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1. WO1996031500 - NOVEL HETEROCYCLIC COMPOUNDS

Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]
CLAIMS
i A compound of formula I


wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C^-alky! or C^-alkoxy; and
Y is -C_H2-N-CH2-, -CH2-N-C_H2-, -(C_ = O)-N-CH2-, -CH2-N-(C = O)-,
-C_H2-C_H-CH2-, -CH2-CH-C.H2-, -CH2-C = CH-, -CH = C-QH2-, -O-CH-CH2-,

-CH2-CH-O-, -S-CH-CH2- or -CH2-CH-S_- wherein only the underscored atoms participate in the ring system; and
X is -O-, -S-, -C(RβR7)-, -CH2CH2-, -CH = CH-CH2-, -CH2-CH = CH-, -CH

(C = O)-, -(C = O)-CH2-, -CH2CH2CH2-, -CH = CH-, -N(R8)-(C = O)-, -(C = O)- N(R8)-, -O-CH2-, -CH2-O-, -S-CH2-, -CH2-S-, -(C = O)-, -N(R9)- or -(S = O)- wherein Rβ, R7, R8 and R9 independently are hydrogen or C^-alkyl; and q is 0 or 1 ; and
p is 0 or 1 ; and
r is 1 , 2 or 3; and
Z is selected from








wherein n is 1 or 2; and
R3 is -(CH2)mOH or -(CH2),COR4 wherein m is 0, 1 , 2, 3, 4, 5 or 6 and s is 0 or 1 and wherein R4 is -OH, -NH2, -NHOH or
and
R5 is hydrogen, halogen, trifluoromethyl, hydroxy, C,.β-alkyl or

alkoxy; and
R10 is hydrogen,
or phenyl optionally substituted with halogen, trifluoromethyl, hydroxy,
and
R1 is hydrogen or
and
AU is optionally a single bond or a double bond;
or a pharmaceutically acceptable salt thereof.

2-. A method of preparing a compound according to claim 1 ,
CHARACTERIZED in

a) reacting a compound of formula II

wherein R\ R2, X, Y, p, q and r are as defined above and W is a suitable leaving group such as halogen, p-toluene sulphonate or mesylate, with a compound of formula III

HZ (III)

wherein Z is as defined above to form a compound of formula I; or

b) hydrolyzing a compound of formula I, wherein R4 is
to form a compound of formula I wherein R4 is OH.

3_i A pharmaceutical composition comprising as active component a compound according to claim 1 together with a pharmaceutically carrier or diluent.

4 A pharmaceutical composition suitable for treating neurogenic inflammation comprising an effective amount of a compound according to claim 1 together with a pharmaceutically acceptable carrier or diluent.

J The pharmaceutical composition according to claim 3 or 4 comprising between 0.5 mg and 1000 mg of the compound according to claim 1 per unit dose.

£ . A method of treating neurogenic inflammation in a subject in need of such treatment comprising administering to said subject an effective amount of a compound according to claim 1 .

" . A method of treating neurogenic inflammation in a subject in need of such treatment comprising administering to said subject a pharmaceutical composition according to claim 4.

J The use of a compound according to claim 1 for preparing a medicament for treatment of neurogenic inflammation.