公开(公告)号：US06455561B1

公开(公告)日：2002-09-24

申请号：US09976811

申请日：2001-10-12

Applicant: Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

Inventor： Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

IPC: A61K3142

CPC classification number: C07D405/12 ,  C07D413/12

Abstract: The present invention pertains to compositions and methods for treating disease states which are capable of being modulated by inhibition of phosphodiesterase IV or Tumour Necrosis Factor, or that is a pathological condition associated with a function of phosphodiesterase IV, eosinophil accumulation or a function of the eosinophil, said method comprising administering to a person or animal in need of such treatment an effective amount of the compound of a formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C 1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof

Abstract translation: 本发明涉及用于治疗能够通过抑制磷酸二酯酶IV或肿瘤坏死因子调节的疾病状态的组合物和方法，或者是与磷酸二酯酶IV，嗜酸性粒细胞积累或嗜酸性粒细胞的功能相关的病理状况 所述方法包括向需要这种治疗的人或动物施用有效量的化学式R 1是任选被一个或多个氟取代的C 1-3烷基; R 2是CH 2 OCH 3或2或3-四氢呋喃基; R 3是 部分式（A），（B）或（C）R 4的吡唑，咪唑或异恶唑基是C 1-3烷基; 和R 5和R 6可以相同或不同，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

公开(公告)号：US5728712A

公开(公告)日：1998-03-17

申请号：US650672

申请日：1996-05-20

Applicant: John Gary Montana ,  Hazel Joan Dyke ,  Robert James Maxey ,  Christopher Lowe

Inventor： John Gary Montana ,  Hazel Joan Dyke ,  Robert James Maxey ,  Christopher Lowe

IPC: C07D209/08 ,  C07D215/58 ,  C07D217/08 ,  C07D237/32 ,  A61K31/435 ,  C07D217/24

CPC classification number: C07D215/58 ,  C07D209/08 ,  C07D217/08 ,  C07D237/32

Abstract: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract translation: 3,4-二取代苯基磺酰胺通过TNF或磷酸二酯酶抑制具有治疗效用。

公开(公告)号：US06403791B1

公开(公告)日：2002-06-11

申请号：US09779963

申请日：2001-02-09

Applicant: 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

Inventor： 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: C07D41304

CPC classification number: C07D413/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5925636A

公开(公告)日：1999-07-20

申请号：US859509

申请日：1997-05-20

Applicant: Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

Inventor： Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

IPC: C07D307/79 ,  A61K31/00 ,  A61K31/34 ,  A61K31/343 ,  A61K31/345 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P11/14 ,  A61P11/16 ,  A61P17/06 ,  A61P19/10 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P31/10 ,  A61P35/02 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D20060101 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/84 ,  C07D307/86 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D307/83 ,  C07D401/12

CPC classification number: C07D405/12 ,  C07D307/86 ,  C07D405/14 ,  C07D417/14

Abstract: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).

Abstract translation: 具有式（i）的化合物，其中基团R 1，R 2，R 3，R 4和R 5在本文中定义。 本发明的化合物可用于治疗能够通过抑制介导细胞活性的蛋白质（例如肿瘤坏死因子（TNF））和/或磷酸二酯酶IV（PDE IV）来调节的疾病状态。

公开(公告)号：US06331556B2

公开(公告)日：2001-12-18

申请号：US09780657

申请日：2001-02-09

Applicant: Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

Inventor： Hazel Joan Dyke ,  Christopher Lowe ,  John Gary Montana

IPC: A61K31422

CPC classification number: C07D405/12 ,  C07D413/12

Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C)  R4 is C1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.

Abstract translation: 式R 1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CH 2 OCH 3或2或3-四氢呋喃基; R 3是部分式（A），（B）或（B）的吡唑，咪唑或异恶唑基， C）R 4是C 1-3烷基; 和R 5和R 6可以相同或不同，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。

公开(公告)号：US6066657A

公开(公告)日：2000-05-23

申请号：US246335

申请日：1999-02-09

Applicant: Hazel Joan Dyke ,  John Gary Montana ,  Christopher Lowe ,  Karen Ann Runcie ,  Alan Findlay Haughan ,  Verity Margaret Sabin ,  Duncan Hannah ,  Louise Picken ,  Andrew Sharpe

Inventor： Hazel Joan Dyke ,  John Gary Montana ,  Christopher Lowe ,  Karen Ann Runcie ,  Alan Findlay Haughan ,  Verity Margaret Sabin ,  Duncan Hannah ,  Louise Picken ,  Andrew Sharpe

IPC: C07D307/80 ,  A61K31/343 ,  A61K31/443 ,  A61K31/4545 ,  A61K31/506 ,  A61P1/04 ,  A61P3/14 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/00 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P27/16 ,  A61P29/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D307/82 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/44 ,  A61K31/36

CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: A compound of formula (i) ##STR1## has therapeutic utility via inhibition of phosphodiesterase and THF release.

Abstract translation: 式（i）化合物通过抑制磷酸二酯酶和THF释放具有治疗效用。

公开(公告)号：US5804588A

公开(公告)日：1998-09-08

申请号：US859508

申请日：1997-05-20

Applicant: Hazel Joan Dyke ,  John Gary Montana ,  Christopher Lowe ,  Hannah Jayne Kendall ,  Verity Margaret Sabin

Inventor： Hazel Joan Dyke ,  John Gary Montana ,  Christopher Lowe ,  Hannah Jayne Kendall ,  Verity Margaret Sabin

IPC: C07D215/26 ,  A61K31/00 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/06 ,  A61P43/00 ,  C07D215/48 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D215/00

CPC classification number: C07D401/12 ,  A61K45/06 ,  C07D215/48 ,  C07D401/14 ,  C07D417/12

Abstract: The subject invention concerns novel compounds of the general formula (i) ##STR1## that are useful in treating disease states, such as those states associated with proteins that mediate cellular activity. The compounds of the subject invention can be used, for example, to inhibit tumor necrosis factor and/or phosphodiesterase IV, The subject invention also concerns methods for treating disease states using the compounds of the invention.

Abstract translation: 本发明涉及可用于治疗疾病状态的通式（i）“IMAGE”的新化合物，例如与介导细胞活性的蛋白质相关的那些状态。 本发明的化合物可用于例如抑制肿瘤坏死因子和/或磷酸二酯酶IV。本发明还涉及使用本发明化合物治疗疾病状态的方法。

公开(公告)号：US5773467A

公开(公告)日：1998-06-30

申请号：US761102

申请日：1996-12-05

Applicant: Hazel Joan Dyke ,  Hannah Jayne Kendall ,  Christopher Lowe ,  John Gary Montana

Inventor： Hazel Joan Dyke ,  Hannah Jayne Kendall ,  Christopher Lowe ,  John Gary Montana

IPC: A61K31/00 ,  A61K31/34 ,  A61K31/343 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P43/00 ,  C07D307/79 ,  C07D307/80 ,  C07D307/86 ,  C07D405/12 ,  C07D405/14 ,  C07D307/78

CPC classification number: C07D307/79 ,  C07D307/80 ,  C07D307/86 ,  C07D405/12 ,  C07D405/14

Abstract: Benzofuran carboxides and sulphonamides have therapeutic utility, e.g. in the treatment of inflammation and asthma, by virtue of their ability to inhibit phosphodiesterases and tumor necrosis factor.

Abstract translation: 苯并呋喃羧酰胺和磺酰胺具有治疗效用，例如 在治疗炎症和哮喘方面，凭借其抑制磷酸二酯酶和肿瘤坏死因子的能力。

公开(公告)号：US20080242655A1

公开(公告)日：2008-10-02

申请号：US11947656

申请日：2007-11-29

Applicant: Simon Charles Goodacre ,  Karen Williams ,  Stephen Price ,  Hazel Joan Dyke ,  John Gary Montana ,  Mark S. Stanley ,  Liang Bao ,  Wendy Lee

Inventor： Simon Charles Goodacre ,  Karen Williams ,  Stephen Price ,  Hazel Joan Dyke ,  John Gary Montana ,  Mark S. Stanley ,  Liang Bao ,  Wendy Lee

IPC: A61K31/397 ,  C07D471/02 ,  A61K31/4439 ,  C07D209/04 ,  A61P35/00 ,  A61P29/00 ,  A61K31/404 ,  C07D237/26 ,  A61K31/5025

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物，更具体地涉及抑制MEK激酶活性的唑烷基化合物。 本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

公开(公告)号：US5972936A

公开(公告)日：1999-10-26

申请号：US859510

申请日：1997-05-20

Applicant: Hazel Joan Dyke ,  John Gary Montana

Inventor： Hazel Joan Dyke ,  John Gary Montana

IPC: C07D307/79 ,  A61K31/00 ,  A61K31/34 ,  A61K31/343 ,  A61K31/345 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P11/14 ,  A61P11/16 ,  A61P17/06 ,  A61P19/10 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P31/10 ,  A61P35/02 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D20060101 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/84 ,  C07D307/86 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D307/83 ,  C07D401/12

CPC classification number: C07D405/12 ,  C07D307/86 ,  C07D405/14 ,  C07D417/14

Abstract: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).