US 9,040,523 B2 · Antifungal 5,6-dihydro-4H-pyrrolo[1,2-α][1,4]-benzodiazepines and 6H-pyrrolo[1,2-α][1,4]benzodiazepines substituted with benzene derivatives

Abstract

The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines of Formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Claims12

Dependent claims

A compound of formula (I)

or a stereoisomeric form thereof, wherein
R1 is hydrogen, halo, C1-4alkyl or C1-4alkyloxy;
R2 is hydrogen or halo;
R3 and R4 are hydrogen;
or R3 and R4 taken together form a bond;
R5 is C1-4alkylcarbonyl, C1-4alkylsulphonyl, C1-4alkylsulphinyl, or C1-4alkyl substituted with one hydroxyl moiety;
R6 is hydrogen or halo;
or a pharmaceutically acceptable addition salt thereof.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/989,233Filed 18 Nov 2011

Priority

EP 1019232124 Nov 2010

Published

US 2013/0274250 A117 Oct 2013

Granted

26 May 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification4 codes

C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61P 31/10
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antimycotics
C07D
Heterocyclic compounds
A61P
Therapeutic uses of medicines

Antifungal 5,6-dihydro-4H-pyrrolo[1,2-α][1,4]-benzodiazepines and 6H-pyrrolo[1,2-α][1,4]benzodiazepines substituted with benzene derivatives

Life of this patent

Antifungal 5,6-dihydro-4H-pyrrolo[1,2-α][1,4]-benzodiazepines and 6H-pyrrolo[1,2-α][1,4]benzodiazepines substituted with benzene derivatives

Life of this patent

Abstract

Claims12