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1.发明申请NOVEL PROCESS FOR THE PREPARATION OF ACYLGUANIDINES AND ACYLTHIOUREAS 审中-公开制备ACYLGUANIDINES和ACYLTHIOUREAS的新方法公开(公告)号：US20130109856A1
公开(公告)日：2013-05-02
申请号：US13662792
申请日：2012-10-29
发明人： Joerg KLEY , Daniel HAERLE , Guenter LINZ , Sandra STEHLE
IPC分类号： C07D241/28 , C07D261/08 , C07C231/02 , C07D241/44 , C07D403/12
CPC分类号： C07C231/14 , C07C231/00 , C07C231/10 , C07C233/11 , C07C235/28 , C07D233/48 , C07D241/06 , C07D241/28 , C07D241/40 , C07D241/44 , C07D261/08 , C07D403/12
摘要： The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译： 本发明涉及一种制备通式（I）化合物及其盐的新方法，特别是其与无机或有机酸和碱的生理上可接受的盐，其具有有价值的药理学性质，特别是对上皮的抑制作用 钠通道，其用于治疗疾病，特别是肺和气道疾病的用途。
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2.发明申请公开(公告)号：US20180002312A1
公开(公告)日：2018-01-04
申请号：US15542905
申请日：2016-01-07
发明人： Joerg KLEY , Dieter HAMPRECHT , Armin HECKEL
IPC分类号： C07D401/14 , C07D405/14 , C07D403/12 , A61K45/06 , A61K31/675 , A61K31/541 , A61K31/5377 , C07F9/6558 , A61K31/497
CPC分类号： C07D401/14 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/675 , A61K45/06 , C07D403/12 , C07D405/14 , C07F9/4006 , C07F9/5304 , C07F9/65068 , C07F9/65583
摘要： The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R1, R2, R3, R4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
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公开(公告)号：US20230000878A1
公开(公告)日：2023-01-05
申请号：US17741009
申请日：2022-05-10
发明人： Annekatrin Charlotte HEIMANN , Sandra Ruth HANDSCHUH , Christoph HOENKE , Cédrickx GODBOUT , Christian GNAMM , Patrick GROSS , Joerg KLEY , Christian Andreas KUTTRUFF , Dirk REINERT , Raphael STUBER
IPC分类号： A61K31/5386 , A61K39/395 , A61K45/06 , A61K31/496 , A61K31/4412 , C07D491/048 , A61K31/5377 , A61K31/519 , C07D519/00 , A61P37/06
摘要： The invention relates to new proline derivatives of formula (I) as cGAS inhibitors, wherein
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are defined as in claim 1, and prodrugs or pharmaceutically acceptable salts of these compounds
for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).-
公开(公告)号：US20180186774A1
公开(公告)日：2018-07-05
申请号：US15907432
申请日：2018-02-28
发明人： Armin HECKEL , Dieter HAMPRECHT , Joerg KLEY
IPC分类号： C07D403/12 , A61K45/06 , C07D401/14 , A61K31/497 , A61K31/5377
CPC分类号： C07D403/12 , A61K31/497 , A61K31/5377 , A61K45/06 , C07D401/14
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and Z− have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
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公开(公告)号：US20180002314A1
公开(公告)日：2018-01-04
申请号：US15542896
申请日：2016-01-07
发明人： Armin HECKEL , Sara FRATTINI , Joerg KLEY
IPC分类号： C07D403/12 , C07D405/14 , C07D401/14 , A61K45/06 , A61K31/497 , A61K31/675 , A61K31/551 , A61K31/5377 , C07F9/6509 , C07C53/18
CPC分类号： C07D403/12 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K31/675 , A61K45/06 , C07C53/18 , C07D401/14 , C07D403/14 , C07D405/14 , C07F9/650994
摘要： The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z− have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.
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公开(公告)号：US20170313732A1
公开(公告)日：2017-11-02
申请号：US15654301
申请日：2017-07-19
发明人： Armin HECKEL , Dieter HAMPRECHT , Joerg KLEY , Dieter WIEDENMAYER
IPC分类号： C07F9/6558 , C07D403/12 , C07D401/14 , C07C53/06 , A61K31/497 , A61K45/06 , A61K31/675 , A61K31/541 , C07D405/14 , C07C53/18
CPC分类号： C07F9/65583 , A61K31/497 , A61K31/541 , A61K31/675 , A61K45/06 , C07C53/06 , C07C53/18 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, and Z have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
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公开(公告)号：US20170050992A1
公开(公告)日：2017-02-23
申请号：US15241150
申请日：2016-08-19
发明人： Armin HECKEL , Dieter HAMPRECHT , Joerg KLEY , Dieter WIEDENMAYER
IPC分类号： C07F9/6558 , A61K31/541 , A61K45/06 , C07D401/14 , A61K31/675 , C07D403/12 , A61K31/497 , C07D405/14 , C07C53/18
CPC分类号： C07F9/65583 , A61K31/497 , A61K31/541 , A61K31/675 , A61K45/06 , C07C53/06 , C07C53/18 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, and Z− have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
摘要翻译： 其中R1，R2，R3和Z-具有如说明书或其药学上可接受的盐中所示的含义之一，以使用式（I）化合物作为药物，包含至少一种化合物 式（I）化合物，以及含有一种或多种式（I）化合物的药物组合。
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公开(公告)号：US20230002401A1
公开(公告)日：2023-01-05
申请号：US17741050
申请日：2022-05-10
发明人： Annekatrin Charlotte HEIMANN , Sandra Ruth HANDSCHUH , Christoph HOENKE , Christian GNAMM , Cédrickx GODBOUT , Patrick GROSS , Joerg KLEY , Christian Andreas KUTTRUFF , Dirk REINERT , Raphael STUBER
IPC分类号： C07D491/048
摘要： The invention relates to new proline derivatives of formula (I) as cGAS inhibitors, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and G are defined as in claim 1, and prodrugs or pharmaceutically acceptable salts of these compounds for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).
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公开(公告)号：US20180009789A1
公开(公告)日：2018-01-11
申请号：US15542908
申请日：2016-01-07
发明人： Joerg KLEY , Joerg P. HEHN , Armin HECKEL
IPC分类号： C07D403/12 , C07D403/14 , C07D401/14 , A61K45/06 , A61K31/5377 , C07D405/14 , A61K31/497
CPC分类号： C07D403/12 , A61K31/497 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R1, R2, R3, R4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
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公开(公告)号：US20170050952A1
公开(公告)日：2017-02-23
申请号：US15241146
申请日：2016-08-19
发明人： Armin HECKEL , Dieter HAMPRECHT , Joerg KLEY
IPC分类号： C07D403/12 , A61K45/06 , C07D401/14 , A61K31/497 , A61K31/5377
CPC分类号： C07D403/12 , A61K31/497 , A61K31/5377 , A61K45/06 , C07D401/14
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and Z− have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
摘要翻译： 其中R1，R2和Z-具有如说明书或其药学上可接受的盐中具有的含义之一，以使用式（I）化合物作为药物，包含至少一种式（I）化合物 I）以及含有一种或多种式（I）化合物的药物组合。
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