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MXPA02003792A - Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados. - Google Patents

Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados.

Info

Publication number
MXPA02003792A
MXPA02003792A MXPA02003792A MXPA02003792A MXPA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A
Authority
MX
Mexico
Prior art keywords
receptors
pyrazole derivatives
serotonin receptors
candidate compounds
human serotonin
Prior art date
Application number
MXPA02003792A
Other languages
English (en)
Inventor
J Thomsen William
Original Assignee
Arena Pharm 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 Arena Pharm Inc filed Critical Arena Pharm Inc
Publication of MXPA02003792A publication Critical patent/MXPA02003792A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Medicinal Chemistry (AREA)
  • Cell Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

En la presente invencion se describen formas activadas constitutivamente no endogenas de los receptores 5HT2A humano y 5HT2c humano y usos de dichos receptores para seleccionar compuestos candidato. Ademas se describen los compuestos candidatos identificados por los metodos de seleccion que actuan en los receptores 5HT2A. Ademas se describe una nueva clase de compuestos (I) los cuales actuan en los receptores 5HT2A. Esta nueva clase comprende los compuestos candidato. En la formula (A) W es F, CI, Br, I, alquilo C1-8 de cadena recta o ramificada, cicloalquilo C3-8, alquilcicloalquilo C4-9 o alquenilo C2-8 ; X es O o S o NR2; Y es NR3R4, o (CH2)mR5 u O(CH 2)nR6; M es un entero entre 0 y 4, inclusive; N es un entero entre 0 y 4 inclusive; Z es H, alquilo C1-8 de cadena recta o ramificada, cicloalquilo C3-8 alquilcicloalquilo C4-9 o alquenilo C2-8; R1, R2, R3 y R10 son tal como se definen en la solicitud.
MXPA02003792A 1999-10-15 2000-10-13 Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados. MXPA02003792A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/418,721 US6150393A (en) 1998-12-18 1999-10-15 Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
PCT/US2000/028347 WO2001029008A1 (en) 1999-10-15 2000-10-13 Pyrazole derivatives which modulate human serotonin receptors

Publications (1)

Publication Number Publication Date
MXPA02003792A true MXPA02003792A (es) 2004-09-06

Family

ID=23659316

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA02003792A MXPA02003792A (es) 1999-10-15 2000-10-13 Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados.

Country Status (8)

Country Link
US (1) US6150393A (es)
EP (1) EP1244632A1 (es)
CN (1) CN1411448A (es)
AU (1) AU1201001A (es)
CA (1) CA2387031A1 (es)
IL (1) IL149111A0 (es)
MX (1) MXPA02003792A (es)
WO (1) WO2001029008A1 (es)

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US7279324B2 (en) * 2001-01-23 2007-10-09 Duke University Nucleic acid encoding G-protein coupled receptor with modified DRY motif
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CN1816524B (zh) 2003-01-16 2012-06-27 阿卡蒂亚药品公司 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂
DE10315569A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
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DE10315572A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
PL1558582T3 (pl) * 2003-07-22 2006-05-31 Arena Pharm Inc Diarylowe i aryloheteroarylowe pochodne mocznika jako modulatory receptora serotoninowego 5-HT2A użyteczne w profilaktyce i w leczeniu zaburzeń związanych z tym receptorem
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WO2005021505A1 (en) * 2003-09-03 2005-03-10 Galapagos Nv The claimed invention relates to novel 4-piperidinecarboxamide and the use thereof for the preparation of medicaments against 5-ht2a receptor-related disorders
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Also Published As

Publication number Publication date
EP1244632A1 (en) 2002-10-02
CN1411448A (zh) 2003-04-16
CA2387031A1 (en) 2001-04-26
AU1201001A (en) 2001-04-30
US6150393A (en) 2000-11-21
IL149111A0 (en) 2002-11-10
WO2001029008A1 (en) 2001-04-26

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