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PE20010641A1 - Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b - Google Patents

Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b

Info

Publication number
PE20010641A1
PE20010641A1 PE2000000989A PE0009892000A PE20010641A1 PE 20010641 A1 PE20010641 A1 PE 20010641A1 PE 2000000989 A PE2000000989 A PE 2000000989A PE 0009892000 A PE0009892000 A PE 0009892000A PE 20010641 A1 PE20010641 A1 PE 20010641A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
heteroaryl
serotonin
phenyl
Prior art date
Application number
PE2000000989A
Other languages
English (en)
Inventor
Paul Adrian Wyman
Mervyn Thompson
Howard Marshall
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 PE20010641A1 publication Critical patent/PE20010641A1/es

Links

Classifications

    • 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

Landscapes

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

Abstract

SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA I, DONDE: Ra ES UN GRUPO i, P1 ES FENILO, NAFTILO, HETEROARILO; R1 Y R2 SON HALOGENO, ALQUILO C1-C6, CICLOALQUILO C3-C6, CO-ALQUILO C1-C6, SR6, SO2NR6R7, NR6CONR7R8, ENTRE OTROS; R6, R7 Y R8 SON H, ALQUILO C1-C6; a ES 0-3; Ra ES UN GRUPO ii; P2 ES FENILO, HETEROARILO, ANILLO HETEROCICLICO DE 5-7 MIEMBROS; P3 ES FENILO, NAFTILO, HETEROARILO; A ES UN ENLACE, O, CARBONILO, CH2, NR4; R4 ES H, ALQUILO C1-C6; O R2 ES UN HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6, HALOGENO, CO-ALQUILO C1-C6, ENTRE OTROS; R3 ES HALOGENO, ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS; b Y c SON 0-3; Y ES UN ENLACE, CH2, O, NR5; R5 ES H, ALQUILO C1-C6; W ES -(CR9R10)t-, -HC=CH-, t ES 2-4; R9 Y R10 SON H, ALQUILO C1-C6; Rb ES H, HALOGENO, HIDROXI, ALQUILO C1-C6, CF3, CO-ALQUILO C1-C6, ENTRE OTROS; Ro ES H, ALQUILO C1-C6, Rd Y Re SON ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS CIS-1-[(2-CLORO-3-TRIFLUOROMETILFENIL)ACETIL]-6-(3,4,5-TRIMETILPIPERAZIN-1-IL)INDOL; CIS-1-[(2-FLUORO-3-TRIFLUOROMETILFENIL)ACETIL]-5-METOXI-6-(3,4,5-TRIMETILPIPERAZIN-1-IL)INDOLINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE SEROTONINA 5-HT1B Y PUEDE SER UTIL PARA EL TRATAMIENTO DE LA DEPRESION
PE2000000989A 1999-09-25 2000-09-22 Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b PE20010641A1 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
PE20010641A1 true PE20010641A1 (es) 2001-07-14

Family

ID=27255501

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000989A PE20010641A1 (es) 1999-09-25 2000-09-22 Derivados de piperazina como antagonistas del receptor de serotonina 5-ht1b

Country Status (27)

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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20020030126A (ko) * 1999-09-25 2002-04-22 피터 기딩스 5―ht1b 길항제로서의 피페라진 유도체
US6642252B2 (en) 2000-11-07 2003-11-04 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
US6906192B2 (en) 2000-11-07 2005-06-14 Bristol Myers Squibb Company Processes for the preparation of 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
JP2006527757A (ja) 2003-06-18 2006-12-07 ファイザー・プロダクツ・インク 新規なピペラジニル−アリールオキシ−n−アリールラクタムおよびピペラジニル−ヘテロアリールオキシ−n−アリールラクタム
WO2006010629A1 (en) 2004-07-28 2006-02-02 Glaxo Group Limited Piperazine derivatives useful for the treatment of gastrointestinal disorders
JP5391691B2 (ja) 2006-03-31 2014-01-15 和光純薬工業株式会社 ピラゾール系シアニン色素
TW200808709A (en) 2006-03-31 2008-02-16 Glaxo Group Ltd Novel compounds
US8680136B2 (en) 2010-08-10 2014-03-25 Rempex Pharmaceuticals, Inc. Cyclic boronic acid ester derivatives and therapeutic uses thereof
WO2013033461A1 (en) 2011-08-31 2013-03-07 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
WO2014107536A1 (en) 2013-01-04 2014-07-10 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9241947B2 (en) 2013-01-04 2016-01-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
US9642869B2 (en) 2013-01-04 2017-05-09 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
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
US10385074B2 (en) 2014-05-05 2019-08-20 Rempex Pharmaceuticals, Inc. Synthesis of boronate salts and uses thereof
CA2947041A1 (en) 2014-05-19 2015-11-26 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
AU2015284307A1 (en) 2014-07-01 2017-02-02 Rempex Pharmaceuticals, 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
WO2016149393A1 (en) 2015-03-17 2016-09-22 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
GB2543498A (en) 2015-10-19 2017-04-26 Schlumberger Holdings Corrosion inhibition
KR102403296B1 (ko) 2016-06-30 2022-05-27 큐펙스 바이오파마 인코포레이티드 보론산 유도체 및 이의 치료적 용도
BR112020007138B1 (pt) 2017-10-11 2023-03-21 Qpex Biopharma, Inc Derivados de ácido borônico, métodos de síntese, composição farmacêutica e uso dos mesmos
CN112424209A (zh) 2018-04-20 2021-02-26 Qpex生物制药有限公司 硼酸衍生物及其治疗用途
WO2020183011A1 (en) 2019-03-14 2020-09-17 Institut Curie Htr1d inhibitors and uses thereof in the treatment of cancer

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PT533268E (pt) 1991-09-18 2002-02-28 Glaxo Group Ltd Derivados de benzanilida como antagonistas de 5-ht1d
DE69417427T2 (de) * 1993-09-03 1999-11-25 Smithkline Beecham P.L.C., Brentford Indol- und indolin-derivate als 5ht1d rezeptor antagonisten
EP0946551A2 (en) * 1996-12-19 1999-10-06 Smithkline Beecham Plc N-piperazin-1-ylphenyl-benzamide derivatives
JP2001526643A (ja) * 1997-04-18 2001-12-18 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 5ht1a、5ht1bおよび5ht1d受容体アンタゴニスト活性を合わせ持つ化合物を含む二環式アリールまたは二環式複素環
CA2288662A1 (en) * 1997-04-18 1998-11-12 Smithkline Beecham P.L.C. Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity
GB9725931D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Novel compounds
KR20020030126A (ko) * 1999-09-25 2002-04-22 피터 기딩스 5―ht1b 길항제로서의 피페라진 유도체

Also Published As

Publication number Publication date
HUP0202787A3 (en) 2003-12-29
MY122391A (en) 2006-04-29
JP2003510317A (ja) 2003-03-18
PT1216239E (pt) 2004-05-31
CO5200839A1 (es) 2002-09-27
DK1216239T3 (da) 2004-06-14
NZ517865A (en) 2003-11-28
MXPA02003175A (es) 2002-09-30
PL362900A1 (en) 2004-11-02
US6747030B1 (en) 2004-06-08
NO20021459D0 (no) 2002-03-22
DE60008262T2 (de) 2004-12-16
WO2001023374A1 (en) 2001-04-05
AR029454A1 (es) 2003-07-02
AU765020B2 (en) 2003-09-04
NO20021459L (no) 2002-03-22
TR200200795T2 (tr) 2002-07-22
ES2211624T3 (es) 2004-07-16
IL148818A0 (en) 2002-09-12
HK1046909B (en) 2004-12-03
EP1216239A1 (en) 2002-06-26
ATE259363T1 (de) 2004-02-15
HK1046909A1 (en) 2003-01-30
EP1216239B1 (en) 2004-02-11
AU7783600A (en) 2001-04-30
BR0014279A (pt) 2002-05-21
CN1190432C (zh) 2005-02-23
KR20020030126A (ko) 2002-04-22
DE60008262D1 (de) 2004-03-18
CZ20021038A3 (cs) 2002-08-14
HUP0202787A2 (hu) 2002-12-28
CA2385737A1 (en) 2001-04-05
US20040176388A1 (en) 2004-09-09
CN1399635A (zh) 2003-02-26

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