Hoffmann-La Roche Inc.

Andrea Cesura

Stephan Rover

Geo Adam

Andrew William Thomas

Rene Wyler

Rosa Maria Rodriguez Sarmiento

Jurgen Wichmann

Francedillaois Jenck

Emmanuel Pinard

Sabine Kolczewski

Guido Galley

Michelangelo Scalone

J&uuml;rgen Wichmann

Fran&ccedil;ois Jenck

Caido Galley

Stephan R&ouml;ver

Frederick Monsma, Jr

Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.

Mitochrondrial permeability transition pore affinity labels and modulators

This invention relates to phthalimido derivatives of the formulawherein X is &#x2014;N&#x2550; or &#x2014;CH&#x2550;, and Rto Rand m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.

Phthalimido derivatives and a process for their preparation

Isoquinoline derivatives

Pyridine amido derivatives

Di-or triaza-spiro &lsqb;4,5&rsqb; decane derivatives

The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;

Piperidine derivatives

The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl;

Diaza-spiro[3,5] nonane derivatives

The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen;

1,3,8-triazaspiro[4,5]decan-4-one derivatives

The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.

1,3,8,-triaza spiro (4,5)decan-4-on derivatives

The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R Signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,

Use of N-(4-aryl-thiazol-2-yl)-sulfonamides

The invention is concerned with the use of sulfonamide derivatives of the general formula ##STR1## wherein R signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino,

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Basel, Switzerland

Andrea Cesura