Leslie Morales Robinson

US Patent:

6410580, Jun 25, 2002

Filed:

Aug 2, 2000

Appl. No.:

09/601462

Inventors:

Paivi Jaana Kukkola - Whitehouse Station NJ
Leslie Ann Robinson - Del Mar CA
Junichi Sakaki - Kawasaki, JP
Motowo Nakajima - Ashiya, JP

Assignee:

Novartis AG - Basel

International Classification:

C07D27506

US Classification:

514373, 514444, 514471, 549 59, 549476, 548210

Abstract:

Compounds of formula (I) wherein W is âOH or âNHOH; X is an optionally substituted heterocycle, NR SO R , heterocyclylalkythio, CONR R or NR COR ; Y, Z, R -R and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.

US Patent:

62779877, Aug 21, 2001

Filed:

Feb 3, 1999

Appl. No.:

9/243854

Inventors:

Paivi Jaana Kukkola - Whitehouse Station NJ
Leslie Anne Robinson - Del Mar CA
Motowo Nakajima - Ashiya, JP
Junichi Sakaki - Takarazuka, JP

Assignee:

Novartis AG - Basel

International Classification:

C07D23972
C07D20948
C07D27504
A61K 31415
A61K 3140

US Classification:

544285

Abstract:

Compounds of formula ##STR1## wherein W is --OH or --NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH. sub. 2). sub. m moiety by a ring nitrogen, --CONR. sub. 2 R. sub. 3, --NR. sub. 1 COR. sub. 2, --NR. sub. 1 SO. sub. 2 R. sub. 2, --NR. sub. 1 CONR. sub. 2 R. sub. 3, --NR. sub. 1 COOR. sub. 4, heteroarylthio, alkylthio, arylalkylthio, heteroarylalkylthio, heterocycloalkylalkylthio, heterocycloalkylthio or arylthio; Y is carbon, nitrogen, oxygen or sulfur, provided that when Y is carbon, n is 2; Z is alkyl, aryl, alkoxy, aryloxy, aralkoxyaryl, aralkoxyheteroaryl, heteroaryl, heterocycloalkyl, heteroaryloxy, --CONR. sub. 2 R. sub. 3, --NR. sub. 1 COR. sub. 2, --NR. sub. 1 CONR. sub. 2 R. sub. 3, --OCONR. sub. 2 R. sub. 3, --NR. sub. 1 COOR. sub. 4, or --SO. sub. 2 R. sub.

US Patent:

59770759, Nov 2, 1999

Filed:

Oct 21, 1997

Appl. No.:

8/945329

Inventors:

Gary Michael Ksander - Milford NJ
Paivi Jaana Kukkola - Morristown NJ
Leslie Anne Robinson - Warren NJ

Assignee:

Novartis AG - Basel

International Classification:

A61K 3805

US Classification:

514 19

Abstract:

The present invention relates to the compounds of formula (I) ##STR1## wherein R is carboxy, esterified carboxy, carbamoyl, N-(alkyl or aryl)-carbamoyl, cyano, 5-tetrazolyl or CONH--SO. sub. 2 --R. sub. 4 ; R. sub. 1 is hydrogen, lower alkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R. sub. 2 is hydrogen or lower alkyl, or R. sub. 1 and R. sub. 2 represent lower alkylene to form together with the carbon and nitrogen atoms to which they are attached an azacycloalkane ring; R. sub. 3 is heterocyclic or carbocyclic (aryl or biaryl)-lower alkyl; Y is lower alkylidenyl, 3- to 10-membered cycloalkylidenyl which may be substituted by oxo, alkylenedioxy, hydroxy, acyloxy, lower alkoxy; or Y is 5- to 10-membered cycloalkylidenyl fused to a saturated or unsaturated carbocyclic 5- or 6-membered ring; or Y is 5- to 8-membered oxacycloalkylidenyl, 5- to 8-membered (thia-, oxothia- or dioxothia-) cycloalkylidenyl, or 5- to 8-membered azacycloalkylidenyl optionally N-substituted by lower alkyl or aryl-lower alkyl; R. sub. 4 represents hydrogen, lower alkyl, carbocyclic aryl, heterocyclic aryl, cycloalkyl, (carbocyclic aryl, heterocyclic aryl, cycloalkyl, hydroxy, acyloxy, or lower alkoxy)-lower alkyl, lower alkyl substituted by carboxyl, by esterified carboxyl or by amidated carboxyl; Ar represents carbocyclic or heterocyclic aryl; and pharmaceutically acceptable salts thereof; which are useful as endothelin inhibitors in mammals.