HUP0001123A2 - Kombinált 5HT1A, 5HT1B és 5HT1D receptor antagonista aktivitással rendelkező indolszármazékok - Google Patents

Kombinált 5HT1A, 5HT1B és 5HT1D receptor antagonista aktivitással rendelkező indolszármazékok

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Publication number
HUP0001123A2
HUP0001123A2 HU0001123A HUP0001123A HUP0001123A2 HU P0001123 A2 HUP0001123 A2 HU P0001123A2 HU 0001123 A HU0001123 A HU 0001123A HU P0001123 A HUP0001123 A HU P0001123A HU P0001123 A2 HUP0001123 A2 HU P0001123A2
Authority
HU
Hungary
Prior art keywords
group
alkyl
hydrogen
atom
alkoxy
Prior art date
Application number
HU0001123A
Other languages
English (en)
Inventor
Laramie Mary Gaster
Harshad Kantilal Rami
Paul Adrian Wyman
Original Assignee
Smithkline Beecham Plc.
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 GBGB9707829.9A external-priority patent/GB9707829D0/en
Priority claimed from GBGB9801882.3A external-priority patent/GB9801882D0/en
Application filed by Smithkline Beecham Plc. filed Critical Smithkline Beecham Plc.
Publication of HUP0001123A2 publication Critical patent/HUP0001123A2/hu
Publication of HUP0001123A3 publication Critical patent/HUP0001123A3/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links

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

Abstract

A találmány (I) általános képletű központi idegrendszerre hatóvegyületekre - amelyek képletében Ra (i) általános képletű csoport; P1 fenilcsoport, biciklusos arilcsoport, mono- vagy heterociklusoscsoport; R1 hidrogén-, halogénatom, alkil-, cikloalkil-, alkil-karbonil-,alkoxi-, hidroxi-, hidroxi-alkil-, hidroxi-alkoxi-, alkoxi-alkoxi-,alkanoil-, nitro-, trifluor-metil-, ciano-, -SR9, -SOR9, -SO2R9, -SO2NR10R11, -CO2R10, -CONR10R11, -CO2NR10R11, -CONR10(CH2)cCO2R11, -(CH2)pNR10R11, -(CH2)cCONR10R11, -(CH2)cNR10COR11, -(CH2)cCO2(alkil),-CO2(CH2)cOR10, -NR10R11, -NR10CO2R11, -NR10CONR10R11, -CR10=NOR11, -NR10COOR11 vagy -CNR10=NOR11 csoport; R9, R10 és R11 hidrogénatom vagy alkilcsoport; c 1, 2, 3 vagy 4; R2 hidrogén-, halogénatom, alkil-, cikloalkil-, cikloalkenil-,alkoxi-, alkanoil-, aril-, acil-oxi-, hidroxi-, nitro-, trifluor-metil-, ciano-, -CO2R10, -CONR10R11 vagy -NR10R11; és a 1, 2 vagy 3; vagy Ra (ii) általános képletű csoport, P2 és P3 jelentése fenilcsoport, biciklusos arilcsoport, mono- vagybiciklusos heterociklusos csoport; A kémiai kötés, oxigénatom vagy S(O)m, karbonil-, metilén-, etilén-vagy NR4 csoport; m 0, 1 vagy 2; R4 hidorgénatom vagy alkilcsoport; R1 az (i) képletnél meghatározott, vagy R1 adott esetben szubsztituált heterociklusos csoport; R2 és R3 hidrogén-, halogénatom, alkil-, cikloalkil-, cikloalkenil-,alkoxi-, alkanoil-, aril-, acil-oxi-, hidroxi-, nitro-, trifluor-metil-, ciano-, -CO2R10, -CONR10R11 vagy -NR10R11 csoport; valamint a és b 0, 1, 2 vagy 3; Y imino- vagy NR5 csoport, ahol R5 alkilcsoport, vagy Y metiléncsoport vagy oxigénatom; V oxigén- vagy kénatom; D nitrogén-, szénatom vagy metincsoport; W -(CR16R17)t- csoport, ahol t 2, 3 vagy 4, valamint R16 és R17 hidrogénatom vagy alkilcsoport, vagy W -(CR16R17)u-J- csoport, ahol u 0, 1, 2 vagy 3, és J oxigén-, kénatom, -CR16=CR17-, -CR16=N-, =CR16O-, =CR16S- vagy=CR16-NR17- csoport; X nitrogén- vagy szénatom; Rb hidrogén-, halogénatom, hidroxi-, alkil-, trifluor-metil-, alkoxi-,alkenil- vagy cikloalkilcsoport, amely adott esetben szubsztituált; Rc hidrogénatom vagy alkilcsoport; és ...... egyes kötés, ha X nitrogénatom vagy egyes vagy kettős kötés, haX szénatom - és sóira vonatkozik. A találmány kiterjed a vegyületekelőállítási eljárására, valamint a vegyületeket hatóanyagkénttartalmazó gyógyszerkészítményekre is. Ó
HU0001123A 1997-04-18 1998-04-14 Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity HUP0001123A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9707829.9A GB9707829D0 (en) 1997-04-18 1997-04-18 Novel compounds
GBGB9801882.3A GB9801882D0 (en) 1998-01-29 1998-01-29 Novel compounds
PCT/EP1998/002262 WO1998050358A1 (en) 1997-04-18 1998-04-14 Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity

Publications (2)

Publication Number Publication Date
HUP0001123A2 true HUP0001123A2 (hu) 2001-04-28
HUP0001123A3 HUP0001123A3 (en) 2002-04-29

Family

ID=26311401

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0001123A HUP0001123A3 (en) 1997-04-18 1998-04-14 Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity

Country Status (17)

Country Link
EP (1) EP0975593A1 (hu)
JP (1) JP2001524116A (hu)
KR (1) KR20010006487A (hu)
CN (1) CN1260781A (hu)
AR (1) AR013076A1 (hu)
AU (1) AU732863B2 (hu)
BR (1) BR9809092A (hu)
CA (1) CA2288662A1 (hu)
CO (1) CO4950608A1 (hu)
HU (1) HUP0001123A3 (hu)
IL (1) IL132409A0 (hu)
NO (1) NO995065L (hu)
NZ (1) NZ500252A (hu)
PL (1) PL336317A1 (hu)
TR (1) TR199902590T2 (hu)
TW (1) TW509687B (hu)
WO (1) WO1998050358A1 (hu)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9725931D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Novel compounds
WO2000006550A1 (fr) * 1998-07-31 2000-02-10 Nippon Soda Co., Ltd. Composes phenylazole, procede de production desdits composes et medicaments pour le traitement de l'hyperlipidemie
GB9827882D0 (en) * 1998-12-17 1999-02-10 Smithkline Beecham Plc Novel compounds
UA62015C2 (en) 1998-12-28 2003-12-15 Pfizer Prod Inc Benzoizoxazol derivatives, a pharmaceutical composition (variants) based thereon (variants) and a method for treatment (variants)
GB9912413D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912417D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
EP1196380A2 (en) * 1999-07-15 2002-04-17 NPS Allelix Corp. Indoles and indazoles for the treatment of migraine
ATE259363T1 (de) 1999-09-25 2004-02-15 Smithkline Beecham Plc Piperazinderivate als 5-ht1b antagonisten
ES2234683T3 (es) * 1999-11-05 2005-07-01 Smithkline Beecham Plc Derivados de isoquinolina y quinazolina con actividad combinada sobre los receptores 5ht1a, 5ht1b y 5ht1d.
GB9926303D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
DE10051981A1 (de) 2000-10-20 2002-05-02 Bayer Ag Substituierte Phenyluracile
GB0106419D0 (en) 2001-03-15 2001-05-02 Smithkline Beecham Plc Novel compounds
GB0106586D0 (en) * 2001-03-16 2001-05-09 Smithkline Beecham Plc Novel compounds
EP1401813B1 (en) * 2001-06-07 2007-02-07 F. Hoffman-la Roche AG New indole derivatives with 5-ht6 receptor affinity
EP2033953A1 (en) 2002-02-15 2009-03-11 Glaxo Group Limited Vanilloid receptor modulators
AU2003233231B2 (en) 2002-05-13 2009-02-26 F. Hoffmann-La Roche Ag Benzoxazine derivatives as 5-HT6 modulators and uses thereof
AU2004299201B2 (en) 2003-12-09 2009-12-03 F. Hoffmann-La Roche Ag Benzoxazine derivatives and uses thereof
AU2008335709A1 (en) * 2007-12-13 2009-06-18 Amgen Inc. Gamma secretase modulators
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
CN102924330A (zh) * 2012-09-03 2013-02-13 华东理工大学 一种规模化制备5-氨基-1-萘腈的方法
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
CN103467374A (zh) * 2013-08-30 2013-12-25 江苏弘和药物研发有限公司 一种8-溴-4-羧基喹啉的合成方法
RS62301B1 (sr) 2013-12-20 2021-09-30 Astex Therapeutics Ltd Biciklična heterociklična jedinjenja i njihove upotrebe u terapiji
CN115197099A (zh) * 2022-05-30 2022-10-18 安徽昊帆生物有限公司 N-Boc-1,4-苯二胺的制备方法

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
GB9119920D0 (en) * 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
ES2162792T3 (es) * 1991-09-18 2002-01-16 Glaxo Group Ltd Derivados de benzanilida como antagonistas de 5-ht1d.
GB9119932D0 (en) * 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
US5834471A (en) * 1993-08-06 1998-11-10 Smithkline Beecham P.L.C. Amide derivatives as 5HT1D receptor antagonists
WO1995006044A1 (en) * 1993-08-20 1995-03-02 Smithkline Beecham Plc Amide and urea derivatives as 5ht1d receptor antagonists
WO1995006637A1 (en) * 1993-09-03 1995-03-09 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists

Also Published As

Publication number Publication date
TW509687B (en) 2002-11-11
AU7431098A (en) 1998-11-27
NO995065D0 (no) 1999-10-15
IL132409A0 (en) 2001-03-19
AR013076A1 (es) 2000-12-13
EP0975593A1 (en) 2000-02-02
AU732863B2 (en) 2001-05-03
TR199902590T2 (xx) 2000-06-21
NZ500252A (en) 2001-07-27
KR20010006487A (ko) 2001-01-26
PL336317A1 (en) 2000-06-19
CN1260781A (zh) 2000-07-19
BR9809092A (pt) 2002-01-22
WO1998050358A1 (en) 1998-11-12
JP2001524116A (ja) 2001-11-27
CA2288662A1 (en) 1998-11-12
NO995065L (no) 1999-10-15
HUP0001123A3 (en) 2002-04-29
CO4950608A1 (es) 2000-09-01

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