ATE409482T1 - Cathepsincystein-proteasehemmer - Google Patents

Cathepsincystein-proteasehemmer

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Publication number
ATE409482T1
ATE409482T1 AT02723314T AT02723314T ATE409482T1 AT E409482 T1 ATE409482 T1 AT E409482T1 AT 02723314 T AT02723314 T AT 02723314T AT 02723314 T AT02723314 T AT 02723314T AT E409482 T1 ATE409482 T1 AT E409482T1
Authority
AT
Austria
Prior art keywords
protease inhibitors
cathepsincystein
compounds
inhibitors
cathepsins
Prior art date
Application number
AT02723314T
Other languages
English (en)
Inventor
Petpiboon Prasit
Christopher Ian Bayly
Joel Stephane Robichaud
W Cameron Black
Eduardo Setti
Robert Rydzewski
James Palmer
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
Application filed by Merck Frosst Canada Ltd, Axys Pharm Inc filed Critical Merck Frosst Canada Ltd
Application granted granted Critical
Publication of ATE409482T1 publication Critical patent/ATE409482T1/de

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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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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    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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AT02723314T 2001-03-02 2002-03-01 Cathepsincystein-proteasehemmer ATE409482T1 (de)

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Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1364659B1 (de) * 2001-02-08 2009-11-11 Ono Pharmaceutical Co., Ltd. Mittel zur behandlung von harnwegserkrankungen, umfassend mittel zur kontrolle des lpa-rezeptors
BRPI0308208B8 (pt) * 2002-03-05 2021-05-25 Axys Pharm Inc compostos inibidores de catepsina cisteína protease e composições farmacêuticas compreendendo os mesmos
JP4505329B2 (ja) * 2002-09-04 2010-07-21 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害薬
SE0203712D0 (sv) * 2002-12-13 2002-12-13 Astrazeneca Ab Novel compounds
US7109243B2 (en) 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
US7384970B2 (en) 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7662849B2 (en) 2003-06-04 2010-02-16 Virobay, Inc. Amidino compounds as cysteine protease inhibitors
US7173051B2 (en) 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
CN100393700C (zh) * 2003-06-30 2008-06-11 麦克弗罗斯特(加拿大)公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
WO2005012269A1 (ja) 2003-08-05 2005-02-10 Ajinomoto Co., Inc. 新規アゾール化合物
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
AU2004266740B2 (en) * 2003-08-21 2010-08-26 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
CN1842515A (zh) * 2003-08-27 2006-10-04 默克弗罗斯特加拿大有限公司 组织蛋白酶抑制剂
BRPI0410979A (pt) 2003-09-18 2006-07-04 Axys Pharm Inc composto, composição farmacêutica, e, métodos para tratar uma doença em um animal mediada pela catepsina s e para tratar um paciente submetido a uma terapia
US20050065178A1 (en) * 2003-09-19 2005-03-24 Anwer Basha Substituted diazabicycloakane derivatives
US7399765B2 (en) 2003-09-19 2008-07-15 Abbott Laboratories Substituted diazabicycloalkane derivatives
BRPI0415826A (pt) 2003-10-24 2007-01-02 Aventis Pharmaceuticals Holdin derivados de ceto-oxadiazol como inibidores de catepsina
AU2004296905A1 (en) * 2003-12-12 2005-06-23 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
US20070259951A1 (en) * 2003-12-19 2007-11-08 Smithkline Beecham Corporation Compounds, Compositions and Methods
US7449481B2 (en) 2004-04-13 2008-11-11 Cephalon, Inc. Thio-substituted biaryl-methanesulfinyl derivatives
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
EP1819667B1 (de) 2004-12-02 2012-10-17 ViroBay, Inc. Sulfonamidverbindungen als cysteinprotease-inhibitoren
JP5086524B2 (ja) 2005-01-13 2012-11-28 ルネサスエレクトロニクス株式会社 コントローラ・ドライバ及びそれを用いた液晶表示装置
JP4743837B2 (ja) 2005-01-13 2011-08-10 ルネサスエレクトロニクス株式会社 コントローラ・ドライバ及びそれを用いる液晶表示装置並びに液晶駆動方法
EP1865940B1 (de) 2005-03-21 2013-02-13 Virobay, Inc. Alpha-ketoamid-verbindungen als cysteinproteasehemmer
MX2007011739A (es) 2005-03-22 2008-03-14 Celera Genomics Compuestos que contienen sulfonilo como inhibidores de cisteina proteasa.
CA2616677A1 (en) 2005-07-27 2007-02-08 F. Hoffmann-La Roche Ag Cathepsin k inhibitors
DK1976828T3 (en) 2005-12-29 2017-03-06 Celtaxsys Inc DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
MX2009003563A (es) 2006-10-04 2009-04-15 Virobay Inc Compuestos que contienen di-fluoro como inhibidores de proteasa de cisteina.
EP1939181A1 (de) * 2006-12-27 2008-07-02 sanofi-aventis Heteroaryl-substituierte Carboxamide und deren Verwendung für die Stimulierung der NO Synthase Expression
AU2008216906A1 (en) * 2007-02-14 2008-08-21 Karolinska Innovations Ab Compositions for increasing body weight, use and methods
WO2009001129A1 (en) * 2007-06-26 2008-12-31 Astrazeneca Ab 1-cyanocyclopropyl-derivatives as cathepsin k inhibitors
US8354446B2 (en) 2007-12-21 2013-01-15 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (SARMs) and uses thereof
JP5185697B2 (ja) 2008-05-28 2013-04-17 ルネサスエレクトロニクス株式会社 表示装置、表示パネルドライバ、表示パネルの駆動方法、及び表示パネルドライバへの画像データ供給方法
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
BR112013003631B1 (pt) 2010-08-18 2021-10-13 Samumed, Llc Beta- e gama-dicetonas e gama-hidroxicetonas e composições farmacêuticas que as compreendem
US8999975B2 (en) * 2011-09-19 2015-04-07 Boehringer Ingelheim International Gmbh Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
KR102252567B1 (ko) 2013-02-22 2021-05-17 사뮤메드, 엘엘씨 Wnt/베타-카테닌 신호전달 경로 활성자로서 감마-디케톤
CA2905340C (en) 2013-03-12 2022-05-31 Celtaxsys, Inc. Low dose oral formulations of acebilustat
JP6441830B2 (ja) * 2013-03-14 2018-12-19 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 カテプシンｃの置換２−アザ−ビシクロ［２．２．１］ヘプタン−３−カルボン酸（シアノ−メチル）−アミド阻害剤
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
JP6441831B2 (ja) 2013-03-14 2018-12-19 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 カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤
AU2014240042C1 (en) 2013-03-14 2019-09-05 Celltaxis, Llc Inhibitors of leukotriene A4 hydrolase
WO2014152518A2 (en) 2013-03-14 2014-09-25 Celtaxsys, Inc. Inhibitors of leukotriene a4 hydrolase
WO2014140081A1 (en) 2013-03-14 2014-09-18 Boehringer Ingelheim International Gmbh Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c
WO2014152536A2 (en) 2013-03-14 2014-09-25 Celtaxsys, Inc. Inhibitors of leukotriene a4 hydrolase
WO2015054089A1 (en) * 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015108988A2 (en) 2014-01-17 2015-07-23 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
WO2016016242A1 (en) 2014-08-01 2016-02-04 Boehringer Ingelheim International Gmbh Substituted oxetanes and their use as inhibitors of cathepsin c
WO2016029021A1 (en) 2014-08-20 2016-02-25 Samumed, Llc Gamma-diketones for treatment and prevention of aging skin and wrinkles
LT3191487T (lt) 2014-09-12 2019-10-10 Boehringer Ingelheim International Gmbh Katepsino c spirocikliniai inhibitoriai
US10464896B2 (en) 2015-06-11 2019-11-05 Basilea Pharmaceutica International AG Efflux-pump inhibitors and therapeutic uses thereof
US10494364B2 (en) 2015-08-29 2019-12-03 Sunshin Lake Pharma Co., Ltd Cathepsin K inhibitors and application thereof
MX2019014042A (es) * 2017-05-23 2020-02-05 Lundbeck La Jolla Research Center Inc Inhibidores pirazolicos de magl.
EP3801559A4 (de) 2018-05-31 2022-03-02 Celltaxis, LLC Verfahren zur minderung von lungenexazerbationen bei patienten mit atemwegserkrankungen
UY39276A (es) 2020-06-19 2022-01-31 Bayer Ag Uso de compuestos de 1,3,4–oxadiazol–2–ilpirimidina para controlar microorganismos fitopatógenos, métodos de uso y composiciones.
CN115466225A (zh) * 2022-08-16 2022-12-13 中国科学院上海药物研究所 一种酰胺类化合物及其制备方法、药物组合物和用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE629580A (de) * 1961-03-16
CN1273444C (zh) 1997-11-05 2006-09-06 诺瓦提斯公司 二肽腈
JP2002537294A (ja) 1999-02-20 2002-11-05 アストラゼネカ アクチボラグ カテプシンｌ及びカテプシンｓの阻害剤としてのジ−及びトリペプチドニトリル誘導体
WO2000049007A1 (en) 1999-02-20 2000-08-24 Astrazeneca Ab Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsin s
US6395897B1 (en) * 1999-03-02 2002-05-28 Boehringer Ingelheim Pharmaceuticals, Inc. Nitrile compounds useful as reversible inhibitors of #9 cathepsin 5
US6849605B1 (en) * 1999-03-05 2005-02-01 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
YU66101A (sh) 1999-03-15 2004-07-15 Axys Pharmaceuticals Inc. Nova jedinjenja i kompozicije kao inhibitori proteaze
KR20020005665A (ko) * 1999-04-09 2002-01-17 추후보정 카스파제 저해제 및 그것의 용도
US6617426B1 (en) * 1999-06-22 2003-09-09 Merck & Co Inc Cysteinyl protease inhibitors
US20010041700A1 (en) * 1999-07-30 2001-11-15 Younes Bekkali Novel succinate derivative compounds useful as cysteine protease inhibitors
GB9917909D0 (en) * 1999-07-31 1999-09-29 Synphar Lab Inc Cysteine protease inhibitors
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
WO2001068645A2 (en) 2000-03-15 2001-09-20 Axys Pharmaceuticals, Inc. N-cyanomethylcarboxamides and their use as protease inhibitors
AU2001256981A1 (en) * 2000-04-06 2001-10-23 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
ATE304526T1 (de) 2000-05-15 2005-09-15 Novartis Pharma Gmbh N-substituierte peptidylnitrile als cystein- cathepsin-inhibitoren
US6462076B2 (en) * 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
US6878706B1 (en) * 2002-04-05 2005-04-12 Boehringer Ingelheim Pharmaceuticals Inc. Cyanamides useful as reversible inhibitors of cysteine proteases

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