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WO2006058720A3 - Novel compounds for the treatment of neurological disorders - Google Patents

Novel compounds for the treatment of neurological disorders Download PDF

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Publication number
WO2006058720A3
WO2006058720A3 PCT/EP2005/012765 EP2005012765W WO2006058720A3 WO 2006058720 A3 WO2006058720 A3 WO 2006058720A3 EP 2005012765 W EP2005012765 W EP 2005012765W WO 2006058720 A3 WO2006058720 A3 WO 2006058720A3
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
novel compounds
neurological disorders
disease
compounds
Prior art date
Application number
PCT/EP2005/012765
Other languages
French (fr)
Other versions
WO2006058720A2 (en
Inventor
Andre Johannes Niestroj
Ulrich Heiser
Ingo Schulz
Jens-Ulrich Rahfeld
Joachim Baer
Hans-Ulrich Demuth
Original Assignee
Probiodrug Ag
Andre Johannes Niestroj
Ulrich Heiser
Ingo Schulz
Jens-Ulrich Rahfeld
Joachim Baer
Hans-Ulrich Demuth
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
Priority claimed from US10/976,677 external-priority patent/US20050137142A1/en
Priority claimed from US11/002,169 external-priority patent/US20050171112A1/en
Application filed by Probiodrug Ag, Andre Johannes Niestroj, Ulrich Heiser, Ingo Schulz, Jens-Ulrich Rahfeld, Joachim Baer, Hans-Ulrich Demuth filed Critical Probiodrug Ag
Priority to JP2007543765A priority Critical patent/JP2008521853A/en
Priority to EP05826439A priority patent/EP1824846A2/en
Publication of WO2006058720A2 publication Critical patent/WO2006058720A2/en
Publication of WO2006058720A3 publication Critical patent/WO2006058720A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to novel inhibitors of prolyl endopeptidase of formula (I): W-KCONH-X-CON-Y-CO-Z, wherein K, W; X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer’s disease. Down Syndrome, Parkinson disease and Chorea Huntington.
PCT/EP2005/012765 2003-11-03 2005-11-30 Novel compounds for the treatment of neurological disorders WO2006058720A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2007543765A JP2008521853A (en) 2004-12-02 2005-11-30 Novel compounds for the treatment of neurological diseases
EP05826439A EP1824846A2 (en) 2003-11-03 2005-11-30 Novel compounds for the treatment of neurological disorders

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US51671703P 2003-11-03 2003-11-03
US10/976,677 US20050137142A1 (en) 2003-11-03 2004-10-29 Combinations useful for the treatment of neuronal disorders
US11/002,169 US20050171112A1 (en) 2003-11-03 2004-12-02 Combinations useful for the treatment of neuronal disorders
US11/002,169 2004-12-02
US68413705P 2005-05-24 2005-05-24
US60/684,137 2005-05-24

Publications (2)

Publication Number Publication Date
WO2006058720A2 WO2006058720A2 (en) 2006-06-08
WO2006058720A3 true WO2006058720A3 (en) 2006-07-27

Family

ID=38331139

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2005/012765 WO2006058720A2 (en) 2003-11-03 2005-11-30 Novel compounds for the treatment of neurological disorders

Country Status (2)

Country Link
EP (1) EP1824846A2 (en)
WO (1) WO2006058720A2 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE554085T1 (en) 2006-11-30 2012-05-15 Probiodrug Ag NEW INHIBITORS OF GLUTAMINYL CYCLASE
EP2117540A1 (en) 2007-03-01 2009-11-18 Probiodrug AG New use of glutaminyl cyclase inhibitors
DK2142514T3 (en) 2007-04-18 2015-03-23 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
ES2586231T3 (en) 2010-03-03 2016-10-13 Probiodrug Ag Glutaminyl cyclase inhibitors
EA022420B1 (en) 2010-03-10 2015-12-30 Пробиодруг Аг Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP5945532B2 (en) 2010-04-21 2016-07-05 プロビオドルグ エージー Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
DK3461819T3 (en) 2017-09-29 2020-08-10 Probiodrug Ag GLUTAMINYL CYCLASE INHIBITORS

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0154353A2 (en) * 1984-03-09 1985-09-11 Kabushiki Kaisha Yakult Honsha An anti-amnestic agent
EP0201741A2 (en) * 1985-04-16 1986-11-20 Suntory Limited Dipeptide derivatives, processes for preparing them, pharmaceutical composition and use
US5547978A (en) * 1993-01-15 1996-08-20 Meiji Seika Kaisha, Ltd. Derivatives of pyrrolidin-2-ylcarbonylheterocyclic compounds
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005075436A2 (en) * 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
WO2005103043A1 (en) * 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer’s disease

Family Cites Families (14)

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Publication number Priority date Publication date Assignee Title
JPS6137764A (en) 1984-07-31 1986-02-22 Suntory Ltd Novel physiologically active compound having anti-prolyl-endopeptidase activity
EP0268190B1 (en) 1986-11-20 1993-06-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives
CA1339423C (en) 1988-09-14 1997-09-02 Yuji Ono Pyridine compounds and pharmaceutical use thereof
JP2511605B2 (en) 1990-06-04 1996-07-03 ファイザー・インコーポレーテッド Aromatic pyrrolidine and thiazolidinamides
US5536737A (en) 1992-11-20 1996-07-16 Japan Tobacco Inc. Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof
EP0709373B1 (en) 1993-07-23 2001-10-17 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Pyrrolidine derivative
KR100341982B1 (en) 1993-12-02 2002-11-30 메렐 파마슈티칼스 인크. Prolyl Endopeptidase Inhibitors
HUT76640A (en) 1995-08-17 1997-10-28 Chinoin Gyogyszer Es Vegyeszet Compounds of pharmaceutical activity cyclic amide derivatives, pharmaceutical compositions containing them, process for producing them and their use
US5763576A (en) 1995-10-06 1998-06-09 Georgia Tech Research Corp. Tetrapeptide α-ketoamides
HUP9700442A1 (en) 1997-02-14 1999-09-28 Chinoin Gyógyszer és Vegyészeti Termékek Gyára Rt. Cyclic amide derivatives, pharmaceutical compositions containing them, process for producing them and their use
DE19828114A1 (en) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs of unstable inhibitors of dipeptidyl peptidase IV
WO1999067228A1 (en) 1998-06-24 1999-12-29 Aventis Pharmaceuticals Products Inc. Fluorophenyl resin compounds
DE19828113A1 (en) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs of Dipeptidyl Peptidase IV Inhibitors
JP2003505008A (en) 1998-08-17 2003-02-12 コーテック インコーポレーテッド Serine protease inhibitors containing α-ketoheterocycles

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0154353A2 (en) * 1984-03-09 1985-09-11 Kabushiki Kaisha Yakult Honsha An anti-amnestic agent
EP0201741A2 (en) * 1985-04-16 1986-11-20 Suntory Limited Dipeptide derivatives, processes for preparing them, pharmaceutical composition and use
US5547978A (en) * 1993-01-15 1996-08-20 Meiji Seika Kaisha, Ltd. Derivatives of pyrrolidin-2-ylcarbonylheterocyclic compounds
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005075436A2 (en) * 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
WO2005103043A1 (en) * 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer’s disease

Non-Patent Citations (25)

* Cited by examiner, † Cited by third party
Title
BIOORG. MED. CHEM. LETT., vol. 10, no. 1, 2000, pages 45 - 48 *
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 22, 15 November 2004 (2004-11-15), pages 5579 - 5583, XP004598598 *
BR. J. PHARMACOL., vol. 117, no. 5, 1996, pages 986 - 992 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378930 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378931 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378932 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378933 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378934 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378935 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378936 *
DATABASE BEILSTEIN Beilstein Institut zur Förderung der Wissenschaften, Frankfurt/Main, DE; XP002378937 *
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DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; FERRARIS, D. ET AL.: "Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors", XP002378939, retrieved from STN Database accession no. 2004:863108 *
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JOYEAU, R. ET AL.: "Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, EDITIONS SCIENTIFIQUE ELSEVIER, PARIS, FR, vol. 35, no. 2, February 2000 (2000-02-01), pages 257 - 266, XP004330419, ISSN: 0223-5234 *
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TSUTSUMI, S. ET AL.: "alpha-Ketothiazole Inhibitors of Prolyl Endopeptidase", BIOORG. MED. CHEM. LETT., vol. 4, no. 6, 1994, pages 831 - 834, XP004229391 *
TSUTSUMI, S. ET AL.: "Prolyl Endopeptidase Inhibitors. II. A Peptidyl alpha-Keto Thiazole Derivative", ACTA CRYST., vol. C51, 1995, pages 1925 - 1927, XP009065454 *
TSUTSUMI, S. ET AL.: "Synthesis and Sructure-Activity Relationships of Peptidyl alpha-Keto Heterocycles as Novel Inhibitors of Prolyl Endopeptidase", J. MED. CHEM., vol. 37, no. 21, 1994, pages 3492 - 3502, XP002067396 *

Also Published As

Publication number Publication date
WO2006058720A2 (en) 2006-06-08
EP1824846A2 (en) 2007-08-29

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