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公开(公告)号:US20200157073A1
公开(公告)日:2020-05-21
申请号:US16604157
申请日:2018-04-04
发明人: Hartmut BECK , Raimund KAST , Mark MEININGHAUS , Chantal FUERSTNER , Timo STELLFELD , Clemens-Jeremias VON BUEHLER , Lisa DIETZ , Michaela BAIRLEIN , Johanna ANLAHR , Hannah JOERISSEN , Peter HAUFF , Joerg MUELLER , Karoline DROEBNER , Jens NAGEL
IPC分类号: C07D401/04 , A61P11/00 , A61P1/16 , A61P13/12 , C07D215/50 , C07D413/04 , C07D417/04
摘要: The present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.
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公开(公告)号:US20220016258A1
公开(公告)日:2022-01-20
申请号:US17464565
申请日:2021-09-01
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Beatrix STELTE-LUDWIG , Dennis KIRCHHOFF , Lisa DIETZ , Christoph MAHLERT , Simone GREVEN , Stephan MÄRSCH , Sandra BERNDT , Anette SOMMER , Stefanie HAMMER
摘要: The invention relates to novel binder-drug conjugates (ADCs) having improved properties, to active metabolites of these ADCs and to processes for their preparation. The present invention furthermore relates to the use of these conjugates for the treatment and/or prevention of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases.
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公开(公告)号:US20240148715A1
公开(公告)日:2024-05-09
申请号:US18506944
申请日:2023-11-10
发明人: Eva Maria BECKER-PELSTER , Hanna TINEL , Michael HAHN , Dieter LANG , Gerrit WEIMANN , Johannes NAGELSCHMITZ , Lisa DIETZ , Soundos SALEH , David JUNG , Ildiko TEREBESI , Tobias MUNDRY , Annett RICHTER , Britta OLENIK , Birgit KEIL , Bernd RÖSLER , Peter FEY , Heiko SCHIRMER , Guido BECKER , Clemens BOTHE , Helene FABER , Julian EGGER , Mark PARRY , David WARD , Cecile VITRE
CPC分类号: A61K31/47 , A61K9/0075 , A61P9/12
摘要: The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the whole course of the disease, wherein the inhalative dosage form preferably comprises the combination of the active ingredient and a pharmaceutically suitable excipient or carrier, while preferably the active ingredient and a pharmaceutically suitable excipient are filled in a hard capsule.
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公开(公告)号:US20190328897A1
公开(公告)日:2019-10-31
申请号:US16472749
申请日:2017-12-14
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Beatrix STELTE-LUDWIG , Dennis KIRCHHOFF , Lisa DIETZ , Christoph MAHLERT , Simone GREVEN , Stephan MÄRSCH , Sandra BERNDT , Anette SOMMER , Stefanie HAMMER
摘要: The invention relates to novel binder-drug conjugates (ADCs) having improved properties, to active metabolites of these ADCs and to processes for their preparation. The present invention furthermore relates to the use of these conjugates for the treatment and/or prevention of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases.
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公开(公告)号:US20230338559A1
公开(公告)日:2023-10-26
申请号:US18182093
申请日:2023-03-10
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Beatrix STELTE-LUDWIG , Dennis KIRCHHOFF , Lisa DIETZ , Christoph MAHLERT , Simone GREVEN , Stephan MÄRSCH , Sandra BERNDT , Anette SOMMER , Stefanie HAMMER
CPC分类号: A61K47/6803 , A61K47/65 , A61K47/6849 , A61K47/6855 , A61P35/00 , C07K16/2827 , C07K16/2863 , C07K16/2866 , C07K16/2878 , C07K16/32 , A61K2039/505
摘要: The invention relates to novel binder-drug conjugates (ADCs) having improved properties, to active metabolites of these ADCs and to processes for their preparation. The present invention furthermore relates to the use of these conjugates for the treatment and/or prevention of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases.
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公开(公告)号:US20190351066A1
公开(公告)日:2019-11-21
申请号:US16472634
申请日:2017-12-18
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Leo MARX , Sarah Anna Liesa JOHANNES , Beatrix STELTE-LUDWIG , Lisa DIETZ , Hannah JOERISSEN , Christoph MAHLERT , Simone GREVEN , Anette SOMMER
IPC分类号: A61K47/68 , C07D207/335 , A61K31/402 , A61K47/65 , A61P35/00
摘要: The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are released by legumain cleavage, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers. Reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as structural motif, as a result of slowed legumain cleavage, achieves an increase in stability in the lysosomes of healthy organs while simultaneously maintaining the high anti-tumour effect.
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公开(公告)号:US20190077752A1
公开(公告)日:2019-03-14
申请号:US16087928
申请日:2017-03-21
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Leo MARX , Sarah Anna Liesa JOHANNES , Beatrix STELTE-LUDWIG , Lisa DIETZ , Carsten TERJUNG , Christoph MAHLERT , Simone GREVEN , Anette SOMMER , Sandra BERNDT
IPC分类号: C07D207/335 , C07D401/12 , C07D401/14 , A61K47/68 , A61K47/65
摘要: The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers.
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公开(公告)号:US20170240566A1
公开(公告)日:2017-08-24
申请号:US15503578
申请日:2015-08-25
发明人: Alexandros VAKALOPOULOS , Gaelle VALOT , Markus FOLLMANN , Damian BROCKSCHNIEDER , Johannes-Peter STASCH , Tobias MARQUARDT , Adrian TERSTEEGEN , Frank WUNDER , Lisa DIETZ , Dieter LANG , Ursula KRENZ
IPC分类号: C07D519/00 , A61K31/519 , C07D487/04 , A61K45/06
CPC分类号: C07D519/00 , A61K31/519 , A61K45/06 , C07D487/04
摘要: The present application relates to novel amino-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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公开(公告)号:US20240043379A1
公开(公告)日:2024-02-08
申请号:US18175265
申请日:2023-02-27
发明人: Hans-Georg LERCHEN , Anne-Sophie REBSTOCK , Leo MARX , Sarah Anna Liesa JOHANNES , Beatrix STELTE-LUDWIG , Lisa DIETZ , Carsten TERJUNG , Christoph MAHLERT , Simone GREVEN , Anette SOMMER , Sandra BERNDT
IPC分类号: C07D207/335 , A61K47/65 , A61K47/68 , C07D401/12 , C07D401/14
CPC分类号: C07D207/335 , A61K47/65 , A61K47/6889 , C07D401/14 , A61K47/6845 , A61K47/6849 , C07D401/12 , A61K47/6803
摘要: The invention relates to novel prodrugs or conjugates of the general formula (Ia)
in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers.-
公开(公告)号:US20180022751A1
公开(公告)日:2018-01-25
申请号:US15548310
申请日:2016-02-02
发明人: Alexandros VAKALOPOULOS , Damian BROCKSCHNIEDER , Frank WUNDER , Johannes-Peter STASCH , Tobias MARQUARDT , Lisa DIETZ , Min Jian Volkhart LI
IPC分类号: C07D487/04 , A61K45/06 , A61K31/695 , A61K31/4985 , C07B59/00 , C07F7/08
CPC分类号: C07D487/04 , A61K31/4985 , A61K31/695 , A61K45/06 , C07B59/002 , C07B2200/05 , C07F7/0812
摘要: The present application relates to novel substituted imidazo[1,2-a]pyrazine carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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