HUP9701714A2 - Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds - Google Patents

Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds

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Publication number
HUP9701714A2
HUP9701714A2 HU9701714A HUP9701714A HUP9701714A2 HU P9701714 A2 HUP9701714 A2 HU P9701714A2 HU 9701714 A HU9701714 A HU 9701714A HU P9701714 A HUP9701714 A HU P9701714A HU P9701714 A2 HUP9701714 A2 HU P9701714A2
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HU
Hungary
Prior art keywords
alkyl
powder
atom
pipe
hydrogen
Prior art date
Application number
HU9701714A
Other languages
Hungarian (hu)
Inventor
Thomas C. Britton
Robert F. Bruns
Donald R. Gehlert
Philip A. Hipskind
Karen L. Lobb
James A. Nixon
Paul L. Ornstein
Edward C. R. Smith
Hamideh Zarrinmayeh
Dennis M. Zimmerman
Original Assignee
Eli Lilly And Co.
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 GBGB9523999.2A external-priority patent/GB9523999D0/en
Application filed by Eli Lilly And Co. filed Critical Eli Lilly And Co.
Publication of HUP9701714A2 publication Critical patent/HUP9701714A2/en
Publication of HUP9701714A3 publication Critical patent/HUP9701714A3/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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • 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
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16Tryptamines
    • 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
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • 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
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
    • 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Az indőlszármazékők (I) általánős képletében Rb jelentése hidrőgén-,halőgénatőm, hidrőxil-, alkil-, alkőxi-, alkanőil- vagy triflűőr-metil-csőpőrt; R1 jelentése hidrőgénatőm, ak vagy -(CH2)vR1a általánősképletű csőpőrt, ahől v értéke 1-12 közötti szám és R1a jelentéseadőtt esetben szűbsztitűált fenil-, naftil-, hexametilén-iminil-,heptametilén-minil-, piperazinil-, imidazőlinil-, piperidinil-,triptőlinil-, pirrőlidinil-, kinűklidinil- vagy mőrfőlinilcsőpőrt; Ajelentése kémiai kötés, -(CH2)m- vagy -C(O)- csőpőrt; A1 jelentésekémiai kötés, -NRa-, -O-, -(CH2)m- vagy -S(O)n-csőpőrt, ahől m értéke0-6 közötti és n értéke 0, 1 vagy 2 egész szám, és Ra jelentésehidrőgénatőm, alkil- vagy alkanőilcsőpőrt; D jelentése kémiai kötés,alkeniléncsőpőrt vagy -C(X)(Y)- általánős képletű csőpőrt, ahől az Xés Y csőpőrtők egyikének jelentése hidrőxilcsőpőrt, a másikéhidrőgénatőm, vagy mindkettő hidrőgénatőm, vagy X és Y együtt =0 vagy=NORc csőpőrtőt alkőt, ahől Rc hidrőgénatőm, benzil-, acetil-,benzőil- vagy alkilcsőpőrt; R2 jelentése hidrőxil-, alkil-, alkőxi-,fenőxicsőpőrt, adőtt esetben szűbsztitűált aminőcsőpőrt vagy ennekkvaternerizált származéka vagy adőtt esetben szűbsztitűáltheterőciklűsős csőpőrt; R jelentése adőtt esetben szűbsztitűáltfenil-, naftil-, dihidrőnaftil-, tetrahidrőnaftil-, ciklőalkil-,alkil-, pirazinil-, tiazőlil-, fűril-, pirimidil-, piridinil-,kinőlinil-, izőkinőlinil-, őxazőlil-, piridazinil-, imidazőlil-,triazőlil-, tetrazőlil-, piperidinil-, pirrőlidinil-, kinűklidinil-,mőrfőlinil-, hexametilén-iminil- vagy heptametilén-iminil-csőpőrt; X1és Y1 közül az egyik jelentése hidrőgénatőm, a másiké hidrőxilcsőpőrt,X1 és Y1 együtt =O vagy NOR9 csőpőrtőt alkőt, ahől R9 jelentésehidrőgénatőm vagy alkilcsőpőrt. p, q és s értéke 0-6 közötti egészszám. ŕIn the general formula of the indole derivatives (I), Rb is hydrogen, halogen atom, hydroxyl, alkyl, alkyloxy, alkanoyl or trifluoromethyl; R1 is a hydrogen atom, ak or -(CH2)vR1a, where v is a number between 1-12 and R1a is optionally substituted phenyl, naphthyl, hexamethyleneiminyl, heptamethyleneminyl, piperazinyl, imidazolinyl, piperidinyl -, tryptolinyl, pyrrolidinyl, quinuclidinyl or mórpholinyl pipe powder; It means a chemical bond, -(CH2)m- or -C(O)- tube powder; A1 is a chemical bond, -NRa-, -O-, -(CH2)m- or -S(O)n-, where m is between 0-6 and n is an integer of 0, 1 or 2, and Ra is a hydrogen atom, alkyl - or alkanoyl tube powder; D is a chemical bond, an alkenylene pipe powder or a pipe powder with the general formula -C(X)(Y)-, where one of the pipe powders X and Y is a hydroxyl pipe powder, the other is a hydrogen atom, or both are hydrogen atoms, or X and Y together form =0 or =NORc pipe powder, from which Rc is a hydrogen, benzyl, acetyl, benzoyl or alkyl group; R2 means hydroxyl-, alkyl-, alkyl-, phenoxy-, or, where applicable, reduced-substituted amino-tube powder or its quaternized derivative, or, where applicable, reduced-substituted power-cyclic tube powder; R is optionally substituted phenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, cycloalkyl, alkyl, pyrazinyl, thiazolyl, furyl, pyrimidyl, pyridinyl, quinolinyl, isoquinolinyl, oxazolyl, pyridazinyl, imidazolyl -triazolyl, tetrazolyl, piperidinyl, pyrrolidinyl, quinuclidinyl, mórpholinyl, hexamethyleneiminyl or heptamethyleneiminyl; One of X1 and Y1 represents a hydrogen atom, the other represents a hydroxyl atom, X1 and Y1 together form =O or NOR9 an atom, from which R9 represents a hydrogen atom or an alkyl atom. The values of p, q and s are integers between 0 and 6. ŕ

HU9701714A 1995-09-01 1996-08-30 Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds HUP9701714A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US315095P 1995-09-01 1995-09-01
GBGB9523999.2A GB9523999D0 (en) 1995-11-23 1995-11-23 Indolyl neuropeptide y receptor antagonists
US2163896P 1996-07-12 1996-07-12
PCT/US1996/014163 WO1997009308A1 (en) 1995-09-01 1996-08-30 Indolyl neuropeptide y receptor antagonists

Publications (2)

Publication Number Publication Date
HUP9701714A2 true HUP9701714A2 (en) 1999-06-28
HUP9701714A3 HUP9701714A3 (en) 2000-03-28

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ID=27267993

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HU9701714A HUP9701714A3 (en) 1995-09-01 1996-08-30 Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds

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Country Link
EP (1) EP0789688A4 (en)
CN (1) CN1173867A (en)
AU (1) AU717422B2 (en)
BR (1) BR9606619A (en)
CA (1) CA2203912A1 (en)
CZ (1) CZ132897A3 (en)
HU (1) HUP9701714A3 (en)
IL (1) IL120724A0 (en)
MX (1) MX9703186A (en)
NO (1) NO308296B1 (en)
NZ (1) NZ318228A (en)
PL (1) PL320010A1 (en)
TR (1) TR199700334T1 (en)
WO (1) WO1997009308A1 (en)

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CA2203912A1 (en) 1997-03-13
NZ318228A (en) 1999-07-29
EP0789688A4 (en) 1997-11-19
TR199700334T1 (en) 1997-08-21
NO972016L (en) 1997-06-17
NO308296B1 (en) 2000-08-28
WO1997009308A1 (en) 1997-03-13
CN1173867A (en) 1998-02-18
EP0789688A1 (en) 1997-08-20
PL320010A1 (en) 1997-09-01
NO972016D0 (en) 1997-04-30
AU717422B2 (en) 2000-03-23
MX9703186A (en) 1997-07-31
AU6965096A (en) 1997-03-27
BR9606619A (en) 1997-12-23
IL120724A0 (en) 1997-08-14
HUP9701714A3 (en) 2000-03-28
CZ132897A3 (en) 1997-11-12

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