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1. 发明申请

US20130310411A1 NOVEL ACRIDINE DERIVATIVES 审中-公开
标题翻译：新型吡啶衍生物
公开(公告)号：US20130310411A1
公开(公告)日：2013-11-21
申请号：US13876656
申请日：2011-09-29
申请人： Marc Geoffery Hummersone , David Cousin , Mark Frigerio
发明人： Marc Geoffery Hummersone , David Cousin , Mark Frigerio
IPC分类号： C07D495/04 , C07D491/052
CPC分类号： C07D495/04 , C07D491/04 , C07D491/052
摘要： The present invention relates to novel acridine derivatives of formula (I), or pharmaceutically acceptable salts thereof, which are inhibitors of the telomerase enzyme function. These compounds are useful for the treatment cellular proliferation disorders, such as cancer.
摘要翻译：本发明涉及作为端粒酶功能抑制剂的式（I）的新型吖啶衍生物或其药学上可接受的盐。这些化合物可用于治疗细胞增殖紊乱，如癌症。

2. 发明授权

US09024018B2 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds and their use 有权
标题翻译： 3-取代-8-取代-3H-咪唑并[5,1-d] [1,2,3,5]四嗪-4-酮化合物及其用途
公开(公告)号：US09024018B2
公开(公告)日：2015-05-05
申请号：US13376945
申请日：2010-06-23
申请人： Marc Geoffery Hummersone , Malcolm Francis Graham Stevens , David Cousin
发明人： Marc Geoffery Hummersone , Malcolm Francis Graham Stevens , David Cousin
IPC分类号： C07D487/04 , C07D401/14 , C07D403/14 , A61K31/4188 , A61K31/427 , A61P35/00 , C07D417/04 , C07D417/14 , C07D413/04
CPC分类号： C07D487/04 , C07C2601/02
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及3-取代-8-取代-3H-咪唑并[5,1-d] [1,2,3,5]四嗪-4-酮化合物下式，其中-A和-B如本文所定义（在本文中统称为38TM化合物）：本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内，抑制细胞增殖，以及治疗增殖性疾病如癌症等，以及制备这些化合物的方法。

3. 发明授权

US08450479B2 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5-tetrazine-8-carboxylic acid amides and their use 有权
标题翻译： 3-取代-4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5-四嗪-8-羧酸酰胺及其用途
公开(公告)号：US08450479B2
公开(公告)日：2013-05-28
申请号：US12808604
申请日：2008-12-16
申请人： Malcolm Francis Graham Stevens , David Cousin , Sharon Jennings , Andrew James McCarroll , John Gareth Williams , Marc Geoffery Hummersone , Jihong Zhang
发明人： Malcolm Francis Graham Stevens , David Cousin , Sharon Jennings , Andrew James McCarroll , John Gareth Williams , Marc Geoffery Hummersone , Jihong Zhang
IPC分类号： C07D487/04 , C07D519/00 , C07F7/10 , C07F9/141 , A61K31/395 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00 , C07F7/10 , C07F7/1804 , C07F9/6561
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及某些3-取代-4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5]四嗪 - 8-羧酸酰胺（本文统称为3TM化合物）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制细胞增殖以及治疗增殖性疾病例如癌症等的用途，以及制备此类化合物。

4. 发明申请

US20130012706A1 Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines 审中-公开
标题翻译：用于合成4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5]四嗪的方法和中间体
公开(公告)号：US20130012706A1
公开(公告)日：2013-01-10
申请号：US13581874
申请日：2011-02-25
申请人： Marc Geoffery Hummersone , David Cousin
发明人： Marc Geoffery Hummersone , David Cousin
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of general formula (II), or a salt or solvate thereof: wherein A is independently -A1, -A2, -A3, -A4, -A5, -A6, or -A7, wherein: -A1 is independently C5-12heteroaryl, and is optionally substituted; -A2 is independently thioamido or substituted thioamido; -A3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A4 is independently hydroxamic acid or hydroxamate; -A5 is independently carboxamide or substituted carboxamide; -A6 is independently aliphatic C2-6alkenyl, and is optionally substituted; and -A7 is independently carboxy or C1-4alkyl-carboxylate; and its use in the synthesis of temozolomide and analogues thereof.
摘要翻译：本发明提供通式（II）的化合物或其盐或溶剂合物：其中A独立地为-A1，-A2，-A3，-A4，-A5，-A6或-A7，其中：-A1 独立地是C 5-12杂芳基，并且任选被取代; -A2独立地是硫代酰氨基或取代的硫代酰氨基; -A3独立地是亚氨酰胺基，取代的亚氨代酰氨基，N-羟基亚氨基酰胺基或取代的N-羟基亚氨基酰胺基; -A4独立为异羟肟酸或异羟肟酸盐; -A5独立地是甲酰胺或取代的甲酰胺; -A6独立地是脂族C 2-6烯基，并且是任选取代的; -A7独立地是羧基或C1-4烷基 - 羧酸酯; 及其在替莫唑胺及其类似物合成中的应用。

5. 发明申请

US20120083513A1 3-Substituted-8-Substituted-3H-Imidazo[5,1-d][1,2,3,5]tetrazin-4-one Compounds and Their Use 有权
标题翻译： 3-取代的8-取代的3H-咪唑并[5,1-d] [1,2,3,5]四嗪-4-酮化合物及其用途
公开(公告)号：US20120083513A1
公开(公告)日：2012-04-05
申请号：US13376945
申请日：2010-06-23
申请人： Marc Geoffery Hummersone , Malcolm Francis Graham Stevens , David Cousin
发明人： Marc Geoffery Hummersone , Malcolm Francis Graham Stevens , David Cousin
IPC分类号： A61K31/444 , A61K31/4245 , A61K31/427 , A61P35/00 , A61K31/422 , A61K31/423 , A61K31/4188 , C07D487/04 , C12N5/09 , A61K31/428
CPC分类号： C07D487/04 , C07C2601/02
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及3-取代-8-取代-3H-咪唑并[5,1-d] [1,2,3,5]四嗪-4-酮化合物下式，其中-A和-B如本文所定义（在本文中统称为38TM化合物）：本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内，抑制细胞增殖，以及治疗增殖性疾病如癌症等，以及制备这些化合物的方法。

6. 发明申请

US20100286088A1 3-Substituted-4-Oxo-3,4-Dihydro-Imidazo[5,1-d][1,2,3,5-Tetrazine-8-Carboxylic Acid Amides and Their Use 有权
标题翻译： 3-取代-4-氧代-3,4-二氢咪唑并[5,1-d] [1,2,3,5-四嗪-8-羧酸酰胺及其用途
公开(公告)号：US20100286088A1
公开(公告)日：2010-11-11
申请号：US12808604
申请日：2008-12-16
申请人： Malcolm Francis Graham Stevens , David Cousin , Sharon Jennings , Andrew James McCarroll , John Gareth Williams , Marc Geoffery Hummersone , Jihong Zhang
发明人： Malcolm Francis Graham Stevens , David Cousin , Sharon Jennings , Andrew James McCarroll , John Gareth Williams , Marc Geoffery Hummersone , Jihong Zhang
IPC分类号： A61K31/4188 , C07D487/04 , A61K31/4545 , A61K31/5377 , C07F7/10 , A61K31/695 , A61K31/4245 , A61K31/4192 , C07F9/40 , A61K31/683 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00 , C07F7/10 , C07F7/1804 , C07F9/6561
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及某些3-取代-4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5]四嗪 - 8-羧酸酰胺（本文统称为3TM化合物）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制细胞增殖以及治疗增殖性疾病例如癌症等的用途，以及制备此类化合物。

7. 外观设计

USD296034S Shoe upper 失效
公开(公告)号：USD296034S
公开(公告)日：1988-06-07
申请号：US105688
申请日：1987-10-08
申请人： Lawrence Selbiger , David Cousin
设计人： Lawrence Selbiger , David Cousin

8. 发明授权

US5255451A Insert member for use in an athletic shoe 失效
标题翻译：插入成员用于运动鞋
公开(公告)号：US5255451A
公开(公告)日：1993-10-26
申请号：US754157
申请日：1991-09-03
申请人： James K. Tong , David Cousin , Dan Richard
发明人： James K. Tong , David Cousin , Dan Richard
IPC分类号： A43B13/18
CPC分类号： A43B13/181 , A43B3/0057
摘要： An insert member for use in an athletic shoe. The insert member is made of a material which includes a plurality of rows of alternating peaks and valleys.
摘要翻译：用于运动鞋的插入件。插入构件由包括多排交替的峰和谷的材料制成。

9. 外观设计

USD305577S Shoe upper 失效
公开(公告)号：USD305577S
公开(公告)日：1990-01-23
申请号：US304832
申请日：1989-02-01
申请人： Craig L. Feller , David Cousin , Mona McCrea
设计人： Craig L. Feller , David Cousin , Mona McCrea

10. 外观设计

USD295687S Shoe upper 失效
公开(公告)号：USD295687S
公开(公告)日：1988-05-17
申请号：US87750
申请日：1987-08-21
申请人： Lawrence Selbiger , David Cousin
设计人： Lawrence Selbiger , David Cousin

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