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WO1996016079A3 - Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l - Google Patents

Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l Download PDF

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Publication number
WO1996016079A3
WO1996016079A3 PCT/JP1995/002389 JP9502389W WO9616079A3 WO 1996016079 A3 WO1996016079 A3 WO 1996016079A3 JP 9502389 W JP9502389 W JP 9502389W WO 9616079 A3 WO9616079 A3 WO 9616079A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
cathepsin
inhibitor
group
alpha
Prior art date
Application number
PCT/JP1995/002389
Other languages
English (en)
Other versions
WO1996016079A2 (fr
Inventor
Takashi Sohda
Yukio Fujisawa
Tsuneo Yasuma
Junji Mizoguchi
Original Assignee
Takeda Chemical Industries Ltd
Takashi Sohda
Yukio Fujisawa
Tsuneo Yasuma
Junji Mizoguchi
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 Takeda Chemical Industries Ltd, Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi filed Critical Takeda Chemical Industries Ltd
Priority to AU39358/95A priority Critical patent/AU3935895A/en
Priority to EP95937173A priority patent/EP0793673A1/fr
Priority to CA002200964A priority patent/CA2200964A1/fr
Publication of WO1996016079A2 publication Critical patent/WO1996016079A2/fr
Publication of WO1996016079A3 publication Critical patent/WO1996016079A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07C237/22—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 having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Inhibiteur de cathepsine L qui comporte un composé de formule générale (Ia) dans laquelle Q représente une liaison directe ou 1 ou 2 restes d'acides aminé qui peuvent être substitutés; R1 représente un atome d'hydrogène ou un groupe hydrocarbure ou un groupe hétérocyclique qui peut être substitué; R4 représente un groupe acyle ou un groupe carboxyle qui peut être estérifié et R5 et R6 représentent indépendamment un atome d'hydrogène ou un groupe hydrocarbure ou un groupe hétérocyclique qui peut être substitué ou R5 et R6 peuvent se lier pour former un cycle; ou sel dudit inhibiteur, qui présente une forte activité de suppression de la résorption osseuse et est utile pour prévenir ou traiter l'ostéoporose.
PCT/JP1995/002389 1994-11-24 1995-11-24 Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l WO1996016079A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU39358/95A AU3935895A (en) 1994-11-24 1995-11-24 Alpha-ketoamide derivatives as cathepsin l inhibitor
EP95937173A EP0793673A1 (fr) 1994-11-24 1995-11-24 Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l
CA002200964A CA2200964A1 (fr) 1994-11-24 1995-11-24 Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP6/290132 1994-11-24
JP29013294 1994-11-24

Publications (2)

Publication Number Publication Date
WO1996016079A2 WO1996016079A2 (fr) 1996-05-30
WO1996016079A3 true WO1996016079A3 (fr) 1996-09-12

Family

ID=17752214

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1995/002389 WO1996016079A2 (fr) 1994-11-24 1995-11-24 Derives d'alpha-cetoamide utilises comme inhibiteurs de cathepsine l

Country Status (4)

Country Link
EP (1) EP0793673A1 (fr)
AU (1) AU3935895A (fr)
CA (1) CA2200964A1 (fr)
WO (1) WO1996016079A2 (fr)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997046514A1 (fr) * 1996-05-31 1997-12-11 Novartis Ag Procede de preparation de derives hydrazine utiles en tant qu'intermediaires dans la preparation d'analogues peptidiques
US6150378A (en) * 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
US6774212B2 (en) * 1999-12-03 2004-08-10 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
US6703513B1 (en) * 2000-06-02 2004-03-09 K-Quay Enterprises Llc Production and use of derivatized homoserine lactones
WO2002002546A1 (fr) 2000-06-30 2002-01-10 Seikagaku Corporation Amides d'acide carboxylique, azides et amino-alcools et procedes de preparation de $g(a)-ceto amides a l'aide de ces derniers
EP1411933A1 (fr) * 2001-08-03 2004-04-28 SmithKline Beecham Corporation Derives d'alpha-cetoamide utilises en tant qu'inhibiteurs de la cathepsine k
JP2005515254A (ja) 2002-01-17 2005-05-26 スミスクライン ビーチャム コーポレーション カテプシンｋ阻害剤として有用なシクロアルキルケトアミド誘導体
US7402606B2 (en) 2002-04-10 2008-07-22 Smithkline Beecham Corporation Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
ES2332363T3 (es) 2002-07-22 2010-02-03 Senju Pharmaceutical Co., Ltd. Nuevos derivados de alfa-cetoamida y su uso.
EA019277B1 (ru) * 2008-12-19 2014-02-28 МЕДИВИР ЮКей ЛТД. Ингибиторы цистеинпротеазы
GB201001070D0 (en) 2010-01-22 2010-03-10 St George's Hospital Medical School Theraputic compounds and their use
EP2633855A1 (fr) 2012-03-01 2013-09-04 Veterinärmedizinische Universität Wien Inhibiteurs de la protéase pour le traitement d'infections par Trichomonas gallinae
CN105189478B (zh) 2013-01-07 2019-10-22 南加州大学 脱氧尿苷三磷酸酶抑制剂
US9765099B2 (en) 2013-05-08 2017-09-19 Board Of Regents, The University Of Texas System STAT6 inhibitors
WO2017006283A1 (fr) 2015-07-08 2017-01-12 Cv6 Therapeutics (Ni) Limited Inhibiteurs de désoxyuridine triphosphatase contenant une liaison cyclopropano
DK3319939T3 (da) 2015-07-08 2025-02-24 Cv6 Therapeutics Ni Ltd Hydantoin indeholdende deoxyuridintriphosphatase-inhibitorer
WO2017006271A1 (fr) 2015-07-08 2017-01-12 University Of Southern California Inhibiteurs de désoxyuridine triphosphatase contenant une liaison sulfonyle aminée
WO2017006270A1 (fr) 2015-07-08 2017-01-12 University Of Southern California Inhibiteurs de la désoxyuridine triphosphatase
CN116731101A (zh) 2016-06-01 2023-09-12 雅斯娜 用于治疗多种疾病的n-己酸-l-酪氨酸-l-异亮氨酸-(6)-氨基己酰胺的衍生物
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
US11377439B2 (en) 2016-06-21 2022-07-05 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
US11168059B2 (en) 2016-11-23 2021-11-09 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
WO2018098207A1 (fr) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Hydantoïne contenant des inhibiteurs de la désoxyuridine triphosphatase
US11174271B2 (en) 2016-11-23 2021-11-16 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
US10858344B2 (en) 2016-11-23 2020-12-08 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2018098208A1 (fr) * 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Inhibiteurs de désoxyuridine triphosphatase liés à un cycle azote
US11247984B2 (en) 2017-01-05 2022-02-15 Cv6 Therapeutics (Ni) Limited Uracil containing compounds

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0468339A2 (fr) * 1990-07-27 1992-01-29 Nippon Kayaku Kabushiki Kaisha Dérivés d'amide-alpha-céto ayant une activité inhibante de protéases
WO1992012140A1 (fr) * 1990-12-28 1992-07-23 Georgia Tech Research Corporation Cetoamides, cetoacides et cetoesters peptidiques
WO1992011850A2 (fr) * 1990-12-28 1992-07-23 Cortex Pharmaceuticals, Inc. Utilisation d'inhibiteurs de la calpaine dans l'inhibition et le traitement de la neurodegenerescence
WO1994000095A2 (fr) * 1992-06-24 1994-01-06 Cortex Pharmaceuticals, Inc. Emploi d'inhibiteurs de calpaine dans l'inhibition et le traitement d'etats medicaux associes a une activite de calpaine accrue
WO1994008941A1 (fr) * 1992-10-16 1994-04-28 Corvas International, Inc. Ceto-amide d'arginine comme inhibiteurs enzymatiques
EP0603769A1 (fr) * 1992-12-25 1994-06-29 Mitsubishi Chemical Corporation Dérivés d'alpha-aminocétones

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0468339A2 (fr) * 1990-07-27 1992-01-29 Nippon Kayaku Kabushiki Kaisha Dérivés d'amide-alpha-céto ayant une activité inhibante de protéases
WO1992012140A1 (fr) * 1990-12-28 1992-07-23 Georgia Tech Research Corporation Cetoamides, cetoacides et cetoesters peptidiques
WO1992011850A2 (fr) * 1990-12-28 1992-07-23 Cortex Pharmaceuticals, Inc. Utilisation d'inhibiteurs de la calpaine dans l'inhibition et le traitement de la neurodegenerescence
WO1994000095A2 (fr) * 1992-06-24 1994-01-06 Cortex Pharmaceuticals, Inc. Emploi d'inhibiteurs de calpaine dans l'inhibition et le traitement d'etats medicaux associes a une activite de calpaine accrue
WO1994008941A1 (fr) * 1992-10-16 1994-04-28 Corvas International, Inc. Ceto-amide d'arginine comme inhibiteurs enzymatiques
EP0603769A1 (fr) * 1992-12-25 1994-06-29 Mitsubishi Chemical Corporation Dérivés d'alpha-aminocétones

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ESSER, R.E. ET AL.: "Cysteine proteinase inhibitors decrease articular cartilage and bone destruction in chronic inflammatory arthritis", ARTHRITIS & RHEUMATISM, vol. 37, no. 2, 1 February 1994 (1994-02-01), pages 236 - 247, XP000566128 *
LI, Z. ET AL.: "Peptide alpha-keto ester, alpha-keto amide, and alpha-keto acid inhibitors of calpains and other csyteine proteases", J. MED. CHEM., vol. 36, 1993, pages 3472 - 3480, XP000565670 *

Also Published As

Publication number Publication date
WO1996016079A2 (fr) 1996-05-30
AU3935895A (en) 1996-06-17
EP0793673A1 (fr) 1997-09-10
CA2200964A1 (fr) 1996-05-30

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