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31. 发明授权

US5905070A �5--Caboxamido or 5--fluoro!--�2', 3'--unsaturated or 3'--modified!--pyrimidine nucleosides 失效
标题翻译： 5-Carboxamido或5-fluoro-Ä2'，3'-不饱和或3'-修饰的 - 嘧啶核苷
公开(公告)号：US5905070A
公开(公告)日：1999-05-18
申请号：US1084
申请日：1997-12-30
申请人： Raymond F. Schinazi , Dennis C. Liotta
发明人： Raymond F. Schinazi , Dennis C. Liotta
IPC分类号： C07D239/34 , A61K9/20 , A61K31/505 , A61K31/513 , A61K31/522 , A61K31/675 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K38/21 , A61K45/06 , A61P31/12 , A61P31/18 , A61P31/20 , A61P37/04 , C07D239/38 , C07D405/04 , C07H19/06 , A61K38/00
CPC分类号： A61K31/7068 , A61K31/70 , A61K45/06 , C07H19/06
摘要： A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a �5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a �5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
摘要翻译：公开了用于治疗人和其他宿主动物中的HIV和HBV感染的方法和组合物，其包括给予有效量的[5-甲酰氨基或5-氟] -2'，3'-二脱氧-2' ，3'-二脱氢嘧啶核苷或[5-甲酰氨基或5-氟] -3'-修饰的嘧啶核苷或其混合物或药学上可接受的衍生物，包括5'或N4烷基化或酰化衍生物，或其药学上可接受的盐在药学上可接受的载体中。

32. 发明授权

US5892025A Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers 失效
标题翻译： 1,3-氧硫杂环戊烷核苷对映异构体的拆分方法及抗病毒活性
公开(公告)号：US5892025A
公开(公告)日：1999-04-06
申请号：US115780
申请日：1998-07-14
申请人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi
发明人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi
IPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07H19/00 , C07H19/06 , C07H19/10 , A61K31/70 , A61K31/505
CPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07H19/00 , C07H19/06 , C07H19/10
摘要： A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
摘要翻译：一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于在其中一种对映异构体中反应的酶的酶的步骤。核苷对映异构体（ - ） - 2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷是以类似方式复制的有效的抗HIV，HBV和其他病毒的抗病毒剂。

33. 发明授权

US5814639A Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds 失效
标题翻译： 2'-脱氧-5-氟-3'-硫代胞苷及其相关化合物的合成，组合和用途的方法
公开(公告)号：US5814639A
公开(公告)日：1998-09-29
申请号：US17820
申请日：1993-02-16
申请人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi
发明人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi
IPC分类号： A61K31/505 , A61K20060101 , A61K31/00 , A61K31/39 , A61K31/513 , A61K31/695 , A61K31/7064 , A61K31/7068 , A61P31/12 , A61P31/18 , C07D20060101 , C07D239/02 , C07D327/04 , C07D405/04 , C07D411/04 , C07D451/00 , C07F7/18 , C07H19/06 , C07H19/10 , C12P19/38 , C12P41/00
CPC分类号： C07D405/04 , C07D327/04 , C07D411/04 , C07H19/06 , C07H19/10
摘要： The present invention relates to a method of preparing the antiviral compounds 2'-deoxy-5-fluoro-3'thiacytidine (FTC) and various prodrug analogues of FTC from inexpensive precursors with the option of introducing functionality as needed; methods of using these compounds, particularly in the prevention and treatment of AIDS; and the compounds themselves. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds and related compounds.
摘要翻译：本发明涉及一种从便宜的前体制备抗病毒化合物2'-脱氧-5-氟-3'-硫杂胞苷（FTC）和FTC的各种前药类似物的方法，可根据需要引入功能; 使用这些化合物的方法，特别是在预防和治疗艾滋病方面; 和化合物本身。这种合成途径允许这些化合物和相关化合物的生物活性异构体的立体选择性制备。

34. 发明授权

US5602245A One vessel stereoselective glycosylation of purines and pyrimidines 失效
标题翻译：嘌呤和嘧啶的一种血管立体选择性糖基化
公开(公告)号：US5602245A
公开(公告)日：1997-02-11
申请号：US970691
申请日：1992-11-04
申请人： Julie Wurster , Dennis C. Liotta , Jianying Wang , Lawrence J. Wilson
发明人： Julie Wurster , Dennis C. Liotta , Jianying Wang , Lawrence J. Wilson
IPC分类号： C07H19/04 , C07H19/06 , C07H19/16 , C07H1/00 , C07C313/14 , C07D305/10 , C07H19/00
CPC分类号： C07H19/04 , C07H19/06 , C07H19/16
摘要： A process for the preparation of 2',3' dideoxynucleosides, 2'-deoxynucleosides, and 2',3'-dideoxy-2',3'-didehydronucleosides is provided that includes the synchronous addition of a stereoselecting moiety (a directing group) and a protected purine or pyrimidine base to 5-(S)-6-(protected-oxy)-4,5-dihydrofuran in the presence of a Lewis acid. This one vessel reaction eliminates the need to separately prepare and purify a 2'-substituted ribose derivative that in a second step is condensed with a purine or pyrimidine base. The process can be easily modified to increase the stereoselectivity of formation of the .beta.-anomeric nucleoside as necessary.
摘要翻译：提供了制备2'，3'二脱氧核苷，2'-脱氧核苷和2'，3'-二脱氧-2'，3'-二脱氢核苷的方法，包括立体选择部分（导向基团）的同步加入，和受保护的嘌呤或嘧啶碱基与路易斯酸存在下的5-（S）-6-（保护氧基）-4,5-二氢呋喃。这一容器反应消除了分开制备和纯化2'-取代的核糖衍生物的需要，其中第二步与嘌呤或嘧啶碱基缩合。该方法可以容易地修饰，以增加形成β-异构核苷的立体选择性。

35. 发明授权

US5599796A Treatment of urogenital cancer with boron neutron capture therapy 失效
标题翻译：用硼中子捕获治疗泌尿生殖系癌
公开(公告)号：US5599796A
公开(公告)日：1997-02-04
申请号：US334759
申请日：1994-11-04
申请人： Raymond F. Schinazi , Thomas E. Keane , Dennis C. Liotta
发明人： Raymond F. Schinazi , Thomas E. Keane , Dennis C. Liotta
IPC分类号： C12N15/09 , A61K31/69 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7076 , A61K31/7088 , A61K41/00 , A61K48/00 , A61K49/00 , A61K49/08 , A61N5/00 , A61P13/02 , A61P15/00 , A61P31/12 , A61P35/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/04 , C07H23/00 , C12N9/12 , C12N15/10 , C12N15/113 , C12Q1/68 , A61K43/00
CPC分类号： C07H21/00 , A61K41/0095 , A61K49/085 , A61K49/10 , C07H19/06 , C07H19/10 , C07H19/20 , C07H23/00 , C12N15/10 , C12N15/113 , C12N9/1276 , C12Q1/6816 , C12Q1/6827 , C12Q1/6886 , C12N2310/318 , C12N2310/33 , C12N2310/3527
摘要： Methods and compositions for treating urogenital tumors, and particular, cancer of the prostate, bladder, and kidney, with BCNT, are disclosed. Any boron-containing compound that is sufficiently lipophilic to pass through the appropriate urogenital membranes in a quantity high enough to achieve therapy on irradiation with low-energy neutrons can be used. Carboranyl-containing nucleosides and oligonucleotides are particularly suited for use in BNCT of urogenital tumors. Preferred compounds include 5-carboranyl-2'-deoxyuridine (CDU) and 5-o-carboranyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil (CFAU). Nucleosides and oligonucleotides bearing an -O-[(carboran-1-yl)alkyl]phosphate, S-[(carboran-1-yl)alkyl]phosphorothioate, or Se-[(carboran-1-yl)alkyl]phosphoroselenoate in place of the (carboran-1-yl)phosphonate moiety can be used. Oligonucleotides of specific gene sequences that include one or more 3',5'-linking-(carboran-1-yl)phosphonate moieties can also be used in antisense therapy in the selective modification of gene expression. Compounds can be used in urogenital BNCT therapy that contain boron clusters as a means to enhance lipophilicity wherein the boron is not enriched in .sup.10 B, but instead, in the .sup.11 B isotope. The therapy is accomplished by administering the boron-containing compound by any appropriate route, including by intravenous injection, oral delivery or by catheter or other direct means, in such a manner that the compound accumulates in the target tumor. After desired accumulation of the compound in the tumor, the site is irradiated with an effective amount of low energy neutrons.
摘要翻译：公开了用BCNT治疗泌尿生殖肿瘤，特别是前列腺癌，膀胱癌和肾癌的方法和组合物。可以使用任何足够亲油的通过合适的泌尿生殖膜的含硼化合物，其量足够高以实现对低能中子的照射治疗。含有硼烷基的核苷和寡核苷酸特别适用于泌尿生殖器肿瘤的BNCT。优选的化合物包括5-碳硼烷基-2'-脱氧尿苷（CDU）和5-邻硼烷基-1-（2-脱氧-2-氟-β-阿拉伯呋喃糖基）尿嘧啶（CFAU）。具有-O - [（碳硼烷-1-基）烷基]磷酸酯，S - [（碳硼烷-1-基）烷基]硫代磷酸酯或Se - [（碳硼烷-1-基）烷基]亚硒酸酯的核苷和寡核苷酸就位的（碳硼烷-1-基）膦酸酯部分。包括一个或多个3'，5'-连接 - （碳硼烷-1-基）膦酸酯部分的特定基因序列的寡核苷酸也可用于基因表达的选择性修饰中的反义治疗。化合物可用于含有硼簇的泌尿生殖系BNCT治疗，作为增强亲脂性的手段，其中硼不富含10B，而是在11B同位素中。通过任何合适的途径施用含硼化合物，包括通过静脉内注射，口服递送或通过导管或其它直接方式，使化合物累积在靶肿瘤中。在化合物在肿瘤中期望的积聚之后，用有效量的低能中子照射该部位。

36. 发明授权

US5462724A Sensitizing agents for use in boron neutron capture therapy 失效
公开(公告)号：US5462724A
公开(公告)日：1995-10-31
申请号：US380520
申请日：1995-01-30
申请人： Raymond F. Schinazi , Dennis C. Liotta
发明人： Raymond F. Schinazi , Dennis C. Liotta
IPC分类号： A61K31/505 , A61K31/52 , A61K41/00 , C07D411/04 , C07F5/02 , C07F7/18 , C07F9/12 , C07F9/6596 , A61K31/69
CPC分类号： A61K31/70 , A61K31/505 , A61K31/52 , A61K41/0038 , A61K41/0095 , C07D411/04 , C07F5/027 , C07F7/1856 , C07F9/12 , C07F9/6596
摘要： Compounds of formula I and II ##STR1## in which B contains a carboranyl group and one of R.sub.3 and R.sub.4 is a carboranyl group or a boronic acid or ester are useful sensitizing agents for boron neutron capture therapy.

37. 发明授权

US5232837A Method of altering sphingolipid metabolism and detecting fumonisin ingestion and contamination 失效
标题翻译：改变脂质代谢和检测霉菌素摄入和污染的方法
公开(公告)号：US5232837A
公开(公告)日：1993-08-03
申请号：US740426
申请日：1991-08-05
申请人： Alfred H. Merrill, Jr. , Elaine W. Wang , Dennis C. Liotta , Ronald T. Riley
发明人： Alfred H. Merrill, Jr. , Elaine W. Wang , Dennis C. Liotta , Ronald T. Riley
IPC分类号： A61K31/13 , A61K31/22 , A61K31/225 , C07C215/10
CPC分类号： A61K31/225 , A61K31/13 , A61K31/22 , C07C215/10 , Y10S436/815
摘要： This invention provides a method of altering the metabolism of sphingolipids in a cell comprising contacting the cell with a fumonisin, or an analog thereof. The invention also provides a method of detecting the consumption of a fumonisin or a fumonisin analog in a subject comprising (A) detecting, in a sample from the subject, the state of the metabolic pathway of sphingolipids and (B) comparing the state of the metabolic pathway to that of a normal subject, the presence of a change in the state of the metabolic pathway indicating the consumption of a fumonisin or a fumonisin analog. Also provided is a method of detecting the presence of a fumonisin or fumonisin analog contamination in a sample from a food or feed comprising detecting a reaction of the metabolic pathway of sphingolipids, the presence of the reaction indicating the presence of a fumonisin or fumonisin analog contamination. Furthermore, novel fumonisin analogs and compositions comprising fumonisins and fumonisin analogs are provided.
摘要翻译：本发明提供了改变细胞中鞘脂代谢的方法，包括使细胞与伏马毒素或其类似物接触。本发明还提供一种检测受试者中伏马菌素或伏马菌素类似物的消耗的方法，包括（A）在受试者的样品中检测鞘脂代谢途径的状态和（B）比较代谢途径与正常受试者的代谢途径，代谢途径状态的变化表明伏马菌素或伏马菌素类似物的消耗。还提供了检测来自食物或饲料的样品中伏马毒素或伏马菌素类似物污染物的存在的方法，包括检测鞘脂代谢途径的反应，表明存在伏马菌素或伏马菌素类似物污染的反应。此外，提供了包含伏马毒素和伏马菌素类似物的新型伏马菌素类似物和组合物。

38. 发明授权

US09527881B2 Steroid analogues for neuroprotection 有权
标题翻译：用于神经保护的类固醇类似物
公开(公告)号：US09527881B2
公开(公告)日：2016-12-27
申请号：US12918036
申请日：2009-02-26
申请人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
发明人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
IPC分类号： A61K31/58 , A61K31/56 , A61P21/00 , C07G3/00 , C07J21/00 , C07J41/00 , C07J7/00 , C07J9/00
CPC分类号： A61K31/573 , C07J9/00
摘要： Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
摘要翻译：提供的是在类固醇环系统的C3和/或C20位置上被极性取代基官能化的类固醇类似物，其具有改善的水溶性。还提供了包含类固醇类似物的药物组合物和使用新型类固醇类似物在中枢神经系统损伤后治疗和预防患者神经变性的方法。

39. 发明授权

US09079852B2 NMDA receptor antagonists for neuroprotection 有权
标题翻译：用于神经保护的NMDA受体拮抗剂
公开(公告)号：US09079852B2
公开(公告)日：2015-07-14
申请号：US13862647
申请日：2013-04-15
申请人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Scott Myers , Yesim Altas Tahirovic
发明人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Scott Myers , Yesim Altas Tahirovic
IPC分类号： A61K31/421 , A61K31/4166 , A61K31/495 , C07D241/04 , C07D263/18 , C07D233/08 , C07D209/34 , C07C217/20 , C07C235/20 , C07C311/08 , C07D215/227 , C07D233/34 , C07D235/26 , C07D263/58 , C07D295/088 , C07D211/52 , C07D213/74 , C07D233/32
CPC分类号： C07D209/34 , C07C217/20 , C07C235/20 , C07C311/08 , C07D211/52 , C07D213/74 , C07D215/227 , C07D233/32 , C07D233/34 , C07D235/26 , C07D263/58 , C07D295/088
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3−-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(═O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
摘要翻译：提供了治疗或预防与NMDA受体活性相关的病症的化合物，药物组合物和方法，包括神经性疼痛，中风，创伤性脑损伤，癫痫以及相关的神经系统事件或神经变性。化合物为通式I，或其药学上可接受的盐，酯，前药或衍生物：其中：（L）k-Ar1为取代或未取代的单或双环芳基或杂芳基; W是键，烷基或烯基; X是键，NR 1或O，并且每个R 1和R 2独立地是H，烷基，烯基或芳烷基，或者R 1和R 2一起形成5-8元环; R 3 -R 6选自某些具体取代基或羰基; Y是键，O，S，SO，SO 2，CH 2，NH，N（烷基）或NHC（= O）; 并且Z是OH，NR 6 R 7，NR 8 SO 2（烷基），NR 8 C（O）NR 6 R 7，NR 8 C（O）O（烷基），NR 8 - 二氢噻唑或NR 8 - 二氢咪唑，或其中Z可与Ar 2融合形成选定的杂环。

40. 发明授权

US08420680B2 NMDA receptor antagonists for neuroprotection 有权
标题翻译：用于神经保护的NMDA受体拮抗剂
公开(公告)号：US08420680B2
公开(公告)日：2013-04-16
申请号：US12165308
申请日：2008-06-30
申请人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Yesim Altas Tahirovic , Scott J. Myers
发明人： Dennis C. Liotta , James P. Snyder , Stephen F. Traynelis , Lawrence Wilson , Cara Mosley , Raymond J. Dingledine , Yesim Altas Tahirovic , Scott J. Myers
IPC分类号： A61K31/4166 , A61K31/421 , A61K31/495 , C07D241/04 , C07D263/18 , C07D233/08
CPC分类号： C07D209/34 , C07C217/20 , C07C235/20 , C07C311/08 , C07D211/52 , C07D213/74 , C07D215/227 , C07D233/32 , C07D233/34 , C07D235/26 , C07D263/58 , C07D295/088
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3−R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(═O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
摘要翻译：提供了治疗或预防与NMDA受体活性相关的病症的化合物，药物组合物和方法，包括神经性疼痛，中风，创伤性脑损伤，癫痫以及相关的神经系统事件或神经变性。化合物为通式I，或其药学上可接受的盐，酯，前药或衍生物：其中：（L）k-Ar1为取代或未取代的单或双环芳基或杂芳基; W是键，烷基或烯基; X是键，NR 1或O，并且每个R 1和R 2独立地是H，烷基，烯基或芳烷基，或者R 1和R 2一起形成5-8元环; R 3 -R 6选自某些具体取代基或羰基; Y是键，O，S，SO，SO 2，CH 2，NH，N（烷基）或NHC（= O）; 并且Z是OH，NR 6 R 7，NR 8 SO 2（烷基），NR 8 C（O）NR 6 R 7，NR 8 C（O）O（烷基），NR 8 - 二氢噻唑或NR 8 - 二氢咪唑，或其中Z可与Ar 2融合形成选定的杂环。

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