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121. 发明授权

US5703086A Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions 失效
公开(公告)号：US5703086A
公开(公告)日：1997-12-30
申请号：US471797
申请日：1995-06-06
申请人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
发明人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
IPC分类号： C07C279/16 , C07C279/26 , C07D239/48 , C07D251/48 , A61K31/505
CPC分类号： C07D239/48 , C07C279/16 , C07C279/26 , C07D251/48
摘要： The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.

122. 发明授权

US5700466A Method of ameliorating or preventing septic shock using a monoclonal antibody specific to cachectin/tumor necrosis factor 失效
标题翻译：使用特异于恶性胶质瘤/肿瘤坏死因子的单克隆抗体改善或预防败血性休克的方法
公开(公告)号：US5700466A
公开(公告)日：1997-12-23
申请号：US348764
申请日：1994-12-02
申请人： Stephen D. Wolpe , Anthony Cerami
发明人： Stephen D. Wolpe , Anthony Cerami
IPC分类号： A61K38/00 , A61K39/00 , C07K14/47 , C07K14/52 , C07K14/525 , C07K16/18 , C07K16/24 , C07K16/38 , C12N5/0789 , C12P1/00 , C12P21/08 , C12Q1/02 , G01N33/53 , A61K39/395 , A61K39/40 , A61K38/19
CPC分类号： G01N33/53 , C07K14/4702 , C07K14/4703 , C07K14/523 , C07K14/525 , C07K16/18 , C07K16/24 , C07K16/241 , C07K16/38 , C12N5/0647 , C12P1/00 , C12Q1/02 , A61K38/00 , A61K39/00 , C12N2501/21 , C12N2501/22 , G01N2333/52 , G01N2400/40
摘要： The present invention pertains to the novel hybridoma SDW18.1.1, hybridomas obtained from SDW18.1.1, monoclonal antibodies obtained from such hybridomas and derivatives of such monoclonal antibodies. The novel hybridomas are formed by fusion of cells from a mouse myeloma line and spleen cells from a mouse previously immunized with cachectin/TNF. Diagnostic and therapeutic utilities for the monoclonal antibodies and their derivatives are proposed, and testing procedures, materials in kit form and pharmaceutical compositions are likewise set forth.
摘要翻译：本发明涉及新型杂交瘤SDW18.1.1，从SDW18.1.1获得的杂交瘤，从这样的杂交瘤获得的单克隆抗体和这种单克隆抗体的衍生物。通过将来自小鼠骨髓瘤细胞系的细胞和先前用恶病质/ TNF免疫的小鼠的脾细胞融合，形成新的杂交瘤。提出了用于单克隆抗体及其衍生物的诊断和治疗用途，同样阐述了测试程序，试剂盒形式的材料和药物组合物。

123. 发明授权

US5585344A Liver-derived receptors for advanced glycosylation endproducts and uses thereof 失效
标题翻译：用于晚期糖基化终产物的肝衍生受体及其用途
公开(公告)号：US5585344A
公开(公告)日：1996-12-17
申请号：US749438
申请日：1991-08-23
申请人： Helen Vlassara , Zhi Yang , Anthony Cerami
发明人： Helen Vlassara , Zhi Yang , Anthony Cerami
IPC分类号： A61K8/64 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K38/00 , A61K38/19 , A61K38/20 , A61K38/21 , A61K38/38 , A61K39/00 , A61Q11/00 , A61Q19/08 , C07D405/14 , C07K14/705 , C07K16/28 , G01N33/50 , G01N33/533 , G01N33/573 , G01N33/68 , A61K38/17
CPC分类号： G01N33/6893 , A61K31/155 , A61K31/195 , A61K31/415 , A61K31/4178 , A61K39/0005 , A61K8/64 , A61Q19/08 , C07D405/14 , C07K14/705 , C07K16/28 , C07K16/2803 , G01N33/5091 , G01N33/533 , G01N33/573 , G01N33/68 , G01N33/6842 , G01N33/6887 , A61K2039/6081 , A61K38/00 , C07K2317/34 , C07K2317/77 , G01N2333/922
摘要： The present invention relates to receptors for advanced glycosylation endproducts derived from rat liver membranes, and that specifically comprise proteins determined to possess molecular masses of about 90 kD and 60 kD, respectively, as assessed by migration during SDS-PAGE. Partial N-terminal sequences have been determined and diagnostic and therapeutic agents, compositions and methods are proposed.
摘要翻译：本发明涉及来自大鼠肝膜的晚期糖基化终产物的受体，并且其特异性包括通过SDS-PAGE期间的迁移评估分别确定具有约90kD和60kD的分子量的蛋白质。已经确定了部分N-末端序列，并提出了诊断和治疗剂，组合物和方法。

124. 发明授权

US5574040A Pyrimidine compounds and methods of use to derivatize neighboring lysine residues in proteins under physiologic conditions 失效
标题翻译：嘧啶化合物和用于在生理条件下衍生蛋白质中相邻赖氨酸残基的方法
公开(公告)号：US5574040A
公开(公告)日：1996-11-12
申请号：US369830
申请日：1995-01-06
申请人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
发明人： Michael I. Bukrinsky , Anthony Cerami , Peter Ulrich
IPC分类号： C07C279/16 , C07C279/26 , C07D239/48 , C07D251/48 , A61K31/505
CPC分类号： C07D239/48 , C07C279/16 , C07C279/26 , C07D251/48
摘要： A compound according to the formula: ##STR1## wherein A=CH.sub.3 or CH.sub.2 CH.sub.3 and ##STR2## wherein X=NH.sub.2, CH.sub.2 or CH.sub.2 CH.sub.3 ; X'=CH.sub.3 or CH.sub.2 CH.sub.3 ; Y=NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z=H, CH.sub.3 or CH.sub.2 CH.sub.3 ; or ##STR3## wherein Y' and Z', indepedently, = H, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 or N.sup.+ (CH.sub.3).sub.3 ; and salts thereof.
摘要翻译：其中A = CH 3或CH 2 CH 3和其中X = NH 2，CH 2或CH 2 CH 3;（2）其中X = NH 2，CH 2或CH 2 CH 3; X'= CH 3或CH 2 CH 3; Y = NH 2，NHCH 3，N（CH 3）2; 和Z = H，CH 3或CH 2 CH 3; （3）其中Y'和Z'独立地为= H，NH 2，NHCH 3，N（CH 3）2或N +（CH 3）3; 及其盐。

125. 发明授权

US4822776A Lipoprotein lipase suppression by endotoxin-induced mediator (shock assay) 失效
标题翻译：通过内毒素诱导的介质抑制脂蛋白脂肪酶（休克测定）
公开(公告)号：US4822776A
公开(公告)日：1989-04-18
申请号：US792372
申请日：1985-10-29
申请人： Anthony Cerami , Masanobu Kawakami
发明人： Anthony Cerami , Masanobu Kawakami
IPC分类号： A61K38/00 , A61K39/00 , C07K14/47 , C07K14/52 , C07K16/24 , C07K16/38 , C12N5/0789 , C12P1/00 , G01N33/53 , A61K37/02 , A61K35/26 , A61K37/64
CPC分类号： G01N33/53 , C07K14/4703 , C07K14/523 , C07K16/24 , C07K16/241 , C07K16/38 , C12N5/0647 , C12P1/00 , A61K38/00 , A61K39/00 , C12N2501/21 , C12N2501/22 , G01N2333/52 , G01N2400/40 , Y10S514/909 , Y10S530/829 , Y10S530/838
摘要： A mediator substance exhibiting inhibitory effect upon anabolic enzyme activity in mammals, is prepared by a method comprising gathering a sample of macrophage cells from a mammal, incubating a portion of the macrophage cells with a stimulating mateThis invention was made in the course of a grant from the National Institutes of Health.
摘要翻译：通过包括从哺乳动物收集巨噬细胞样品，将一部分巨噬细胞与与入侵事件相关的刺激物质孵育并诱导与哺乳动物合成代谢酶活性显示抑制作用的介体物质巨噬细胞产生介体物质。例如，刺激剂材料可以包括内毒素，锥虫等，并且可以观察到的酶范围从脂蛋白脂肪酶，乙酰辅酶A羧化酶和脂肪酸合成酶到用于红细胞生长和分化的诱导剂。介体物质可以用于产生抗体，其反过来可用于测试各种侵入性刺激如感染等的存在或量。也考虑了试剂盒形式的测试程序和合适的材料。介体物质同样可用作筛选剂的方法，以测试潜在有效的抗休克剂或化学物质。

126. 发明授权

US4469681A Method and system for the controlled release of biologically active substances to a body fluid 失效
标题翻译：将生物活性物质控制释放到体液的方法和系统
公开(公告)号：US4469681A
公开(公告)日：1984-09-04
申请号：US278358
申请日：1981-06-29
申请人： Michael Brownlee , Anthony Cerami
发明人： Michael Brownlee , Anthony Cerami
IPC分类号： A61K38/28 , A61K47/48 , A61M31/00 , A61K37/26
CPC分类号： A61K38/28 , A61K47/48261 , A61M31/002 , Y10S514/866
摘要： A process and system for controlled delivery of a biologically active substance to an animal body fluid which comprises contacting fluid with a reversible complex of a conjugate (1) and a binding macromolecule (2), wherein the conjugate (1) comprises a biologically active portion which is intended to be proportionately released into a body fluid stream in response to varying concentration levels of a component of the body fluid stream, and a complexing substrate portion which conjugates with the biologically active portion and which is characterized by affinity to the binding macromolecule (2), competitivey or non-competitively with the variable component of the body fluid; thereby causing the component present in the body fluid to complex to the binding macromolecule and thus releasing the conjugate (1) therefrom into the fluid.The process and system are particularly applicable for the glucose-controlled release of insulin and other hypoglycemic agents in the treatment of diabetes.
摘要翻译：一种用于将生物活性物质受控输送到动物体液的方法和系统，其包括使流体与缀合物（1）和结合大分子（2）的可逆复合物接触，其中所述缀合物（1）包含生物活性部分其旨在响应于体液流的组分的不同浓度水平而成比例地释放到体液中，以及与生物活性部分共轭并且其特征在于对结合大分子的亲和力的络合底物部分（ 2），与体液的可变成分有竞争力或非竞争性; 从而使存在于体液中的组分与结合大分子复合，从而将共轭物（1）从其中释放到流体中。该方法和系统特别适用于糖尿病治疗中胰岛素和其他降血糖药的葡萄糖控制释放。

127. 发明授权

US4462989A Method and agents for arresting infection 失效
标题翻译：阻止感染的方法和药剂
公开(公告)号：US4462989A
公开(公告)日：1984-07-31
申请号：US374580
申请日：1982-05-03
申请人： Anthony Cerami
发明人： Anthony Cerami
IPC分类号： A61K31/74 , A61K33/00 , A61K38/16 , A61K38/17 , A61K38/40 , A61K39/395 , A61L15/46 , A61K37/00
CPC分类号： A61L15/46 , A61K31/74 , A61K33/00 , A61K38/168 , A61K38/1709 , A61K38/40 , A61K39/395 , A61L2300/256 , A61L2300/404
摘要： A method and associated agents for the arrest of infections resulting from organism growth in contact with an iron-containing body fluid, comprising administering an agent capable of immobilizing the body fluid so that the iron it contains is nutritionally unavailable for the organism. In the instance where the body fluid is blood, the agent may be administered in amounts effective to bind all of the available red blood cells or hemoglobin, to prevent breakdown of either and consequent release of iron to the organism.The agents preferably include materials capable of binding red blood cells and iron, such as haptoglobin, colloidal silica, anion exchange resins and mixtures thereof. Preferably, colloidal silica is used either alone or in a composite with a polyolefin elastomer such as polyisobutylene.The agents may be coated on carriers or substrates, such as gauze pads, tampons and the like, and may be thus utilized topically, as well as intraperitoneally.
摘要翻译：一种用于阻止与含铁体液接触的生物体生长引起的感染的方法和相关药物，其包括施用能够固定体液的药剂，使得其含有的铁在生物体内不可用。在体液为血液的情况下，可以有效地结合所有可用的红细胞或血红蛋白的剂量施用该药剂，以防止铁分解并随之释放到生物体中。试剂优选包括能够结合红细胞和铁的材料，例如触珠蛋白，胶体二氧化硅，阴离子交换树脂及其混合物。优选地，胶体二氧化硅单独使用或与聚烯烃弹性体如聚异丁烯的复合材料中使用。药剂可以涂覆在载体或基底上，例如纱布垫，卫生棉条等，并且可以局部地以及腹膜内地使用。

128. 发明授权

US4424216A Method for the reduction of mucin viscosity 失效
标题翻译：粘蛋白粘度降低的方法
公开(公告)号：US4424216A
公开(公告)日：1984-01-03
申请号：US62503
申请日：1979-07-31
申请人： Anthony Cerami , Nina F. Tabachnik
发明人： Anthony Cerami , Nina F. Tabachnik
IPC分类号： A61K31/13 , A61K31/095 , A61K31/16 , A61K31/185 , A61K31/66 , A61P11/00 , A61P11/10
CPC分类号： A61K31/095
摘要： A method for reducing mucin viscosity which comprises administering an effective dose of a compound having protected sulfhydryl groups which metabolize in vivo to produce free sulfhydryl groups.
摘要翻译：一种降低粘蛋白粘度的方法，其包括施用有效剂量的具有受体巯基的化合物，其在体内代谢产生游离的巯基。

129. 发明授权

US4348387A Method and system for the controlled release of biologically active substances to a body fluid 失效
标题翻译：将生物活性物质控制释放到体液的方法和系统
公开(公告)号：US4348387A
公开(公告)日：1982-09-07
申请号：US62484
申请日：1979-07-31
申请人： Michael Brownlee , Anthony Cerami
发明人： Michael Brownlee , Anthony Cerami
IPC分类号： A61K38/00 , A61K9/00 , A61K38/28 , A61K39/00 , A61K47/48 , A61M1/00 , A61M1/36 , A61M31/00 , A61P3/08 , A61K37/26 , C07C103/52
CPC分类号： A61K38/28 , A61K47/48261 , A61M31/002
摘要： A process and system for controlled delivery of a biologically active substance to an animal body fluid which comprises contacting fluid with a reversible complex of a conjugate (1) and a binding macromolecule (2), wherein the conjugate (1) comprises a biologically active portion which is intended to be proportionately released into a body fluid stream in response to varying concentration levels of a component of the body fluid stream, and a complexing substrate portion which conjugates with the biologically active portion and which is characterized by affinity to the binding macromolecule (2), competitively or non-competitively with the variable component of the body fluid; thereby causing the component present in the body fluid to complex to the binding macromolecule and thus releasing the conjugate (1) therefrom into the fluid.The process and system are particularly applicable for the glucose-controlled release of insulin and other hypoglycemic agents in the treatment of diabetes.
摘要翻译：一种用于将生物活性物质受控输送到动物体液的方法和系统，其包括使流体与缀合物（1）和结合大分子（2）的可逆复合物接触，其中所述缀合物（1）包含生物活性部分其旨在响应于体液流的组分的不同浓度水平而成比例地释放到体液中，以及与生物活性部分共轭并且其特征在于对结合大分子的亲和力的络合底物部分（ 2）与体液的可变成分竞争性或非竞争性; 从而使存在于体液中的组分与结合大分子复合，从而将共轭物（1）从其中释放到流体中。该方法和系统特别适用于糖尿病治疗中胰岛素和其他降血糖药的葡萄糖控制释放。

130. 发明授权

US4247533A Hemoglobin A.sub.1c radioimmunoassay 失效
标题翻译：血红蛋白A1c放射免疫测定
公开(公告)号：US4247533A
公开(公告)日：1981-01-27
申请号：US901618
申请日：1978-05-01
申请人： Anthony Cerami , Ronald J. Koenig , Jamshid Javid , Penelope K. Pettis
发明人： Anthony Cerami , Ronald J. Koenig , Jamshid Javid , Penelope K. Pettis
IPC分类号： G01N33/53 , C07G99/00 , C07K16/18 , G01N33/72 , G01N33/48 , B65D71/00 , G01T1/00
CPC分类号： C07K16/18 , G01N33/723 , Y10S436/804 , Y10S436/808 , Y10S436/811
摘要： Sheep antiserum developed against the human glycohemoglobin, Hb A.sub.1c, distinguishes this fraction from the major component Hb A.sub.o. Partial cross relativity is observed with Hb A.sub.1a and Hb A.sub.1b, as well as with analogous glycohemoglobins from mouse and dog hemolysates. The reactivity of the hemoglobins with this specific antiserum is abolished by the reduction of the keto group of the sugar ligand. The immunological specificity displayed provides the basis of a quantitative assay for Hb A.sub.1c, which is suitable for studies of clinical and experimental diabetes.
摘要翻译：针对人类糖基血红蛋白Hb A1c开发的羊抗血清与主要成分Hb Ao区分开。使用Hb A1a和Hb A1b以及来自小鼠和狗溶血的类似糖基血红蛋白观察到部分相对性。通过还原糖配体的酮基来消除血红蛋白与该特异性抗血清的反应性。显示的免疫学特性为Hb A1c的定量测定提供了基础，适用于临床和实验性糖尿病的研究。

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