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UY25144A1 - DERIVATIVES OF 2- (4-ARIL OR HETEROARIL-PIPERAZIN-1-ILMETIL) -1H -INDOL - Google Patents

DERIVATIVES OF 2- (4-ARIL OR HETEROARIL-PIPERAZIN-1-ILMETIL) -1H -INDOL

Info

Publication number
UY25144A1
UY25144A1 UY25144A UY25144A UY25144A1 UY 25144 A1 UY25144 A1 UY 25144A1 UY 25144 A UY25144 A UY 25144A UY 25144 A UY25144 A UY 25144A UY 25144 A1 UY25144 A1 UY 25144A1
Authority
UY
Uruguay
Prior art keywords
alkyl
trifluoromethyl
dopamine
piperazin
mammal
Prior art date
Application number
UY25144A
Other languages
Spanish (es)
Inventor
Hans Rollema
Stevin Howard Zorn
Patricia Ann Seymour
Mark Jerome Majechrzak
Anton Franz Josef Fliri
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 UY25144A1 publication Critical patent/UY25144A1/en

Links

Classifications

    • 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

Se trata de compuestos de fórmula l (como por ejemplo: 2-[4-(3-trifluorometil-fenil)-piperazin-1-ilmetil]-1H-indol) o la sal farmacéuticamente aceptable del mismo, donde la lines discontinua representa un doble enlace opcional; a es 0 ó 1 cuando a es 0, X puede formar un doble enlace opcional con el carbono adyacente a V; T es N ó CH; V es CHR10; X es N o CR11; Y, Z pueden ser N ó CR12;. R1 es H, F, Cl, Br, trifluorometilo, trifluorometoxi, CN, o alquilo; R2, R6, R7, R8 y R9 están cada uno de ellos seleccionados entre H, F, Cl, CN, alquilo ó alcoxilo; R3 y R4 significan H ó alquilo y R5 es H, alcoxi, trifluorometilo, CN, alquilo o R13CO. Un procedimiento para tratar un trastorno del sistema de dopamina en un mamifero,el cual incluye trastornos psicóticos, del movimiento, gastrointestinales, abuso de sustancias químicas, trastornos vasculares y cardiovasculares, oculares y del sueno, que comprende la administración a dicho mamifero de un cantidad de un compuesto selectivo del receptor D4 de dopamina o una sal farmacéuticamente aceptable del mismo, junto con uno o más agonistas del receptor D1, D3, o D5 de la dopamina, que es eficaz para dicho trastorno.These are compounds of formula l (such as: 2- [4- (3-trifluoromethyl-phenyl) -piperazin-1-ylmethyl] -1H-indole) or the pharmaceutically acceptable salt thereof, where the dashed lines represent a optional double bond; a is 0 or 1 when a is 0, X can form an optional double bond with the carbon adjacent to V; T is N or CH; V is CHR10; X is N or CR11; Y, Z can be N or CR12 ;. R1 is H, F, Cl, Br, trifluoromethyl, trifluoromethoxy, CN, or alkyl; R2, R6, R7, R8 and R9 are each selected from H, F, Cl, CN, alkyl or alkoxy; R3 and R4 signify H or alkyl and R5 is H, alkoxy, trifluoromethyl, CN, alkyl or R13CO. A method of treating a disorder of the dopamine system in a mammal, which includes psychotic, movement, gastrointestinal, chemical abuse, vascular and cardiovascular, eye and sleep disorders, comprising administering to said mammal an amount of a dopamine D4 receptor selective compound or a pharmaceutically acceptable salt thereof, together with one or more dopamine D1, D3, or D5 receptor agonists, which is effective for said disorder.

UY25144A 1997-08-15 1998-08-17 DERIVATIVES OF 2- (4-ARIL OR HETEROARIL-PIPERAZIN-1-ILMETIL) -1H -INDOL UY25144A1 (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
UY25144A1 true UY25144A1 (en) 2000-12-29

Family

ID=22000003

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25144A UY25144A1 (en) 1997-08-15 1998-08-17 DERIVATIVES OF 2- (4-ARIL OR HETEROARIL-PIPERAZIN-1-ILMETIL) -1H -INDOL

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)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EE04588B1 (en) * 1997-10-27 2006-02-15 Neurosearch A/S Heteroaryl diazacycloalkanes as cholinergic ligands for acetylcholine nicotine receptors, their use as pharmaceuticals and pharmaceutical composition containing them
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
DE60011817T2 (en) 1999-12-30 2005-07-14 H. Lundbeck A/S 4-PHENYL-1-PIPERAZINYL, -PIPERIDINYL AND -ETRAHYDROPYRIDYL DERIVATIVES
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
US6803362B2 (en) 2001-03-09 2004-10-12 Ortho-Mcneil Pharmaceutical Inc. Heterocyclic compounds
PL377087A1 (en) 2002-09-06 2006-01-23 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
EP1731505B1 (en) 2004-03-30 2015-01-14 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
MX2009011416A (en) 2007-04-23 2009-11-05 Janssen Pharmaceutica Nv Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists.
CN101663292A (en) 2007-04-23 2010-03-03 詹森药业有限公司 4-Alkoxypyridazine derivatives as rapidly dissociating dopamine 2 receptor antagonists
BRPI0915834A2 (en) 2008-07-03 2015-11-03 Janssen Pharmaceutica Nv Substituted 6- (1-piperazinyl) -pyridazines as 5-ht6 receptor antagonists
AU2009275887B2 (en) 2008-07-31 2013-06-20 Janssen Pharmaceutica Nv Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists
CN109843872B (en) * 2017-09-20 2022-08-30 杭州英创医药科技有限公司 Polycyclic compounds as IDO inhibitors and/or IDO-HDAC dual inhibitors
WO2021216665A1 (en) * 2020-04-22 2021-10-28 Anima Biotech Inc. Collagen 1 translation inhibitors and methods of use thereof

Family Cites Families (11)

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GB944443A (en) * 1959-09-25 1900-01-01
ATE148464T1 (en) * 1991-07-03 1997-02-15 Upjohn Co SUBSTITUTED INDOLES AS ANTI-AIDS PHARMACEUTICAL PREPARATIONS
JPH05255089A (en) * 1991-12-18 1993-10-05 Sanwa Kagaku Kenkyusho Co Ltd Antiviral agent
JPH08502958A (en) * 1992-10-23 1996-04-02 メルク シヤープ エンド ドーム リミテツド Dopamine receptor subtype ligand
GB9305644D0 (en) * 1993-03-18 1993-05-05 Merck Sharp & Dohme Therapeutic agents
US5576336A (en) * 1993-03-18 1996-11-19 Merck Sharp & Dohme Limited Indole derivatives as dopamine D4 antagonists
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
ZA968661B (en) * 1995-11-17 1998-04-14 Upjohn Co Oxazolidinone antibacterial agent with tricyclic substituents.
TW504510B (en) * 1996-05-10 2002-10-01 Janssen Pharmaceutica Nv 2,4-diaminopyrimidine derivatives

Also Published As

Publication number Publication date
HRP980441A2 (en) 1999-04-30
WO1999009025A3 (en) 1999-04-15
IL133960A0 (en) 2001-04-30
NO20000722L (en) 2000-02-14
SK1352000A3 (en) 2000-08-14
AR017019A1 (en) 2001-08-22
CN1265660A (en) 2000-09-06
IS5336A (en) 2000-01-11
PE106299A1 (en) 1999-11-02
ZA987304B (en) 2000-02-14
OA11286A (en) 2003-10-22
HUP0003425A2 (en) 2001-10-28
JP2002536291A (en) 2002-10-29
EP1003739A2 (en) 2000-05-31
CO4960656A1 (en) 2000-09-25
EA200000023A1 (en) 2000-08-28
NO20000722D0 (en) 2000-02-14
DZ2583A1 (en) 2003-02-22
AU8457298A (en) 1999-03-08
BR9811557A (en) 2000-08-22
PL338947A1 (en) 2000-12-04
TR200000414T2 (en) 2000-08-21
CA2297486C (en) 2005-05-03
KR20010022507A (en) 2001-03-15
AP9801321A0 (en) 2000-02-14
WO1999009025A2 (en) 1999-02-25
ID23803A (en) 2000-05-11
MA24632A1 (en) 1999-04-01
HUP0003425A3 (en) 2002-02-28
PA8457001A1 (en) 2000-09-29
TNSN98151A1 (en) 2005-03-15
BG104069A (en) 2001-05-31
CA2297486A1 (en) 1999-02-25

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Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20121130