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公开(公告)号:US06897214B2
公开(公告)日:2005-05-24
申请号:US10136276
申请日:2002-05-02
IPC分类号: A61P35/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D521/00 , C07D40/00 , A61K31/535 , C07D239/72
CPC分类号: C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译: 本发明涉及式I的喹唑啉衍生物,其中X 1是直链,或基团如CO,C(R 2)2, 和CH(OR 2); 其中Q 1是苯基,萘基或5或6元杂芳基部分和Q 1至多3个取代基; 其中m为1或2,并且每个R 1可以为诸如氢,卤代和三氟甲基的基团; 并且其中Q 2可以是苯基或9或10元双环杂环部分,Q 2任选地带有至多3个取代基; 或其药学上可接受的盐; 其制备方法,含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。
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公开(公告)号:US06288103B1
公开(公告)日:2001-09-11
申请号:US09485107
申请日:2000-02-03
IPC分类号: A61K31404
CPC分类号: C07D409/12 , C07D209/42
摘要: The invention concerns pharmaceutically useful indoles of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, as well as pharmaceutical compositions containing them. The novel compounds possess inhibitory activity against monocyte chemoattractant protein-1 (MCP-1). The invention further concerns the use of such indoles in the treatment of a disease or condition mediated by MCP-1.
摘要翻译: 本发明涉及式(I)的药学有用的吲哚,其中Z,X,T,A,R 1,R 2,p和q具有本文定义的任何含义及其药学上可接受的盐或体内可水解的酯,以及 作为含有它们的药物组合物。 新化合物对单核细胞趋化蛋白-1(MCP-1)具有抑制活性。 本发明还涉及这种吲哚在治疗MCP-1介导的疾病或病症中的应用。
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3.
公开(公告)号:US20090054409A1
公开(公告)日:2009-02-26
申请号:US12088678
申请日:2006-09-29
IPC分类号: A61K31/551 , C07D403/04 , C07D413/08 , C07D243/08 , A61K31/506 , A61P35/02 , A61P37/00 , A61P17/06 , A61P19/00 , A61P9/00 , A61P35/04 , A61K31/5377 , C07D239/02 , A61K31/496
CPC分类号: C07D471/04
摘要: Compounds of formula (I): which possess cell-cycle inhibitory activity are described.
摘要翻译: 描述了具有细胞周期抑制活性的式(I)化合物。
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公开(公告)号:US06399602B1
公开(公告)日:2002-06-04
申请号:US09152070
申请日:1998-09-11
IPC分类号: C07D40100
CPC分类号: C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译: 本发明涉及式I的喹唑啉衍生物,其中X1是直接键或诸如CO,C(R 2)2和CH(OR 2)的基团;其中Q 1是苯基,萘基或5-或6-元杂芳基部分和Q 1 任选地带有至多3个取代基;其中m是1或2,并且每个R 1可以是诸如氢,卤代和三氟甲基的基团; 并且其中Q2可以是苯基或9或10元双环杂环部分,Q2任选地带有至多3个取代基;或其药学上可接受的盐;其制备方法,含有它们的药物组合物及其受体酪氨酸激酶 治疗增殖性疾病如癌症的抑制性质。
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公开(公告)号:US5952333A
公开(公告)日:1999-09-14
申请号:US930044
申请日:1997-09-26
申请人: Andrew John Barker
发明人: Andrew John Barker
IPC分类号: A61K31/505 , A61K31/517 , A61P35/00 , A61P43/00 , C07D239/94
CPC分类号: C07D239/94
摘要: The invention concerns the quinazoline derivative 6-(2-methoxyethylamino)-7-methoxy-4-(3'-methylanilino)quinazoline, or a pharmaceutically-acceptable salt thereof, processes for its preparation, pharmaceutical compositions containing the compound and the use of the receptor tyrosine kinase inhibitory properties of the compound in the treatments of proliferative disease such as cancer.
摘要翻译: PCT No.PCT / GB96 / 00962 Sec。 371日期:1997年9月26日 102(e)1997年9月26日PCT PCT 1996年4月23日PCT公布。 公开号WO96 / 33981 日期1996年10月31日本发明涉及喹唑啉衍生物6-(2-甲氧基乙氨基)-7-甲氧基-4-(3'-甲基苯胺基)喹唑啉或其药学上可接受的盐,其制备方法, 化合物和使用化合物在增殖性疾病如癌症治疗中的受体酪氨酸激酶抑制性质。
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公开(公告)号:US5814630A
公开(公告)日:1998-09-29
申请号:US800830
申请日:1997-02-13
IPC分类号: A61K31/00 , A61K31/505 , A61K31/517 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P9/00 , A61P13/00 , A61P13/08 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D403/04 , C07D405/04 , C07D409/04 , A61K31/495 , C07D401/02 , C07D403/02
CPC分类号: C07D403/04 , C07D405/04 , C07D409/04
摘要: The invention concerns quinazoline compounds of the formula I ##STR1## wherein Q.sup.1 is a 5- or 6-membered heteroaryl moiety and Q.sup.1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R.sup.1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q.sup.2 is phenyl which optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译: 本发明涉及式I的喹唑啉化合物其中Q1是5-或6-元杂芳基部分,并且Q1任选地带有至多3个取代基; 其中m为1或2,并且每个R 1可以为诸如氢,卤代和三氟甲基的基团; 并且其中Q2是任选地带有至多3个取代基的苯基; 或其药学上可接受的盐; 其制备方法,含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。
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公开(公告)号:US06953809B2
公开(公告)日:2005-10-11
申请号:US10194969
申请日:2002-07-15
IPC分类号: C07D401/04 , A61K31/00 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/06 , A61P43/00 , C07D209/04 , C07D209/42 , C07D405/06 , C07D409/04 , C07D413/12
CPC分类号: A61K31/00
摘要: The invention concerns the use of a compound of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.
摘要翻译: 本发明涉及式(I)化合物的用途,其中Z,X,T,A,R 1,R 2,p和q具有 本文定义的含义及其药学上可接受的盐或体内可水解的酯,用于治疗由单核细胞趋化蛋白-1(MCP-1)介导的疾病或病症。 式(I)的某些组分是新的,并且与其药物组合物一起提供作为本发明的进一步特征。
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公开(公告)号:US5866572A
公开(公告)日:1999-02-02
申请号:US796483
申请日:1997-02-13
IPC分类号: A61P35/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D521/00 , A61K31/505 , A61K31/535
CPC分类号: C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein X.sup.1 is a direct link or a group such as CO, C(R.sup.2).sub.2 and CH(OR.sup.2);wherein Q.sup.1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q.sup.1 optionally bears up to 3 substituents;wherein m is 1 or 2 and each R.sup.1 may be a group such as hydrogen, halogeno and trifluoromethyl; andwherein Q.sup.2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q.sup.2 optionally bears up to 3 substituents;or a pharmaceutically-acceptable salt thereof;processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译: 本发明涉及式I的喹唑啉衍生物,其中X1是直接键或诸如CO,C(R 2)2和CH(OR 2)的基团; 其中Q1是苯基,萘基或5-或6-元杂芳基部分,并且Q1任选地带有至多3个取代基; 其中m为1或2,并且每个R 1可以为诸如氢,卤代和三氟甲基的基团; 并且其中Q2可以是苯基或9-或10-元双环杂环部分,Q2任选地带有多达3个取代基; 或其药学上可接受的盐; 其制备方法,含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途。
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9.
公开(公告)号:US07745428B2
公开(公告)日:2010-06-29
申请号:US12088678
申请日:2006-09-29
IPC分类号: C07D471/04 , A61K31/437
CPC分类号: C07D471/04
摘要: Compounds of formula (I): which possess cell-cycle inhibitory activity are described.
摘要翻译: 描述了具有细胞周期抑制活性的式(I)化合物。
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公开(公告)号:US5942514A
公开(公告)日:1999-08-24
申请号:US930043
申请日:1997-09-26
申请人: Andrew John Barker
发明人: Andrew John Barker
IPC分类号: A61K31/505 , A61K31/517 , A61P35/00 , A61P43/00 , C07D239/94
CPC分类号: C07D239/94
摘要: The invention concerns quinazoline derivatives of formula wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno; and R.sup.1 is 1-4C)alkoxy-(2-4C)alkylamino; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
摘要翻译: PCT No.PCT / GB96 / 00960 Sec。 371日期:1997年9月26日 102(e)1997年9月26日PCT PCT 1996年4月23日PCT公布。 出版物WO96 / 33979 日期:1996年10月31日本发明涉及下式的喹唑啉衍生物,其中n为1,2或3,每个R 2独立地为卤代; 并且R 1是1-4C)烷氧基 - (2-4C)烷基氨基; 或其药学上可接受的盐; 其制备方法,含有它们的药物组合物以及该化合物的受体酪氨酸激酶抑制性质用于治疗增殖性疾病例如癌症的用途。
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