公开(公告)号：US07189712B2

公开(公告)日：2007-03-13

申请号：US10530810

申请日：2003-10-10

申请人： Matthew Lee Brown ,  Mui Cheung ,  Scott Howard Dickerson ,  Cassandra Gauthier ,  Philip Anthony Harris ,  Robert Neil Hunter ,  Gregory Pacofsky ,  Michael Robert Peel ,  Jeffrey Alan Stafford

发明人： Matthew Lee Brown ,  Mui Cheung ,  Scott Howard Dickerson ,  Cassandra Gauthier ,  Philip Anthony Harris ,  Robert Neil Hunter ,  Gregory Pacofsky ,  Michael Robert Peel ,  Jeffrey Alan Stafford

IPC分类号： A61K31/541 ,  A61K31/5355 ,  A61K31/496 ,  A61K31/4525 ,  A61K31/443 ,  A61K31/421 ,  C07D417/10 ,  C07D413/10

CPC分类号： C07D263/48 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

摘要： Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

摘要翻译： 本文描述了可用作VEGFR2，CDK2和CDK4抑制剂的恶唑衍生物。 所述的发明还包括制备这种恶唑衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。

公开(公告)号：US06268391B1

公开(公告)日：2001-07-31

申请号：US09446586

申请日：2000-04-07

申请人： Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  David Kendall Jung ,  Karen Elizabeth Lackey ,  Robert Walton McNutt, Jr. ,  Michael Robert Peel ,  James Marvin Veal

发明人： Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  David Kendall Jung ,  Karen Elizabeth Lackey ,  Robert Walton McNutt, Jr. ,  Michael Robert Peel ,  James Marvin Veal

IPC分类号： A61K31404

CPC分类号： C07D249/08 ,  C07D209/34 ,  C07D231/12 ,  C07D233/56 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04

摘要： Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.

摘要翻译： 通式（I）的化合物，其中：R 1为H或任选地与R 2连接形成选自5至10元芳基，杂芳基或杂环基环的稠环，R 2和R 3独立地为H，HET，芳基， C 12-12脂族基，CN，NO 2，卤素，R 10，-OR 10，-SR 10，-S（O）R 10，-SO 2 R 10，-NR 10 R 11，-NR 11 R 12，-NR 12 COR 11，-NR 12 CO 2 R 11，-NR 12 CONR 11 R 12，-NO 12 SO 2 R 11， NR 12）NHR 11，-COR 11，-CO 2 R 11，-CONR 12 R 11，-SO 2 NR 12 R 11，-OCONR 12 R 11，C（NR 12）NR 12 R 11，R 6和R 7独立地为卤素，CN，NO 2，-CONR 10 R 11，-SO 2 NR 10 R 11，-NR 10 R 11或-OR 11， 其中R 10和R 11如下所定义; R8是OH，NHSO2R12或NHCOCF3; 及其在治疗中的应用，特别是治疗由cRaf1激酶介导的疾病。

公开(公告)号：US07279473B2

公开(公告)日：2007-10-09

申请号：US10499179

申请日：2002-12-11

申请人： Jennifer G. Badiang ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  David Kendall Jung ,  Michael Robert Peel ,  Michael John Reno ,  Tara Renae Rheault ,  Kirk Lawrence Stevens ,  Francis Xavier Tavares ,  James Marvin Veal

发明人： Jennifer G. Badiang ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  David Kendall Jung ,  Michael Robert Peel ,  Michael John Reno ,  Tara Renae Rheault ,  Kirk Lawrence Stevens ,  Francis Xavier Tavares ,  James Marvin Veal

IPC分类号： C07D487/04 ,  A61K31/5025

CPC分类号： C07D487/04

摘要： Fused pyradazine derivatives which are usefule as CDK inhibitors are described herein. The described invention alos includes methods of making such fused pyradazine derivatives as wells as methods of using the same in the treatment of hyperproliferative diseases.

摘要翻译： 本文描述了用作CDK抑制剂的熔融哒嗪衍生物。 所述的本发明包括使这样的融合的哒嗪衍生物作为使用它们的方法用于治疗过度增殖性疾病的方法。

公开(公告)号：US06369086B1

公开(公告)日：2002-04-09

申请号：US09262351

申请日：1999-03-04

申请人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

发明人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

IPC分类号： A61K314439

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D209/40 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of such kinases as well as protecting a patient undergoing chemotherapy from chemotherapy induced alopecia.

摘要翻译： 本发明一般涉及新型取代的羟基吲哚化合物和组合物。 这样的化合物和组合物可用作治疗通过抑制或拮抗蛋白激酶激活的信号通路而减轻的疾病或病症的药理学作用。 特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出蛋白质酪氨酸激酶和蛋白质丝氨酸/苏氨酸激酶抑制，并且其可用于通过抑制这种激酶抑制肿瘤生长以及保护接受化疗的患者 化疗引起秃发。

公开(公告)号：US20120277258A1

公开(公告)日：2012-11-01

申请号：US13545029

申请日：2012-07-10

申请人： Amogh Boloor ,  Mui Cheung ,  Philip Anthony Harris ,  Kevin Hinkle ,  Christopher P. Laudeman ,  Jeffrey Alan Stafford ,  James Marvin Veal

发明人： Amogh Boloor ,  Mui Cheung ,  Philip Anthony Harris ,  Kevin Hinkle ,  Christopher P. Laudeman ,  Jeffrey Alan Stafford ,  James Marvin Veal

IPC分类号： A61K31/506 ,  A61P35/00

CPC分类号： C07D239/30 ,  C07D231/56 ,  C07D235/08 ,  C07D403/12 ,  C07D413/14

摘要： Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

摘要翻译： 本文描述了可用作VEGFR2抑制剂的嘧啶衍生物。 所述的发明还包括制备此类嘧啶衍生物的方法以及使用该嘧啶衍生物的方法来治疗过度增殖性疾病。

公开(公告)号：US07105529B2

公开(公告)日：2006-09-12

申请号：US09999331

申请日：2001-11-30

申请人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

发明人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

IPC分类号： A61K31/505 ,  A61K31/44 ,  A61K31/425

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D209/40 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

公开(公告)号：US06541503B2

公开(公告)日：2003-04-01

申请号：US09924431

申请日：2001-08-08

申请人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

发明人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

IPC分类号： A61K31429

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D209/40 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

公开(公告)号：US06387919B1

公开(公告)日：2002-05-14

申请号：US09486960

申请日：2000-06-06

申请人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

发明人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

IPC分类号： A61K314045

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D209/40 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

摘要翻译： 式（I）化合物：其中X为N，CH，CCF 3或C（C 1-12脂族基）; R 4是磺酸，C 1-12脂族磺酰基，磺酰基-C 1-12脂族基，C 1-12脂族磺酰基-C 1-6脂族基，C 1-6脂族氨基，R 7磺酰基，R 7磺酰基-C 1-12脂族基， R7-氨基磺酰基，R7-氨基磺酰基-C1-12脂族，R7-磺酰氨基，R7-磺酰氨基-C12-12脂族，氨基磺酰基氨基，二-C1-12脂族氨基，二-C1-12脂族氨基羰基，二-C1-12脂族 氨基磺酰基，二-C 1-12脂族氨基，二-C1-12脂族氨基羰基，二C1-12脂族氨基磺酰基-C1-12脂族基，（R8）1-3 - 芳基氨基，（R8）1-3 - 芳基磺酰基，（ R8）1-3-芳基 - 氨基磺酰基，（R8）1-3-芳基 - 磺酰基氨基，Het-氨基，Het-磺酰基，Het-氨基磺酰基，氨基亚氨基氨基或氨基亚氨基磺酰基，R5是氢; 并且其中R 4和R 5任选地连接以形成稠环，包含它们的药物制剂及其在治疗中的用途，特别是用于治疗由CDK2活性介导的疾病，例如由癌症化学疗法或放射治疗引起的脱发。

公开(公告)号：US07163940B2

公开(公告)日：2007-01-16

申请号：US10433881

申请日：2001-11-26

申请人： F. Leslie Boyd ,  Stanley D Chamberlain ,  Mui Cheung ,  Kristjan Gudmundsson ,  Philip Anthony Harris ,  Brian A Johns ,  David Kendall Jung ,  Michael Robert Peel ,  Jennifer G Badiang ,  Connie Jo Sexton

发明人： F. Leslie Boyd ,  Stanley D Chamberlain ,  Mui Cheung ,  Kristjan Gudmundsson ,  Philip Anthony Harris ,  Brian A Johns ,  David Kendall Jung ,  Michael Robert Peel ,  Jennifer G Badiang ,  Connie Jo Sexton

IPC分类号： C07D471/04 ,  A61K31/435 ,  C07D401/04

CPC分类号： C07D471/04

摘要： The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

摘要翻译： 本发明提供式（I）化合物：其中所有变量如本文所定义，含有该化合物的药物组合物，其制备方法及其作为药剂的用途。

公开(公告)号：US07034030B2

公开(公告)日：2006-04-25

申请号：US10473196

申请日：2002-03-20

申请人： Michael John Alberti ,  Stanley D. Chamberlain ,  Mui Cheung ,  Kristjan Gudmundsson ,  Philip Anthony Harris ,  Brian A. Johns ,  David Kendall Jung ,  Michael Robert Peel ,  Jennifer Badiang Stanford

发明人： Michael John Alberti ,  Stanley D. Chamberlain ,  Mui Cheung ,  Kristjan Gudmundsson ,  Philip Anthony Harris ,  Brian A. Johns ,  David Kendall Jung ,  Michael Robert Peel ,  Jennifer Badiang Stanford

IPC分类号： C07D403/04 ,  A61K31/505

CPC分类号： C07D471/04

摘要： The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

摘要翻译： 本发明提供式（I）化合物：其中所有变量如本文所定义，含有该化合物的药物组合物，其制备方法及其作为药剂的用途。