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公开(公告)号:US20240350655A1
公开(公告)日:2024-10-24
申请号:US18556602
申请日:2022-04-22
发明人: Christian Ewald STIEGER , Christian Peter Richard HACKENBERGER , Marc-André KASPER , Philipp OCHTROP
IPC分类号: A61K47/68 , A61K47/54 , C07F9/32 , C07F9/6518 , C07F9/6524 , C07F9/653 , C07F9/6558 , C07F9/6561
CPC分类号: A61K47/6851 , A61K47/548 , A61K47/68031 , C07F9/3217 , C07F9/6518 , C07F9/6524 , C07F9/65324 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要: Disclosed are novel conjugates and methods for the preparation thereof. One of the methods for the preparation of a conjugate comprises a step of: acting a compound of formula (I), with a thiol-containing molecule of formula (II), wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, a small molecule, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).
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公开(公告)号:US11958880B2
公开(公告)日:2024-04-16
申请号:US17853591
申请日:2022-06-29
CPC分类号: C07K1/1075 , C12P21/005 , C12P21/02 , C12Y603/02025
摘要: The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
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公开(公告)号:US11926614B2
公开(公告)日:2024-03-12
申请号:US17253668
申请日:2019-06-19
发明人: Stefan Krauss , Marc Nazare , Lari Lehtio , Jo Waaler , Anita Wegert , Ruben Gerardus George Leenders
IPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07B2200/07
摘要: The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or a C3-6 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
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公开(公告)号:US20220106356A1
公开(公告)日:2022-04-07
申请号:US17460791
申请日:2021-08-30
发明人: Christian Hackenberger , Marc André Kasper , Maria Glanz , Tom Sauer , Dominik Schumacher , Jonas Helma-Smets , Heinrich Leonhardt , Andreas Stengl
摘要: Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III) with an azide of formula (IV) to prepare a compound of formula (V) (II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI) resulting in a compound of formula (VII)
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公开(公告)号:US20210040145A1
公开(公告)日:2021-02-11
申请号:US16993877
申请日:2020-08-14
摘要: The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
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公开(公告)号:US10596168B2
公开(公告)日:2020-03-24
申请号:US16096868
申请日:2017-04-26
发明人: Gerd Krause , Inna Hoyer , Edgar Specker , Jens Furkert , Patrick Marcinkowski , Jens-Peter Von Kries , Martin Neuenschwander , Marc Nazare
IPC分类号: A61K31/429 , A61K31/495 , A61P5/14 , A61P35/00
摘要: Chemical compounds are useful in the treatment of a subject afflicted by a thyroid disease. The compounds exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and can be used in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
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公开(公告)号:US20200091682A1
公开(公告)日:2020-03-19
申请号:US16467719
申请日:2017-12-13
发明人: Ivano GIUNTONI , Lutz GEELHAAR
摘要: The invention relates to a laser device (100) comprising a substrate (10), on the surface of which an optical waveguide (11) is arranged, which has an optical resonator (12, 13) with such a resonator length that at least one resonator mode forms a stationary wave in the resonator (12, 13), and an amplification medium that is arranged on a surface of the optical waveguide (11), wherein the amplification medium comprises a photonic crystal (20) having a plurality of column- and/or wall-shaped semiconductor elements (21) which are arranged periodically on the surface of the optical waveguide (11) while protruding from the optical waveguide (11), and wherein the photonic crystal (20) is designed to optically interact with the at least one resonator mode of the optical resonator (12, 13) and to amplify light having a wavelength of the at least one resonator mode of the optical resonator (12, 13). The invention also relates to methods for the operation and production of the laser device.
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公开(公告)号:US10476517B2
公开(公告)日:2019-11-12
申请号:US16092883
申请日:2017-04-12
发明人: Florian Hühn
摘要: The present disclosure relates to a modulator for a digital amplifier and a device comprising such a modulator and a digital amplifier.The modulator includes a pulse shaper and a control unit for controlling the pulse shaper to convert an input signal into a bit stream configured for a digital amplifier which encodes an amplitude value per clock of a carrier signal. The pulse shaper can represent a respective amplitude value of the input signal with different bit patterns. The control unit includes an assignment of the control commands to associated amplitude values resulting from amplification of the associated bit patterns with the digital amplifier is stored or at least is provided in that the control unit selects a control command per clock by means of the assignment and the amplitude value of the input signal and drives the pulse shaper accordingly.
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公开(公告)号:US10416081B2
公开(公告)日:2019-09-17
申请号:US15725448
申请日:2017-10-05
发明人: Bernd Sumpf , Martin Maiwald
摘要: Optical systems and methods for spectroscopy are described. The optical system may be particularly suitable for Raman spectroscopy and includes a multispectral excitation source, designed to emit monochromatic excitation radiation successively at at least two different excitation wavelengths along a common beam axis; an elongated flow volume with a longitudinal axis, designed to direct a particle flow along the longitudinal axis; an excitation beam path, designed to irradiate the monochromatic excitation radiation into the flow volume at a first position and the second position that are located in the flow volume and the first position is spaced apart from the second position; and a detection device, designed to wavelength-selectively filter and detect a portion of a radiation scattered from the first position at a first filter wavelength and to wavelength-selectively filter and detect a portion of a radiation scattered from the second position at a second filter wavelength.
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公开(公告)号:US20190134024A1
公开(公告)日:2019-05-09
申请号:US16096868
申请日:2017-04-26
发明人: Gerd KRAUSE , Inna HOYER , Edgar SPECKER , Jens FURKERT , Patrick MARCINKOWSKI , Jens-Peter VON KRIES , Martin NEUENSCHWANDER , Marc NAZARE
IPC分类号: A61K31/495 , A61K31/429 , A61P35/00 , A61P5/14
CPC分类号: A61K31/495 , A61K31/429 , A61P5/14 , A61P35/00
摘要: Chemical compounds are useful in the treatment of a subject afflicted by a thyroid disease. The compounds exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and can be used in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
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