HUP0202787A2 - 5-HT1B antagonista piperazinszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents

5-HT1B antagonista piperazinszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0202787A2
HUP0202787A2 HU0202787A HUP0202787A HUP0202787A2 HU P0202787 A2 HUP0202787 A2 HU P0202787A2 HU 0202787 A HU0202787 A HU 0202787A HU P0202787 A HUP0202787 A HU P0202787A HU P0202787 A2 HUP0202787 A2 HU P0202787A2
Authority
HU
Hungary
Prior art keywords
group
alkyl
hydrogen
general formula
heteroaryl
Prior art date
Application number
HU0202787A
Other languages
English (en)
Inventor
Howard Marshall
Mervyn Thompson
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 GBGB9922831.4A external-priority patent/GB9922831D0/en
Priority claimed from GB0001936A external-priority patent/GB0001936D0/en
Priority claimed from GB0013873A external-priority patent/GB0013873D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of HUP0202787A2 publication Critical patent/HUP0202787A2/hu
Publication of HUP0202787A3 publication Critical patent/HUP0202787A3/hu

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    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/10Heterocyclic 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 carbon chain containing aromatic rings
    • 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings
    • 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

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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)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A találmány (I) általános képletű vegyületekre - amelyek képletében Ra(i) általános képletű csoport, amelyben P1 fenil-, naftil- vagyheteroarilcsoport; R1 halogénatom, alkil-, cikloalkil-, alkoxi-,hidroxi-, hidroxi-alkil-, nitro-, trifluor-metil-, ciano-, -SR6, -SOR6, -SO2R6, -SO2NR6R7, -CO2R6, -CONR6R7, -OCONR6R7, -NR6R7, -NR6CO2R7, -NR6CONR7R8, -CR6=NOR7 csoport; ahol R6, R7 és R8hidrogénatom vagy alkilcsoport; és a 0, 1, 2 vagy 3; vagy Ra (ii)általános képletű csoport, amelyben P2 fenil-, naftil-, heteroaril-,heterociklusos csoport; P3 fenil-, naftil- vagy heteroarilcsoport; Akémiai kötés, oxigénatom, karbonil-, metilén- vagy NR4 csoport; aholR4 hidrogénatom vagy alkilcsoport; R2 az (i) általános képletnél R1-nél meghatározott, vagy R2 adott esetben szubsztituált heteroaril-vagy heterociklusos csoport; R3 halogénatom, alkil-, cikloalkil-,alkoxi-, alkil-karbonil-, hidroxi-, nitro-, trifluor-metil-, ciano-, -CO2R6, -CONR6R7, -NR6R7 csoport, ahol R6 és R7 a fentiekbenmeghatározott; b és c 0, 1, 2 vagy 3; Y kémiai kötés, metiléncsoport,oxigénatom, NR5 csoport; R5 hidrogénatom vagy alkilcsoport; W -(CR9R10)t- csoport, ahol t 2, 3 vagy 4, valamint R9 és R10hidrogénatom vagy alkilcsoport, vagy W viniléncsoport (-CH=CH-); Rbhidrogén-, halogénatom, hidroxi-, alkil-, trifluor-metil-, alkil-karbonil-, ciano- vagy alkoxicsoport; Rc hidrogénatom vagyalkilcsoport; valamint Rd és Re alkilcsoport és gyógyászatilag elfogadható sóikra vonatkozik. A találmánykiterjed a vegyületek előállítási eljárására, gyógyászatialkalmazására, valamint a vegyületeket tartalmazógyógyszerkészítményekre is. Ó
HU0202787A 1999-09-25 2000-09-21 Piperazine derivatives as 5-ht1b antagonists, process for their preparation and pharmaceutical compositions containing them HUP0202787A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB9922831.4A GB9922831D0 (en) 1999-09-25 1999-09-25 Novel compounds
GB0001936A GB0001936D0 (en) 2000-01-27 2000-01-27 Novel compounds
GB0013873A GB0013873D0 (en) 2000-06-07 2000-06-07 Novel compounds
PCT/EP2000/009442 WO2001023374A1 (en) 1999-09-25 2000-09-21 Piperazine derivatives as 5-ht1b antagonists

Publications (2)

Publication Number Publication Date
HUP0202787A2 true HUP0202787A2 (hu) 2002-12-28
HUP0202787A3 HUP0202787A3 (en) 2003-12-29

Family

ID=27255501

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202787A HUP0202787A3 (en) 1999-09-25 2000-09-21 Piperazine derivatives as 5-ht1b antagonists, process for their preparation and pharmaceutical compositions containing them

Country Status (27)

Country Link
US (2) US6747030B1 (hu)
EP (1) EP1216239B1 (hu)
JP (1) JP2003510317A (hu)
KR (1) KR20020030126A (hu)
CN (1) CN1190432C (hu)
AR (1) AR029454A1 (hu)
AT (1) ATE259363T1 (hu)
AU (1) AU765020B2 (hu)
BR (1) BR0014279A (hu)
CA (1) CA2385737A1 (hu)
CO (1) CO5200839A1 (hu)
CZ (1) CZ20021038A3 (hu)
DE (1) DE60008262T2 (hu)
DK (1) DK1216239T3 (hu)
ES (1) ES2211624T3 (hu)
HK (1) HK1046909B (hu)
HU (1) HUP0202787A3 (hu)
IL (1) IL148818A0 (hu)
MX (1) MXPA02003175A (hu)
MY (1) MY122391A (hu)
NO (1) NO20021459L (hu)
NZ (1) NZ517865A (hu)
PE (1) PE20010641A1 (hu)
PL (1) PL362900A1 (hu)
PT (1) PT1216239E (hu)
TR (1) TR200200795T2 (hu)
WO (1) WO2001023374A1 (hu)

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EP1216239B1 (en) * 1999-09-25 2004-02-11 SmithKline Beecham plc Piperazine derivatives as 5-ht1b antagonists
US6906192B2 (en) 2000-11-07 2005-06-14 Bristol Myers Squibb Company Processes for the preparation of acid derivatives useful as serine protease inhibitors
CA2428191A1 (en) 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
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
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
WO2004110994A1 (en) * 2003-06-18 2004-12-23 Pfizer Products Inc. Novel piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
WO2006010629A1 (en) 2004-07-28 2006-02-02 Glaxo Group Limited Piperazine derivatives useful for the treatment of gastrointestinal disorders
ATE535525T1 (de) 2006-03-31 2011-12-15 Wako Pure Chem Ind Ltd Cyaninfarbstoff vom pyrazoltyp
AR060213A1 (es) 2006-03-31 2008-06-04 Glaxo Group Ltd Compuesto de piperazinil - piridinil -bencensulfonamida , su uso para fabricar un medicamento proceso para la preparacion del mismo composicion farmaceutica que lo comprende y proceso para prepararla
BR112013003045B1 (pt) 2010-08-10 2021-08-31 Rempex Pharmaceuticals, Inc. Composto e respectivo uso, composição farmacêutica, recipiente estéril e método para preparar composição farmacêutica para administração
US9012491B2 (en) 2011-08-31 2015-04-21 Rempex Pharmaceuticals, Inc. Heterocyclic boronic acid ester derivatives and therapeutic uses thereof
US9156858B2 (en) 2012-05-23 2015-10-13 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US10561675B2 (en) 2012-06-06 2020-02-18 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
CN102766139B (zh) * 2012-08-14 2014-09-17 江苏先声药物研究有限公司 阿齐沙坦的多晶型物及其制备方法
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9101638B2 (en) 2013-01-04 2015-08-11 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
CA2894891A1 (en) 2013-01-04 2014-07-10 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
MX2015008627A (es) 2013-01-04 2015-09-23 Rempex Pharmaceuticals Inc Derivados de acido boronico y usos terapeuticos de los mismos.
RS59488B1 (sr) 2014-05-05 2019-12-31 Rempex Pharmaceuticals Inc Sinteza boronatnih soli i njihove upotrebe
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
KR20170007448A (ko) 2014-05-19 2017-01-18 렘펙스 파머수티클스 인코퍼레이티드 보론산 유도체 및 그의 치료적 용도
EP3164406B1 (en) 2014-07-01 2024-12-25 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
WO2016081297A1 (en) 2014-11-18 2016-05-26 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
GB2532990A (en) 2014-12-05 2016-06-08 Schlumberger Holdings Corrosion inhibition
US20180051041A1 (en) 2015-03-17 2018-02-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
GB2543498A (en) * 2015-10-19 2017-04-26 Schlumberger Holdings Corrosion inhibition
US10294249B2 (en) 2016-06-30 2019-05-21 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
US11286270B2 (en) 2017-10-11 2022-03-29 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis thereof
EP3781576B1 (en) 2018-04-20 2024-06-12 Qpex Biopharma, Inc. Boronic acid derivatives and therapeutic uses thereof
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer

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DE69232003T2 (de) * 1991-09-18 2002-04-25 Glaxo Group Ltd., Greenford Benzanilidderivate als 5-HT1D-Antagonisten
WO1995006637A1 (en) * 1993-09-03 1995-03-09 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists
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EP1216239B1 (en) * 1999-09-25 2004-02-11 SmithKline Beecham plc Piperazine derivatives as 5-ht1b antagonists

Also Published As

Publication number Publication date
JP2003510317A (ja) 2003-03-18
MXPA02003175A (es) 2002-09-30
HUP0202787A3 (en) 2003-12-29
BR0014279A (pt) 2002-05-21
WO2001023374A1 (en) 2001-04-05
CA2385737A1 (en) 2001-04-05
EP1216239B1 (en) 2004-02-11
DE60008262T2 (de) 2004-12-16
ES2211624T3 (es) 2004-07-16
AU7783600A (en) 2001-04-30
DE60008262D1 (de) 2004-03-18
CZ20021038A3 (cs) 2002-08-14
CN1190432C (zh) 2005-02-23
TR200200795T2 (tr) 2002-07-22
US20040176388A1 (en) 2004-09-09
CN1399635A (zh) 2003-02-26
US6747030B1 (en) 2004-06-08
CO5200839A1 (es) 2002-09-27
IL148818A0 (en) 2002-09-12
PE20010641A1 (es) 2001-07-14
AU765020B2 (en) 2003-09-04
HK1046909A1 (en) 2003-01-30
MY122391A (en) 2006-04-29
ATE259363T1 (de) 2004-02-15
NZ517865A (en) 2003-11-28
KR20020030126A (ko) 2002-04-22
EP1216239A1 (en) 2002-06-26
HK1046909B (en) 2004-12-03
PL362900A1 (en) 2004-11-02
AR029454A1 (es) 2003-07-02
NO20021459D0 (no) 2002-03-22
DK1216239T3 (da) 2004-06-14
NO20021459L (no) 2002-03-22
PT1216239E (pt) 2004-05-31

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