Pharmaceutical compositions for the treatment of female sexual disorders
First Claim
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1. ) A method for the treatment of female sexual disorders comprising administration of therapeutically effective amount of a compound of formula 1 wherein R1 is a group selected from among halogen, —
- O—
C1-C4-alkyl, and —
C(halogen)3;
L is a linker, selected from the bridging groups —
C1-C6-alkylene, —
C1-C4-alkylene-O—
, —
C1-C4-alkylene-O—
CO—
, —
C1-C4-alkylene-N H—
, —
C1-C4-alkylene-NH—
CO—
, —
C2-C6-alkenylene, —
C2-C4-alkenylene-O—
, —
C2-C4-alkenylene-O—
CO—
, —
C2-C4-alkenylene-NH—
, —
C2-C4-alkenylene-NH—
CO—
, —
C2-C6-alkynylene, —
C2-C4-alkynylene-O—
, —
C2-C4-alkynylene-O—
CO—
, —
C2-C4-alkynylene-N H—
, and —
C2-C4-alkynylene-NH—
CO—
, which may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, ═
O, —
C(halogen)3 and —
O—
C1-C4-alkyl;
R2 is —
NH2, —
NHC1-C4-alkyl, —
N(C1-C4-alkyl)2, or a group selected from among —
C1-C6-alkyl and —
C3-C6-cycloalkyl which may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, ═
O, —
C(halogen)3, —
O—
C1-C4-alkyl, —
O—
C6-C10-aryl, —
NH2, —
NHC1-C4-alkyl, —
N(C1-C4-alkyl)2, —
C2-C4-alkenyl and —
C2-C4-alkynyl, or R2 is —
C6-C10-aryl, optionally substituted by one or more, preferably one group selected from among, —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3, —
O—
C1-C4-alkyl, —
NH2, —
NH—
C1-C4-alkyl, —
N(C1-C4-alkyl)2, and a nitrogen containing heteroaromatic ring, wherein said nitrogen containing heteroaromatic ring may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3, and —
O—
C1-C4-alkyl, and wherein said nitrogen containing heteroaromatic ring my optionally be linked to the —
C6-C10-aryl group via a bridging group selected from among —
O—
, —
S—
, and —
NH—
, or R2 is a group selected from among wherein X is either N or —
CR3—
;
Y is either —
NR5—
, —
O—
, —
S—
, —
SO2—
, —
CH2—
or —
CO—
;
A is absent or a ring system selected from among B is absent or a ring system selected from among
rein the arrows indicate the positions where the ring is annellated to the five membered nitrogen heterocycle, and wherein R3 is selected from among hydrogen, —
C1-C4-alkyl, —
CH2—
NH2, —
CH2—
NH—
C1-C4-alkyl, —
CH2—
N(C1-C4-alkyl)2, —
NH2, —
NH—
C1-C4-alkyl, and —
N(C1-C4-alkyl)2;
R4 is selected from among hydrogen, —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3 and —
O—
C1-C4-alkyl, R5 is selected from among hydrogen, —
C1-C4-alkyl, —
C6-C10-aryl, and —
C1-C4-alkylen-C6-C10-aryl;
a pharmaceutically acceptable acid addition salt thereof, a hydrate or solvate thereof, or in the form of the individual optical isomer, mixture of the individual enantiomers or a racemate thereof.
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Abstract
The invention relates to a method for the treatment of female sexual disorders comprising administration of a therapeutically effective amount of a compound of general formula 1
-
Citations
13 Claims
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1. ) A method for the treatment of female sexual disorders comprising administration of therapeutically effective amount of a compound of formula 1
wherein R1 is a group selected from among halogen, — - O—
C1-C4-alkyl, and —
C(halogen)3;
L is a linker, selected from the bridging groups —
C1-C6-alkylene, —
C1-C4-alkylene-O—
, —
C1-C4-alkylene-O—
CO—
, —
C1-C4-alkylene-N H—
, —
C1-C4-alkylene-NH—
CO—
, —
C2-C6-alkenylene, —
C2-C4-alkenylene-O—
, —
C2-C4-alkenylene-O—
CO—
, —
C2-C4-alkenylene-NH—
, —
C2-C4-alkenylene-NH—
CO—
, —
C2-C6-alkynylene, —
C2-C4-alkynylene-O—
, —
C2-C4-alkynylene-O—
CO—
, —
C2-C4-alkynylene-N H—
, and—
C2-C4-alkynylene-NH—
CO—
, which may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, ═
O, —
C(halogen)3 and —
O—
C1-C4-alkyl;
R2 is —
NH2, —
NHC1-C4-alkyl, —
N(C1-C4-alkyl)2, or a group selected from among —
C1-C6-alkyl and —
C3-C6-cycloalkyl which may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, ═
O, —
C(halogen)3, —
O—
C1-C4-alkyl, —
O—
C6-C10-aryl, —
NH2, —
NHC1-C4-alkyl, —
N(C1-C4-alkyl)2, —
C2-C4-alkenyl and —
C2-C4-alkynyl, orR2 is —
C6-C10-aryl, optionally substituted by one or more, preferably one group selected from among, —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3, —
O—
C1-C4-alkyl, —
NH2, —
NH—
C1-C4-alkyl, —
N(C1-C4-alkyl)2, and a nitrogen containing heteroaromatic ring, wherein said nitrogen containing heteroaromatic ring may optionally be substituted by one or more, preferably one group selected from among —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3, and —
O—
C1-C4-alkyl, and wherein said nitrogen containing heteroaromatic ring my optionally be linked to the —
C6-C10-aryl group via a bridging group selected from among —
O—
, —
S—
, and —
NH—
, orR2 is a group selected from among wherein X is either N or —
CR3—
;
Y is either —
NR5—
, —
O—
, —
S—
, —
SO2—
, —
CH2—
or —
CO—
;
A is absent or a ring system selected from among B is absent or a ring system selected from among
rein the arrows indicate the positions where the ring is annellated to the five membered nitrogen heterocycle, and whereinR3 is selected from among hydrogen, —
C1-C4-alkyl, —
CH2—
NH2, —
CH2—
NH—
C1-C4-alkyl, —
CH2—
N(C1-C4-alkyl)2, —
NH2, —
NH—
C1-C4-alkyl, and —
N(C1-C4-alkyl)2;
R4 is selected from among hydrogen, —
C1-C4-alkyl, —
OH, halogen, —
C(halogen)3 and —
O—
C1-C4-alkyl,R5 is selected from among hydrogen, —
C1-C4-alkyl, —
C6-C10-aryl, and —
C1-C4-alkylen-C6-C10-aryl;
a pharmaceutically acceptable acid addition salt thereof, a hydrate or solvate thereof, or in the form of the individual optical isomer, mixture of the individual enantiomers or a racemate thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- O—
Specification