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PE20020253A1 - 3-AZABICYCLE DERIVATIVES [3.1.0] HEXANE AS LIGANDS OF OPIACEAN RECEPTORS - Google Patents

3-AZABICYCLE DERIVATIVES [3.1.0] HEXANE AS LIGANDS OF OPIACEAN RECEPTORS

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Publication number
PE20020253A1
PE20020253A1 PE2001000604A PE2001000604A PE20020253A1 PE 20020253 A1 PE20020253 A1 PE 20020253A1 PE 2001000604 A PE2001000604 A PE 2001000604A PE 2001000604 A PE2001000604 A PE 2001000604A PE 20020253 A1 PE20020253 A1 PE 20020253A1
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PE
Peru
Prior art keywords
alkyl
ethyl
hexane
derivatives
halo
Prior art date
Application number
PE2001000604A
Other languages
Spanish (es)
Inventor
Bernard Joseph Banks
Douglas James Critcher
Stephen Paul Gibson
David Morris Gethin
Ashley Edward Fenwick
Original Assignee
Pfizer
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of PE20020253A1 publication Critical patent/PE20020253A1/en

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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
    • C07D401/12Heterocyclic 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
    • 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
    • A61P1/08Drugs 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS 3-AZABICICLO[3.1.0]HEXANO DE FORMULA I DONDE Ar ES FENILO OPCIONALMENTE CONDENSADO CON BENCENO O UN ANILLO HETEROARILO DE 5 A 6 MIEMBROS; R1 ES H, HALO, NO2, NH2, NY2WY1, HET, AD, OE, ENTRE OTROS; Y2 ES H, ALQUILO C1-C6, ALQUENILO C3-C6, ENTRE OTROS; W ES SO2, CO, C(O)O, P(Y1)=S, ENTRE OTROS; Y1 ES ALQUILO C1-C10 CON HALOGENO, OH, ALCOXI C1-C4, ALCANOILOXI C1-C6, ENTRE OTROS; HET ES HETEROCICLICO CON 4 HETEROATOMOS SELECCIONADOS DE N, O, S QUE PUEDE COMPRENDER HASTA 3 ANILLOS SUSTITUIDOS CON ALQUILO C1-C6, ALCOXI C1-C6, ENTRE OTROS; A ES ALQUILENO C1-C4, ALQUENILENO C2-C4, ALQUINILENO C2-C4 CON ALQUILO C1-C4, ALCOXI C1-C4, HALOGENO, OH; D ES H, OH, CN, ENTRE OTROS; E ES H, CONR23R23, ENTRE OTROS. R23 ES H, ALQUILO C1-C4, HALOALQUILO C1-C4; R2 ES H, HALO; R3 ES H, CN, HALO; R4 ES ALQUILO C1-C10, ALQUENILO; R5 Y R8 SON H, ALQUILO C1-C6; R6, R7, R9 Y R10 SON H; n ES 0-2; q ES 0-1. SON COMPUESTOS PREFERIDOS N-(3-{6-ETIL-3-[2-(2-HIDROXIETOXI)-ETIL]-3-AZABICICLO-[3.1.0]HEX-6-IL}-FENIL)METANOSULFONAMIDA, N-(3-{3-{2-[2-(DIMETILAMINO)ETOXI)-ETIL]-6-ETIL-3-AZABICICLO-[3.1.0]HEX-6-IL}-FENIL)METANOSULFONAMIDA, ENTRE OTROS. LOS DERIVADOS DE 3-AZABICICLO[3.1.0]HEXANO SON LIGANDOS DE RECEPTORES OPIACEOS Y SON UTILES PARA EL TRATAMIENTO DEL SINDROME DEL INTESTINO IRRITABLE, ESTRENIMIENTO, NAUSEAS, VOMITOSREFERS TO 3-AZABYCYCLE [3.1.0] HEXANE DERIVATIVES OF FORMULA I WHERE Ar IS PHENYL OPTIONALLY CONDENSED WITH BENZENE OR A 5 TO 6 MEMBER HETEROARYL RING; R1 IS H, HALO, NO2, NH2, NY2WY1, HET, AD, OE, AMONG OTHERS; Y2 IS H, C1-C6 ALKYL, C3-C6 ALKYL, AMONG OTHERS; W IS SO2, CO, C (O) O, P (Y1) = S, AMONG OTHERS; Y1 IS C1-C10 ALKYL WITH HALOGEN, OH, C1-C4 ALCOXY, C1-C6 ALKANOYLOXY, AMONG OTHERS; HET IS HETEROCYCLIC WITH 4 HETEROATOMS SELECTED FROM N, O, S WHICH CAN INCLUDE UP TO 3 RINGS REPLACED WITH C1-C6 ALKYL, C1-C6 ALCOXI, AMONG OTHERS; A IS C1-C4 ALKYLENE, C2-C4 ALKYLENE, C2-C4 ALKYLENE WITH C1-C4 ALKYL, C1-C4 ALCOXY, HALOGEN, OH; D IS H, OH, CN, AMONG OTHERS; E IS H, CONR23R23, AMONG OTHERS. R23 IS H, C1-C4 ALKYL, C1-C4 HALOALKYL; R2 IS H, HALO; R3 IS H, CN, HALO; R4 IS C1-C10 ALKYL, ALKENYL; R5 AND R8 ARE H, C1-C6 ALKYL; R6, R7, R9 AND R10 ARE H; n IS 0-2; q IS 0-1. PREFERRED COMPOUNDS ARE N- (3- {6-ETHYL-3- [2- (2-HYDROXYETOXY) -ETHYL] -3-AZABICYCLO- [3.1.0] HEX-6-IL} -PHENYL) METHANOSULFONAMIDE, N- ( 3- {3- {2- [2- (DIMETHYLAMINO) ETHOXY) -ETHYL] -6-ETHYL-3-AZABICYCLE- [3.1.0] HEX-6-IL} -PHENYL) METHANOSULFONAMIDE, AMONG OTHERS. THE DERIVATIVES OF 3-AZABICYCLO [3.1.0] HEXANE ARE BINDERS OF OPIOUS RECEPTORS AND ARE USEFUL FOR THE TREATMENT OF THE SYNDROME OF THE IRRITABLE INTESTINE, STRENGTH, NAUSEA, VOMITING

PE2001000604A 2000-06-23 2001-06-21 3-AZABICYCLE DERIVATIVES [3.1.0] HEXANE AS LIGANDS OF OPIACEAN RECEPTORS PE20020253A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0015562.2A GB0015562D0 (en) 2000-06-23 2000-06-23 Heterocycles

Publications (1)

Publication Number Publication Date
PE20020253A1 true PE20020253A1 (en) 2002-04-08

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ID=9894368

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Application Number Title Priority Date Filing Date
PE2001000604A PE20020253A1 (en) 2000-06-23 2001-06-21 3-AZABICYCLE DERIVATIVES [3.1.0] HEXANE AS LIGANDS OF OPIACEAN RECEPTORS

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Country Link
EP (1) EP1292574A1 (en)
JP (1) JP2004512263A (en)
KR (1) KR20040002386A (en)
CN (1) CN1639121A (en)
AP (1) AP2002002698A0 (en)
AR (1) AR028969A1 (en)
AU (1) AU781837B2 (en)
BG (1) BG107329A (en)
BR (1) BR0111867A (en)
CA (1) CA2412188A1 (en)
CZ (1) CZ20023967A3 (en)
DO (1) DOP2001000187A (en)
DZ (1) DZ3368A1 (en)
EA (1) EA005117B1 (en)
GB (1) GB0015562D0 (en)
HR (1) HRP20020998A2 (en)
HU (1) HUP0301228A3 (en)
IL (1) IL153427A0 (en)
IS (1) IS6637A (en)
MA (1) MA26915A1 (en)
MX (1) MXPA02012878A (en)
NO (1) NO20026168L (en)
NZ (1) NZ523141A (en)
OA (1) OA12293A (en)
PA (1) PA8519401A1 (en)
PE (1) PE20020253A1 (en)
PL (1) PL365956A1 (en)
SK (1) SK17172002A3 (en)
TN (1) TNSN01094A1 (en)
UA (1) UA73176C2 (en)
UY (1) UY26787A1 (en)
WO (1) WO2001098267A1 (en)
YU (1) YU91802A (en)
ZA (1) ZA200210278B (en)

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CN1946714B (en) * 2004-02-23 2011-06-15 葛兰素集团有限公司 Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine d3 receptors
GB0507680D0 (en) 2005-04-15 2005-05-25 Glaxo Group Ltd Compounds
US7807698B2 (en) 2005-06-14 2010-10-05 Glaxo Group Limited Azabicyclo[3.1.0]hexane derivatives as modulators of the dopamine D3 receptor
WO2007113258A1 (en) * 2006-04-03 2007-10-11 Glaxo Group Limited Azabicyclo [3. 1. o] hexane derivatives as modulators of dopamine d3 receptors
ES2393815T3 (en) 2007-03-30 2012-12-28 Tioga Pharmaceuticals, Inc. Kappa opioid agonists for the treatment of irritable bowel syndrome with predominant and alternating diarrhea
TWI423801B (en) * 2007-08-27 2014-01-21 Theravance Inc 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists
JP5736040B2 (en) 2010-06-11 2015-06-17 ローズ テクノロジーズ Transition metal catalyzed process and its use for the preparation of N-allyl compounds
BR112013007566A2 (en) 2010-09-28 2016-08-02 Panacea Biotec Ltd new bicyclic compounds
WO2015076310A1 (en) * 2013-11-20 2015-05-28 株式会社 三和化学研究所 Novel 3-azabicyclo[3.1.0]hexane derivative and use thereof for medical purposes
MX388953B (en) 2015-05-20 2025-03-20 Ube Industries NOVEL 3-AZABICICLO[3.1.0]HEXANE DERIVATIVE SALT CRYSTAL AND MEDICATIONAL USES THEREOF.
WO2018152286A1 (en) 2017-02-17 2018-08-23 Trevena, Inc. 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same
KR20190129867A (en) * 2017-02-17 2019-11-20 트레베나, 인코포레이티드. 5-membered aza-heterocycle-containing delta-opioid receptor modulating compounds, and methods of using and preparing the same
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CN108250088B (en) * 2018-01-04 2020-10-30 四川之江高新材料股份有限公司 The preparation method of N,N,N'-trimethyl-N'-hydroxyethyl bisaminoethyl ether
CN115825305B (en) * 2022-10-21 2024-09-20 昆明理工大学 Molecularly imprinted solid-phase microextraction fiber and preparation method and application thereof

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Also Published As

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HUP0301228A2 (en) 2003-08-28
PL365956A1 (en) 2005-01-24
BG107329A (en) 2003-07-31
UY26787A1 (en) 2002-01-31
CN1639121A (en) 2005-07-13
JP2004512263A (en) 2004-04-22
PA8519401A1 (en) 2002-12-30
MA26915A1 (en) 2004-12-20
BR0111867A (en) 2003-07-01
AR028969A1 (en) 2003-05-28
NO20026168L (en) 2003-02-18
TNSN01094A1 (en) 2005-11-10
WO2001098267A1 (en) 2001-12-27
EP1292574A1 (en) 2003-03-19
HRP20020998A2 (en) 2004-02-29
YU91802A (en) 2006-05-25
NO20026168D0 (en) 2002-12-20
MXPA02012878A (en) 2003-05-14
DOP2001000187A (en) 2002-03-30
OA12293A (en) 2004-03-18
DZ3368A1 (en) 2001-12-27
IS6637A (en) 2002-11-28
ZA200210278B (en) 2003-12-19
UA73176C2 (en) 2005-06-15
AU781837B2 (en) 2005-06-16
NZ523141A (en) 2005-06-24
AU6259101A (en) 2002-01-02
WO2001098267A8 (en) 2003-02-27
IL153427A0 (en) 2003-07-06
GB0015562D0 (en) 2000-08-16
EA200201269A1 (en) 2003-06-26
KR20040002386A (en) 2004-01-07
AP2002002698A0 (en) 2002-12-31
CZ20023967A3 (en) 2004-02-18
SK17172002A3 (en) 2004-09-08
CA2412188A1 (en) 2001-12-27
HUP0301228A3 (en) 2005-08-29
EA005117B1 (en) 2004-10-28

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