JPWO2021160716A5 - - Google Patents

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Publication number
JPWO2021160716A5
JPWO2021160716A5 JP2022548997A JP2022548997A JPWO2021160716A5 JP WO2021160716 A5 JPWO2021160716 A5 JP WO2021160716A5 JP 2022548997 A JP2022548997 A JP 2022548997A JP 2022548997 A JP2022548997 A JP 2022548997A JP WO2021160716 A5 JPWO2021160716 A5 JP WO2021160716A5
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Japan
Prior art keywords
group
tautomer
salt
compound according
moiety
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Pending
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JP2022548997A
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Japanese (ja)
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JP2023513906A (en
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Priority claimed from PCT/EP2021/053284 external-priority patent/WO2021160716A1/en
Publication of JP2023513906A publication Critical patent/JP2023513906A/en
Publication of JPWO2021160716A5 publication Critical patent/JPWO2021160716A5/ja
Pending legal-status Critical Current

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Claims (11)

式（Ｉ）の化合物
Figure 2021160716000001
 （式中、
Ｒは、
Figure 2021160716000002
 からなるＲ－Ｇ１群から選択され、
Ｒ1は、ＨおよびＦからなるＲ1－Ｇ１群から選択され、
部分＝Ａ1－ＣＲ＝Ａ2－は、＝Ｎ－ＣＲ＝Ｎ－、＝Ｎ－ＣＲ＝ＣＨ－および＝ＣＨ－ＣＲ＝Ｎ－からなるＡ－Ｇ１群から選択され、
部分－Ｌ1＝Ｌ2－は、－Ｎ＝Ｎ－、－Ｎ＝ＣＨ－および－ＣＨ＝Ｎ－からなるＬ－Ｇ１群から選択される）
および／もしくはその互変異性体
またはその塩。 Compound of formula (I)
Figure 2021160716000001
 (In the formula,
R is
Figure 2021160716000002
 selected from the R-G1 group consisting of,
R 1 is selected from the group R 1 -G1 consisting of H and F;
the moiety =A 1 -CR=A 2 - is selected from the group AG1 consisting of =N-CR=N-, =N-CR=CH- and =CH-CR=N-;
The moiety -L 1 =L 2 - is selected from the group L-G1 consisting of -N=N-, -N=CH- and -CH=N-)
and/or its tautomer or salt thereof. Ｒが、
Figure 2021160716000003
 からなるＲ－Ｇ２群から選択される、
請求項１に記載の化合物
および／もしくはその互変異性体
またはその塩。 R is
Figure 2021160716000003
 selected from the R-G2 group consisting of,
A compound according to claim 1 and/or a tautomer thereof or a salt thereof. Ｒが、
Figure 2021160716000004
 からなるＲ－Ｇ３群から選択される、
請求項１に記載の化合物
および／もしくはその互変異性体
またはその塩。 R is
Figure 2021160716000004
 selected from the R-G3 group consisting of,
A compound according to claim 1 and/or a tautomer thereof or a salt thereof. Ｒが、
Figure 2021160716000005
 からなるＲ－Ｇ４群から選択される、
請求項１に記載の化合物
および／もしくはその互変異性体
またはその塩。 R is
Figure 2021160716000005
 selected from the R-G4 group consisting of,
A compound according to claim 1 and/or a tautomer thereof or a salt thereof. 部分＝Ａ1－ＣＲ＝Ａ2－が、＝Ｎ－ＣＲ＝Ｎ－からなるＡ－Ｇ２群から選択される、
請求項１から４までのいずれか１項に記載の化合物
および／もしくはその互変異性体
またはその塩。 the part =A 1 -CR=A 2 - is selected from the group A-G2 consisting of =N-CR=N-;
A compound according to any one of claims 1 to 4 and/or a tautomer thereof or a salt thereof. 部分＝Ａ1－ＣＲ＝Ａ2－が、＝Ｎ－ＣＲ＝ＣＨ－からなるＡ－Ｇ３群から選択される、
請求項１から４までのいずれか１項に記載の化合物
および／もしくはその互変異性体
またはその塩。 the moiety =A 1 -CR=A 2 - is selected from the group A-G3 consisting of =N-CR=CH-;
A compound according to any one of claims 1 to 4 and/or a tautomer thereof or a salt thereof. 部分＝Ａ1－ＣＲ＝Ａ2－が、＝ＣＨ－ＣＲ＝Ｎ－からなるＡ－Ｇ４群から選択される、
請求項１から４までのいずれか１項に記載の化合物
および／もしくはその互変異性体
またはその塩。 the moiety =A 1 -CR=A 2 - is selected from the group A-G4 consisting of =CH-CR=N-;
A compound according to any one of claims 1 to 4 and/or a tautomer thereof or a salt thereof. 式（Ｉ）の化合物が、
Figure 2021160716000006
Figure 2021160716000007
からなる群から選択される、
請求項１から７までのいずれか１項に記載の化合物
および／もしくはその互変異性体
またはその塩。 The compound of formula (I) is
Figure 2021160716000006
Figure 2021160716000007
selected from the group consisting of
A compound according to any one of claims 1 to 7 and/or a tautomer thereof or a salt thereof. 請求項１から８までのいずれか１項に記載の化合物および／またはその互変異性体の薬学的に許容される塩。 9. A pharmaceutically acceptable salt of a compound according to any one of claims 1 to 8 and/or a tautomer thereof. １つもしくは複数の請求項１から９までのいずれか１項に記載の化合物および／またはその互変異性体、あるいは薬学的に許容されるその塩を含み、１種もしくは複数の不活性担体および／または希釈剤を一緒に含んでもよい、医薬組成物。 comprising one or more compounds according to any one of claims 1 to 9 and/or tautomers thereof, or pharmaceutically acceptable salts thereof, and one or more inert carriers and Pharmaceutical compositions, which may also contain diluents. 眼疾患の処置、好ましくは、糖尿病性黄斑浮腫、加齢黄斑変性および／または脈絡膜血管新生の処置のための、請求項１０に記載の医薬組成物。 Pharmaceutical composition according to claim 10, for the treatment of eye diseases, preferably for the treatment of diabetic macular edema, age-related macular degeneration and/or choroidal neovascularization.
JP2022548997A 2020-02-13 2021-02-11 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors. Pending JP2023513906A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20157257 2020-02-13
EP20157257.5 2020-02-13
PCT/EP2021/053284 WO2021160716A1 (en) 2020-02-13 2021-02-11 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors

Publications (2)

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JP2023513906A JP2023513906A (en) 2023-04-04
JPWO2021160716A5 true JPWO2021160716A5 (en) 2024-01-26

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US (1) US11851418B2 (en)
EP (1) EP4103561A1 (en)
JP (1) JP2023513906A (en)
CN (1) CN115087652B (en)
AR (1) AR121340A1 (en)
TW (1) TW202144331A (en)
WO (1) WO2021160716A1 (en)

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TW202144330A (en) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors
TW202144331A (en) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors

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US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
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TW202144330A (en) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors
TW202144331A (en) 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors

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