Hoffmann-la Roche Inc.

Harvard College

Other

Christian D Lerner

Jason D Brubaker

Andrew G Myers

Mark G Charest

Dionicio R Siegel

Philippe Pflieger

Daniel Hunziker

Alexander Flohr

Song Yang

Katrin Groebke Zbinden

Ulrike Obst Sander

Min Wang

Chengang Zhou

Bernd Kuhn

Roland Jakob-Roetne

Jens-Uwe Peters

Tanja Schulz-Gasch

Markus Rudolph

Jianhua Wang

Xingchun Han

Cornelia Hertel

Yongguang Wang

Jacques Bailly

Yongqiang Liu

Sébastien Schmitt

Sandra Marie Joseph Grall-Ulsemer

Mathis Braendlin

Mingming Li

Matthias Heinrich Nettekoven

Hans Hilpert

Bernd Buettelmann

Caterina Bissantz

Matthias Koerner

Werner Mueller

Roland Humm

Pius Waldmeier

Bernd Puellmann

Thorsten Muser

Jean-Baptiste Blanc

Thomas Ryckmans

Herve Schaffhauser

Ralph Paulini

François Diederich

René Bonnafous

Lukas Kreis

Christian Kramer

Jason D Brubacker

The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, D, Rto R, and Rto Rare as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

Heterocyclic compounds

The disclosure provides novel imidazole pyrazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, Rand Rto Rare as described herein:  Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.

Imidazole-pyrazole derivatives

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Synthesis of tetracyclines and analogues thereof

The present invention relates to compounds having the general formula (Ia) or (Ib), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease, in particular influenza.

Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease

The present invention relates to compounds of formula wherein the substituents are described in claimand to the pharmaceutically acceptable salts thereof. These compounds inhibit the enzyme catechol-O-methyltransferase (COMT). The compounds may be used for the treatment of Parkinson's disease, depression, cognitive impairment and motor symptoms, resistant depression, cognitive impairment, mood and negative symptoms of schizophrenia.

COMT inhibitors

The present invention relates to compounds of formula (I) and its use for the treatment of neurological disorders. 

Triazolo compounds

The invention relates to compounds of formula I 

Pyrrolidino heterocycles

The present invention provides compounds of formula (Ia) and (Ib) 

Triazolo compounds as PDE10 inhibitors

The present invention relates to compounds of formula I wherein A, n, Rto Rand Rto Rare as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Glucocorticoid receptor antagonists

The present invention relates to compounds of formula I wherein Rto R, R, Rand Rare as defined in the description and claims and Rsignifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds

Growing community of inventors

Binningen, Switzerland

Christian D Lerner