摘要:
Arylidene and heteroarylidene oxindole derivatives of formula (I) ##STR1## wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline;R is hydrogen or an oxo (.dbd.O) group when Y is tetralin; orR is hydrogen when Y is naphthalene, quinoline or isoquinoline;each of R.sup.1 and R.sup.2 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;m is zero, 1 or 2;n is zero, 1, 2 or 3;each of R.sup.3 and R.sup.4 independently is hydrogen, halogen, cyano, C.sub.1 -C.sub.6 alkyl, carboxy, nitro or --NR.sup.6 R.sup.7 in which each of R.sup.6 and R.sup.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.
摘要:
The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin;and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl and R.sub.3, R.sub.4 and R.sub.5 are hydrogen; whereas when Y is indole, then R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro or --NHR, in which R is as defined above, R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, carboxy, nitro or --NHR, wherein R is as defined above, and R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;as anti-angiogenic agent is disclosed.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
A new class of pyrazolo derivative compounds having the formula where R and R1 have the meanings given herein. The pyrazolo derivative compounds are useful in treating cell proliferative disorders caused by and/or associated with an altered cell cycle dependent kinase activity in mammals. The compounds may be provided in pharmaceutical compositions or in a kit.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要:
Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.