CO4960656A1 - 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

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Publication number
CO4960656A1
CO4960656A1 CO98046788A CO98046788A CO4960656A1 CO 4960656 A1 CO4960656 A1 CO 4960656A1 CO 98046788 A CO98046788 A CO 98046788A CO 98046788 A CO98046788 A CO 98046788A CO 4960656 A1 CO4960656 A1 CO 4960656A1
Authority
CO
Colombia
Prior art keywords
alkyl
hydrogen
cyano
nitrogen
trifluoromethyl
Prior art date
Application number
CO98046788A
Other languages
Spanish (es)
Inventor
Franz Josef Fliri Anton
Mark Jerome Majchrzak
Seymour Patricia Ann
Howard Zorn Stevin
Hans Rollema
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 CO4960656A1 publication Critical patent/CO4960656A1/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

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

Abstract

Un compuesto de la fórmula I:o la sal farmacéuticamente aceptable del mismo, donde la línea discontinua representa un doble enlace opcional; a es O ó 1, en el que cuando a es O, X puede formar un doble enlace opcional con el carbono adyacente a V; V es CHR10 , en el que R10 es hidrógeno o alquilo (C1 -C6 ); T es nitrógeno o CH; X es nitrógeno o CR11 , en el que R11 es hidrógeno, alquilo (C1 -C6 ), alcoxi (C1 -C6 ), hidroxi o ciano; Y y Z son cada uno de ellos independientemente nitrógeno o CR12 , en el que R12 es hidrógeno, cloro, bromo, trifluorometilo, trifluorometoxi, ciano, alcoxi (C1 -C6 ) o alquilo (C1 -C6 ); R1 es hidrógeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano o alquilo (C1 -C6 ); R2 , R6 , R7 , R8 y R9 están cada uno de ellos independientemente seleccionados entre hidrógeno, fluoro, cloro, bromo, trifluorometilo, trifluorometoxi, ciano, alcoxi (C1 -C6 ) y alquilo (C1 -C6 ); R3 y R4 son cada uno de ellos independientemente hidrógeno o alquilo (C1 -C6 ); y R5 es hidrógeno, alcoxi (C1 -C6 ), trifluorometilo, ciano, alquilo (C1 -C6 ) o R13 CO, en el que R13 es amino, alquil(C1 -C6 )amino, (alquilo (C1 -C6 ))2 amino, alquilo (C1 -C6 ), arilo (C6 -C10 );o cuando a es 1, R1 y R10 se pueden unir con los carbonos a los que están unidos para formar un compuesto de fórmula 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 O ó 1; y A y B son cada uno de ellos independientemente CH, CH2 , oxígeno, azufre, NH o nitrógeno; con la condición de que cuando X es nitrógeno, el doble enlace opcional entre X y V no existe; con la condición de que cuando b es O, el doble enlace opcional entre A y B no existe; y con la condición de que cuando b es 1, A y B no pueden ser ninguno de ellos oxígeno o azufre.A compound of formula I: or the pharmaceutically acceptable salt thereof, where the broken line represents an optional double bond; a is O or 1, where when a is O, X can form an optional double bond with the carbon adjacent to V; V is CHR10, where R10 is hydrogen or (C1-C6) alkyl; T is nitrogen or CH; X is nitrogen or CR11, where R11 is hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy, hydroxy or cyano; Y and Z are each independently nitrogen or CR12, where R12 is hydrogen, chlorine, bromine, trifluoromethyl, trifluoromethoxy, cyano, (C1-C6) alkoxy or (C1-C6) alkyl; R1 is hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano or (C1-C6) alkyl; R2, R6, R7, R8 and R9 are each independently selected from hydrogen, fluoro, chloro, bromo, trifluoromethyl, trifluoromethoxy, cyano, C1-C6 alkoxy and (C1-C6) alkyl; R3 and R4 are each independently hydrogen or (C1-C6) alkyl; and R5 is hydrogen, (C1-C6) alkoxy, trifluoromethyl, cyano, (C1-C6) alkyl or R13 CO, where R13 is amino, (C1-C6) alkyl, ((C1-C6) alkyl) 2 amino, (C1-C6) alkyl, (C6 -C10) aryl; or when a is 1, R1 and R10 may join with the carbons to which they are attached to form a compound of formula in which the dashed lines represent bonds optional; T, X, Y, Z, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined above; b is O 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 O, 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 either oxygen or sulfur.

CO98046788A 1997-08-15 1998-08-14 DERIVATIVES OF 2- (4-ARIL OR HETEROARIL-PIPERAZIN-1-ILMETIL) 1H- INDOL CO4960656A1 (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
CO4960656A1 true CO4960656A1 (en) 2000-09-25

Family

ID=22000003

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98046788A CO4960656A1 (en) 1997-08-15 1998-08-14 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)

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BR9813279B1 (en) * 1997-10-27 2010-11-16 homopiperazine derivative, pharmaceutical composition, and use of the homopiperazine derivative.
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
PT1464641E (en) 1999-12-30 2008-07-01 Lundbeck & Co As H 4-phenyl-piperazinyl, -piperidinyl and tetrahydropyridyl derivatives as dopamine d4 antagonists
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
MXPA03008143A (en) * 2001-03-09 2005-08-16 Johnson & Johnson Heterocyclic compounds.
WO2004022060A2 (en) 2002-09-06 2004-03-18 Janssen Pharmaceutica, N.V. (1h-benzoimidazol-2-yl)-(piperazinyl)-methanone derivatives and related compounds as histamine h4-receptor antagonists for the treatment of inflammatory and allergic disorders
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
EP2253315A1 (en) 2004-03-30 2010-11-24 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
JP5431306B2 (en) 2007-04-23 2014-03-05 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Thia (dia) zole as a fast dissociating dopamine 2 receptor antagonist
PT2148873E (en) 2007-04-23 2012-11-20 Janssen Pharmaceutica Nv 4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
RU2502734C2 (en) 2008-07-03 2013-12-27 Янссен Фармацевтика Нв 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
JP2020534336A (en) * 2017-09-20 2020-11-26 ハンジョウ イノゲート ファーマ カンパニー リミテッドHangzhou Innogate Pharma Co., Ltd. Polycyclic compounds as IDO inhibitors and / or IDO-HDAC double inhibitors
AU2021259580A1 (en) * 2020-04-22 2022-11-24 Anima Biotech Inc. Collagen 1 translation inhibitors and methods of use thereof

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Also Published As

Publication number Publication date
AP9801321A0 (en) 2000-02-14
KR20010022507A (en) 2001-03-15
AR017019A1 (en) 2001-08-22
EA200000023A1 (en) 2000-08-28
CA2297486A1 (en) 1999-02-25
ID23803A (en) 2000-05-11
AU8457298A (en) 1999-03-08
NO20000722L (en) 2000-02-14
UY25144A1 (en) 2000-12-29
HRP980441A2 (en) 1999-04-30
OA11286A (en) 2003-10-22
MA24632A1 (en) 1999-04-01
TNSN98151A1 (en) 2005-03-15
BR9811557A (en) 2000-08-22
JP2002536291A (en) 2002-10-29
PL338947A1 (en) 2000-12-04
NO20000722D0 (en) 2000-02-14
BG104069A (en) 2001-05-31
PA8457001A1 (en) 2000-09-29
TR200000414T2 (en) 2000-08-21
HUP0003425A3 (en) 2002-02-28
ZA987304B (en) 2000-02-14
WO1999009025A3 (en) 1999-04-15
CN1265660A (en) 2000-09-06
CA2297486C (en) 2005-05-03
PE106299A1 (en) 1999-11-02
HUP0003425A2 (en) 2001-10-28
WO1999009025A2 (en) 1999-02-25
IS5336A (en) 2000-01-11
EP1003739A2 (en) 2000-05-31
SK1352000A3 (en) 2000-08-14
DZ2583A1 (en) 2003-02-22
IL133960A0 (en) 2001-04-30

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