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61. 发明专利

AU2003251559A8 Heterocyclic inhibitors of kinases 未知
公开(公告)号：AU2003251559A8
公开(公告)日：2004-01-06
申请号：AU2003251559
申请日：2003-06-18
申请人： SQUIBB BRISTOL MYERS CO
发明人： BORZILLERI ROBERT M , BHIDE RAJEEV S , TOKARSKI JOHN S , CAI ZHEN-WEI
IPC分类号： C07D277/20 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P35/00 , A61P43/00 , C07D233/70 , C07D233/84 , C07D233/88 , C07D263/28 , C07D263/46 , C07D263/48 , C07D277/34 , C07D277/36 , C07D277/38 , C07D277/42 , C07D417/12 , C07D417/14 , C07D263/38 , C07C233/88
摘要： The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

63. 发明专利

PE01262001A1 PIRROLOTRIAZINAS COMO INHIBIDORES DE CINASAS 未知
公开(公告)号：PE01262001A1
公开(公告)日：2001-04-22
申请号：PE0004842000
申请日：2000-05-22
申请人： SQUIBB BRISTOL MYERS CO
发明人： BHIDE RAJEEV S , HUNT JOHN T , BORZILLERI ROBERT M , QIAN LIGANG
IPC分类号： A61K31/53 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/53
摘要： SE REFIERE A PIRROLOTRIAZINAS DE FORMULA I DONDE: X E Y SON O, OCO, S, SO, SO2, CO, NR10, NR11CO, ENTRE OTROS; Z ES O, S, N, CR20; R1 ES H, CH3, OH, OCH3, SH, SCH3, OCOR21, SOR22, SO2R23, ENTRE OTROS; R2 Y R3 SON H, ALQUILO, ALQUENILO, ENTRE OTROS; CUANDO X ES HALO, NITRO, CIANO, R2 ESTA AUSENTE; CUANDO Y ES HALO, NITRO, CIANO, R3 ESTA AUSENTE; R4 Y R5 SON H, ALQUILO, ARILO, HETEROCICLO, ENTRE OTROS; R6 ES H, ALQUILO, ARILO, HETEROCICLO, NR7R8, OR9, ENTRE OTROS; R7, R8, R9, R13, R14, R21 SON H, ALQUILO, ARILO, HETERICICLO; R22, R23 SON ALQUILO, ARILO, HETEROCICLO; R2 NO ES H; SI X ES SO, SO2, NR13CO2, NR14SO2; R3 NO ES H SI Y ES SO, SO2, NR13CO2, NR14SO2. SON COMPUESTOS PREFERIDOS N-(4-CLOROFENIL)PIRROLO[2,1-f][1,2,4]TRIAZIN-4-AMINA, 2-METIL-5-(PIRROLO[2,1-f][1,2,4]TRIAZIN-4-ILAMINO)FENOL, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN AGENTE ANTICANCEROSO O CITOTOXICO TAL COMO TAMOXIFEN, TOREMIFEN, RALOXIFENO, DROLOXIFENO, YODOXIFENO, ACETATO DE MEGESTROL, ANASTROZOL, LETRAZOL, BORAZOL, EXEMESTANO, FLUTAMIDA, EPOTILONA, ENTRE OTROS. EL COMPUESTO I ES UN INHIBIDOR DE TIROSINCINASA, DE LOS RECEPTORES DEL FACTOR DE CRECIMIENTO Y TIENE EFECTO ANTIANGIOGENICO, EFECTO REDUCTOR DE LA PERMEABILIDAD VASCULAR Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS, AUTOINMUNES, CANCER, INFLAMACION

64. 发明专利

CZ20000058A3 Epothilone derivatives 未知
公开(公告)号：CZ20000058A3
公开(公告)日：2001-01-17
申请号：CZ20000058
申请日：1998-06-16
申请人： SQUIBB BRISTOL MYERS CO
发明人： VITE GREGORY D , BORZILLERI ROBERT M , KIM SOONG-HOON , JOHNSON JAMES A
IPC分类号： C07D491/044 , A61K31/335 , A61K31/395 , A61K31/427 , A61P19/00 , A61P35/00 , A61P43/00 , C07D225/00 , C07D273/00 , C07D277/26 , C07D313/00 , C07D417/06 , C07D417/08 , C07D491/04 , C07D493/04 , C07D498/04
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04

65. 发明专利

TR200000065T2 未知
公开(公告)号：TR200000065T2
公开(公告)日：2000-11-21
申请号：TR200000065
申请日：1998-06-16
申请人： SQUIBB BRISTOL MYERS CO
发明人： VITE GREGORY D , BORZILLERI ROBERT M , KIM SOONG-HOON , JOHNSON JAMES A
IPC分类号： C07D491/044 , A61K31/335 , A61K31/395 , A61K31/427 , A61P19/00 , A61P35/00 , A61P43/00 , C07D225/00 , C07D273/00 , C07D277/26 , C07D313/00 , C07D417/06 , C07D417/08 , C07D491/04 , C07D493/04 , C07D498/04
摘要： The present invention relates to compounds of the formulaQ is selected from the group consisting ofG is selected from the group consisting of alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo,W is O or NR 15 ;X is O or H,H;Y is selected from the group consisting of O; H,OR 16 ; OR 17 ,OR 17 ; NOR 18 ; H,NOR 19 ; H,NR 20 R 21 ; H,H; or CHR 22 ; OR 17 OR 17 can be a cyclic ketal;Z 1 , and Z 2 are selected from the group consisting of CH 2 , O, NR 23 , S, or SO 2 , wherein only one of Z and Z 2 is a heteroatom;B 1 and B 2 are selected from the group consisting of OR 24 , or OCOR 25 , or O 2 CNR 26 R 27 ; when B 1 is H and Y is OH, H they can form a six-membered ring ketal or acetal;D is selected from the group consisting of NR 28 R 29 , NR 30 COR 31 or saturated heterocycleR 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 13 , R 14 , R 18 , R 19 , R 20 , R 21 , R 22 , R 26 , and R 27 are selected from the group H, alkyl, substituted alkyl, or aryl and when R 1 and R 2 are alkyl can be joined to form a cycloalkyl; R 3 and R 4 are alkyl can be joined to form a cycloalkyl;R 9 , R 10 , R 16 , R 17 , R 24 , R 25 , and R 31 are selected from the group H, alkyl, or substituted alkyl;R 8 , R 11 , R 12 , R 28 , R 30 , R 32 , R 33 , and R 30 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo;R 15 , R 23 and R 29 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R 32 C=O, R 33 SO 2 , hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds whereinW and X are both O; andR 1 , R 2 , R 7 , are H; andR 3 , R 4 , R 6 , are methyl; andR 8 , is H or methyl; andZ 1 , and Z 2 , are CH 2 ; andG is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; andQ is as defined above are excluded.

66. 发明专利

BG104068A EPOTILON DERIVATIVES 未知
公开(公告)号：BG104068A
公开(公告)日：2000-09-29
申请号：BG10406800
申请日：2000-01-10
申请人： SQUIBB BRISTOL MYERS CO
发明人： VITE GREGORY D , BORZILLERI ROBERT M , KIM SOONG-HOON , JOHNSON JAMES A
IPC分类号： C07D491/044 , A61K31/335 , A61K31/395 , A61K31/427 , A61P19/00 , A61P35/00 , A61P43/00 , C07D225/00 , C07D273/00 , C07D277/26 , C07D313/00 , C07D417/06 , C07D417/08 , C07D491/04 , C07D493/04 , C07D498/04
摘要： The compounds have the formula where G is selected from the group of the following substituents: the meaning of which is listed in the description, Q is selected from the group of the substituents alkyl, substituted alkyl, substituted or unsubstituted aryl, heterocyclo with the following formulae W is O or NR15, X is O or H, H; Y is O, H, OR16; OR17, OR17; NOR18, H,NOR19, H, NR220R21; H,H; or CHR22; OR17OR17 can be cyclic ketal; Z1 & Z2 are from the group of CH2, O, NR23, S or SO2, but only one of Z1 and Z2 can be heteroatom;B1 & B2 are OR24 or OCOR25, or O2CNR26R27; when B1 is H and Y is OH, H, they can form a six-atom ring ketal or acetal; D is selected from the group NR28R29, NR30COR31 or saturated heterocycle; R1, R2, R3, R4, R6, R7, R13, R14, R18, R19, R20, R21, R22, R26 and R27 are selected from the group H, alkyl, substututed alkyl, or aryl, and when R1 & R2 are alkyl, they can be bound to form cycloalkyl; when R3 & R4 are alkyl, they can be bound in order to form cycloalkyl; R9, R10, R16, R17, R24, R25 and R 31 are selected from H, alkyl, or substituted alkyl; R8, R11, R12, R28, R30, R32, R33 & R30 are selected from H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl or heterocyclo; R 15, R23 & R29 are selected from H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R32C=O, R33SO2, hydroxy, O-alkyl or O-substituted alkyl. The invention also relates to their pharmaceutically acceptable salts, to their solvates or hydrates, optical and stereoisomers provided that no compounds shall be included where W & X are simultaneously O and R1, R2, R7 are H; R3, R4, R6 are methyl; R8 is H or methyl, Z1 & Z2 are CH2; G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl and Q has the meaning given above. 6 claims

67. 发明专利

ZA985938B Epothilone derivatives. 未知
公开(公告)号：ZA985938B
公开(公告)日：2000-01-10
申请号：ZA985938
申请日：1998-07-06
申请人： SQUIBB BRISTOL MYERS CO
发明人： VITE GREGORY D , BORZILLERI ROBERT M , KIM SOONG-HOON , JOHNSON JAMES A
IPC分类号： C07D313/00 , A61K20060101 , A61K31/335 , A61K31/395 , A61P35/00 , C07D20060101 , C07D , A61K

68. 发明专利

EA037112B1 ИНГИБИТОРЫ TGF- 未知
公开(公告)号：EA037112B1
公开(公告)日：2021-02-08
申请号：EA201791955
申请日：2016-02-26
申请人： RIGEL PHARMACEUTICALS INC , SQUIBB BRISTOL MYERS CO
发明人： KINSELLA TODD , GELMAN MARINA , HONG HUI , DARWISH IHAB S , SINGH RAJINDER , YU JIAXIN , BORZILLERI ROBERT M , VELAPARTHI UPENDER , LIU PEIYING , DARNE CHETAN , RAHAMAN HASIBUR , WARRIER JAYAKUMAR SANKARA
IPC分类号： C07D401/04 , A61K31/4164 , A61K31/426 , A61P35/00 , C07D403/04 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Визобретениираскрытысоединенияимидазолаформулы (I°) иихфармацевтическиприемлемыесоли, атакжефармацевтическиекомпозициии способыихприменения,где Z представляетсобой , X, A, R1, возможныезаместители Z идругиезаместителираскрытыв описании. Соединениев соответствиис изобретениемингибирует TGF- иможетбытьиспользованодлялечениязаболеванияилисостояния, опосредованногоиливызванного TGF-.

69. 发明专利

ZA201704739B HETEROARYLENE-BRIDGED BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING 未知
公开(公告)号：ZA201704739B
公开(公告)日：2019-02-27
申请号：ZA201704739
申请日：2017-07-13
申请人： SQUIBB BRISTOL MYERS CO
发明人： MCDONALD IVAR M , CHOWDARI NAIDU S , JOHNSON WALTER LEWIS , ZHANG YONG , BORZILLERI ROBERT M , GANGWAR SANJEEV
摘要： and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

70. 发明专利

AU2016284340A1 Macrocyclic benzodiazepine dimers, conjugates thereof, preparation and uses 未知
公开(公告)号：AU2016284340A1
公开(公告)日：2018-02-08
申请号：AU2016284340
申请日：2016-06-22
申请人： SQUIBB BRISTOL MYERS CO
发明人： ZHANG YONG , BORZILLERI ROBERT M , TEBBEN ANDREW J , STANG ERIK M , DONNELL ANDREW F , SCHROEDER GRETCHEN M , PEREZ HEIDI L , WEI DONNA D
IPC分类号： C07D519/00 , A61K31/5513 , A61K31/5517 , A61P35/00
摘要： Macrocyclic benzodiazepine dimers having a structure represented by formula (I) where A and B are independently according to formulae (Ia) or (Ib) ]; and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).

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