KR102295740B1 - 카텝신 c의 억제제로서 치환된 2-아자-바이사이클로[2.2.1]헵탄-3-카복실산(벤질-시아노-메틸)-아미드 - Google Patents

카텝신 c의 억제제로서 치환된 2-아자-바이사이클로[2.2.1]헵탄-3-카복실산(벤질-시아노-메틸)-아미드 Download PDF

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KR102295740B1
KR102295740B1 KR1020157025088A KR20157025088A KR102295740B1 KR 102295740 B1 KR102295740 B1 KR 102295740B1 KR 1020157025088 A KR1020157025088 A KR 1020157025088A KR 20157025088 A KR20157025088 A KR 20157025088A KR 102295740 B1 KR102295740 B1 KR 102295740B1
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alkylene
alkyl
ring
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KR20150128722A (ko
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랄프 안데르스케비츠
마티아스 그라우어트
마르크 그룬들
페터 빌헬름 헤벨
토르슈텐 오스트
알렉산더 파우츠
슈테판 페터스
플로리안 빈더
빅토르 빈톤약
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베링거 인겔하임 인터내셔날 게엠베하
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Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2689526T3 (es) 2013-03-14 2018-11-14 Janssen Pharmaceutica Nv Moduladores de P2X7
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 P2x7調節劑
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 P2x7調控劑
DK2970283T3 (da) * 2013-03-14 2021-01-25 Boehringer Ingelheim Int Substituerede 2-aza-bicyclo[2.2.1]heptan-3-carboxylsyre-(benzyl-cyano-methyl)-amider som inhibitorer af cathepsin-c
JP6294953B2 (ja) 2013-03-14 2018-03-14 ヤンセン ファーマシューティカ エヌ.ベー. P2x7調節物質
NO2699580T3 (enExample) 2014-01-24 2018-02-24
WO2015140717A1 (en) 2014-03-18 2015-09-24 Iteos Therapeutics Novel 3-indol substituted derivatives, pharmaceutical compositions and methods for use
WO2016016242A1 (en) 2014-08-01 2016-02-04 Boehringer Ingelheim International Gmbh Substituted oxetanes and their use as inhibitors of cathepsin c
KR102510588B1 (ko) 2014-09-12 2023-03-17 베링거 인겔하임 인터내셔날 게엠베하 카텝신 c의 스피로사이클릭 억제제
EP3191492B1 (en) 2014-09-12 2019-01-09 Janssen Pharmaceutica NV P2x7 modulators
WO2016039983A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulating n-acyl-triazolopyrazines
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
WO2016139355A1 (en) 2015-03-05 2016-09-09 Prozymex A/S N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors
DK3265452T3 (en) * 2015-03-05 2020-06-08 Neuprozyme Therapeutics ApS Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors
CA2994604A1 (en) 2015-08-07 2017-02-16 Bayer Cropscience Aktiengesellschaft 2-(het)aryl-substituted condensed heterocyclic derivatives as pest control agents
UY37137A (es) 2016-02-24 2017-09-29 Merial Inc Compuestos antiparasitarios de isoxazolina, formulaciones inyectables de acción prolongada que los comprenden, métodos y usos de los mismos
MX2019003887A (es) * 2016-10-03 2019-11-18 Sigilon Therapeutics Inc Compuestos, dispositivos y usos de los mismos.
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
WO2018237368A1 (en) * 2017-06-23 2018-12-27 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Composition, uses, and methods of treating spinal disc degeneration through sonic hedgehog signaling pathway
CN107266373A (zh) * 2017-08-01 2017-10-20 安徽拜善晟制药有限公司 一种原料药达沙布韦的制备方法
WO2019121143A1 (en) 2017-12-20 2019-06-27 Basf Se Substituted cyclopropyl derivatives
PL3758708T3 (pl) 2018-03-01 2025-03-31 Astrazeneca Ab Kompozycje farmaceutyczne zawierające (2s)-{(1s)-1-cyjano-2-[4-(3-metylo-2-okso-2,3-dihydro-1,3-benzoksazol-5-ilo)fenylo]etylo}-1,4-oksazepano-2-karboksyamid
US12162994B2 (en) 2018-03-02 2024-12-10 Sigilon Therapeutics, Inc. Biocompatible hydrogel capsules and process for preparing same
AU2019232437A1 (en) 2018-03-07 2020-10-08 Bayer Aktiengesellschaft Identification and use of ERK5 inhibitors
TW202014181A (zh) 2018-04-04 2020-04-16 美商希吉隆醫療公司 可植入顆粒及相關方法
EP3823627A4 (en) 2018-07-17 2022-04-20 Insmed Incorporated CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR THE TREATMENT OF LUPUS ENEHROPATHY
CA3111309A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
CN113164459B (zh) 2018-09-28 2024-09-03 詹森药业有限公司 单酰基甘油脂肪酶调节剂
US11633399B2 (en) 2018-12-25 2023-04-25 Sol-Gel Technologies Ltd. Treatment of skin disorders with compositions comprising an EGFR inhibitor
CN110006871A (zh) * 2019-02-20 2019-07-12 常州大学 一个基于外源性组胺检测的细胞模型以及应用
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
CA3176946A1 (en) 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
JP2023535332A (ja) 2020-07-20 2023-08-17 インスメッド インコーポレイテッド 好中球セリンプロテアーゼを抽出するおよびジペプチジルペプチダーゼ1媒介性病態を治療するための方法
CN114106005B (zh) * 2020-08-26 2025-08-01 西藏海思科制药有限公司 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途
CN114159446A (zh) * 2020-09-11 2022-03-11 中国科学院上海营养与健康研究所 组织蛋白酶c抑制剂在治疗肿瘤转移中的应用
JP2023551488A (ja) * 2020-12-04 2023-12-08 瑞石生物医薬有限公司 カテプシンcの小分子阻害剤及びその医薬的使用
EP4289827A4 (en) * 2021-02-05 2025-01-22 Medshine Discovery Inc. CONDENSED RING DERIVATIVES CONTAINING 1,4-OXAZEPANE
CA3215375A1 (en) * 2021-04-29 2022-11-03 Insmed Incorporated Certain n-(1-cyano-2-phenylethyl)-1,4-oxazepane-2-carboxamides for treating cystic fibrosis
CN113831360A (zh) * 2021-09-10 2021-12-24 中钢集团南京新材料研究院有限公司 酰胺邻位导向硼化合成1-咔唑-硼酸频哪醇酯的方法
CN116462677A (zh) * 2022-01-20 2023-07-21 上海和誉生物医药科技有限公司 一种多稠环prmt5抑制剂及其制备方法和应用
US20230234973A1 (en) * 2022-01-27 2023-07-27 Heron Neutron Medical Corp. Intermediate, preparing method thereof, and method of preparing drug
CN114773345B (zh) * 2022-03-22 2024-01-02 盐城工业职业技术学院 一种哌嗪二酮衍生物及其制备方法
CN117279889B (zh) * 2022-04-28 2025-04-25 深圳湾实验室 经取代的氟硫酸盐及其用途
AU2023296161A1 (en) 2022-06-13 2025-01-02 Alivexis, Inc. Azacycloalkyl carbonyl cyclic amine compound
PE20251891A1 (es) 2022-12-16 2025-07-25 Syngenta Crop Protection Ag Derivados de bencimidazol
CN115974824B (zh) * 2022-12-27 2024-09-24 瑞石生物医药有限公司 一种组织蛋白酶c小分子抑制剂
EP4646265A1 (en) 2023-01-06 2025-11-12 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof
WO2025167969A1 (en) * 2024-02-07 2025-08-14 Insmed Incorporated Dipeptidyl peptidase 1 inhibitors and uses thereof
WO2025214073A1 (en) * 2024-04-12 2025-10-16 Insmed Incorporated Dipeptidyl peptidase 1 inhibitors and uses thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004531486A (ja) 2001-03-02 2004-10-14 メルク フロスト カナダ アンド カンパニー カテプシンシステインプロテアーゼ阻害薬
JP2005501017A (ja) 2001-06-08 2005-01-13 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド システインプロテアーゼの可逆的阻害剤として有効な新規なニトリル
WO2009047829A1 (ja) 2007-10-12 2009-04-16 Fujitsu Limited Ip電話自動試験システム及び方法
JP2011506421A (ja) 2007-12-12 2011-03-03 アストラゼネカ・アクチエボラーグ ペプチジルニトリル類およびジペプチジルペプチダーゼi阻害剤としてのその使用
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
WO2013041497A1 (en) 2011-09-19 2013-03-28 Boehringer Ingelheim International Gmbh Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4125727A (en) 1976-10-18 1978-11-14 American Cyanamid Company Method of preparing imidazoisoindolediones
GB8922355D0 (en) 1989-10-04 1989-11-22 British Telecomm Sealing gland
US6960597B2 (en) 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
DE20012487U1 (de) 2000-07-19 2001-04-05 Wenger, Lukas, 85521 Ottobrunn Beheizbare Scheibenwischer an Kraftfahrzeugen
TW200306189A (en) 2002-03-21 2003-11-16 Merz Pharma Gmbh & Co Kgaa Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists
JP2006527704A (ja) 2003-06-18 2006-12-07 プロザイメックス・アクティーゼルスカブ プロテアーゼ阻害剤
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
WO2005065778A1 (en) * 2004-01-08 2005-07-21 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US20060223846A1 (en) 2005-03-08 2006-10-05 Dyatkin Alexey B Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists
EP2072519A4 (en) 2006-09-28 2009-10-21 Banyu Pharma Co Ltd DIARYLKETIMINDERIVAT
BRPI1015540A2 (pt) 2009-05-07 2019-09-24 Astrazeneca Ab ''composto de 1-cianoetil-heterociclilcarboxamida substituídos 750''
WO2010142985A1 (en) 2009-06-10 2010-12-16 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
PE20142400A1 (es) 2012-04-27 2015-02-04 Glaxo Group Ltd Compuestos novedosos
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
KR101719893B1 (ko) 2012-05-22 2017-03-24 제넨테크, 인크. N-치환된 벤즈아미드 및 통증의 치료에서 이들의 용도
US8859774B2 (en) 2012-05-25 2014-10-14 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
JO3459B1 (ar) 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
NZ706857A (en) 2012-09-28 2018-05-25 Ignyta Inc Azaquinazoline inhibitors of atypical protein kinase c
WO2014056942A1 (en) 2012-10-09 2014-04-17 Boehringer Ingelheim International Gmbh Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets
SG10201705989YA (en) 2012-10-15 2017-08-30 Epizyme Inc Substituted benzene compounds
PE20150778A1 (es) 2012-10-16 2015-05-23 Janssen Pharmaceutica Nv Moduladores de quinolinilo unidos a metileno de ror-gamma-t
CA2888816A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
HK1210611A1 (en) 2012-12-21 2016-04-29 Quanticel Pharmaceuticals Inc Histone demethylase inhibitors
BR112015014752B1 (pt) 2012-12-21 2022-07-05 Plexxikon, Inc Compostos e seus uso para modulação de cinase
US9233974B2 (en) 2012-12-21 2016-01-12 Gilead Sciences, Inc. Antiviral compounds
WO2014124230A2 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
WO2014159248A1 (en) 2013-03-14 2014-10-02 Newlink Genetics Corporation Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
DK2970283T3 (da) * 2013-03-14 2021-01-25 Boehringer Ingelheim Int Substituerede 2-aza-bicyclo[2.2.1]heptan-3-carboxylsyre-(benzyl-cyano-methyl)-amider som inhibitorer af cathepsin-c
HK1213251A1 (zh) 2013-03-14 2016-06-30 Novartis Ag 作为突变idh抑制剂的3-嘧啶-4-基-恶唑烷-2-酮化合物
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 P2x7調節劑
US20160001608A1 (en) 2014-07-03 2016-01-07 Bridgestone Americas Tire Operations, Llc Sidewall decoration on rim guard
CN106687453B (zh) 2014-09-12 2019-07-19 葛兰素史克知识产权第二有限公司 作为溴结构域抑制剂的四氢喹啉衍生物
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
AR101696A1 (es) 2014-09-12 2017-01-04 Lilly Co Eli Compuestos de azetidiniloxifenilpirrolidina

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004531486A (ja) 2001-03-02 2004-10-14 メルク フロスト カナダ アンド カンパニー カテプシンシステインプロテアーゼ阻害薬
JP2005501017A (ja) 2001-06-08 2005-01-13 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド システインプロテアーゼの可逆的阻害剤として有効な新規なニトリル
WO2009047829A1 (ja) 2007-10-12 2009-04-16 Fujitsu Limited Ip電話自動試験システム及び方法
JP2011506421A (ja) 2007-12-12 2011-03-03 アストラゼネカ・アクチエボラーグ ペプチジルニトリル類およびジペプチジルペプチダーゼi阻害剤としてのその使用
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
WO2013041497A1 (en) 2011-09-19 2013-03-28 Boehringer Ingelheim International Gmbh Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c
US20130172327A1 (en) 2011-09-19 2013-07-04 Boehringer Ingelheim International Gmbh Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c

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