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US 2003/0125383 A1Published application
Substituted urea retinoid agonists
AssigneeRoche Bioscience, a division of Syntex (U.S.A.) LLC
InventorsMichael Klaus, Jean-Marc Lapierre
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Abstract
The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.
Claims33
A compound according to structural formula (I):
- 28
- or a pharmaceutically available salt, solvate or hydrate thereof wherein:
- n is an integer from 0 to 2;
- X is S, O or NR4R5;
- R4 and R5 are independently hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl, or optionally together with the nitrogen atom to which they are attached form a heterocyclyl ring;
- A is aryl or heteroaryl;
- Y is CO2R6, C(O)SR7or C(O)NR8R9;
- R1 and R3 are independently hydrogen, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl-alkyl, haloalkyl, heteroaryl, heteroarylalkyl, heteroalkyl, heterocyclyl or heterocyclylalkyl;
- and
- R2 is hydrogen, alkyl, hydroxy or oxo;
- R6 is hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl;
- R7 is hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl;
- R8 and R9 are independently hydrogen, alkyl, aryl, arylalkyl, cycloalkyl or cycloalkyl-alkyl, or together with the nitrogen atom to which they are attached form a heterocyclyl ring;
- with the proviso that R1 is not hydrogen or alkyl when R3 is hydrogen.
11 more elements
Dependencies are inferred from the claim text.