Ciba-geigy Corporation

Speedel Pharma Ag

Circomed LLC

Daniel Bellus

Hans Zweifel

Angelo Storni

Walter Schilling

Pierre Martin

Hans Greuter

Eginhard Steiner

Marcus Baumann

Niklaus Buhler

Alex Alder

Werner Fory

Laurenz Gsell

Jaroslav Stanek

Elmar Sturm

Willy Meyer

Dieter Reinehr

Kurt Weber

Rudolf Kirchmayr

Hanspeter Fischer

Hans Tobler

Adrian Waldner

Roger F Malherbe

Louis Felder

Guglielmo Kabas

Alwyn Spencer

Achim Roloff

Hans-Ulrich Blaser

Alessandro Dondoni

Barbara Staehelin

Herman Kempen

Jaroslaw Stanek

The invention relates to new thienotriazolodiazepine derivatives of the formula (1) wherein Ris CH, Ris CHor &#x2014;(CH)&#x2014;Ror &#x2014;(CH)&#x2014;O&#x2014;Ror &#x2014;(CH)&#x2014;S&#x2014;Rwherein n is 1, 2, 3 or 4 and Ris CH, CHCHor CHCHOCH, and Ris hydrogen or &#x2014;OCHO&#x2014; or &#x2014;OCHCHO&#x2014; connected to the ortho/meta position or meta/para position of the phenyl ring; or wherein Rand Rare hydrogen and Ris &#x2014;OCHO&#x2014; Or &#x2014;OCHCHO&#x2014; connected to the ortho/meta position or meta/para position of the phenyl ring; and pharmaceutically acceptable acid addition salts thereof. These compounds and pharmaceutical compositions containing them are useful in the treatment and prevention of atherosclerotic artery diseases, such as myocardial infarction and stroke, and of Alzheimer's disease. 

Thienotriazolodiazepine derivatives active on apo A

Process for the preparation of aryloctanoyl amides

1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

Certain 1-phenyl-cyclobutane-1,3-dicarboxylic acid type compounds

1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

Substituted azabicycloheptanes, the use thereof, pharmaceutical

The invention relates to a process for the preparation of pyridine-2,3-dicarboxylic acid derivatives of formula ##STR1## which process comprises reacting a hydrazone of formula II ##STR2## with a maleic acid derivative of formula III ##STR3## to give a 1-amino-1,4-dihydropyridine-2,3-dicarboxylic acid derivative of formula IV ##STR4## and subsequently removing R.sub.9 R.sub.10 NH. In the above formulae, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, R.sub.10 and X are as defined in claim 1. The pyridine-2,3-dicarboxylic acid derivatives of formula I are intermediates for the preparation of herbicidal compounds.

Process for the preparation of pyridine-2-3-dicarboxylic acid

Substituted-3-azabicyclo[3.1.1]heptane-2,4-diones useful for treating

Anhydrides of formula V ##STR1## where A' is --CH.sub.2 CH.sub.2 --, and R and R.sub.1 independently of one another are hydrogen, halogen, alkyl having 1 to 4 carbon atoms or methoxy are valuable intermediates for the preparation of tricyclic imidyl derivatives. These imidyl derivatives form photocrosslinkable polymers useful for making printing plates and photoresists.

6,7-Dihydro-5H-benzocycloheptene-8,9-dicarboxylic acid anhydrides

Anhydrides of formula V ##STR1## where A' is --OCH.sub.2 -- with the oxygen atom bonded to the aromatic ring and R and R.sub.1 independently of one another are hydrogen, halogen, alkyl having 1 to 4 carbon atoms or methoxy are valuable intermediates for the preparation of tricyclic imidyl derivatives. These imidyl derivatives form photocrosslinkable polymers useful for making printing plates and photoresists.

2,3-Dihydro-1-benzoxepine-4,5-dicarboxylic acid anhydrides

The invention relates to vinylstilbene compounds of the formula ##STR1## wherein Q is the grouping --COX or ##STR2## These compounds are obtained by reacting 1 molar equivalent of a compound of the formula II ##STR3## wherein X is chlorine, bromine or iodine, in the presence of a base and with the addition of palladium metal or of palladium compounds, as catalyst, which, under the reaction conditions, form labile palladium(O) compounds which do not contain phosphorus, with 1 molar equivalent of a compound of the formula III or with 1 molar equivalent of each of the compounds of the formulae III and IV ##STR4##

Process for the production of vinylstilbene compounds

Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## �n=1 or 2, Y=a bridge member and X=a functional group! are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.

Tricyclic imidyl derivatives

Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.

Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as pohtoresists.

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Riehen, Switzerland

Daniel Bellus