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1. 发明申请

US20080119457A1 Benzene, Pyridine, and Pyridazine Derivatives 审中-公开
标题翻译：苯，吡啶和哒嗪衍生物
公开(公告)号：US20080119457A1
公开(公告)日：2008-05-22
申请号：US11844816
申请日：2007-08-24
申请人： Kenneth He Huang , John Mangette , Thomas Barta , Steven E. Hall , James Veal , Philip Hughes
发明人： Kenneth He Huang , John Mangette , Thomas Barta , Steven E. Hall , James Veal , Philip Hughes
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/501 , C07D413/02 , C07D403/02
CPC分类号： C07D207/02 , C07D209/04 , C07D231/22 , C07D231/38 , C07D231/56 , C07D333/22 , C07D471/04 , C07D487/04 , C07D491/04
摘要： Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein A, Q1, Q2, Q3, R31, and R41 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译：公开了式I的化合物和药学上可接受的盐，其中A，Q 1，Q 2，Q 3，R 31， SUB＆gt;和R 41'如本文所定义。式I化合物可用于治疗与细胞增殖相关的疾病和/或病症，例如癌症，炎症，关节炎，血管生成等。还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

2. 发明申请

US20060035901A1 Methotrexate derivatives useful for treating cancer and arthritis 审中-公开
标题翻译：甲氨喋呤衍生物可用于治疗癌症和关节炎
公开(公告)号：US20060035901A1
公开(公告)日：2006-02-16
申请号：US11186404
申请日：2005-07-21
申请人： Gunnar Hanson , Thomas Barta , James Veal , Roy Ware
发明人： Gunnar Hanson , Thomas Barta , James Veal , Roy Ware
IPC分类号： C07D475/02 , A61K31/525
CPC分类号： C07D487/04 , C07D475/04 , C07D475/08 , G01N33/5011 , G01N2333/9015
摘要： The present invention provides novel derivatives of MTX. The novel derivatives have increased selectivity, inhibit the activity of Her2, EGFR, or B-Raf to a greater degree than MTX, and display greater antiproliferative activity than MTX. Also provided are pharmaceutical compositions containing the novel derivatives, to methods of preparation of such derivatives, to methods of inhibiting the biological activity of polypeptides, methods of inhibiting cell proliferation, and the use of the novel compounds in therapy, particularly for the treatment of neoplastic, hyperproliferative, and immune disorders, including cancer, arthritis, and psoriasis.
摘要翻译：本发明提供MTX的新型衍生物。新型衍生物具有增加的选择性，抑制Her2，EGFR或B-Raf的活性比MTX更大程度，并且显示比MTX更大的抗增殖活性。还提供了含有新衍生物的药物组合物，这些衍生物的制备方法，抑制多肽的生物学活性的方法，抑制细胞增殖的方法，以及新型化合物在治疗中的用途，特别是用于治疗肿瘤，过度增殖和免疫疾病，包括癌症，关节炎和牛皮癣。

3. 发明授权

US07678803B2 Quinazoline derivatives for the treatment of cancer 有权
标题翻译：喹唑啉衍生物用于治疗癌症
公开(公告)号：US07678803B2
公开(公告)日：2010-03-16
申请号：US11844584
申请日：2007-08-24
申请人： Kenneth He Huang , James Veal , Thomas Barta , Emilie D. Smith , Wei Ma , Andy Ommen
发明人： Kenneth He Huang , James Veal , Thomas Barta , Emilie D. Smith , Wei Ma , Andy Ommen
IPC分类号： A61K31/517
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D471/04
摘要： The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I wherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q3 is CR2, X1 is N or CRc, Y is CRc, X2 and X3 are each C(R5)(R6), R7 is O. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer The current invention is also directed toward pharmaceutical compositions comprising compounds of the invention.
摘要翻译：本发明涉及其中Q1是CR1，Q2是N，Q4和Q5各自是CR1，Q3是CR2，X1是N或CRc，Y是CRc，X2和X3各自为C的化合物和药学上可接受的盐（R 5）（R 6），R 7为O.式I的化合物可用于治疗与细胞增殖相关的疾病和/或病症，例如癌症。本发明还涉及包含本发明化合物的药物组合物。

4. 发明申请

US20080032991A1 2, 8-disubstituted Naphthyridine Derivatives 审中-公开
标题翻译： 2,8-二取代的萘啶衍生物
公开(公告)号：US20080032991A1
公开(公告)日：2008-02-07
申请号：US11872471
申请日：2007-10-15
申请人： Gunnar Hanson , Roy Ware , Thomas Barta , He Huang
发明人： Gunnar Hanson , Roy Ware , Thomas Barta , He Huang
IPC分类号： A61K31/4375 , A61K31/4545 , A61K31/496 , A61P19/02 , A61P29/00 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D405/14
摘要： Disclosed are compounds of formula A: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, R3, R21, A1, A2, X, and Z are as defined herein. Compounds of formula A are useful in the treatment of diseases and/or conditions related to cell differentiation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译：公开了式A的化合物及其药学上可接受的盐，其中R 1，R 2，R 2，R 3， R 21，A 1，A 2，X和Z如本文所定义。式A的化合物可用于治疗与细胞分化相关的疾病和/或病症，例如癌症，炎症，关节炎，血管生成等。还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

5. 发明申请

US20070212690A1 Folate Antagonists Having Improved Selectivity 审中-公开
标题翻译：叶酸拮抗剂改善选择性
公开(公告)号：US20070212690A1
公开(公告)日：2007-09-13
申请号：US10577570
申请日：2004-10-28
申请人： Jeffrey Partridge
发明人： Jeffrey Partridge
IPC分类号： C12Q1/68 , C12Q1/26
CPC分类号： C12Q1/527 , C12Q1/25 , G01N33/5008 , G01N33/574 , G01N33/6893 , G01N33/82 , G01N2500/00 , G01N2800/24
摘要： The present invention provides methods for identifying improved folate antagonists. The improved folate antagonists identified by the methods of the invention have increased selectivity. The increased selectivity of the folate antagonists results in a reduced risk of adverse effects following treatment with the improved folate antagonists. The improved folate antagonists are identified based on their reduced binding affinity for at least one enzyme selected from glutathione synthase, pyruvate carboxylase, propionyl-CoA carboxylase, biotin carboxylase, acetyl-CoA carboxylase, and methylcrotonyl-CoA carboxylase. According to the invention, folate antagonists having reduced affinity for at least one enzyme selected from this group of enzymes are selected for the treatment of neoplastic, hyperproliferative, and immune disorders.
摘要翻译：本发明提供用于鉴定改善的叶酸拮抗剂的方法。通过本发明的方法鉴定的改善的叶酸拮抗剂具有增加的选择性。叶酸拮抗剂的增加的选择性导致用改善的叶酸拮抗剂治疗后的不良反应的风险降低。基于对至少一种选自谷胱甘肽合成酶，丙酮酸羧化酶，丙酰-CoA羧化酶，生物素羧化酶，乙酰辅酶A羧化酶和甲基色素-coA羧化酶的酶的结合亲和力降低，鉴定出改良的叶酸拮抗剂。根据本发明，选择具有降低的对选自该组酶的至少一种酶的亲和力的叶酸拮抗剂用于治疗肿瘤，过度增殖和免疫疾病。

6. 发明申请

US20040215009A1 Alkyl-linked nucleotide compositions 失效
标题翻译：烷基连接的核苷酸组合物
公开(公告)号：US20040215009A1
公开(公告)日：2004-10-28
申请号：US10762078
申请日：2004-01-21
申请人： Serenex, Inc.
发明人： Klass P. Hardeman , Steven E. Hall , Roy W. Ware , Lindsay A. Hinkley , Matthew G. Jenks
IPC分类号： C07H021/04 , C12Q001/68
CPC分类号： B01D15/3819 , B01J20/289 , C07H21/04
摘要： Alkyl-linked nucleotide compositions and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.
摘要翻译：提供了烷基连接的核苷酸组合物和包含烷基连接的核苷酸的核苷酸亲和介质。接头通常是可以是3,4,5,6,7,8,9,10或更长碳链的疏水接头。本发明还包括合成烷基连接的核苷酸，核苷酸亲和介质的方法及其用于亲和层析和筛选方法的方法。

7. 发明申请

US20110183977A1 BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES 有权
公开(公告)号：US20110183977A1
公开(公告)日：2011-07-28
申请号：US13081637
申请日：2011-04-07
申请人： Kenneth He Huang , Jeron Eaves , Gunnar J. Hanson , James Veal , Thomas Barta , Lifeng Geng , Lindsay Hinkley
发明人： Kenneth He Huang , Jeron Eaves , Gunnar J. Hanson , James Veal , Thomas Barta , Lifeng Geng , Lindsay Hinkley
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/415 , A61K31/405 , C07D413/12 , C07D401/12 , C07D403/12 , C07D209/04 , A61P31/10 , C07D409/12 , C07D405/12 , A61P29/00 , A61P35/00 , A61P31/00 , A61P19/02 , A61P37/00 , A61P25/00 , A61P9/00 , A61P35/02 , A61P3/00 , A61P11/00
CPC分类号： C07D409/12 , A61K31/404 , A61K31/416 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/00 , A61K45/06 , A61N5/10 , C07D209/08 , C07D209/14 , C07D231/54 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

8. 发明授权

US07371852B2 Alkyl-linked nucleotide compositions 失效
标题翻译：烷基连接的核苷酸组合物
公开(公告)号：US07371852B2
公开(公告)日：2008-05-13
申请号：US10762078
申请日：2004-01-21
申请人： Klass P. Hardeman , Steven E. Hall , Roy W. Ware , Lindsay A. Hinkley , Matthew G. Jenks
发明人： Klass P. Hardeman , Steven E. Hall , Roy W. Ware , Lindsay A. Hinkley , Matthew G. Jenks
IPC分类号： C07H21/00 , G01N33/566 , G01N33/543
CPC分类号： B01D15/3819 , B01J20/289 , C07H21/04
摘要： Alkyl-linked nucleotide non-homogeneous solid supports and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.
摘要翻译：提供了烷基连接的核苷酸非均相固体载体和包含烷基连接的核苷酸的核苷酸亲和介质。接头通常是可以是3,4,5,6,7,8,9,10或更长碳链的疏水接头。本发明还包括合成烷基连接的核苷酸，核苷酸亲和介质的方法及其用于亲和层析和筛选方法的方法。

9. 外观设计

USD563562S1 Gel box for an auto sample feed gel system 有权
标题翻译：用于自动进样凝胶系统的凝胶盒
公开(公告)号：USD563562S1
公开(公告)日：2008-03-04
申请号：US29223479
申请日：2005-02-15
申请人： William Edward Cosselmon , Stephen E. Allen , Robert Patrick Fadden , Jeffrey M. Partridge
设计人： William Edward Cosselmon , Stephen E. Allen , Robert Patrick Fadden , Jeffrey M. Partridge

10. 发明授权

US07282506B2 2,8-disubstituted naphthyridine derivatives 失效
标题翻译： 2,8-二取代的萘啶衍生物
公开(公告)号：US07282506B2
公开(公告)日：2007-10-16
申请号：US11196532
申请日：2005-08-03
申请人： Gunnar J. Hanson , Roy W. Ware, Jr. , Thomas E. Barta , He Huang
发明人： Gunnar J. Hanson , Roy W. Ware, Jr. , Thomas E. Barta , He Huang
IPC分类号： C07D471/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , C07D405/14
摘要： Disclosed are compounds of formula A: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, R3, R21, A1, A2, X, and Z are as defined herein. Compounds of formula A are useful in the treatment of diseases and/or conditions related to cell differentiation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译：公开了式A的化合物及其药学上可接受的盐，其中R 1，R 2，R 2，R 3， R 21，A 1，A 2，X和Z如本文所定义。式A的化合物可用于治疗与细胞分化相关的疾病和/或病症，例如癌症，炎症，关节炎，血管生成等。还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

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