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71. 发明授权

US06468981B1 Compositions and methods for targeting pharmaceutically active materials to cells containing androgen receptors 失效
标题翻译：将药物活性物质靶向含有雄激素受体的细胞的组合物和方法
公开(公告)号：US06468981B1
公开(公告)日：2002-10-22
申请号：US08283238
申请日：1994-07-29
申请人： John Anthony Petros , Dennis C. Liotta
发明人： John Anthony Petros , Dennis C. Liotta
IPC分类号： A01N4304
CPC分类号： C07J41/0038 , A61K47/645 , A61K48/00 , A61K51/0493 , A61K51/088 , A61K2123/00
摘要： A water soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to a polycationic material. This molecule may be complexed with therapeutic or diagnostic nucleic acids. Methods of diagnosis and therapy using these compositions are also provided, including gene therapy treatments for prostate cancer.
摘要翻译：提供了一种用于核酸至具有雄激素受体（优选前列腺细胞）的细胞的水溶性递送系统，其包含能够结合所述受体的类固醇部分，所述类固醇部分与聚阳离子材料共价连接。该分子可与治疗或诊断核酸复合。还提供了使用这些组合物的诊断和治疗方法，包括前列腺癌的基因疗法治疗。

72. 发明授权

US5872107A 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：US5872107A
公开(公告)日：1999-02-16
申请号：US792370
申请日：1997-02-03
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
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 in 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，以化合物累积在靶肿瘤中的方式来实现治疗。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。

73. 发明授权

US5827727A Method of resolution of 1,3-oxathiolane nucleoside enantiomers 失效
标题翻译： 1,3-氧硫杂环戊烷核苷对映体的拆分方法
公开(公告)号：US5827727A
公开(公告)日：1998-10-27
申请号：US483653
申请日：1995-06-07
申请人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi , Yung-Chi Cheng
发明人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi , Yung-Chi Cheng
IPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07H19/00 , C07H19/06 , C07H19/10 , C12P17/16 , C12P41/00
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 preferentially 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. In particular, deaminase, PPL, PLE and subtilisn are used to resolve 1,3-oxathiolane nucleoside enantiomers.
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优先催化其中一种对映异构体中的反应的酶的步骤。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。特别地，使用脱氨酶，PPL，PLE和枯草芽孢杆菌来分解1,3-氧硫杂环戊烷核苷对映异构体。

74. 发明授权

US5587514A Diastereoselective synthesis of hydroxyethylene dipeptide isosteres 失效
标题翻译：羟基亚乙基二肽等位基因的非对称选择性合成
公开(公告)号：US5587514A
公开(公告)日：1996-12-24
申请号：US148990
申请日：1993-11-08
申请人： Dennis C. Liotta , Bharat R. Lagu
发明人： Dennis C. Liotta , Bharat R. Lagu
IPC分类号： C07C227/32 , C07C229/22 , C07C231/18 , C07C237/06 , C07C237/20 , C07D307/33 , C07K5/02
CPC分类号： C07D307/33 , C07C227/32 , C07C229/22 , C07C231/18 , C07C237/06 , C07C237/20 , C07K5/0207
摘要： A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
摘要翻译：从α-N，N-二（被保护的） - 氨基（烷基或取代的烷基）甲基酮合成羟基亚乙基二肽等离子体的方法，其可以在工业规模上有效地进行。该方法具有优异的非对映选择性和化学效率，可用于制备各种用于各种用途的羟基亚乙基二肽等位基因，包括作为HIV-1蛋白酶抑制剂和肾素抑制剂。

75. 发明授权

US5204466A Method and compositions for the synthesis of BCH-189 and related compounds 失效
标题翻译：用于合成BCH-189及相关化合物的方法和组合物
公开(公告)号：US5204466A
公开(公告)日：1993-04-20
申请号：US473318
申请日：1990-02-01
申请人： Dennis C. Liotta , Woo-Baeg Choi
发明人： Dennis C. Liotta , 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 BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
摘要翻译：本发明涉及一种从便宜的前体制备BCH-189和BCH-189的各种类似物的方法，可根据需要引入功能。这种合成途径允许这些化合物的生物活性异构体，β-BCH-189和相关化合物的立体选择性制备。此外，可以控制核苷4'位置的化学结构以产生对映异构体富集的β-BCH-189及其类似物。

76. 发明申请

US20140275529A1 SUBUNIT SELECTIVE NMDA RECEPTOR POTENTIATORS FOR THE TREATMENT OF NEUROLOGICAL CONDITIONS 审中-公开
标题翻译：选择性NMDA受体拮抗剂治疗神经病症的潜力
公开(公告)号：US20140275529A1
公开(公告)日：2014-09-18
申请号：US14292957
申请日：2014-06-02
申请人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
发明人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
IPC分类号： C07D217/16 , C07D491/056 , C07D405/06 , C07D413/06 , C07D401/06 , C07D409/06
CPC分类号： C07D217/16 , C07D209/08 , C07D215/22 , C07D239/88 , C07D263/58 , C07D277/34 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D491/056
摘要： Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
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，包括精神分裂症，帕金森病，认知障碍，抑郁症，神经性疼痛，中风，创伤性脑损伤，癫痫和相关的神经系统事件或神经变性。公开了通式A-J的化合物及其药学上可接受的盐，酯，前药或衍生物。

77. 发明授权

US08822462B2 Subunit selective NMDA receptor potentiators for the treatment of neurological conditions 有权
标题翻译：亚基选择性NMDA受体增强剂用于治疗神经病症
公开(公告)号：US08822462B2
公开(公告)日：2014-09-02
申请号：US13146201
申请日：2010-01-28
申请人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
发明人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
IPC分类号： A61K31/535
CPC分类号： C07D217/16 , C07D209/08 , C07D215/22 , C07D239/88 , C07D263/58 , C07D277/34 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D491/056
摘要： Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
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，包括精神分裂症，帕金森病，认知障碍，抑郁症，神经性疼痛，中风，创伤性脑损伤，癫痫和相关的神经系统事件或神经变性。公开了通式A-J的化合物及其药学上可接受的盐，酯，前药或衍生物。

78. 发明授权

US08168583B2 2-fluoronucleosides 有权
标题翻译： 2-氟核苷
公开(公告)号：US08168583B2
公开(公告)日：2012-05-01
申请号：US12510083
申请日：2009-07-27
申请人： Raymond F. Schinazi , Dennis C. Liotta , Chung K. Chu , J. Jeffrey McAtee , Junxing Shi , Yongseok Choi , Kyeong Lee , Joon H. Hong
发明人： Raymond F. Schinazi , Dennis C. Liotta , Chung K. Chu , J. Jeffrey McAtee , Junxing Shi , Yongseok Choi , Kyeong Lee , Joon H. Hong
IPC分类号： A01N61/00 , A61K48/00 , C07H1/00 , C07G3/00
CPC分类号： A61K31/7076 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/708 , C07D405/04 , C07D473/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： 2′-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了可用于治疗乙型肝炎感染，丙型肝炎感染，HIV和异常细胞增殖（包括肿瘤和癌症）的2'-氟 - 核苷化合物。所述化合物具有以下通式：其中碱是嘌呤或嘧啶碱; R 1是OH，H，OR 3，N 3，CN，卤素，CF 3，低级烷基，氨基，低级烷基氨基，二（低级）烷基氨基或烷氧基; R2是H，磷酸盐或稳定的磷酸盐前药; 酰基或其它药学上可接受的苄基，脂质，氨基酸，肽或胆固醇; 烷基，磷酸酯或其它药学上可接受的离去基团; 或其药学上可接受的盐。

79. 发明授权

US08114994B2 2′ and 3′-substituted cyclobutyl nucleoside analogs for the treatment viral infections and abnormal cellular proliferation 有权
标题翻译： 2'和3'-取代的环丁基核苷类似物用于治疗病毒感染和异常细胞增殖
公开(公告)号：US08114994B2
公开(公告)日：2012-02-14
申请号：US12368876
申请日：2009-02-10
申请人： Dennis C. Liotta , Shuli Mao , Michael Hager , Raymond F Schinazi
发明人： Dennis C. Liotta , Shuli Mao , Michael Hager , Raymond F Schinazi
IPC分类号： A61K31/505 , A61K31/513 , A61K31/52 , C07D473/18 , C07D473/34 , C07D239/47 , C07D239/54
CPC分类号： C07H19/06 , C07H19/16
摘要： Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
摘要翻译：提供的环丁基核苷及其用于治疗感染的方法，包括逆转录病毒科（包括HIV），肝炎病毒科（包括HBV）或黄病毒科（包括BVDV和HCV）感染或与异常细胞增殖有关的病症，包括动物，特别是人类。

80. 发明申请

US20120028977A1 Subunit Selective NMDA Receptor Potentiators For The Treatment Of Neurological Conditions 有权
标题翻译：亚基选择性NMDA受体电位器治疗神经病症
公开(公告)号：US20120028977A1
公开(公告)日：2012-02-02
申请号：US13146201
申请日：2010-01-28
申请人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
发明人： Stephen F. Traynelis , Dennis C. Liotta , Rose M. Santangelo , Ethel C. Garnier
IPC分类号： A61K31/472 , C07D405/06 , C07D413/06 , C07D491/056 , C07D239/56 , C07D233/42 , C07D333/68 , C07D409/12 , C07D333/38 , C07D213/75 , C07D261/14 , C07C229/38 , A61K31/4725 , A61K31/5377 , A61K31/4741 , A61P25/18 , A61P25/16 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/28 , A61P25/08 , A61P25/14 , A61P29/00 , A61P19/08 , A61P19/10 , A61P35/00 , C07D217/16
CPC分类号： C07D217/16 , C07D209/08 , C07D215/22 , C07D239/88 , C07D263/58 , C07D277/34 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D491/056
摘要： Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
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，包括精神分裂症，帕金森病，认知障碍，抑郁症，神经性疼痛，中风，创伤性脑损伤，癫痫和相关的神经系统事件或神经变性。公开了通式A-J的化合物及其药学上可接受的盐，酯，前药或衍生物。

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