Hoffmann-la Roche Inc.

Narendra Panday

Henrietta Dehmlow

Bernd Kuhn

Matthew Wright

Hans Hilpert

Hasane Ratni

Wolfgang Haap

Fabienne Ricklin

Katrin Groebke Zbinden

Johannes Aebi

Jean Ackermann

Raffaello Masciadri

Olivier Morand

Markus Boehringer

Thomas Weller

Alexander Chucholowski

Tanja Schulz-Gasch

Jacques Himber

Sabine Wallbaum

Uwe Grether

Hans G Richter

Rainer Eugen Martin

Konrad H Bleicher

Georges Hirth

Minmin Yang

Beat Wirz

Hans Iding

Hans-Peter Maerki

Eric Joseph Niesor

Roland Humm

Christoph Martin Stahl

Gregory Martin Benson

Lilli Anselm

Franz Schuler

Stefan Thomi

Dietmar Knopp

Katrin Gröbke Zbinden

Xavier Marie Warot

The present invention relates to compounds of the formula (I) wherein R, R, R, R, R, X, X, X, X, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR&#x3b1; and/or LXR&#x3b2; agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.

Tetrahydrocarbazoles and derivatives

The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein Rto R, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Hexafluoroisopropanol derivatives

The invention is concerned with cyclic amines of formula (I) wherein Xto X, Yto Y, R, Rand 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 and for treating diseases associated with coagulation factor Xa.

Cyclic amines

The invention is concerned with novel heteroaryl carboxamides of formula (I) wherein A, R, R, X, Y, Z and m 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 for the treatment or prevention of thrombotic disorders.

Heteroaryl carboxamides

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 invention is concerned with novel cycloalkane carboxamides of formula (I) wherein X, X, Y, Y, R, R, 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 the coagulation factor Xa and can be used as medicaments.

Factor Xa inhibitors

The invention is concerned with novel benzimidazole derivatives of formula (I) wherein Rto Rare as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.

Benzimidazole derivatives

The invention is concerned with novel pyrrolidine derivatives of formula (I) wherein X, Y, R, Rand 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.

Pyrrolidine 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 relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R, R, R, R, R, R, A, m, n and p are defined as in claim. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.

Indolyl derivatives as liver-X-receptor (LXR) modulators

The invention is concerned with novel hexafluoroisopropanol substituted ether derivatives of formula (I): wherein Rto Rare as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Hexafluoroisopropanol substituted ether derivatives

The present invention relates to compounds of formula I wherein R, R, R, R, R, U, V, W, k and m are as defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasit infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Aminoalkylamide substituted cyclohexyl 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.

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Basel, Switzerland

Narendra Panday