Novartis Ag

Speedel Experimenta Ag

Dirk Behnke

Peter Herold

Robert Mah

Vincenzo Tschinke

Stefan Stutz

Aleksandar Stojanovic

Christiane Marti

Stjepan Jelakovic

Michael Siegfried Quirmbach

Nathalie Jotterand

Manuel Koller

David Orain

David Carcache

Peter Ertl

Claudia Betschart

Vinod Shashikant Chaudhari

Simona Cotesta

Chetan Pandit

Sangamesh Badiger

Jun Liu

Jürgen Wagner

Silvio Ofner

Timothy Z Hoffman

Juergen Klaus Maibaum

Christoph Schumacher

Samuel Hintermann

Isabelle Lyothier

Qihui Jin

Yefen Zou

Murali Chebrolu

Frank Peter Hollinger

Zenon D Konteatis

Yun Feng Xie

Jianfeng Pan

Xueshi Hao

Cameron Lee

Jürgen Hans-Hermann Hinrichs

Arnaud Lacoste

Jennifer Lee Ludington

Tingting Mo

Arndt Meyer

Frada Berenshteyn

Yahu Liu

Xin Qu

Jan Tchorz

Shanshan Yan

Michael Quirmbach

Frank Hollinger

Jennifer L Ludington

The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein. The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.

6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors

The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

Diazepinone derivatives

The invention relates to compound of the formula (I') in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. 

Disubstituted heteroaryl-fused pyridines

The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. 

Diaza-spiro[5.5]undecanes

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 present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors. 

Substituted piperidines as renin 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

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. 

Process for preparing a compound of the formula (I) in which Rand Rare each independently H, C-C-alkyl, halogen, polyhalo-C-C-alkoxy, polyhalo-C-C-alkyl, C-C-alkoxy, C-C-alkoxy-C-C-alkyl, or C-C-alkoxy-C-C-alkoxy, where Rand Rare not both H, and Ris C-C-alkyl, which is characterized in that a) a compound of the formula (II) in which Rand Rare each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which 'alkyl' is as defined above for Rto give a compound of the formula (I). 

Process for preparing organic compounds

Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent. 

Substituted piperidines

Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which Ris straight-chain C-alkanoyloxy, straight-chain C-alkoxy, straight-chain C-alkoxy-straight-chain-C-alkoxy, straight-chain C-alkoxycarbonylamino, straight-chain C-alkylcarbonylamino, optionally N-mono- or N,N-di-C-alkylated amino or hydroxy or straight-chain omega-hydroxy-C-alkyl. 

Substituted 4-phenyl piperidines for use as renin inhibitors

Growing community of inventors

Grenzach-Wyhlen, Germany

Dirk Behnke