US 6,784,173 B2Granted

Aromatic dicarboxylic acid derivatives

AssigneeHoffmann-La Roche Inc.

InventorsUlrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann

Life of this patent

Estimating the term…

Abstract

Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.

Claims27

Dependent claims

A compound of formula I

is a thiophene ring that may be unsubstituted or substituted by 1 or 2 substituents independently selected from a halogen atom, a C1-4-alkyl-, trifluoromethyl-, hydroxy-, C1-4-alkoxy-, nitro-, amino-, C1-4-alkylamino-, di[C1-4-alkyl]-amino-, C1-4-alkanoylamino, C1-3-alkylenedioxy- or an acyl group;
and
R1 and R2 are each independently selected from hydrogen,
a branched or unbranched C1-4-alkyl group that may be unsubstituted or substituted with 1 or more substituents independently selected from halogen, hydroxy-, nitro-, an amino group, a carbocyclic group or a heterocyclic group,
and wherein at a chain length of longer than 2 carbon atoms, one or more non adjacent atoms may be replaced by oxygen, nitrogen or sulfur atoms,
and wherein 2 atoms may be bound together by a double or triple bond,
a carbocyclic group, and
a heterocyclic group,
or alternatively, the group —NR1R2 forms a 3-6 membered ring that may contain additional heteroatoms independently selected from nitrogen, oxygen and sulfur, said ring optionally being annulated to a carbocyclic ring or a heterocyclic ring, and said —NR1R2 ring being unsubstituted or optionally substituted by 1, 2, or 3 substituents independently selected from a halogen atom, an C1-4-alkyl-, trifluoromethyl-, hydroxy-, C1-4-alkoxy-, aryl-, hetaryl-, arylalkyl, arylalkyloxy-, aryloxy, C1-3-alkylenedioxy-, nitro-, amino-, C1-4-alkylamino-, di[C1-4-alkyl]amino-, C1-4-alkanoylamino- or an acyl-group;
and
their enantiomers, diastereoisomers, racemates and physiologically acceptable salts thereof.

8 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/167,677Filed 11 Jun 2002
Priority: EP 0111449615 Jun 2001
Published: US 2003/0013757 A116 Jan 2003
Granted: 31 Aug 2004
Term ends: Not estimatedThe source records don’t support an estimate.

Classification16 codes

C07D 213/40
Radicals substituted by singly-bound nitrogen atoms: acylated substituent nitrogen atom
A61P 35/00
Antineoplastic agents
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00
C07C 259/10
Without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids: having carbon atoms of hydroxamic groups bound to…

Family

US 2003/0013757 A1Pre-grant publication · published 16 Jan 2003
US 6,784,173 B2This patent

From the US filing history. Foreign family members aren’t listed.

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