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41. 发明授权

US6063759A Conjugate of biologically active compound and polar lipid conjugated to a microparticle for biological targeting 失效
公开(公告)号：US6063759A
公开(公告)日：2000-05-16
申请号：US60011
申请日：1998-04-14
申请人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
发明人： Milton B. Yatvin , Michael H B Stowell , Vincent S. Gallicchio , Michael J. Meredith
IPC分类号： A61K9/16 , A61K47/48 , C07H19/06 , C07H19/10 , C12N5/08 , A01N37/18 , A61K9/127 , A61K47/00 , C07K17/00
CPC分类号： A61K9/167 , A61K47/48046 , A61K47/48053 , A61K47/48315 , A61K47/48884 , B82Y5/00 , C07H19/06 , C07H19/10 , Y10S530/811 , Y10S530/813 , Y10S530/814 , Y10S530/815
摘要： Methods and reagents are provided for specifically targeting biologically active compounds such as antiviral and antimicrobial drugs, or prodrugs containing the biologically active compound to specific sites such as specific organelles in phagocytic mammalian cells. The biologically active compound or prodrug is linked to a microparticle with a linker that is non-specifically or specifically cleaved inside a phagocytic mammalian cell. Alternatively, the biologically active compound or prodrug is impregnated into a porous microparticle or coated on a nonporous microparticle, and then coated with a coating material that is non-specifically or specifically degraded inside a phagocytic mammalian cell. The prodrug contains the biologically active compound linked to a polar lipid such as ceramide with a specific linker such as a peptide that is specifically cleaved to activate the prodrug in a phagocytic mammalian cell infected with a microorganism. A microparticle linked antimicrobial drug or prodrug may be used for killing a microorganism infecting a phagocytic mammalian cell in vivo or in vitro.

42. 发明授权

US6046011A Mammalian adrenocorticotropic hormone receptors and uses 失效
标题翻译：哺乳动物促肾上腺皮质激素受体和用途
公开(公告)号：US6046011A
公开(公告)日：2000-04-04
申请号：US105298
申请日：1998-06-26
申请人： Roger D. Cone , Kathleen G. Mountjoy
发明人： Roger D. Cone , Kathleen G. Mountjoy
IPC分类号： C07H21/04 , C07K14/72 , C12N5/06 , C12N15/12 , C12P21/08 , C12Q1/68 , G01N33/566 , G01N33/567 , G01N33/74
CPC分类号： G01N33/566 , C07K14/723 , C12Q1/6876 , G01N33/74 , C12Q2600/158 , G01N2333/695 , G01N2333/72 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to a mammalian adrenocorticotropic hormone receptor. The invention is directed toward the isolation, characterization and pharmacological use of mammalian adreocorticotropic hormone receptor, the gene corresponding to this receptor, a recombinant eukaryotic expression construct capable of expressing a mammalian adrenocorticotropic hormone receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize mammalian adrenocorticotropic hormone receptor. The invention also provides methods for screening ACTH-R agonists and antagonists in vitro using prerations of receptor from such cultures of eukaryotic cells transformed with a recombinant eukaryotic expression construct comprising the ACTH-R receptor gene. The invention specifically provides human and bovine ACTH-R genes.
摘要翻译：本发明涉及哺乳动物促肾上腺皮质激素受体。本发明涉及哺乳动物促肾上腺皮质激素受体的分离，表征和药理学应用，该受体是相应于该受体的基因，能够在转化真核细胞的培养物中表达哺乳动物促肾上腺皮质激素受体的重组真核表达构建体和转化的真核生物合成哺乳动物促肾上腺皮质激素受体的细胞。本发明还提供了使用由包含ACTH-R受体基因的重组真核表达构建体转化的真核细胞的这种培养物的受体的预测体外筛选ACTH-R激动剂和拮抗剂的方法。本发明特别提供人和牛ACTH-R基因。

43. 发明授权

US5994087A Mammalian melanocortin receptors and uses 失效
标题翻译：哺乳动物黑皮质素受体和用途
公开(公告)号：US5994087A
公开(公告)日：1999-11-30
申请号：US475637
申请日：1995-06-07
申请人： Roger D. Cone , Linda Roselli-Rehfuss , Kathleen G. Mountjoy , Linda S. Robbins
发明人： Roger D. Cone , Linda Roselli-Rehfuss , Kathleen G. Mountjoy , Linda S. Robbins
IPC分类号： C07K14/72 , C12N15/12 , G01N33/74 , G01N33/567 , G01N33/48 , G01N33/53 , G01N33/574
CPC分类号： G01N33/74 , C07K14/723
摘要： The present invention relates to a mammalian melanocortin receptor. The invention is directed toward the isolation, characterization and pharmacological use of a mammalian melanocortin receptor (MC3-R). The invention specifically provides a particular melanocortin receptor, termed MC3-R, isolated as a complementary DNA copy of mRNA corresponding to the gene for this receptor in rats. Also provided is a eukaryotic recombinant expression construct capable of expressing a mammalian melanocortin receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize a mammalian melanocortin receptor. The invention also provides methods for screening in vitro agonists and antagonists of such a melanocortin receptor using preparations of receptor protein from such cultures of eukaryotic cells transformed with a recombinant expression construct.
摘要翻译：本发明涉及哺乳动物黑皮质素受体。本发明涉及哺乳动物黑皮质素受体（MC3-R）的分离，表征和药理学应用。本发明特别提供了一种称为MC3-R的特异性黑皮质素受体，其被分离为相应于大鼠该受体基因的mRNA的互补DNA拷贝。还提供了能够在转化的真核细胞和合成哺乳动物黑皮质素受体的转化真核细胞的这种培养物中表达哺乳动物黑皮质素受体的真核重组表达构建体。本发明还提供了使用来自用重组表达构建体转化的真核细胞的这种培养物的受体蛋白质的制备物筛选这种黑皮质素受体的体外激动剂和拮抗剂的方法。

44. 发明授权

US5882926A Excitatory amino acid transporter gene and uses 失效
标题翻译：兴奋性氨基酸转运蛋白基因及用途
公开(公告)号：US5882926A
公开(公告)日：1999-03-16
申请号：US948569
申请日：1997-10-10
申请人： Susan G. Amara , Jeffrey L. Arriza , Scott Eliasof , Michael P. Kavanaugh
发明人： Susan G. Amara , Jeffrey L. Arriza , Scott Eliasof , Michael P. Kavanaugh
IPC分类号： A61K38/00 , C07K14/47 , C12N5/00 , C07H21/04 , C07K1/00 , C12N15/00
CPC分类号： C07K14/47 , A61K38/00 , C07K2319/00 , C12N2799/023
摘要： This invention relates to novel mammalian excitatory amino acid transporter proteins and genes encoding such proteins. The invention is directed towards the isolation, characterization and use of human excitatory amino acid transporter proteins for pharmacological screening of analogues, agonists, antagonists, inhibitors, modulators and facilitators of excitatory amino acid transport in a variety of tissues, particularly neuronal tissues. This invention provides isolated nucleic acid encoding a novel excitatory amino acid transporter subtype that is specifically expressed in retina. Also provided are recombinant expression constructs capable of expressing this novel transporter in transformed prokaryotic and eukaryotic cells, and also provides such transformed cell cultures producing the novel human transporter. Purified transporter protein and membranes comprising the transporter protein are also provided. The invention provides methods of screening compounds in vitro for transporter binding properties using said preparations of protein and membranes from transformed cell cultures, as well as from amphibian oocytes expressing the human transporter protein provided herein.
摘要翻译：本发明涉及新型的哺乳动物兴奋性氨基酸转运蛋白和编码这种蛋白质的基因。本发明涉及人类兴奋性氨基酸转运蛋白的分离，表征和用途，用于药物筛选各种组织，特别是神经元组织中兴奋性氨基酸转运的类似物，激动剂，拮抗剂，抑制剂，调节剂和促进剂。本发明提供编码在视网膜中特异性表达的新型兴奋性氨基酸转运子亚型的分离的核酸。还提供了能够在转化的原核和真核细胞中表达该新型转运蛋白的重组表达构建体，并且还提供产生新型人转运蛋白的转化细胞培养物。还提供了纯化的转运蛋白和包含转运蛋白的膜。本发明提供了使用所述来自转化细胞培养物的蛋白质和膜的制备以及来自表达本文提供的人类转运蛋白的两栖动物卵母细胞的体外筛选化合物的转运蛋白结合特性的方法。

45. 发明授权

US5880260A Dopamine receptors and genes 失效
公开(公告)号：US5880260A
公开(公告)日：1999-03-09
申请号：US474892
申请日：1995-06-07
申请人： Olivier Civelli , James R. Bunzow , David K. Grandy , Curtis A. Machida
发明人： Olivier Civelli , James R. Bunzow , David K. Grandy , Curtis A. Machida
IPC分类号： A61K38/00 , C07K14/705 , C07K16/28 , C12N15/00 , C12N15/12 , C12Q1/68
CPC分类号： C07K14/70571 , C07K16/286 , C12N15/00 , C12Q1/6876 , A01K2217/05 , A61K38/00 , C12Q2600/158
摘要： A mammalian D.sub.2 dopamine receptor gene has been cloned. Thus, DNA sequences encoding all or a part of the dopamine receptor are provided, as well as the corresponding polypeptide sequences and methods for producing the same both synthetically and via expression of a corresponding sequence from a host transformed with a suitable vector carrying the corresponding DNA sequence. The various structural information provided by this invention enables the preparation of labeled or unlabeled immunospecific species, particularly antibodies, as well as nucleic acid probes labeled in conventional fashion. Pharmaceutical compositions and methods of using various products of this invention are also provided.

46. 发明授权

US5744594A DNA encoding ATP-sensitive potassium channel genes 失效
标题翻译：编码ATP敏感钾通道基因的DNA
公开(公告)号：US5744594A
公开(公告)日：1998-04-28
申请号：US385186
申请日：1995-02-07
申请人： John P. Adelman , Michael J. Ashford , Chris T. Bond
发明人： John P. Adelman , Michael J. Ashford , Chris T. Bond
IPC分类号： C07K14/705 , C07H21/02 , C07H21/04
CPC分类号： C07K14/705
摘要： This invention relates to DNA and protein compositions useful in the diagnosis and treatment of diabetes, heart disease and skeletal muscle disease. More specifically, this invention relates to DNA and protein compositions for ATP-sensitive potassium channel proteins, and methods of using these compositions.
摘要翻译：本发明涉及可用于诊断和治疗糖尿病，心脏病和骨骼肌疾病的DNA和蛋白质组合物。更具体地，本发明涉及ATP敏感性钾通道蛋白质的DNA和蛋白质组合物，以及使用这些组合物的方法。

47. 发明授权

US5738999A L-AP4 sensitive glutamate receptors 失效
标题翻译： L-AP4敏感谷氨酸受体
公开(公告)号：US5738999A
公开(公告)日：1998-04-14
申请号：US453862
申请日：1995-05-30
申请人： Thomas P. Segerson , J. Mark Kinzie , Eileen R. Mulvihill , Julie A. Saugstad , Gary L. Westbrook
发明人： Thomas P. Segerson , J. Mark Kinzie , Eileen R. Mulvihill , Julie A. Saugstad , Gary L. Westbrook
IPC分类号： C07K14/705 , C07K16/28 , G01N33/566
CPC分类号： C07K14/70571
摘要： Metabotropic receptor mGluR7 is identified and sequenced. The mGluR7 receptor subfamily mediates inhibition of transmitter release at selected glutamatergic synapses. The receptors, mGluR7-specific peptides and antibodies thereto are used to identify agonists and antagonists of G protein coupled glutamate receptor mediated neuronal transmitter release, as well as in methods of diagnosis and therapy.
摘要翻译：鉴定和测序代谢受体mGluR7。 mGluR7受体亚家族在选择的谷氨酸能突触中介导发射体释放的抑制。受体，mGluR7特异性肽及其抗体用于鉴定G蛋白偶联谷氨酸受体介导的神经元发射体释放的激动剂和拮抗剂，以及诊断和治疗方法。

48. 发明授权

US5698438A Bacterial hemoglobin receptor gene 失效
标题翻译：细菌血红蛋白受体基因
公开(公告)号：US5698438A
公开(公告)日：1997-12-16
申请号：US326670
申请日：1994-10-18
申请人： Igor Stojiljkovic , Magdalene So , Vivian Hwa , Fred Heffron , Xavier Nassif
发明人： Igor Stojiljkovic , Magdalene So , Vivian Hwa , Fred Heffron , Xavier Nassif
IPC分类号： A61K38/00 , A61K39/00 , C07K14/22 , C12N1/21 , C12N15/31 , C12N15/74
CPC分类号： C07K14/22 , A61K38/00 , A61K39/00 , Y10S530/825
摘要： The present invention relates to a novel bacterial hemoglobin receptor protein and genes that encode such a protein. The invention is directed toward the isolation, characterization, diagnostic and therapeutic use of a bacterial hemoglobin receptor protein, nucleic acid encoding such a protein, recombinant expression constructs comprising such nucleic acids and cells transformed therewith, and antibodies and epitopes of such hemoglobin receptor proteins. The invention relates particularly to hemoglobin receptor proteins and genes encoding such proteins from Neisseria species, especially N. meningitidis. Methods for the diagnostic and therapeutic use of the proteins, epitopes, antibodies and nucleic acids of the invention are also provided, including the use of the proteins, epitopes, antibodies and nucleic acids of the invention for the production of vaccines effective in providing immunization of a human against infection by pathogenic bacteria of Neisseria species.
摘要翻译：本发明涉及一种新的细菌性血红蛋白受体蛋白质和编码这种蛋白质的基因。本发明涉及细菌血红蛋白受体蛋白的分离，表征，诊断和治疗用途，编码这种蛋白质的核酸，包含这种核酸的重组表达构建体和与其转化的细胞，以及这些血红蛋白受体蛋白的抗体和表位。本发明特别涉及血红蛋白受体蛋白和编码奈瑟氏球菌（Neisseria），特别是脑膜炎奈瑟氏菌（N脑膜炎奈瑟氏球菌）的蛋白质的基因。还提供了本发明的蛋白质，表位，抗体和核酸的诊断和治疗用途的方法，包括使用本发明的蛋白质，表位，抗体和核酸来生产有效提供免疫的疫苗一种人抵抗奈瑟氏球菌病原菌的感染。

49. 发明授权

US5597922A Glycine receptor antagonist pharmacophore 失效
标题翻译：甘氨酸受体拮抗剂药效团
公开(公告)号：US5597922A
公开(公告)日：1997-01-28
申请号：US281995
申请日：1994-07-29
申请人： Sui X. Cai , John F. W. Keana , Eckard Weber
发明人： Sui X. Cai , John F. W. Keana , Eckard Weber
IPC分类号： A61K31/404 , A61K31/4184 , A61K31/47 , A61K31/4704 , A61K31/498 , A61K31/5025 , A61K31/517 , A61K31/536 , A61K31/538 , A61K31/55 , A61K31/551 , A61K31/553 , C07B59/00 , C07D209/34 , C07D209/38 , C07D215/22 , C07D215/227 , C07D215/38 , C07D223/16 , C07D235/26 , C07D235/28 , C07D241/38 , C07D241/44 , C07D241/52 , C07D243/24 , C07D245/06 , C07D265/26 , C07D265/36 , C07F5/02 , A61K31/495 , A61K31/535
CPC分类号： C07D215/227 , A61K31/404 , A61K31/4184 , A61K31/47 , A61K31/4704 , A61K31/498 , A61K31/5025 , A61K31/517 , A61K31/536 , A61K31/538 , A61K31/55 , A61K31/551 , A61K31/553 , C07B59/002 , C07D209/34 , C07D209/38 , C07D215/22 , C07D215/38 , C07D223/16 , C07D235/26 , C07D235/28 , C07D241/38 , C07D241/44 , C07D241/52 , C07D243/24 , C07D245/06 , C07D265/26 , C07D265/36 , C07F5/02 , C07F5/025
摘要： Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
摘要翻译：治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防多动症的不良后果通过向需要这种治疗的动物施用与甘氨酸受体具有高结合性的化合物来公开兴奋性氨基酸以及治疗焦虑症，慢性疼痛，抽搐和诱导麻醉。

50. 发明授权

US5554729A Mammalian adrenocorticotropic hormone receptors and uses 失效
标题翻译：哺乳动物促肾上腺皮质激素受体和用途
公开(公告)号：US5554729A
公开(公告)日：1996-09-10
申请号：US77673
申请日：1993-06-15
申请人： Roger D. Cone , Kathleen G. Mountjoy
发明人： Roger D. Cone , Kathleen G. Mountjoy
IPC分类号： C07H21/04 , C07K14/72 , C12N5/06 , C12N15/12 , C12P21/08 , C12Q1/68 , G01N33/566 , G01N33/567 , G01N33/74 , C07K14/705 , C07K14/71
CPC分类号： G01N33/566 , C07K14/723 , C12Q1/6876 , G01N33/74 , C12Q2600/158 , G01N2333/695 , G01N2333/72 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to a mammalian adrenocorticotropic hormone receptor. The invention is directed toward the isolation, characterization and pharmacological use of mammalian adrenocorticotropic hormone receptor, the gene corresponding to this receptor, a recombinant eukaryotic expression construct capable of expressing a mammalian adrenocorticotropic hormone receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that synthesize mammalian adrenocorticotropic hormone receptor. The invention also provides methods for screening ACTH.sup.R agonists and antagonists in vitro using preparations of receptor from such cultures of eukaryotic cells transformed with a recombinant eukaryotic expression construct comprising the ACTH.sup.R receptor gene. The invention specifically provides human and bovine ACTH.sup.R genes.
摘要翻译：本发明涉及哺乳动物促肾上腺皮质激素受体。本发明涉及哺乳动物促肾上腺皮质激素受体的分离，表征和药理学应用，该受体是相应于该受体的基因，能够在转化的真核细胞和转化真核生物培养物中表达哺乳动物促肾上腺皮质激素受体的重组真核表达构建体合成哺乳动物促肾上腺皮质激素受体的细胞。本发明还提供了使用由包含ACTHR受体基因的重组真核表达构建体转化的真核细胞的这种培养物的受体制备体外筛选ACTHR激动剂和拮抗剂的方法。本发明特别提供人和牛ACTHR基因。

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