公开(公告)号：AU748469B2

公开(公告)日：2002-06-06

申请号：AU8592198

申请日：1998-07-27

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN-SOO ,  TASKER ANDREW S ,  GELDERN THOMAS W VON ,  KESTER JEFFREY A ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: C07D491/048 ,  A61K31/40 ,  A61K31/41 ,  A61K31/423 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/495 ,  A61K31/506 ,  A61K31/535 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/08 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/06 ,  A61P35/00 ,  A61P43/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D403/04 ,  C07D405/00 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056

公开(公告)号：SK1452000A3

公开(公告)日：2001-05-10

申请号：SK1452000

申请日：1998-07-27

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN-SOO ,  TASKER ANDREW S ,  GELDERN THOMAS W VON ,  KESTER JEFFREY A ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: C07D491/048 ,  A61K31/40 ,  A61K31/41 ,  A61K31/423 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/495 ,  A61K31/506 ,  A61K31/535 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/08 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/06 ,  A61P35/00 ,  A61P43/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D403/04 ,  C07D405/00 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056

公开(公告)号：NZ330818A

公开(公告)日：2000-05-26

申请号：NZ33081897

申请日：1997-02-12

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN SOO ,  TASKER ANDREW S ,  VON GELDERN THOMAS W ,  KESTER JEFFREY A ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: A61K31/395 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/421 ,  A61K31/425 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/506 ,  A61K31/675 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P25/06 ,  A61P43/00 ,  C07D207/16 ,  C07D211/60 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D453/02 ,  C07D471/04 ,  C07D491/04 ,  C07F9/572

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin. Endothelin has been shown to constrict arteries and veins, increase mean arterial blood pressure, decrease cardiac output, increase cardiac contractility in vitro, stimulate mitogenesis in vascular smooth muscle including guinea pig trachea, human urinary bladder strips and rat uterus in vitro, induce formation of gastric ulcers, stimulate release of atrial natriuretic factor in vitro and in vivo, increase plasma levels of vasopressin, aldosterone and catecholamines, inhibit release of renin in vitro and stimulate release of gonadotropins in vitro. The compound of formula (I) wherein, Z is -C(R18)(R19)-or -C(O)- wherein R18 and R19 are independently selected from hydrogen and lower alkyl; n is 0 or 1; R is (CH2)m-W wherein m is an integer from 0-6 and W is (a) -C(O)2-G wherein G is H or a carboxy protecting group, (b) -PO3H2, (c) -P(O)(OH)E wherein E is hydrogen, lower alkyl or arylalkyl, (d) -CN, (e) -C(O)NHR17 wherein R17 is lower alkyl, (f) alkylaminocarbonyl, (g) dialkylaminocarbonyl, (h) tetrazolyl, (i) hydroxy, (j) alkoxy, (k) sulfonamido, (l) -C(O)NHS(O)2R16 wherein R16 is loweralkyl, haloalkyl, aryl or dialkylamino, (m) -S(O)2NHC(O)R16, (n)-(u) are represented in the figures provided; R1-R25 are selected from common hydrocarbon groups.

公开(公告)号：NO20000542L

公开(公告)日：2000-04-04

申请号：NO20000542

申请日：2000-02-02

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN-SOO ,  TASKER ANDREW S ,  GELDERN THOMAS W VON ,  KESTER JEFFREY ALAN ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: C07D491/048 ,  A61K31/40 ,  A61K31/41 ,  A61K31/423 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/495 ,  A61K31/506 ,  A61K31/535 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/08 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/06 ,  A61P35/00 ,  A61P43/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D403/04 ,  C07D405/00 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056 ,  A61K

公开(公告)号：NO20000542A

公开(公告)日：2000-04-04

申请号：NO20000542

申请日：2000-02-02

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN-SOO ,  TASKER ANDREW S ,  GELDERN THOMAS W VON ,  KESTER JEFFREY ALAN ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: C07D491/048 ,  A61K31/40 ,  A61K31/41 ,  A61K31/423 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/495 ,  A61K31/506 ,  A61K31/535 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/08 ,  A61P13/12 ,  A61P21/00 ,  A61P21/04 ,  A61P25/06 ,  A61P35/00 ,  A61P43/00 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D403/04 ,  C07D405/00 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056 ,  A61K

CPC classification number: C07D207/27 ,  C07D207/16 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

公开(公告)号：AU2262097A

公开(公告)日：1997-09-02

申请号：AU2262097

申请日：1997-02-12

Applicant: ABBOTT LAB

Inventor： WINN MARTIN ,  BOYD STEVEN A ,  HUTCHINS CHARLES W ,  JAE HWAN-SOO ,  TASKER ANDREW S ,  GELDERN THOMAS W VON ,  KESTER JEFFREY A ,  SORENSEN BRYAN K ,  SZCZEPANKIEWICZ BRUCE G ,  HENRY KENNETH J JR ,  LIU GANG ,  WITTENBERGER STEVEN J ,  KING STEVEN A

IPC: A61K31/395 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/421 ,  A61K31/425 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/495 ,  A61K31/506 ,  A61K31/675 ,  A61P1/00 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P25/06 ,  A61P43/00 ,  C07D207/16 ,  C07D211/60 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D453/02 ,  C07D471/04 ,  C07D491/04 ,  C07F9/572 ,  C07F9/59

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

公开(公告)号：AU653959B2

公开(公告)日：1994-10-20

申请号：AU8531591

申请日：1991-08-02

Applicant: ABBOTT LAB

Inventor： BAKER WILLIAM R ,  BOYD STEVEN A ,  FUNG ANTHONY K L ,  STEIN HERMAN H ,  DENISSEN JON F ,  HUTCHINS CHARLES W ,  ROSENBERG SAUL H

IPC: A61K31/445 ,  A61K31/4427 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61P9/12 ,  A61P43/00 ,  C07D211/46 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D451/14 ,  C07D498/08

公开(公告)号：NZ706401A

公开(公告)日：2015-08-28

申请号：NZ70640110

申请日：2010-05-06

Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

Inventor： HUTCHINS CHARLES W ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  KLING ANDREAS ,  JANTOS KATJA ,  MACK HELMUT

IPC: C07D207/26 ,  A61K31/4412 ,  C07D211/76 ,  C07D233/34 ,  C07D239/10

Abstract: Disclosed herein are carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). Additionally disclosed is the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity, interleukin-I, TNF or A&bgr; level, such as malaria, HIV or disorders associated with the kidneys. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

公开(公告)号：PH12013502359A1

公开(公告)日：2014-11-10

申请号：PH12013502359

申请日：2013-11-15

Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

Inventor： MACK HELMUT ,  KLING ANDREAS ,  JANTOS KATJA ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  HUTCHINS CHARLES W

IPC: C07D233/34 ,  A61K31/4412 ,  C07D207/26 ,  C07D211/76 ,  C07D239/10

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

公开(公告)号：ES2414934T3

公开(公告)日：2013-07-23

申请号：ES11160830

申请日：2010-06-10

Applicant: ABBOTT LAB ,  ABBVIE BAHAMAS LTD

Inventor： RANDOLPH JOHN T ,  DEGOEY DAVID A ,  KATI WARREN M ,  HUTCHINS CHARLES W ,  DONNER PAMELA L ,  KRUEGER ALLAN C ,  MOTTER CHRISTOPHER E ,  NELSON LISSA T ,  PATEL SACHIN V ,  MATULENKO MARK A ,  KEDDY RYAN G ,  JINKERSON TAMMIE K ,  HUTCHINSON DOUGLAS K ,  FLENTGE CHARLES A ,  WAGNER CHARLES A ,  MARING CLARENCE J ,  TUFANO MICHAEL D ,  BETEBENNER DAVID A ,  ROCKWAY TODD W ,  LIU DACHUN ,  PRATT JOHN K ,  SARRIS KATHY ,  WOLLER KEVIN R ,  WAGAW SEBLE H ,  CALIFANO JEAN C ,  LI WENKE ,  CASPI DANIEL D ,  BELLIZZI MARY E ,  YI GAO

IPC: C07D403/14 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/4439 ,  A61P31/14 ,  C07D401/14 ,  C07D417/14

Abstract: Un compuesto de Fórmula I, o una sal farmacéuticamente aceptable del mismo,**Fórmula** donde: X es donde el átomo de nitrógeno del anillo está unido directamente a -L3-D, y donde X está opcionalmentesustituido uno o más A; L1, L2 y L3 son enlaces; cada uno de A y B es independientemente **Fórmula** y cada uno está opcional e independientemente sustituido con uno o más RA; D es carbociclo C3-C12 o heterociclo de 3 a 12 miembros, y está opcionalmente sustituido con uno o más RA;Y es -G-C(R1R2)N(R5)-T-RD, -G-C(R3R4)C(R6R7)-T-RD, N(RB)C(O)C(R1R2)N(R5)-T-RD, o N(RB)C(O)C(R3R4)C(R6R7)-T-RD; Z es -G-C(R8R9)N(R12)-T-RD, -G-C(R10R11)C(R13R14)-T-RD, -N(RB)C(O)C(R8R9)N(R12)-T-RD o N(RB)C(O)C(R10R11)C(R13R14)-T-RD; R1 es RC, y R2 y R5, tomados junto con los átomos a los que están acoplados, forman un heterociclo de 3 a 12miembros que está opcionalmente sustituido con uno o más RA.