AU2002304833B2 - Tetrahydro-pyrazino (1,2-A) indoles for the treatment of central nervous disorders - Google Patents

Tetrahydro-pyrazino (1,2-A) indoles for the treatment of central nervous disorders Download PDF

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Publication number
AU2002304833B2
AU2002304833B2 AU2002304833A AU2002304833A AU2002304833B2 AU 2002304833 B2 AU2002304833 B2 AU 2002304833B2 AU 2002304833 A AU2002304833 A AU 2002304833A AU 2002304833 A AU2002304833 A AU 2002304833A AU 2002304833 B2 AU2002304833 B2 AU 2002304833B2
Authority
AU
Australia
Prior art keywords
methyl
pyrazino
indole
compound
tetrahydro
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
AU2002304833A
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English (en)
Other versions
AU2002304833A1 (en
Inventor
Paul Hebeisen
Patrizio Mattei
Marc Muller
Hans Richter
Stephan Roever
Sven Taylor
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.)
F Hoffmann La Roche AG
Ligand UK Research Ltd
Original Assignee
F Hoffmann La Roche AG
Vernalis Research Ltd
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Filing date
Publication date
Application filed by F Hoffmann La Roche AG, Vernalis Research Ltd filed Critical F Hoffmann La Roche AG
Publication of AU2002304833A1 publication Critical patent/AU2002304833A1/en
Application granted granted Critical
Publication of AU2002304833B2 publication Critical patent/AU2002304833B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2002304833A 2001-03-13 2002-03-06 Tetrahydro-pyrazino (1,2-A) indoles for the treatment of central nervous disorders Ceased AU2002304833B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0106177.9 2001-03-13
GBGB0106177.9A GB0106177D0 (en) 2001-03-13 2001-03-13 Piperazine derivatives
PCT/EP2002/002443 WO2002072584A2 (en) 2001-03-13 2002-03-06 Tetrahydro-pyrazino (1,2-a) indoles for the treatment of central nervous disorders

Publications (2)

Publication Number Publication Date
AU2002304833A1 AU2002304833A1 (en) 2003-03-20
AU2002304833B2 true AU2002304833B2 (en) 2006-05-04

Family

ID=9910578

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002304833A Ceased AU2002304833B2 (en) 2001-03-13 2002-03-06 Tetrahydro-pyrazino (1,2-A) indoles for the treatment of central nervous disorders

Country Status (20)

Country Link
US (1) US6844345B2 (enExample)
EP (1) EP1370561B1 (enExample)
JP (1) JP4230225B2 (enExample)
KR (1) KR100618748B1 (enExample)
CN (1) CN1245405C (enExample)
AR (1) AR035945A1 (enExample)
AT (1) ATE422498T1 (enExample)
AU (1) AU2002304833B2 (enExample)
BR (1) BR0208111A (enExample)
CA (1) CA2438596C (enExample)
DE (1) DE60231107D1 (enExample)
ES (1) ES2320739T3 (enExample)
GB (1) GB0106177D0 (enExample)
GT (1) GT200200048A (enExample)
MX (1) MXPA03008338A (enExample)
PA (1) PA8540801A1 (enExample)
PE (1) PE20021043A1 (enExample)
UY (1) UY27204A1 (enExample)
WO (1) WO2002072584A2 (enExample)
ZA (1) ZA200306613B (enExample)

Families Citing this family (21)

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Publication number Priority date Publication date Assignee Title
US6762132B1 (en) * 2000-08-31 2004-07-13 Micron Technology, Inc. Compositions for dissolution of low-K dielectric films, and methods of use
AU2003243089B2 (en) 2002-06-19 2010-01-07 Biovitrum Ab (Publ) Novel compounds, their use and preparation
CL2004000826A1 (es) 2003-04-25 2005-03-04 Pfizer Uso de un agonista para el receptor 5-ht2c para preparar un medicamento util en el tratamiento de la incontinencia urinaria provocada por estres, con la condicion de que el agonista no sea 1-[6-cloro-5-(trifluorometil)-2-piridinil]piperazina (org-129
JP4917018B2 (ja) * 2004-05-03 2012-04-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 選択的アンドローゲン受容体モジュレーター（ｓａｒｍｓ）としての新規インドール化合物
WO2006022420A1 (ja) 2004-08-25 2006-03-02 Takeda Pharmaceutical Company Limited 腹圧性尿失禁の予防・治療剤及びそのスクリーニング方法
DE602006017741D1 (de) * 2005-11-18 2010-12-02 Hoffmann La Roche Azaindol-2-carboxamid-derivate
ATE448230T1 (de) * 2005-12-09 2009-11-15 Hoffmann La Roche Für die behandlung von obesitas geeignete tricyclische amidderivate
JP5528699B2 (ja) 2006-05-16 2014-06-25 武田薬品工業株式会社 縮合複素環化合物およびその用途
JP5520051B2 (ja) 2007-11-15 2014-06-11 武田薬品工業株式会社 縮合ピリジン誘導体およびその用途
EP2254886B1 (en) 2008-03-28 2016-05-25 Nerviano Medical Sciences S.r.l. 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
EP2510949A4 (en) 2009-12-11 2013-11-13 Astellas Pharma Inc THERAPEUTICS FOR FIBROMYALGIA
WO2011149036A1 (ja) * 2010-05-27 2011-12-01 国立大学法人 東京大学 抗炎症薬
US20130267500A1 (en) 2010-09-01 2013-10-10 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level
EP2825541B1 (en) 2012-03-16 2016-06-22 Vitae Pharmaceuticals, Inc. Liver x receptor modulators
BR112014022780A8 (pt) 2012-03-16 2021-06-15 Vitae Pharmaceuticals Inc composto modulador de receptor de fígado x, composição farmacêutica que o compreende e seu uso
MY185216A (en) * 2012-08-06 2021-04-30 Hoffmann La Roche Piperazino[1,2-a]indol-ones and [1, 4]diazepino[1,2-a]indol-1-one
MX2015013915A (es) * 2013-04-02 2015-12-11 Hoffmann La Roche Piperazino[1,2-a]indol-1-onas y [1,4]diazepino[1,2-a]indol-1-ona.
WO2015066344A1 (en) 2013-11-01 2015-05-07 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
CN106317058B (zh) * 2016-08-17 2018-10-02 广东省微生物研究所 化合物dichotocejpin A及其制备方法和在制备治疗糖尿病药物中的应用
JOP20190239A1 (ar) 2017-04-19 2019-10-09 Neurocrine Biosciences Inc مركبات مثبطة لـ vmat2 وتركيبات منها
EP3733204A4 (en) 2017-12-27 2021-09-15 Takeda Pharmaceutical Company Limited THERAPEUTIC AGENT FOR URINARY INCONTINENCE OF STRESS AND FECAL INCONTINENCE

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0572863A1 (de) * 1992-06-05 1993-12-08 F. Hoffmann-La Roche Ag ZNS Pyrazinoindole
US5854245A (en) * 1996-06-28 1998-12-29 Merck & Co., Inc. Fibrinogen receptor antagonists
WO2000044753A1 (en) * 1999-01-29 2000-08-03 Vernalis Research Limited Pirazino(aza)indole derivatives

Family Cites Families (12)

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US3317524A (en) * 1965-02-04 1967-05-02 American Home Prod Substituted 1, 2, 3, 4-tetrahydro-pyrazino[1, 2-a]indoles
CA1247547A (en) * 1983-06-22 1988-12-28 Paul Hadvary Leucine derivatives
CA1328881C (en) 1984-12-21 1994-04-26 Pierre Barbier Process for the manufacture of oxetanones
CA1270837A (en) 1984-12-21 1990-06-26 Hoffmann-La Roche Limited Oxetanones
CA2035972C (en) 1990-02-23 2006-07-11 Martin Karpf Process for the preparation of oxetanones
US5274143A (en) 1991-07-23 1993-12-28 Hoffmann-La Roche Inc. Process for the preparation of (R)-3-hexyl-5,6-dihydro-4-hydroxy-6-undecyl-2H-pyran-2-one and (R)-5,6-dihydro-6-undecyl-2H-pyran-2,4(3H)-dione
AU3831495A (en) * 1994-10-20 1996-05-15 American Home Products Corporation Indole derivatives useful as serotonergic agents
US6004996A (en) * 1997-02-05 1999-12-21 Hoffman-La Roche Inc. Tetrahydrolipstatin containing compositions
US6267952B1 (en) 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
DE69916288T2 (de) 1998-08-14 2005-03-24 F. Hoffmann-La Roche Ag Lipasehemmer und chitosan enthaltende arzneimittel
ATE293970T1 (de) 1998-08-14 2005-05-15 Hoffmann La Roche Lipasehemmer enthaltende pharmazeutische zusammensetzungen
AU2001283955B2 (en) * 2000-07-31 2006-05-18 F. Hoffmann-La Roche Ag Piperazine derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0572863A1 (de) * 1992-06-05 1993-12-08 F. Hoffmann-La Roche Ag ZNS Pyrazinoindole
US5854245A (en) * 1996-06-28 1998-12-29 Merck & Co., Inc. Fibrinogen receptor antagonists
WO2000044753A1 (en) * 1999-01-29 2000-08-03 Vernalis Research Limited Pirazino(aza)indole derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
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Also Published As

Publication number Publication date
JP4230225B2 (ja) 2009-02-25
MXPA03008338A (es) 2003-12-11
ES2320739T3 (es) 2009-05-28
KR100618748B1 (ko) 2006-08-31
ATE422498T1 (de) 2009-02-15
EP1370561A2 (en) 2003-12-17
US20020169163A1 (en) 2002-11-14
GT200200048A (es) 2002-11-15
PE20021043A1 (es) 2002-11-19
CA2438596C (en) 2008-07-08
GB0106177D0 (en) 2001-05-02
AR035945A1 (es) 2004-07-28
DE60231107D1 (de) 2009-03-26
KR20030080255A (ko) 2003-10-11
CN1245405C (zh) 2006-03-15
US6844345B2 (en) 2005-01-18
EP1370561B1 (en) 2009-02-11
BR0208111A (pt) 2004-03-02
ZA200306613B (en) 2004-11-25
WO2002072584A2 (en) 2002-09-19
WO2002072584A3 (en) 2003-01-03
CA2438596A1 (en) 2002-09-19
PA8540801A1 (es) 2005-02-04
UY27204A1 (es) 2002-09-30
JP2004532823A (ja) 2004-10-28
CN1529706A (zh) 2004-09-15

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired