Phthalazinones

Details Phthalazinones Phthalazinones

1999-07-14

2000-08-15

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544237, 544116, 514248, C07D23732, C07D40106, C07D41306, A61K 31502

Patent

active

061037184

DESCRIPTION:

BRIEF SUMMARY
FIELD OF APPLICATION OF THE INVENTION

The invention relates to novel Phthalazinones which are used in the pharmaceutical industry for the production of medicaments.


KNOWN TECHNICAL BACKGROUND

International Patent Application WO91/12251 describes phthalazinones having bronchodilating and thromboxane A2 synthetase inhibiting properties. International Patent Application WO94/12461 describes 3-aryl-pyridazin-6-one derivates as selective PDE4 inhibitors.


DESCRIPTION OF THE INVENTION

It has now been found that phthalazinones, which are described in greater details below, have surprising and particularly advantageous properties.
The invention thus relates to compounds of the formula I, ##STR1## in which R1 is 1-4C-alkoxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, which is completely or predominantly substituted by fluorine. --CH(R.sub.b).sub.2 or --C.sub.p H.sub.2p --Ar, in which 3-7C-alkenyl, 3-7C-alkynyl, phenyl-3-4C-alkenyl, 7-10C-polycycloalkyl, naphthyl, pyridyl, pyrazinyl, pyridazinyl, primidyl, quinazolinyl, quinoxalinyl, cinnolinyl, isoquinolyl, quinolyl, indanyl, benzoxazolyl, benzothiazolyl, oxazolyl, thiazolyl, N-methylpiperidyl, tetrahydropyranyl, tetrahydrothiapyranyl, or an unsubstituted or by R61 and/or R62 substituted phenyl radical, in which carboxy-1-4C-alkyl, 1-4C-alkoxycarbonyl, hydroxy-1-4C-alkyl, amino, mono- or di-1-4-C-alkylamino, 1-4C-alkylcarbonylamino, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, aminosulfonyl, mono- or di-1-4C-alkylaminosulfonyl, 4-methylphenylsulfonamido, tetrazol-5-yl, 2-(1-4C-alkyl)tetrazol-5-yl or 2-benzyl-tetrazol-5-yl and carboxyphenyloxy, phenoxy, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, 1-4C-alkylcarbonylamino, 1-4C-alkoxycarbonyl, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, amino, mono- or di-1-4C-alkylamino, or an unsubstituted or by R71 and/or R72 substituted piperidyl, piperazinyl, pyrrolidinyl or morpholinyl radical, where phenanthrenyl or anthracenyl radical, in which aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonyloxy, 1-4C-alkoxycarbonyl, amino, mono- or di-1-4C-alkylamino, 1-4C-alkylcarbonylamino, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, and completely or predominantly substituted by fluorine, primidinyl, quinazolinyl, quinoxalinyl, cinnolinyl, isoquinolyl, quinolyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzotriazolyl, N-benzosuccinimidyl, imidazolyl, pyrazolyl, oxazolyl, thiazolyl, furyl, thienyl, pyrrolyl, a 2-(1-4C-alkyl)-thiazol-4-yl radical, or a phenyl radical substituted by R10 and/or R11, in which carboxyl, carboxy-1-4C-alkyl, 1-4C-alkylcarbonyloxy, 1-4C-alkoxycarbonyl, amino, mono- or di-1-4C-alkyl-amino, 1-4C-alkylcarbonylamino, aminocarbonyl or mono- or di-1-4-C-alkylamino-carbonyl, and
On embodiment (embodiment a) of the invention are compounds of the formula I, in which substituted by fluorine, which is completely or predominantly substituted by fluorine, --CH(R9).sub.2 or --C.sub.p H.sub.2p --Ar, in which 3-7C-alkenyl, 3-7C-alkynyl, phenyl-3-4C-alkenyl, bornyl, norbornyl, adamantyl or an unsubstituted or by R61 and/or R62 substituted phenyl radical, in which 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, 1-4C-alkylcarbonylamino, 1-4C-alkoxycarbonyl, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, amino, mono- or di-1-4C-alkylamino, or an unsubstituted or by R71 and/or R72 substituted piperidyl, piperazinyl, pyrrolidinyl or morpholinyl radical, where phenanthrenyl or anthracenyl radical, in which aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonyloxy, 1-4C-alkoxycarbonyl, amino, mono- or di-1-4C-alkylamino, 1-4C-alkylcarbonylamino, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, and completely or predominantly substituted by fluorine, primidinyl, quinazolinyl, quinoxalinyl, cinnolinyl, isoquinolyl, quinolyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzotriazolyl, imida

REFERENCES:
patent: 4289774 (1981-09-01), Schacht et al.
patent: 5849741 (1998-12-01), Watanable et al.

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