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1. 发明申请

WO2005028474A3 PYRAZOLOQUINOLINE DERIVATIVES AS CHK-1 INHIBITORS 审中-公开
标题翻译：作为CHK-1抑制剂的吡唑啉衍生物
公开(公告)号：WO2005028474A3
公开(公告)日：2005-06-02
申请号：PCT/US2004016837
申请日：2004-05-28
申请人： MILLENNIUM PHARM INC , BOYLE ROBERT GEORGE , IMOGAI HASSAN JULIEN , CHERRY MICHAEL , HUMPHRIES ALFRED JOHN , NAVARRO EVA FIGUEROA , OWEN DAVID RODNEY , DALES NATALIE A , LAMARCHE MATTHEW , CULLIS COURTNEY , GOULD ALEXANDRA E
发明人： BOYLE ROBERT GEORGE , IMOGAI HASSAN JULIEN , CHERRY MICHAEL , HUMPHRIES ALFRED JOHN , NAVARRO EVA FIGUEROA , OWEN DAVID RODNEY , DALES NATALIE A , LAMARCHE MATTHEW , CULLIS COURTNEY , GOULD ALEXANDRA E
IPC分类号： A61K31/435 , A61K31/4745 , A61K45/06 , C07D471/04 , C07D471/14 , C07F5/02 , C07F7/08 , A61P35/00
CPC分类号： C07D471/04 , A61K31/435 , A61K45/06 , C07D471/14 , C07F7/0814 , A61K2300/00
摘要： The application discloses inhibitors of Chk-1of the following general formula (I).
摘要翻译：本申请公开了以下通式（I）的Chk-1抑制剂。

2. 发明申请

WO0239997A3 ACE-2 MODULATING COMPOUNDS AND USE THEREOF 审中-公开
标题翻译： ACE-2调节化合物及其用途
公开(公告)号：WO0239997A3
公开(公告)日：2002-11-28
申请号：PCT/US0145703
申请日：2001-10-31
申请人： MILLENNIUM PHARM INC , ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A , PATANE MICHAEL , KADAMBI VIVEK J , SOLOMON MICHAEL , STRICKER-KRONGRAD ALAIN
发明人： ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A , PATANE MICHAEL , KADAMBI VIVEK J , SOLOMON MICHAEL , STRICKER-KRONGRAD ALAIN
IPC分类号： A61K31/00 , A61K31/195 , A61K31/196 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4035 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61P3/04 , C07D231/12 , C07K16/40 , A61K31/198 , A61K31/415 , A61K31/4152 , A61K31/428 , C07C237/40 , C07D213/55 , C07D213/68 , C07D231/06 , C07D231/08 , C07D261/08 , C07D263/32 , C07D277/22 , C07D277/82 , C07D333/54
CPC分类号： A61K31/196 , A61K31/00 , A61K31/195 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4035 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , C07K16/40
摘要： ACE-2 modulating compounds for the treatment of body disorders are disclosed. Methods of using the compounds and pharmaceutical compositiosn containing the compounds are also claimed.
摘要翻译：公开了用于治疗身体疾病的ACE-2调节化合物。还要求使用含有化合物的化合物和药物组合物的方法。

3. 发明申请

WO2006041773A2 LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： LACTAM化合物作为蛋白激酶抑制剂有用
公开(公告)号：WO2006041773A2
公开(公告)日：2006-04-20
申请号：PCT/US2005035458
申请日：2005-10-03
申请人： MILLENNIUM PHARM INC , BLACKBURN CHRISTOPHER , CLAIBORNE CHRISTOPHER F , CULLIS COURTNEY A , DALES NATALIE A , PATANE MICHAEL A , STIRLING MATTHEW , STRADELLA OMAR G , WEATHERHEAD GABRIEL S
发明人： BLACKBURN CHRISTOPHER , CLAIBORNE CHRISTOPHER F , CULLIS COURTNEY A , DALES NATALIE A , PATANE MICHAEL A , STIRLING MATTHEW , STRADELLA OMAR G , WEATHERHEAD GABRIEL S
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译：本发明提供了可用作蛋白激酶抑制剂的新化合物。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

4. 发明申请

WO0066104A2 ACE-2 INHIBITING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译： ACE-2抑制化合物及其使用方法
公开(公告)号：WO0066104A2
公开(公告)日：2000-11-09
申请号：PCT/US0011550
申请日：2000-04-28
申请人： MILLENNIUM PHARM INC
发明人： ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A
IPC分类号： C07D233/64 , A61K31/198 , A61K31/341 , A61K31/381 , A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61P1/00 , A61P1/02 , A61P5/30 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P19/02 , A61P21/00 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07D209/20 , C07D213/55 , C07D231/12 , C07D233/54 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/20 , C07D277/30 , C07D277/40 , C07D277/42 , C07D307/54 , C07D333/24 , C07D405/06 , C07D413/04 , A61K31/00
CPC分类号： C07D231/12 , C07B2200/07 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07C2601/02 , C07C2601/14 , C07D209/20 , C07D213/55 , C07D233/64 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/30 , C07D277/40 , C07D277/42 , C07D333/24 , C07D405/06
摘要： ACE-2 inhibiting compounds are disclosed. Methods of using the compounds and pharmaceutical compositions containing the compounds are also claimed.
摘要翻译：公开了ACE-2抑制化合物。还要求保护使用化合物和含有这些化合物的药物组合物的方法。

5. 发明申请

WO0066104A9 ACE-2 INHIBITING COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译： ACE-2抑制化合物及其使用方法
公开(公告)号：WO0066104A9
公开(公告)日：2002-08-29
申请号：PCT/US0011550
申请日：2000-04-28
申请人： MILLENNIUM PHARM INC
发明人： ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A
IPC分类号： C07D233/64 , A61K31/198 , A61K31/341 , A61K31/381 , A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61P1/00 , A61P1/02 , A61P5/30 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P19/02 , A61P21/00 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07D209/20 , C07D213/55 , C07D231/12 , C07D233/54 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/20 , C07D277/30 , C07D277/40 , C07D277/42 , C07D307/54 , C07D333/24 , C07D405/06 , C07D413/04 , A61K31/00 , A61K31/4172 , A61K31/4174 , A61K31/4178
CPC分类号： C07D231/12 , C07B2200/07 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07C2601/02 , C07C2601/14 , C07D209/20 , C07D213/55 , C07D233/64 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/30 , C07D277/40 , C07D277/42 , C07D333/24 , C07D405/06
摘要： ACE-2 inhibiting compounds are disclosed. Methods of using the compounds and pharmaceutical compositions containing the compounds are also claimed.
摘要翻译：公开了ACE-2抑制化合物。还要求保护使用化合物和含有这些化合物的药物组合物的方法。

6. 发明专利

AU2012201059A1 Lactam compounds useful as protein kinase inhibitors 未知
公开(公告)号：AU2012201059A1
公开(公告)日：2012-03-15
申请号：AU2012201059
申请日：2012-02-23
申请人： MILLENNIUM PHARM INC
发明人： BLACKBURN CHRISTOPHER , CLAIBORNE CHRISTOPHER F , CULLIS COURTNEY A , DALES NATALIE A , PATANE MICHAEL A , STIRLING MATTHEW , STRADELLA OMAR G , WEATHERHEAD GABRIEL S
IPC分类号： C07D487/04 , A61K31/55
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

7. 发明专利

AR045689A1 COMPUESTOS DERIVADOS DE 2,5-DIHIDRO-PIRAZOLO[4,3-C]QUINOLIN-4-ONA COMO INHIBIDORES DE CHK-1 Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：AR045689A1
公开(公告)日：2005-11-09
申请号：ARP040101835
申请日：2004-05-28
申请人： MILLENNIUM PHARM INC
发明人： BOYLE ROBERT GEORGE , IMOGAI HASSAN JULIEN , CHERRY MICHAEL , HUMPHRIES ALFRED JOHN , NAVARRO EVA FIGUEROA , OWEN DAVID RODNEY , DALES NATALIE A , LAMARCHE MATTHEW , CULLIS COURTNEY , GOULD ALEXANDRA E
IPC分类号： A61K31/435 , A61K31/4745 , A61K45/06 , C07D471/04 , C07D471/14 , C07F5/02 , C07F7/08 , C07D491/14 , C07D495/14 , C07D215/00 , C07D231/00 , C07D249/00
摘要： Se describen inhibidores de Chk-1, composiciones farmacéutias que los contienen y métodos para usar los mismos para terapia contra el cáncer. Reivindicación 1: Un compuesto representado por la siguiente fórmula estructural (1) o una sasl farmacéuticamente aceptable del mismo, donde : el anillo A es un grupo aromático monocíclico que está opcionalmente substituido en uno o más átomos substituibles del anillo y está opcionalmente condensado con un segundo grupo aromático monocíclico, el anillo B; el anillo B está opcionalmente substituido en uno o más átomos substituibles del anillo; Y1 es N o CR3; R1 es -H, -CONR11R12, -COOR12, -C(=NR11)-NR11R12, un grupo heteroarilo opcionalmente substituido, un grupo heterocíclico no aromático opcionalmente substituido, y W1 es una cadena lineal de alquilideno C1-6; R1 es -OR12, -NR11R12, -CN, -NR11CONR11R12, -NR11COR12, -NH-C(=NR11)NR11R12, -N=C(NR11R12)2, -SO2NR11R12, -NR11SO2R12, -OC(O)R12, -NR11C(O)OR12, -O-C(O)-OR12, -OC(O)- NR11R12, -NR11CO-CH(OR12a)-R12, -NR11CO-CH(NR12aR12a)-R12, -NR11CO-(CH2)nCH(NR12aR12a)-R12, -OC(O)-CH(OR12a)-R12, -OC(O)-CH(NR12aR12a)-R12, -NR11-CO-C(R12cR12c)-OR12, -NR11CO-C(R12cR12c)-NR11R12, -OC(O)-C(R12cR12c)-OR12, -OC(O)-C(R12cR12c)-NR11R12, - NR11-C(R12)-C(O)OR12, -NR11-C(R12)-C(O)NR11R12, -NR11-C(R12)CH2OR12, cicloalquilo o -Ph y W1 es un grupo alquilideno C2-6 lineal; o -W1-R1 es -H; donde el grupo alquilideno representado por W1 está opcionalmente monosubstituido con -OR12b, - N(R12b)2, oxo, halo, o un grupo espirocicloalquilo y donde el grupo alquilideno representado por W1 está opcionalmente substituido con uno o más grupos -CH3, con la condición de que el grupo alquilideno representado por W1 esté monosubstituido con - OR12b o -N(R12b)2 cuando R1 es cicloalquilo o -Ph; y R2 es -H o un grupo que se puede escindir in vivo; R3 es -H, halógeno, alquilo, haloalquilo o -V1-R3a, donde V1 es un enlace covalente o un alquilideno C1-4 opcionalmente substituido con uno o más -ORa, -NRbRc, alquilo, hidroxialquilo, alcoxialquilo, aminoalquilo, o con un grupo espirocicloalquilo; R3a es -ORa, -SRa, -CONRbRc, -NRbRc, -NHC(O)NRaRb, -CN, -COOH, -COORa, -NHC(O)H, -NHC(O)Ra, -OC(O)Ra, -CO(O)NRbRC, -NHC(O)-ORa, -S(O)2NRbRC, - S(O)2(Ra), boronato, boronato de alquilo, -C(=NRa)-NRbRc, -NH-C(=NRa)NRbRc, -NH-C(=NRa)Ra, un grupo cicloalifático opcionalmente substituido o heterocíclico no aromático, o un grupo aromático o aralquilo opcionalmente substituido; Ra es -H, alquilo o un grupo aromático o aralquilo opcionalmente substituido; y Rb y Rc son independientemente -H, alquilo o un grupo aromático o aralquilo opcionalmente substituido; o -NRbRc es un grupo heterocíclico no aromático opcionalmente substituido que contiene nitrógeno; X es O, S, N, o CR4 cuando R1 es -CONR11R12, -COOR12, -C(=NR11)-NR11R12, un grupo heteroarilo opcionalmente substituido, un grupo heterocíclico no aromático opcionalmente substituido, -OR12, -NR11R12, -CN, -NR11CONR11R12, - NR11COR12, -NH-C(=NR11)NR11R12, -N=C(NR11R12)2, -SO2NR11R12, -NR11SO2R12, -OC(O)R12, -NR11C(O)OR12, -OC(O)-NR11R12, -NR11CO-CH(OR12a)-R12, -NR11CO-CH(NR12aR12a)-R12, -NR11CO-(CH2)nCH(NR12aR12a)-R12, -OC(O)-CH(OR12a)-R12, -OC(O)-CH(NR12aR12a)-R12, - NR11CO-C(R12cR12c)-OR12, -NR11CO-C(R12cR12c)-NR11R12, -OC(O)-C(R12cR12c)-OR12, -OC(O)-C(R12cR12c)-NR11R12, -NR11-C(R12)-C(O)OR12, -NR11-C(R12)-C(O)NR11R12, -NR11-C(R12)CH2OR12, cicloalquilo o -Ph; y X1 es C-W2-R5 cuando R1 es -H y cuando -W1-R1 es - H; W2 es una cadena lineal de alquilideno C1-6, opcionalmente monosubstituida con -OR12b, -N(R12b)2, o un grupo espirocicloalquilo o con uno o más grupos -CH3; donde el grupo alquilideno C1-6 representado por W2 opcionalmente tiene un grupo ciclopropilo, un grupo ciclopropilo monometilado o un grupo ciclopropilo dimetilado condensado al mismo; y donde un átomo de carbono en el grupo alquilideno C1-6 representado por W2 está opcionalmente substituido con T; T es un enlace covalente, -C- , -O-, -S-, -N(R6)-, -S(O)-, -SO2-, -C(O)-, -OC(O)-, -C(O)O-, -N(R6)C(O)-, -C(O)N(R6)-, -SO2N(R6)-, o -N(R6)SO2-; R4 es -H, alquilo C1-3, haloalquilo C1-3, halógeno, hidroxi, alcoxi C1-3, haloalcoxi C1-3, -NH2, alquilamina C1-3, dialquilamina C1-3, - NHC(O)H, -NHC(O)(alquilo C1-3), -C(O)NH2, -C(O)NH(alquilo C1-3) o -C(O)N(alquilo C1-3)2; R5 es un grupo heteroarilo opcionalmente substituido, un grupo heterocíclico no aromático opcionalmente substituido, -OR12, -NR11R12, -CN, -NR11CONR11R12, - NR11SO2R12, -NR11COR12, -NH-C(=NR11)NR11R12, -SO2NR11R12, -CONR11R12, -COOR12, -OC(O)R12, -NR11C(O)OR12, -OC(O)-NR11R12, -NR11CO-CH(OR12a)-R12, -NR11CO-CH(NR12aR12a)-R12, -OC(O)-CH(OR12a)-R12, -OC(O)-CH(NR12aR12a)-R12, -NR11CO-C(R12cR12c)-OR12, - NR11CO-C(R12cR12c)-NR11R12, -OC(O)-C(R12cR12c)-OR12, -OC(O)-C(R12cR12c)-NR11R12, -CH(NR11R12)-Ph, -CH(NR11R12)-(cicloalquilo), un grupo cicloalquilo o un grupo fenilo substituido con -V2-OR12, -V-NR11R12, donde V2 es un enlace covalente o un grupo alquileno C1-5; R6 es -H o alquilo C1-3 ; cada R11 es independientemente -H o un grupo alquilo C1-3; y cada R12 es independientemente -H, un grupo alquilo, aromático, aralquilo, heterocíclico no aromático o heterociclilalquilo no aromático opcionalmente substituido; o -NR11R12 es un grupo heterocíclico no aromático que contiene nitrógeno; cada R12a es independientemente -H, un grupo alquilo C1-3, -C(O)H, -C(O)-(alquilo C1-3), -C(O)NH2, -C(O)NH-(alquilo C1-3), -C(O)N-(alquilo C1-3)2, - C(O)O-(alquilo C1-3), -S(O)2(alquilo C1-3) o -NR12aR12a tomados conjuntamente es un grupo heterocíclico no aromático substituido o no substituido que contiene nitrógeno; cada R12b es independientemente -H o un grupo alquilo C1-3 o -NR12bR12b tomados conjuntamente es un grupo heterocíclico no aromático substituido o no substituido que contiene nitrógeno; cada R12c es independientemente -H, un grupo alquilo C1-3 o -C(R12cR12c)- tomados conjuntamente es un grupo cicloalquilo C3-8; Ph es un grupo fenilo opcionalmente substituido; y n es un entero de 1 a 4.

8. 发明专利

AU4500200A Ace-2 inhibiting compounds and methods of use thereof 未知
公开(公告)号：AU4500200A
公开(公告)日：2000-11-17
申请号：AU4500200
申请日：2000-04-28
申请人： MILLENNIUM PHARM INC
发明人： ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A
IPC分类号： C07D233/64 , A61K31/198 , A61K31/341 , A61K31/381 , A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61P1/00 , A61P1/02 , A61P5/30 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P19/02 , A61P21/00 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07D209/20 , C07D213/55 , C07D231/12 , C07D233/54 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/20 , C07D277/30 , C07D277/40 , C07D277/42 , C07D307/54 , C07D333/24 , C07D405/06 , C07D413/04 , A61K31/00
摘要： ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV):wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.

10. 发明专利

NO20015274D0 未知
公开(公告)号：NO20015274D0
公开(公告)日：2001-10-29
申请号：NO20015274
申请日：2001-10-29
申请人： MILLENNIUM PHARM INC
发明人： ACTON SUSAN L , OCAIN TIMOTHY D , GOULD ALEXANDRA E , DALES NATALIE A , GUAN BING , BROWN JAMES A
IPC分类号： C07D233/64 , A61K31/198 , A61K31/341 , A61K31/381 , A61K31/405 , A61K31/415 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61P1/00 , A61P1/02 , A61P5/30 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P19/02 , A61P21/00 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07D209/20 , C07D213/55 , C07D231/12 , C07D233/54 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/20 , C07D277/30 , C07D277/40 , C07D277/42 , C07D307/54 , C07D333/24 , C07D405/06 , C07D413/04 , C07C
摘要： ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV):wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.

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