JP6427506B2 - 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 - Google Patents

置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 Download PDF

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JP6427506B2
JP6427506B2 JP2015560617A JP2015560617A JP6427506B2 JP 6427506 B2 JP6427506 B2 JP 6427506B2 JP 2015560617 A JP2015560617 A JP 2015560617A JP 2015560617 A JP2015560617 A JP 2015560617A JP 6427506 B2 JP6427506 B2 JP 6427506B2
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クリスチャン グナム
クリスチャン グナム
トルステン ウースト
トルステン ウースト
シュテファン ペーテルス
シュテファン ペーテルス
クラウス ルドルフ
クラウス ルドルフ
ホルガー ヘッシュ
ホルガー ヘッシュ
ウーヴェ ヨルク リース
ウーヴェ ヨルク リース
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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JP2015560617A 2013-03-04 2014-02-26 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 Active JP6427506B2 (ja)

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PCT/EP2014/053718 WO2014135414A1 (en) 2013-03-04 2014-02-26 Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity

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JP2017522350A (ja) * 2014-07-31 2017-08-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用

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Publication number Priority date Publication date Assignee Title
US20140221335A1 (en) 2013-02-06 2014-08-07 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9458113B2 (en) * 2014-07-31 2016-10-04 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9475779B2 (en) * 2014-07-31 2016-10-25 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9657015B2 (en) * 2014-07-31 2017-05-23 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
EP3599234B1 (en) * 2015-09-18 2021-04-07 Boehringer Ingelheim International GmbH Stereoselective process
US9856232B1 (en) 2017-06-20 2018-01-02 King Saud University Dihydropyrimidinone derivatives
US10047071B1 (en) 2018-01-15 2018-08-14 King Saud University Dihydropyrimidinone derivatives
US10111873B1 (en) 2018-01-17 2018-10-30 King Saud University Dihydropyrimidinone derivatives
CN114650819A (zh) 2019-09-17 2022-06-21 美莱奥生物制药第四有限公司 用于治疗移植物排斥、闭塞性细支气管炎综合征和移植物抗宿主病的阿维来司他
US20230218596A1 (en) 2020-04-16 2023-07-13 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating coronavirus infection
KR20240090272A (ko) 2021-10-20 2024-06-21 메레오 바이오파마 4 리미티드 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
JP2000273087A (ja) 1999-03-24 2000-10-03 Mitsui Chemicals Inc 非対称２−イミダゾリジノン類の製造方法
CA2470813A1 (en) 2001-12-20 2003-07-03 Bayer Healthcare Ag 1,4-dihydro-1,4-diphenylpyridine derivatives
US7385076B2 (en) 2002-05-31 2008-06-10 Sun Pharmaceutical Industries Limited Process for the preparation of phenylcarbamates
GB0219896D0 (en) 2002-08-27 2002-10-02 Bayer Ag Dihydropyridine derivatives
US7230017B2 (en) 2002-08-27 2007-06-12 Bayer Healthcare Ag Dihydropyridinone derivatives
BR0314186A (pt) 2002-09-10 2005-08-09 Bayer Healthcare Ag Derivados de pirimidinona como agentes terapêuticos contra processos inflamatórios, isquêmicos e remodeladores, agudos e crÈnicos
CA2498052C (en) 2002-09-10 2011-05-17 Bayer Healthcare Ag Heterocyclic derivatives
GB2392910A (en) 2002-09-10 2004-03-17 Bayer Ag 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors
SE0302324D0 (sv) 2003-08-28 2003-08-28 Astrazeneca Ab Novel compounds
EP1723121B1 (en) 2004-02-26 2012-07-25 Bayer Pharma Aktiengesellschaft 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors
CA2557272C (en) 2004-02-26 2012-09-11 Bayer Healthcare Ag Heterocyclic derivatives
PL201306B1 (pl) 2004-07-28 2009-03-31 Politechnika Wroclawska Sposób wytwarzania N,N'-alkilidenobis(karbaminianów) dialkilowych
GB0502258D0 (en) 2005-02-03 2005-03-09 Argenta Discovery Ltd Compounds and their use
DE102005028845A1 (de) 2005-06-22 2006-12-28 Sanofi-Aventis Deutschland Gmbh Substituierte Heterocyclen, ihre Verwendung als Medikament sowie enthaltende pharmazeutische Zubereitungen
GB0512940D0 (en) 2005-06-24 2005-08-03 Argenta Discovery Ltd Compounds and their use
BRPI0617513A2 (pt) 2005-10-20 2011-07-26 Sumitomo Chemical Co compostos de benzoilurÉia, processo para a produÇço e uso dos mesmos e mÉtodo para controlar pestes
WO2009013444A1 (en) 2007-07-25 2009-01-29 Argenta Discovery Limited Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
PT2024367E (pt) 2006-05-04 2010-12-03 Pulmagen Therapeutics Inflammation Ltd Tetra-hidropirrolopirimidinadionas e a sua utilização a título de inibidores da elastase de neutrófilos humana
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
GB0610765D0 (en) 2006-05-31 2006-07-12 Proskelia Sas Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
DE102006031314A1 (de) 2006-07-01 2008-01-03 Bayer Healthcare Aktiengesellschaft Verwendung von 1,4-Diaryl-dihydropyrimidin-2-on-Derivaten zur Behandlung der pulmonalen arteriellen Hyptertonie
US20100010024A1 (en) 2006-07-01 2010-01-14 Bayer Healthcare Ag Use of1,4-diaryl-dihydropyrimidine-2-on derivatives for treating pulmonary arterial hypertension
CN101225083A (zh) * 2007-01-16 2008-07-23 北京摩力克科技有限公司 四氢喹唑啉酮类化合物及其用于制备治疗和预防病毒性疾病的药物的用途
WO2009037413A1 (en) 2007-09-19 2009-03-26 Argenta Discovery Limited Dimers of 5- [ (4-cyanophenyl) sulfinyl] -6-methyl-2-oxo-1- [3- (trifluoromethyl)phenyl] -1,2-dihydropyridine-3-carboxamide as inhibitors of human neutrophil elastase for treating respiratory diseases
GB0721866D0 (en) 2007-11-07 2007-12-19 Argenta Discovery Ltd Pharmaceutical compounds having dual activities
WO2009060158A1 (en) 2007-11-07 2009-05-14 Argenta Discovery Limited 4- (4-cyanophenyl) -1- (3-trifluoromethylphenyl) -3,4, 6, 7-tetrahydro-1h-pyrrolo [3, 4- d] pyrimidine-2, 5-dione derivatives and their use as human neutrophil elastase inhibitors
WO2009060206A1 (en) 2007-11-07 2009-05-14 Argenta Discovery Limited 3,4,6,7-tetrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-diones and their therapeutic use
DE102007061766A1 (de) 2007-12-20 2009-06-25 Bayer Healthcare Ag 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
DE102008022521A1 (de) 2008-05-07 2009-11-12 Bayer Schering Pharma Aktiengesellschaft 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung
DE102008052013A1 (de) 2008-10-17 2010-04-22 Bayer Schering Pharma Aktiengesellschaft 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
ATE548355T1 (de) 2007-12-20 2012-03-15 Bayer Pharma AG 4- (4-cyano-2-thioaryl) -dihydropyrimidinone und ihre verwendung
DE102009004197A1 (de) 2009-01-09 2010-07-15 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung
DE102009016553A1 (de) 2009-04-06 2010-10-07 Bayer Schering Pharma Aktiengesellschaft Sulfonamid- und Sulfoximin-substituierte Diaryldihydropyrimidinone und ihre Verwendung
US8865704B2 (en) 2009-10-07 2014-10-21 Siena Biotech S.P.A. Wnt pathway antagonists
MY160249A (en) 2010-01-08 2017-02-28 Catabasis Pharmaceuticals Inc Fatty acid fumarate derivatives and their uses
WO2011094953A1 (en) 2010-02-08 2011-08-11 F. Hoffmann-La Roche Ag Compounds for the treatment and prevention of influenza
GB201004179D0 (en) 2010-03-12 2010-04-28 Pulmagen Therapeutics Inflamma Enzyme inhibitors
GB201004178D0 (en) 2010-03-12 2010-04-28 Pulmagen Therapeutics Inflamma Enzyme inhibitors
JP2013177318A (ja) 2010-06-30 2013-09-09 Dainippon Sumitomo Pharma Co Ltd ジヒドロピリミジノン誘導体およびその医薬用途
US9040516B2 (en) 2011-08-01 2015-05-26 Sumitomo Dainippon Pharma Co., Ltd. Uracil derivative and use thereof for medical purposes
WO2013037809A1 (en) 2011-09-14 2013-03-21 Chiesi Farmaceutici S.P.A. Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017522350A (ja) * 2014-07-31 2017-08-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用

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