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1. 发明申请

US20100137319A1 PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH 审中-公开
标题翻译：吡咯烷酮化合物有效地作为激酶抑制剂和治疗与激素相关的条件的方法
公开(公告)号：US20100137319A1
公开(公告)日：2010-06-03
申请号：US12701405
申请日：2010-02-05
申请人： Harold Mastalerz , Dolatral M. Vyas , George L. Trainor , Ashvinikumar V. Gavai
发明人： Harold Mastalerz , Dolatral M. Vyas , George L. Trainor , Ashvinikumar V. Gavai
IPC分类号： A61K31/53 , C07D487/04 , A61P35/00 , A61P37/08 , A61P11/06 , A61P31/10 , A61P31/12 , A61P19/08 , A61P25/28 , A61P25/00 , A61P3/00
CPC分类号： C07D487/04
摘要： The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
摘要翻译：本发明涉及至少一种吡咯并三嗪衍生物，至少一种包含至少一种吡咯并三嗪衍生物的药物组合物和至少一种使用至少一种吡咯并三嗪衍生物以治疗至少一种激酶相关病症的方法。

2. 发明授权

US5625081A Fluorescent dye intermediates 失效
标题翻译：荧光染料中间体
公开(公告)号：US5625081A
公开(公告)日：1997-04-29
申请号：US181284
申请日：1994-01-13
申请人： George L. Trainor
发明人： George L. Trainor
IPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/68 , G01N27/447 , C07D311/82
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/65121 , C07F9/65586 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6869 , G01N27/44721 , G01N27/44726
摘要： Intermediates for fluorescent dyes based on 9-carboxyethyl-6-hydroxy-3-oxo-3H-xanthene which are useful as reporters for reporter-labeled DNA fragments are described. The intermediates are protected fluorescent dyes bearing acyloxy groups at the 3 and 9 positions and an alkoxy group at the 9 position. Deprotection of the protected fluorescent dye by treatment with aqueous ammonia regenerates free dye.
摘要翻译：描述了基于9-羧基乙基-6-羟基-3-氧代-3H-呫吨的荧光染料的中间体，其可用作报告物标记的DNA片段的报道。中间体是在3和9位上带有酰氧基的保护的荧光染料和9位的烷氧基。通过用氨水处理来保护荧光染料的脱保护再生游离染料。

3. 发明授权

US5470967A Oligonucleotide analogs with sulfamate linkages 失效
标题翻译：具有氨基磺酸酯键的寡核苷酸类似物
公开(公告)号：US5470967A
公开(公告)日：1995-11-28
申请号：US507693
申请日：1990-04-10
申请人： Edward M. Huie , George L. Trainor
发明人： Edward M. Huie , George L. Trainor
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61K31/7125 , A61K48/00 , A61P31/12 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04 , C12Q1/68
CPC分类号： C07H21/00
摘要： Oligonucleotides possessing at least one sulfamate or sulfamide internucleotides linkages. These compounds can be used as specific hybridization probes to detect complementary nucleic acid sequences.
摘要翻译：具有至少一个氨基磺酸盐或磺酰胺核苷酸键的寡核苷酸。这些化合物可以用作特异性杂交探针以检测互补核酸序列。

4. 发明授权

US5306618A Method systems and reagents for DNA sequencing 失效
标题翻译：用于DNA测序的方法系统和试剂
公开(公告)号：US5306618A
公开(公告)日：1994-04-26
申请号：US821569
申请日：1992-01-16
申请人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr. , Frank W. Hobbs, Jr. , George L. Trainor
发明人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr. , Frank W. Hobbs, Jr. , George L. Trainor
IPC分类号： C07D311/82 , C07D311/84 , C07D311/86 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04 , C07D487/04 , C07F9/6512 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C09B11/28 , C09K11/06 , C12N15/09 , C12Q1/68 , G01N27/447 , G01N33/50 , G01N33/58
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/65121 , C07F9/65586 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6869 , G01N27/44721 , G01N27/44726 , Y10S435/808 , Y10S435/968 , Y10S436/805 , Y10T436/13
摘要： A DNA sequencing system and method are described to detect the presence of radiant energy emitted from different excited reporter dye-labeled species (DNA fragments) following separation in time and/or space, and the identity of the species which emit radiant energy closely spaced in wavelength. Functions of the emitted energy are obtained which vary over the wavelengths of the closely spaced spectra in different senses and the functions ratioed, whereby the ratio is indicative of the identity of the DNA fragments.The emitting portion of the reporter-labeled DNA fragment is preferably one of a family of fluorescent dyes based on 9-carboxyethyl-6-hydroxy-3-oxo-3H-xanthene. These xanthene dyes are covalently attached to the DNA fragments through the carboxylic acid functionality, preferably via an amide linkage. The dyes may be protected by including an alkoxy group at the 9-position. A spacer may be inserted between the dye and the amine. The fluorescent dye preferably is attached to the DNA chain terminators and provides many advantages. Thus only DNA sequencing fragments resulting from bona fide termination events will carry a reporter. The DNA sequencing may also be labeled using the xanthene dyes which have general utility as fluorescent labels. Also acyclonucleoside triphosphates are described as being useful as chain terminators in DNA sequencing using a modification of the Sanger method.
摘要翻译：描述了DNA测序系统和方法以检测在时间和/或空间分离之后从不同激发的报道染料标记物种（DNA片段）发射的辐射能的存在，以及发射辐射能的物质的身份波长。获得发射能量的功能，其在不同感官中的紧密间隔的光谱的波长上变化，并且功能的比例，其中该比率指示DNA片段的身份。报道分子标记的DNA片段的发射部分优选为基于9-羧基乙基-6-羟基-3-氧代-3H-呫吨的荧光染料族之一。这些呫吨染料通过羧酸官能团共价连接到DNA片段上，优选通过酰胺键连接。可以通过在9位包括烷氧基来保护染料。可以在染料和胺之间插入间隔物。荧光染料优选连接到DNA链终止剂上并提供许多优点。因此，只有真正终止事件导致的DNA测序片段才会携带记者。 DNA测序也可以使用具有通用作为荧光标记的呫吨染料进行标记。也称为二环磷酸核苷三磷酸可用作DNA测序中的连锁终止子，使用Sanger方法的修饰。

5. 发明授权

US07045540B2 Selective estrogen receptor modulators 有权
标题翻译：选择性雌激素受体调节剂
公开(公告)号：US07045540B2
公开(公告)日：2006-05-16
申请号：US11152888
申请日：2005-06-15
申请人： Robert F. Kaltenbach , Simon P. Robinson , George L. Trainor
发明人： Robert F. Kaltenbach , Simon P. Robinson , George L. Trainor
IPC分类号： A61K31/31 , C07D257/04
CPC分类号： C07D257/04 , C07C51/487 , C07C57/50 , C07C59/54 , C07C59/72 , C07C69/618 , C07C69/734 , C07C255/34 , C07C311/51 , C07C2601/10 , C07C2602/10 , C07C2602/12 , C07D277/80 , C07D311/58 , C07D333/34
摘要： The present invention provides, inter alia, triphenylethylene derivatives, such as, 5-{2-[4-(1,2-Diphenyl-but-1-enyl)-phenyl]-vinyl}-1H-tetrazole, as selective estrogen receptor modulators. Also provided are methods for treating estrogen stimulated diseases in mammals including, but not limited to, for example, breast, uterine, ovarian, prostate and colon cancer; osteoporosis; endometriosis; uterine fibroid; Alzheimer's disease; macular degeneration; urinary incontinence; and type II diabetes, as well as, pharmaceutical compositions comprising at least one compound of the present invention.
摘要翻译：本发明特别提供三苯基乙烯衍生物，例如5- {2- [4-（1,2-二苯基 - 丁-1-烯基） - 苯基] - 乙烯基} -1H-四唑，作为选择性雌激素受体调制器还提供了用于治疗哺乳动物中雌激素刺激的疾病的方法，包括但不限于例如乳腺癌，子宫癌，卵巢癌，前列腺癌和结肠癌; 骨质疏松症子宫内膜异位症子宫肌瘤阿尔茨海默氏病; 黄斑变性; 尿失禁和II型糖尿病，以及包含至少一种本发明化合物的药物组合物。

6. 发明授权

US06927224B2 Selective estrogen receptor modulators 有权
标题翻译：选择性雌激素受体调节剂
公开(公告)号：US06927224B2
公开(公告)日：2005-08-09
申请号：US10216253
申请日：2002-08-09
申请人： Robert F. Kaltenbach , Simon P. Robinson , George L. Trainor
发明人： Robert F. Kaltenbach , Simon P. Robinson , George L. Trainor
IPC分类号： C07D295/08 , A61K31/085 , A61K31/18 , A61K31/192 , A61K31/195 , A61K31/24 , A61K31/27 , A61K31/277 , A61K31/352 , A61K31/381 , A61K31/429 , A61K31/4453 , A61P1/00 , A61P3/10 , A61P9/00 , A61P13/00 , A61P13/08 , A61P15/00 , A61P19/10 , A61P25/28 , A61P35/00 , A61P43/00 , C07C51/487 , C07C57/50 , C07C59/54 , C07C59/72 , C07C69/618 , C07C69/734 , C07C255/34 , C07C311/51 , C07D257/04 , C07D277/80 , C07D311/58 , C07D333/34 , C07C311/00
CPC分类号： C07D257/04 , C07C51/487 , C07C57/50 , C07C59/54 , C07C59/72 , C07C69/618 , C07C69/734 , C07C255/34 , C07C311/51 , C07C2601/10 , C07C2602/10 , C07C2602/12 , C07D277/80 , C07D311/58 , C07D333/34
摘要： The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.
摘要翻译：本发明特别提供三苯基乙烯衍生物，例如3- {4- [6-（3-甲氧基 - 苯基）-8,9-二氢-7H-苯并环庚烯-5-基] - 苯基} - 丙烯酸，作为选择性雌激素受体调节剂。还提供了用于治疗和/或预防哺乳动物包括乳腺，子宫，卵巢，前列腺和结肠癌，骨质疏松症，心血管疾病和良性增殖性疾病的哺乳动物中雌激素刺激性疾病的方法，以及本发明化合物的药物组合物发明。

7. 发明授权

US5558991A DNA sequencing method using acyclonucleoside triphosphates 失效
标题翻译：使用三环磷酸核苷三磷酸的DNA测序方法
公开(公告)号：US5558991A
公开(公告)日：1996-09-24
申请号：US192915
申请日：1994-02-07
申请人： George L. Trainor
发明人： George L. Trainor
IPC分类号： C07D311/82 , C07D311/84 , C07D311/86 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04 , C07D487/04 , C07F9/6512 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C09B11/28 , C09K11/06 , C12N15/09 , C12Q1/68 , G01N27/447 , G01N33/50 , G01N33/58
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/65121 , C07F9/65586 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6869 , G01N27/44721 , G01N27/44726 , Y10S435/808 , Y10S435/968 , Y10S436/805 , Y10T436/13
摘要： Acyclonucleoside triphosphates are described as being useful as chain terminators in DNA sequencing using a modification of the Sanger method.
摘要翻译：亚克隆核苷三磷酸被描述为可用作DNA测序中的连锁终止子，使用Sanger方法的修饰。

8. 发明授权

US5332666A Method, system and reagents for DNA sequencing 失效
标题翻译：用于DNA测序的方法，系统和试剂
公开(公告)号：US5332666A
公开(公告)日：1994-07-26
申请号：US780347
申请日：1991-10-22
申请人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr. , Frank W. Hobbs, Jr. , George L. Trainor
发明人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr. , Frank W. Hobbs, Jr. , George L. Trainor
IPC分类号： C07D311/82 , C07D311/84 , C07D311/86 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04 , C07D487/04 , C07F9/6512 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/14 , C07H19/20 , C07H21/00 , C09B11/28 , C09K11/06 , C12N15/09 , C12Q1/68 , G01N27/447 , G01N33/50 , G01N33/58 , C12P19/34
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/65121 , C07F9/65586 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6869 , G01N27/44721 , G01N27/44726 , Y10S435/808 , Y10S435/968 , Y10S436/805 , Y10T436/13
摘要： A DNA sequencing system and method are described to detect the presence of radiant energy emitted from different excited reporter dye-labeled species (DNA fragments) following separation in time and/or space, and the identity of the species which emit radiant energy closely spaced in wavelength. Functions of the emitted energy are obtained which vary over the wavelengths of the closely spaced spectra in different senses and the functions ratioed, whereby the ratio is indicative of the identity of the DNA fragments. The emitting portion of the reporter-labeled DNA fragment is preferably one of a family of fluorescent dyes based on 9-carboxyethyl-6-hydroxy-3-oxo-3H-xanthene. These xanthene dyes are covalently attached to the DNA fragments through the carboxylic acid functionality, preferably via an amide linkage. The dyes may be protected by including an alkoxy group at the 9-position. A spacer may be inserted between the dye and the amine. The fluorescent dye preferably is attached to the DNA chain terminators and provides many advantages. Thus only DNA sequencing fragments resulting from bona fide termination events will carry a reporter. The DNA sequencing may also be labeled using the xanthene dyes which have general utility as fluorescent labels. Also acyclonucleoside triphosphates are described as being useful as chain terminators in DNA sequencing using a modification of the Sanger method.
摘要翻译：描述了DNA测序系统和方法以检测在时间和/或空间分离之后从不同激发的报道染料标记物种（DNA片段）发射的辐射能的存在，以及发射辐射能的物质的身份波长。获得发射能量的功能，其在不同感官中的紧密间隔的光谱的波长上变化，并且功能的比例，其中该比率指示DNA片段的身份。报道分子标记的DNA片段的发射部分优选为基于9-羧基乙基-6-羟基-3-氧代-3H-呫吨的荧光染料族之一。这些呫吨染料通过羧酸官能团共价连接到DNA片段上，优选通过酰胺键连接。可以通过在9位包括烷氧基来保护染料。可以在染料和胺之间插入间隔物。荧光染料优选连接到DNA链终止剂上并提供许多优点。因此，只有真正终止事件导致的DNA测序片段才会携带记者。 DNA测序也可以使用具有通用作为荧光标记的呫吨染料进行标记。也称为二环磷酸核苷三磷酸可用作DNA测序中的连锁终止子，使用Sanger方法的修饰。

9. 发明授权

US5276143A Dideoxyfructonucleosides and deoxyfructonucleotides 失效
标题翻译：脱氧果糖核苷和脱氧果糖核苷酸
公开(公告)号：US5276143A
公开(公告)日：1994-01-04
申请号：US631567
申请日：1990-12-21
申请人： Subramaniam Sabesan , George L. Trainor
发明人： Subramaniam Sabesan , George L. Trainor
IPC分类号： C07H19/04 , C07H19/06 , C07H19/10 , C07H21/00 , C07H19/073 , C07H19/14 , C07H19/207
CPC分类号： C07H19/04 , C07H19/06 , C07H19/10 , C07H21/00
摘要： Disclosed are deoxyfructonucleotides and dideoxyfructonucleotides which may be used as propagators and terminators in DNA extension reactions.
摘要翻译：公开了可用作DNA延伸反应中的传播子和终止子的脱氧核糖核苷酸和二脱氧呋喃糖基核苷酸。

10. 发明授权

US5242796A Method, system and reagents for DNA sequencing 失效
标题翻译：用于DNA测序的方法，系统和试剂
公开(公告)号：US5242796A
公开(公告)日：1993-09-07
申请号：US780346
申请日：1991-10-22
申请人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr , Frank W. Hobbs, Jr. , George L. Trainor
发明人： James M. Prober , Rudy J. Dam , Charles W. Robertson, Jr , Frank W. Hobbs, Jr. , George L. Trainor
IPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/6512 , C07F9/6558 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/68 , G01N27/447
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/65121 , C07F9/65586 , C07F9/6561 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6869 , G01N27/44721 , G01N27/44726
摘要： A DNA sequencing system and method are described to detect the presence of radiant energy emitted from different excited reporter dye-labeled species (DNA fragments) following separation in time and/or space, and the identity of the species which emit radiant energy closely spaced in wavelength. Functions of the emitted energy are obtained which vary over the wavelengths of the closely spaced spectra in different senses and the functions ratioed, whereby the ratio is indicative of the identity of the DNA fragments.The emitting portion of the reporter-labeled DNA fragment is preferably one of a family of fluorescent dyes based on 9-carboxyethyl-6-hydroxy-3-oxo-3 H-xanthene. These xanthene dyes are covalently attached to the DNA fragments through the carboxylic acid functionality, preferably via an amide linkage. The dyes may be protected by including an alkoxy group at the 9-position. A spacer may be inserted between the dye and the amine. The fluorescent dye preferably is attached to the DNA chain terminators and provides many advantages. Thus only DNA sequencing fragments resulting from bona fide termination events will carry a reporter. The DNA sequencing may also be labeled using the xanthene dyes which have general utility as fluorescent labels. Also acyclonucleoside triphosphates are described as being useful as chain terminators in DNA sequencing using a modification of the Sanger method.
摘要翻译：描述了DNA测序系统和方法以检测在时间和/或空间分离之后从不同激发的报道染料标记物种（DNA片段）发射的辐射能的存在，以及发射辐射能的物质的身份波长。获得发射能量的功能，其在不同感官中的紧密间隔的光谱的波长上变化，并且功能的比例，其中该比率指示DNA片段的身份。报道分子标记的DNA片段的发射部分优选为基于9-羧基乙基-6-羟基-3-氧代-3H-呫吨的荧光染料族之一。这些呫吨染料通过羧酸官能团共价连接到DNA片段上，优选通过酰胺键连接。可以通过在9位包括烷氧基来保护染料。可以在染料和胺之间插入间隔物。荧光染料优选连接到DNA链终止剂上并提供许多优点。因此，只有真正终止事件导致的DNA测序片段才会携带记者。 DNA测序也可以使用具有通用作为荧光标记的呫吨染料进行标记。也称为二环磷酸核苷三磷酸可用作DNA测序中的连锁终止子，使用Sanger方法的修饰。

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