公开(公告)号：EP1595871A3

公开(公告)日：2005-11-30

申请号：EP05017791.4

申请日：2000-06-02

申请人： NPS PHARMACEUTICALS, INC.

发明人： The designation of the inventor has not yet been filed

IPC分类号： C07D241/44 ,  C07D215/54 ,  C07D209/42 ,  C07D213/82 ,  C07D307/68 ,  C07D307/84 ,  C07D333/38 ,  C07D333/68 ,  A61K31/495 ,  A61K31/404 ,  A61P25/00

CPC分类号： C07D213/81 ,  A61K31/404 ,  A61K31/495 ,  C07D209/42 ,  C07D213/82 ,  C07D215/12 ,  C07D215/20 ,  C07D215/38 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D217/26 ,  C07D231/12 ,  C07D233/56 ,  C07D241/42 ,  C07D241/44 ,  C07D249/08 ,  C07D277/68 ,  C07D277/70 ,  C07D307/68 ,  C07D307/84 ,  C07D333/38 ,  C07D333/68 ,  C07D401/04 ,  C07D401/12 ,  C07D491/04

摘要： The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

摘要翻译： 本发明提供了对代谢型谷氨酸受体有活性的化合物和含有这些化合物的药物组合物。 这些化合物可用于治疗神经疾病和病症。 还公开了制备这些化合物的方法。

公开(公告)号：EP1210344B1

公开(公告)日：2005-10-19

申请号：EP00955657.2

申请日：2000-08-18

申请人： NPS PHARMACEUTICALS, INC.

发明人： VAN WAGENEN, Bradford, C. ,  STORMANN, Thomas, M. ,  MOE, Scott, T. ,  SHEEHAN, Susan, M. ,  MCLEOD, Donald, A. ,  SMITH, Daryl, L. ,  ISAAC, Methvin, Benjamin ,  SLASSI, Abdelmalik

IPC分类号： C07D413/04 ,  C07D401/04 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D413/04

摘要： Compound of formula (II) wherein X, Y, and Z are independently selected from the group consisting of N, O, S, C, and CO wherein at least one of X, Y, and Z is a heteroatom; Ar?1 and Ar2¿ are independently selected from the group consisting of a heterocyclic or fused heterocyclic moiety and an aromatic moiety; act as antagonist at metabotropic glutamate receptors, and are useful for treating neurological diseases and disorders.

摘要翻译： 式（II）化合物，其中X，Y和Z独立地选自N，O，S，C和CO，其中X，Y和Z中的至少一个为杂原子; Ar 1和Ar 2独立地选自杂环或稠合的杂环部分和芳族部分; 充当代谢型谷氨酸受体的拮抗剂，并且可用于治疗神经疾病和病症。

公开(公告)号：EP1576962A1

公开(公告)日：2005-09-21

申请号：EP05075497.7

申请日：1999-03-04

申请人： NPS PHARMACEUTICALS, INC.

发明人： Artman, Linda D. ,  Balandrin, Manuel F.

IPC分类号： A61K35/78 ,  A61K31/16 ,  A61K31/19 ,  A61K31/60 ,  A61K31/165

CPC分类号： A61K31/19 ,  A61K31/16 ,  A61K31/165 ,  A61K31/60 ,  A61K36/84 ,  A61K2300/00

摘要： Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, and other valerian-related compounds, in combination with NSAIDs exhibit clinically significant pharmacological properties which implicate a treatment for acute muscular aches, strains, and sprains which occur from a localized, external insult to a particular muscle or muscle group outside of, or peripheral to, the CNS. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

公开(公告)号：EP1466888A1

公开(公告)日：2004-10-13

申请号：EP04008763.7

申请日：1994-10-21

申请人： NPS PHARMACEUTICALS, INC.

发明人： Nemeth, Edward F. ,  Van Wagenen, Bradford C ,  Balandrin, Manuel F. ,  Delmar, Eric G. ,  Moe, Scott T.

IPC分类号： C07C211/30 ,  C07C217/62 ,  C07C217/58 ,  C07C323/32 ,  A61K31/13

CPC分类号： A61K31/70 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/275 ,  A61K31/335 ,  A61K31/34 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/395 ,  A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/55 ,  A61K31/715 ,  A61K38/16 ,  C07C211/27 ,  C07C211/29 ,  C07C211/30 ,  C07C211/42 ,  C07C215/52 ,  C07C217/58 ,  C07C217/60 ,  C07C217/62 ,  C07C225/16 ,  C07C229/38 ,  C07C233/05 ,  C07C255/58 ,  C07C317/32 ,  C07C323/32 ,  C07C2601/14 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D213/38 ,  C07D233/64 ,  C07D319/18 ,  C07K14/705 ,  G01N33/5008 ,  G01N33/566 ,  G01N33/567 ,  G01N33/6872 ,  G01N33/6893 ,  G01N33/84 ,  G01N2500/10 ,  G01N2800/04

摘要： The present invention features molecules with general structure (I) or (II) which can modulate on or activities of an inorganic ion receptor. Preferably, the molecule can mimic or block the effect of extracellular Ca 2+ on a calcium receptor. The preferred use of such molecules is to treat diseases or disorders by altering inorganic ion receptor activity, preferably calcium receptor activity.

摘要翻译： 本发明具有能够调节无机离子受体活性或其活性的具有通式结构（I）或（II）的分子。 优选地，分子可以模拟或阻断细胞外Ca 2+对钙受体的作用。 这种分子的优选用途是通过改变无机离子受体活性，优选钙受体活性来治疗疾病或病症。

公开(公告)号：EP1385520A2

公开(公告)日：2004-02-04

申请号：EP02709437.4

申请日：2002-02-08

申请人： NPS PHARMACEUTICALS, INC.

发明人： ARTMAN, Linda, D.

IPC分类号： A61K31/495 ,  A61K31/22 ,  A61K31/10

CPC分类号： A61K31/22 ,  A61K31/10 ,  A61K31/121 ,  A61K31/185 ,  A61K31/495 ,  C12Q1/34 ,  G01N2500/02 ,  A61K2300/00

摘要： A method of treating a neurologic or neuropsychiatric disorder or disease in a mammal is provided. The method comprises administering a fatty acid amide hydrolase inhibitor in an amount sufficient to inhibit deamidation of a fatty acid amide. A method of identifying a fatty acid amide hydrolase inhibitor useful in the treatment of a neurologic or neuropsychiatric disorder is also provided. A method of identifying a fatty acid amide or fatty acid useful in the treatment of a neurologic or neuropsychiatric disorder is also provided.

公开(公告)号：EP1123922A3

公开(公告)日：2004-01-02

申请号：EP00121960.9

申请日：1994-10-26

申请人： NPS PHARMACEUTICALS, INC.

发明人： Barmore, Robert M. ,  Mueller, Alan L. ,  Van Wagenen, Braford C. ,  Delmar, Eric G. ,  Balandrin, Manuel F. ,  Moe, Scott T. ,  Artman, Linda T.

IPC分类号： A61K31/165 ,  A61K31/404 ,  A61P9/10 ,  A61P25/28 ,  A61P25/04 ,  C07D209/18 ,  C07C279/14 ,  C07C237/22 ,  C07C233/22 ,  C07C235/34

CPC分类号： A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/295 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4409 ,  A61K31/4462 ,  A61K31/4465 ,  C07C233/22 ,  C07C235/34 ,  C07C237/22 ,  C07C279/14 ,  C07D209/18 ,  G01N2800/28

摘要： Method for identifying a compound useful for the therapeutic treatment of a neurological disease or disorder such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease or Parkinson's Disease,. or useful as a muscle relaxant, analgesic, or adjuvant to general anesthetics. The compounds is active on a receptor-operated calcium channel, including, but not limited to, that present as part of an NMDA receptor-ionophore complex, a calcium-permeable AMPA receptor, or a nicotinic cholinergic receptor, as a noncompetitive antagonist. The method includes identifying a compound which bonds to the receptor-operated calcium channel at the site bound by the arylalkylamines Compound 1, Compound 2 or Compound 3.

公开(公告)号：EP1275635A1

公开(公告)日：2003-01-15

申请号：EP02019566.5

申请日：1995-10-23

申请人： NPS PHARMACEUTICALS, INC.

发明人： Van Wagenen, Bradford C. ,  Balandrin, Manuel F. ,  Moe, Scott T. ,  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 extacellular Ca 2+ on a calcium receptor.

摘要翻译： 本发明具有能够调节一种或多种无机离子受体活性的通式a），b），c）的化合物和通过调节无机离子受体来治疗疾病或病症的方法 活动。 优选地，化合物可以模拟或阻断细胞外Ca 2+对钙受体的作用。

公开(公告)号：EP1254106A1

公开(公告)日：2002-11-06

申请号：EP01910349.8

申请日：2001-01-24

申请人： SmithKline Beecham Corporation ,  NPS PHARMACEUTICALS, INC.

发明人： LAGO, Amparo M. ,  CALLAHAN, James, Francis ,  BHATNAGAR, Pradip, Kumar ,  DEL MAR, Eric, G. ,  BRYAN, William, M. ,  BURGESS, Joelle, L.

IPC分类号： C07C255/50 ,  A61K31/277

CPC分类号： C07D303/22 ,  C07C69/616 ,  C07C69/738 ,  C07C211/30 ,  C07C233/05 ,  C07C251/48 ,  C07C255/57 ,  C07C255/58 ,  C07C2602/08 ,  C07C2602/10

摘要： Novel calcilytic compounds and methods of using them are provided.

公开(公告)号：EP1225888A2

公开(公告)日：2002-07-31

申请号：EP00982701.5

申请日：2000-10-19

申请人： NPS PHARMACEUTICALS, INC.

发明人： WELLS, David, S. ,  MARRIOTT, Thomas, B. ,  RAJEWSKI, Lian, G. ,  PIPKIN, James, D. ,  HASLAM, John, L.

IPC分类号： A61K31/195 ,  A61K31/16 ,  A61K31/19 ,  A61K31/60 ,  A61K31/22 ,  A61K31/165 ,  A61K31/18 ,  A61K31/255 ,  A61K31/27 ,  A61K9/28 ,  A61K9/50

CPC分类号： A61K31/27 ,  A61K9/205 ,  A61K9/2866 ,  A61K9/5042 ,  A61K31/16 ,  A61K31/18 ,  A61K31/19 ,  A61K31/255

摘要： Sustained-release compositions for delivering therapeutic concentrations of isovaleramide, isovaleric acid, and certain structurally related compounds are provided for the treatment for a variety of pathological conditions, including epilepsy and spasticity, which are ameliorated by effecting a modulation of CNS activity. The ability of the compositions to sustain relatively constant levels of the drug at a therapeutic dose in the serum for extended periods of time enables a once or twice daily administration schedule.

公开(公告)号：EP1176953A2

公开(公告)日：2002-02-06

申请号：EP00910383.9

申请日：2000-03-01

申请人： NPS PHARMACEUTICALS, INC.

发明人： ARTMAN, Linda, D. ,  BALANDRIN, Manuel ,  SMITH, Robert, L.

IPC分类号： A61K31/19 ,  A61K31/16 ,  A61K31/22 ,  A61K31/197 ,  A61K31/198 ,  A61K31/616 ,  A61K31/575 ,  A61K31/222 ,  A61K31/167 ,  A61K31/18 ,  A61K31/255 ,  A61K31/27 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/06

CPC分类号： A61K31/616 ,  A61K31/16 ,  A61K31/167 ,  A61K31/18 ,  A61K31/19 ,  A61K31/197 ,  A61K31/198 ,  A61K31/22 ,  A61K31/222 ,  A61K31/255 ,  A61K31/27 ,  A61K31/575 ,  A61K36/84 ,  Y10S514/923

摘要： Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and certain structurally related compounds exhibit clinically significant pharmacological properties which implicate a treatment for a variety of pathological conditions, including spasticity and convulsions, which are ameliorated by effecting a modulation of CNS activity. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.