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AR001787A1 - Un compuesto oxazolidin sustituido particularmenteutil como inhibidor de calpaina y/o catepsina b e n el tratamiento de trastornos neurodegenerativos agudos o cronicos y composiciones farmacéuticas que incluyen dicho compuesto - Google Patents

Un compuesto oxazolidin sustituido particularmenteutil como inhibidor de calpaina y/o catepsina b e n el tratamiento de trastornos neurodegenerativos agudos o cronicos y composiciones farmacéuticas que incluyen dicho compuesto

Info

Publication number
AR001787A1
AR001787A1 AR33495896A AR33495896A AR001787A1 AR 001787 A1 AR001787 A1 AR 001787A1 AR 33495896 A AR33495896 A AR 33495896A AR 33495896 A AR33495896 A AR 33495896A AR 001787 A1 AR001787 A1 AR 001787A1
Authority
AR
Argentina
Prior art keywords
compound
pharmaceutical compositions
compositions including
calpain
acute
Prior art date
Application number
AR33495896A
Other languages
English (en)
Inventor
Norton P Peet
Shujaath Mehdi
Matthew D Linnik
Michael R Angelastro
Hwa-Ok Kim
Original Assignee
Hoecht Marion Roussell 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 Hoecht Marion Roussell Inc filed Critical Hoecht Marion Roussell Inc
Publication of AR001787A1 publication Critical patent/AR001787A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los compuestos poseen la fórmula general (I), donde R y Q son cada uno independientemente hidrógeno, OH, alquilo C1-C4, alcoxi C1-C4, NO2, NH2 ohalógeno; R1 y R2 son cada uno independientemente alquilo C1-C4; R3 es hidrógeno, alcanoiloC1-C8 (II); R4 y R5 son cada uno independientementehidrógeno, alquilo C1-C4 o bencilo; R6 es T-butiloxicarbonilo, carbobenciloxi o (III); donde Z es N o CH y B es un grupo de fórmulas (IV), donde R eshidrógeno o un grupo alquilo C1-C6; R7 es hidrógeno o metilo; R8 es alquilo C1-C4; m es el entero cero o uno; n es el entero cero o uno; p es el enterocero a tres; y q es el entero cero a tres; y las sales farmacéuticamente aceptables del mismo. También se describen composiciones farmacéuticas queincluyen dichos compuestos y un vehículo farmacéuticamente aceptable.
AR33495896A 1995-01-11 1996-01-09 Un compuesto oxazolidin sustituido particularmenteutil como inhibidor de calpaina y/o catepsina b e n el tratamiento de trastornos neurodegenerativos agudos o cronicos y composiciones farmacéuticas que incluyen dicho compuesto AR001787A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37119295A 1995-01-11 1995-01-11

Publications (1)

Publication Number Publication Date
AR001787A1 true AR001787A1 (es) 1997-12-10

Family

ID=23462894

Family Applications (1)

Application Number Title Priority Date Filing Date
AR33495896A AR001787A1 (es) 1995-01-11 1996-01-09 Un compuesto oxazolidin sustituido particularmenteutil como inhibidor de calpaina y/o catepsina b e n el tratamiento de trastornos neurodegenerativos agudos o cronicos y composiciones farmacéuticas que incluyen dicho compuesto

Country Status (23)

Country Link
US (1) US5691368A (es)
EP (1) EP0802909B1 (es)
JP (1) JP4157601B2 (es)
KR (1) KR100393701B1 (es)
CN (1) CN1088456C (es)
AR (1) AR001787A1 (es)
AT (1) ATE206413T1 (es)
AU (1) AU692044B2 (es)
CA (1) CA2210258C (es)
DE (1) DE69523072T2 (es)
DK (1) DK0802909T3 (es)
ES (1) ES2165441T3 (es)
FI (1) FI972935L (es)
HU (1) HUT77649A (es)
IL (1) IL116724A (es)
MX (1) MX9705235A (es)
NO (1) NO309267B1 (es)
NZ (1) NZ298999A (es)
PT (1) PT802909E (es)
SI (1) SI0802909T1 (es)
TW (1) TW454001B (es)
WO (1) WO1996021655A2 (es)
ZA (1) ZA96100B (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1270882B (it) * 1993-10-05 1997-05-13 Isagro Srl Oligopeptidi ad attivita' fungicida
US5925633A (en) * 1996-03-06 1999-07-20 Synphar Laboraties, Inc. 3-Substituted-4-oxa-1-azabicyclo 3,2,0!heptan-7-one as cysteine protease inhibitors
AU6134498A (en) * 1997-03-07 1998-09-22 Hoechst Marion Roussel, Inc. Method of treating trauma associated with brain, spinal cord or peripheral nerveinjury using carbobenzyloxy n-protected di- and tripeptide phenylalaninals
WO2000021550A2 (en) * 1998-10-13 2000-04-20 President And Fellows Of Harvard College Methods and compositions for treating neurodegenerative diseases
JP2002529422A (ja) * 1998-11-12 2002-09-10 リサーチ コーポレイション テクノロジーズ，インコーポレイテッド 虚血により傷害を受けた組織の処置法
EP1159273A1 (en) * 1999-03-02 2001-12-05 Boehringer Ingelheim Pharmaceuticals Inc. Compounds useful as reversible inhibitors of cathepsin s
EP1516877A1 (en) * 1999-03-15 2005-03-23 Axys Pharmaceuticals, Inc. Amine derivatives as protease inhibitors
JP2002539190A (ja) 1999-03-15 2002-11-19 アクシス・ファーマシューティカルズ・インコーポレイテッド プロテアーゼ阻害剤としての新規化合物および組成物
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
NZ518420A (en) 1999-11-05 2004-02-27 Sod Conseils Rech Applic Heterocyclic compounds having an inhibitory activity on calpains or a trapping activity on reactive oxygen species (ROS's) and their use as medicines
FR2800737B1 (fr) * 1999-11-05 2006-06-30 Sod Conseils Rech Applic Nouveaux composes heterocycliques et leur application a titre de medicaments
EP1315971A2 (en) * 2000-07-31 2003-06-04 The Regents of The University of California Model for alzheimer's disease and other neurodegenerative diseases
US7064123B1 (en) 2000-12-22 2006-06-20 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
KR20040044920A (ko) 2001-09-14 2004-05-31 아벤티스 파마슈티칼스 인크. 카뎁신 억제제로서 신규한 화합물 및 조성물
JP2005514353A (ja) 2001-11-14 2005-05-19 アベンティス・ファーマスーティカルズ・インコーポレイテツド カテプシンｓ阻害剤としてのオリゴペプチドおよびそれらを含有する組成物
WO2004084830A2 (en) * 2003-03-21 2004-10-07 Buck Institute Method for treating alzheimer’s dementia
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7109243B2 (en) * 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
WO2004089395A2 (en) * 2003-04-01 2004-10-21 Aventis Pharmaceuticals Inc. Use of an inhibitor of cathepsin-s or -b to treat or prevent chronic obstructive pulmonary disease
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
US7173051B2 (en) * 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7256207B2 (en) * 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
FR2863268B1 (fr) * 2003-12-09 2006-02-24 Sod Conseils Rech Applic Nouveaux derives du 2-hydroxytetrahydrofuranne et leur application a titre de medicaments
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
WO2010003092A1 (en) * 2008-07-03 2010-01-07 University Of Massachusetts Methods and compositions for reducing inflammation and treating inflammatory disorders
CA2772488C (en) 2009-09-11 2018-04-17 Probiodrug Ag Heterocyclic derivatives as inhibitors of glutaminyl cyclase
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
WO2024018245A1 (en) 2022-07-22 2024-01-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of calpain inhibitors for the treatment of the diabetic kidney disease
WO2024153744A1 (en) 2023-01-20 2024-07-25 Institut National de la Santé et de la Recherche Médicale Autophagy activators for the treatment of rhabdomyolysis
WO2025153685A1 (en) * 2024-01-18 2025-07-24 Firmenich Sa 3-acyl-oxazolidin-5-one properfumes

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3867364A (en) * 1968-11-21 1975-02-18 Microbial Chem Res Found Process for the synthesis of leupeptins and their analogues
US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
US4277395A (en) * 1980-06-16 1981-07-07 Richardson-Merrell Inc. Novel enzyme inhibitors
JPS5754157A (en) * 1980-09-19 1982-03-31 Nippon Kayaku Co Ltd L-argininal derivative and its preparation
US4535167A (en) * 1981-12-14 1985-08-13 Merck & Co. Inc. Chiral, N-protected, N-substituted α-amino acids
GB2124233B (en) * 1982-07-19 1985-09-18 Nat Res Dev Synthetic peptides and their preparation
US4845079A (en) * 1985-01-23 1989-07-04 Luly Jay R Peptidylaminodiols
US5214129A (en) * 1985-01-23 1993-05-25 Abbott Laboratories Peptidylaminodiols
US5091575A (en) * 1985-01-23 1992-02-25 Abbott Laboratories Peptidylaminodiols
US5496927A (en) * 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
JPH079705B2 (ja) * 1986-05-28 1995-02-01 オリンパス光学工業株式会社 光カ−ド用デ−タ記録再生装置
US4851387A (en) * 1986-10-14 1989-07-25 Banyu Pharmaceutical Co., Ltd. 5-substituted amino-4-hydroxy-pentanoic acid derivatives and their use
US5032577A (en) * 1986-12-31 1991-07-16 Abbott Laboratories Peptidylaminodiols
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
US4820691A (en) * 1987-06-24 1989-04-11 E. R. Squibb & Sons, Inc. Amino acid 1,2-diketo derivatives as renin inhibitors
EP0313847A3 (en) * 1987-10-01 1989-11-29 G.D. Searle & Co. Non-peptidyl alpha-succinamidoacyl aminodiols as anti-hypertensive agents
WO1989007109A1 (en) * 1988-02-01 1989-08-10 The Upjohn Company Renin inhibiting peptides with polar end groups
JPH03505875A (ja) * 1988-07-08 1991-12-19 スミスクライン・ベックマン・コーポレイション レトロウイルス・プロテアーゼ結合ペプチド
ZA897514B (en) * 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
US4990525A (en) * 1988-12-22 1991-02-05 Rohm And Haas Company Synergistic microbicidal combinations containing 3-isothiazolone and commerical biocides
US5510531A (en) * 1989-04-10 1996-04-23 Suntory Limited Proteinase inhibitor
JP2701932B2 (ja) * 1989-04-10 1998-01-21 サントリー株式会社 タンパク質分解酵素阻害剤
CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
HU9203505D0 (en) * 1990-06-01 1993-01-28 Du Pont Merck Pharma 1,4-diamino-2,3-dihydroxi-butane compounds
DE4037437A1 (de) * 1990-11-24 1992-05-27 Hoechst Ag Aminodiol-derivate
CA2098609A1 (en) * 1990-12-28 1992-06-29 Raymond T. Bartus Use of calpain inhibitors in the inhibition and treatment of neurodegeneration
JPH06504547A (ja) * 1990-12-28 1994-05-26 ジョージア・テック・リサーチ・コーポレーション ペプチドケトアミド、ケト酸およびケトエステル
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
AU655831B2 (en) * 1991-08-22 1995-01-12 Merrell Pharmaceuticals Inc. Novel orally-active elastase inhibitors
EP0580161A1 (en) * 1992-07-22 1994-01-26 THE McLEAN HOSPITAL CORPORATION Prophylactic and therapeutic treatment of Alzheimer's disease
DE69321087T2 (de) * 1992-12-25 1999-05-20 Mitsubishi Chemical Corp., Tokio/Tokyo Alpha-aminoketon Derivate
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
ATE211129T1 (de) * 1993-10-01 2002-01-15 Merrell Pharma Inc Inhibitoren von beta-amyloid-protein-herstellung

Also Published As

Publication number Publication date
AU692044B2 (en) 1998-05-28
US5691368A (en) 1997-11-25
NO973216D0 (no) 1997-07-10
ZA96100B (en) 1996-07-24
CA2210258C (en) 2002-10-01
WO1996021655A3 (en) 1996-09-06
PT802909E (pt) 2002-03-28
DK0802909T3 (da) 2002-01-28
DE69523072T2 (de) 2002-06-20
NZ298999A (en) 1999-01-28
MX9705235A (es) 1997-10-31
IL116724A (en) 2000-08-31
JP4157601B2 (ja) 2008-10-01
AU4473196A (en) 1996-07-31
JPH10512257A (ja) 1998-11-24
SI0802909T1 (en) 2002-02-28
NO973216L (no) 1997-09-09
NO309267B1 (no) 2001-01-08
KR100393701B1 (ko) 2003-11-28
ES2165441T3 (es) 2002-03-16
WO1996021655A2 (en) 1996-07-18
EP0802909A2 (en) 1997-10-29
CN1173174A (zh) 1998-02-11
TW454001B (en) 2001-09-11
ATE206413T1 (de) 2001-10-15
IL116724A0 (en) 1996-05-14
FI972935A0 (fi) 1997-07-10
CA2210258A1 (en) 1996-07-18
FI972935A7 (fi) 1997-07-10
DE69523072D1 (en) 2001-11-08
HUT77649A (hu) 1998-07-28
FI972935L (fi) 1997-07-10
EP0802909B1 (en) 2001-10-04
CN1088456C (zh) 2002-07-31

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