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51. 发明申请

US20040220133A1 Composition and method for inhibiting platelet aggregation 失效
标题翻译：抑制血小板聚集的组合物和方法
公开(公告)号：US20040220133A1
公开(公告)日：2004-11-04
申请号：US10814007
申请日：2004-03-31
发明人： Jose L. Boyer , James G. Douglass III , Sammy R. Shaver , Krzysztof Bednarski , Benjamin R. Yerxa , Gillian M. Olins
IPC分类号： C07H019/04 , A61K031/7076 , A61K031/7072
CPC分类号： C07H19/20 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , C07H19/04 , C07H19/10 , C07H19/207 , C07H21/00
摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5null-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5null-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5null-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.
摘要翻译：本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。该方法还涉及治疗血栓形成的方法。该方法包括向受试者施用包含治疗有效量的P2Y12受体拮抗剂化合物的药物组合物，其中所述量有效结合血小板上的P2Y12受体并抑制ADP诱导的血小板聚集。可用于本发明的P2Y12受体拮抗剂化合物包括单核苷5'-单磷酸酯，单核苷多聚磷酸酯和通式I的二核苷多聚磷酸酯或其盐。本发明还提供了单核苷5'-单磷酸酯，单核苷多磷酸盐和二核苷多磷酸的新型化合物。本发明还提供了包含单核苷5'-单磷酸酯，单核苷多磷酸盐或二核苷多磷酸盐的药物制剂。

52. 发明授权

US06750340B2 Bisphosphonate conjugates and methods of making and using the same 有权
标题翻译：双膦酸盐缀合物及其制备和使用方法
公开(公告)号：US06750340B2
公开(公告)日：2004-06-15
申请号：US09731598
申请日：2000-12-07
申请人： Nelly Padioukova , Sergey Mikhailov , H. B. F. Dixon , Grigorii Tzeitline
发明人： Nelly Padioukova , Sergey Mikhailov , H. B. F. Dixon , Grigorii Tzeitline
IPC分类号： C07F96512
CPC分类号： C07H19/10 , A61K31/675 , A61K47/54 , A61K47/548 , A61K51/0497 , C07F9/58 , C07H19/207
摘要： The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
摘要翻译：本发明涉及特定的二膦酸盐化合物，特别是双膦酸盐缀合物，其可用于治疗围绕骨和骨相关疾病如骨癌和骨质疏松症的软组织。

53. 发明授权

US06723321B2 Autoinducer synthase modulating compounds and uses thereof 失效
标题翻译：自动诱导剂合成酶调节化合物及其用途
公开(公告)号：US06723321B2
公开(公告)日：2004-04-20
申请号：US09227488
申请日：1999-01-06
申请人： E. Peter Greenberg , John E. Cronan, Jr. , Bryce V. Plapp , Matthew R. Parsek
发明人： E. Peter Greenberg , John E. Cronan, Jr. , Bryce V. Plapp , Matthew R. Parsek
IPC分类号： A61K3900
CPC分类号： C07H19/16 , A61K31/7076 , C07H19/207 , C12Q1/25 , Y02A50/473 , Y10S424/832
摘要： Provided are compositions and methods useful for modulating the activity of autoinducer synthase catalysts. A method for identifing modulators of the autoinducer synthesis reaction is also provided. Such modulators are useful for controlling bacterial growth and can be used for therapeutic treatment of bacterial infections particularly in immunocompromised subjects. They are also useful in treating disease states associated with autoinducer synthesis and biofilm development.
摘要翻译：提供可用于调节自动诱导合成酶催化剂活性的组合物和方法。还提供了用于鉴定自动诱导剂合成反应的调节剂的方法。这样的调节剂可用于控制细菌生长，并且可用于细菌感染的治疗性治疗，特别是在免疫受损的受试者中。它们也可用于治疗与自身诱导剂合成和生物膜发育相关的疾病状态。

54. 发明申请

US20030144499A1 Photocleavable protecting groups and methods for their use 失效
标题翻译：可透光保护组及其使用方法
公开(公告)号：US20030144499A1
公开(公告)日：2003-07-31
申请号：US10348917
申请日：2003-01-22
申请人： Affymetrix, Inc.
发明人： Glenn H. McGall , Ngo Q. Nam , Richard P. Rava
IPC分类号： C07H021/04 , C07H019/16 , C07H019/06 , C07H019/067 , C07H019/073 , C07H019/09
CPC分类号： C07H21/00 , B01J2219/00432 , C07B2200/11 , C07H19/10 , C07H19/20 , C07H19/207 , C07K1/061 , C40B40/04 , C40B50/14 , C40B60/14 , G01N33/54353 , Y02P20/55
摘要： Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula ArnullC(R1)(R2)nullOnullC(O)null wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to ArnullC(R1)(R2)nullOnullC(O)null via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1 and R2 are H, X is not linked to ArnullC(R1)(R2)nullOnullC(O)null via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the nullPYMOCnull protecting group, pyrenylmethyloxycarbonyl, where Ar is pyrenyl and R1 and R2 are H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
摘要翻译：提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。保护基具有通式Ar-C（R 1）（R 2）-O-C（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族基团或其杂原子衍生物; R 1和R 2独立地为H，任选取代的烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族化合物，或前述的乙烯衍生物; X是离去基团，经由杂原子连接到Ar-C（R 1）（R 2）-O-C（O） - 或固体载体上的化学片段; 条件是当Ar为1-芘基且R 1和R 2为H时，X不能通过氮原子与Ar-C（R 1）（R 2）-O-C（O） - 连接。优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar，R 1和R 2上的取代基是给电子基团的实施方案。特别优选的保护基是“PYMOC”保护基，芘基甲氧基羰基，其中Ar是芘基，R 1和R 2是H.还提供了一种从组分分子在载体上形成多种化合物的方法，每种化合物占据使用上述保护的化合物分离预定区域的载体。

55. 发明授权

US06323187B1 Therapeutic dinucleotide and derivatives 失效
标题翻译：治疗二核苷酸和衍生物
公开(公告)号：US06323187B1
公开(公告)日：2001-11-27
申请号：US09316571
申请日：1999-05-21
申请人： Benjamin R. Yerxa , William Pendergast , Janet L. Rideout , Maryse Picher , Richard C. Boucher, Jr. , M. Jackson Stutts
发明人： Benjamin R. Yerxa , William Pendergast , Janet L. Rideout , Maryse Picher , Richard C. Boucher, Jr. , M. Jackson Stutts
IPC分类号： A01N4304
CPC分类号： A61K31/7048 , A61K31/70 , C07H19/207 , C07H21/00
摘要： The present invention relates to P1-(cytidine 5′-)-P-(uridine 5′-)tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media.
摘要翻译：本发明涉及P2Y2和/或P2Y4嘌呤能受体的高度稳定和选择性激动剂的P1-（胞苷5' - ） - （ - 尿苷5' - ）四磷酸及其盐，酯和酰胺及其制剂。本发明的化合物可用于治疗慢性阻塞性肺疾病如慢性支气管炎，原发性纤毛运动障碍，囊性纤维化，以及预防由于不动的肺炎，以及诱导痰及其咳痰。此外，由于它们具有清除保留的粘液分泌物和刺激睫状肌搏动频率的一般能力，本发明的化合物也可用于治疗鼻窦炎和中耳炎。

56. 发明申请

US20010041346A1 METHOD FOR ASSAYING COMPOUNDS AFFECTING SMOOTH MUSCLE CONTRACTILE STATE 审中-公开
标题翻译：测定影响平滑肌肉收缩状态的化合物的方法
公开(公告)号：US20010041346A1
公开(公告)日：2001-11-15
申请号：US09354354
申请日：1999-07-14
发明人： MICHAEL E. MENDELSOHN
IPC分类号： G01N033/573
CPC分类号： C12N9/1205 , C07H19/207 , C12N9/16 , G01N33/6887 , G01N2500/00
摘要： The invention provides a method for assaying compounds that affect smooth muscle cell function by determining the interaction between a cyclic GMP-dependent protein kinase, and a myosin phosphatase myosin-binding subunit.
摘要翻译：本发明提供了通过测定环状GMP依赖性蛋白激酶和肌球蛋白磷酸酶肌球蛋白结合亚基之间的相互作用来测定影响平滑肌细胞功能的化合物的方法。

57. 发明授权

US6022963A Synthesis of oligonucleotide arrays using photocleavable protecting groups 失效
标题翻译：使用可光致发光的保护基合成寡核苷酸阵列
公开(公告)号：US6022963A
公开(公告)日：2000-02-08
申请号：US630148
申请日：1996-04-10
申请人： Glenn H. McGall , Ngo Quoc Nam
发明人： Glenn H. McGall , Ngo Quoc Nam
IPC分类号： C07B61/00 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00
CPC分类号： C07H19/10 , C07H19/20 , C07H19/207 , C40B50/14 , C07B2200/11 , C40B40/04 , Y02P20/55 , Y10S436/807
摘要： Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar--C(R.sub.1)(R.sub.2)--O--C(O)-- wherein:Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof;R.sub.1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; andX is a leaving group, a chemical fragment linked to Ar--C(R.sub.1)(R.sub.2)--O--C(O)-- via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R.sub.1 =R.sub.2 =H, X is not linked to Ar--C(R.sub.1)(R.sub.2)--O--C(O)-- via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R.sub.1 and R.sub.2 are electron donating groups. A particularly preferred protecting group is the "PYMOC" protecting group, pyrenylmethyloxycarbonyl, where Ar=pyrenyl and R.sub.1 =R.sub.2 =H.Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
摘要翻译：提供了新的化合物，其可用作化学合成中的连接基团，优选在寡核苷酸和多肽的固相合成中。这些化合物通常是光不稳定的并且包括可以通过光解去除以揭示反应性基团的保护基团。保护基具有通式Ar-C（R 1）（R 2）-O-C（O） - ，其中：Ar是任选取代的稠合多环芳基或杂芳族基团或其杂原子衍生物; R 1和R 2独立地为H，任选取代的烷基，烯基或炔基，任选取代的芳基或任选取代的杂芳族化合物，或前述的乙烯衍生物; X是离去基团，经由杂原子连接到Ar-C（R 1）（R 2）-O-C（O） - 或固体载体上的化学片段; 条件是当Ar是1-芘基且R 1 = R 2 = H时，X不经由氮原子与Ar-C（R 1）（R 2）-O-C（O） - 连接。优选的实施方案是其中Ar是稠合多环芳烃并且其中Ar，R 1和R 2上的取代基是给电子基团的实施方案。特别优选的保护基是“PYMOC”保护基，芘基甲氧基羰基，其中Ar =芘基，并且R 1 = R 2 = H。还提供了使用上述保护的化合物从成分分子形成多个化合物在载体上的方法，每种化合物占据支持体的单独的预定区域。

58. 发明授权

US5480982A Crystalline potassium salt of thinonicotinamide adenine dinucleotide phosphate 失效
标题翻译：薄烟酰胺腺嘌呤二核苷酸磷酸盐的结晶钾盐
公开(公告)号：US5480982A
公开(公告)日：1996-01-02
申请号：US945989
申请日：1992-11-05
申请人： Kouji Sugita , Tetsuo Kitahara , Masatsugu Nonobe , Tsuyosi Fujita
发明人： Kouji Sugita , Tetsuo Kitahara , Masatsugu Nonobe , Tsuyosi Fujita
IPC分类号： C07B63/00 , C07H19/207 , C07H21/02
CPC分类号： C07H19/207
摘要： The present invention relates to a novel crystalline thio-NADP potassium salt, which is produced by preparing thionicotinamide adenine dinucleotide phosphate (thio-NADP) into the potassium salt thereof and thereafter crystallizing the salt. Conventionally known non-crystalline thio-NADP sodium salt has a strong hygroscopic property to deliquesce on contact with air, of which the storage is therefore difficult. The crystalline thio-NADP potassium salt of the present invention has no hygroscopic property so that it does not deliquesce on contact with air, which can be used as research reagents, diagnostic agents and the like for a long period of time and which can be stored for a long period of time.
摘要翻译： PCT No.PCT / JP92 / 00260 Sec。 371日期：1992年11月5日 102（e）日期1992年11月5日PCT 1991年3月5日PCT公布。出版物WO92 / 本发明涉及一种新的结晶硫代NADP钾盐，其通过将硫酰 - 鸟嘌呤二核苷酸磷酸（硫代NADP）制备到其钾盐中，然后使该盐结晶而制备。常规已知的非结晶硫代NADP钠盐与空气接触时具有很强的吸湿性，因此难以储存。本发明的结晶硫代NADP钾盐没有吸湿性，因此在与空气接触时不会潮解，可长时间用作研究试剂，诊断剂等，并且可以储存很长一段时间。

59. 发明授权

US4661448A Method for producing reduced-form coenzyme 失效
标题翻译：生成还原型辅酶的方法
公开(公告)号：US4661448A
公开(公告)日：1987-04-28
申请号：US711213
申请日：1985-03-13
申请人： Sadaji Yokoyama , Shinichiro Suye
发明人： Sadaji Yokoyama , Shinichiro Suye
IPC分类号： C07H19/207 , C12P19/36 , C12Q1/00 , C12N9/04 , C12Q1/32
CPC分类号： C07H19/207 , C12P19/36 , C12Q1/008
摘要： A method for producing a reduced-form coenzyme by reacting malic acid with either nicotinamide adenine dinucleotide or nicotinamide adenine dinucleotide phosphate in the presence of malate dehydrogenase to obtain the corresponding reduced product. The reaction is preferably carried out under reduced pressure, while removing carbon dioxide, formed during the reaction, from the reaction system.
摘要翻译：在苹果酸脱氢酶的存在下，通过苹果酸与烟酰胺腺嘌呤二核苷酸或烟酰胺腺嘌呤二核苷酸磷酸酯反应来制备还原型辅酶的方法，以获得相应的还原产物。反应优选在减压下进行，同时从反应体系中除去反应期间形成的二氧化碳。

60. 发明授权

US4255566A Flavin adenine dinucleotide derivatives and labeled conjugates prepared therefrom 失效
标题翻译：黄素腺嘌呤二核苷酸衍生物和由其制备的标记的缀合物
公开(公告)号：US4255566A
公开(公告)日：1981-03-10
申请号：US122292
申请日：1980-02-19
申请人： Robert J. Carrico , Richard D. Johnson
发明人： Robert J. Carrico , Richard D. Johnson
IPC分类号： C07H19/207 , C07H21/00 , G01N33/535 , G01N33/94 , C07H19/20 , C07H17/00
CPC分类号： C07H21/00 , C07H19/207 , G01N33/535 , G01N33/94
摘要： A flavin adenine dinucleotide (FAD) derivative of the formula: ##STR1## wherein n is an integer from 2 through 10, and preferably is 6. The derivatives are intermediates in the preparation of FAD-labeled conjugates useful as reagents in specific binding assays for determining ligands (e.g., antigens and haptens) in liquid media such as serum. Also provided are certain FAD-labeled conjugates, particularly an FAD-theophylline conjugate.
摘要翻译：下式的黄素腺嘌呤二核苷酸（FAD）衍生物：其中n是2-10的整数，优选为6.所述衍生物是制备用作特异性结合测定中的试剂的FAD标记的缀合物的中间体在液体培养基如血清中测定配体（例如抗原和半抗原）。还提供某些FAD标记的缀合物，特别是FAD-茶碱缀合物。

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