PE20070180A1 - Compuestos de bencilpiperazina como agonistas del receptor gpr38 - Google Patents

Compuestos de bencilpiperazina como agonistas del receptor gpr38

Info

Publication number
PE20070180A1
PE20070180A1 PE2006000888A PE2006000888A PE20070180A1 PE 20070180 A1 PE20070180 A1 PE 20070180A1 PE 2006000888 A PE2006000888 A PE 2006000888A PE 2006000888 A PE2006000888 A PE 2006000888A PE 20070180 A1 PE20070180 A1 PE 20070180A1
Authority
PE
Peru
Prior art keywords
phenyl
methyl
piperidinamine
piperazinyl
fluorophenyl
Prior art date
Application number
PE2006000888A
Other languages
English (en)
Inventor
Christopher Norbert Johnson
David Timothy Macpherson
Steven James Stanway
Geoffrey Stemp
Mervyn Thompson
Susan Marie Westaway
Original Assignee
Glaxo Group Ltd
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 GB0515381A external-priority patent/GB0515381D0/en
Priority claimed from GB0611469A external-priority patent/GB0611469D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE20070180A1 publication Critical patent/PE20070180A1/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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE BENCILPIPERAZINA DE FORMULA (I), EN DONDE A ES FENILO O HETEROARILO DE 6 MIEMBROS OPCIONALMENTE SUSTITUIDO CON, ALQUILO O ALCOXI(C1-C4); R1 Y R2 SON INDEPENDIENTEMENTE H O ALQUILO(C1-C4); R3 ES FENILO O HETEROARILO DE 5 A 6 MIEMBROS OPCIONALMENTE SUSTITUIDO; X ES (CR4R5)n; n ES 1 O 2; Y ES NH, O O CH2; R4 Y R5 SON INDEPENDIENTEMENTE H Y ALQUILO(C1-C4); LOS CARBONOS C* DE LA PIPERAZINA TIENEN LA CONFIGURACION 3R,5S. SON PREFERIDOS: 1-[(4-{[(3R,5S)-3,5-DIMETIL-1-PIPERAZINIL]METIL}FENIL)ACETIL]-N-(4-FLUOROFENIL)-4-PIPERIDINAMINA, N-(3-FLUOROFENIL)-1-[(4-{[(3S)-3-METIL-PIPERAZINIL]METIL}FENIL)ACEIL]-4-PIPERIDINAMINA, N-(4-FLUOROFENIL)-1-[(4-{[(3S)-3-METIL-1-PIPERAZINIL]METIL}-FENIL)ACETIL]-4-PIPERIDINAMINA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON AGONISTAS PARCIAL O TOTAL DEL RECEPTOR GPR38 (RECEPTOR ACOPLADO A PROTEINA G), Y SON UTILES PARA EL TRATAMIENTO DE TRASTORNOS GASTROINTESTINALES ASOCIADOS CON HOPOMOTILIDAD, TAL COMO TRANSTORNOS FUNCIONALES DEL INTESTINO, DISPEPSIA FUNCIONAL O SINDROME DE INTESTINO IRRITABLE
PE2006000888A 2005-07-26 2006-07-24 Compuestos de bencilpiperazina como agonistas del receptor gpr38 PE20070180A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0515381A GB0515381D0 (en) 2005-07-26 2005-07-26 Compounds
GB0611469A GB0611469D0 (en) 2006-06-09 2006-06-09 Compounds

Publications (1)

Publication Number Publication Date
PE20070180A1 true PE20070180A1 (es) 2007-04-25

Family

ID=37560776

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000888A PE20070180A1 (es) 2005-07-26 2006-07-24 Compuestos de bencilpiperazina como agonistas del receptor gpr38

Country Status (28)

Country Link
US (2) US8536182B2 (es)
EP (2) EP2441763A1 (es)
JP (1) JP4938777B2 (es)
KR (1) KR101281435B1 (es)
AR (1) AR054508A1 (es)
AU (1) AU2006274212B2 (es)
BR (1) BRPI0613987A2 (es)
CA (1) CA2616513C (es)
CR (1) CR9722A (es)
CY (1) CY1113257T1 (es)
DK (1) DK1907374T3 (es)
EA (1) EA014061B1 (es)
EG (1) EG26235A (es)
ES (1) ES2390812T3 (es)
HR (1) HRP20120833T1 (es)
IL (1) IL188854A (es)
JO (1) JO2747B1 (es)
MA (1) MA29723B1 (es)
MX (1) MX2008001211A (es)
MY (1) MY150098A (es)
NO (1) NO340489B1 (es)
NZ (1) NZ565062A (es)
PE (1) PE20070180A1 (es)
PL (1) PL1907374T3 (es)
PT (1) PT1907374E (es)
SI (1) SI1907374T1 (es)
TW (1) TWI376375B (es)
WO (1) WO2007012479A2 (es)

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GB0611907D0 (en) 2006-06-15 2006-07-26 Glaxo Group Ltd Compounds
SI1907374T1 (sl) * 2005-07-26 2012-11-30 Glaxo Group Ltd Derivati benzilpiperazina uporabni za zdravljenje gastrointestinalnih motenj
GB0524814D0 (en) * 2005-12-05 2006-01-11 Glaxo Group Ltd Compounds
NZ570078A (en) 2006-01-27 2011-10-28 Ms Science Corp Piperidine and piperazine derivatives
MX2009000110A (es) 2006-06-28 2009-01-23 Glaxo Group Ltd Derivados de piperazinilo utiles en el tratamiento de enfermedades mediadas por el receptor grp38.
GB0723317D0 (en) 2007-11-28 2008-01-09 Glaxo Group Ltd Compounds
KR101575703B1 (ko) 2009-02-27 2015-12-10 라퀄리아 파마 인코포레이티드 모틸린 수용체에 대해 작용제 활성을 가진 옥시인돌 유도체
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
CN113292485B (zh) * 2021-06-08 2023-10-27 河南大学 苄基哌嗪脲类trpv1拮抗和mor激动双靶点药物及制备方法和应用

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Also Published As

Publication number Publication date
DK1907374T3 (da) 2012-10-15
CA2616513C (en) 2013-02-19
EA014061B1 (ru) 2010-08-30
MY150098A (en) 2013-11-29
MX2008001211A (es) 2008-03-24
ES2390812T3 (es) 2012-11-16
EA200800421A1 (ru) 2008-06-30
NO20081014L (no) 2008-04-10
WO2007012479A2 (en) 2007-02-01
KR20080037663A (ko) 2008-04-30
US20090054456A1 (en) 2009-02-26
NZ565062A (en) 2011-02-25
CY1113257T1 (el) 2016-04-13
JO2747B1 (en) 2014-03-15
TW200745081A (en) 2007-12-16
CA2616513A1 (en) 2007-02-01
PL1907374T3 (pl) 2012-12-31
JP4938777B2 (ja) 2012-05-23
IL188854A (en) 2013-08-29
AR054508A1 (es) 2007-06-27
US20130317041A1 (en) 2013-11-28
EP2441763A1 (en) 2012-04-18
WO2007012479A3 (en) 2007-04-26
AU2006274212A1 (en) 2007-02-01
EG26235A (en) 2013-05-07
HK1116477A1 (en) 2008-12-24
JP2009502842A (ja) 2009-01-29
AU2006274212B2 (en) 2011-06-09
TWI376375B (en) 2012-11-11
KR101281435B1 (ko) 2013-07-02
BRPI0613987A2 (pt) 2011-03-01
PT1907374E (pt) 2012-11-05
CR9722A (es) 2008-04-10
SI1907374T1 (sl) 2012-11-30
HRP20120833T1 (hr) 2012-11-30
US8536182B2 (en) 2013-09-17
MA29723B1 (fr) 2008-09-01
EP1907374B1 (en) 2012-08-22
EP1907374A2 (en) 2008-04-09
NO340489B1 (no) 2017-05-02
IL188854A0 (en) 2008-04-13

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