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US 2003/0158409 A1Published application
Pyridine derivatives inhibiting angiogenesis and/or vegf receptor tyrosine kinase
AssigneeNovartis AG
InventorsGuido Bold, Paul William Manley
Life of this patent
Estimating the term…
Abstract
The invention relates to pyridine derivatives of formula (I), wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds. 1
Claims21
A compound of formula I
- 97
- wherein
- A, D and T, independently of one another, are each N, CH or CR4, with the proviso that at least one of A and D is CR4 when T is N;
- R4 is lower alkyl, lower alkenyl, lower alkylthio, mercapto, free, etherified or esterified hydroxy, unsubstituted, mono- or disubstituted amino or halogen;
- B and E, independently of one another, are each N or CH;
- G is C1-C6-alkylene, C2-C6-alkenylene, acyloxy- or hydroxy-substituted C1-C6-alkylene or C3-CH6-alkenylene, C1-C2-alkyleneoxy, C1-C2-alkylenethio, C1-C2-alkyleneimino, —CH2—O—CH2—, —CH2—S—CH2—, —CH2—NH—CH2—, oxa, thia or imino;
- n is 0to 2;
- Q is lower alkyl, whereby A, D and T are not substituted by Q if they represent CR4;
- r is 0to 5;
- R1 und R1′ independently of one another are each hydrogen or lower alkyl;
- R2 and R3
- a) independently of one another, are each lower alkyl;
- or
- b) together form a bridge of the part formula I*,
- 98
- wherein
- the ring members T1, T2, T3 and T4, independently of one another, are each nitrogen or CH, and binding is achieved via the atoms T1 and T4, the bonds characterised by a wavy line, independently of one another, are each either single or double bonds, m is 0 to 4 and Z is a substituent of one or more carbon atoms, whereby Z is unsubstituted, mono- or disubstituted amino, halogen, unsubstituted or substituted alkyl, free, etherified or esterified hydroxy, nitro, cyano, free or esterified carboxy, alkanoyl, unsubstituted, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl lower alkylsulfonyl or alkylphenylsulfonyl, whereby if more than 1 radical Z is present (m≧2), the substituents Z are identical or different;
- W is hydrogen, unsubstituted, mono- or disubstituted amino, halogen, unsubstituted or substituted alkyl, free, etherified or esterified hydroxy, nitro, cyano, free or esterified carboxy, alkanoyl, unsubstituted, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl lower alkylsulfonyl or alkylphenylsulfonyl;
- X is —N(R5)—, oxa, or thia;
- and
- R5 is H or lower alkyl;
- and Y is hydrogen, aryl, which is unsubstituted or substituted by one or more substituents, heterocyclyl, which is unsubstituted or substituted by one or more substituents, or unsubstituted or substituted cycloalkyl;
- or a tautomer of the said compound;
- or an N-oxide of the said compound or tautomers thereof, whereby one or more N atoms carry an oxygen atom;
- or a salt of the said compounds.
22 more elements
Dependencies are inferred from the claim text.