公开(公告)号：US5981513A

公开(公告)日：1999-11-09

申请号：US45522

申请日：1998-03-21

Applicant: Lawrence I. Kruse ,  An-Chih Chang ,  Diane L. DeHaven-Hudkins ,  John J. Farrar ,  Forrest Gaul ,  Virendra Kumar ,  Michael Anthony Marella ,  Alan L. Maycock ,  Wei Yuan Zhang

Inventor： Lawrence I. Kruse ,  An-Chih Chang ,  Diane L. DeHaven-Hudkins ,  John J. Farrar ,  Forrest Gaul ,  Virendra Kumar ,  Michael Anthony Marella ,  Alan L. Maycock ,  Wei Yuan Zhang

IPC: C07D295/12 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/495 ,  A61K31/496 ,  A61P17/04 ,  A61P25/04 ,  C07D207/09 ,  C07D207/12 ,  C07D209/08 ,  C07D209/18 ,  C07D209/42 ,  C07D213/56 ,  C07D241/04 ,  C07D273/08 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D207/04

CPC classification number: A61K31/404 ,  A61K31/40 ,  A61K31/4439 ,  C07D209/42 ,  C07D213/56 ,  C07D241/04

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formula II having the structure: ##STR1## wherein X.sub.4, X.sub.5 ;R.sub.1, R.sub.2 ; andAr and n are as described in the specification.

Abstract translation: 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 具有以下结构的式II化合物：其中X 4，X 5; R1，R2; Ar和n如说明书中所述。

公开(公告)号：US5763445A

公开(公告)日：1998-06-09

申请号：US891833

申请日：1997-07-14

Applicant: Lawrence I. Kruse ,  An-Chih Chang ,  Diane L. DeHaven-Hudkins ,  John J. Farrar ,  Forrest Gaul ,  Virendra Kumar ,  Michael Anthony Marella ,  Alan L. Maycock ,  Wei Yuan Zhang

Inventor： Lawrence I. Kruse ,  An-Chih Chang ,  Diane L. DeHaven-Hudkins ,  John J. Farrar ,  Forrest Gaul ,  Virendra Kumar ,  Michael Anthony Marella ,  Alan L. Maycock ,  Wei Yuan Zhang

IPC: C07D295/12 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/495 ,  A61K31/496 ,  A61P17/04 ,  A61P25/04 ,  C07D207/09 ,  C07D207/12 ,  C07D209/08 ,  C07D209/18 ,  C07D209/42 ,  C07D213/56 ,  C07D241/04 ,  C07D273/08 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

CPC classification number: A61K31/404 ,  A61K31/40 ,  A61K31/4439 ,  C07D209/42 ,  C07D213/56 ,  C07D241/04

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formular I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ; R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; and Y, Z and n are as described in the specification.

Abstract translation: 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 式I，II，III和IV的化合物具有以下结构：X（X），X（X），X R1，R2，R3，R4; Y，Z和n如说明书所述。

公开(公告)号：US5147875A

公开(公告)日：1992-09-15

申请号：US443986

申请日：1989-11-30

Applicant: William J. Coates ,  Lawrence I. Kruse

Inventor： William J. Coates ,  Lawrence I. Kruse

IPC: A61K31/505 ,  A61K31/517 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  C07C237/30 ,  C07C237/42 ,  C07C237/44 ,  C07C323/63 ,  C07D239/91

CPC classification number: C07D239/91 ,  C07C237/42

Abstract: This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.

公开(公告)号：US4859779A

公开(公告)日：1989-08-22

申请号：US302640

申请日：1989-01-27

Applicant: Joseph A. Finkelstein ,  Lawrence I. Kruse ,  Thomas B. Leonard

Inventor： Joseph A. Finkelstein ,  Lawrence I. Kruse ,  Thomas B. Leonard

IPC: C07D233/90

CPC classification number: C07D233/90

Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

Abstract translation: 具有抑制多巴胺-β-羟化酶活性的具有式“IMAGE”的强效多巴胺-β-羟化酶抑制剂，包括这些抑制剂的药物组合物，以及使用这些抑制剂抑制哺乳动物中多巴胺-β-羟化酶活性的方法。 还公开了可用于制备本发明的抑制剂的新型中间体。

公开(公告)号：US4835154A

公开(公告)日：1989-05-30

申请号：US56018

申请日：1987-06-01

Applicant: Joseph A. Finkelstein ,  Lawrence I. Kruse

Inventor： Joseph A. Finkelstein ,  Lawrence I. Kruse

IPC: A61K31/415 ,  A61P1/04 ,  A61P7/10 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P25/00 ,  A61P43/00 ,  C07D233/84 ,  C07D233/90

CPC classification number: C07D233/84

Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

公开(公告)号：US4810811A

公开(公告)日：1989-03-07

申请号：US88773

申请日：1987-08-24

Applicant: Carl Kaiser ,  Lawrence I. Kruse

Inventor： Carl Kaiser ,  Lawrence I. Kruse

IPC: C07C331/24 ,  C07D257/04 ,  C07C155/08

CPC classification number: C07D257/04 ,  C07C331/24

Abstract: The compounds of this invention are 1-phenylalkyl-2-mercaptotetrazole compounds which are dopamine-.beta.-hydroxylase inhibitors.

Abstract translation: 本发明的化合物是作为多巴胺-β-羟化酶抑制剂的1-苯基烷基-2-巯基四唑化合物。

公开(公告)号：US4798843A

公开(公告)日：1989-01-17

申请号：US71515

申请日：1987-07-09

Applicant: Lawrence I. Kruse

Inventor： Lawrence I. Kruse

IPC: A61K31/415 ,  A61P1/04 ,  A61P7/10 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P25/00 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C225/16 ,  C07C255/59 ,  C07C301/00 ,  C07C311/37 ,  C07C313/00 ,  C07C317/32 ,  C07C317/44 ,  C07D233/84

CPC classification number: C07D233/84

Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutial compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

公开(公告)号：US4772723A

公开(公告)日：1988-09-20

申请号：US723689

申请日：1985-04-16

Applicant: James S. Frazee ,  Carl Kaiser ,  Lawrence I. Kruse

Inventor： James S. Frazee ,  Carl Kaiser ,  Lawrence I. Kruse

IPC: C07C217/62 ,  C07D233/54 ,  C07D233/84 ,  C07D233/90 ,  C07D233/04

CPC classification number: C07D233/64 ,  C07C217/62 ,  C07D233/84 ,  C07D233/90

Abstract: Potent DBH Inhibitors having the formula: ##STR1## wherein R is --CO.sub.2 H or --CH.sub.2 NHR.sup.1 can be used to inhibit DBH activity in mammals.

Abstract translation: 具有下式的强力DBH抑制剂：其中R为-CO2H或-CH2NHR1，可用于抑制哺乳动物中的DBH活性。

公开(公告)号：US4767862A

公开(公告)日：1988-08-30

申请号：US88624

申请日：1987-08-24

Applicant: Carl Kaiser ,  Lawrence I. Kruse

Inventor： Carl Kaiser ,  Lawrence I. Kruse

IPC: A61K31/47 ,  A61K31/472 ,  A61P25/02 ,  C07D217/20

CPC classification number: C07D217/20

Abstract: Compounds having the formula ##STR1## are .beta.-adrenergic receptor antagonists. Also disclosed are pharmaceutical compositions and methods for producing .beta.-adrenergic receptor antagonistic activity in animals including man.

公开(公告)号：US4634711A

公开(公告)日：1987-01-06

申请号：US761936

申请日：1985-08-02

Applicant: Carl Kaiser ,  Lawrence I. Kruse ,  Stephen T. Ross

Inventor： Carl Kaiser ,  Lawrence I. Kruse ,  Stephen T. Ross

IPC: A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4427 ,  A61P1/04 ,  A61P7/10 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P25/02 ,  A61P43/00 ,  C07D213/64 ,  C07D213/65 ,  C07D213/89 ,  C07D401/06 ,  C12N9/99 ,  A61K31/415

CPC classification number: C07D401/06

Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

Abstract translation: 具有下式的有效的多巴胺-β-羟化酶抑制剂：其可用于抑制多巴胺-β-羟化酶活性，包括这些抑制剂的药物组合物，以及使用这些抑制剂抑制哺乳动物中多巴胺-β-羟化酶活性的方法。 还公开了可用于制备本发明的抑制剂的新型中间体。