Novartis Ag

The Medicines Company (leipzig) Gmbh

Speedel Experimenta Ag

The Medicines Company

Stjepan Jelakovic

Peter Herold

Robert Mah

Vincenzo Tschinke

Stefan Stutz

Aleksandar Stojanovic

Christiane Marti

Dirk Behnke

Andrea Schweinitz

Alexander Schulze

Claudia Reichelt

Friedrich-Alexander Ludwig

Mohammed Daghish

Michael Siegfried Quirmbach

Nathalie Jotterand

Frank Peter Hollinger

Zenon D Konteatis

Bibia Bennacer

Jennifer Lee Ludington

Ting Kang

Michael Quirmbach

Frank Hollinger

Jennifer L Ludington

The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.

Trypsin-like serine protease inhibitors, and their preparation and use

The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; Ris selected from the group consisting of &#x2014;CHNH, and Ris selected from the group consisting of &#x2014;H, &#x2014;OH, &#x2014;NHand acetyl; Ris selected from the group consisting of &#x2014;H, benzyloxycarbonyl and benzylsulfonyl; and Ris selected from the group consisting of &#x2014;OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;SO&#x2014;, methylene, &#x2014;CH(OH)&#x2014;, &#x2014;CH(NH)&#x2014;, &#x2014;CH(CH&#x2014;OH)&#x2014;, &#x2014;CH(CH&#x2014;NH)&#x2014; or &#x2014;N(R)&#x2014;, Ris selected from the group consisting of &#x2014;H or a simple (C-C) alkyl and Ris selected from the group consisting of &#x2014;H, a simple (C-C) alkyl or a simple (C-C) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa

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

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

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

Organic compounds

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. 

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. 

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Freiburg, Germany

Stjepan Jelakovic