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公开(公告)号：US20120245040A1
公开(公告)日：2012-09-27
申请号：US13040674
申请日：2011-03-04
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译： 本发明提供合成包含编码寡核苷酸标签的分子文库的方法。
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公开(公告)号：US08084419B2
公开(公告)日：2011-12-27
申请号：US11173901
申请日：2005-06-30
申请人： Malcolm L. Gefter
发明人： Malcolm L. Gefter
IPC分类号： A61K38/09
摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptide and a plurality of ligands are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. Methods of making the complexes of the invention, and methods of these complexes are also disclosed.
摘要翻译： 公开了包含肽和多个配体的水不溶性络合物的持续递送制剂。 本发明的制剂允许在施用复合物之后以较小的体积装载高浓度的肽并延长药物活性肽的递送时间，例如一个月。 本发明的络合物可以研磨或粉碎成细粉末。 以粉末形式，络合物形成稳定的水性悬浮液和分散体，适于注射。 还公开了制备本发明配合物的方法和这些络合物的方法。
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公开(公告)号：US07972992B2
公开(公告)日：2011-07-05
申请号：US11015458
申请日：2004-12-17
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
IPC分类号： C40B50/00
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides methods of synthesizing a molecule comprising a functional moiety which is operatively linked to an encoding oligonucleotide. The methods include providing an initiator compound comprising an initial functional moiety comprising n building blocks, wherein the initial functional moiety comprises at least one reactive group, and is operatively linked to an initial oligonucleotide; reacting the initiator compound with a building block comprising at least one complementary reactive group, under conditions suitable for reaction of the complementary reactive group to form a covalent bond; and reacting the initial oligonucleotide with an incoming oligonucleotide corresponding to the building block in the presence of an enzyme which catalyzes ligation of the initial oligonucleotide and the incoming oligonucleotide, under conditions suitable for ligation of the incoming oligonucleotide and the initial oligonucleotide to form an encoding oligonucleotide.
摘要翻译： 本发明提供合成包含与编码寡核苷酸有效连接的功能部分的分子的方法。 所述方法包括提供包含起始功能部分的引发剂化合物，其包含n个结构单元，其中所述初始功能部分包含至少一个反应性基团，并且可操作地连接到初始寡核苷酸; 使引发剂化合物与包含至少一个互补反应性基团的构建块在适于互补反应性基团反应以形成共价键的条件下反应; 并在初始寡核苷酸和入侵寡核苷酸的连接酶存在下，使初始寡核苷酸与对应于构建单元的入侵寡核苷酸反应，在适合连接引入寡核苷酸和初始寡核苷酸的条件下形成编码寡核苷酸 。
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44.发明授权公开(公告)号：US07175828B2
公开(公告)日：2007-02-13
申请号：US10677076
申请日：2003-09-30
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
CPC分类号： C07K5/101 , A61K38/00 , C07K5/1027 , C07K7/06 , C07K14/4711 , G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3–5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样肽的逆反异构体，优选Abeta 17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团包括环状，杂环，多环和支链烷基。 优选的羧基末端修饰基团包括酰胺基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。
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公开(公告)号：US07037889B2
公开(公告)日：2006-05-02
申请号：US09953247
申请日：2001-09-13
申请人： Malcolm L. Gefter
发明人： Malcolm L. Gefter
IPC分类号： A61K38/00
摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptide and a plurality of ligands are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. Methods of making the complexes of the invention, and methods of these complexes are also disclosed.
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公开(公告)号：US06211153B1
公开(公告)日：2001-04-03
申请号：US09438718
申请日：1999-11-11
IPC分类号： A61K3800
CPC分类号： A61K38/09 , Y10S514/80 , A61K2300/00
摘要： Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.
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47.发明授权公开(公告)号：US06180609B2
公开(公告)日：2001-01-30
申请号：US09438174
申请日：1999-11-11
IPC分类号： A61K3800
CPC分类号： A61K38/09 , Y10S514/80 , A61K2300/00
摘要： Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.
摘要翻译： 公开了治疗前列腺癌的方法。 本发明的方法通常特征在于与第二疗法组合施用于LHRH-R拮抗剂的受试者。 在一个实施方案中，该第二疗法是去除或破坏前列腺肿瘤组织，例如根治性前列腺切除术，冷冻手术或X射线治疗（外部或间质）的程序。 在另一个实施方案中，第二疗法是与LHRH-R拮抗剂治疗同时或之后用LHRH-R激动剂治疗。 本发明的方法还可以包括与LHRH-R拮抗剂联合给予受试者的抗雄激素和/或抑制性类固醇生物合成。
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48.发明授权Hapten-carrier conjugates for use in drug-abuse therapy and methods for preparation 失效用于药物滥用治疗的穿孔载体缀合物和制备方法
公开(公告)号：US5840307A
公开(公告)日：1998-11-24
申请号：US457206
申请日：1995-06-01
申请人： Philip A. Swain , Victoria Carol Schad , Julia Lea Greenstein , Mark Adrian Exley , Barbara Saxton Fox , Stephen P. Powers , Malcolm L. Gefter
发明人： Philip A. Swain , Victoria Carol Schad , Julia Lea Greenstein , Mark Adrian Exley , Barbara Saxton Fox , Stephen P. Powers , Malcolm L. Gefter
IPC分类号： A61K47/48 , A61P25/30 , A61K39/385 , A61K39/00 , A61K39/395 , C07P451/02
CPC分类号： C07K16/44 , A61K39/0013 , A61K47/4833 , A61K2039/6037
摘要： Hapten-carrier conjugates capable of eliciting anti hapten antibodies in vivo by administering, in a therapeutic composition, are disclosed. Anti-hapten antibodies elicited compete with free hapten upon subsequent challenge of a vaccinated individual. Methods of preparing said conjugates and therapeutic compositions are also disclosed. Where the hapten is a drug of abuse, a therapeutic composition containing the hapten-carrier conjugate is particularly useful in the treatment of drug addiction, more particularly, cocaine addiction. Passive immunization using antibodies raised against conjugates of the instant invention is also disclosed. The therapeutic composition is suitable for co-therapy with other conventional drugs.
摘要翻译： 公开了通过在治疗组合物中施用能够在体内引发抗半抗原抗体的穿孔载体缀合物。 抗半抗原抗体引起与免疫半抗原的竞争，随后对接种疫苗的个体进行攻击。 还公开了制备所述缀合物和治疗组合物的方法。 当半抗原是滥用药物时，含有半抗原 - 载体结合物的治疗组合物特别可用于治疗药物成瘾，特别是可卡因成瘾。 还公开了使用针对本发明的缀合物产生的抗体的被动免疫。 该治疗组合物适用于与其它常规药物共同治疗。
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公开(公告)号：US5817626A
公开(公告)日：1998-10-06
申请号：US404831
申请日：1995-03-14
申请人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
发明人： Mark A. Findeis , Howard Benjamin , Marc B. Garnick , Malcolm L. Gefter , Arvind Hundal , Laura Kasman , Gary Musso , Ethan R. Signer , James Wakefield , Michael J. Reed
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that act to modulate the aggregation of natural .beta. amyloid peptides (.beta.-AP) are disclosed. The .beta. amyloid modulators of the invention can promote .beta.-AP aggregation or, more preferably, can inhibit natural .beta.-AP aggregation. Furthermore, the modulators are capable of altering natural .beta.-AP aggregation when the natural .beta.-APs are in a molar excess amount relative to the modulators. Preferred .beta. amyloid modulators comprise amino-terminally biotinylated .beta. amyloid peptide compounds. Pharmaceutical compositions comprising the compounds of the invention, and methods of altering natural .beta.-AP aggregation using the compounds of the invention, are also disclosed.
摘要翻译： 公开了用于调节天然β淀粉样肽（β-AP）聚集的化合物。 本发明的β淀粉样蛋白调节剂可以促进β-AP聚集，更优选可以抑制天然β-AP聚集。 此外，当天然β-APs相对于调节剂摩尔过量时，调节剂能够改变天然的β-AP聚集。 优选的β淀粉样蛋白调节剂包含氨基末端生物素化的β淀粉样蛋白肽化合物。 还公开了包含本发明化合物的药物组合物和使用本发明化合物改变天然β-AP聚集的方法。
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公开(公告)号：US5019384A
公开(公告)日：1991-05-28
申请号：US434548
申请日：1989-11-13
申请人： Malcolm L. Gefter , Jean G. Guillet
发明人： Malcolm L. Gefter , Jean G. Guillet
IPC分类号： A61K39/00 , A61K39/015 , A61K39/12 , A61K39/21
CPC分类号： A61K39/12 , A61K39/00 , A61K39/015 , A61K39/36 , A61K39/39 , A61K2039/55516 , A61K2039/55566 , C12N2760/16034
摘要： Novel methods or compositions are provided for modulating the immune system, so as to be able to selectively stimulate or inactivate lymphocytes in relation to a particular transplantation antigen content. Particularly, mixtures may be employed associated with the more common transplanatation antigens of a host population. In this manner, a large number of people can be treated, for example, by immunization, stimulation of particular T-cells or B-cells in relation to a pathogenic invasion of other aberrant state, e.g. neoplasia, treatment of autoimmune diseases, and the like. Particularly, the compositions may involve an oligopeptide involving as a first region a consensus sequence and an epitope or the first region may be joined to a second region comprising an antibody target sequence which is capable of competing with an epitopic site of an antigen of interest.
摘要翻译： 提供了用于调节免疫系统的新方法或组合物，以便能够相对于特定的移植抗原含量选择性地刺激或灭活淋巴细胞。 特别地，可以使用与宿主群体更常见的转化抗原相关的混合物。 以这种方式，可以例如通过免疫接种，特异性T细胞或B细胞相对于其他异常状态的病原性入侵的刺激来治疗大量的人，例如。 瘤形成，自身免疫性疾病的治疗等。 特别地，组合物可以涉及涉及作为第一区域的共有序列和表位的寡肽，或者第一区域可以连接到包含能够与感兴趣的抗原的表位位点竞争的抗体靶序列的第二区域。
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