5- or 6-membered ring together with the N-atom wherein R is selected from CH2, NH, O and S; X is selected from H, F, Cl, Br, C1-C3 alkyl, OH, carboxyl, alkoxycarbonyl and alkoxy wherein the alkyl moiety is C1-C3 alkyl, benzyloxy, amino, and mono- and dialkylamino; and R is selected from H and CH3; and pharmaceutically acceptable acid addition and base salts thereof. The compounds possess antineoplastic properties against mammalian, particularly experimental animal, tumor systems. The compounds of the invention are aminoalkylated derivatives of rebeccamycin produced by first reacting rebeccamycin with a strong base to obtain a reactive intermediate and then reacting the reactive intermediate with an aminoalkyl compound.

4. 发明专利

DE69524154D1 未知
公开(公告)号：DE69524154D1
公开(公告)日：2002-01-10
申请号：DE69524154
申请日：1995-07-27
申请人： BRISTOL MYERS SQUIBB CO
发明人： WONG HENRY S , WITTMAN MARK D
IPC分类号： A61K31/335 , A61K31/337 , A61K36/00 , A61P35/00 , C07D305/14 , C07D407/12
摘要： The present invention concerns taxane derivatives of formula I, wherein R is hydrogen, C1-8 alkyloxy, C2-8 alkenyloxy, or C2-8 alkynyloxy, each can be optionally substituted with hydroxy; R is hydroxy, -OC(O)R or -OC(O)OR ; R and R are independently C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, or -Z-R ; p is zero or one; Z is a direct bond, C1-8 alkylene or C2-8 alkenediyl; R is aryl, substituted aryl, C3-8 cycloalkyl or heteroaryl; and R is C1-8 alkyl optionally, substituted with one to six same or different halogen atoms, C3-8 cycloalkyl or C2-8 alkenyl; or R is a radical of the formula wherein D is a bond or C1-8 alkyl; and R , R and R are independently hydrogen, amino, C1-8 alkylamino, di-C1-8alkylamino, halogen, C1-8 alkyl, or C1-8 alkyloxy, their use as antitumor agents and pharmaceutical compositions containing the novel compounds.

5. 发明专利

NO306727B1 未知
公开(公告)号：NO306727B1
公开(公告)日：1999-12-13
申请号：NO930388
申请日：1993-02-04
申请人： BRISTOL MYERS SQUIBB CO
发明人： UEDA YASUTSUGU , WONG HENRY S , FARINA VITTORIO , MIKKILINENI AMARENDRA B , VYAS DOLATRAI M , DOYLE TERRENCE
IPC分类号： A61K31/335 , A61K31/337 , A61K31/665 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48 , C07F9/38 , A61K31/66

7. 发明专利

DE3783577D1 未知
公开(公告)号：DE3783577D1
公开(公告)日：1993-02-25
申请号：DE3783577
申请日：1987-11-20
申请人： BRISTOL MYERS SQUIBB CO
发明人： KANEKO TAKUSHI , WONG HENRY S , UTZIG JACOB J
IPC分类号： C07H19/23 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61P35/00 , C07H19/044
摘要： There are disclosed analogs of the antitumor agent, rebeccamycin, having the formula wherein: n is an integer from 1 to 6; A and A are selected from H and -(CH2)nNR R and at least one of A and A is -(CH2)n-NR R ; R and R , independently, are selected from hydrogen, unsubstituted and substituted C1-C6 alkyl, aralkyl having 1 to 3 carbons in the alkyl moiety and unsubstituted phenyl or phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, carboxyl, alkoxycarbonyl, and amino and mono- and di-lower-alkylamino groups in the aryl moiety, and aryl selected from unsubstituted phenyl and phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, amino, mono- and dialkylamino, nitro, carboxyl, alkoxycarbonyl, and cyano groups provided that both R and R are not each aryl and, when taken together, R and R may be selected from -(CH2)4- and (CH2)2-R -(CH2)2- to form a 5- or 6-membered ring together with the N-atom wherein R is selected from CH2, NH, O and S; X is selected from H, F, Cl, Br, C1-C3 alkyl, OH, carboxyl, alkoxycarbonyl and alkoxy wherein the alkyl moiety is C1-C3 alkyl, benzyloxy, amino, and mono- and dialkylamino; and R is selected from H and CH3; and pharmaceutically acceptable acid addition and base salts thereof. The compounds possess antineoplastic properties against mammalian, particularly experimental animal, tumor systems. The compounds of the invention are aminoalkylated derivatives of rebeccamycin produced by first reacting rebeccamycin with a strong base to obtain a reactive intermediate and then reacting the reactive intermediate with an aminoalkyl compound.

8. 发明专利

NO310238B1 未知
公开(公告)号：NO310238B1
公开(公告)日：2001-06-11
申请号：NO934614
申请日：1993-12-15
申请人： BRISTOL MYERS SQUIBB CO
发明人： GOLIK JERZY , VYAS DOLATRAI , WRIGHT JOHN J , WONG HENRY S , KADOW JOHN F , THOTATHIL JOHN K , LI WEN-SEN , KAPLAN MURRAY ARTHUR , PERRONE ROBERT KEVIN
IPC分类号： A61K31/665 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48 , C07F9/11 , A61K31/675
摘要： The present invention concerns novel water-soluble phosphonooxymethyl ethers of taxane derivatives, their use as antitumor agents, and pharmaceutical compositions containing the novel compounds.

9. 发明专利

NO934614A 未知
公开(公告)号：NO934614A
公开(公告)日：1994-06-27
申请号：NO934614
申请日：1993-12-15
申请人： BRISTOL MYERS SQUIBB CO
发明人： GOLIK JERZY , VYAS DOLATRAI , WRIGHT JOHN J , WONG HENRY S , KADOW JOHN F , THOTATHIL JOHN K , LI WEN-SEN , KAPLAN MURRAY ARTHUR , PERRONE ROBERT KEVIN
IPC分类号： A61K31/665 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48 , C07F9/11
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07F7/1856 , C07F9/65512 , C07F9/65586 , H01L21/4839

10. 发明专利

DE3783577T2 未知
公开(公告)号：DE3783577T2
公开(公告)日：1993-05-19
申请号：DE3783577
申请日：1987-11-20
申请人： BRISTOL MYERS SQUIBB CO
发明人： KANEKO TAKUSHI , WONG HENRY S , UTZIG JACOB J
IPC分类号： C07H19/23 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61P35/00 , C07H19/044
摘要： There are disclosed analogs of the antitumor agent, rebeccamycin, having the formula wherein: n is an integer from 1 to 6; A and A are selected from H and -(CH2)nNR R and at least one of A and A is -(CH2)n-NR R ; R and R , independently, are selected from hydrogen, unsubstituted and substituted C1-C6 alkyl, aralkyl having 1 to 3 carbons in the alkyl moiety and unsubstituted phenyl or phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, carboxyl, alkoxycarbonyl, and amino and mono- and di-lower-alkylamino groups in the aryl moiety, and aryl selected from unsubstituted phenyl and phenyl substituted with 1 to 3 alkyl, alkoxy, hydroxy, halo, amino, mono- and dialkylamino, nitro, carboxyl, alkoxycarbonyl, and cyano groups provided that both R and R are not each aryl and, when taken together, R and R may be selected from -(CH2)4- and (CH2)2-R -(CH2)2- to form a 5- or 6-membered ring together with the N-atom wherein R is selected from CH2, NH, O and S; X is selected from H, F, Cl, Br, C1-C3 alkyl, OH, carboxyl, alkoxycarbonyl and alkoxy wherein the alkyl moiety is C1-C3 alkyl, benzyloxy, amino, and mono- and dialkylamino; and R is selected from H and CH3; and pharmaceutically acceptable acid addition and base salts thereof. The compounds possess antineoplastic properties against mammalian, particularly experimental animal, tumor systems. The compounds of the invention are aminoalkylated derivatives of rebeccamycin produced by first reacting rebeccamycin with a strong base to obtain a reactive intermediate and then reacting the reactive intermediate with an aminoalkyl compound.

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