Novartis Ag

Ciba-Geigy Corporation

Irm LLC

Allocyte Pharmaceuticals Ag

Novartis Pharma Gmbh

Pascal Furet

Werner Breitenstein

Paul William Manley

Sandra Jacob

Marcus Baumann

Nils Ostermann

Juergen Klaus Maibaum

Giorgio Caravatti

Claus Ehrhardt

Keiichi Masuya

Philipp Grosche

Fumiaki Yokokawa

Robert W Lang

Richard Sedrani

Yuki Iwaki

Konrad Oertle

Takeru Ehara

Shinichiro Matsunaga

Nathanael Schiander Gray

Yi Liu

Werner Fory

Manfred Boger

Guido Bold

Xiaolin Li

Valentina Molteni

Robert Nyfeler

Marc Lang

Vito Guagnano

Tetsuo Uno

Terence Alfred Kelly

Qiang Ding

Guobao Zhang

Bing Li

Jon Christopher Loren

Juliet Nabakka

Xiaodong Liu

Hans H Bosshard

Donatella Chianelli

Sylvain Cottens

Oliver Simic

Takanori Kanazawa

Kazuhide Konishi

Hans Michael Buerger

Margaret A Cudd

Andreas Von Sprecher

Andreas Beck

Genji Iwasaki

Joseph Schoepfer

Edgar Jacoby

Taebo Sim

Edwige Liliane Jeanne Lorthiois

Paul Wenk

Kenji Hayakawa

Junichi Sakaki

Holger Sellner

Masaki Suzuki

Motowo Nakajima

Shinichi Koizumi

Yuko Hitomi

Atsushi Toyao

Juerg Zimmermann

Tatsuhiko Kasaoka

Carsten Spanka

Andreas Marzinzik

Carole Pissot Soldermann

Timothy M Ramsey

Gabriele Weitz-Schmidt

Shimpei Kawakami

Gisbert Schneider

Atsuko Iwasaki

Claus Erhardt

Atsuko Nihonyanagi

Marianne Huerzeler

Riccardo Mancuso

Juerg Zimmerman

Uerg Zimmermann

The present invention relates to novel compounds which are capable of inhibiting the interaction of LFA-1 with its counter ligands.

Small molecule LFA-1 inhibitors

The invention relates to compounds of formula (I) wherein the substituents X, R, R, Rand Rhave the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

Compounds and compositions as protein kinase 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 invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.

Compounds and compositions as c-kit and PDGFR kinase 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

The invention relates to 3,5-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 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula I wherein R1, R2, T, R3 and R4 are as defined in the specification. 

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, 

&#x3b1;-Amino hydroxamic acid derivative of the formula I, in which R is C-C-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C-C-cycloalkyl or unsubstituted or substituted C-C-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C-C-alkenyl or C-C-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C-C-cycloalkyl or unsubstituted or substituted C-C-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N;and the other symbols are as defined in claimare described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).

Arylsulfonamido-substituted hydroxamic acid derivatives

The invention relates to compounds of formula 

Inhibitors of tyrosine kinases

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 invention relates to novel substituted N-(3-benzoylaminophenyl)-4-pyridyl-2-pyrimidinamine derivatives, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, and a method for the treatment of such a disease.

Pyrimidineamide derivatives and the use thereof

The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.

The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.

N-phenyl-3-pyrimidine-amine derivatives

N-phenyl-2-pyrimidine-amine derivatives

Growing community of inventors

Basel, Switzerland

Werner Breitenstein