JP7773377B2 - アスタシンプロテイナーゼのヘテロ芳香族インヒビター - Google Patents

アスタシンプロテイナーゼのヘテロ芳香族インヒビター

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JP7773377B2
JP7773377B2 JP2021574193A JP2021574193A JP7773377B2 JP 7773377 B2 JP7773377 B2 JP 7773377B2 JP 2021574193 A JP2021574193 A JP 2021574193A JP 2021574193 A JP2021574193 A JP 2021574193A JP 7773377 B2 JP7773377 B2 JP 7773377B2
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JPWO2020249760A5 (https=
JP2022536183A5 (https=
JP2022536183A (ja
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ラムズベック ダニエル
タン キャスリン
シュレンジグ ダグマール
バックホルツ ミルコ
サイニス ホルガー
シリング ステファン
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ビボリョン セラピューティクス エヌブイ
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07D207/325Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008518923A (ja) 2004-11-01 2008-06-05 ヌアダ,リミテッド・ライアビリティ・カンパニー 化合物およびその使用方法
JP2008538778A (ja) 2005-04-25 2008-11-06 ノバルティス アクチエンゲゼルシャフト ペプチド脱ホルミル酵素(pdf)阻害剤として有用なイミダゾ[1,2−a]ピリジン誘導体
WO2017182433A1 (en) 2016-04-18 2017-10-26 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of meprin alpha and beta

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1036004B (it) * 1968-05-21 1979-10-30 Abc Ist Biolog Chem Spa Acidt 3 indolil adetoidrossamici
US4146721A (en) * 1969-09-12 1979-03-27 Byk Gulden Lomberg Chemische Fabrik Gmbh Pyrazol-4-acetic acid compounds
US4021448A (en) * 1975-10-21 1977-05-03 Sterling Drug Inc. 2-Substituted-indole-1-lower-alkanecarboxamides
KR100432928B1 (ko) * 2001-04-26 2004-05-28 주식회사 코오롱 신규한 하이드록스아믹산 유도체, 신규한 그의 중간체화합물 및 그들의 제조방법
AU2008252628A1 (en) 2007-05-18 2008-11-27 Inhibox Ltd. Bicyclosulfonyl acid (BCSA) compounds and their use as therapeutic agents

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008518923A (ja) 2004-11-01 2008-06-05 ヌアダ,リミテッド・ライアビリティ・カンパニー 化合物およびその使用方法
JP2008538778A (ja) 2005-04-25 2008-11-06 ノバルティス アクチエンゲゼルシャフト ペプチド脱ホルミル酵素(pdf)阻害剤として有用なイミダゾ[1,2−a]ピリジン誘導体
WO2017182433A1 (en) 2016-04-18 2017-10-26 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Novel inhibitors of meprin alpha and beta

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
Adiguzel, Ekrem; et al,Synthesis and characterization of two new hydroxamic acids derivatives and their metal complexes. An investigation on the keto/enol, E/Z and hydroxamate/hydroximate forms,Journal of Molecular Structure,2017年,1127,403-412
Boularot, Adrien; et al,Discovery and Refinement of a New Structural Class of Potent Peptide Deformylase Inhibitors,Journal of Medicinal Chemistry,2007年,50(1),10-20
Claudia, Broder; et al,The metalloproteases meprin α and meprin β: unique enzymes in inflammation, neurodegeneration, cancer and fibrosis,Biochemimal Journal ,2013年,450 (2),253-264
REGISTRY(STN)[online],2018年03月28日,[検索日 2024.05.07] CAS登録番号 2200851-01-8化合物名2-(2-Phenylindol-1-yl)ethanehydroxamic acid,Supplier: Aurora Fine Chemicals、他9化合物(以下掲載日2019年2月26日以前 2273732-43-5、2202158-90-3、2202117-28-8、2201507-56-2、2201200-27-1、2200774-84-9、2199624-48-9、2199624-46-7、2197349-81-6)
REGISTRY(STN)[online],2018年03月29日,[検索日 2024.05.07] CAS登録番号 2201199-73-5化合物名1-(6-Chloro-2-pyrazinyl)-N-hydroxy-3,5-dimethyl-1H-pyrazole-4-acetamide,Supplier: Aurora Fine Chemicals、他13化合物(以下掲載日2018年3月29日以前 2200650-99-1、2199033-69-5、2199032-24-9、2198494-27-6、2140041-65-0、1933544-85-4、1881136-11-3、1875233-24-1、1872076-39-5、1863670-90-9、1863524-28-0、1862304-68-4、1850144-05-6)
Wolz, Russell L.; et al,Mapping the active site of meprin-A with peptide substrates and inhibitors,Biochemistry,1991年,30(34),8488-93

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