Novartis Ag

Speedel Experimenta Ag

Christoph Schumacher

Peter Herold

Robert Mah

Stefan Stutz

Vincenzo Tschinke

Michael Siegfried Quirmbach

Thomas Holbro

Gary Michael Ksander

Qi-Ying Hu

Julien Papillon

Aleksandar Stojanovic

Christiane Marti

Erik Meredith

Dirk Behnke

Lauren Gilchrist Monovich

Nathalie Jotterand

Michael Quirmbach

Isabelle Lyothier

The present invention relates to the NEP inhibitor pro-drug N-(3-carboxy-1-oxopropyl)-(4S)-p-phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid ethyl ester, or a pharmaceutically acceptable salt thereof; or the NEP inhibitor N-(3-carboxy-1-oxopropyl)-(4S)-p-phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid, or a pharmaceutically acceptable salt thereof, pro-drug for use in the treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling; a method for treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling comprising administration of a therapeutically effective amount, or a prophylactically effective amount, of the NEP inhibitor or the NEP inhibitor pro-drug, or a pharmaceutically acceptable salt pro-drug thereof, to a subject, e.g. a human subject, in need of such treatment. The present invention further relates to a pharmaceutical composition or a commercial package comprising the NEP inhibitor or the NEP inhibitor pro-drug, or a pharmaceutically acceptable salt thereof, pro-drug for use in the treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling.

Inhibitors for treating diseases characterized by atrial enlargement or remodeling

The present invention relates to the NEP inhibitor pro-drug N-(3-carboxy-1-oxopropyl)-(4S)-p -phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid ethyl ester, or a pharmaceutically acceptable salt thereof; or the NEP inhibitor N-(3-carboxy-1-oxopropyl)-(4S)-p -phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid, or a pharmaceutically acceptable salt thereof, pro-drug for use in the treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling; a method for treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling comprising administration of a therapeutically effective amount, or a prophylactically effective amount, of the NEP inhibitor or the NEP inhibitor pro-drug, or a pharmaceutically acceptable salt pro-drug thereof, to a subject, e.g. a human subject, in need of such treatment. The present invention further relates to a pharmaceutical composition or a commercial package comprising the NEP inhibitor or the NEP inhibitor pro-drug, or a pharmaceutically acceptable salt thereof, pro-drug for use in the treatment, prevention or delay of progression of a disease characterized by atrial enlargement and/or remodeling.

The present invention relates to a method of treating a disease or disorder characterized by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or &#x2014;C(O)N(R)(R) wherein Rand Rare independently &#x2014;(C-C) alkyl, or &#x2014;(C-C) alkyl-(C-C) aryl, wherein each of Rand Ris optionally substituted by &#x2014;(C-C) alkoxy; R, R, and R, are independently hydrogen, halogen, cyano or &#x2014;(C-C) aryl, wherein said &#x2014;(C-C) aryl is optionally substituted by halogen, with the proviso that no more than one of R, R, and Ris hydrogen; and Rand Rare hydrogen; or a pharmaceutically acceptable salt thereof. 

Use of an adrenal hormone-modifying agent

The application relates to novel heterocyclic compounds of the general formula (I) in which R, R, R, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors. 

Tetrahydro-imidazo [1,5-A] pyridyin derivatives as aldosterone synthase inhibitors

The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or &#x2014;C(O)N(R)(R) wherein Rand Rare independently &#x2014;(C-C)alkyl, or &#x2014;(C-C)alkyl-(C-C)aryl, wherein each of Rand Ris optionally substituted by &#x2014;(C-C)alkoxy; R, R, and R, are independently hydrogen, halogen, cyano or &#x2014;(C-C) aryl, wherein said &#x2014;(C-C)aryl is optionally substituted by halogen, with the proviso that no more than one of R, R, and Ris hydrogen; and Rand Rare hydrogen; or a pharmaceutically acceptable salt thereof.

The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R, R, W, X, Y, Z and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors. 

Heterocyclic spiro-compounds as aldosterone synthase inhibitors

The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R, R, U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors. 

The application relates to novel heterocyclic compounds of the general formula (I) in which R, R, R, W, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors. 

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Bettingen, Switzerland

Christoph Schumacher