公开(公告)号：WO1995021612A3

公开(公告)日：1995-08-17

申请号：PCT/US1994012293

申请日：1994-10-26

Applicant: NPS PHARMACEUTICALS, INC. ,  MUELLER, Alan, L. ,  VAN WAGENEN, Bradford, C. ,  DELMAR, Eric, G. ,  BALANDRIN, Manuel, F. ,  MOE, Scott, T. ,  ARTMAN, Linda, D.

Inventor： NPS PHARMACEUTICALS, INC.

IPC: A61K31/165

公开(公告)号：WO1994028888A1

公开(公告)日：1994-12-22

申请号：PCT/US1994006356

申请日：1994-06-10

Applicant: NPS PHARMACEUTICALS, INC. ,  BALANDRIN, Manuel, F. ,  VAN WAGENEN, Bradford, C.

Inventor： NPS PHARMACEUTICALS, INC.

IPC: A61K31/16

CPC classification number: A61K31/16 ,  Y10S514/923

Abstract: Isovaleramide has been found to exhibit mild anxiolytic (anxiety-reducing) activity at low to moderate dosage levels and mild sedative activity at somewhat higher dosage levels. In contrast to certain other materials thought to be anxiolytic or mildly sedative, isovaleramide is non-cytotoxic and does not paradoxically stimulate the central nervous system. Isovaleramide is therefore useful as a mild anxiolytic and mild sedative agent which can be made available to the general public.

Abstract translation: 已经发现异戊酰胺在低至中等剂量水平下呈现轻度抗焦虑（焦虑降低）活性，并且在较高剂量水平下呈现温和的镇静作用。 与被认为是抗焦虑或轻度镇静的某些其他物质相反，异戊酰胺是非细胞毒性的，并不矛盾地刺激中枢神经系统。 因此，异戊酰胺可作为轻度抗焦虑和温和的镇静剂，可向公众提供。

公开(公告)号：WO1993004373A1

公开(公告)日：1993-03-04

申请号：PCT/US1992007175

申请日：1992-08-21

Applicant: NPS PHARMACEUTICALS, INC. ,  NEMETH, Edward, F. ,  VAN WAGENEN, Bradford, C. ,  BALANDRIN, Manuel, F.

Inventor： NPS PHARMACEUTICALS, INC.

IPC: G01N33/566

CPC classification number: A61K31/70 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/165 ,  A61K31/275 ,  A61K31/395 ,  A61K31/40 ,  A61K31/44 ,  A61K31/55 ,  A61K31/715 ,  A61K38/16 ,  C07C211/27 ,  C07C211/29 ,  C07C211/30 ,  C07C211/42 ,  C07C215/52 ,  C07C217/58 ,  C07C217/60 ,  C07C225/16 ,  C07C229/38 ,  C07C233/05 ,  C07C255/58 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D213/38 ,  C07D233/64 ,  C07K14/705 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5044 ,  G01N33/5091 ,  G01N33/566 ,  G01N33/567 ,  G01N33/6872 ,  G01N2500/10 ,  G01N2500/20 ,  G01N2800/04

Abstract: 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 Ca receptors. 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 Ca receptors as an agonist 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, keratinocytes, parafollicular thyroid cells and placental throphoblasts and a pharmaceutically acceptable carrier.

Abstract translation: 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Ca 2+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作为激动剂或拮抗剂的一种或多种Ca 2+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，角质形成细胞，旁叶状甲状腺细胞和胎盘滋养细胞和药学上可接受的载体。

公开(公告)号：WO1998016185A2

公开(公告)日：1998-04-23

申请号：PCT/US1997018710

申请日：1997-10-17

Applicant: NPS PHARMACEUTICALS, INC.

Inventor： NPS PHARMACEUTICALS, INC. ,  SANGUINETTI, Michael, C. ,  MUELLER, Alan, L.

IPC: A61K00/00

CPC classification number: C07K14/43518 ,  A01N63/02 ,  A61K38/00 ,  C07K14/705

Abstract: Specific potent transient outward potassium channel inhibitors, and polypeptides derived from spider venom are described. Also described are methods of screening for agents specifically active on transient outward potassium channels or other types of potassium channels, methods of treating a disease or condition by administering an agent active on a transient outward potassium channel or certain agents active on other potassium channels, and methods of using a potassium channel inhibitor derived from spider venom as an insecticidal agent.

Abstract translation: 描述了特异性有效的瞬时外向钾通道抑制剂和源自蜘蛛毒液的多肽。 还描述了筛选对瞬时外向钾通道或其他类型的钾通道特异性活性的药物的方法，通过施用在瞬时外向钾通道上有活性的药剂或在其它钾通道上有活性的药剂来治疗疾病或病症的方法，以及 使用衍生自蜘蛛毒液的钾通道抑制剂作为杀虫剂的方法。

公开(公告)号：WO1998001417A1

公开(公告)日：1998-01-15

申请号：PCT/JP1997002358

申请日：1997-07-08

Applicant: KIRIN BEER KABUSHIKI KAISHA ,  NPS PHARMACEUTICALS, INC. ,  SAKAI, Teruyuki ,  TAKAMI, Atsuya ,  SUZUKI, Rika

Inventor： KIRIN BEER KABUSHIKI KAISHA ,  NPS PHARMACEUTICALS, INC.

IPC: C07C211/30

CPC classification number: C07D207/335 ,  C07B2200/07 ,  C07C211/30 ,  C07C217/20 ,  C07C217/58 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C317/18 ,  C07C317/28 ,  C07C323/25 ,  C07C2603/18 ,  C07D209/08 ,  C07D209/14 ,  C07D209/88 ,  C07D213/38 ,  C07D213/40 ,  C07D213/70 ,  C07D215/36 ,  C07D241/12 ,  C07D263/58 ,  C07D277/28 ,  C07D277/74 ,  C07D281/06 ,  C07D307/52 ,  C07D307/91 ,  C07D311/30 ,  C07D317/58 ,  C07D333/20 ,  C07D333/34

Abstract: Novel calcium receptor-active compounds represented by the following general formula: Ar1-[CR R ]p-X-[CR R ]q-[CR R ]-NR -[CR R ]-Ar2 wherein Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroaryl-methyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R , R , R , R , R , R , R , R and R represent, for example, each hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6; and q is an integer of from 0 to 14.

Abstract translation: 由以下通式表示的新型钙受体活性化合物：Ar1- [CR 1 R 2] pX- [CR 3 R 4] q- [CR 5 R 6] - NR 7 - [CR 8 R 9] -Ar 2，其中Ar 1选自芳基，杂芳基，双（芳基甲基）氨基，双（杂芳基 - 甲基）氨基和芳基甲基（杂芳基甲基）氨基; X选自氧，硫，亚磺酰基，磺酰基，羰基和氨基; R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9表示例如各自 氢或烷基; Ar 2选自芳基和杂芳基; p是0至6的整数; q为0〜14的整数。

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

Applicant: NPS PHARMACEUTICALS, INC. ,  SMITHKLINE BEECHAM PLC ,  SMITHKLINE BEECHAM

Inventor： 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: C07C217/34

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO1996025041A1

公开(公告)日：1996-08-22

申请号：PCT/US1996002030

申请日：1996-02-16

Applicant: NPS PHARMACEUTICALS, INC.

Inventor： NPS PHARMACEUTICALS, INC. ,  JOHNSON, Janice, H. ,  KRAL, Robert, M. ,  KRAPCHO, Karen

IPC: A01N37/18

CPC classification number: A01N37/46 ,  A01N63/00 ,  C07K14/43518 ,  Y10S530/858

Abstract: This invention relates to the purification of a family of insecticidally effective peptides isolated from the spider, Calisoga sp., characterized by their neurotoxic effect on insect pest and low mammalian toxicity. The cDNA sequences for three of these peptides have been isolated, and the complete coding sequence is provided. This invention also discloses methods for producing recombinant peptides, as well as methods of utilizing these peptides as insecticidal agents.

Abstract translation: 本发明涉及从蜘蛛（Calisoga sp。）分离的一类杀虫有效肽的纯化，其特征在于它们对害虫的神经毒性作用和低的哺乳动物毒性。 已经分离了三种这些肽的cDNA序列，并提供了完整的编码序列。 本发明还公开了重组肽的制备方法，以及利用这些肽作为杀虫剂的方法。

公开(公告)号：WO1995001996A1

公开(公告)日：1995-01-19

申请号：PCT/US1994007595

申请日：1994-07-07

Applicant: FMC CORPORATION ,  NPS PHARMACEUTICALS, INC.

Inventor： FMC CORPORATION ,  NPS PHARMACEUTICALS, INC. ,  JACKSON, John, Randolph, Hunter ,  KRAPCHO, Karen, Joanne ,  KRAL, Robert, Marden, Jr.

IPC: C07K15/08

CPC classification number: C07K14/43518 ,  A61K38/00 ,  C12N2799/026

Abstract: This invention provides a family of insecticidally effective proteins and particular members of that family which may be isolated from the venom of the spider Filistata hibernalis, DNA encoding such proteins, insecticidal compositions of these proteins or the DNA encoding them, and methods for controlling invertebrate pests. Recombinant expression vectors and host cells and methods for producing insecticidally effective peptides are also provided.

Abstract translation: 本发明提供了一种杀虫有效的蛋白质和该家族的特定成员，其可以从蜘蛛丝状丝虫的毒液中分离，编码这些蛋白质的DNA，这些蛋白质的杀虫组合物或其编码的DNA，以及控制无脊椎动物害虫的方法 。 还提供了重组表达载体和宿主细胞以及用于产生杀虫有效肽的方法。

公开(公告)号：WO1994021278A1

公开(公告)日：1994-09-29

申请号：PCT/US1994002750

申请日：1994-03-14

Applicant: NPS PHARMACEUTICALS, INC.

Inventor： NPS PHARMACEUTICALS, INC. ,  SANGUINETTI, Michael, C. ,  MUELLER, Alan, L.

IPC: A61K37/02

CPC classification number: C07K14/43518 ,  A01N63/02 ,  A61K38/00 ,  G01N33/6872 ,  G01N2500/00

Abstract: Specific potent transient outward potassium channel inhibitors, and polypeptides derived from spider venom, and uses thereof.

Abstract translation: 特异性瞬时外向钾通道抑制剂，以及衍生自蜘蛛毒液的多肽及其用途。

公开(公告)号：WO1993004041A1

公开(公告)日：1993-03-04

申请号：PCT/US1992006598

申请日：1992-08-13

Applicant: PFIZER INC. ,  NPS PHARMACEUTICALS, INC. ,  SACCOMANO, Nicholas, A. ,  VOLKMANN, Robert, A.

Inventor： PFIZER INC. ,  NPS PHARMACEUTICALS, INC.

IPC: C07D209/18

CPC classification number: C07D213/81 ,  C07D209/18 ,  C07D209/20 ,  C07D209/42 ,  C07D213/56 ,  C07D213/82 ,  C07D215/14 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D241/42 ,  C07D241/44 ,  C07F17/02

Abstract: Compounds having the formula R-(CH2)m-CO-R' wherein R is a 5 to 7 member azacylic system or an 8 to 11 member azabicyclic system, having 1 or 2 nitrogen atoms, or any such system substituted with one or more of F, Cl, Br, OH, C1 to C4 alkyl, C1 to C4 alkoxy, CF3, phenyl, amino, C1 to C4 alkylamino and di(C1 to C4 alkyl)amino; m is 0 or 1; R' is -[NH(CH2)n]xNH2; each n is independently 2 to 5; and x is 1 to 6, and their pharmaceutically acceptable acid addition salts are potent excitatory amino acid neurotransmitter antagonists. These compounds are useful as mammalian psychotherapeutants, as the active ingredient in pharmaceutical compositions for treating conditions in mammals which are mediated by excitatory amino acid neurotransmitters and in the control of invertrebrate pests.