Godecke Aktiengesellschaft

Goedecke Aktiengesellschaft

Warner-lambert Company

Karl Mannhardt

Johannes Hartenstein

Gerhard Satzinger

Jurgen Kleinschroth

Hartmut Osswald

Edgar Fritschi

Bernd Wagner

Gunter Weinheimer

Manfred F Herrmann

Wolfgang Steinbrecher

Jorgen Kleinschroth

Christoph Schachtele

Claus Rudolph

Uwe Trostmann

Gunter Wolf

Dieter Marme

Horst-Dietmar Tauschel

Gonter Weinheimer

Dieter Muster

The present invention covers a novel series of 2-acyloxypropylamine derivatives, processes for preparing them, compositions containing them, and methods for using them. The compounds are active in the inhibition of protein kinase C and thrombocyto aggregation stimulated by diacylglycerols.

2-acyloxypropylamino derivatives, processes for the preparation thereof,

4-Alkoxy-pyrido[2,3-d]pyrimidine derivatives are described as well as processes for their preparation. For reason of their vasospasmolytic effects these compounds are mainly indicated for the treatment of cerebral, cardiac, and peripheral vascular diseases such as myocardiac ischemia, cerebral infarction, pulmonary thromboses, as well as in cases of arterioschlerosis and other stenotic disorders. They are therefore valuable agents for combating cardiovascular mortality.

4-alkoxy-pyrido[2,3-d]pyrimidine derivatives for treatment of myocardiac

The present invention describes 1,6-naphthyridine derivatives of the general formula: ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromatic or heteroaromatic ring, R.sup.2 is a straight-chained or branched alkyl radical containing up to four carbon atoms or a benzyl radical, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radicals or an alkoxycarbonyl radical containing up to four carbon atoms, R.sup.4 is a straight-chained or branched alkyl radical containing up to four carbons and R.sup.5 is a carboxyl group or a straight-chained, branched or cyclic alkoxycarbonyl radical which contains up to 17 carbon atoms and optionally also contains an oxygen, sulphur or nitrogen atom; as well as the pharmacologically acceptable salts thereof, which are useful for treating diseases of the blood vessels.

1,6-naphthyridine derivatives useful for treating diseases of the blood

The present invention provides 1,6-naphthyridine derivatives of formula ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromatic or heteroaromatic ring or an unsubstituted or substituted condensed aromatic or heterocyclic ring system, R.sup.2 is a straight-chained or branched alkyl radical containing up to 4 carbon atoms, a benzyl radical or a straight-chained or branched, substituted or unsubstituted aminoalkyl radical containing up to 8 carbon atoms, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radical or an alkoxycarbonyl radical, in each case containing up to 4 carbon atoms, R.sup.4 is a straight-chained or branched hydrocarbon radical containing up to 21 carbon atoms, which can also contain oxygen, sulphur, nitrogen or halogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems, or is an amino, cyano, formyl, halogenomethyl or dihalomethyl radical and R.sup.5 is an alkoxycarbonyl radical or an unsubstituted or substituted carboxamide radical with, in each case, up to 21 carbon atoms which can also contain oxygen, sulphur or nitrogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems or is a carboxyl or cyano group as well as the pharmaceutically acceptable salts thereof. The compounds are useful for blood vessel diseases. The present invention also provides processes for the preparation of these 1,6-naphthyridine derivatives, pharmaceutical compositions containing them, and methods for using them.

1,6-naphthyridine derivatives

The present invention provides a unique series of pyrido[4,3-b][1,6]naphthyridine derivatives. The compounds are calcium antagonists and are useful for blood vessel diseases. This invention also covers processes for preparing the compounds, pharmaceutical compositions containing them, and methods for using them.

Treating blood vessel diseases with

New 1,6-naphthyridinone derivatives of the formula I ##STR1## are herein described wherein R.sup.1 represents an unsubstituted or substituted aromatic or heteroaromatic ring;

Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis

4-Alkoxy-pyrido[2,3-d]pyrimidine derivatives are described as well as processes for their preparation. For reason of their vasospasmolytic effects these compounds are mainly indicated for the treatment of cerebral, cardiac, and peripheral vascular diseases such as myocardiac ischemia, cerebral infarction, pulmonary thromboses, as well as in cases of arteriosclerosis and other stenotic disorders. They are therefore valuable agents for combating cardiovascular mortality.

4-alkoxy-pyrido[2,3-d]pyrimidine derivatives

The invention concerns new 5-alkoxy-pyrido[4,3-d]pyrimidine derivatives and pharmacologically acceptable salts thereof, as well as a chemically novel process for their preparation. The new compounds are used in the control of cerebral, cardiac or peripheral vascular diseases or of stenotic symptoms.

5-alkoxy-pyrido[4,3-d]pyrimidine derivatives

The invention concerns new 5-oxo-pyrido[4,3-d]pyrimidine derivatives and the pharmacologically acceptable salts thereof, as well as a chemically novel process for the preparation of the new compounds and their use in the control of cerebral, cardiac, or peripheral vascular diseases or of stenotic symptoms.

5-oxo-pyrido[4,3-]pyrimidine derivatives

4-Oxo-pyrido[2,3-d]pyrimidine derivatives are herein described as well as processes for their preparation. These compounds possess valuable pharmacological properties. As calcium antagonists they exert vasospasmolytic, vasodilatory, and antihypertensive activities. Surprisingly some of the compounds also have the effect of increasing contractility. They are therefore particularly suited for the treatment of vascular diseases.

4-oxo-pyrido[2,3-d]pyrimidinone derivatives

The invention is concerned with partially new compounds of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group with up to four carbon atoms and R.sup.2 a substituted phenyl radical and the pharmacologically acceptable salts thereof. The compounds can be prepared according to known procedures and show surprisingly a cardiovascular efficacy. They are capable of decompensating cardiac insufficiencies to a large extent. In addition to the new compounds, claim is also made for pharmaceutical compositions which contain compounds according to the general formula and their application for controlling cardiac and vascular diseases.

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Elzach-Oberprechtal, Germany

Karl Mannhardt