Novartis Ag

Other

Focke & Co.

Novartis Pharma Gmbh

Claus Ehrhardt

Rainer Albert

Richard Sedrani

Nils Ostermann

Juergen Klaus Maibaum

Werner Breitenstein

Michael David Shultz

Ruben Alberto Tommasi

Leslie Wighton McQuire

Peter Von Matt

Sylvain Cottens

Olivier Rogel

Pascal Rigollier

Gerhard Zenke

Jean-Pierre Evenou

Jürgen Wagner

Nigel Graham Cooke

Josef Gottfried Meingassner

Holger Sellner

Keiichi Masuya

Yuki Iwaki

Philipp Grosche

Takeru Ehara

Klaus Hinterding

Fumiaki Yokokawa

Sompong Wattanasin

Ulrich Hommel

Kazuhide Konishi

Gabriele Weitz-Schmidt

Yuko Hitomi

Atsushi Toyao

Karl Welzenbach

Stefanie Flohr

Wilfried Bauer

Peter Ettmayer

Oliver Simic

Joerg Kallen

Edwige Liliane Jeanne Lorthiois

Takanori Kanazawa

Masaki Suzuki

Andreas Marzinzik

Peter Nussbaumer

Osamu Irie

Stefan Andreas Randl

Rolf Baenteli

Ulrich Hassiepen

Klemens Högenauer

Frederic Berst

Ursula Bodendorf

Bernd Gerhartz

Atsuko Iwasaki

Gabriele Weitz Schmidt

J&ouml;rg Kallen

Atsuko Nihonyanagi

Edwige Liliane Lorthiois

Fran&ccedil;ois Nuninger

J&uuml;rgen Wagner

Janet Dawson

Didier Roche

Edgar Jacoby

Hermann Roesink

The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

ArylSulfonamide-based matrix metalloprotease inhibitors

Arylsulfonamide based matrix metalloprotease inhibitors

Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

4-phenylpiperidine derivatives as renin inhibitors

The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.

Kallikrein 7 modulators

Arylsulfonamide-based matrix metalloprotease inhibitors

3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification. 

Organic compounds

3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula I, 

Compounds of formula I, wherein X, a, b, R, R, R, Rand Rare as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators

Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

Indolylmaleimide derivatives

The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis.

Compounds of the present invention having the formula (I) exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders. 

The present invention relates to amino-propanol derivatives, process for their production, their uses in treating and/or preventing diseases or disorders mediated by lymphocyte interactions, and pharmaceutical compositions containing them. For example, Compounds of formula I wherein A, R, R, R, Rand Rare as defined in the specification are described.

Amino-propanol derivatives as sphingosine-1-phosphate receptor modulator

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Lörrach, Germany

Claus Ehrhardt