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

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)
  • 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)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
HUP0400651A2 (hu) 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
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
BRPI0410561A (pt) 2003-06-18 2006-06-20 Pfizer Prod Inc lactamas de piperazinileteroarilóxi-n-arill e de piperazinilarilóxi
RU2007107349A (ru) 2004-07-28 2008-09-10 Глэксо Груп Лимитед (GB) Пиперазиновые производные, применение для лечения желудочно-кишечных расстройств
ATE535525T1 (de) 2006-03-31 2011-12-15 Wako Pure Chem Ind Ltd Cyaninfarbstoff vom pyrazoltyp
PE20080176A1 (es) 2006-03-31 2008-04-25 Glaxo Group Ltd Compuestos de arilpiperazina sulfonamida como agonista de los receptores de secretagogos de la hormona de crecimiento (ghs)
KR102205755B1 (ko) 2010-08-10 2021-01-22 렘펙스 파머수티클스 인코퍼레이티드 고리형 보론산 에스터 유도체의 결정 형태
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
JP2016509594A (ja) 2013-01-04 2016-03-31 レンペックス・ファーマシューティカルズ・インコーポレイテッド ボロン酸誘導体及びその治療的使用
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
JP6324409B2 (ja) 2013-01-04 2018-05-16 レンペックス・ファーマシューティカルズ・インコーポレイテッド ボロン酸誘導体及びその治療的使用
FI3604316T3 (fi) 2014-05-05 2024-02-29 Melinta Therapeutics Inc Boronaattisuolojen synteesi
US9687497B1 (en) 2014-05-05 2017-06-27 Rempex Pharmaceuticals, Inc. Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof
AU2015264418A1 (en) 2014-05-19 2016-11-10 Rempex Pharmaceuticals, Inc. Boronic acid derivatives and therapeutic uses thereof
EA201692301A1 (ru) 2014-07-01 2017-06-30 Ремпекс Фармасьютикалз, Инк. Производные бороновой кислоты и их терапевтическое применение
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
UA124464C2 (uk) 2016-06-30 2021-09-22 Кьюпекс Біофарма, Інк. Похідні боронової кислоти та їх терапевтичні застосування
EP3694864B1 (en) 2017-10-11 2025-03-05 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis thereof
WO2019204419A1 (en) 2018-04-20 2019-10-24 The Medicines Company (San Diego), Llc 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
AU2021266715A1 (en) 2020-05-05 2022-11-17 Qpex Biopharma, Inc. Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2162792T3 (es) * 1991-09-18 2002-01-16 Glaxo Group Ltd Derivados de benzanilida como antagonistas de 5-ht1d.
JP3328936B2 (ja) * 1993-09-03 2002-09-30 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 5ht1dレセプター拮抗薬用インドールおよびインドリン誘導体
JP2001506995A (ja) * 1996-12-19 2001-05-29 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 N−ピペラジン−1−イルフェニル−ベンズアミド誘導体
US6159979A (en) * 1997-04-18 2000-12-12 Smithkline Beecham P.L.C. Bicyclic aryl or a bicyclic heterocyclic ring containing compounds having a combined 5HT1A, 5HT1B and 5HT1D receptor antagonistic activity
AU732863B2 (en) * 1997-04-18 2001-05-03 Smithkline Beecham Plc Indole derivatives having combined 5HT1A, 5HT1B and 5HT1D receptor antagonist activity
GB9725931D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Novel compounds
EP1216239B1 (en) * 1999-09-25 2004-02-11 SmithKline Beecham plc Piperazine derivatives as 5-ht1b antagonists

Also Published As

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

Similar Documents

Publication Publication Date Title
HUP0202787A2 (hu) 5-HT1B antagonista piperazinszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
NO20044731L (no) Kinolin- og isokinolinderivater fremgangsmate for fremstilling derav og anvendelse derav som betennelseshemmere
ECSP066967A (es) Derivados de tetrahidroquinolina y un procedimiento para preparar los mismos
DE60010076D1 (de) Chinolinderivate als antibakterielle mittel
WO2007137030A3 (en) Cns active fused bicycloheterocycle substituted azabicyclic alkane derivatives
DK1678166T3 (da) Proteinkinaseinhibitorer
HUP0203971A2 (hu) Imidazoimidazolok és -triazolok mint gyulladásellenes szerek és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
NO20060664L (no) N-substituerte benzimidazolyl C-kit inhibitorer
HUP0402376A2 (hu) Imidazol-4-karboxamid-származékok, előállításuk és az ezeket tartalmazó, elhízás kezelésére alkalmas gyógyszerkészítmények
DE69930926D1 (de) Benzolsulfonamid-derivate und ihre anwendung als arzneimittel
DE60001623D1 (de) Sulfamoylheteroarylpyrazolverbindungen zur Verwendung als analgetisches/entzündungshemmendes Mittel
NO20061432L (no) N3 alkylerte benzimidazolederivater som MEK-inhibitorer
AR039127A1 (es) Compuesto de quinolina, procedimiento para su preparacion, composicion farmaceutica que lo comprende y uso del mismo para la fabricacion de un medicamento
WO2004069803A3 (en) Mono-acylated o-phenylendiamines derivatives and their use against cancer
NO20060665L (no) N-substituerte pyrazolyl-amidyl-benzimidazolyl C-kit inhibitorer
HUP0303070A2 (hu) 3,4-Dihidro-izokinolin-származékok és ezeket hatóanyagként tartalmazó gyógyszerkészítmények
MY129796A (en) Novel anti-inflammatory androstane derivatives
DE602008001725D1 (de) 1-(1-benzylpiperidin-4-yl)benzimidazol-5-carbonsäurederivate zur behandlung von diabetes mellitus
BR0108816A (pt) Derivados de quinolina como antagonistas alfa-2
TR200302047T4 (tr) Anti-iltihabik / analjezik maddeler olarak heteroaril fenil pirazol bileşikleri.
MY139887A (en) Tetrahydronaphthyridine derivatives and a process for preparing the same.
MX2009007954A (es) Derivado de heterocicliden-n-(aril) acetamida.
ATE211740T1 (de) Substituierte indazolderivate
US20170334842A1 (en) Inhibitors of the mitf molecular pathway
AR005233A1 (es) Derivados de 1,2,3,4-tetrahidroquinolina, procesos para su preparacion, una composicion farmaceutica y el uso en la elaboracion de un medicamento

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees