CN108707140B - 蛋白酶c抑制剂 - Google Patents

蛋白酶c抑制剂 Download PDF

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Publication number
CN108707140B
CN108707140B CN201810715894.0A CN201810715894A CN108707140B CN 108707140 B CN108707140 B CN 108707140B CN 201810715894 A CN201810715894 A CN 201810715894A CN 108707140 B CN108707140 B CN 108707140B
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alkylene
alkyl
independently
optionally
substitution
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CN108707140A (zh
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R·安德斯凯维茨
M·格劳尔特
M·格伦德尔
P·W·黑贝尔
T·奥斯特
A·波奇
S·彼得斯
F·宾德
V·文顿亚克
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Boehringer Ingelheim International GmbH
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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
EP3112366B1 (en) 2013-03-14 2018-02-28 Janssen Pharmaceutica NV P2x7 modulators
AU2014230814B2 (en) * 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 P2x7調控劑
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 P2x7調節劑
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
JP6529575B2 (ja) * 2014-08-01 2019-06-12 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 置換オキセタンおよびそれらのカテプシンcの阻害薬としての使用
US20180118749A1 (en) 2014-09-12 2018-05-03 Janssen Pharmaceutica Nv P2x7 modulators
PL3191487T3 (pl) * 2014-09-12 2020-03-31 Boehringer Ingelheim International Gmbh Spirocykliczne inhibitory katepsyny C
EP3191492B1 (en) 2014-09-12 2019-01-09 Janssen Pharmaceutica NV P2x7 modulators
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
AU2016227618B2 (en) * 2015-03-05 2020-06-04 Neuprozyme Therapeutics ApS Peptidyl nitril compounds as dipeptidyl peptidase I inhibitors
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
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
CA3039203A1 (en) 2016-10-03 2018-04-12 Sigilon Therapeutics, Inc. Compounds, devices, and uses thereof
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
EP3641757A4 (en) * 2017-06-23 2021-03-24 New York Society for the Ruptured and Crippled Maintaining the Hospital for Special Surgery COMPOSITION, USES, AND METHOD OF TREATMENTAL DISC DEGENERATION BY A HEDGEHOG SOUND PATH
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
KR102738945B1 (ko) 2018-03-01 2024-12-04 아스트라제네카 에이비이 (2s)-n-{(1s)-1-시아노-2-[4-(3-메틸-2-옥소-2,3-디하이드로-1,3-벤족사졸-5-일)페닐]에틸}-1,4-옥사제판-2-카복스아미드를 포함하는 약학 조성물
WO2019169245A1 (en) 2018-03-02 2019-09-06 Sigilon Therapeutics, Inc. Biocompatible hydrogel capsules and process for preparing same
JP2021515767A (ja) 2018-03-07 2021-06-24 バイエル・アクチエンゲゼルシヤフト Erk5阻害剤の同定及び使用
JP7534219B2 (ja) 2018-04-04 2024-08-14 シギロン セラピューティクス, インコーポレイテッド 移植可能な粒子及び関連方法
KR20210032431A (ko) 2018-07-17 2021-03-24 인스메드 인코포레이티드 루푸스 신염을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카복스아미드
CA3111309A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
JOP20210058A1 (ar) 2018-09-28 2021-03-24 Janssen Pharmaceutica Nv مُعدلات ليباز أُحادِيُّ الجلِيسِريد
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
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
MX2022011902A (es) 2020-03-26 2023-01-04 Janssen Pharmaceutica Nv Moduladores de la monoacilglicerol lipasa.
CA3181285A1 (en) 2020-07-20 2022-01-27 Jessica BASSO Methods for extracting neutrophil serine proteases and treating dipeptidyl peptidase 1-mediated conditions
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
EP4257588A4 (en) * 2020-12-04 2024-10-16 Reistone Biopharma Company Limited SMALL MOLECULE INHIBITOR OF CATHEPSIN C AND ITS MEDICINAL USE
CN116783189A (zh) * 2021-02-05 2023-09-19 南京明德新药研发有限公司 含1,4-氧杂氮杂环庚烷的并环类衍生物
JP2024516826A (ja) * 2021-04-29 2024-04-17 インスメッド インコーポレイテッド 嚢胞性線維症を治療するためのある特定のn-(1-シアノ-2-フェニルエチル)-1,4-オキサゼパン-2-カルボキサミド
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
CN119317620A (zh) 2022-06-13 2025-01-14 亚力维克希斯股份有限公司 氮杂环烷基羰基环状胺化合物
EP4634162A1 (en) 2022-12-16 2025-10-22 Syngenta Crop Protection AG Benzimidazole derivatives
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
CN120584108A (zh) 2023-01-06 2025-09-02 英斯梅德股份有限公司 新型可逆dpp1抑制剂及其用途
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1921907A (zh) * 2004-01-08 2007-02-28 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
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
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 (43)

* 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
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
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
US20070099958A1 (en) 2003-06-18 2007-05-03 Prozymex A/S Protease inhibitors
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
WO2006096807A1 (en) 2005-03-08 2006-09-14 Janssen Pharmaceutica N.V. Aza-bridged-bicyclic amino acid derivatives as alpha 4 integrin antagonists
US20090247560A1 (en) 2006-09-28 2009-10-01 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
EA201000958A1 (ru) 2007-12-12 2010-12-30 Астразенека Аб Пептидилнитрилы и их применение в качестве ингибиторов дипептидилпептидазы i
EP2427445A1 (en) 2009-05-07 2012-03-14 AstraZeneca AB Substituted 1-cyanoethylheterocyclylcarboxamide compounds 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
WO2012119941A1 (en) * 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
WO2013160418A1 (en) 2012-04-27 2013-10-31 Glaxo Group Limited Novel compounds
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
PE20150400A1 (es) 2012-05-22 2015-03-27 Genentech Inc Benzamidas n-sustituidas y su uso en el tratamiento del dolor
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
WO2014052699A1 (en) 2012-09-28 2014-04-03 Cephalon, Inc. Azaquinazoline inhibitors of atypical protein kinase c
JP2015533134A (ja) 2012-10-09 2015-11-19 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 錠剤の機械的安定性に適切な少なくとも1種の水和物形成活性物質及び/又はアジュバントを含有する機械的に安定な錠剤、特にアルギニン含有錠剤の製造における選択的に水分調整された打錠材料の使用
NZ706739A (en) 2012-10-15 2018-11-30 Epizyme Inc Substituted benzene compounds
AU2013331496B2 (en) 2012-10-16 2017-07-27 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ROR-gamma-t
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9233974B2 (en) 2012-12-21 2016-01-12 Gilead Sciences, Inc. Antiviral compounds
CN105026372B (zh) 2012-12-21 2018-06-05 赛尔基因昆蒂赛尔研究公司 组蛋白脱甲基酶抑制剂
KR20150119012A (ko) 2013-02-08 2015-10-23 셀진 아빌로믹스 리서치, 인코포레이티드 Erk 억제제 및 이의 용도
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
AU2014229313B2 (en) 2013-03-14 2016-07-28 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 P2x7調節劑
AU2014230814B2 (en) * 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
RU2667509C2 (ru) 2013-03-14 2018-09-21 Ньюлинк Джинетикс Корпорейшин Трициклические соединения в качестве ингибиторов иммуносупрессии, опосредуемой метаболизированием триптофана
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
WO2016003723A1 (en) 2014-07-03 2016-01-07 Bridgestone Americas Tire Operations, Llc Sidewall decoration on rim guard
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
PT3191476T (pt) 2014-09-12 2019-01-17 Glaxosmithkline Ip No 2 Ltd Derivados de tetra-hidroquinolina como inibidores de bromodomínio

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1921907A (zh) * 2004-01-08 2007-02-28 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
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
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

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WO2014140075A1 (en) 2014-09-18
CN108707140A (zh) 2018-10-26
TW201522307A (zh) 2015-06-16
US20210260027A1 (en) 2021-08-26
HK1211579A1 (en) 2016-05-27
EP2970283B1 (en) 2020-11-11
BR112015019720B8 (pt) 2023-10-10
US9713606B2 (en) 2017-07-25
UY35391A (es) 2014-09-30
US8987249B2 (en) 2015-03-24
BR112015019720A2 (pt) 2017-07-18
AU2014230814B2 (en) 2017-12-21
PL2970283T3 (pl) 2021-05-31
US10238633B2 (en) 2019-03-26
PH12015501964B1 (en) 2019-07-17
CL2015002301A1 (es) 2016-06-03
US20230310373A1 (en) 2023-10-05
US20190167636A1 (en) 2019-06-06

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