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PE20021043A1 - DERIVADOS DE PIRAZINO[1,2-a]INDOL COMO AGONISTAS DEL RECEPTOR 5HT2 - Google Patents

DERIVADOS DE PIRAZINO[1,2-a]INDOL COMO AGONISTAS DEL RECEPTOR 5HT2

Info

Publication number
PE20021043A1
PE20021043A1 PE2002000197A PE2002000197A PE20021043A1 PE 20021043 A1 PE20021043 A1 PE 20021043A1 PE 2002000197 A PE2002000197 A PE 2002000197A PE 2002000197 A PE2002000197 A PE 2002000197A PE 20021043 A1 PE20021043 A1 PE 20021043A1
Authority
PE
Peru
Prior art keywords
pirazino
indol
tetrahydro
cycloalkyl
alkyl
Prior art date
Application number
PE2002000197A
Other languages
English (en)
Inventor
Paul Hebeisen
Patrizio Mattei
Taylor Sven
Hans Richter
Stephan Roever
Marc Muller
Original Assignee
Vernalis Res Ltd
Hoffmann La Roche
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 Vernalis Res Ltd, Hoffmann La Roche filed Critical Vernalis Res Ltd
Publication of PE20021043A1 publication Critical patent/PE20021043A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A DERIVADOS DE PIRAZINO-INDOL DE FORMULA I DONDE R1, R2, R3, R4 SON H, HALOGENO, HIDROXILO, ALQUILO, CICLOALQUILO, ARILALQUILO, ARILO, ALCOXILO, ALCOXIALQUILO, ENTRE OTROS; UNO DE R1, R2, R3, R4 NO ES H; R5 ES H, ALQUILO, CICLOALQUILO; R6 ES H, ALQUILO, CICLOALQUILO, HIDROXIALQUILO, ALCOXIALQUILO; R7 ES H, HALOGENO, ALQUILO, CICLOALQUILO, HIDROXIALQUILO, CARBOXIALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS (R)-6-TIENIL-4-METIL-1,2,3,4-TETRAHIDRO-PIRAZINO[1,2-a]INDOL; (R)-4,6-DIMETIL-1,2,3,4-TETRAHIDRO-PIRAZINO[1,2-a]INDOL; (R)-7-CLORO-4-METIL-1,2,3,4-TETRAHIDRO-PIRAZINO[1,2-a]INDOL, (R)-6-ETIL-4-METIL-1,2,3,4-TETRAHIDRO-PIRAZINO[1,2-a]INDOL, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION Y AL USO DEL COMPUESTO CON UN INHIBIDOR DE LIPASA COMO ORLISTAT. LOS COMPUESTOS SON AGONISTAS DEL RECEPTOR 5-HT2C Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE OBESIDAD, TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL, TRASTORNOS CARDIOVASCULARES, TROMBOSIS, DISFUNCION DE LA MOTILIDAD GASTROINTESTINAL, OBESIDAD, ENCEFALITIS, MENINGITIS
PE2002000197A 2001-03-13 2002-03-12 DERIVADOS DE PIRAZINO[1,2-a]INDOL COMO AGONISTAS DEL RECEPTOR 5HT2 PE20021043A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0106177.9A GB0106177D0 (en) 2001-03-13 2001-03-13 Piperazine derivatives

Publications (1)

Publication Number Publication Date
PE20021043A1 true PE20021043A1 (es) 2002-11-19

Family

ID=9910578

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000197A PE20021043A1 (es) 2001-03-13 2002-03-12 DERIVADOS DE PIRAZINO[1,2-a]INDOL COMO AGONISTAS DEL RECEPTOR 5HT2

Country Status (20)

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

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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
WO2005110985A2 (en) * 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Indole, benzofuran and benzothiophene derivatives as selective androgen receptor modulators (sarms)
EP1792629A4 (en) 2004-08-25 2010-08-25 Takeda Pharmaceutical MEANS FOR THE PREVENTION / TREATMENT OF STRESS-RELATED HARNINE INCONTINENCE AND PRECAUTIONARY METHOD FOR THIS
EP1966199B1 (en) * 2005-11-18 2010-10-20 F. Hoffmann-La Roche AG Azaindole-2-carboxamide derivatives
CN101321761A (zh) * 2005-12-09 2008-12-10 霍夫曼-拉罗奇有限公司 用于治疗肥胖病的三环酰胺衍生物
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
WO2009063992A1 (ja) 2007-11-15 2009-05-22 Takeda Pharmaceutical Company Limited 縮合ピリジン誘導体およびその用途
JP5767101B2 (ja) 2008-03-28 2015-08-19 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な3,4−ジヒドロ−2h−ピラジノ[1,2−a]インドール−1−オン誘導体、これらの調製方法、およびこれらを含む医薬組成物
EP2510949A4 (en) 2009-12-11 2013-11-13 Astellas Pharma Inc THERAPEUTICS FOR FIBROMYALGIA
US20130143812A1 (en) * 2010-05-27 2013-06-06 Sekisui Medical Co., Ltd. Anti-inflammatory drug
WO2012030953A1 (en) 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level
LT2825542T (lt) 2012-03-16 2016-12-27 Vitae Pharmaceuticals, Inc. Kepenų x receptoriaus moduliatoriai
AU2013232066B2 (en) 2012-03-16 2017-07-06 Vitae Pharmaceuticals, Inc. Liver X receptor modulators
AR092041A1 (es) 2012-08-06 2015-03-18 Hoffmann La Roche Piperazino[1,2-a]indol-1-onas y [1,4]diazepino[1,2-a]indol-1-ona
CN105246895B (zh) * 2013-04-02 2017-09-22 豪夫迈·罗氏有限公司 哌嗪并[1,2‑a]吲哚‑1‑酮和[1,4]二氮杂环庚烷并[1,2‑a]吲哚‑1‑酮
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

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Also Published As

Publication number Publication date
ATE422498T1 (de) 2009-02-15
ZA200306613B (en) 2004-11-25
MXPA03008338A (es) 2003-12-11
ES2320739T3 (es) 2009-05-28
BR0208111A (pt) 2004-03-02
UY27204A1 (es) 2002-09-30
US6844345B2 (en) 2005-01-18
DE60231107D1 (de) 2009-03-26
KR20030080255A (ko) 2003-10-11
AU2002304833B2 (en) 2006-05-04
CA2438596C (en) 2008-07-08
GT200200048A (es) 2002-11-15
EP1370561B1 (en) 2009-02-11
JP4230225B2 (ja) 2009-02-25
PA8540801A1 (es) 2005-02-04
EP1370561A2 (en) 2003-12-17
WO2002072584A2 (en) 2002-09-19
JP2004532823A (ja) 2004-10-28
GB0106177D0 (en) 2001-05-02
WO2002072584A3 (en) 2003-01-03
CA2438596A1 (en) 2002-09-19
US20020169163A1 (en) 2002-11-14
CN1529706A (zh) 2004-09-15
AR035945A1 (es) 2004-07-28
CN1245405C (zh) 2006-03-15
KR100618748B1 (ko) 2006-08-31

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