Novartis Ag

Speedel Experimenta Ag

Christiane Marti

Peter Herold

Vincenzo Tschinke

Stefan Stutz

Aleksandar Stojanovic

Robert Mah

Michael Siegfried Quirmbach

Stjepan Jelakovic

Dirk Behnke

Nathalie Jotterand

Bibia Bennacer

Christoph Schumacher

Frank Peter Hollinger

Zenon D Konteatis

Jennifer Lee Ludington

Michael Quirmbach

Isabelle Lyothier

Frank Hollinger

Jennifer L Ludington

Heterocyclic compounds of the general formula (I) are provided in which R, R, R, R, Rand 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 aldostereone synthase inhibitors, 

Bis-heterocyclic imidazolyl compounds

Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R, R, Q, m and n have the meanings explained in detail in the description. Also provided are a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors. 

Imidazo compounds

Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R, R', Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors. 

Spiro-imidazo compounds

The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R, R, R, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.

Condensed imidazole derivatives as aldosterone synthase inhibitors

Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is &#x2014;CH&#x2014;; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, Ris Calkyl or Ccycloalkyl; Ris independently of one another H, Calkyl, Calkoxycarbonyl or Calkanoyl; Ris Calkenyl, Calkyl, unsubstituted or substituted aryl-Calkyl or Ccycloalkyl; Ris -L-R; L is Calkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; Ris a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from Calkyl, Calkoxy, cyano, halogen, Calkoxy-Calkyl, hydroxy-Calkyl or dialkylamino, or if m=0: is also saturated Cheterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from Calkyl, Calkoxy, cyano, halogen, Calkoxy-Calkyl, hydroxy-Calkyl or dialkylamino, or if m=1: is also saturated Cheterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from Calkyl, Calkoxy, cyano, halogen, C-alkoxy-Calkyl, hydroxy-Calkyl or dialkylamino; have renin-inhibiting properties and can be used as medicines for the treatment of hypertension. 

5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension

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. 

Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim, have renin-inhibiting properties and can be used as medicines. 

Alcanoic acid amides substituted by saturated O-heterocycles

The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R, R, R, Rand 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. 

The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R, R, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors. 

The invention relates to novel amino alcohols of the general formula (I) where X, R, R, R, R, Rand Rare each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors. 

Organic compounds

The application relates to novel alkanamides of the general formula (I) where X is &#x2014;CH&#x2014; or &#x3e;CH&#x2014;OH; (A) Ris e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; Ris C-C-alkyl or C-C-cydoalkyl; Rare each independently H, C-C-alkyl, C-alkoxycarbonyl or C-C-alkanoyl; Ris C-C-alkyl, C-C-cycloalkyl, C-C-alkenyl or unsubstituted or substituted arylC-C-alkyl; Ris C-C-alkyl, C-C-hydroxyalkyl, C-C-alkoxy-C-C-alkyl, C-C-alkanoyloxy C-C-alkyl, C-C-aminoalkyl, C-C-alkylamino-C-C-alkyl, C-C-dialkylamino-C-C-alkyl, C-C-alkanoylamido-C-C-alkyl, HO(O)C&#x2014;C-C-alkyl, C-C-alkyl-O&#x2014;(O)C&#x2014;C-C-alkyl, HN&#x2014;C(O)&#x2014;C-C-alkyl, C-C-alkyl-HN&#x2014;C(O)&#x2014;C-C-alkyl, (C,-C-alkyl)N&#x2014;C(O)&#x2014;C-C-alkyl, C-C-alkenyl, C-C-alkynyl, cyano-C-C-alkyl, halo-C-C-alkyl, optionally substituted aryl-C-C-alkyl, optionally substituted C-C-cycloalkyl-C-C-alkyl or optionally substituted heterocydyl-C-C-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension. 

5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension

The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R, R, R, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.

Compounds of the general formula (I) in which the meanings of the substituents R, R, R, R, X, Z and n as stated in claim 1 have renin-inhibiting properties and can be used as medicines. 

Substituted piperidines as renin inhibitors

The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R, R, R, Q, m and n have the meanings explained in detail in the description, and * designates an asymmetric carbon atom, a process for their preparation and the use of these compounds as medicaments, in particular as aromatase inhibitors. 

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Allschwil, Switzerland

Christiane Marti