摘要:
Fibrinogen receptor antagonists having the structure X--Y--Z--A--B and pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g., ##STR1##
摘要:
A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要:
Compounds of the general formula ##STR1## and the pharmaceutically acceptable salts thereof whereinn is an integer of from 0 to 6;Y is CH.sub.2, O, SO.sub.2, --CONH--, --NHCO--, or ##STR2## R.sup.1 and R.sup.2 are independently hydrogen,C.sub.1-8 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,amino C.sub.1-4 alkyl,C.sub.1-4 alkylamino C.sub.1-4 alkyl, orC.sub.3-8 cycloalkylwherein R.sup.1 and R.sup.2 may be unsubstituted or substituted with one or more groups chosen from R.sup.3, whereR.sup.3 ishydrogen,C.sub.1-6 alkyl,hydroxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,C.sub.1-4 alkyloxy C.sub.0-4 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,halogen, orCF.sub.3 ;R.sup.4 isC.sub.1-6 alkyl,heterocyclyl C.sub.0-4 alkyl, oraryl C.sub.0-4 alkyl;R.sup.5 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-3 alkyl, orC.sub.1-6 alkylcarbonyloxymethylare used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
摘要:
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要:
A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要:
Fibrinogen receptor antagonists of the formula: ##STR1## wherein A,B,D,E,Y are as defined in the specification, are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
摘要:
Compounds of the general formula ##STR1## Y is an integer of from 0 to 6 is chosen from: O,SO.sub.2,--CONH--,--NHCO--,--CH2-- or ##STR2## R.sup.1 is substituted or unsubstituted mono- or polycyclic saturated hetero-cyclic ring system having 1, 2 or 3 heteroatoms where said heteroatoms are independently chosen from N, O and S and said substituents are chosen from the group comprising R.sup.2 ;R.sup.2 isC.sub.1-6 alkyl,aryl C.sub.0-6 alkyl,hydroxy C.sub.0-6 alkyl,C.sub.1-6 alkoxy C.sub.0-6 alkyl,carboxy C.sub.0-6 alkyloxo,halogen,CF.sub.3,C.sub.0-4 alkylamino-C.sub.0-6 alkyl orC.sub.0-4 dialkylamino-C.sub.0-6 alkyl;R.sup.3 isC.sub.1-8 alkyl or cycloalkyl,aryl C.sub.0-4 alkyl,hydroxy C.sub.0-4 alkylC.sub.1-4 alkyloxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,halogen,CF.sub.3 orhydrogen;R.sup.4 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orC.sub.1-6 alkylcarbonyloxymethyl; andR.sup.5 isC.sub.1-6 alkyl,aryl C.sub.0-4 alkyl orheterocycly C.sub.0-4 alkyland the pharmaceutically acceptable salts thereof; are used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
摘要:
A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要:
Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.