Bayer Healthcare Aktiengesellschaft

Bayer Schering Pharma Ag

Bayer Aktiengesellschaft

Bayer Intellectual Property Gmbh

Basilea Pharmaceutica Ag

Bayer Pharma Aktiengesellschaft

Basilea Pharmaceutica International Ag

Intermed Discovery Gmbh

Jens Pohlmann

Thomas Lampe

Karl-Heinz Schlemmer

Elisabeth Perzborn

Alexander Straub

Susanne Röhrig

Josef Pernerstorfer

Joseph Pernerstorfer

Susanne Rohrig

Christoph Freiberg

Mitsuyuki Shimada

Guido Schiffer

Nina Brunner

Ben Newton

Michael Otteneder

Rainer Endermann

Peter Nell

Niels Svenstrup

Felix Bachmann

Heidi Lane

Don Gary Benjamin

Christoph Moroni

Josef Pernerstofer

Stefan Reinelt

Martin Stieger

Stephan Jordan

Mitsuyuki 905 Laurel Court Nara Minami Shimada

Disclosed are compounds of formula (I) wherein A is CH or N, B is CR or N; and D is CR; R represents hydrogen, OH or NH; R1 and R2, independently of each other, represent hydrogen, N(R3), halogen, cyano, nitro, R4-C1-C4alkyl, R4-C1-C4halogenoalkyl, OH, R4-C1-C4alkoxy, R4-C1-C4halogenoalkoxy, SH, R4-C1-C4alkythio, R4-C1-C4halogenoalkylthio; R3 represents, independently at each occurrence, hydrogen, R4-C1-C4alkyl or R4-C1-C4halogenoalkyl; R3a represents, independently at each occurrence, hydrogen or C1-C4 alkyl; R4 represents, independently at each occurrence, hydrogen, halogen, cyano, OH, SH, NH, NH(CH) or N(CH); X represents a group of formula -E- or -E-F&#x2014;, wherein E and F are different from each other and represent a group selected from &#x2014;C(R3a)2-, &#x2014;(C&#x2550;O)&#x2014;, &#x2014;NR3a- and &#x2014;O&#x2014; and F is linked to Y, with the proviso that if X represents -E-F&#x2014; one of E or F represents &#x2014;C(R3a)- or &#x2014;(C&#x2550;O)&#x2014;; Y represents a group selected from C1-C6alkyl, mono- or bicyclic C3-C11cycloalkyl, which may be partially unsaturated, mono- or bicyclic 3 to 11-membered heterocycloalkyl, which may be partially unsaturated, a mono- or bicyclic group comprising at least one aryl or heteroaryl cycle, wherein said heterocycloalkyl group and said group comprising at least one heteroaryl cycle comprise one or more heteroatoms selected from nitrogen, oxygen and sulfur and said group Y is either unsubstituted or substituted by one or more substituents and comprises including its substituents one or more than one nitrogen atom having a lone electron pair; and Z represents a mono- or bicyclic group comprising at least one aryl or heteroaryl cycle, said heteroaryl cycle comprising one or more heteroatoms selected from nitrogen, oxygen and sulfur, which aryl or heteroaryl group is unsubstituted or substituted by one or more substituents; including tautomers of said compounds, mixtures of two tautomeric forms of said compounds, and pharmaceutically acceptable salts of said compounds, tautomers thereof or mixtures of two tautomeric forms thereof, preferably with the proviso that Y comprises one or more primary amino group &#x2014;NH, when X represents &#x2014;(C&#x2550;O)&#x2014; or &#x2014;(C&#x2550;O)&#x2014;NR3a-, wherein R3a represents hydrogen or C1-C4alkyl; which are useful for the treatment of proliferation disorders or diseases, such as cancer. 

Substituted mono- and polyazanaphthalene derivatives and their use

The invention relates to novel Rauwolfia alkaloid derivatives of formula (I) combinations of Rauwolfia alkaloid derivatives and a mitochondrial inhibitor, e.g. metformin, and the use of Rauwolfia alkaloid derivatives in combination with mitochondrial inhibitor for the treatment of cancer and for achieving clinical immunosuppression. The invention also relates to a fluorescence-based method for predicting the sensitivity of a cancer cell towards a compound of formula (I). 

Combination therapy for the treatment of cancer and immunosuppression

The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.

Substituted oxazolidinones and their use in the field of blood coagulation

A compound of formula II in which Z is C or N and the Z ring is optionally further substituted; Ris H, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; and Ris a group selected from (b), (c), and (d): 

Furazanobenzimidazoles as prodrugs to treat neoplastic or autoimmune diseases

The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases. 

Substituted oxazolidinones for combinational therapy

The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing the compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.

Substituted 2-oxo-3-phenyl-5-carbonylaminomethyl-1,3-oxazolines and their use as anticoagulant and antithrombotics

The invention relates to compounds of general formula (I), to a method for the production thereof, to pharmaceutical compositions containing them, and to their use in the treatment and/or prophlaxis of diseases in humans or animals, particularly bacterial infections diseases. The compounds are derivatives of the natural substances andrimide and moiramide B.

Derivatives of andrimide and moiramide B having antibacterial properties

The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.

Substituted isoindoles and their use

The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in people or animals, especially diseases of bacterial infection.

Cinnamic acid amides

The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis of diseases in people or animals, especially diseases of bacterial infection.

Arylamides

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Wuppertal, Germany

Jens Pohlmann