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1. 发明申请

US20110262354A1 CYANINE-CONTAINING COMPOUNDS FOR CANCER IMAGING AND TREATMENT 审中-公开
标题翻译：用于癌症成像和治疗的含氰胺的化合物
公开(公告)号：US20110262354A1
公开(公告)日：2011-10-27
申请号：US12668460
申请日：2008-07-10
申请人： Leland W. K. Chung , Ruoxiang Wang , Haiyen E. Zhau , Lucjan Strekowski , Maged Henary , Gabor Patonay , James J. Krutak , Xiaojian Yang , Guodong Zhu
发明人： Leland W. K. Chung , Ruoxiang Wang , Haiyen E. Zhau , Lucjan Strekowski , Maged Henary , Gabor Patonay , James J. Krutak , Xiaojian Yang , Guodong Zhu
IPC分类号： A61K49/00 , A61P35/00 , C12N5/00 , A61K31/404 , C07D403/08 , C12Q1/02
CPC分类号： A61K49/00 , A61K31/404 , C07D209/10 , C07D209/60 , C07D209/92 , G01N33/5008
摘要： This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.
摘要翻译：本发明一般涉及含花青化合物; 包含含花青化合物的药物组合物; 以及使用含花青素化合物进行癌细胞成像，癌细胞生长抑制，以及检测癌细胞的方法等。与正常细胞相比，本发明的化合物优先被癌细胞吸收。这可以在癌症治疗，诊断，跟踪和成像领域的许多用途。

2. 发明授权

US5304647A Method of preparation of halogenated diazines 失效
标题翻译：卤代二嗪的制备方法
公开(公告)号：US5304647A
公开(公告)日：1994-04-19
申请号：US572676
申请日：1990-08-24
申请人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
发明人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
IPC分类号： C07D237/30 , C07D239/30 , C07D239/78 , C07D409/04 , C07D409/14 , C07D237/12 , C07D239/72
CPC分类号： C07D239/30 , C07D237/30 , C07D239/78 , C07D409/04 , C07D409/14
摘要： A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
摘要翻译：一种制备取代的卤代二氮的方法，其可用作合成新型未取代杂双环化合物的中间体及其产物。该反应包括加入有机锂试剂，随后加成产物脱氢。反应在一个反应容器中进行，而不分离取代的卤代二氢二嗪中间体。反应在中等温度和短时间内进行，这降低了副反应的可能性并提高了产率。此外，后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。该方法简单，高效，产品成品率高。取代的卤代二嗪用作合成含有芳族部分，二嗪和其它具有生物活性的其它芳族部分如噻吩，苯或萘的未稠合的杂双环化合物的中间体。

3. 发明授权

US5304554A 4-[(alkyl or dialkyl)amino]quinolines and their method of preparation 失效
标题翻译： 4 - [（烷基或二烷基）氨基]喹啉及其制备方法
公开(公告)号：US5304554A
公开(公告)日：1994-04-19
申请号：US849790
申请日：1992-03-11
申请人： Lucjan Strekowski , Roman L. Wydra , Steven E. Patterson , Raymond F. Schinazi
发明人： Lucjan Strekowski , Roman L. Wydra , Steven E. Patterson , Raymond F. Schinazi
IPC分类号： C07D215/46 , C07D221/18 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/54 , A61K31/495 , A61K31/50 , A61K31/535
CPC分类号： C07D401/04 , C07D215/46 , C07D221/18 , C07D401/14 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.
摘要翻译：公开了通过2-（三氟甲基）苯胺或其衍生物与烷基乙烯基酮和烷基酮，烷基杂芳基酮或环酮酮缩合制备的新的4 - [（烷基或二烷基）氨基]喹啉，相应的酮亚胺，其被阴离子环化成喹啉。喹啉可用作DNA的嵌入剂，并且还抑制包括HIV在内的逆转录病毒的复制。

4. 发明授权

US4963676A Di-substituted phthalazines 失效
标题翻译：二取代酞嗪
公开(公告)号：US4963676A
公开(公告)日：1990-10-16
申请号：US400502
申请日：1989-08-30
申请人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
发明人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
IPC分类号： C07D237/30 , C07D239/30 , C07D239/78 , C07D409/04 , C07D409/14
CPC分类号： C07D239/30 , C07D237/30 , C07D239/78 , C07D409/04 , C07D409/14
摘要： A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of novel unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
摘要翻译：一种制备取代的卤代二氮的方法，其可用作合成新型未取代杂双环化合物的中间体及其产物。该反应包括加入有机锂试剂，随后加成产物脱氢。反应在一个反应容器中进行，而不分离取代的卤代二氢二嗪中间体。反应在中等温度和短时间内进行，这降低了副反应的可能性并提高了产率。此外，后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。该方法简单，高效，产品成品率高。取代的卤代二嗪用作合成含有芳族部分，二嗪和另外具有生物活性的其它芳族部分如噻吩，苯或萘的新型未稠合的杂双环化合物的中间体。

5. 发明授权

US06479504B1 Antagonism of immunostimulatory CpG-oligonucleotides by 4-aminoquinolines and other weak bases 失效
标题翻译：免疫刺激CpG寡核苷酸由4-氨基喹啉和其他弱碱的拮抗作用
公开(公告)号：US06479504B1
公开(公告)日：2002-11-12
申请号：US09595875
申请日：2000-06-16
申请人： Donald E. Macfarlane , Lucjan Strekowski , Lori Manzel , Fyaz M. D. Ismail , Gordon B. Barlin
发明人： Donald E. Macfarlane , Lucjan Strekowski , Lori Manzel , Fyaz M. D. Ismail , Gordon B. Barlin
IPC分类号： A61K3144
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/5377 , C07D215/42 , C07D215/44 , C07D215/46 , C07D219/12 , C07D401/12 , C07D409/12
摘要： The present invention relates generally to the field of immunology. More particularly it concerns compositions and methods for inhibiting stimulation of the immune system. The compounds and methods comprise compounds that are analogs and derivatives of chloroquine, such as 4-aminoquinolines, and other weak bases. They can be used in preventative and therapeutic treatments of autoimmune diseases and phenomena, transplant rejection such as host-versus-graft disease, and sepsis.
摘要翻译：本发明一般涉及免疫学领域。更具体地，涉及用于抑制免疫系统刺激的组合物和方法。化合物和方法包括氯喹的类似物和衍生物如4-氨基喹啉和其它弱碱的化合物。它们可用于预防和治疗自身免疫性疾病和现象，移植排斥反应如宿主与移植物疾病和败血症。

6. 发明授权

US5800995A Sequencing near infrared and infrared fluorescence labeled DNA for detecting using laser diodes and suitable labels therefor 失效
公开(公告)号：US5800995A
公开(公告)日：1998-09-01
申请号：US706004
申请日：1996-08-30
申请人： Gabor Patonay , Narasimhachari Narayanan , Lucjan Strekowski , Lyle Richard Middendorf , Malgorzata Lipowska
发明人： Gabor Patonay , Narasimhachari Narayanan , Lucjan Strekowski , Lyle Richard Middendorf , Malgorzata Lipowska
IPC分类号： C07D209/12 , C07D209/60 , C09B23/00 , C09B23/01 , C12N15/09 , C12Q1/68 , G01N21/64 , G01N27/447 , G01N33/58 , G01N33/53
CPC分类号： C07D209/60 , C09B23/0066 , C12Q1/6816 , C12Q1/6869 , G01N21/6428 , G01N21/6458 , G01N27/447 , G01N27/44721 , G01N27/44726 , Y10S435/968 , Y10S436/80
摘要： To sequence DNA automatically, DNA marked with far infrared, near infrared, or infrared fluorescent dyes are electrophoresed in a plurality of channels through a gel electrophoresis slab or capillary tubes wherein the DNA samples are resolved in accordance with the size of DNA fragments in the gel electrophoresis slab or capillary tubes into fluorescently marked DNA bands. The separated samples are scanned photoelectrically with a laser diode and a sensor, wherein the laser scans with scanning light at a wavelength within the absorbance spectrum of said fluorescently marked DNA samples and light is sensed at the emission wavelength of the marked DNA.

7. 发明授权

US5571388A Sequencing near infrared and infrared fluorescense labeled DNA for detecting using laser diodes and suitable labels thereof 失效
标题翻译：测量近红外和红外荧光标记的DNA，用于检测激光二极管及其合适的标签
公开(公告)号：US5571388A
公开(公告)日：1996-11-05
申请号：US204627
申请日：1994-03-01
申请人： Gabor Patonay , Narasimhachari Narayanan , Lucjan Strekowski , Lyle R. Middendorf , Malgorzata Lipowska
发明人： Gabor Patonay , Narasimhachari Narayanan , Lucjan Strekowski , Lyle R. Middendorf , Malgorzata Lipowska
IPC分类号： C07D209/12 , C07D209/60 , C09B23/00 , C09B23/01 , C12N15/09 , C12Q1/68 , G01N21/64 , G01N27/447 , G01N33/58 , G01N27/26
CPC分类号： C07D209/60 , C09B23/0066 , C12Q1/6816 , C12Q1/6869 , G01N21/6428 , G01N21/6458 , G01N27/447 , G01N27/44721 , G01N27/44726 , Y10S435/968 , Y10S436/80
摘要： To sequence DNA automatically, DNA marked with far infrared, near infrared, or infrared fluorescent dyes are electrophoresed in a plurality of channels through a gel electrophoresis slab or capillary tubes wherein the DNA samples are resolved in accordance with the size of DNA fragments in the gel electrophoresis slab or capillary tubes into fluorescently marked DNA bands. The separated samples are scanned photoelectrically with a laser diode and a sensor, wherein the laser scans with scanning light at a wavelength within the absorbance spectrum of said fluorescently marked DNA samples and light is sensed at the emission wavelength of the marked DNA.
摘要翻译：为了自动序列DNA，用远红外线，近红外或红外荧光染料标记的DNA通过凝胶电泳板或毛细管在多个通道中进行电泳，其中根据凝胶中DNA片段的大小来分离DNA样品电泳板或毛细管进入荧光标记的DNA条带。分离的样品用激光二极管和传感器进行光电扫描，其中激光扫描具有在所述荧光标记的DNA样品的吸收光谱内的波长的扫描光，并且在标记的DNA的发射波长处感测光。

8. 发明授权

US4929726A Novel diazines and their method of preparation 失效
标题翻译：新型二嗪类及其制备方法
公开(公告)号：US4929726A
公开(公告)日：1990-05-29
申请号：US153998
申请日：1988-02-09
申请人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
发明人： Lucjan Strekowski , Maria Mokrosz , Donald B. Harden
IPC分类号： C07D237/30 , C07D239/30 , C07D239/78 , C07D409/04 , C07D409/14
CPC分类号： C07D239/30 , C07D237/30 , C07D239/78 , C07D409/04 , C07D409/14
摘要： A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.The substituted halogenodiazines are used as intermediates in the synthesis of novel unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.
摘要翻译：一种制备取代的卤代二氮的方法，其可用作合成新型未取代杂双环化合物的中间体及其产物。该反应包括加入有机锂试剂，随后加成产物脱氢。反应在一个反应容器中进行，而不分离取代的卤代二氢二嗪中间体。反应在中等温度和短时间内进行，这降低了副反应的可能性并提高了产率。此外，后处理步骤在两相条件下进行以防止取代的卤代二嗪水解成取代的羟基二嗪。该方法简单，高效，产品成品率高。取代的卤代二嗪用作合成含有芳族部分，二嗪和另外具有生物活性的其它芳族部分如噻吩，苯或萘的新型未稠合的杂双环化合物的中间体。

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