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)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU729590B2 (en) * 1996-10-23 2001-02-08 Sanofi-Aventis Cosmetic composition containing a neuropeptide Y receptor antagonist
EP0975584B1 (en) * 1997-04-16 2002-09-25 Arqule, Inc. Synthesis and use of alpha-ketoamide derivatives and arrays
US6143931A (en) 1997-04-16 2000-11-07 Arqule, Inc. Synthesis and use of α-ketoamide derivatives and arrays
US6337332B1 (en) 1998-09-17 2002-01-08 Pfizer Inc. Neuropeptide Y receptor antagonists
US6200990B1 (en) * 1998-12-21 2001-03-13 Alcon Laboratories, Inc. Neuroprotective agents having antioxidant and NMDA antagonist activity
EP1184373A4 (en) * 1999-04-20 2004-10-20 Meiji Seika Kaisha Tricyclic compounds
US6469006B1 (en) * 1999-06-15 2002-10-22 Bristol-Myers Squibb Company Antiviral indoleoxoacetyl piperazine derivatives
MXPA00006605A (en) 1999-07-02 2004-12-09 Pfizer Bicycliccarbonyl indole compounds as anti-inflammatory/analgesic agents.
AU2001234958A1 (en) 2000-02-11 2001-08-20 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
JP2003525901A (en) * 2000-03-09 2003-09-02 イーライ・リリー・アンド・カンパニー Method for treating renal dysfunction with sPLA2 inhibitor
US6900226B2 (en) 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
TWI224101B (en) 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
EP1397130B1 (en) 2001-06-20 2007-07-25 Wyeth Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
US6673829B2 (en) 2001-09-14 2004-01-06 Novo Nordisk A/S Aminoazetidine,-pyrrolidine and -piperidine derivatives
EP1430027B1 (en) 2001-09-14 2010-09-01 High Point Pharmaceuticals, LLC Novel aminoazetidine, -pyrrolidine and -piperidine derivatives
EP1501826B1 (en) 2002-02-01 2006-09-27 F. Hoffman-la Roche AG Substituted indoles as alpha-1 agonists
MXPA05006287A (en) 2002-12-10 2005-09-08 Wyeth Corp Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1).
ES2268480T3 (en) 2002-12-10 2007-03-16 Wyeth ACID DERIVATIVES 3-RENT- AND 3-ARILALQUILO-1H-INDOL-1-IL-ACETICO REPLACED AS INHIBITORS OF THE INHIBITOR OF THE PLASMINOGEN-1 ACTIVATOR (PAI-1).
DE60324183D1 (en) 2002-12-10 2008-11-27 Wyeth Corp Aryl-, aryloxy- und alkyloxysubstituierte 1h-indol-3-yl-glyoxylsäurederivateals inhibitoren des plasminogenaktivatorinhibitors-1 (pai-1)
UA80453C2 (en) 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
BR0316574A (en) 2002-12-10 2005-10-04 Wyeth Corp Substituted 3-carbonyl-1h-indol-1-yl acetic acid derivatives as plasminogen activator inhibitor-1 inhibitors (parent-1)
WO2004054581A2 (en) * 2002-12-13 2004-07-01 Smithkline Beecham Corporation Cyclohexyl compounds as ccr5 antagonists
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2005030754A1 (en) * 2003-09-24 2005-04-07 Janssen Pharmaceutica, N.V. Indole or quinoline derivatives as non-pepticid npy y2 receptor inhibitors useful for the treatment of anxiolytic and depressive disorders and obesity
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7351726B2 (en) 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7420083B2 (en) 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7332521B2 (en) 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
NZ546887A (en) 2003-11-03 2009-04-30 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
JP4996926B2 (en) 2004-02-05 2012-08-08 プロビオドルグ エージー Novel inhibitors of glutaminyl cyclase
CN101039936A (en) 2004-08-23 2007-09-19 惠氏公司 Oxazolo-naphthyl acids as plasminogen activator inhibitor type-1(pai-1) modulators useful in the treatment of thrombosis and cardiovascular diseases
KR20070103744A (en) 2005-01-27 2007-10-24 와이어쓰 Processes and compounds for the preparation of substituted naphthylindole derivatives
EP1919866A2 (en) 2005-08-17 2008-05-14 Wyeth a Corporation of the State of Delaware Substituted indoles and use thereof
WO2007046112A1 (en) * 2005-10-19 2007-04-26 Suven Life Sciences Inc. Arylthioether tryptamine derivatives as functional 5-ht6 ligands
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
CA2679446C (en) 2007-03-01 2016-05-17 Probiodrug Ag New use of glutaminyl cyclase inhibitors
DK2142514T3 (en) 2007-04-18 2015-03-23 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
ES2676289T3 (en) 2008-06-19 2018-07-18 Takeda Pharmaceutical Company Limited Heterocyclic compound and its use
WO2011029920A1 (en) 2009-09-11 2011-03-17 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
BR112012022478B1 (en) 2010-03-10 2021-09-21 Probiodrug Ag HETEROCYCLIC GLUTAMINYL CYCLASE INHIBITORS (QC, EC 2.3.2.5), THEIR PREPARATION PROCESS, AND PHARMACEUTICAL COMPOSITION
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
AU2012253402A1 (en) * 2011-05-12 2013-05-02 Proteostasis Therapeutics, Inc. Proteostasis regulators
US20140301947A1 (en) 2011-06-06 2014-10-09 Imperial Innovations Limited Methods to predict binding affinity of tspo imaging agents to tspo
CN104829465B (en) 2015-02-13 2018-04-27 普济生物科技(台州)有限公司 A kind of preparation method of 4- isopropylaminos-n-butyl alcohol
CN105949135A (en) * 2016-05-10 2016-09-21 湖南欧亚生物有限公司 Synthetic method of selexipag
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
CN111377821A (en) * 2018-12-28 2020-07-07 南京艾德凯腾生物医药有限责任公司 Method for synthesizing 4-isopropylamino-1-butanol

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2931323A1 (en) * 1979-08-02 1981-02-26 Kali Chemie Pharma Gmbh NEW N-AMINOALKYLINDOL DERIVATIVES AND THEIR SALTS
US5264420A (en) * 1990-09-27 1993-11-23 Merck & Co., Inc. Fibrinogen receptor antagonists
US5206382A (en) * 1991-06-27 1993-04-27 Fidia Georgetown Institute For The Neurosciences Indole derivatives, pharmaceutical compositions and methods of treating neurological and psychiatric disorders
WO1993023374A1 (en) * 1992-05-08 1993-11-25 Otsuka Pharmaceutical Factory, Inc. Indole derivative
TW270114B (en) * 1993-10-22 1996-02-11 Hoffmann La Roche
IL115613A0 (en) * 1994-10-20 1996-01-19 Lilly Co Eli Bicyclic neuropeptide y receptor antagonists

Also Published As

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

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