ATE395911T1 - Cathepsin-cystein-protease-hemmer - Google Patents

Cathepsin-cystein-protease-hemmer

Info

Publication number
ATE395911T1
ATE395911T1 AT03716238T AT03716238T ATE395911T1 AT E395911 T1 ATE395911 T1 AT E395911T1 AT 03716238 T AT03716238 T AT 03716238T AT 03716238 T AT03716238 T AT 03716238T AT E395911 T1 ATE395911 T1 AT E395911T1
Authority
AT
Austria
Prior art keywords
protease inhibitors
cathepsin
cystein protease
compounds
inhibitors
Prior art date
Application number
AT03716238T
Other languages
English (en)
Inventor
Christopher Bayly
Cameron Black
Serge Leger
Chun Sing Li
Dan Mckay
Christophe Mellon
Jacques Yves Gauthier
Cheuk Lau
Michel Therien
Vouy-Linh Truong
Michael Green
Bernard Hirschbein
James Janc
James Palmer
Chitra Baskaran
Original Assignee
Merck Frosst Canada Ltd
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=ATE395911(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Frosst Canada Ltd, Axys Pharm Inc filed Critical Merck Frosst Canada Ltd
Application granted granted Critical
Publication of ATE395911T1 publication Critical patent/ATE395911T1/de

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    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/20—Carboxylic 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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    • C07C255/17—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and doubly-bound oxygen atoms bound to the same acyclic carbon skeleton
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    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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    • C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
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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 (en) * 2003-08-27 2005-03-10 Merck Frosst Canada Ltd. Cathepsin inhibitors
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 (en) * 2003-12-12 2005-06-23 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
EP1715920A4 (de) * 2004-01-08 2009-03-18 Merck Frosst Canada Ltd Cathepsincysteinproteasehemmer
US7429674B2 (en) 2004-04-14 2008-09-30 Merck & Co. Inc.. Process for preparing fluoroleucine alkyl esters
WO2006017455A2 (en) 2004-08-04 2006-02-16 Merck & Co., Inc. Diastereoselective reductive amination process
CA2580065A1 (en) * 2004-09-17 2006-03-30 Schering Ag Processes and intermediates for preparing cysteine protease inhibitors
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 (en) 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
EP1841730A4 (de) * 2005-01-19 2010-10-27 Merck Frosst Canada Ltd Cathepsin-k-inhibitoren und atherosklerose
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 (en) * 2005-03-02 2006-09-08 Agency For Science, Technology And Research Conjugated organic molecules for molecular electronic devices
MX2007011617A (es) * 2005-03-21 2008-03-13 Applera Corp Compuestos de alfa-cetoamida como inhibidores de la cisteina proteasa.
EP1866277B1 (de) * 2005-03-22 2014-06-25 Virobay, Inc. Sulfonylhaltige verbindungen als cysteinproteaseinhibitoren
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 (en) * 2005-07-26 2007-02-01 Merck Frosst Canada Ltd. Papain family cysteine protease inhibitors for the treatment of parasitic diseases
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 (en) 2007-02-26 2008-09-04 Merck & Co., Inc. Formulations for cathepsin k inhibitors
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 (en) * 2007-11-29 2009-06-04 Merck Frosst Canada Ltd. Cysteine protease inhibitors for the treatment of parasitic diseases
WO2009096198A1 (ja) * 2008-02-01 2009-08-06 Pharma Ip Limited Liability Intermediary Corporations 新規ビアリール誘導体
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 (de) * 2011-02-14 2020-03-25 Merck Sharp & Dohme Corp. Cathepsin-cysteinproteasehemmer
US20130331597A1 (en) * 2011-03-02 2013-12-12 Guy Humphrey Amidation process
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
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 (de) 2012-06-13 2019-07-20 Incyte Holdings Corp Substituierte tricyclische verbindungen als fgfr-inhibitoren
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
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 (de) 2013-05-16 2016-03-23 Sandoz AG Tablette mit höherer odanacatib-wirkstoffbeladung
EP2808012A1 (de) 2013-05-29 2014-12-03 ratiopharm GmbH Verfahren zur Herstellung einer Dosierform mit Odanacatib
US9481707B2 (en) 2013-06-14 2016-11-01 Seikagaku Corporation α-oxoacyl amino-caprolactam derivative
WO2014199645A1 (ja) 2013-06-14 2014-12-18 生化学工業株式会社 α－オキソアシルアミノカプロラクタム体
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 (en) 2013-12-16 2015-06-25 Novartis Ag 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders
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 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA2976766A1 (en) 2015-03-25 2016-09-29 Novartis Ag Formylated n-heterocyclic derivatives as fgfr4 inhibitors
EP3310779B1 (de) 2015-06-19 2019-05-08 Novartis AG Verbindungen und zusammensetzungen zur hemmung der aktivität von 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 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
US10494364B2 (en) 2015-08-29 2019-12-03 Sunshin Lake Pharma Co., Ltd Cathepsin K inhibitors and application thereof
WO2017089389A1 (en) * 2015-11-26 2017-06-01 F. Hoffmann-La Roche Ag Trypanosomes inhibitors
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 (de) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals, Inc. Allosterische octahydrocyclopenta[c]pyrrolinhibitoren von shp2
NL2020021B1 (en) * 2017-12-05 2019-06-13 Academisch Ziekenhuis Leiden Cathepsin inhibitors
EP3720840B1 (de) 2017-12-05 2022-01-19 Academisch Ziekenhuis Leiden (h.o.d.n. LUMC) Cathepsin-hemmer
WO2019190117A1 (ko) 2018-03-28 2019-10-03 한림제약(주) 2-시아노피리미딘-4-일 카르바메이트 혹은 유레아 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
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 (de) 2018-09-29 2024-03-06 Novartis AG Verfahren zur herstellung einer verbindung zur hemmung der aktivität von 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 (de) 2019-04-05 2022-02-09 Université de Bretagne Occidentale Protease-aktivierte rezeptor-2-inhibitoren zur behandlung einer sensorischen neuropathie, die durch eine marine neurotoxische vergiftung induziert wird
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4013749A1 (de) 2019-08-15 2022-06-22 Black Diamond Therapeutics, Inc. Alkinylchinazolin-verbindungen
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021195206A1 (en) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Polymorphic forms and related uses
WO2022043557A1 (en) 2020-08-31 2022-03-03 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
EP4204020A1 (de) 2020-08-31 2023-07-05 Advanced Accelerator Applications International S.A. Verfahren zur behandlung von psma-exprimierenden krebsarten
WO2022043556A1 (en) 2020-08-31 2022-03-03 Novartis Ag Stable radiopharmaceutical composition
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
CA3208313A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022170052A1 (en) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof
EP4323350A1 (de) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinonverbindungen
EP4323349A1 (de) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinonamidverbindungen zur behandlung von krankheiten im zusammenhang mit gspt1
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
WO2023284730A1 (en) 2021-07-14 2023-01-19 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
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 (en) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors

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 (en) 1999-02-20 2000-08-24 Astrazeneca Ab Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsin s
DK1178958T3 (da) * 1999-03-15 2004-06-21 Axys Pharm Inc N-cyanomethylamider som proteaseinhibitorer
WO2001019808A1 (en) * 1999-09-16 2001-03-22 Axys Pharmaceuticals, Inc. Chemical compounds and compositions and their use as cathepsin s inhibitors
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 (de) * 2001-08-15 2016-07-13 The Board of Governors for Higher Education State of Rhode Island and Providence Plantations Scsi-zu-ip-cache-speichereinrichtung und -verfahren
CA2466115A1 (en) * 2001-11-13 2003-05-22 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Cyanoalkylamino derivatives as protease inhibitors
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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