PATENTSCOPE: EN_ALL:nmr AND PA:bayer

METHOD FOR THE SYNTHESIS OF CYCLIC DEPSIPEPTIDES (Fri, 17 May 2019)
The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
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TETRAZOLYLPROPYL DERIVATIVES AND THEIR USE AS FUNGICIDES (Fri, 17 May 2019)
The present invention relates to tetrazolylpropyl derivatives of formula (I) wherein one of V1 and V2 represents CR3 and the other one of V1 and V2 represents N, Q represents a 6- membered aromatic cycle as defined in the specification, and R1, R2, R3, R4, and R5 are defined as disclosed in the specification, to compositions comprising such compounds, to the use of said compounds as fungicides, as well as to particular intermediates useful in the synthesis of said tetrazolylpropyl derivatives.
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PRODRUGS OF SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to prodrugs of 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro- 2-hydroxypropyl] -4,5-dihydro- 1H-1,2,4-triazol-1-yl Jmethyl)-1- [3-(trifluoromethyl)-pyridin-2-yl] - 1H-1,2,4-triazole-5-carboxamide, 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2- hydroxypropyl] -4,5-dihydro- 1H-1,2,4-triazol-1-yl} methyl)-1- [2-(trifluoromethyl)-phenyl] -1H- 1,2,4-triazole-5-carboxamide and 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2- hydroxypropyl] -4,5-dihydro-1H-1,2,4-triazol-1-yl} methyl)-1-(3-chloropyridin-2-yl)-1H-1,2,4- triazole-5-carboxamide, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases. 5
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AROMATIC SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF ISCHEMIC STROKE (Fri, 03 May 2019)
A compound of formula (I) or an N-oxide, a salt, a hydrate, a solvate, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer for use in the treatment or prophylaxis of brain ischemia, ischemic brain injury, Ischemic Stroke (IS), haemorrhagic stroke, traumatic brain injury, spinal cord injury.
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SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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AMINE SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to novel amine substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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PROCESS FOR PREPARING BENZOTHIOPHEN-2YL BORONATE (Fri, 03 May 2019)
A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.
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NOVEL PYRAZOLO-PYRROLO-PYRIMIDINE-DIONE DERIVATIVES AS P2X3 INHIBITORS (Fri, 03 May 2019)
The present invention covers substituted Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
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PRODRUGS OF SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to prodrugs of 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro- 2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoromethyl)-pyridin-2-yl]- 1H-1,2,4-triazole-5-carboxamide, 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2- hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[2-(trifluoromethyl)-phenyl]-1H-5 1,2,4-triazole-5-carboxamide and 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2- hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-(3-chloropyridin-2-yl)-1H-1,2,4- triazole-5-carboxamide, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of 10 renal and cardiovascular diseases.
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SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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4H-PYRROLO[3,2-C]PYRIDIN-4-ONE DERIVATIVES (Fri, 03 May 2019)
Compounds of formula (I) processes for their production and their use as pharmaceuticals.
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SUBSTITUTED TRIAZOLE DERIVATIVES AND USES THEREOF (Fri, 03 May 2019)
Substituted triazole derivatives and uses thereof The present invention relates to novel substituted 1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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SUBSTITUTED 3-PHENYLQUINAZOLIN-4(3H)-ONES AND USES THEREOF (Fri, 05 Apr 2019)
The present invention covers substituted 3-Phenylquinazolin-4(3H)-one compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of various inflammatory and fibrotic diseases of the respiratory tract and of the lungs as well as lung cancer, as a sole agent or in combination with other active ingredients.
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SUBSTITUTED 3-PHENYLQUINAZOLIN-4(3H)-ONES AND USES THEREOF (Fri, 05 Apr 2019)
The present invention covers substituted 3-Phenylquinazolin-4(3H)-one compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of various inflammatory and fibrotic diseases of the respiratory tract and of the lungs as well as lung cancer, as a sole agent or in combination with other active ingredients.
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USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS (Fri, 01 Mar 2019)
The present invention relates the use of compound 1 for the treatment of arthritis especially rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, as well as other other immune- mediated rheumatic diseases.
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4-OXO-2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE-7-CARBOXAMIDES (Fri, 22 Feb 2019)
The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7- carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.
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DIHYDROOXADIAZINONES (Fri, 08 Feb 2019)
The present invention provides dihydrooxydiazinone compounds of general formula (I) : in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
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QUINOLINE DERIVATIVES FOR TREATING INFECTIONS WITH HELMINTHS (Fri, 08 Feb 2019)
The present invention covers quinoline compounds of general formula (I), in which A, R1, R2, R3, R4, R5, R6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
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6-PHENYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES AS PDE3A AND PDE3B INHIBITORS FOR TREATING CANCER (Fri, 08 Feb 2019)
The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)- one derivatives of formula (I) : The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)- one derivatives of formula (I) :
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