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1. 发明授权

US5869623A Boronic compound complexing reagents and complexes 失效
标题翻译：硼化合物络合剂和配合物
公开(公告)号：US5869623A
公开(公告)日：1999-02-09
申请号：US956204
申请日：1997-10-22
申请人： Mark L. Stolowitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
发明人： Mark L. Stolowitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
IPC分类号： C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/44 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/02 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, intermediate reagents of those reagents, and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene group with an electronegative moiety; and BAS is a biologically active species.
摘要翻译：公开了硼化合物络合试剂，那些试剂的中间试剂和合成这些试剂的方法。在本文所述的进一步反应后，可以使用这些试剂，包括通式II所示的试剂，与硼酸化合物如苯基硼酸或其衍生物复合。通式II在一个实施方案中，基团Z包括长度为至多约6碳当量的饱和或不饱和链的间隔基，至少约6至18个碳当量长度的无支链饱和或不饱和链一个中间体酰胺或二硫化物部分，和长度为约3至12个碳当量的聚乙二醇链; 基团R2是具有电负性部分的烷基和亚甲基之一; 而BAS是一种生物活性物种。

2. 发明授权

US5847192A Boronic compound complexing reagents and complexes 失效
标题翻译：硼化合物络合剂和配合物
公开(公告)号：US5847192A
公开(公告)日：1998-12-08
申请号：US689341
申请日：1996-08-05
申请人： Mark L. Stolowitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
发明人： Mark L. Stolowitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
IPC分类号： C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/44 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/02 , C07F5/04 , C07K5/02 , G01N33/543 , C07C233/50 , C07C233/46
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1##
摘要翻译：公开了硼化合物络合试剂和合成这些试剂的方法。在本文所述的进一步反应后，可以使用这些试剂，包括通式I和通式II所示的试剂，与硼酸化合物如苯基硼酸或其衍生物复合。一般公式I 通用二级

3. 发明授权

US5859210A Boronic compound complexing reagents and complexes 失效
标题翻译：硼化合物络合剂和配合物
公开(公告)号：US5859210A
公开(公告)日：1999-01-12
申请号：US956195
申请日：1997-10-22
申请人： Mark L. Stowolitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
发明人： Mark L. Stowolitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
IPC分类号： C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/44 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/02 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula IV and General Formula VI. In one embodiment, the reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.
摘要翻译：硼化合物络合剂，硼化合物络合物，以及合成这些试剂和络合物的方法。这些试剂和络合物包括通式IV和通式VI所示的那些试剂和络合物。在一个实施方案中，通式IV的试剂可用于与硼化合物如通式VI所示的络合物形成络合物。通式IV通式VI在一个实施方案中，基团Z包含选自长度最多约6碳当量的饱和或不饱和链的间隔基，约6至18的无支链饱和或不饱和链长度的碳当量与中间体酰胺或二硫化物部分中的至少一种和长度为约3至12碳当量的聚乙二醇链; 基团R3选自具有电负性取代基的H，烷基和亚甲基或亚乙基部分中的一个; BAS和BAS *是生物活性物种。

4. 发明授权

US5744627A Boronic compound complexing reagents and complexes 失效
标题翻译：硼化合物络合剂和配合物
公开(公告)号：US5744627A
公开(公告)日：1998-04-28
申请号：US691929
申请日：1996-08-05
申请人： Mark L. Stowolitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
发明人： Mark L. Stowolitz , Robert J. Kaiser , Kevin P. Lund , Steven M. Torkelson
IPC分类号： C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/44 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/02 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula III, General Formula IV, and General Formula VI. In one embodiment, the reagents of General Formula III may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula IV. The reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1##
摘要翻译：硼化合物络合剂，硼化合物络合物，以及合成这些试剂和络合物的方法。这些试剂和络合物包括通式III，通式IV和通式VI所示的试剂和络合物。在一个实施方案中，通式III的试剂可用于在与生物活性物质（BAS）缩合后生产通式IV的试剂。通式IV的试剂可用于与硼化合物如通式VI所示的络合物形成络合物。方程式IV 通用VI

5. 发明授权

US08778625B2 2-(2-hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors 有权
标题翻译： 2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-甲脒衍生物作为因子VIIA抑制剂
公开(公告)号：US08778625B2
公开(公告)日：2014-07-15
申请号：US13607402
申请日：2012-09-07
申请人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
发明人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
IPC分类号： C12Q1/56
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译：本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。还公开了制备这些抑制剂的方法。

6. 发明申请

US20080242644A1 Factor Viia Inhibitor 审中-公开
标题翻译：因子Viia抑制剂
公开(公告)号：US20080242644A1
公开(公告)日：2008-10-02
申请号：US11597334
申请日：2005-06-02
申请人： Steven M. Torkelson , Tomas Vojkovsky
发明人： Steven M. Torkelson , Tomas Vojkovsky
IPC分类号： A61K31/4184 , C07D235/04 , A61K31/4436 , A61K31/60 , A61P7/02
CPC分类号： C07D235/18
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译：本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。还公开了制备这些抑制剂的方法。

7. 发明授权

US08299110B2 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors 有权
标题翻译： 2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-甲脒衍生物作为因子VIIa抑制剂
公开(公告)号：US08299110B2
公开(公告)日：2012-10-30
申请号：US13100107
申请日：2011-05-03
申请人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
发明人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
IPC分类号： A61K31/4184
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译：本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。还公开了制备这些抑制剂的方法。

8. 发明授权

US5955612A Fluorescent labeling reagents 失效
标题翻译：荧光标记试剂
公开(公告)号：US5955612A
公开(公告)日：1999-09-21
申请号：US862746
申请日：1997-05-23
申请人： Clarence N. Ahlem , Steven M. Torkelson
发明人： Clarence N. Ahlem , Steven M. Torkelson
IPC分类号： G01N33/533 , C07D221/22
CPC分类号： G01N33/533
摘要： A class of sulforhodamine labeling reagents capable of binding with a biomolecular species to produce a conjugate with fluorescent properties. The sulforhodamine labeling reagents have the structure: ##STR1## The group X is selected from an alkyl, an olefin, a monocyclic aliphatic saturated hydrocarbon, an aryl, or nothing at all. The group Y is selected from an amide, a substituted amide, or nothing at all. The group Z is selected from a monocyclic aliphatic hydrocarbon, an aryl, or an alkyl, as defined with respect to group X, a polyethylene glycol chain of the general form (CH.sub.2 CH.sub.2 O).sub.n, or nothing at all. The alkyl or polyethylene glycol chain may further have inert intermediate amide, ether, or disulfide functionalities. The group X, group Y, and group Z cannot all be nothing at all or non-existent. The group R is an electrophilic moiety suitable for conjugation of the fluorescent labeling reagent with a biomolecular species. Also disclosed is a method of making the reagents.
摘要翻译：能够与生物分子物质结合以产生具有荧光性质的共轭物的一类磺酰罗丹明标记试剂。磺酰罗丹明标记试剂具有以下结构：基团X选自烷基，烯烃，单环脂族饱和烃，芳基或根本没有。基团Y选自酰胺，取代的酰胺或根本没有。基团Z选自关于基团X所定义的单环脂族烃，芳基或烷基，一般形式（CH 2 CH 2 O）n的聚乙二醇链，根本没有。烷基或聚乙二醇链还可以具有惰性中间体酰胺，醚或二硫化物官能团。 X组，Y组和Z组不能全部完全不存在或不存在。基团R是适于将荧光标记试剂与生物分子物质缀合的亲电子部分。还公开了制备试剂的方法。

9. 发明申请

US20110269806A1 2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS 有权
标题翻译：作为因子VIIA抑制剂的2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-羧酰胺衍生物
公开(公告)号：US20110269806A1
公开(公告)日：2011-11-03
申请号：US13100107
申请日：2011-05-03
申请人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
发明人： Aleksandr Kolesnikov , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
IPC分类号： A61K31/4184 , A61P7/00
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译：本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。还公开了制备这些抑制剂的方法。

10. 发明申请

US20090054432A1 2-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors 审中-公开
标题翻译： 2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-甲脒衍生物作为因子VIIA抑制剂
公开(公告)号：US20090054432A1
公开(公告)日：2009-02-26
申请号：US12255540
申请日：2008-10-21
申请人： Aleksandr KOLESNIKOV , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
发明人： Aleksandr KOLESNIKOV , Roopa Rai , William Dvorak Shrader , Steven M. Torkelson , Kieron E. Wesson , Wendy B. Young
IPC分类号： A61K31/5377 , A61K31/4184 , A61K31/4439 , A61P35/00 , A61K31/41 , A61K31/454
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
摘要翻译：本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。还公开了制备这些抑制剂的方法。

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