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US 8,410,134 B2Granted
8-oxy-quinoline derivatives as bradykinin B2 receptor modulators
AssigneeShire Orphan Therapies GmbH
InventorsChristoph Gibson, Thomas Tradler, Karsten Schnatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Matthias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
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Abstract
The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
Claims36
A Compound of the formula (I):
- or a pharmacologically acceptable salt, wherein
- A is a 6-membered heteroaryl having from 1 to 3 heteroatoms each independently selected from N or O, wherein said 6-membered heteroaryl is substituted with from 2 to 4 substituents each independently selected from halogen atom, oxygen atom, hydroxy, cyano, amino, nitro, mercapto, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R5 is halogen atom, hydroxy, cyano, nitro, mercapto, alkyl, alkenyl, alkynyl, or heteroalkyl;
- R6 is optionally substituted alkyl;
- optionally substituted alkenyl;
- 5-membered heterocycloalkyl having from 1 to 3 heteroatoms each independently selected from N, O or S, or cycloalkyl, wherein said 5-membered heterocycloalkyl or cycloalkyl is substituted with from 0 to 3 substituents each independently selected from halogen atom, oxygen atom, hydroxy, cyano, amino, nitro, mercapto, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- 5-membered heteroaryl having from 1 to 4 heteroatoms each independently selected from N, O or S, wherein said 5-membered heteroaryl is substituted with from 0 to 3 substituents each independently selected from halogen atom, oxygen atom, hydroxy, cyano, amino, nitro, mercapto, alkyl, alkenyl, alkynyl, heteroalkyl, optionally substituted aryl or optionally substituted heteroaryl;
- or —S—R10;
- R10 is 5-membered heterocycloalkyl having from 1 to 3 heteroatoms each independently selected from N, O or S, or cycloalkyl, wherein said 5-membered heterocycloalkyl or cycloalkyl is substituted with from 0 to 4 substituents each independently selected from halogen atom, oxygen atom, hydroxy, cyano, amino, nitro, mercapto, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- or 5-membered heteroaryl having from 1 to 4 heteroatoms each independently selected from N, O or S, wherein said 5-membered heteroaryl is substituted with from 0 to 4 substituents each independently selected from halogen atom, oxygen atom, hydroxy, cyano, amino, nitro, mercapto, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R7 is hydrogen atom, halogen atom, hydroxy, cyano, amino, nitro, alkyl, or heteroalkyl;
- R8 is hydrogen atom or halogen atom;
- and
- R17 is hydrogen atom or halogen atom.
11 more elements
A compound of the formula (II):
- or a pharmacologically acceptable salt thereof, wherein
- A is a 6-membered heteroaryl having 1 heteroatom, wherein said heteroatom is N, and wherein said 6-membered heteroaryl is substituted with 3 substituents each independently selected from halogen atom, alkyl and heteroalkylcycloalkyl;
- R5 is alkyl;
- R6 is a 5-membered heterocycloalkyl having 2 heteroatoms, wherein each heteroatom is N, and wherein said 5-membered heterocycloalkyl is substituted with 1 substituent, wherein said substituent is a halogen atom;
- and
- R7, R8 and R17 are hydrogen atom.
3 more elements
The compound of formula (III):
- or a pharmacologically acceptable salt thereof.
Dependencies are inferred from the claim text.