-
公开(公告)号：US20210267947A1
公开(公告)日：2021-09-02
申请号：US17251576
申请日：2019-06-28
IPC分类号： A61K31/4192 , C07D403/04
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, R4, n and m are as defined herein, which have valuable pharmacological properties, in particular bind to the GPR142 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as type 2 diabetes.
-
公开(公告)号：US20160235706A1
公开(公告)日：2016-08-18
申请号：US15097857
申请日：2016-04-13
发明人： Matthias ECKHARDT , Sara FRATTINI , Elke LANGKOPF , Holger WAGNER
IPC分类号： A61K31/343 , C07D307/80 , A61K31/5377 , A61K31/4025 , C07D405/12 , A61K31/4178 , C07D407/12 , A61K31/41 , C07D405/14 , A61K31/443 , A61K31/4155 , C07D417/12 , A61K31/427 , A61K31/4709 , A61K31/36 , A61K31/357 , A61K31/351 , A61K31/416 , A61K31/404 , A61K31/422 , C07D413/12 , A61K31/4196 , A61K31/4245 , A61K45/06
CPC分类号： A61K31/343 , A61K31/085 , A61K31/09 , A61K31/192 , A61K31/34 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D307/80 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译： 本发明涉及通式I的化合物，其中基团（Het）Ar和R 1如权利要求1中所定义，其具有有价值的药理学性质，特别是与GPR40受体结合并调节其活性。 该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。
-
![CYCLIC ETHER DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXYAMIDE](/abs-image/US/2018/05/17/US20180134720A1/abs.jpg.150x150.jpg)
公开(公告)号：US20180134720A1
公开(公告)日：2018-05-17
申请号：US15865695
申请日：2018-01-09
发明人： Christoph HOENKE , Barbara BERTANI , Marco FERRARA , Giacomo FOSSATI , Sara FRATTINI , Riccardo GIOVANNINI , Scott HOBSON
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
-
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.
-
![CYCLIC ETHER DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXYAMIDE](/abs-image/US/2023/09/14/US20230286993A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230286993A1
公开(公告)日：2023-09-14
申请号：US18320264
申请日：2023-05-19
发明人： Christoph HOENKE , Barbara BERTANI , Marco FERRARA , Giacomo FOSSATI , Sara FRATTINI , Riccardo GIOVANNINI , Scott HOBSON
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of formula (I)
wherein R1, R2, R3, R5, R6 and A are as defined herein. The compounds of formula (1) are inhibitors of phosphodiesterase 2 and useful in treating central nervous system diseases and other diseases. The invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.-
![CYCLIC ETHER DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXYAMIDE](/abs-image/US/2020/02/06/US20200039991A1/abs.jpg.150x150.jpg)
公开(公告)号：US20200039991A1
公开(公告)日：2020-02-06
申请号：US16600965
申请日：2019-10-14
发明人： Christoph HOENKE , Barbara BERTANI , Marco FERRARA , Giacomo FOSSATI , Sara FRATTINI , Riccardo GIOVANNINI , Scott HOBSON
IPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases.In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
-
公开(公告)号：US20180305339A1
公开(公告)日：2018-10-25
申请号：US15953523
申请日：2018-04-16
发明人： Sara FRATTINI , Iain LINGARD , Dieter Wolfgang HAMPRECHT , Remko Alexander BAKKER , Matthias ECKHARDT , Andreas GOLLNER , Joerg P. HEHN , Elke LANGKOPF , Holger WAGNER , Bernd WELLENZOHN , Dieter WIEDENMAYER
IPC分类号： C07D401/14 , A61K31/444 , A61K45/06 , A61K31/506
CPC分类号： C07D401/14 , A61K31/444 , A61K31/506 , A61K45/06 , A61P3/10
摘要： Disclosed are heteroarylcarboxamides of formula (I), and pharmaceutically acceptable salts thereof, wherein A, T, R1, R2 and R3 are as defined herein. Also disclosed are methods of using these compounds for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.
-
公开(公告)号：US20180305338A1
公开(公告)日：2018-10-25
申请号：US15770762
申请日：2016-10-20
发明人： Sara FRATTINI , Remko BAKKER , Riccardo GIOVANNINI , Dieter HAMPRECHT , Iain LINGARD , Alexander PAUTSCH , Bernd WELLENZOHN
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/438 , C07D413/14 , A61K31/444 , A61K45/06
CPC分类号： C07D401/14 , A61K31/438 , A61K31/444 , A61K31/4709 , A61K45/06 , C07D403/12 , C07D413/14
摘要： The present invention relates to compounds of general formula I, wherein D1 to D3, A, R1, R2, Y and n are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema.
-
![CYCLIC ETHER DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINE-3-CARBOXYAMIDE](/abs-image/US/2021/02/04/US20210032259A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210032259A1
公开(公告)日：2021-02-04
申请号：US17075091
申请日：2020-10-20
发明人： Christoph HOENKE , Barbara BERTANI , Marco FERRARA , Giacomo FOSSATI , Sara FRATTINI , Riccardo GIOVANNINI , Scott HOBSON
IPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
-
公开(公告)号：US20180319771A1
公开(公告)日：2018-11-08
申请号：US15770763
申请日：2016-10-20
发明人： Sara FRATTINI , Remko BAKKER , Riccardo GIOVANNINI , Giacomo FOSSATI , Dieter HAMPRECHT , Iain LINGARD , Alexander PAUTSCH , Bernd WELLENZOHN
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , C07D405/14 , C07D491/052 , C07D498/04 , C07D498/10 , A61P3/10
CPC分类号： C07D401/14 , A61K45/06 , A61K2300/00 , A61P3/10 , C07D405/14 , C07D471/04 , C07D487/04 , C07D491/052 , C07D498/04 , C07D498/10
摘要： The present invention relates to compounds of general formula (I), wherein D1 to D3, -A-, n, R1, R2, Y1, L and y2 are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema.
-
-
-
-
-
-
-
-
-
搜索结果
12 条记录 (耗时 0.02 秒)
