PATENTSCOPE: EN_ALL:nmr AND PA:bayer

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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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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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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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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SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES (Fri, 25 Jan 2019)
The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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NOVEL SUBSTITUTED ISOTHIAZOLOPYRIDONES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES AND/OR PLANT GROWTH REGULATORS (Fri, 11 Jan 2019)
The invention relates to the technical field of the herbicides and/or plant growth regulators. Specifically, the invention primarily relates to novel substituted isothiazolopyridones, and compositions comprising said novel substituted isothiazolopyridones. Further, the present invention relates to processes for the preparation said novel substituted isothiazolopyridones and their use as herbicides and/or plant growth regulators.
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NOVEL ISOTHIAZOLO-BASED BICYCLES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES AND/OR PLANT GROWTH REGULATORS (Fri, 11 Jan 2019)
The invention relates to the technical field of herbicides and/or plant growth regulators. Specifically, the invention relates to novel isothiazolo-based bicycles, and compositions comprising said novel isothiazolo-based bicycles. Further, the present invention relates to processes for the preparation said novel isothiazolo-based bicycles and their use as herbicides and/or plant growth regulators.
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NEW AZAQUINOLINE DERIVATIVES (Fri, 04 Jan 2019)
The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, 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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NOVEL STEROIDAL 17-BETA HETEROARYL COMPOUNDS AS INHIBITORS OF AKR1C3 (Fri, 04 Jan 2019)
The invention relates to novel steroidal 17-beta heteroaryl compounds as AKR1C3 inhibitors, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for the production of medicaments for treatment and/or prophylaxis of diseases, especially of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as well as prostate cancer including castration-resistant prostate cancer as a sole agent or in combination with other active ingredients.
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METHOD FOR PREPARING SUBSTITUTED 4-AMINOINDANE DERIVATIVES (Fri, 04 Jan 2019)
The present invention relates to a method for preparing substituted 4-aminoindane derivatives of the general formula (I) by rearrangement of compounds of the formula (II) in HF, wherein R1, R2, R3, R4, and R5 have the definitions as specified in the description.
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THIAZOLE COMPOUNDS USEFUL AS PRMT5 INHIBITORS (Fri, 04 Jan 2019)
The present invention provides PRMT5 inhibiting compounds of general formula (I). A compound of general formula (I), in which R1, R2, R3, R4, R5, R6, R7, L1 and L2 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 disorders, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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PROCESS FOR THE PREPARATION OF 2,3,4-TRISUBSTITUTED QUINOLINES (Fri, 28 Dec 2018)
The invention relates to a process for preparing 2,3,4-trisubstituted quinolines from ketimines and haloalkylamino reagents.
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SUBSTITUTED BRIDGED DIAZEPANE DERIVATIVES AND USE THEREOF AS TASK-1 AND TASK-3 INHIBITORS (Fri, 21 Dec 2018)
The present application relates to novel imidazopyridinyl- or imidazopyrimidinyl-substituted, bridged 1,4-diazepane derivatives of formula (I), to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of respiratory disorders including, sleep-related respiratory disorders such as obstructive sleep apnoeas and central sleep apnoeas and snoring. Formula (I) in which the ring Q represents a bridged 1,4-diazepane cycle
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SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES AS MAP4K1 MODULATORS FOR THE TREATMENT OF CANCER DISEASES (Fri, 21 Dec 2018)
The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2a, R2b, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES (Fri, 21 Dec 2018)
The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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SUBSTITUTED BRIDGED DIAZEPANE DERIVATIVES AND USE THEREOF (Fri, 21 Dec 2018)
The present application relates to novel imidazopyridinyl-or imidazopyrimidinyl-substituted, bridged 1,4-diazepane derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of respiratory disorders including, sleep-related respiratory disorders such as obstructive sleep apnoeas and central sleep apnoeas and snoring.
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SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES (Fri, 21 Dec 2018)
The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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SAFENERS AND FORMULATIONS CONTAINING SAFENERS, BIOCIDES AND INOCULANTS (Fri, 21 Dec 2018)
Safeners are provided which reduce the toxicity of biocide-containing pesticide formulations on microbial inoculants. The safeners of the invention comprise a sulfite, such as sodium bisulfite and/or a hydrazine. The safeners of the invention optionally further comprise an amine, such as N,N-dimethylamine. Pesticidal formulations comprising a pesticide, a biocide and a safener of the invention are also provided. Methods of using the safeners and pesticidal formulations of the invention to treat plants are further provided.
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AROMATIC SULFONAMIDE DERIVATIVES AS ANTAGONISTS OR NEGATIVE ALLOSTERIC MODULATORS OF P2X4 RECEPTOR (Fri, 23 Nov 2018)
Substituted aromatic sulfonamides of formula (I), pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, especially for the treatment of pain.
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