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1. 发明申请

WO1993014201A1 DNA ENCODING A HUMAN 5-HT1F RECEPTOR AND USES THEREOF 审中-公开
标题翻译：编码人类5-HT1F受体的DNA及其用途
公开(公告)号：WO1993014201A1
公开(公告)日：1993-07-22
申请号：PCT/US1993000149
申请日：1993-01-08
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , WEINSHANK, Richard, L. , BRANCHEK, Theresa , HARTIG, Paul, R.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C12N15/00
CPC分类号： G01N33/5091 , A01K2217/05 , A61K31/70 , A61K38/00 , C07K14/70571 , G01N33/5008 , G01N33/5041 , G01N33/566 , G01N33/942 , G01N2500/00
摘要： This invention provides an isolated nucleic acid molecule encoding a human 5-HT1F receptor, an isolated protein which is a human 5-HT1F receptor, vectors comprising an isolated nucleic acid molecule encoding a human 5-HT1F receptors, mammalian cells comprising such vectors, antibodies directed to the human 5-HT1F receptor, nucleic acid probes useful for detecting nucleic acid encoding human 5-HT1F receptors, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a human 5-HT1F receptor, pharmaceutical compounds related to human 5-HT1F receptors, and nonhuman transgenic animals which express DNA a normal or a mutant human 5-HT1F receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatment involving the human 5-HT1F receptor.
摘要翻译：本发明提供了编码人5-HT1F受体的分离的核酸分子，人5-HT1F受体的分离蛋白，包含编码人5-HT1F受体的分离的核酸分子的载体，包含这种载体的哺乳动物细胞，抗体针对人5-HT1F受体，可用于检测编码人5-HT1F受体的核酸的核酸探针，与编码人5-HT1F受体的核酸分子的任何序列互补的反义寡核苷酸，与人5-HT1F受体相关的药物化合物 -HT1F受体和非人类转基因动物，其表达正常或突变型人类5-HT1F受体的DNA。本发明还提供了确定配体结合，检测表达，药物筛选和涉及人5-HT1F受体的治疗的方法。

2. 发明申请

WO9726853A3 DNA ENCODING GALANIN GALR2 RECEPTORS AND USES THEREOF 审中-公开
标题翻译： DNA编码GALANIN GALR2受体及其用途
公开(公告)号：WO9726853A3
公开(公告)日：1997-10-23
申请号：PCT/US9701301
申请日：1997-01-24
申请人： SYNAPTIC PHARMA CORP , SMITH KELLI E , GERALD CHRISTOPHE P G , WEINSHANK RICHARD L , LINEMEYER DAVID , BRANCHEK THERESA , FORRAY CARLOS
发明人： SMITH KELLI E , GERALD CHRISTOPHE P G , WEINSHANK RICHARD L , LINEMEYER DAVID , BRANCHEK THERESA , FORRAY CARLOS
IPC分类号： A01K67/027 , A61K31/00 , A61K31/70 , A61K31/7088 , A61K38/00 , A61K39/00 , A61K39/395 , A61K45/00 , A61K48/00 , A61P3/00 , A61P3/04 , A61P25/28 , A61P29/00 , C07K14/705 , C07K14/72 , C07K16/28 , C12N5/00 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , G01N33/53 , G01N33/566 , A61K
CPC分类号： C12P21/02 , A01K2217/05 , A61K38/00 , A61K39/00 , A61K48/00 , C07K14/72
摘要： This invention provides isolated nucleic acids encoding mammalian galanin receptors, isolated galanin receptor proteins, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.

3. 发明申请

WO1997026853A2 DNA ENCODING GALANIN GALR2 RECEPTORS AND USES THEREOF 审中-公开
标题翻译： DNA编码GALANIN GALR2受体及其用途
公开(公告)号：WO1997026853A2
公开(公告)日：1997-07-31
申请号：PCT/US1997001301
申请日：1997-01-24
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , SMITH, Kelli, E. , GERALD, Christophe, P., G. , WEINSHANK, Richard, L. , LINEMEYER, David , BRANCHEK, Theresa , FORRAY, Carlos
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K00/00
CPC分类号： C12P21/02 , A01K2217/05 , A61K38/00 , A61K39/00 , A61K48/00 , C07K14/72
摘要： This invention provides isolated nucleic acids encoding mammalian galanin receptors, isolated galanin receptor proteins, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.
摘要翻译：本发明提供了编码哺乳动物甘丙肽受体的分离的核酸，分离的甘丙肽受体蛋白，包含编码哺乳动物甘丙肽受体的分离的核酸的载体，包含这种载体的细胞，针对哺乳动物甘丙肽受体的抗体，用于检测编码哺乳动物甘丙肽受体，与编码哺乳动物甘丙肽受体的核酸的唯一序列互补的反义寡核苷酸，表达编码正常或突变型哺乳动物甘丙肽受体的DNA的非人转基因动物，以及确定化合物与哺乳动物甘丙肽受体结合的方法。

4. 发明申请

WO1995028157A1 USE OF ALPHA-1C SPECIFIC COMPOUNDS TO TREAT BENIGN PROSTATIC HYPERPLASIA 审中-公开
标题翻译：使用ALPHA-1C特异性化合物治疗原发性高血压
公开(公告)号：WO1995028157A1
公开(公告)日：1995-10-26
申请号：PCT/US1995004203
申请日：1995-04-04
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GLUCHOWSKI, Charles , FORRAY, Carlos, C. , CHIU, George , BRANCHEK, Theresa, A. , WETZEL, John, M. , HARTIG, Paul, R.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K31/445
CPC分类号： A61K31/55 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D211/58 , C07D401/12 , C07D405/12 , C07D495/06
摘要： The subject invention provides a method of treating benign prostatic hyperplasia or inhibiting contraction of a prostate tissue in a subject in need thereof which comprises administering to the subject a therapeutically effective amount of an alpha 1C antagonist which binds to a human alpha 1C adrenergic receptor with a binding affinity greater than 50-fold higher than the binding affinity with which the alpha 1C antagonist binds to a human alpha 1b adrenergic receptor, provided that the alpha 1C antagonist is not 2,6-Dimethyl-4-(4-nitrophenyl)-1, 4-dihydropyridine-3, 5-dicarboxylic acid N-[3-(4,4-diphenylpiperidin-1-yl)-propyl] amide ester hydrochloride hydrate.
摘要翻译：本发明提供了治疗有需要的受试者的前列腺增生或抑制前列腺组织收缩的方法，其包括向受试者施用治疗有效量的α1C拮抗剂，其与α1肾上腺素能受体结合结合亲和力大于α1C拮抗剂与α1α拮抗剂与人α1b肾上腺素能受体结合的结合亲和力的50倍，条件是α1C拮抗剂不是2,6-二甲基-4-（4-硝基苯基）-1 ，4-二氢吡啶-3,5-二羧酸N- [3-（4,4-二苯基哌啶-1-基） - 丙基]酰胺酯盐酸盐水合物。

5. 发明申请

WO1994014957A2 DNA ENCODING 5-HT4 SEROTONIN RECEPTORS AND USES THEREOF 审中-公开
标题翻译： DNA编码5-HT4丝氨酸受体及其用途
公开(公告)号：WO1994014957A2
公开(公告)日：1994-07-07
申请号：PCT/US1993012586
申请日：1993-12-22
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GERALD, Christophe , HARTIG, Paul , BRANCHEK, Theresa, A. , WEINSHANK, Richard, L.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C12N15/00
CPC分类号： C07K14/70571
摘要： This invention provides an isolated nucleic acid molecule encoding a mammalian 5-HT4 receptor and an isolated nucleic acid molecule encoding a human 5-HT4 receptor, an isolated protein which is a mammalian 5-HT4 receptor, an isolated protein which is a human 5-HT4 receptor, vectors comprising an isolated nucleic acid molecule encoding a mammalian 5-HT4 receptor, vectors comprising an isolated nucleic acid molecule encoding a human 5-HT4 receptor, mammalian cells comprising such vectors, antibodies directed to the 5-HT4 receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian or human 5-HT4 receptor, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a mammalian or human 5-HT4 receptor, pharmaceutical compounds related to the human 5-HT4 receptor, and nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian or human 5-HT4 receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with a human 5-HT4 receptor.
摘要翻译：本发明提供编码哺乳动物5-HT4受体的分离的核酸分子和编码人5-HT 4受体的分离的核酸分子，分离的核酸分子是哺乳动物5-HT 4受体，分离的蛋白质，其是人5- HT4受体，包含编码哺乳动物5-HT4受体的分离的核酸分子的载体，包含编码人5-HT 4受体的分离的核酸分子的载体，包含该载体的哺乳动物细胞，针对5-HT 4受体的抗体，核酸可用于检测编码哺乳动物或人类5-HT4受体的核酸的探针，与编码哺乳动物或人类5-HT4受体的核酸分子的任何序列互补的反义寡核苷酸，与人5-HT 4受体相关的药物化合物，和表达编码正常或突变的哺乳动物或人类5-HT4受体的DNA的非人类转基因动物。本发明还提供了用于确定配体结合，检测表达，药物筛选和用于减轻与人5-HT 4受体相关的异常的治疗的方法。

6. 发明申请

WO1994010989A1 USE OF ALPHA-1C SPECIFIC COMPOUNDS TO TREAT BENIGN PROSTATIC HYPERPLASIA 审中-公开
标题翻译：使用ALPHA-1C特异性化合物治疗原发性高血压
公开(公告)号：WO1994010989A1
公开(公告)日：1994-05-26
申请号：PCT/US1993010950
申请日：1993-11-12
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GLUCHOWSKI, Charles , FORRAY, Carlos, C. , CHIU, George , BRANCHEK, Theresa, A. , WETZEL, John, M. , HARTIG, Paul, R.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K31/135
CPC分类号： C07D401/12 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , A61K31/55 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D211/58 , C07D405/12 , C07D495/06
摘要： A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human alpha 1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human alpha 1A adrenergic receptor, a human alpha 1B adrenergic receptor and a human histamine H1 receptor, and, binds to a human alpha 2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such alpha 1C adrenergic receptor. Compounds meeting these criteria are provided.
摘要翻译：一种治疗受试者的良性前列腺增生的方法，其包括向所述受试者施用治疗有效量的结合人α1C肾上腺素能受体的化合物，所述化合物的结合亲和力比结合亲和力高10倍，与人α1B肾上腺素能受体，人α1B肾上腺素能受体和人组胺H1受体结合，并结合人α2肾上腺素能受体，其结合亲和力比其结合亲和力低10倍该化合物与这种α1C肾上腺素能受体结合。提供符合这些标准的化合物。

7. 发明申请

WO1994009828A1 DNA ENCODING A HUMAN SEROTONIN RECEPTOR (5-HT4B) AND USES THEREOF 审中-公开
标题翻译：编码人类SEROTONIN受体（5-HT4B）的DNA及其用途
公开(公告)号：WO1994009828A1
公开(公告)日：1994-05-11
申请号：PCT/US1993010553
申请日：1993-10-29
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , BARD, Jonathan, A. , BRANCHEK, Theresa , WEINSHANK, Richard, L.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K48/00
CPC分类号： C12N15/8509 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2217/072 , A01K2217/075 , A01K2227/10 , A01K2227/105 , A01K2267/03 , A01K2267/0356 , A01K2267/0375 , A61K38/00 , C07K14/70571
摘要： This invention provides an isolated nucleic acid molecule encoding a mammalian 5-HT4B receptor and an isolated nucleic acid molecule encoding a human 5-HT4B receptor, an isolated protein which is mammalian 5-HT4B receptor, vectors comprising an isolated nucleic acid molecule encoding a mammalian 5-HT4B receptor, vectors comprising an isolated nucleic acid molecule encoding a human 5-HT4B receptor, mammalian cells comprising such vectors, antibodies directed to the 5-HT4B receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian or human 5-HT4B receptor, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a mammalian or human 5-HT4B receptor, pharmaceutical compounds related to the human 5-HT4B receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with a human 5-HT4B receptor.
摘要翻译：本发明提供编码哺乳动物5-HT4B受体的分离的核酸分子和编码人5-HT4B受体的分离的核酸分子，其是哺乳动物5-HT4B受体的分离的蛋白质，载体包含编码哺乳动物的分离的核酸分子 5-HT4B受体的载体，包含编码人5-HT4B受体的分离的核酸分子的载体，包含这种载体的哺乳动物细胞，针对5-HT4B受体的抗体，用于检测编码哺乳动物或人5- HT4B受体，与编码哺乳动物或人类5-HT4B受体的核酸分子的任何序列互补的反义寡核苷酸，与人5-HT4B受体相关的药物化合物。本发明还提供了用于确定配体结合，检测表达，药物筛选和用于减轻与人5-HT4B受体相关的异常的治疗的方法。

8. 发明申请

WO1997046250A1 METHODS OF MODIFYING FEEDING BEHAVIOR, COMPOUNDS USEFUL IN SUCH METHODS, AND DNA ENCODING A HYPOTHALAMIC ATYPICAL NEUROPEPTIDE Y/PEPTIDE YY RECEPTOR (Y5) 审中-公开
标题翻译：改良饲料行为的方法，这种方法有用的化合物和编码高血压神经元神经营养素Y /肽受体（Y5）的DNA
公开(公告)号：WO1997046250A1
公开(公告)日：1997-12-11
申请号：PCT/US1997009504
申请日：1997-06-04
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GERALD, Christophe, P., G. , WEINSHANK, Richard, L. , WALKER, Mary, W. , BRANCHEK, Theresa
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K38/02
CPC分类号： C07K14/70571 , A01K2217/05 , A61K38/00
摘要： The invention provides methods of modifying feeding behavior, including increasing or decreasing food consumption, e.g., in connection with treating obesity, bulimia or anorexia. These methods involve administration of compounds that are selective agonists or antagonists for the Y5 receptor. One such compound has structure (I). In addition, this invention provides an isolated nucleic acid molecule encoding a Y5 receptor, an isolated Y5 receptor protein, vectors comprising an isolated nucleic acid molecule encoding a Y5 receptor, cells comprising such vectors, antibodies directed to the Y5 receptor, nucleic acid probes useful for detecting nucleic acid encoding Y5 receptors, antisense aligonucleotides complementary to any unique sequences of a nucleic acid molecule which encodes a Y5 receptor, and nonhuman transgenic animals which express DNA encoding a normal or a mutant Y5 receptor.
摘要翻译：本发明提供了改变进食行为的方法，包括增加或减少食物消耗，例如与治疗肥胖，贪食或厌食有关的方法。这些方法包括施用作为Y5受体的选择性激动剂或拮抗剂的化合物。一种这样的化合物具有结构（I）。此外，本发明提供编码Y5受体，分离的Y5受体蛋白质的分离的核酸分子，包含编码Y5受体的分离的核酸分子的载体，包含该载体的细胞，针对Y5受体的抗体，有用的核酸探针用于检测编码Y5受体的核酸，与编码Y5受体的核酸分子的任何独特序列互补的反义寡核苷酸，以及表达编码正常或突变Y5受体的DNA的非人转基因动物。

9. 发明申请

WO1996011006A1 5-HT1F MEDIATED INHIBITION OF NEUROGENIC MENINGEAL EXTRAVASATION 审中-公开
标题翻译： 5-HT1F介导的神经源性男性外阴性的抑制作用
公开(公告)号：WO1996011006A1
公开(公告)日：1996-04-18
申请号：PCT/US1995013010
申请日：1995-10-03
申请人： ELI LILLY AND COMPANY , AUDIA, James, Edmund , BRANCHEK, Theresa , COHEN, Marlene, Lois , JOHNSON, Kirk, Willis , PHEBUS, Lee, Alan
发明人： ELI LILLY AND COMPANY
IPC分类号： A61K31/445
CPC分类号： A61K31/135 , A61K31/00 , A61K31/403 , A61K31/4045 , A61K31/454 , A61K31/48
摘要： The present invention provides a method for the treatment of migraine and associated disorders which relies on a novel mechanism of action. By treating a migraineur with compounds or compositions which are selective agonists of 5-HT1F receptors relative to other serotonin receptors which produce unwanted effects like vasoconstriction, the neurogenic meningeal extravasation which leads to the pain of migraine is inhibited and the physiological liabilities of compounds exhibiting vasoconstriction or other side effects are avoided.
摘要翻译：本发明提供了一种依赖于新的作用机制的偏头痛和相关疾病的治疗方法。通过用相对于产生不想要的血管收缩作用的其他5-羟色胺受体的5-羟色胺受体的选择性激动剂的化合物或组合物来治疗偏头痛，导致偏头痛的神经源性脑膜外渗受到抑制，并且具有血管收缩的化合物的生理负荷或其他副作用。

10. 发明申请

WO1995021245A1 NUCLEIC ACID ENCODING NEUROPEPTIDE Y/PEPTIDE YY (Y2) RECEPTORS AND USES THEREOF 审中-公开
标题翻译：核酸编码神经元Y /肽YY（Y2）受体及其用途
公开(公告)号：WO1995021245A1
公开(公告)日：1995-08-10
申请号：PCT/US1995001469
申请日：1995-02-03
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GERALD, Christophe , WALKER, Mary, W. , BRANCHEK, Theresa , WEINSHANK, Richard
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C12N05/10
CPC分类号： C07K14/70571 , A01K2217/05 , A61K38/00 , C12N2799/026
摘要： This invention provides isolated nucleic acid molecules encoding Y2 receptors, an isolated, purified Y2 receptor protein, vectors comprising isolated nucleic acid molecules encoding Y2 receptors, mammalian, insect, bacterial and yeast cells comprising such vectors, antibodies directed to the Y2 receptors, nucleic acid probes useful for detecting nucleic acid encoding Y2 receptors, antisense oligonucleotides complementary to unique sequences of a nucleic acid molecule which encodes a Y2 receptor, pharmaceutical compounds related to the Y2 receptors, and nonhuman transgenic animals which express nucleic acid encoding a normal or mutant Y2 receptor. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and methods of treatment involving Y2 receptors.
摘要翻译：本发明提供编码Y2受体的分离的核酸分子，分离的，纯化的Y2受体蛋白，包含编码Y2受体的分离的核酸分子，包含这种载体的哺乳动物，昆虫，细菌和酵母细胞的载体，针对Y2受体的抗体，核酸可用于检测编码Y2受体的核酸的探针，与编码Y2受体的核酸分子的唯一序列互补的反义寡核苷酸，与Y2受体相关的药物化合物和表达编码正常或突变的Y2受体的核酸的非人转基因动物。本发明还提供了确定配体结合，检测表达，药物筛选和涉及Y2受体的治疗方法的方法。

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