Novartis Ag

Other

Sandoz Gmbh

Richard Sedrani

Sylvain Cottens

Claus Ehrhardt

Rainer Albert

Peter Von Matt

Gerhard Zenke

Jean-Pierre Evenou

Nils Ostermann

Nigel Graham Cooke

Holger Sellner

Werner Breitenstein

Juergen Klaus Maibaum

Finton Sirockin

Kenji Namoto

Stefanie Flohr

Trixi Brandl

Barbara Haeberlin

Jürgen Wagner

Daniel Baeschlin

Garry Fenton

Jacky Vonderscher

Wolfgang Miltz

Michael A Dechantsreiter

Stefan Andreas Randl

Thomas Zoller

Christian Markert

Jonathan E Grob

Valerie Quesniaux Ryffel

Valerie Quesniaux

Bernard Pirard

Val&eacute;rie Quesniaux Ryffel

J&uuml;rgen Wagner

Aengus Macsweeney

Eric Valeur

Sebastian Kopec

Valerie Q Ryffel

Julie Lachal

Perle Nganga

Martin Renatus

Aengus Mac Sweeney

The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. 

Complement pathway modulators and uses thereof

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides

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

Monoclonal antibodies to rapamycin and to 40-O-alkylated derivatives of rapamycin are provided, together with novel haptens, immunogenic conjugates, and processes for making them and assay kits for using them.

Rapamycin assay

The present invention relates to compounds of the formula; and their use in therapy.

Organic compounds

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

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. 

This invention provides a microemulsion pre-concentrate comprising a difficultly soluble active agent and a carrier medium comprising 1) a hydrophilic phase which comprises dimethylisosorbide and/or a lower alkyl alkanoic ester, 2) a lipophilic phase, and 3) a surfactant. The active agent may be a cyclosporin or a macrolide. In another aspect, this invention provides a pharmaceutical composition for enteral or parenteral administration comprising a macrolide and an acid.

Pharmaceutical compositions

Novel derivatives of rapamycin, particularly 9-deoxo-rapamycins, 26-dihydro-rapamycins, and 40-O-substituted and 28,40-O,O-disubstituted rapamycins. are found to have pharmaceutical utility, particularly as immunosuppressants.

O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants

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Basel, Switzerland

Richard Sedrani