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1. 发明申请

WO2006012603A2 ANALOGS OF ISOVALERAMIDE, A PHARMACEUTICAL COMPOSITION INCLUDING THE SAME, AND A METHOD OF TREATING CENTRAL NERVOUS SYSTEM CONDITIONS OR DISEASES 审中-公开
标题翻译：异戊酰胺的类似物，包括其的药物组合物以及治疗中枢神经系统病症或疾病的方法
公开(公告)号：WO2006012603A2
公开(公告)日：2006-02-02
申请号：PCT/US2005/026279
申请日：2005-07-22
申请人： NPS PHARMACEUTICALS, INC. , ARTMAN, Linda, D. , BALANDRIN, Manuel, F. , MOE, Scott, T. , VAN WAGENEN, Bradford, C. , PESYAN, Amir
发明人： ARTMAN, Linda, D. , BALANDRIN, Manuel, F. , MOE, Scott, T. , VAN WAGENEN, Bradford, C. , PESYAN, Amir
IPC分类号： A61K31/00
CPC分类号： C07C53/126 , C07C233/05 , C07C233/08 , C07C233/58 , C07C237/06 , C07C237/14 , C07C309/04 , C07C2601/14
摘要： An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.
摘要翻译：与异戊酰胺相比，异戊酰胺类似物具有增强的效力，增加的半衰期和增加的稳定性中的至少一种。异戊酰胺类似物是环状类似物或非环状类似物。异戊酰胺类似物配制成药物组合物。还公开了治疗中枢神经系统病症或疾病的方法。该方法包括对患有中枢神经系统病症或疾病的患者施用异戊酰胺类似物。

2. 发明申请

WO1997037967A1 CALCILYTIC COMPOUNDS 审中-公开
标题翻译：计算化合物
公开(公告)号：WO1997037967A1
公开(公告)日：1997-10-16
申请号：PCT/US1997005558
申请日：1997-04-04
申请人： NPS PHARMACEUTICALS, INC. , SMITHKLINE BEECHAM PLC , SMITHKLINE BEECHAM
发明人： NPS PHARMACEUTICALS, INC. , SMITHKLINE BEECHAM PLC , SMITHKLINE BEECHAM , VAN WAGENEN, Bradford, C. , DEL MAR, Eric, G. , SHEEHAN, Derek , BARMORE, Robert, M. , KEENAN, Richard, M. , KOTECHA, Nikesh, R. , THOMPSON, Mervyn , CALLAHAN, James, F.
IPC分类号： C07C217/34
CPC分类号： C07C311/29 , A61K31/137 , A61K31/18 , A61K31/277 , C07C217/30 , C07C217/60 , C07C217/62 , C07C255/46 , C07C255/54 , C07C323/25 , C07C2601/14 , C07C2603/74 , C07D213/65 , C07D317/58 , C07D333/70
摘要： The present invention features calcilytic compounds. "Calcilytic compounds" refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
摘要翻译：本发明具有钙化合物。 “钙化合物”是指能够抑制钙受体活性的化合物。还描述了使用钙化合物抑制钙受体活性和/或在患者中获得有益效果; 以及可用于获得另外的钙化合物的技术。

3. 发明申请

WO1997041090A1 INORGANIC ION RECEPTOR-ACTIVE COMPOUNDS 审中-公开
标题翻译：无机离子受体活性化合物
公开(公告)号：WO1997041090A1
公开(公告)日：1997-11-06
申请号：PCT/US1997007371
申请日：1997-04-30
申请人： NPS PHARMACEUTICALS, INC.
发明人： NPS PHARMACEUTICALS, INC. , MOE, Scott, T. , VAN WAGENEN, Bradford, C. , DELMAR, Eric, G. , TROVATO, Richard , BALANDRIN, Manuel, F.
IPC分类号： C07C211/27
CPC分类号： C07C255/58 , A61K31/137 , A61K31/36 , C07C211/29 , C07C211/30 , C07C217/58 , C07C217/62 , C07C255/54 , C07C2601/02 , C07D307/81 , C07D317/58
摘要： The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.
摘要翻译：本发明的特征在于能够调节一种或多种无机离子受体的活性的化合物和使用这些化合物治疗疾病或病症的方法。优选的化合物可以模拟或阻断细胞外钙对细胞表面钙受体的作用。

4. 发明申请

WO1994018959A1 CALCIUM RECEPTOR-ACTIVE MOLECULES 审中-公开
标题翻译：钙受体活性分子
公开(公告)号：WO1994018959A1
公开(公告)日：1994-09-01
申请号：PCT/US1993001642
申请日：1993-02-23
申请人： BRIGHAM AND WOMEN'S HOSPITAL, INC. , NPS PHARMACEUTICALS, INC.
发明人： BRIGHAM AND WOMEN'S HOSPITAL, INC. , NPS PHARMACEUTICALS, INC. , NEMETH, Edward, F. , BROWN, Edward, M. , HEBERT, Steven, C. , VAN WAGENEN, Bradford, C. , BALANDRIN, Manuel, F. , FULLER, Forrest, H. , DEL MAR, Eric, G.
IPC分类号： A61K31/00
CPC分类号： A61K31/70 , A01K2217/05 , A01K2217/075 , A01K2217/30 , A01K2227/10 , A01K2267/03 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/195 , A61K31/235 , A61K31/275 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/55 , C07K14/705 , C07K2319/00 , C12N15/8509
摘要： Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more inorganic-ion receptor. Novel compounds useful in these methods and compositions are also provided. The method includes administering to the patient a therapeutically effective amount of a molecule active at one or more inorganic-ion receptors as an agent or antagonist. Preferably, the molecule is able to act as either a selective agonist or antagonist at a Ca receptor of one or more but not all cells chosen from the group consisting of parathyroid cells, bone osteoclasts, juxtaglomerular kidney cells, proximal tubule kidney cells, distal tubule kidney cell, cell of the thick ascending limb of Henle's loop and/or collecting duct, keratinocyte in the epidermis, parafollicular cell in the thyroid (C-cells), intestinal cell, trophoblast in the placenta, platelet, vascular smooth muscle cell, cardiac atrial cell, gastrin and glucagon secreting cells, kidney mesangial cell and mammary cell.
摘要翻译：用于治疗患有特征在于异常水平的一种或多种组分的患者的方法和组合物，其活性受一种或多种无机离子受体的活性调节或影响。还提供了可用于这些方法和组合物的新型化合物。该方法包括向患者施用治疗有效量的一种或多种作为药剂或拮抗剂的无机 - 离子受体活性的分子。优选地，该分子能够作为一种或多种但不是全部选自甲状旁腺细胞，骨破骨细胞，近肾小球肾细胞，近端小管肾的Ca 2+受体的选择性激动剂或拮抗剂细胞，远端肾小管肾细胞，亨利循环和/或收集管，上皮角质形成细胞，甲状腺旁淋巴细胞（C细胞），肠细胞，胎盘滋养细胞，血小板，血管平滑肌肉细胞，心房心房细胞，胃泌素和胰高血糖素分泌细胞，肾系膜细胞和乳腺细胞。

5. 发明申请

WO1997011934A1 CHIRAL REDUCTIONS OF IMINES LEADING TO THE SYNTHESES OF OPTICALLY ACTIVE AMINES 审中-公开
标题翻译：导致光活性氨基酸合成的基因组的减少
公开(公告)号：WO1997011934A1
公开(公告)日：1997-04-03
申请号：PCT/US1996015506
申请日：1996-09-27
申请人： NPS PHARMACEUTICALS, INC.
发明人： NPS PHARMACEUTICALS, INC. , VAN WAGENEN, Bradford, C. , BARMORE, Robert, M.
IPC分类号： C07C209/52
CPC分类号： C07C209/52
摘要： A process for preparing an R enantiomer of a compound of formula (I) wherein Me is methyl, Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF3, CF2H, CFH2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH2CF3, OH, CN, NO2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH-Me), C(O)N-lower alkyl2 (e.g., C(O)NMe2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH-C(O)-lower alkyl (e.g., NH-C(O)Me), where "lower alkyl" is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I). The process is especially useful to produce compounds (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorophenyl)propanamine and (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(phenyl)propanamine. Enantiomeric excess of the R enantiomer over S enantiomer of greater than 65 % have been achieved.
摘要翻译：制备式（I）化合物的R对映异构体的方法，其中Me是甲基，Ar是3-甲氧基苯基，3-氯苯基或1-萘基，X独立地选自H，F，Cl ，Br，I，苯基，CF 3，CF 2 H，CFH 2，低级烷基（例如Me），O-低级烷基（例如OMe），OCH 2 CF 3，OH，CN，NO 2，C（O） - 低级烷基（O）Me），C（O）O-低级烷基（例如C（O）OMe），C（O）NH-低级烷基（例如C（O）NH-Me）低级烷基2（例如C（O）NMe 2），OC（O） - 低级烷基（例如OC（O）Me）和NH-C（O） - 低级烷基（例如NH-C（O）其中“低级烷基”选自1至6个碳原子，m为1至5之间的整数，通过用还原剂/手性助剂络合物不对称和对映选择性还原亚胺，以产生式（I）化合物的R对映体与式（I）化合物的S对映异构体的对映异构体过量。该方法特别适用于制备化合物（R） - （+） - N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯基）丙胺和（R） - （+） - N- [ - （3-甲氧基苯基）乙基] -3-（苯基）丙胺。 R对映异构体超过S对映异构体的对映异构体过量已达到大于65％。

6. 发明申请

WO1996012697A3 CALCIUM RECEPTOR-ACTIVE COMPOUNDS 审中-公开
公开(公告)号：WO1996012697A3
公开(公告)日：1996-05-02
申请号：PCT/US1995013704
申请日：1995-10-23
申请人： NPS PHARMACEUTICALS, INC.
发明人： NPS PHARMACEUTICALS, INC. , VAN WAGENEN, Bradford, C. , MOE, Scott, T. , BALANDRIN, Manuel, F. , DELMAR, Eric, G. , NEMETH, Edward, F.
IPC分类号： C07C211/27
摘要： The present invention features compounds of general formulae a), b), c), able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders by modulating inorganic ion receptor activity. Preferably, the compound can mimic or block the effect of extracellular Ca2+¿ on a calcium receptor.

8. 发明公开

EP0637237A1 CALCIUM RECEPTOR-ACTIVE MOLECULES 失效
标题翻译：钙受体活性分子。
公开(公告)号：EP0637237A1
公开(公告)日：1995-02-08
申请号：EP93907015.0
申请日：1993-02-23
申请人： BRIGHAM AND WOMEN'S HOSPITAL, INC. , NPS PHARMACEUTICALS, INC.
发明人： NEMETH, Edward, F. , BROWN, Edward, M. , HEBERT, Steven, C. , VAN WAGENEN, Bradford, C. , BALANDRIN, Manuel, F. , FULLER, Forrest, H. , DEL MAR, Eric, G.
IPC分类号： A01K67 , A61K31 , A61K39 , A61K45 , A61K48 , A61P3 , A61P9 , A61P43 , C07K14 , C12N15
CPC分类号： A61K31/70 , A01K2217/05 , A01K2217/075 , A01K2217/30 , A01K2227/10 , A01K2267/03 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/195 , A61K31/235 , A61K31/275 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/55 , C07K14/705 , C07K2319/00 , C12N15/8509
摘要： Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more inorganic-ion receptor. Novel compounds useful in these methods and compositions are also provided. The method includes administering to the patient a therapeutically effective amount of a molecule active at one or more inorganic-ion receptors as an agent or antagonist. Preferably, the molecule is able to act as either a selective agonist or antagonist at a Ca2+ receptor of one or more but not all cells chosen from the group consisting of parathyroid cells, bone osteoclasts, juxtaglomerular kidney cells, proximal tubule kidney cells, distal tubule kidney cell, cell of the thick ascending limb of Henle's loop and/or collecting duct, keratinocyte in the epidermis, parafollicular cell in the thyroid (C-cells), intestinal cell, trophoblast in the placenta, platelet, vascular smooth muscle cell, cardiac atrial cell, gastrin and glucagon secreting cells, kidney mesangial cell and mammary cell.

9. 发明授权

EP0787122B9 CALCIUM RECEPTOR-ACTIVE COMPOUNDS 失效
标题翻译：钙受体 - 活性化合物
公开(公告)号：EP0787122B9
公开(公告)日：2007-10-17
申请号：EP95940547.3
申请日：1995-10-23
申请人： NPS PHARMACEUTICALS, INC.
发明人： VAN WAGENEN, Bradford, C. , MOE, Scott, T. , BALANDRIN, Manuel, F. , DELMAR, Eric, G. , NEMETH, Edward, F.
IPC分类号： C07C211/27 , C07C211/30 , C07C217/58 , C07C211/28 , A61K31/135
CPC分类号： G01N33/6872 , A61K31/135 , A61K31/137 , C07C211/27 , C07C211/28 , C07C211/30 , C07C217/58 , C07C217/62 , C07C225/16 , C07C317/32 , C07C323/32 , C07D319/18 , G01N33/566 , G01N2500/10 , G01N2800/04
摘要： The present invention features compounds of general formulae a), b), c), able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders by modulating inorganic ion receptor activity. Preferably, the compound can mimic or block the effect of extracellular Ca2+ on a calcium receptor.
摘要翻译：本发明的特征是能够调节无机离子受体的一种或多种活性的通式a），b），c）的化合物和通过调节无机离子受体活性来治疗疾病或病症的方法。优选地，该化合物可以模拟或阻断细胞外Ca 2+对钙受体的作用。

10. 发明授权

EP0973730B1 CALCILYTIC COMPOUNDS 失效
标题翻译： CALCIUMREZEPTOR-INHIBITOREN
公开(公告)号：EP0973730B1
公开(公告)日：2004-06-16
申请号：EP98914581.8
申请日：1998-04-08
申请人： SMITHKLINE BEECHAM CORPORATION , NPS PHARMACEUTICALS, INC.
发明人： BARMORE, Robert, M. , BHATNAGAR, Pradip, Kumar , BRYAN, William, M. , BURGESS, Joelle, Lorraine , CALLAHAN, James, Francis , CALVO, Raul, Rolando , DEL MAR, Eric, G. , LAGO, Maria Amparo , NGUYEN, Thomas, The , SHEEHAN, Derek , SMITH, Robert, Lawrence , SOUTHALL, Linda, Sue , VAN WAGENEN, Bradford, C.
IPC分类号： C07C321/22 , C07C311/20 , C07C311/16 , C07C311/08 , C07C255/56 , C07C255/54 , C07C217/58 , C07C217/34 , C07C217/36 , C07D295/26 , C07D295/18 , C07D295/104 , C07D295/092 , C07D267/20 , A61P19/08 , A61P19/10 , A61K31/18 , A61K31/165
CPC分类号： C07D295/192 , C07C255/57 , C07C311/08 , C07C311/21 , C07C311/29 , C07C323/17 , C07C2601/02 , C07C2603/32 , C07D267/20 , C07D295/215
摘要： Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
摘要翻译：提供了具有钙质特性的新型芳基烷基氨基化合物。

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