Novartis Ag

Novartis Pharma Gmbh

Junichi Sakaki

Genji Iwasaki

Kenji Hayakawa

Claudia Betschart

Rene Lattmann

Osamu Irie

Martin Missbach

Motowo Nakajima

Naoki Teno

Eva Altmann

Werner Breitenstein

Shinichiro Matsunaga

Takanori Kanazawa

Paivi Jaana Kukkola

Shinichi Koizumi

Masashi Kishida

Tatsuhiko Kasaoka

John Henry Van Duzer

Keiichi Masuya

Ruben Alberto Tommasi

Leslie Wighton McQuire

Takeru Ehara

Fumiaki Yokokawa

Terance William Hart

Kazuhide Konishi

Leslie Ann Robinson

Paul David Greenspan

Leslie Anne Robinson

Allan Hallett

Scott Douglas Cowen

Atsuko Iwasaki

Hironobu Mitani

Hajime Hirao

Hidefumi Uchiyama

Michihiro Takai

Miyuki Horiuchi

Keigo Gohda

Masaaki Kimura

&#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 provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

Heteroaryl nitrile derivatives

The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with RXR-antagonism, in particular selected from diabetes, complication of diabetes such as retinopathy, nephropathy, neuropathy, and hyperlipidemia, obesity, dyslipidemia, and osteoporosis.

11-phenyl-dibenzodiazepine derivatives as RXR-antagonists

The present invention relates to the use of a 2-cyanopyrimidine compound of the formula wherein

Compounds and compositions useful as cathepsin S inhibitors

The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors. 

Hetereoaryl nitrile derivatives

The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors. 

Pyrrolo pyrimidines as agents for the inhibition of cystein proteases

&#x3b1;-Amino hydroxamic acid derivative of formula (I), in which R is C&#x2013;C-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C&#x2013;C-cycloalkyl or unsubstituted or substituted C&#x2013;C-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C&#x2013;C-alkenyl or C&#x2013;C-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C&#x2013;C-cycloalkyl or unsubstituted or substituted C&#x2013;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 claim, are 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 invasi n) and pulmonary disorders (e.g. emphysema, COPD).

Compounds of formula (I) wherein W is &mdash;OH or &mdash;NHOH; X is an optionally substituted heterocycle, NR SO R , heterocyclylalkythio, CONR R or NR COR ; Y, Z, R -R and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.

Sulfonylamino derivatives which inhibit matrix-degrading metalloproteinases

Dipeptide nitriles

Sulfonylamino acid and sulfonylamino hydroxamic acid derivatives

Growing community of inventors

Ibaraki Pref., Japan

Junichi Sakaki