Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Markus Boehringer

Fabienne Ricklin

Bernd Michael Loeffler

Hans Hilpert

Daniel Hunziker

Bernd Kuhn

Katrin Groebke Zbinden

Wolfgang Haap

Hans Peter Wessel

Narendra Panday

Peter Mohr

Patrizio Mattei

Uwe Grether

Jens-Uwe Peters

Robert Narquizian

Holger Kuehne

Alfred Binggeli

Hans-Peter Maerki

Ramakanth Sarabu

Markus Meyer

Peter Weiss

Thomas Luebbers

Georges Hirth

Matthias Steger

Claus Riemer

Hans Iding

Roland Humm

Jacques Himber

Christoph Martin Stahl

Hans Peter Marty

Dietmar Knopp

The present invention relates to compounds of formula (I) wherein R, R, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

DPP IV inhibitors

The invention is concerned with novel heteroarylacetamides of formula (I)R&#x2014;C(O)&#x2014;N(R)&#x2014;R&#x2014;CH&#x2014;C(O)&#x2014;N(R)(R)&#x2003;&#x2003;(I)wherein Rto Rare as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Heteroarylacetamide inhibitors of factor Xa

The present invention relates to compounds of formula (I) wherein Ris as defined in the description, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Pyrido [2,1-a] isoquinoline derivatives

The present invention relates to compounds of the formula (I) wherein Rand Rare as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or &#x3b2;-cell protection.

4-aminopiperidine derivatives

The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, R, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Dicarboxamide derivatives

The invention is concerned with novel heteroaryl fused cyclic amines of formula (I) wherein A, Xto X, Yto Y, Z, R, R, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments.

Factor Xa inhibitors

The present invention relates to compounds of formula (I) wherein Ris as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Aminocycloalkanes as DPP-IV inhibitors

The present invention relates to compounds of formula (I) wherein wherein R, R, R, R, R, Rand n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPAR&#x3b1; and/or PPAR&#x3b3; agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.

Oxazole derivatives

The present invention provides compounds of formula (I) wherein R, R, Rand Rare as indicated in the description, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

The present invention provides compounds of formula (I)wherein R, R, R, Rand X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Pyridine and pyrimidine derivatives

The present invention relates to compounds of formula (I)wherein wherein R, R, R, R, R, Rand n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPAR&#x3b1; and/or PPAR&#x3b3; agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.

The present invention relates to compounds of formula (I)wherein R, R, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

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Moehlin, Switzerland

Markus Boehringer