Processing

Please wait...

Settings

Settings

1. WO2000039092 - HETEROCYCLIC AMIDES AS INHIBITORS OF FACTOR Xa

Publication Number WO/2000/039092
Publication Date 06.07.2000
International Application No. PCT/US1999/029834
International Filing Date 15.12.1999
Chapter 2 Demand Filed 30.06.2000
IPC
C07D 211/62 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
62attached in position 4
C07D 401/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 409/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
C07D 211/62
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
62attached in position 4
C07D 401/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
C07D 409/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
Applicants
  • ELI LILLY AND COMPANY [US/US]; Lilly Corporate Center Indianapolis, IN 46285, US (AllExceptUS)
  • KLIMKOWSKI, Valentine, Joseph [US/US]; US (UsOnly)
  • KYLE, Jeffrey, Alan [US/US]; US (UsOnly)
  • MASTERS, John, Joseph [US/US]; US (UsOnly)
  • WILEY, Michael, Robert [US/US]; US (UsOnly)
Inventors
  • KLIMKOWSKI, Valentine, Joseph; US
  • KYLE, Jeffrey, Alan; US
  • MASTERS, John, Joseph; US
  • WILEY, Michael, Robert; US
Agents
  • JACKSON, Thomas, E. ; Eli Lilly and Company Lilly Corporate Center Indianapolis, IN 46285, US
Priority Data
60/113,59524.12.1998US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HETEROCYCLIC AMIDES AS INHIBITORS OF FACTOR Xa
(FR) AMIDES HETEROCYCLIQUES INHIBITEURS DU FACTEUR Xa
Abstract
(EN)
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) wherein: Q1 is phenyl or 2-naphthalenyl either of which may bear one or more halo, trifluoromethyl, methoxy or methyl substituents; L1 is a direct bond, methylene, ethylene or ethen-1, 2-diyl; and Q2 is Q2A, Q2B, or Q2C in which Q2A (showing the CO to which it is attached) is of formula (a) in which each of m and n independently is 0 or 1; Q2B is 1-piperazinyl which bears at the 4-position the group R; Q2C is 3,4-didehydropiperidin-4-yl which bears at the 1-position the group R; pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
(FR)
La présente invention concerne un composé (ou un sel acceptable du point de vue pharmaceutique dudit composé) représenté par la formule (I) dans laquelle Q1 est phényle ou 2-naphthalényle, l'un ou l'autre pouvant comporter un ou plusieurs substituants halogéno, trifluorométhyle, méthoxy ou méthyle; L1 est une liaison directe, méthylène, éthylène ou éthèn-1,2-diyle; et Q2 est Q2A, Q2B, ou Q2C, Q2A (représenté avec le CO auquel il est lié) étant de formule (a) dans laquelle m et n sont indépendamment égaux à 0 ou 1; Q2B étant 1-pipérazinyle qui porte le groupe R en position 4; et Q2C étant 3,4-didéshydropipéridine-4-yle qui porte le groupe R en position 1. L'invention concerne également des compositions pharmaceutiques dudit composé et son utilisation comme inhibiteur du facteur Xa, ainsi que son procédé de préparation et les intermédiaires utilisés à cet effet.
Latest bibliographic data on file with the International Bureau