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公开(公告)号：US06787536B2
公开(公告)日：2004-09-07
申请号：US10460894
申请日：2003-06-12
IPC分类号： A61K3133
CPC分类号： C07D213/64 , C07D213/38 , C07D213/74 , C07D239/42 , C07D307/52 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/12
摘要： The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.
摘要翻译： 本发明包括作为基质金属蛋白酶，ADAM或ADAM-TS酶抑制剂的新型化合物，其可用于治疗由这些酶介导的疾病，包括退行性疾病和某些癌症。
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公开(公告)号：US06809100B2
公开(公告)日：2004-10-26
申请号：US09858106
申请日：2001-05-15
IPC分类号： A61K31495
CPC分类号： C07D213/64 , C07D213/38 , C07D213/74 , C07D239/42 , C07D307/52 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/12
摘要： The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.
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公开(公告)号：US06933306B2
公开(公告)日：2005-08-23
申请号：US10280766
申请日：2002-10-25
申请人： Duncan Robert Hannah , Hazel Joan Dyke , Robert John Watson , John Fraser Keily , Andrew Douglas Baxter
发明人： Duncan Robert Hannah , Hazel Joan Dyke , Robert John Watson , John Fraser Keily , Andrew Douglas Baxter
IPC分类号： A61K31/437 , A61K31/472 , A61P1/02 , A61P1/04 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D217/08 , C07D401/12 , C07D471/04 , C07D491/04 , C07D513/04 , A61K31/4365
CPC分类号： C07D401/12 , C07D217/08 , C07D471/04 , C07D491/04 , C07D513/04
摘要： Pharmacologically active compounds are provided as well as pharmaceutical compositions and methods for treating cancer; inflammation; an autoimmune, infectious or ocular disease; or age-related macular degeneration in a mammal.
摘要翻译： 提供药理活性化合物以及用于治疗癌症的药物组合物和方法; 炎; 自身免疫性，感染性或眼部疾病; 或年龄相关的黄斑变性。
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公开(公告)号：US06506773B2
公开(公告)日：2003-01-14
申请号：US09855389
申请日：2001-05-15
申请人： Duncan Robert Hannah , Hazel Joan Dyke , Robert John Watson , John Fraser Keily , Andrew Douglas Baxter
发明人： Duncan Robert Hannah , Hazel Joan Dyke , Robert John Watson , John Fraser Keily , Andrew Douglas Baxter
IPC分类号： A61K31472
CPC分类号： C07D401/12 , C07D217/08 , C07D471/04 , C07D491/04 , C07D513/04
摘要： Pharmacologically active compounds are provided as well as pharmaceutical compositions and methods for treating cancer; inflammation; an autoimmune, infectious or ocular disease; or age-related macular degeneration in a mammal.
摘要翻译： 提供药理活性化合物以及用于治疗癌症的药物组合物和方法; 炎; 自身免疫性，感染性或眼部疾病; 或年龄相关的黄斑变性。
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公开(公告)号：US06469020B2
公开(公告)日：2002-10-22
申请号：US09855978
申请日：2001-05-15
申请人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
发明人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
IPC分类号： A61K314355
CPC分类号： C07D401/12 , C07D217/08 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and or INF&agr;-mediated diseases including degenerative diseases and certain cancers.
摘要翻译： 本发明涉及异羟肟酸和羧酸衍生物。 公开了下式的化合物。 这些化合物可用于治疗由基质金属蛋白酶，ADAM，ADAM-TS酶和/或INFalpha介导的疾病包括退行性疾病和某些癌症的抑制剂介导的疾病。
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公开(公告)号：US06734189B2
公开(公告)日：2004-05-11
申请号：US10236637
申请日：2002-09-06
申请人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
发明人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
IPC分类号： A61K444353
CPC分类号： C07D401/12 , C07D217/08 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and/or TNF&agr;-mediated diseases including degenerative diseases and certain cancers.
摘要翻译： 本发明涉及异羟肟酸和羧酸衍生物。 公开了下式的化合物。 这些化合物可用于治疗由基质金属蛋白酶，ADAM，ADAM-TS酶和/或TNFα介导的疾病包括退行性疾病和某些癌症的抑制剂介导的疾病。
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公开(公告)号：US5753666A
公开(公告)日：1998-05-19
申请号：US691339
申请日：1996-08-02
申请人： Steven Colin Beasley , John Gary Montana , Hazel Joan Dyke , Alan Findlay Haughan , George Martin Buckley , Andrew Douglas Baxter
发明人： Steven Colin Beasley , John Gary Montana , Hazel Joan Dyke , Alan Findlay Haughan , George Martin Buckley , Andrew Douglas Baxter
IPC分类号： C07D471/04 , A61K31/00 , A61K31/4375 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/47 , A61K31/505 , A61K31/519 , A61K31/529 , A61P11/00 , A61P31/00 , A61P31/10 , A61P37/00 , A01N43/54 , C07D471/00
CPC分类号： A61K31/4375 , A61K31/444 , A61K31/47 , A61K31/519
摘要： 1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumor Necrosis Factor activity.
摘要翻译： 1-烷基取代的喹诺酮-3-甲酰胺通过抑制磷酸二酯酶IV酯酶和/或肿瘤坏死因子活性具有治疗效用。
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公开(公告)号：US06403791B1
公开(公告)日：2002-06-11
申请号：US09779963
申请日：2001-02-09
申请人： Hazel Joan Dyke , Alan Findlay Haughan , Christopher Lowe , George Martin Buckley , Richard John Davenport , Andrew Sharpe , Hannah Jayne Kendall , Verity Margaret Sabin , John Gary Montana , Catherine Louise Picken
发明人： Hazel Joan Dyke , Alan Findlay Haughan , Christopher Lowe , George Martin Buckley , Richard John Davenport , Andrew Sharpe , Hannah Jayne Kendall , Verity Margaret Sabin , John Gary Montana , Catherine Louise Picken
IPC分类号： C07D41304
CPC分类号： C07D413/12
摘要： A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.
摘要翻译： 式（Ⅳ）的化合物是任选被一个或多个氟取代的C 1-3烷基; R 2是C 1-6烷基，环烷基或NR 4 R 5; R 3是部分式（A），（B）或（B）的吡唑，咪唑或异恶唑基， C）NR4R5是含氮杂环; R6是C1-3烷基; 和R 7和R 8相同或不同，各自表示C 1-3烷基，卤素，CF 3或CN;或其药学上可接受的盐。
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公开(公告)号：US06169090A
公开(公告)日：2001-01-02
申请号：US09328182
申请日：1999-06-08
申请人： Hazel Joan Dyke , Verity Margaret Sabin , Andrew Sharpe , Alan Findlay Haughan , Christopher Lowe , George Buckley , John Montana
发明人： Hazel Joan Dyke , Verity Margaret Sabin , Andrew Sharpe , Alan Findlay Haughan , Christopher Lowe , George Buckley , John Montana
IPC分类号： C07D491048
CPC分类号： C07D491/04
摘要： The compound, according to formula (i) wherein X and Y are independently CH, N or N-oxide, provided that X and Y do not both represent CH; Z is CO or CS; R1 is alkyl, optionally substituted with one or more halogens; and R2, R3, R4 and R5 are each various organic groups. Such compounds have therapeutic utility, via inhibition of phosphodiesterase IV.
摘要翻译： 根据式（ⅰ）的化合物，其中X和Y独立地是CH，N或N-氧化物，条件是X和Y不都表示CH; Z是CO或CS; R1是烷基，任选被一个或多个 卤素 R2，R3，R4和R5分别是各种有机基团。这些化合物通过抑制磷酸二酯酶IV具有治疗效用。
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公开(公告)号：US06313116B1
公开(公告)日：2001-11-06
申请号：US09780911
申请日：2001-02-09
申请人： Hazel Joan Dyke , Andrew Sharpe , Hannah Jayne Kendall , Richard John Davenport , Verity Margaret Sabin , George Martin Buckley , Marianna Dilani Richard , Alan Findlay Haughan
发明人： Hazel Joan Dyke , Andrew Sharpe , Hannah Jayne Kendall , Richard John Davenport , Verity Margaret Sabin , George Martin Buckley , Marianna Dilani Richard , Alan Findlay Haughan
IPC分类号： A61K31428
CPC分类号： C07D417/12
摘要： Compounds that are inhibitors of phosphodiesterase and have therapeutic utility, are of formula (i) wherein R1 is C3-6 cycoalkyl, or C1-3 alkyl optionally substituted with one or more fluorine atoms; R2 is C1-6 alkyl, C3-6 cycloalkyl, CF3, CH2CF3, C2F5 or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, are each H, C1-3 alkyl, halogen, CF3 or CN, provided that both are not H; or a pharmaceutically-acceptable salt thereof
摘要翻译： 作为磷酸二酯酶抑制剂并具有治疗效用的化合物具有式（ⅰ），其中R 1为C 3-6季烷基或任选被一个或多个氟原子取代的C 1-3烷基; R 2为C 1-6烷基，C 3-6环烷基 ，CF 3，CH 2 CF 3，C 2 F 5或NR 4 R 5; R 3为部分式（A），（B）或（C）的吡唑，咪唑或异恶唑基; NR4R5为含氮杂环; R6为C1-3烷基; 和R 7和R 8相同或不同，各自为H，C 1-3烷基，卤素，CF 3或CN，条件是两者均不为H;或其药学上可接受的盐
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