公开(公告)号：NZ331124A

公开(公告)日：2000-05-26

申请号：NZ33112497

申请日：1997-02-10

Applicant: ABBOTT LAB

Inventor： TASKER ANDREW S ,  BOYD STEVEN A ,  SORENSEN BRYAN K ,  WINN MARTIN ,  JAE HWAN-SOO ,  VON GELDERN THOMAS W ,  HENRY KENNETH J

IPC: A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/675 ,  A61P1/00 ,  A61P7/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P25/04 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D453/02 ,  C07F9/572

Abstract: A compound of above formula (I) or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof. The compounds have use in and a method of antagonizing endothelin and therefore in the treatment of hypertension, congestive heart failure cerebral or myocardial ischemia and artherosclerosis. Specific compounds claimed are exemplified by: Trans,trans-2-(4-propoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1((2,6-diethyl)phenylaminocarbonylmethyl)-pyrrolidine-3-carboxylic acid; [2R,3R,4S]2-(4-methoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(N-((2,6-diethyl)phenylaminocarbonylmethyl)-pyrrolidine-3-carboxylic acid; [2R,3R,4S]2-(4-propoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(N-((2,6-diethyl)phenylaminocarbonylmethyl)-pyrrolidine-3-carboxylic acid; and [2R,3R,4S]2-(4-ethoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(N-((2,6-diethyl)phenylaminocarbonylmethyl)-pyrrolidine-3-carboxylic acid;

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：AU714597B2

公开(公告)日：2000-01-06

申请号：AU2267897

申请日：1997-02-10

Applicant: ABBOTT LAB

Inventor： TASKER ANDREW S ,  BOYD STEVEN A ,  SORENSEN BRYAN K ,  WINN MARTIN ,  JAE HWAN-SOO ,  GELDERN THOMAS W VON ,  HENRY KENNETH J JR

IPC: A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/675 ,  A61P1/00 ,  A61P7/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P25/04 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D453/02 ,  C07F9/572

公开(公告)号：ZA985209B

公开(公告)日：1999-01-06

申请号：ZA985209

申请日：1998-06-15

Applicant: ABBOTT LAB

Inventor： TASKER ANDREW S ,  WINN MARTIN ,  BOYD STEVEN A ,  JAE HWAN-SOO ,  VONGELDERN THOMAS W ,  SORENSEN BRYAN K ,  HENRY KENNETH J

IPC: C07D207/16 ,  C07D405/04 ,  C07D ,  A61K ,  C07F

公开(公告)号：AU7826398A

公开(公告)日：1999-01-04

申请号：AU7826398

申请日：1998-06-08

Applicant: ABBOTT LAB

Inventor： TASKER ANDREW S ,  WINN MARTIN ,  BOYD STEVEN A ,  JAE HWAN-SOO ,  GELDERN THOMAS W VON ,  SORENSEN BRYAN K ,  HENRY KENNETH J JR

IPC: C07D207/16 ,  C07D405/04 ,  A61K31/40

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：ZA9701184B

公开(公告)日：1997-08-27

申请号：ZA9701184

申请日：1997-02-12

Applicant: ABBOTT LAB

Inventor： TASKER ANDREW S ,  VONGELDERN THOMAS W ,  JAE HWAN-SOO ,  SORENSEN BRYAN K ,  WINN MARTIN ,  BOYD STEVEN A ,  HENRY KENNETH J

IPC: A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/675 ,  A61P1/00 ,  A61P7/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P25/04 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D453/02 ,  C07F9/572 ,  C07D ,  A61K ,  C07F

CPC classification number: C07D405/04 ,  A61K9/2059 ,  A61K9/4866

公开(公告)号：ES2386365T3

公开(公告)日：2012-08-17

申请号：ES06717418

申请日：2006-01-05

Applicant: ABBOTT LAB

Inventor： PATEL JYOTI R ,  SHUAI QI ,  LINK JAMES T ,  ROHDE JEFFREY J ,  DINGES JURGEN ,  SORENSEN BRYAN K ,  WINN MARTIN ,  YONG HONG ,  YEH VINCE S

IPC: C07C235/14 ,  A61K31/4402 ,  A61P3/10 ,  C07C317/16 ,  C07C323/41 ,  C07D207/48 ,  C07D213/64 ,  C07D233/54 ,  C07D257/04 ,  C07D261/08

Abstract: Un compuesto de fórmula (I): **Fórmula**en la que:A1 se selecciona del grupo que consiste en alquenilo, alquilo, alquil-NH-alquilo, alquilcarbonilo, alquilsulfonilo,carboxialquilo, carboxicicloalquilo, ciano, cicloalquilo, cicloalquilcarbonilo, cicloalquilsulfonilo, arilo, arilalquilo,ariloxialquilo, arilcarbonilo, arilsulfonilo, heteroarilo, heteroarilalquilo, heteroariloxialquilo, heteroarilsulfonilo,heterociclo, heterocicloalquilo, heterociclooxialquilo, -heterociclosulfonilo, halógeno, haloalquilo,-NR5-[C(R6R7)]n-C(O)-R8, -O-[C(R9R10)]p-C(O)-R11, -OR12, -S-alquilo, -S(O)-alquilo, -N(R13R14), -CO2R15,-C(O)-N(R16R17), -C(R18R19)-OR20, -C(R21R22)-N(R23R24), -C(>=NOH)-N(H)2, -C(R18aR19a)-C(O)N(R23R24),-S(O)2-N(R25R26), y -C(R18aR19a)-S(O)2-N(R25R26);A2, A3 y A4 se seleccionan cada una individualmente del grupo que consiste en hidrógeno, alquenilo, alquilo,alquil-NH-alquilo, alquilcarbonilo, alquilsulfonilo, carboxialquilo, carboxicicloalquilo, ciano, cicloalquilo,cicloalquilcarbonilo, cicloalquilsulfonilo, arilo, arilalquilo, ariloxialquilo, arilcarbonilo, arilsulfonilo, heteroarilo,heteroarilalquilo, heteroariloxialquilo, heteroarilsulfonilo, heterociclo, heterocicloalquilo, heterociclooxialquilo,heterociclosulfonilo, halógeno, haloalquilo, -NR5-[C(R6 R7)]n-C(O)-R8, -O-[C(R9R10)]p-C(O)-R11, -OR12, -S-alquilo,-S(O)-alquilo, -N(R13R14), -CO2R15, -C(O)-N(R16R17), -C(R18R19)-OR20, -C(R21R22)-N(R23R24), -C(>=NOH)-N(H)2,-C(R18aR19a)-C(O)N(R23R24), -S(O)2-N(R25R26) y -C(R18aR19a)-S(O)2-N(R25R26);cada R18a y R19a se selecciona independientemente del grupo que consiste en hidrógeno y alquilo;n es 0 ó 1;p es 0 ó 1;