MA27295A1 - Inhibiteurs de la cathepsine protease a cysteine - Google Patents

Inhibiteurs de la cathepsine protease a cysteine

Info

Publication number
MA27295A1
MA27295A1 MA27826A MA27826A MA27295A1 MA 27295 A1 MA27295 A1 MA 27295A1 MA 27826 A MA27826 A MA 27826A MA 27826 A MA27826 A MA 27826A MA 27295 A1 MA27295 A1 MA 27295A1
Authority
MA
Morocco
Prior art keywords
protease inhibitors
cysteine cathepsin
cathepsin protease
inhibitors
compounds
Prior art date
Application number
MA27826A
Other languages
English (en)
Inventor
Chitra Baskaran
Cameron Black
Michael J Green
James W Janc
Serge Leger
Dan Mckay
James T Palmer
Vouy-Linh Truong
Christopher I Bayly
Jacques Yves Gauthier
Bernard L Hirschbein
Cheuk Lau
Chun Sing Li
Christophe Mellon
Michel Therien
Original Assignee
Merck Frosst Canada Inc
Axys Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27807943&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA27295(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Frosst Canada Inc, Axys Pharm Inc filed Critical Merck Frosst Canada Inc
Publication of MA27295A1 publication Critical patent/MA27295A1/fr

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    • C07C237/20Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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Abstract

Cette invention concerne une nouvelle classe de composés qui sont des inhibiteurs de cystéines protéases, y compris mais sans y être limités, des inhibiteurs des cathepsines K, L, S et B. Ces composés sont utiles pour traiter des maladies dans lesquelles l'inhibition de la résorption osseuse est indiquée, telles que l'ostéoporose.
MA27826A 2002-03-05 2004-08-17 Inhibiteurs de la cathepsine protease a cysteine MA27295A1 (fr)

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Families Citing this family (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9937531B2 (en) 2009-03-10 2018-04-10 Bookit Oy Ajanvarauspalvelu Method and system for delivery of goods
CN1309370C (zh) 2002-02-01 2007-04-11 辉瑞产品公司 使用改进的喷雾干燥设备制备均匀喷雾干燥的固体非晶形药物分散体的方法
BRPI0308208B8 (pt) 2002-03-05 2021-05-25 Axys Pharm Inc compostos inibidores de catepsina cisteína protease e composições farmacêuticas compreendendo os mesmos
WO2003077948A1 (fr) * 2002-03-19 2003-09-25 Kowa Co., Ltd. Myelome : medicaments preventifs/curatifs et methode de diagnostic
DE602004023838D1 (de) * 2003-04-24 2009-12-10 Merck & Co Inc Hemmer der akt aktivität
CN1839114A (zh) * 2003-08-21 2006-09-27 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
WO2005021487A1 (fr) * 2003-08-27 2005-03-10 Merck Frosst Canada Ltd. Inhibiteurs de la cathepsine
TW200524851A (en) * 2003-09-18 2005-08-01 Axys Pharm Inc Haloalkyl containing compounds as cysteine protease inhibitors
NZ546504A (en) 2003-10-24 2009-01-31 Aventis Pharma Inc Novel keto-oxadiazole derivatives as cathepsin inhibitors
WO2005056529A1 (fr) * 2003-12-12 2005-06-23 Merck Frosst Canada Ltd. Inhibiteurs des proteases a cysteine du type cathepsine
EP1715920A4 (fr) * 2004-01-08 2009-03-18 Merck Frosst Canada Ltd Inhibiteurs de cathepsine cysteine protease
US7429674B2 (en) 2004-04-14 2008-09-30 Merck & Co. Inc.. Process for preparing fluoroleucine alkyl esters
WO2006017455A2 (fr) 2004-08-04 2006-02-16 Merck & Co., Inc. Procédé diastéréosélectif d’amination réductrice
CA2580065A1 (fr) * 2004-09-17 2006-03-30 Schering Ag Procedes et produits intermediaires permettant de preparer des inhibiteurs de la cysteine protease
TW200619206A (en) * 2004-09-29 2006-06-16 Anormed Inc Chemokine-binding heterocyclic compound salts, and methods of use thereof
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
JP4988589B2 (ja) * 2004-12-01 2012-08-01 ビロベイ,インコーポレイティド システインプロテアーゼインヒビターとしてのハロアルキル含有化合物
WO2006060810A1 (fr) 2004-12-02 2006-06-08 Schering Aktiengesellschaft Composes de sulfonamide utilises comme inhibiteurs des cysteine proteases
EP1841730A4 (fr) * 2005-01-19 2010-10-27 Merck Frosst Canada Ltd Inhibiteurs de la cathepsine k et atherosclerose
US20090005323A1 (en) * 2005-01-19 2009-01-01 Michael David Percival Cathepsin K Inhibitors and Obesity
PT1855674E (pt) * 2005-03-02 2014-10-08 Merck Canada Inc Composição para a inibição de catepsina k
WO2006093467A1 (fr) * 2005-03-02 2006-09-08 Agency For Science, Technology And Research Molecules organiques conjuguees destinees a des dispositifs electroniques moleculaires
MX2007011617A (es) * 2005-03-21 2008-03-13 Applera Corp Compuestos de alfa-cetoamida como inhibidores de la cisteina proteasa.
EP1866277B1 (fr) * 2005-03-22 2014-06-25 Virobay, Inc. Composes contenant du sulfonyle en tant qu'inhibiteurs de cysteine proteases
JP2008545720A (ja) 2005-06-02 2008-12-18 メルク フロスト カナダ リミテツド カテプシン阻害剤としてのフルオロアルキルアミン誘導体
BRPI0613423A2 (pt) 2005-07-19 2012-12-11 Daiichi Sankyo Co Ltd composição farmacêutica, composto ou um seu sal farmaceuticamente aceitável, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
WO2007012180A1 (fr) * 2005-07-26 2007-02-01 Merck Frosst Canada Ltd. Inhibiteurs de la cystéine protéase de la famille de la papaïne pour le traitement des maladies parasitaires
ES2392675T3 (es) 2006-06-01 2012-12-12 Sanofi Nitrilos espirocíclicos como inhibidores de proteasa
US7622593B2 (en) * 2006-06-27 2009-11-24 The Procter & Gamble Company Human protein tyrosine phosphatase inhibitors and methods of use
US7893112B2 (en) * 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
KR101555931B1 (ko) 2006-10-04 2015-09-30 비로베이, 인코포레이티드 시스테인 프로테아제 억제제로서의 디­플루오로 함유 화합물
MX2009007050A (es) * 2006-12-29 2009-09-23 Abbott Gmbh & Co Kg Compuestos de carboxamida y su uso como inhibidores de calpaina.
WO2008106059A1 (fr) 2007-02-26 2008-09-04 Merck & Co., Inc. Formulations pour inhibiteurs de la cathepsine k
JP5364695B2 (ja) * 2007-04-02 2013-12-11 メルク カナダ インコーポレイテッド カテプシンkインヒビターのアミド化調製方法
CN101970007A (zh) 2007-06-08 2011-02-09 日本化学医药株式会社 脑动脉瘤的治疗或预防药
US20100331545A1 (en) 2007-10-24 2010-12-30 Nippon Chemiphar Co., Ltd. Regulator for signaling toll-like receptor, which comprises cathepsin inhibitor as active ingredient
WO2009067797A1 (fr) * 2007-11-29 2009-06-04 Merck Frosst Canada Ltd. Inhibiteurs de cystéine-protéases pour le traitement de maladies parasitaires
WO2009096198A1 (fr) * 2008-02-01 2009-08-06 Pharma Ip Limited Liability Intermediary Corporations Nouveau derive de biaryle
CN102014635B (zh) * 2008-04-01 2015-12-16 维罗贝股份有限公司 作为半胱氨酸蛋白酶抑制剂的含二氟化合物
US20090291945A1 (en) * 2008-04-09 2009-11-26 Teijin Pharma Limited Cysteine protease inhibitors
US20110065800A1 (en) * 2008-05-14 2011-03-17 Haihong Fan Formulations for cathepsin k inhibitors
SI2421826T1 (sl) * 2009-04-20 2014-02-28 F. Hoffmann-La Roche Ag Derivati prolina kot inhibitorji katepsina
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US9051304B2 (en) * 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP2675440B1 (fr) * 2011-02-14 2020-03-25 Merck Sharp & Dohme Corp. Inhibiteurs de cystéine protéases, les cathepsines
US20130331597A1 (en) * 2011-03-02 2013-12-12 Guy Humphrey Amidation process
WO2012151319A1 (fr) 2011-05-02 2012-11-08 Virobay, Inc. Inhibiteur de cathepsine pour le traitement du cancer des os et de la douleur provoquée par le cancer des os
KR20140034821A (ko) * 2011-05-16 2014-03-20 바이엘 인텔렉쳐 프로퍼티 게엠베하 폐고혈압 및/또는 심부전의 치료 및/또는 예방을 위한 카텝신 k 억제의 용도
US10023862B2 (en) 2012-01-09 2018-07-17 Arrowhead Pharmaceuticals, Inc. Organic compositions to treat beta-catenin-related diseases
ME03300B (fr) 2012-06-13 2019-07-20 Incyte Holdings Corp Composés tricycliques substitués servant d'inhibiteurs des fgfr
WO2014026125A1 (fr) 2012-08-10 2014-02-13 Incyte Corporation Dérivés de pyrazine en tant qu'inhibiteurs de fgfr
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
HUE039052T2 (hu) 2013-02-19 2018-12-28 Novartis Ag Benzotiofénszármazékok és azok készítményei szelektív ösztrogén receptor lebontóként
RU2737434C2 (ru) 2013-03-13 2020-11-30 Форма Терапьютикс, Инк. Новые соединения и композиции для ингибирования fasn
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
EP2996678A1 (fr) 2013-05-16 2016-03-23 Sandoz AG Comprimé à charge médicamenteuse accrue d'odanacatib
EP2808012A1 (fr) 2013-05-29 2014-12-03 ratiopharm GmbH Procédé de production de forme posologique comportant de l'odanacatib
US9481707B2 (en) 2013-06-14 2016-11-01 Seikagaku Corporation α-oxoacyl amino-caprolactam derivative
WO2014199645A1 (fr) 2013-06-14 2014-12-18 生化学工業株式会社 CORPS α-OXOACYL AMINO-CAPROLACTAM
US20160166529A1 (en) * 2013-07-11 2016-06-16 Merck Sharp & Dohme Corp. Formulations for Cathepsin K Inhibitors with Vitamin D
RU2692799C2 (ru) * 2013-10-08 2019-06-27 Мерк Шарп И Доум Корп. Ингибиторы цистеинпротеаз катепсинов
WO2015092634A1 (fr) 2013-12-16 2015-06-25 Novartis Ag Composés et compositions de 1,2,3,4-tétrahydroisoquinoléine en tant qu'antagonistes et agents de dégradation sélectifs des récepteurs des œstrogènes
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
US10093646B2 (en) 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
JP6473457B2 (ja) 2014-01-17 2019-02-20 ノバルティス アーゲー Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CZ2014941A3 (cs) 2014-12-19 2016-06-29 Zentiva, K.S. Příprava vysoce čistého intermediátu pro syntézu Odanacatibu
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
WO2016134294A1 (fr) 2015-02-20 2016-08-25 Incyte Corporation Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA2976766A1 (fr) 2015-03-25 2016-09-29 Novartis Ag Derives n-heterocycliques formyles utilises en tant qu'inhibiteurs de fgfr4
EP3310779B1 (fr) 2015-06-19 2019-05-08 Novartis AG Composés et compositions pour l'inhibition de l'activité de shp2
CN112625028A (zh) 2015-06-19 2021-04-09 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203405A1 (fr) 2015-06-19 2016-12-22 Novartis Ag Composés et compositions pour inhiber l'activité de shp2
US10494364B2 (en) 2015-08-29 2019-12-03 Sunshin Lake Pharma Co., Ltd Cathepsin K inhibitors and application thereof
WO2017089389A1 (fr) * 2015-11-26 2017-06-01 F. Hoffmann-La Roche Ag Inhibiteurs de trypanosomes
CN106866502B (zh) * 2015-12-10 2020-10-09 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
JP6969800B2 (ja) 2016-05-04 2021-11-24 ジェノシアンス ファルマ 増殖性疾患の治療に使用される置換2,4−ジアミノ−キノリン誘導体
EA036446B1 (ru) 2016-06-14 2020-11-11 Новартис Аг Соединения и композиции для подавления активности shp2
MX2019008756A (es) * 2017-01-24 2019-09-11 Astellas Pharma Inc Compuesto de prolinamida sustituida por fenildiflurometilo.
KR101916396B1 (ko) 2017-02-20 2018-11-08 서울대학교 산학협력단 항암제 또는 항균제로 사용될 수 있는 단백질분해효소 저해제
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3681879A1 (fr) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals, Inc. Inhibiteurs allostériques octahydrocyclopenta[c]pyrrole de shp2
NL2020021B1 (en) * 2017-12-05 2019-06-13 Academisch Ziekenhuis Leiden Cathepsin inhibitors
EP3720840B1 (fr) 2017-12-05 2022-01-19 Academisch Ziekenhuis Leiden (h.o.d.n. LUMC) Inhibiteurs de la cathepsine
WO2019190117A1 (fr) 2018-03-28 2019-10-03 한림제약(주) Dérivé de 2-cyanopyrimidin-4-yl carbamate ou d'urée ou sel de celui-ci et composition pharmaceutique le comprenant
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
EA202092649A1 (ru) 2018-05-04 2021-06-21 Инсайт Корпорейшн Соли ингибитора fgfr
US11459340B2 (en) 2018-09-18 2022-10-04 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as Src homology-2 phosphatase inhibitors
AU2019346550A1 (en) 2018-09-25 2021-04-22 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
CN113164776A (zh) 2018-09-25 2021-07-23 黑钻治疗公司 酪氨酸激酶抑制剂组合物、其制备方法和使用方法
EP4282416A3 (fr) 2018-09-29 2024-03-06 Novartis AG Procédé de fabrication d'un composé pour inhiber l'activité de shp2
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3946332A1 (fr) 2019-04-05 2022-02-09 Université de Bretagne Occidentale Inhibiteurs du récepteur 2 activé par une protéase pour le traitement d'une neuropathie sensorielle induite par une intoxication neurotoxique marine
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4013749A1 (fr) 2019-08-15 2022-06-22 Black Diamond Therapeutics, Inc. Composés d'alcynyle quinazoline
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
WO2021076728A1 (fr) 2019-10-16 2021-04-22 Incyte Corporation Hétérocycles bicycliques en tant qu'inhibiteurs de fgfr
WO2021113479A1 (fr) 2019-12-04 2021-06-10 Incyte Corporation Hétérocycles tricycliques en tant qu'inhibiteurs de fgfr
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021195206A1 (fr) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Formes polymorphes et utilisations associées
WO2022043557A1 (fr) 2020-08-31 2022-03-03 Advanced Accelerator Applications International Sa Méthode de traitement de cancers exprimant le psma
EP4204020A1 (fr) 2020-08-31 2023-07-05 Advanced Accelerator Applications International S.A. Méthode de traitement de cancers exprimant le psma
WO2022043556A1 (fr) 2020-08-31 2022-03-03 Novartis Ag Composition pharmaceutique stable
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
CA3208313A1 (fr) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Composes d'isoindolinone
WO2022170052A1 (fr) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Dérivés de quinazoline, dérivés de pyridopyrimidine, dérivés de pyrimidopyrimidine et leurs utilisations
EP4323350A1 (fr) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Composés d'iso-indolinone
EP4323349A1 (fr) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Composés amide d'isoindolinone utilisés pour traiter des maladies associées à gspt1
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
WO2023284730A1 (fr) 2021-07-14 2023-01-19 Nikang Therapeutics, Inc. Dérivés d'alkylidène en tant qu'inhibiteurs de kras
TW202346292A (zh) 2022-03-28 2023-12-01 美商尼坎醫療公司 作為週期蛋白依賴性激酶2抑制劑的磺醯胺基衍生物
WO2023240024A1 (fr) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Dérivés de sulfamide utilisés en tant qu'inhibiteurs de kinase 2 dépendant de la cycline

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR200001189T2 (tr) * 1997-11-05 2000-09-21 Novartis Ag. Dipeptid nitriller.
WO2000049007A1 (fr) 1999-02-20 2000-08-24 Astrazeneca Ab Derives acetamido acetonitriles en tant qu'inhibiteurs de la cathepsine l et/ou s
DK1178958T3 (da) * 1999-03-15 2004-06-21 Axys Pharm Inc N-cyanomethylamider som proteaseinhibitorer
WO2001019808A1 (fr) * 1999-09-16 2001-03-22 Axys Pharmaceuticals, Inc. Composes et compositions chimiques et leur utilisation en tant qu'inhibiteurs de la cathepsine s
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
DE60113406T2 (de) * 2000-05-15 2006-06-29 Novartis Ag N-substituierte peptidylnitrile als cystein-cathepsin-inhibitoren
US7012075B2 (en) * 2001-03-02 2006-03-14 Merck & Co., Inc. Cathepsin cysteine protease inhibitors
EP1595363B1 (fr) * 2001-08-15 2016-07-13 The Board of Governors for Higher Education State of Rhode Island and Providence Plantations Procede et dispositif de memoire cache du protocole scsi vers le protocole ip
CA2466115A1 (fr) * 2001-11-13 2003-05-22 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Derives cyanoalkylamino utilises comme inhibiteurs de la protease
BRPI0308208B8 (pt) * 2002-03-05 2021-05-25 Axys Pharm Inc compostos inibidores de catepsina cisteína protease e composições farmacêuticas compreendendo os mesmos
TW200524851A (en) * 2003-09-18 2005-08-01 Axys Pharm Inc Haloalkyl containing compounds as cysteine protease inhibitors
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
JP2008545720A (ja) * 2005-06-02 2008-12-18 メルク フロスト カナダ リミテツド カテプシン阻害剤としてのフルオロアルキルアミン誘導体

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