PATENTSCOPE: EN_ALL:nmr AND PA:merck

ISOTHIOCYANATO TOLANE DERIVATIVES (Fri, 22 Mar 2019)
The present invention relates to isothiocyanato tolane derivatives of formula I in which the occurring groups have the meanings indicated in claim 1, to a process for their preparation, to liquid-crystalline media comprising same and to high-frequency components comprising these media, especially microwave components for high-frequency devices, such as devices for shifting the phase of microwaves, in particular for microwave phased-array antennas.
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ORGANIC SEMICONDUCTING COMPOUNDS (Fri, 22 Mar 2019)
P17220De -253- Abstract of the Disclosure The invention relates to novel organic semiconducting compounds containing apolycyclicunit, to methods for their preparation and educts or intermediates used therein, to compositions, polymer blends and formulations containing them, to the use of the compounds, compositions and polymer blends as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices, perovskite-based solar cell (PSC) devices,organic photodetectors (OPD), organic field effect transistors (OFET) and organic light emitting diodes (OLED), and to OE, OPV, PSC, OPD,OFET and OLED devices comprising these compounds, compositions or polymer blends.
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DIBENZOFURAN AND DIBENZOTHIOPHENE DERIVATIVES (Fri, 22 Mar 2019)
The present invention relates to dibenzofuran and dibenzothiophene derivatives of the general formula (I) in which the occurring groups and parameters have the meanings indicated in claim 1, to the use thereof in liquid-crystalline or mesogenic media, to liquid-crystal- line or mesogenic media comprising these derivatives, and to electro-optical display elements containing these liquid-crystalline or mesogenic media.
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COMPOUNDS FOR REDUCING THE VISCOSITY OF BIOLOGICAL FORMULATIONS (Fri, 15 Mar 2019)
The present invention relates to pegylated amino acid compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3A, R3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.
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PNEUMOCOCCAL POLYSACCHARIDES AND THEIR USE IN IMMUNOGENIC POLYSACCHARIDE-CARRIER PROTEIN CONJUGATES (Fri, 15 Mar 2019)
The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Steptococcus pneumoniae serotypes.
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PNEUMOCOCCAL POLYSACCHARIDES AND THEIR USE IN IMMUNOGENIC POLYSACCHARIDE-CARRIER PROTEIN CONJUGATES (Fri, 15 Mar 2019)
The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Steptococcus pneumoniae serotypes.
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PNEUMOCOCCAL POLYSACCHARIDES AND THEIR USE IN IMMUNOGENIC POLYSACCHARIDE-CARRIER PROTEIN CONJUGATES (Fri, 15 Mar 2019)
The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Steptococcus pneumoniae serotypes.
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PNEUMOCOCCAL POLYSACCHARIDES AND THEIR USE IN IMMUNOGENIC POLYSACCHARIDE-CARRIER PROTEIN CONJUGATES (Fri, 15 Mar 2019)
The present invention provides capsular polysaccharides from Streptococcus pneumoniae serotypes identified using NMR. The present invention further provides polysaccharide-protein conjugates in which capsular polysaccharides from one or more of these serotypes are conjugated to a carrier protein such as CRM197. Polysaccharide-protein conjugates from one or more of these serotypes may be included in multivalent pneumococcal conjugate vaccines having polysaccharides from multiple additional Steptococcus pneumoniae serotypes.
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PROCESSES FOR THE FORMULATION OF PNEUMOCOCCAL POLYSACCHARIDES FOR CONJUGATION TO A CARRIER PROTEIN (Fri, 15 Mar 2019)
The present invention provides a number of process improvements related to the conjugation of capsular polysaccharides from Streptococcus pneumoniae to a carrier protein. These process are serotype specific and include acid hydrolysis, addition of sodium chloride to the reductive amination reaction, and addition of sucrose to dissolve polysaccharides. Polysaccharide-protein conjugates prepared using the processes of the invention can be included in multivalent pneumococcal conjugate vaccines.
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QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS (Fri, 01 Mar 2019)
The invention relates to quinoxaline derivatives of the general formula (I) and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious disease sand disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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BEZIMIDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS (Fri, 01 Mar 2019)
The invention relates to benzimidazole derivatives of the general formula (I), and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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BORONIC ACID DERIVATIVES (Fri, 01 Mar 2019)
The present invention relates to a-amino boronic acid derivatives. These compounds are useful for inhibiting the activity of immunoproteasome (LMP7) and for the treatment and/or prevention of medical contidions affected by immunoproteasome activity such as inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.
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ORGANIC SEMICONDUCTING POLYMER (Fri, 15 Feb 2019)
The invention relates to novel organic semiconducting polymers, to methods for their preparation and educts or intermediates used therein, to compositions containing them, to the use of the polymers and compositions as organic semiconductors in, or for the preparation of, organic electronic (OE) devices, especially organic photovoltaic (OPV) devices, perovskite-based solar cell (PSC) devices,organic photodetectors (OPD), organic field effect transistors (OFET) and organic light emitting diodes (OLED), and to OE, OPV, PSC, OPD, OFET and OLED devices comprising these polymers or compositions.
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SILICON CARBONACEOUS FILM FORMING COMPOSITION COMPRISING POLYCARBOSILANE AND METHOD FOR MANUFACTURING SILICON CARBONACEOUS FILM USING THE SAME (Fri, 15 Feb 2019)
[Problem]To provide a composition comprising polycarbosilane, which has excellent filling property, can form a film at a lower temperature, and makes electrical property of the produced film excellent. [Means for Solution] A silicon carbonaceous film forming composition comprising polycarbosilane and a solvent, wherein the ratio of the integrated intensity at 3.92 to 4.20 ppm to the integrated intensity at3.60 to 5.50 ppm in the H-NMR spectrum of said polycarbosilane is 27 to 50%.
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NOVEL SUBSTITUTED PYRIDINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS (Fri, 08 Feb 2019)
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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NOVEL SUBSTITUTED PHENYL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS (Fri, 08 Feb 2019)
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS (Fri, 08 Feb 2019)
The invention relates to thiazolopyridine derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
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METALLO-BETA-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF (Fri, 25 Jan 2019)
The present invention relates to metallo-β-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
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TLR7/8 ANTAGONISTS AND USES THEREOF (Fri, 25 Jan 2019)
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
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RING CLOSURE REACTION (Fri, 18 Jan 2019)
The present invention relates to a ring closure reaction useful in synthesizing fused aromatic or heteroaromatic ring systems, which may, for example, be used as organic semiconductor materials.
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ORGANIC ELECTROLUMINESCENT DEVICE (Fri, 11 Jan 2019)
The present application relates to a blue light-emitting organic electroluminescent device (OLED) having an anode, a cathode, at least one blue light-emitting layer and at least one hole-transport layer, wherein the at least one blue light-emitting layer comprises an elongated bis-indenofluorene derivative as a main component and wherein the at least one hole-transport layer comprises a polymer with non-conjugated units as a main component as well as to a method for producing the organic electroluminescent device.
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MATERIALS FOR ELECTRONIC DEVICES (Fri, 04 Jan 2019)
The present application relates to a spirobifluorene derivative of a specific formula (I) which is suitable for use in electronic devices.
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2,3-DIHYDROBENZOTHIOPHENE DERIVATIVES (Fri, 04 Jan 2019)
The present invention relates to 2,3-dihydrobenzothiophenederivatives of the general formula I ( l ) In which the occurring groups and parameters have the meanings indicated in claim 1, to the use thereof in liquid-crystalline or mesogenic media, to liquid-crystal- line or mesogenic media comprising these derivatives, and to electro-opti- cal display elements containing these liquid-crystalline or mesogenic media.
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3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
Disclosed are pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor, uses of the compounds described herein in the potential treatment of prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved, compositions comprising these compounds, uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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5-(PYRIDIN-3-YL)OXAZOLE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
Provided are 5-(pyridin-3-yl) oxazole compounds, the compositions comprising these compounds and the uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
Provided are pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. Provided is also use of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. Provided are also compositions comprising these compounds. Provided is also use of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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5-(PYRIDIN-3-YL)OXAZOLE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (Fri, 04 Jan 2019)
The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES (Fri, 28 Dec 2018)
The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.
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