AR017019A1 - COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES - Google Patents

COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES

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Publication number
AR017019A1
AR017019A1 ARP980104021A ARP980104021A AR017019A1 AR 017019 A1 AR017019 A1 AR 017019A1 AR P980104021 A ARP980104021 A AR P980104021A AR P980104021 A ARP980104021 A AR P980104021A AR 017019 A1 AR017019 A1 AR 017019A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
cyano
nitrogen
trifluoromethyl
Prior art date
Application number
ARP980104021A
Other languages
Spanish (es)
Original Assignee
Pfizer Prod Inc
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
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR017019A1 publication Critical patent/AR017019A1/en

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    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic 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
    • 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
    • C07D209/04Indoles; 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Un compuesto derivado de 2-(4-aril o heteroarilpiperazin-1-ilmetil)-1H-indol de formula (I) o sal farmacéuticamente aceptable del mismo, donde lalínea discontinua representa un doble enlace opcional; a es 0 o 1, en el que cuando a es 0, X puedeforma r un doble enlace opcional con el carbono adyacente aV; V es CHR10, en el que R10 es hidrogeno o alquilo C1-6; T es nitrogeno o CH; X es nitrogeno o CR11, en el que R11 es hidrogeno, alquilo C1-6, alcoxi C1-6,hidroxi o ciano; Y y Z son cadauno de el los independientemente nitrogeno o CR12, en el que R12 es hidrogeno, cloro, bromo, trifluorometilo, trifluorometoxi,ciano, alcoxi C1-6 o alquilo C1-6; R1 es hidrogeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano o alquiloC1-6; R2, R6, R7, R8 y R9 estáncada uno de ellos independientemente seleccionados entre hidrogeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano, alcoxi C1-6 y alquiloC1-6; R3 y R4 son cada uno de ellos independientemente hidrogeno oalquilo C1 -6; y R5 es hidrogeno, alcoxi C1-6, trifluorometilo, ciano, alquilo C1-6 oR13CO, en el que R13 es amino, alquil C1-6-amino, (alquilo C1-6)2 amino, alquilo C1-6, arilo C6-10; o cuando a es 1, R1 y R10 se pueden unir con loscarbonos a losque están uni dos para formar un compuesto de formula (II) en la que las líneas discontinuas representan enlaces opcionales; T, X, Y, Z, R2, R3,R4, R5, R6, R7, R8 y R9 son lo definido anteriormente; b es 0 o 1; y A y B son cada uno de ellosindependientemente CH, CH2,oxígeno, azufre, NH o nitrogeno;con la condicion de que cuando X es nitrogeno, el doble enlace opcional entre X y V no existe; con la condicion de que cuando b es 0, el doble enlaceopcional entre A y B no existe; y con lacondicion de que cuando b es 1, A y B no pueden ser ninguno de ellos oxígeno o azufre. Los compuestos antesmencionados son utiles para el tratamiento de trastornos del sistema de la dopamina. Se describen también composiciones y el uso de loscompuestos enla manufactura de medicamentos.A compound derived from 2- (4-aryl or heteroarylpiperazin-1-ylmethyl) -1H-indole of formula (I) or pharmaceutically acceptable salt thereof, where the broken line represents an optional double bond; a is 0 or 1, where when a is 0, X can form an optional double bond with the carbon adjacent to V; V is CHR10, wherein R10 is hydrogen or C1-6 alkyl; T is nitrogen or CH; X is nitrogen or CR11, wherein R11 is hydrogen, C1-6 alkyl, C1-6 alkoxy, hydroxy or cyano; Y and Z are each independently of the nitrogen or CR12, wherein R12 is hydrogen, chlorine, bromine, trifluoromethyl, trifluoromethoxy, cyano, C1-6 alkoxy or C1-6 alkyl; R1 is hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano or C1-6 alkyl; R2, R6, R7, R8 and R9 are one of them independently selected from hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano, C1-6 alkoxy and C1-6 alkyl; R3 and R4 are each independently hydrogen or C1-6alkyl; and R5 is hydrogen, C1-6 alkoxy, trifluoromethyl, cyano, C1-6 alkyl or R13CO, wherein R13 is amino, C1-6 alkyl, (C1-6 alkyl) 2 amino, C1-6 alkyl, C6 aryl -10; or when a is 1, R1 and R10 can be joined with the carbons to which they are joined to form a compound of formula (II) in which the dashed lines represent optional bonds; T, X, Y, Z, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined above; b is 0 or 1; and A and B are each independently CH, CH2, oxygen, sulfur, NH or nitrogen, with the proviso that when X is nitrogen, the optional double bond between X and V does not exist; with the proviso that when b is 0, the optional double bond between A and B does not exist; and with the proviso that when b is 1, A and B cannot be any of them oxygen or sulfur. The aforementioned compounds are useful for the treatment of disorders of the dopamine system. Compositions and the use of the compounds in the manufacture of medicaments are also described.

ARP980104021A 1997-08-15 1998-08-13 COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES AR017019A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5576497P 1997-08-15 1997-08-15

Publications (1)

Publication Number Publication Date
AR017019A1 true AR017019A1 (en) 2001-08-22

Family

ID=22000003

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980104021A AR017019A1 (en) 1997-08-15 1998-08-13 COMPOUNDS DERIVED FROM 2- (4-ARIL OR HETEROARILPIPERAZIN-1-ILMETIL) -1H-INDOL, COMPOSITIONS AND ITS USE IN THE MANUFACTURE OF MEDICINES

Country Status (30)

Country Link
EP (1) EP1003739A2 (en)
JP (1) JP2002536291A (en)
KR (1) KR20010022507A (en)
CN (1) CN1265660A (en)
AP (1) AP9801321A0 (en)
AR (1) AR017019A1 (en)
AU (1) AU8457298A (en)
BG (1) BG104069A (en)
BR (1) BR9811557A (en)
CA (1) CA2297486C (en)
CO (1) CO4960656A1 (en)
DZ (1) DZ2583A1 (en)
EA (1) EA200000023A1 (en)
HR (1) HRP980441A2 (en)
HU (1) HUP0003425A3 (en)
ID (1) ID23803A (en)
IL (1) IL133960A0 (en)
IS (1) IS5336A (en)
MA (1) MA24632A1 (en)
NO (1) NO20000722D0 (en)
OA (1) OA11286A (en)
PA (1) PA8457001A1 (en)
PE (1) PE106299A1 (en)
PL (1) PL338947A1 (en)
SK (1) SK1352000A3 (en)
TN (1) TNSN98151A1 (en)
TR (1) TR200000414T2 (en)
UY (1) UY25144A1 (en)
WO (1) WO1999009025A2 (en)
ZA (1) ZA987304B (en)

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WO1999021834A1 (en) * 1997-10-27 1999-05-06 Neurosearch A/S Heteroaryl diazacycloalkanes as cholinergic ligands at nicotinic acetylcholine receptors
EP0953567A3 (en) 1998-04-29 2003-04-02 Pfizer Products Inc. Bicyclic substituted piperazine-, piperidine- and tetrahydropyridine derivatives, their preparation and their use as agents with central dopaminergic (dopamine D4 receptor) activity
SK11072002A3 (en) * 1999-12-30 2003-03-04 H. Lundbeck A/S Halo-substituted 4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives, pharmaceutical composition containing the same and use thereof
GB0017952D0 (en) * 2000-07-22 2000-09-13 Univ Manchester Treatment of dyskinesia
EP1177792A3 (en) 2000-07-27 2002-10-23 Pfizer Products Inc. Dopamine D4 Ligands for the treatment of novelty-seeking disorders
WO2002072548A2 (en) * 2001-03-09 2002-09-19 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
US7504426B2 (en) 2002-09-06 2009-03-17 Janssen Pharmaceutica N.V. Heterocyclic compounds
WO2004108671A1 (en) * 2003-06-06 2004-12-16 Suven Life Sciences Limited Substituted indoles with serotonin receptor affinity, process for their preparation and pharmaceutical compositions containing them
WO2005095338A1 (en) 2004-03-30 2005-10-13 Takeda Pharmaceutical Company Limited Alkoxyphenylpropanoic acid derivatives
US7618980B2 (en) 2004-07-14 2009-11-17 Bristol-Myers Squibb Company Pyrrolo(oxo)quinolines as 5HT ligands
US7572805B2 (en) 2004-07-14 2009-08-11 Bristol-Myers Squibb Company Pyrrolo(oxo)isoquinolines as 5HT ligands
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Fast Dissociting Dopamine 2 Receptor Antagonists
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Fast Dissociating Dopamine 2 Receptor Antagonists
JO2849B1 (en) * 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Fast -Dissociating Dopamine 2 Receptor Antagonists
RS52518B (en) 2007-04-23 2013-04-30 Janssen Pharmaceutica N.V. 4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
EP2148879B1 (en) 2007-04-23 2012-11-28 Janssen Pharmaceutica, N.V. Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
CN102159554B (en) 2008-07-03 2014-09-24 詹森药业有限公司 Substituted 6- (1-piperazinyl) -pyridazines as 5-ht6 receptor antagonists
HUE033768T2 (en) 2008-07-31 2017-12-28 Janssen Pharmaceutica Nv Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists
EP3686196B1 (en) * 2017-09-20 2024-06-12 Hangzhou Innogate Pharma Co., Ltd. Polycyclic compound acting as ido inhibitor and/or ido-hdac dual inhibitor
CN115427404A (en) * 2020-04-22 2022-12-02 艾尼莫生物科技公司 Collagen 1 translation inhibitors and methods of use thereof

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DE69217224T2 (en) * 1991-07-03 1997-06-05 Pharmacia & Upjohn Co., Kalamazoo, Mich. SUBSTITUTED INDOLE AS ANTI-AIDS PHARMACEUTICAL PREPARATIONS
JPH05255089A (en) * 1991-12-18 1993-10-05 Sanwa Kagaku Kenkyusho Co Ltd Antiviral agent
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AU6215594A (en) * 1993-03-18 1994-10-11 Merck Sharp & Dohme Limited Indole derivatives as dopamine d4 antagonists
GB9305644D0 (en) * 1993-03-18 1993-05-05 Merck Sharp & Dohme Therapeutic agents
US5814644A (en) * 1993-04-15 1998-09-29 Merck Sharp & Dohme, Ltd. Indole derivatives as dopamine D4 antagonists
DE4414113A1 (en) * 1994-04-22 1995-10-26 Merck Patent Gmbh 3-indolylpiperidines
TW406075B (en) * 1994-12-13 2000-09-21 Upjohn Co Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds
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TW504510B (en) * 1996-05-10 2002-10-01 Janssen Pharmaceutica Nv 2,4-diaminopyrimidine derivatives

Also Published As

Publication number Publication date
EP1003739A2 (en) 2000-05-31
IL133960A0 (en) 2001-04-30
IS5336A (en) 2000-01-11
ZA987304B (en) 2000-02-14
ID23803A (en) 2000-05-11
PL338947A1 (en) 2000-12-04
DZ2583A1 (en) 2003-02-22
PE106299A1 (en) 1999-11-02
WO1999009025A2 (en) 1999-02-25
PA8457001A1 (en) 2000-09-29
TNSN98151A1 (en) 2005-03-15
AP9801321A0 (en) 2000-02-14
WO1999009025A3 (en) 1999-04-15
BG104069A (en) 2001-05-31
HUP0003425A3 (en) 2002-02-28
CA2297486A1 (en) 1999-02-25
UY25144A1 (en) 2000-12-29
HRP980441A2 (en) 1999-04-30
HUP0003425A2 (en) 2001-10-28
CN1265660A (en) 2000-09-06
KR20010022507A (en) 2001-03-15
OA11286A (en) 2003-10-22
CA2297486C (en) 2005-05-03
SK1352000A3 (en) 2000-08-14
CO4960656A1 (en) 2000-09-25
AU8457298A (en) 1999-03-08
MA24632A1 (en) 1999-04-01
NO20000722L (en) 2000-02-14
TR200000414T2 (en) 2000-08-21
NO20000722D0 (en) 2000-02-14
EA200000023A1 (en) 2000-08-28
JP2002536291A (en) 2002-10-29
BR9811557A (en) 2000-08-22

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