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1. WO1997024124 - VITRONECTIN RECEPTOR ANTAGONISTS

Publication Number WO/1997/024124
Publication Date 10.07.1997
International Application No. PCT/US1996/020327
International Filing Date 20.12.1996
Chapter 2 Demand Filed 17.07.1997
IPC
C07D 213/74 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with 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
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 401/12 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
12linked by a chain containing hetero atoms as chain links
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 405/12 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
12linked by a chain containing hetero atoms as chain links
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
A61P 19/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 7/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Applicants
  • SMITHKLINE BEECHAM CORPORATION [US]/[US] (AllExceptUS)
  • ALI, Fadia, E. [US]/[US] (UsOnly)
  • BONDINELL, William, E. [US]/[US] (UsOnly)
  • KEENAN, Richard, M. [US]/[US] (UsOnly)
  • KU, Thomas, Wen, Fu [US]/[US] (UsOnly)
  • MILLER, William, H. [US]/[US] (UsOnly)
  • SAMANEN, James [US]/[US] (UsOnly)
Inventors
  • ALI, Fadia, E.
  • BONDINELL, William, E.
  • KEENAN, Richard, M.
  • KU, Thomas, Wen, Fu
  • MILLER, William, H.
  • SAMANEN, James
Agents
  • McCARTHY, Mary, E.
Priority Data
60/009,36729.12.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) VITRONECTIN RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DU RECEPTEUR DE LA VITRONECTINE
Abstract
(EN)
Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form -(CHRg)a-U-(CHRg)b-V-; Q1, Q2, Q3 and Q4 are independently N or C-Ry, provided that no more than one of Q1, Q2, Q3 and Q4 is N; R' is H or C1-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; Rg is H or C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; Rk is Rg, -C(O)Rg or -C(O)ORg Ri is H, C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl-U'-C1-6alkyl, C3-7cycloalkyl-C0-6alkyl-U'-C1-6alkyl or Ar-C0-6alkyl-U'-C1-6alkyl; Ry is H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r-, -CO2Rg, -CORg or -CONRg2, or C1-6alkyl optionally substituted by halo, -ORg, -SRg, -CN, -NRgR'', -NO2, -CF3, R'S(O)3-, -CO2Rg, -CORg or -CONRg2; U and V are absent or CO, CRg2, C(=CRg2), S(O)c, O, NRg, CRgORg, CRg(ORk)CRg2, CRg2CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)2NRg, NRgS(O)2N=N, NRgNRg, NRgCRg2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C$m(Z)C, Ar or Het; a is 0, 1, 2 or 3; b is 0, 1 or 2; c is 0, 1 or 2; r is 0, 1 or 2; and u is 0 or 1; or pharmaceutically acceptable salts thereof, which are vitronectin receptor antagonists useful in the treatment of osteoporosis.
(FR)
La présente invention concerne des composés de la formule (I), dans laquelle A est une matrice d'antagoniste fibrinogène; W est un fragment de liaison dont la forme est -(CHRg)a-U-(CHRg)b-V-; Q1, Q2, Q3 et Q4 sont, de manière indépendante, N (au maximum l'un d'entre eux) ou C-Ry; R' est H ou alkyle C1-6, cycloalkyle C3-7-alkyle C0-6 ou Ar-alkyle C0-6, Rg est H ou alkyle C1-6, Het-alkyle C0-6, cycloalkyle C3-7-alkyle C0-6 ou Ar-alkyle C0-6; Rk est Rg, -C(O)Rg ou -C(O)ORg, Ri est H, alkyle C1-6, Het-alkyle C0-6, cycloalkyle C3-7-alkyle C0-6, Ar-alkyle C0-6, Het-alkyle C0-6-U'-alkyle C1-6, cycloalkyle C3-7-alkyle C0-6-U'-alkyle C1-6 ou Ar-alkyle C0-6-U'-alkyle C1-6; Ry est H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r-, -CO2Rg, -CORg ou -CONRg2, ou alkyle C1-6 facultativement substitué par halo, -ORg, -SRg, -CN, -NRgR'', -NO2, -CF3, R'S(O)3-, -CO2Rg ou -CONRg2; U and V sont absents ou CO, CRg2, C(=CRg2), S(O)c, O, NRg, CRgORg, CRg(ORk)CRg2, CRg2CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)2NRg, NRgS(O)2N=N, NRgNRg, NRgCRg2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C$m(Z)C, Ar ou Het; a vaut 0, 1, 2 ou 3; b vaut 0, 1 ou 2; c vaut 0, 1 ou 2; r vaut 0, 1 ou 2; et u est 0 ou 1. L'invention concerne aussi des sels de ces composés acceptables sur le plan pharmacologique qui sont des antagonistes de récepteurs de la vitronectine utiles dans le traitement de l'ostéoporose.
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