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1. 发明授权

US07501425B1 Bicyclic pyrimidines and bicyclic 3,4-dihydropyprimidines as inhibitors of cellular proliferation 失效
标题翻译：双环嘧啶和双环3,4-二氢孕蛋黄作为细胞增殖的抑制剂
公开(公告)号：US07501425B1
公开(公告)日：2009-03-10
申请号：US09623737
申请日：1999-05-10
申请人： Ellen Myra Dobrusin , James Marino Hamby , James Bernard Kramer , Mel Conrad Schroeder , Howard Daniel Hollis Showalter , Peter Toogood , Susanne A. Trumpp-Kallmeyer
发明人： Ellen Myra Dobrusin , James Marino Hamby , James Bernard Kramer , Mel Conrad Schroeder , Howard Daniel Hollis Showalter , Peter Toogood , Susanne A. Trumpp-Kallmeyer
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides substituted pyrimido-pyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. The invention compounds have Formula I: where W is NH, S, SO, or SO2, R1 includes alkyl, cycloalkyl, phenyl, substituted phenyl, heteroaryl and substituted heteroaryl; R2 includes alkyl, cycloalkyl, phenyl and substituted phenyl; R3 includes alkyl and aryl such as phenyl and substituted phenyl; R8 and R9 include hydrogen and alkyl, and the pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical formulations comprising a compound of Formula I together with a pharmaceutically acceptable carrier, diluent, or excipient therefor, and a method for treating angiogenesis using said compounds.
摘要翻译：本发明提供了可用于治疗细胞增殖性疾病如癌症和再狭窄以及血管生成和动脉粥样硬化的取代嘧啶嘧啶。本发明化合物具有式I：其中W是NH，S，SO或SO 2，R 1包括烷基，环烷基，苯基，取代的苯基，杂芳基和取代的杂芳基; R2包括烷基，环烷基，苯基和取代的苯基; R3包括烷基和芳基，例如苯基和取代的苯基; R8和R9包括氢和烷基，及其药学上可接受的盐。本发明还提供包含式I化合物及其药学上可接受的载体，稀释剂或赋形剂的药物制剂，以及使用所述化合物治疗血管发生的方法。

2. 发明授权

US06218388B1 Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation 失效
标题翻译：苯并咪唑用于抑制蛋白酪氨酸激酶介导的细胞增殖
公开(公告)号：US06218388B1
公开(公告)日：2001-04-17
申请号：US09459011
申请日：1999-12-10
申请人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
发明人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
IPC分类号： A61K315377
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/4439 , A61K31/5377
摘要： Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
摘要翻译：以下式I的苯并咪唑是蛋白酪氨酸激酶的抑制剂，并且可用于治疗细胞增殖。该化合物特别可用于治疗癌症，动脉粥样硬化，再狭窄和牛皮癣。

3. 发明授权

US5990146A Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation 失效
标题翻译：苯并咪唑用于抑制蛋白酪氨酸激酶介导的细胞增殖
公开(公告)号：US5990146A
公开(公告)日：1999-11-23
申请号：US135470
申请日：1998-08-17
申请人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
发明人： Diane Harris Boschelli , William Alexander Denny , Annette Marian Doherty , James Marino Hamby , Sonya Shah Khatana , James Bernard Kramer , Brian Desmond Palmer , Howard Daniel Hollis Showalter
IPC分类号： A61K31/4184 , A61K31/4439 , A61K31/5377 , C07D235/06 , A61K31/415 , C07D235/08
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/4439 , A61K31/5377
摘要： Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
摘要翻译：以下式I的苯并咪唑是蛋白酪氨酸激酶的抑制剂，可用于治疗细胞增殖。该化合物特别可用于治疗癌症，动脉粥样硬化，再狭窄和牛皮癣。

4. 发明授权

US07169778B2 Pteridinones as kinase inhibitors 失效
标题翻译：蝶啶酮作为激酶抑制剂
公开(公告)号：US07169778B2
公开(公告)日：2007-01-30
申请号：US10070530
申请日：2000-06-21
申请人： William Alexander Denny , Gordon William Rewcastle , Ellen Dobrusin , James Bernard Kramer , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Peter Laurence Toogood
发明人： William Alexander Denny , Gordon William Rewcastle , Ellen Dobrusin , James Bernard Kramer , Dennis Joseph McNamara , Howard Daniel Hollis Showalter , Peter Laurence Toogood
IPC分类号： A61K31/535 , C07D475/00
CPC分类号： C07D475/00
摘要： Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).
摘要翻译：公开了式（Ia），（Ib），（Ic），（Id）的化合物，其中：W是NH，S，SO或SO 2; R 2是（未）取代的芳基，（未）取代的杂芳基或（取代的）取代的碳环或杂环; Q是氢或低级烷基; R 4和R 6相同或不同，表示氢，卤素，低级烷基，低级烷氧基，（未）取代的芳基，（未）取代的杂芳基，（un ）取代的芳基烷基或（未）取代的杂芳基烷基; 和R 8是氢，低级烷基或含有3-7个成员的（未）取代的碳环，其中至多两个成员任选是选自氧和氮的杂原子; 或（R 8）是（un）取代的芳基，（未）取代的杂芳基，（未）取代的芳基烷基或（未）取代的杂芳基烷基。这些化合物可用于治疗细胞增殖性疾病，如癌症和再狭窄。这些化合物是细胞周期蛋白依赖性激酶（cdks）和生长因子介导的激酶的有效抑制剂。本发明还提供了治疗细胞增殖性疾病的方法。本发明还提供含有式（I）化合物的药学上可接受的组合物。

5. 发明授权

US06683183B2 Pyridotriazines and pyridopyridazines 失效
标题翻译：吡啶三嗪和吡啶并哒嗪
公开(公告)号：US06683183B2
公开(公告)日：2004-01-27
申请号：US09970107
申请日：2001-10-03
申请人： James Bernard Kramer , Howard Daniel Hollis Showalter
发明人： James Bernard Kramer , Howard Daniel Hollis Showalter
IPC分类号： C07D48704
CPC分类号： C07D471/04
摘要： This invention relates to bicyclic heterocycles that inhibit cyclin-dependent kinase or tyrosine kinase enzymes, or both, and as such are useful to treat cell proliferative disorders such as angiogenesis, atherosclerosis, restenosis, and cancer as well as immunological disorders such as asthma, rheumatoid arthritis, autoimmune diabetes, and graft rejection associated with transplant surgery in mammals.
摘要翻译：本发明涉及抑制细胞周期蛋白依赖性激酶或酪氨酸激酶或二者的双环杂环，因此可用于治疗细胞增殖性疾病如血管生成，动脉粥样硬化，再狭窄和癌症以及免疫学疾病如哮喘，类风湿病关节炎，自身免疫性糖尿病和与哺乳动物移植手术相关的移植物排斥反应。

6. 发明授权

US07022711B2 2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones 失效
标题翻译： 2-（4-吡啶基）氨基-6-二烷氧基苯基 - 吡啶并[2,3-d]嘧啶-7-酮
公开(公告)号：US07022711B2
公开(公告)日：2006-04-04
申请号：US10343847
申请日：2001-07-20
申请人： James Marino Hamby , Sylvester Klutchko , James Bernard Kramer
发明人： James Marino Hamby , Sylvester Klutchko , James Bernard Kramer
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , A61P9/10 , A61P3/10
CPC分类号： C07D471/04
摘要： This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis.
摘要翻译：本发明提供式（I）的抗血管生成化合物，其可用于治疗由不受控制的细胞增殖如癌症，动脉粥样硬化，类风湿性关节炎和牛皮癣引起的疾病。

7. 发明授权

US08450326B2 Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases 有权
公开(公告)号：US08450326B2
公开(公告)日：2013-05-28
申请号：US12564582
申请日：2009-09-22
申请人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
发明人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
IPC分类号： A61K31/44 , C07D401/04 , C07D239/42 , C07D239/02
摘要： Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).

8. 发明授权

US08536185B2 Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases 有权
公开(公告)号：US08536185B2
公开(公告)日：2013-09-17
申请号：US12564582
申请日：2009-09-22
申请人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
发明人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
IPC分类号： A61K31/44 , C07D401/04 , C07D239/42 , C07D239/02
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D413/04 , C07D417/04 , C07D417/14
摘要： Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).

9. 发明申请

US20100075990A1 MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES 有权
标题翻译：多中心化合物作为H-PGDS的抑制剂及其用于治疗PROSTAGLANDIN D2介导的疾病
公开(公告)号：US20100075990A1
公开(公告)日：2010-03-25
申请号：US12564582
申请日：2009-09-22
申请人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
发明人： Gregory W. Endres , Pil Heui Lee , Kirk Lang Olson , James Bernard Kramer , Fred Lawrence Ciske , Stephen Douglas Barrett
IPC分类号： A61K31/495 , C07D401/04 , C07D239/02 , A61K31/44 , A61P37/04
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D413/04 , C07D417/04 , C07D417/14
摘要： Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
摘要翻译：多杂芳基化合物，它们的制备方法，包含这些化合物的药物组合物及其在预防和治疗前列腺素D2介导的疾病和可通过抑制造血前列腺素D合成酶（H-PGDS）调节的病症）中的药物用途。

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