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WO1999044596A3 - Glycine transport inhibitors - Google Patents

Glycine transport inhibitors Download PDF

Info

Publication number
WO1999044596A3
WO1999044596A3 PCT/EP1999/001309 EP9901309W WO9944596A3 WO 1999044596 A3 WO1999044596 A3 WO 1999044596A3 EP 9901309 W EP9901309 W EP 9901309W WO 9944596 A3 WO9944596 A3 WO 9944596A3
Authority
WO
WIPO (PCT)
Prior art keywords
glycine transport
preparation
transport inhibitors
epilepsy
piperazinyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP1999/001309
Other languages
French (fr)
Other versions
WO1999044596A2 (en
Inventor
Walter Herman Maria Lou Luyten
Frans Eduard Janssens
Ludo Edmond Josephine Kennis
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 to SK1308-2000A priority Critical patent/SK13082000A3/en
Priority to EEP200000482A priority patent/EE200000482A/en
Priority to PL99343435A priority patent/PL343435A1/en
Priority to CA002322164A priority patent/CA2322164A1/en
Priority to BR9907951-8A priority patent/BR9907951A/en
Priority to AU34089/99A priority patent/AU3408999A/en
Priority to HR20000523A priority patent/HRP20000523A2/en
Priority to HU0101048A priority patent/HUP0101048A2/en
Priority to IL13822899A priority patent/IL138228A0/en
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Priority to EP99915541A priority patent/EP1059922A2/en
Priority to JP2000534198A priority patent/JP2002505277A/en
Priority to KR1020007006315A priority patent/KR20010032968A/en
Publication of WO1999044596A2 publication Critical patent/WO1999044596A2/en
Publication of WO1999044596A3 publication Critical patent/WO1999044596A3/en
Priority to BG104685A priority patent/BG104685A/en
Priority to NO20004431A priority patent/NO20004431L/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The present invention is concerned with the use of glycine transport inhibiting [4,4-bis(4-fluorophenyl)butyl]-1-(piperazinyl and piperidinyl) derivatives for the preparation of medicaments for treating disorders of the central and peripheral nervous system, in particular psychoses, pain, epilepsy, neurodegenerative diseases (Alzheimer's disease), stroke, head trauma, multiple sclerosis and the like. The invention further comprises novel compounds, their preparation and their pharmaceutical forms.
PCT/EP1999/001309 1998-03-06 1999-02-26 Glycine transport inhibitors Ceased WO1999044596A2 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
IL13822899A IL138228A0 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
PL99343435A PL343435A1 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
EP99915541A EP1059922A2 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
BR9907951-8A BR9907951A (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
AU34089/99A AU3408999A (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
HR20000523A HRP20000523A2 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
HU0101048A HUP0101048A2 (en) 1998-03-06 1999-02-26 Glycine transport inhibiting [4,4-bis(4-fluorophenyl)butyl]-1-(piperazinyl and piperidinyl) derivatives and their therapeutic use
SK1308-2000A SK13082000A3 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
CA002322164A CA2322164A1 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
EEP200000482A EE200000482A (en) 1998-03-06 1999-02-26 Use of a Glycine Transfer Inhibitory Compound in the manufacture of a medicament, a compound, a composition comprising it, and a process for the preparation of the compound and
JP2000534198A JP2002505277A (en) 1998-03-06 1999-02-26 Glycine transport inhibitor
KR1020007006315A KR20010032968A (en) 1998-03-06 1999-02-26 Glycine transport inhibitors
BG104685A BG104685A (en) 1998-03-06 2000-08-11 Glycine transport inhibitors
NO20004431A NO20004431L (en) 1998-03-06 2000-09-05 Glysintransportinhibitorer

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP98200701.5 1998-03-06
EP98200701 1998-03-06

Publications (2)

Publication Number Publication Date
WO1999044596A2 WO1999044596A2 (en) 1999-09-10
WO1999044596A3 true WO1999044596A3 (en) 2000-02-17

Family

ID=8233444

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1999/001309 Ceased WO1999044596A2 (en) 1998-03-06 1999-02-26 Glycine transport inhibitors

Country Status (17)

Country Link
EP (1) EP1059922A2 (en)
JP (1) JP2002505277A (en)
KR (1) KR20010032968A (en)
CN (1) CN1292698A (en)
AU (1) AU3408999A (en)
BG (1) BG104685A (en)
BR (1) BR9907951A (en)
CA (1) CA2322164A1 (en)
EE (1) EE200000482A (en)
HR (1) HRP20000523A2 (en)
HU (1) HUP0101048A2 (en)
IL (1) IL138228A0 (en)
NO (1) NO20004431L (en)
PL (1) PL343435A1 (en)
SK (1) SK13082000A3 (en)
TR (1) TR200002567T2 (en)
WO (1) WO1999044596A2 (en)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60033859T2 (en) * 1999-06-28 2007-11-08 Janssen Pharmaceutica N.V. Inhibitor of respiratory syncytial virus
UA73749C2 (en) * 1999-11-01 2005-09-15 Diarylenines
CA2406652A1 (en) * 2000-04-20 2001-11-01 Nps Allelix Corp. Aminopiperidines for use as glyt-1 inhibitors
DE10040016A1 (en) * 2000-08-16 2002-02-28 Boehringer Ingelheim Pharma Novel beta-amyloid inhibitors, process for their preparation and their use as pharmaceuticals
CA2422198A1 (en) 2000-09-08 2002-03-14 Gliatech, Inc. Substituted hydrazine derivatives
EP1324986A1 (en) * 2000-09-14 2003-07-09 Gliatech, Inc. Nitrogen-containing compounds and their use as glycine transport inhibitors
AR032653A1 (en) 2001-02-09 2003-11-19 Telik Inc HYPERCYCLIC INHIBITORS OF THE GLICINE TRANSPORTER 2 PHARMACEUTICAL COMPOSITIONS, USE AND METHODS.
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
CN1874777B (en) * 2003-09-09 2012-07-04 弗·哈夫曼-拉罗切有限公司 1-(2-amino-benzoyl)-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
DK1703909T3 (en) * 2003-09-09 2009-06-22 Hoffmann La Roche 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
WO2005058885A2 (en) * 2003-12-18 2005-06-30 Glaxo Group Limited Piperidine derivatives and their use as glycine transporter inhibitors
TW200630337A (en) 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
HRP20090264T1 (en) * 2004-12-09 2009-06-30 F. Hoffmann - La Roche Ag FENIL-PIPERAZIN METANONA DERIVATIVES
BRPI0519054A2 (en) * 2004-12-15 2008-12-23 Hoffmann La Roche Substituted bicyclic and tricyclic phenyl methanones as glycine transporter (glyt-1) inhibitors for the treatment of alzheimer's disease
GB0428233D0 (en) * 2004-12-23 2005-01-26 Glaxo Group Ltd Compounds
PE20061156A1 (en) 2004-12-23 2006-12-16 Glaxo Group Ltd BENZAMIDE DERIVATIVES AS INHIBITING AGENTS OF THE GLYCINE TRANSPORTER
US7485637B2 (en) 2005-01-04 2009-02-03 Hoffmann-La Roche Inc. Benzoyl-tetrahydropiperidine derivatives
MX2007008190A (en) * 2005-01-06 2007-08-07 Hoffmann La Roche Sulfanyl substituted phenyl methanones as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders.
CA2593463C (en) * 2005-01-07 2013-10-08 F. Hoffmann-La Roche Ag [4-(heteroaryl) piperazin-1-yl]-(2,5-substituted -phenyl)methanone derivatives as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders
JP2008527016A (en) * 2005-01-18 2008-07-24 エフ．ホフマン−ラ ロシュ アーゲー 2,5-Disubstituted phenylmethanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric diseases
JP4829900B2 (en) 2005-01-26 2011-12-07 エフ．ホフマン−ラ ロシュ アーゲー Phenylmethanone derivatives and their use as glycine transporter 1 inhibitors
RS51204B (en) 2005-02-07 2010-12-31 F. Hoffmann-La Roche Ag. HETEROCYCLIC SUBSTITUTED PHENYL METHANONS AS GLICIN TRANSPORTER INHIBITORS 1
CN100341871C (en) * 2005-06-03 2007-10-10 复旦大学 Organic sulfur compound containing piperidine structure, its preparation and use
WO2007110449A1 (en) 2006-03-29 2007-10-04 Euro-Celtique S.A. Benzenesulfonamide compounds and their use
WO2007118853A1 (en) 2006-04-13 2007-10-25 Euro-Celtique S.A. Benzenesulfonamide compounds and their use as blockers of calcium channels
WO2007118854A1 (en) 2006-04-13 2007-10-25 Euro-Celtique S.A. Benzenesulfonamide compounds and the use thereof
CA2666750C (en) * 2006-11-01 2014-02-04 Purdue Pharma L.P. Phenylpropionamide compounds and the use thereof
FR2910321B1 (en) 2006-12-21 2009-07-10 Galderma Res & Dev S N C Snc CREAM GEL COMPRISING AT LEAST ONE RETINOID AND BENZOLE PEROXIDE
FR2910320B1 (en) * 2006-12-21 2009-02-13 Galderma Res & Dev S N C Snc EMULSION COMPRISING AT LEAST ONE RETINOID AND BENZOLE PEROXIDE
US8399486B2 (en) 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
WO2009040659A2 (en) 2007-09-28 2009-04-02 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
AU2008335788B2 (en) * 2007-12-12 2012-11-29 Amgen Inc. Glycine transporter-1 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0005318A1 (en) * 1978-04-03 1979-11-14 Janssen Pharmaceutica N.V. N-Heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates
US4219559A (en) * 1979-01-10 1980-08-26 Janssen Pharmaceutica N.V. N-Heterocyclyl-4-piperidinamines
EP0151826A1 (en) * 1984-01-09 1985-08-21 Janssen Pharmaceutica N.V. 4-[(Bicyclic heterocyclyl)-methyl and -hetero]-piperidines
US4695575A (en) * 1984-11-13 1987-09-22 Janssen Pharmaceutica, N.V. 4-[(bicycle heterocyclyl)-methyl and -hetero]-piperidines
WO1999025353A1 (en) * 1997-11-13 1999-05-27 Merck Sharp & Dohme Limited Therapeutic uses of triazolo-pyridazine derivatives

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0005318A1 (en) * 1978-04-03 1979-11-14 Janssen Pharmaceutica N.V. N-Heterocyclyl-4-piperidinamines, methods for their preparation, pharmaceutical compositions comprising them, intermediates therefor, and method for the preparation of the intermediates
US4219559A (en) * 1979-01-10 1980-08-26 Janssen Pharmaceutica N.V. N-Heterocyclyl-4-piperidinamines
EP0151826A1 (en) * 1984-01-09 1985-08-21 Janssen Pharmaceutica N.V. 4-[(Bicyclic heterocyclyl)-methyl and -hetero]-piperidines
US4695575A (en) * 1984-11-13 1987-09-22 Janssen Pharmaceutica, N.V. 4-[(bicycle heterocyclyl)-methyl and -hetero]-piperidines
WO1999025353A1 (en) * 1997-11-13 1999-05-27 Merck Sharp & Dohme Limited Therapeutic uses of triazolo-pyridazine derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JANSSENS ET AL: "New antihistaminic N-heterocyclic 4-piperidinamines. 3. Synthesis and antihistaminic activity of N-(4-piperidinyl)-3H-imidazo[4,5 -b]pyridin-2- amines", JOURNAL OF MEDICINAL CHEMISTRY, vol. 28, 1985, pages 1943 - 1947, XP002104126 *
JANSSENS F ET AL: "NEW ANTIHISTAMINIC N-HETEROCYCLIC 4-PIPERIDINAMINES. 1. SYNTHESIS AND ANTIHISTAMINIC ACTIVITY OF N-(4-PIPERIDINYL)-1H-BENZIMIDAZOL-2 -AMINES", JOURNAL OF MEDICINAL CHEMISTRY, vol. 28, no. 12, 1 January 1985 (1985-01-01), pages 1925 - 1933, XP002074741 *
L. MCCOY ET AL.: "Chronic antipsychotic treatment alters glycine-stimulated NMDA receptor binding in rat brain", NEUROSCIENCE LETTERS, vol. 213, no. 2, 1996, pages 137 - 141, XP002113099 *

Also Published As

Publication number Publication date
TR200002567T2 (en) 2000-11-21
WO1999044596A2 (en) 1999-09-10
NO20004431D0 (en) 2000-09-05
CA2322164A1 (en) 1999-09-10
IL138228A0 (en) 2001-10-31
HUP0101048A2 (en) 2001-10-28
AU3408999A (en) 1999-09-20
CN1292698A (en) 2001-04-25
KR20010032968A (en) 2001-04-25
EE200000482A (en) 2002-02-15
BG104685A (en) 2001-04-30
EP1059922A2 (en) 2000-12-20
NO20004431L (en) 2000-10-30
HRP20000523A2 (en) 2001-02-28
JP2002505277A (en) 2002-02-19
SK13082000A3 (en) 2001-03-12
PL343435A1 (en) 2001-08-13
BR9907951A (en) 2001-01-30

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