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71. 发明申请

US20150359813A1 EFFECTIVE TREATMENT OF ESOPHOGEAL ADENOCARCINOMA USING TRICIRIBINE AND RELATED COMPOUNDS 有权
公开(公告)号：US20150359813A1
公开(公告)日：2015-12-17
申请号：US14832400
申请日：2015-08-21
申请人： University of South Florida
发明人： Jin Q. CHENG
IPC分类号： A61K31/7064 , G01N33/574
CPC分类号： A61K31/7064 , A61K9/0019 , A61K31/70 , A61K31/7042 , A61K31/7052 , C07H19/23 , G01N33/57407 , G01N2333/912
摘要： The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat esophogeal adenocarcinoma by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.

72. 发明授权

US09180138B2 2′-fluoronucleosides 有权
标题翻译： 2'-核糖核苷
公开(公告)号：US09180138B2
公开(公告)日：2015-11-10
申请号：US13437676
申请日：2012-04-02
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 , A61K31/708 , C07D405/04 , C07D473/00 , C07H19/06 , C07H19/10 , C07H19/16 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , 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。

73. 发明授权

US09096632B2 Modulator of activity of adenylate cyclase 有权
标题翻译：腺苷酸环化酶的活性调节剂
公开(公告)号：US09096632B2
公开(公告)日：2015-08-04
申请号：US13880346
申请日：2011-10-20
申请人： Yoshihiro Ishikawa , Satoshi Okumura , Yujiro Hoshino , Seiichi Inoue
发明人： Yoshihiro Ishikawa , Satoshi Okumura , Yujiro Hoshino , Seiichi Inoue
IPC分类号： A01N43/04 , A61K31/70 , C07H19/06 , A61K31/7064 , A61K31/7056 , A61K31/706 , A61K31/7052 , A61K31/7042 , A61K31/7076 , C07H19/19 , A23L1/30
CPC分类号： C07H19/06 , A23L33/10 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7076 , C07H19/19
摘要： The present invention provides a novel compound capable of inhibiting cardiac adenylyl cyclase.The present invention relates to a compound represented by the following formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof: where R1, R2 and R3 each independently represent a hydrogen atom or an acyl group having an acidic or basic substituent, provided that all of R1, R2 and R3 are not simultaneously a hydrogen atom. The present invention also provides a modulator of adenylyl cyclase activity, a pharmaceutical composition and a food composition, all of which comprise the above-described compound or a pharmaceutically acceptable salt, ester or solvate thereof.
摘要翻译：本发明提供能够抑制心脏腺苷酸环化酶的新化合物。本发明涉及由下式（I）表示的化合物或其药学上可接受的盐，酯或溶剂合物：其中R1，R2和R3各自独立地表示氢原子或具有酸性或碱性取代基的酰基， R1，R2和R3的全部不同时为氢原子。本发明还提供腺苷酸环化酶活性的调节剂，药物组合物和食品组合物，它们都包含上述化合物或其药学上可接受的盐，酯或溶剂合物。

74. 发明授权

US09067964B2 Complex and method for enhancing nuclear delivery 有权
标题翻译：复杂和增强核运送的方法
公开(公告)号：US09067964B2
公开(公告)日：2015-06-30
申请号：US13140070
申请日：2009-12-17
申请人： Edvard Smith , Pedro Moreno , Roger Strömberg , Malgorzata Wenska
发明人： Edvard Smith , Pedro Moreno , Roger Strömberg , Malgorzata Wenska
IPC分类号： A01N43/04 , A61K31/70 , C07H19/167 , A61K31/7056 , A61K31/7084 , A61K31/7076 , A61K31/7064 , A61K31/708 , A61K31/7042 , A61K31/706 , A61K31/7052 , A61K31/7115 , A61K31/712 , C07H19/20 , C07H19/207 , C07H21/02
CPC分类号： C07H19/167 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K31/708 , A61K31/7084 , A61K31/7115 , A61K31/712 , C07H19/20 , C07H19/207 , C07H21/02
摘要： The use of at least one nucleic acid based nuclear localization signal including a natural or synthetic m3G-CAP is shown to increase transmembrane transport of a molecular cargo, in particular large molecules, into the nucleus. The use of natural and synthetic m3G-CAP is disclosed and the effect shown with a natural RNA 5′ end nuclear localization signal composed of a 2,2,7-trimethylguanosine CAP (m3G-CAP) coupled to fluorescent Streptavidin in one example, and an antisense oligonucleotide in another. A methylenephosphonate modified m3G-CAP is shown to have improved stability in human serum and in cytosolic extract.
摘要翻译：显示使用至少一种基于核酸的核定位信号，包括天然或合成的m3G-CAP，以增加分子货物特别是大分子进入细胞核的跨膜转运。公开了天然和合成的m3G-CAP的使用，并且在一个实例中用与偶联到荧光链霉亲和素的2,2,7-三甲基鸟苷CAP（m3G-CAP）组成的天然RNA 5'端核定位信号显示的效果，以及另一个反义寡核苷酸。亚甲基膦酸酯改性的m3G-CAP显示在人血清和胞质提取物中具有改善的稳定性。

75. 发明申请

US20150174149A1 COMPOSITIONS INCLUDING TRICIRIBINE AND METHODS OF USE THEREOF 有权
标题翻译：组合物，包括其中的有关物质及其使用方法
公开(公告)号：US20150174149A1
公开(公告)日：2015-06-25
申请号：US14514311
申请日：2014-10-14
申请人： University of South Florida
发明人： Jin Q. CHENG , Said M. Sebti
IPC分类号： A61K31/7064 , A61K39/395 , C07K16/28
CPC分类号： A61K31/7064 , A61K31/282 , A61K31/337 , A61K31/4353 , A61K31/7076 , A61K33/24 , A61K39/39558 , A61K45/06 , A61K2039/505 , C07K16/2863 , C07K2317/24 , C07K2317/76 , A61K2300/00
摘要： This invention encompasses combination therapies including TCN, TCN-P, TCN-PM and/or related compounds and one or more additional anti-cancer agents, for example, taxanes a molecule that modulates the HER2/neu (erbB2) receptor, anthracyclin compounds, epidermal growth factor receptor inhibitor compounds, one or more platinum compounds and bortezomib and derivatives thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
摘要翻译：本发明包括组合疗法，包括TCN，TCN-P，TCN-PM和/或相关化合物和一种或多种另外的抗癌剂，例如紫杉烷类调节HER2 / neu（erbB2）受体的分子，蒽环类化合物，表皮生长因子受体抑制剂化合物，一种或多种铂化合物和硼替佐米及其衍生物和对治疗和预防与异常细胞增殖相关的肿瘤，癌症和其它病症的毒性降低的组合物。

76. 发明授权

US08969313B2 Methods and compounds for preventing and treating a tumour 有权
标题翻译：用于预防和治疗肿瘤的方法和化合物
公开(公告)号：US08969313B2
公开(公告)日：2015-03-03
申请号：US12740912
申请日：2008-11-03
申请人： Qiang Yu
发明人： Qiang Yu
IPC分类号： A61K31/7064 , A61P35/00 , G01N33/53 , A61K31/519 , A61K31/52 , G01N33/50
CPC分类号： A61K31/437 , A61K31/185 , A61K31/519 , A61K31/52 , G01N33/5011 , G01N2800/52
摘要： The invention relates to a method of preventing, inhibiting, arresting or reversing tumorigenesis in a cell as well as a method of inducing apoptosis in a tumor cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I), wherein A is CH or N, R1, R4 and R5 are independent from each other H, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group comprising 0-3 heteroatoms. The heteroatoms may be N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen such as F, Cl, Br or L. R3 is H, F, Cl or an aliphatic or arylaliphatic group that includes 1-8 main chain carbon atoms and 0-3 heteroatoms. The pharmaceutical composition also comprises a histone deacetylase inhibitor.
摘要翻译：本发明涉及一种预防，抑制，阻止或逆转细胞中肿瘤发生的方法以及诱导肿瘤细胞凋亡的方法。该方法包括增加细胞中DACT蛋白或其功能片段的量和/或活性。还提供了包含通式（I）的化合物的药物组合物，其中A为CH或N，R 1，R 4和R 5彼此独立地为H，脂族基团，脂环族基团，芳族基团，芳基脂族基基团和包含0-3个杂原子的芳基脂环基团。杂原子可以是N，O，S或Si。 R 4和R 5可以任选连接以限定脂族烃基桥。 R 2是H或卤素如F，Cl，Br或L.R 3是H，F，Cl或包含1-8个主链碳原子和0-3个杂原子的脂族或芳基脂族基团。药物组合物还包含组蛋白脱乙酰酶抑制剂。

77. 发明申请

US20140303111A1 COMPOSITIONS INCLUDING TRICIRIBINE AND TAXANES AND METHODS OF USE THEREOF 有权
标题翻译：组合物，包括审美和TAXANES及其使用方法
公开(公告)号：US20140303111A1
公开(公告)日：2014-10-09
申请号：US14091073
申请日：2013-11-26
申请人： University of South Florida
发明人： Jin Q. CHENG , Said M. Sebti
IPC分类号： A61K31/7064 , A61K31/337
CPC分类号： A61K31/7064 , A61K9/0019 , A61K9/0053 , A61K31/337 , A61K31/7076 , C12Q1/485 , G01N33/573 , G01N2333/912
摘要： This application relates to combination therapies including triciribine and related compounds and taxanes and compositions with reduced toxicity thr the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
摘要翻译：本申请涉及组合疗法，包括三苯呋嗪和相关化合物以及紫杉烷类和毒性降低的组合物，治疗和预防与异常细胞增殖相关的肿瘤，癌症和其它病症。

78. 发明申请

US20140294856A1 COMBINATION TREATMENT COMPRISING A HDAC6 INHIBITOR AND AN AKT INHIBITOR 审中-公开
标题翻译：包含HDAC6抑制剂和AKT抑制剂的组合治疗
公开(公告)号：US20140294856A1
公开(公告)日：2014-10-02
申请号：US14128144
申请日：2012-06-21
申请人： Eric O. Aboagye , Maciej A. Kaliszczak
发明人： Eric O. Aboagye , Maciej A. Kaliszczak
IPC分类号： A61K31/437 , A61K45/06 , A61K31/7064 , A61K31/185
CPC分类号： A61K31/437 , A61K31/00 , A61K31/165 , A61K31/167 , A61K31/18 , A61K31/185 , A61K31/337 , A61K31/4965 , A61K31/513 , A61K31/65 , A61K31/704 , A61K31/7064 , A61K45/06 , Y02A50/411 , A61K2300/00
摘要： The invention provides compositions comprising a Histone Deacetylase 6 (HDAC6) inhibitor and an AKT inhibitor, pharmaceutical compositions/formulations and kits of parts comprising the same; optionally further comprising one or more anti-cancer agents. The compositions of the invention provide for surprisingly efficacious killing of inter alia, cancer cells. Thus, the invention also provides for the use of the compositions, pharmaceutical compositions and kits of parts in medicine, and further, for use in the prevention or treatment of cancer and/or neuro-degenerative conditions, including Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis (ALS), spinal and bulbar muscular atrophy (SbMA), Rubinstein-Taybi syndrome, Rett syndrome, and Friedreich's ataxia, or autoimmune diseases, including Rheumatoid Arthritis, Myasthenia Gravis, and Multiple Sclerosis.
摘要翻译：本发明提供了组合物，其包含组蛋白脱乙酰酶6（HDAC6）抑制剂和AKT抑制剂，药物组合物/制剂和包含它们的成分试剂盒; 任选地还包含一种或多种抗癌剂。本发明的组合物提供惊人的有效杀伤特别是癌细胞。因此，本发明还提供组合物，药物组合物和药物试剂盒在医学中的用途，并且还用于预防或治疗癌症和/或神经退行性疾病，包括阿尔茨海默氏病，帕金森病，亨廷顿病疾病，肌萎缩性侧索硬化（ALS），脊髓和延髓肌肉萎缩（SbMA），鲁宾斯坦 - 泰比综合征，雷特综合征和弗里德里希共济失调或自身免疫性疾病，包括类风湿关节炎，重症肌无力和多发性硬化。

79. 发明申请

US20140099283A1 2'-CHLORO NUCLEOSIDE ANALOGS FOR HCV INFECTION 审中-公开
标题翻译：用于HCV感染的2'-氯代核苷类似物
公开(公告)号：US20140099283A1
公开(公告)日：2014-04-10
申请号：US14047862
申请日：2013-10-07
申请人： Idenix Pharmaceuticals, Inc. , Universite Montpellier 2 Sciences Et Techniques , Centre National De La Recherche Scientifique
发明人： Gilles GOSSELIN , Christophe Claude PARSY , Francois-Rene ALEXANDRE , Houcine RAHALI , Jean-Francois GRIFFON , Julien MILHAU , Dominique SURLERAUX , Cyril B. DOUSSON , Claire PIERRA , Adel M. MOUSSA , Benjamin Alexander MAYES
IPC分类号： C07H19/10 , A61K45/06 , A61K38/21 , C07H19/20 , A61K31/7076 , A61K31/708 , C07H19/14 , A61K31/7064 , C07H19/12 , A61K31/706 , A61K31/7068 , A61K31/7072 , C07H19/16
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2′-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物是根据式2001的2'-氯核苷：或其药学上可接受的盐，溶剂化物，立体异构形式，互变异构形式或其多晶型，其中B，Z和PD如本文所述。

80. 发明申请

US20130331404A1 Methods and Compositions for Inhibition of Polymerase 审中-公开
公开(公告)号：US20130331404A1
公开(公告)日：2013-12-12
申请号：US13879110
申请日：2011-10-14
申请人： Shanta Bantia , Pravin L. Kotian , Yarlagadda S. Babu
发明人： Shanta Bantia , Pravin L. Kotian , Yarlagadda S. Babu
IPC分类号： C07H7/06 , A61K45/06 , A61K31/7064
摘要： The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents.

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