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1. 发明申请

US20070203147A1 2-Aminothiazole Compounds Useful As Aspartyl Protease Inhibitors 审中-公开
标题翻译：用作天冬氨酰蛋白酶抑制剂的2-氨基噻唑化合物
公开(公告)号：US20070203147A1
公开(公告)日：2007-08-30
申请号：US10593808
申请日：2005-03-25
申请人： Craig Coburn , Amy Espeseth , Shawn Stachel , David Olsen , Daria Hazuda , M. Holloway
发明人： Craig Coburn , Amy Espeseth , Shawn Stachel , David Olsen , Daria Hazuda , M. Holloway
IPC分类号： A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4709 , A61K31/4439 , A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D417/14 , C07D277/40 , C07D277/60 , C07D277/82 , C07D277/84 , C07D417/04 , C07D417/06 , C07D417/08
摘要： The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme and HIV protease are involved.
摘要翻译：本发明涉及作为天冬氨酰蛋白酶抑制剂的2-氨基噻唑化合物，并且是β-分泌酶和HIV蛋白酶的抑制剂，并且其可用于治疗其中涉及β-分泌酶和HIV的疾病，如阿尔茨海默病，艾滋病毒感染和艾滋病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶和HIV蛋白酶的疾病的用途中的用途。

2. 发明申请

US20070202547A1 Methods For Detecting Substances Which Bind To The Amyloid Precursor Protein Or Beta Amyloid Fragments, And Binding Compounds 审中-公开
标题翻译：用于检测与淀粉样蛋白前体蛋白或β淀粉样蛋白片段以及结合化合物结合的物质的方法
公开(公告)号：US20070202547A1
公开(公告)日：2007-08-30
申请号：US10594835
申请日：2005-03-29
申请人： Craig Coburn , Amy Espeseth , Daria Hazuda
发明人： Craig Coburn , Amy Espeseth , Daria Hazuda
IPC分类号： G01N33/542
CPC分类号： G01N33/6896 , C07D307/79 , C07D405/12 , G01N2333/4709 , G01N2500/00
摘要： Disclosed are methods for identifying and evaluating the binding properties of substances to the amyoid precursor protein (APP) or to β-amyloid (Aβ fragments of APP. Also disclosed is a class of benzofuran derivatives of formula (I), which interact specifically with APP or Aβ, and block interaction of APP or Aβ with secreatase or APP or Aβ binding antibodies.
摘要翻译：公开了用于鉴定和评价物质与淀粉样前体蛋白（APP）或β-淀粉样蛋白（APP的Aβ片段）的结合性质的方法。还公开了一类与APP特异性相互作用的式（I）的苯并呋喃衍生物或Abeta，并阻断APP或Abeta与分泌或APP或Abeta结合抗体的相互作用。

3. 发明申请

US20070048320A1 Method for indentifying modulators of PPIL2 useful for treating Alzheimer's disease 审中-公开
标题翻译：用于鉴定治疗阿尔茨海默病的PPIL2调节剂的方法
公开(公告)号：US20070048320A1
公开(公告)日：2007-03-01
申请号：US11514737
申请日：2006-08-31
申请人： Amy Espeseth , Daria Hazuda , Peter Linsley , Qian Huang
发明人： Amy Espeseth , Daria Hazuda , Peter Linsley , Qian Huang
IPC分类号： A61K39/395 , G01N33/567 , A61K39/00
CPC分类号： C07K16/18 , A61K2039/505 , C07K16/40 , C12N9/90 , G01N33/6896 , G01N2333/4709 , G01N2500/10
摘要： Methods for identifying modulators of PPIL2 are described. The methods are particularly useful for identifying analytes that antagonize PPIL2's effect on processing of amyloid precursor protein to Aβ peptide and thus useful for identifying analytes that can be used for treating Alzheimer disease.
摘要翻译：描述了用于鉴定PPIL2调节剂的方法。该方法特别适用于鉴定拮抗PPIL2对淀粉样蛋白前体蛋白加工成Abeta肽的影响的分析物，因此可用于鉴定可用于治疗阿尔茨海默病的分析物。

4. 发明申请

US20060270841A1 Assays to monitor amyloid precursor protein processing 审中-公开
标题翻译：监测淀粉样蛋白前体蛋白加工的测定
公开(公告)号：US20060270841A1
公开(公告)日：2006-11-30
申请号：US10504446
申请日：2003-02-25
申请人： Amy Espeseth , Marc Ferrer , Osvaldo Flores , Daria Hazuda , James Inglese , Michael Miller , Bruce Register , Xiao-Ping Shi , Adam Simon , Paul Zuck
发明人： Amy Espeseth , Marc Ferrer , Osvaldo Flores , Daria Hazuda , James Inglese , Michael Miller , Bruce Register , Xiao-Ping Shi , Adam Simon , Paul Zuck
IPC分类号： C12Q1/68 , C07H21/04 , C12P21/06 , C12N9/64
CPC分类号： C07K14/47 , C07K14/4702 , C07K14/4711 , C07K2319/00 , C07K2319/50 , G01N2500/10
摘要： The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and γ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.
摘要翻译：本发明提供了DNA构建体，遗传工程化宿主细胞和用于鉴定淀粉样前体蛋白（APP）处理抑制剂的方法。该方法提供了在单次测定中方便地鉴定β-分泌酶和γ-分泌酶抑制剂以及其它形式的APP处理。该方法依赖于APP和转录因子的融合蛋白，其中APP处理释放转录因子，允许转录因子激活报告基因的转录。抑制剂被鉴定为阻断或减少转录因子从融合蛋白释放的物质，从而导致报告基因读出的减少。

5. 发明授权

US06245806B1 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US06245806B1
公开(公告)日：2001-06-12
申请号：US09625246
申请日：2000-07-25
申请人： Anne Dombrowski , Sheo Singh , Deborah L. Zink , Ana Teran , Fernando Pelaez , Daria Hazuda
发明人： Anne Dombrowski , Sheo Singh , Deborah L. Zink , Ana Teran , Fernando Pelaez , Daria Hazuda
IPC分类号： A61K31335
CPC分类号： C07D493/08 , A61K31/352 , A61K45/06 , C12P17/181 , C12R1/645 , A61K2300/00
摘要： Novel tetracyclic aromatic ketones are natural product compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. Further, the novel fungal cultures MF6388 (ATCC 74478), Sterile Fungus, and MF6591 (ATCC 74477), Ascochyta sp. are also disclosed. Further, the cultures Sterile Fungus MF6388 (ATCC 74478) and Ascochyta sp. MF6591 (ATCC 74477) are also disclosed, as well as processes for making compounds of the present invention employing the cultures.
摘要翻译：新型四环芳族酮是用于抑制HIV整合酶，预防或治疗艾滋病毒感染和治疗艾滋病的天然产物化合物，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合，免疫调节剂，抗生素或疫苗。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。此外，新型真菌培养物MF6388（ATCC 74478），无菌真菌和MF6591（ATCC 74477），Ascochyta sp。也被披露。此外，培养无菌真菌MF6388（ATCC 74478）和Ascochyta sp。还公开了MF6591（ATCC 74477），以及使用培养物制备本发明化合物的方法。

6. 发明申请

US20070248613A1 Human Antibodies Interacting with Hiv Gp41 有权
标题翻译：人类抗体与HIF Gp41相互作用
公开(公告)号：US20070248613A1
公开(公告)日：2007-10-25
申请号：US11628164
申请日：2005-05-31
申请人： John Shiver , Michael Miller , Romas Geleziunas , Daria Hazuda , Peter Kim , Debra Eckert , Michael Root , Simon Lennard , Elisabetta Bianchi
发明人： John Shiver , Michael Miller , Romas Geleziunas , Daria Hazuda , Peter Kim , Debra Eckert , Michael Root , Simon Lennard , Elisabetta Bianchi
IPC分类号： A61K39/395 , A61K33/00 , A61P31/18 , C07H21/04 , C07K16/00 , C12N15/00 , C12P21/06 , G01N33/566
CPC分类号： G01N33/56988 , C07K16/1063 , C07K2317/21 , C07K2317/622 , C07K2317/76 , G01N2500/00
摘要： Human scFvs are disclosed which interact with a conformational epitope along the pre-hairpin, N-helix coiled coil structure within the heptad repeat 1 (HR1) region of gp41 of HIV. These antibodies, as well as IgG conversions, are shown to neutralize diverse HIV isolates. Isolated nucleic acid molecules are also disclosed which encode relevant portions of these antibodies, as well as the purified forms of the expressed antibodies or relevant antibody fragments, such as VH and VL chains. The antibody compositions disclosed within this specification may provide for a therapeutic treatment against HIV infection by reducing viral load levels within an infected individual, thus prolonging the asymptomatic phase of HIV infection. These antibodies will also be useful in assays to identify HIV antiviral compounds as well as allowing for the identification of candidate HIV vaccines, such as HIV peptide vaccines.
摘要翻译：披露了人scFv，其与艾滋病病毒gp41的七重复重复1（HR1）区域内的前发夹，N-螺旋卷曲螺旋结构与构象表位相互作用。显示出这些抗体以及IgG转化中和多种HIV分离物。还公开了分离的核酸分子，其编码这些抗体的相关部分，以及所表达的抗体或相关抗体片段的纯化形式，例如V H H和V L >链。在本说明书中公开的抗体组合物可通过降低受感染个体内的病毒载量水平来提供抗HIV感染的治疗性治疗，从而延长HIV感染的无症状期。这些抗体也可用于鉴定HIV抗病毒化合物的测定，以及允许鉴定候选的HIV疫苗，例如HIV肽疫苗。

7. 发明申请

US20060216272A1 Therapeutic immunization of hiv-infected individuals 审中-公开
标题翻译： HIV感染者的治疗免疫
公开(公告)号：US20060216272A1
公开(公告)日：2006-09-28
申请号：US10571651
申请日：2004-09-14
申请人： Emilio Emini , John Shiver , Danilo Casimiro , Daria Hazuda , William Scheilf
发明人： Emilio Emini , John Shiver , Danilo Casimiro , Daria Hazuda , William Scheilf
IPC分类号： A61K48/00
CPC分类号： A61K39/21 , A61K39/12 , A61K2039/53 , A61K2039/545 , A61K2039/55 , C07K14/005 , C12N7/00 , C12N15/86 , C12N2710/10343 , C12N2740/15022 , C12N2740/15034 , C12N2740/15071 , C12N2740/16134 , C12N2740/16222
摘要： The present invention provides an improved method for eliciting a therapeutic immune response in an individual infected with human immunodeficiency virus (“HIV”). The method comprises administering an adenoviral vaccine composition expressing an HIV antigen to an individual with controlled viremia. Immunization of infected individuals in this manner elicits a cellular-mediated immune response against the virus that is significant both in the level of the response and the breadth of the response. The therapeutic immune response that ensues is capable of effectively maintaining low titers of virus and, thus, offers the prospect of reducing individual dependency on antiviral therapy.
摘要翻译：本发明提供了在感染人类免疫缺陷病毒（“HIV”）的个体中引发治疗性免疫应答的改进方法。该方法包括向具有受控制的病毒血症的个体施用表达HIV抗原的腺病毒疫苗组合物。以这种方式免疫感染的个体引起针对病毒的细胞介导的免疫应答，其在反应水平和反应的广度方面是显着的。随后的治疗性免疫应答能够有效地维持低滴度的病毒，从而提供减少个体对抗病毒治疗依赖性的前景。

8. 发明申请

US20140328799A1 COMPOSITIONS USEFUL FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：用于治疗病毒性疾病的组合物
公开(公告)号：US20140328799A1
公开(公告)日：2014-11-06
申请号：US14355363
申请日：2012-10-26
申请人： Steven S. Carroll , John A. McCauley , David B. Olsen , Vincenzo Summa , Michael Rowley , Mark W. Stahlhut , Daria Hazuda
发明人： Steven S. Carroll , John A. McCauley , David B. Olsen , Vincenzo Summa , Michael Rowley , Mark W. Stahlhut , Daria Hazuda
IPC分类号： A61K38/06 , A61K31/553 , A61K31/519 , A61K31/4178 , A61K31/7064
CPC分类号： A61K38/06 , A61K31/403 , A61K31/407 , A61K31/4178 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/553 , A61K31/7064 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395 , A61K2300/00
摘要： The present invention is directed to compositions comprising inhibitors of hepatitis C virus (HCV) protease and one or more additional therapeutically effective agents. Uses of such compositions as HCV inhibitors and methods of treating infection by HCV by administration of such compositions are also disclosed.
摘要翻译：本发明涉及包含丙型肝炎病毒（HCV）蛋白酶抑制剂和一种或多种另外的治疗有效试剂的组合物。还公开了使用这些组合物作为HCV抑制剂和通过施用这种组合物治疗HCV感染的方法。

9. 发明申请

US20070219354A1 Assays using amyloid precursor proteins with modified beta-secretase cleavage sites to monitor beta-secretase activity 审中-公开
公开(公告)号：US20070219354A1
公开(公告)日：2007-09-20
申请号：US11714985
申请日：2007-03-07
申请人： Daria Hazuda , Elizabeth Chen Dodson , Ming-Tain Lai , Min Xu , Xiao-Ping Shi , Adam Simon , Guoxin Wu , Yueming Li , Bruce Register
发明人： Daria Hazuda , Elizabeth Chen Dodson , Ming-Tain Lai , Min Xu , Xiao-Ping Shi , Adam Simon , Guoxin Wu , Yueming Li , Bruce Register
IPC分类号： C07K16/00 , C07K14/00
CPC分类号： C07K7/06 , A01K2217/05 , A01K2267/0306 , A61K38/00 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K14/4711 , C07K16/18 , C12P21/06 , C12Q1/37 , G01N33/5088 , G01N33/6896 , G01N2500/00 , G01N2800/52
摘要： Provided are methods of identifying inhibitors of β-secretase that employ modified β-secretase substrates. The modified β-secretase substrates have β-secretase cleavage sites that are altered from wild type. The amino acid sequences of the altered β-secretase cleavage sites contain different amino acids in at least one of the positions P2-P1-P1′-P2′ of the β-secretase cleavage site. Many of the modified β-secretase substrates are more efficient substrates for β-secretase than are corresponding substrates having wild-type sequences, that is, these modified substrates are more susceptible to enzymatic breakdown by β-secretase. Recombinant polynucleotide molecules encoding the modified β-secretase substrates are provided. Antibodies that recognize cleavage products of the modified β-secretase substrates are provided. Stable cell lines expressing the modified β-secretase substrates are provided. Transgenic animals expressing the modified β-secretase substrates are provided.

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