公开(公告)号：US07582630B2

公开(公告)日：2009-09-01

申请号：US10530985

申请日：2003-10-14

申请人： Scott Howard Dickerson ,  Francis Xavier Tavares ,  Huiqiang Zhou

发明人： Scott Howard Dickerson ,  Francis Xavier Tavares ,  Huiqiang Zhou

IPC分类号： A01N43/60 ,  A01N43/58 ,  A61K31/495 ,  A61K31/50 ,  C07D487/00

CPC分类号： C07D487/04 ,  A61K31/5025

摘要： The present invention relates to pyrazaolpyradazine derivatives that inhibit GSK3 (glycogen synthase kinase), pharmaceutical compositions containing these derivatives, and methods for their use in the treatment of disorder characterized by misregulation of GSK3.

摘要翻译： 本发明涉及抑制GSK3（糖原合成酶激酶）的吡唑并吡嗪衍生物，含有这些衍生物的药物组合物及其用于治疗以GSK3失调为特征的病症的方法。

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：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：US07071217B2

公开(公告)日：2006-07-04

申请号：US10362743

申请日：2001-08-23

申请人： Scott Howard Dickerson ,  Robert N Hunter ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael J. Luzzio ,  Edgar Raymond Wood, III

发明人： Scott Howard Dickerson ,  Robert N Hunter ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael J. Luzzio ,  Edgar Raymond Wood, III

IPC分类号： A61K31/44 ,  C07D401/02

CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D417/12

摘要： The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.

摘要翻译： 本发明涉及结构（I）的羟吲哚衍生物，含有它们的组合物及其使用和制造方法。 这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用，特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。 这种疾病状态包括肿瘤生长，再狭窄，动脉粥样硬化，疼痛和血栓形成。特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出Trk家族蛋白酪氨酸激酶抑制，并且其可用于癌症治疗和慢性疼痛适应症 。

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：US5661155A

公开(公告)日：1997-08-26

申请号：US452337

申请日：1995-05-26

申请人： William Pendergast ,  Scott Howard Dickerson

发明人： William Pendergast ,  Scott Howard Dickerson

IPC分类号： A61K31/505 ,  A61K31/00 ,  A61K31/50 ,  A61K31/501 ,  A61K31/517 ,  A61P31/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/02 ,  C07D20060101 ,  C07D239/70 ,  C07D239/88 ,  C07D239/90 ,  C07D239/95 ,  C07D403/12 ,  C07D417/12

CPC分类号： C07D403/12 ,  C07D239/70 ,  C07D239/88 ,  C07D417/12

摘要： The present invention relates to bezoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.

摘要翻译： 本发明涉及含有它们的药物制剂及其在药物中的用途的苯偶氮唑啉胸苷酸合酶抑制剂。