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PE20050222A1 - TRIAZOLE COMPOUNDS AS VASOPRESSIN ANTAGONISTS - Google Patents

TRIAZOLE COMPOUNDS AS VASOPRESSIN ANTAGONISTS

Info

Publication number
PE20050222A1
PE20050222A1 PE2004000165A PE2004000165A PE20050222A1 PE 20050222 A1 PE20050222 A1 PE 20050222A1 PE 2004000165 A PE2004000165 A PE 2004000165A PE 2004000165 A PE2004000165 A PE 2004000165A PE 20050222 A1 PE20050222 A1 PE 20050222A1
Authority
PE
Peru
Prior art keywords
alkyl
tetraaza
benzo
chloro
ring
Prior art date
Application number
PE2004000165A
Other languages
Spanish (es)
Inventor
Justin Stephen Bryans
Patrick Stephen Johnson
Alan Stobie
Thomas Ryckmans
Original Assignee
Pfizer
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 filed Critical Pfizer
Publication of PE20050222A1 publication Critical patent/PE20050222A1/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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE TRIAZOL DE FORMULA (I), DONDE V ES -(CH2)d(O)e-, -CO-, O -CH(ALQUILOC1-C6); W ES -O-, -S(O)a- O -N(R1)-; R1 ES H, ALQUILO(C1-C6), (CH2)bCOR2, CO(CH2)bNR2R3, SO2R2, (CH2)cOR2, (CH2)cNR2R3 O (CH2)bhet1; het1 ES UN HETEROCICLO DE 3 A 8 ATOMOS QUE PUEDE CONTENER O, N O S, OPCIONALMENTE SUSTITUIDOS CON ALQUILO(C1-C6); X E Y SON H, ALQUILO(C1-C6), HALOGENO, OH, CF3, OCF3, OR4; Z ES -(CH2)f(O)g-, -CO-, O -CH(ALQUILO(C1-C6))-; EL ANILLO A ES UN HETEROCICLO SATURADO QUE CONTIENE N, DE 4 A 7 MIEMBROS OPCIONALMENTE SUSTITUIDO CON OH Y AL MENOS UN N DEL ANILLO PUEDE ESTAR SUSTITUIDO CON O; EL ANILLO B ES UN FENILO O UN HETEROCICLO INSATURADO QUE CONTIENE N, DE 4 A 7 MIEMBROS, OPCIONALMENTE SUSTITUIDO CON OH, HALOGENO, CN, CONH2, CF3, OCF3, Y AL MENOS UN N PUEDE ESTAR SUSTITUIDO CON O. SON COMPUESTOS PREFERIDOS: TRICLOROHIDRATO DE 8-CLORO-5-METIL-1-(3,4,5,6-TETRAHIDRO-2H-[1,2']BIPIRIDINIL-4-IL)-5,6-DIHIDRO-4H-2,3,5,10b-TETRAAZA-BENZO[e]AZULENO, 8-CLORO-5-METANOSULFONIL-1-(3,4,5,6-TETRAHIDRO-2H-[1,2']-BIPIRIDINIL-4-IL)-5,6-DIHIDRO-4H-2,3,5,10b-TETRAAZA-BENZO[e]AZULENO, DIMETILAMINO DEL ACIDO 8-CLORO-1-(1-PIRIMIDIN-2-IL-PIPERIDIN-4-IL)-4H,6H-2,3,5,10b-TETRAAZA-BENZO[e]AZULENO-5-SULFONICO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE ELABORACION Y COMPUESTOS INTERMEDIOS. UNA FORMULACION FARMACEUTICA QUE LOS CONTIENE. ESTOS COMPUESTOS MUESTRAN UNA ACTIVIDAD ANTAGONISTA DE VASOPRESINA Y PUEDEN USARSE EN EL TRATAMIENTO DE DISMENORREAREFERS TO TRIAZOLE DERIVATIVES OF FORMULA (I), WHERE V IS - (CH2) d (O) e-, -CO-, O -CH (ALKYLOC1-C6); W IS -O-, -S (O) a- O -N (R1) -; R1 IS H, (C1-C6) ALKYL, (CH2) bCOR2, CO (CH2) bNR2R3, SO2R2, (CH2) cOR2, (CH2) cNR2R3 O (CH2) bhet1; het1 IS A HETEROCYCLE OF 3 TO 8 ATOMS THAT MAY CONTAIN O, N OR S, OPTIONALLY SUBSTITUTED WITH ALKYL (C1-C6); X AND Y ARE H, (C1-C6) ALKYL, HALOGEN, OH, CF3, OCF3, OR4; Z IS - (CH2) f (O) g-, -CO-, O -CH ((C1-C6) ALKYL) -; THE RING A IS A SATURATED HETEROCYCLE CONTAINING N, FROM 4 TO 7 MEMBERS OPTIONALLY SUBSTITUTED WITH OH AND AT LEAST ONE N OF THE RING MAY BE SUBSTITUTED WITH O; RING B IS AN INSATURATED PHENYL OR HETEROCYCLE CONTAINING N, FROM 4 TO 7 MEMBERS, OPTIONALLY SUBSTITUTED WITH OH, HALOGEN, CN, CONH2, CF3, OCF3, AND AT LEAST ONE N MAY BE SUBSTITUTED WITH O. PREFERRED COMPOUNDS ARE: 8-CHLORO-5-METHYL-1- (3,4,5,6-TETRAHYDRO-2H- [1,2 '] BIPYRIDINYL-4-IL) -5,6-DIHYDRO-4H-2,3 TRICHLOROHYDRATE, 5,10b-TETRAAZA-BENZO [e] BLUE, 8-CHLORO-5-METHANOSULPHONYL-1- (3,4,5,6-TETRAHYDRO-2H- [1,2 '] - BIPYRIDINYL-4-IL) -5 , 6-DIHYDRO-4H-2,3,5,10b-TETRAAZA-BENZO [e] AZULENE, 8-CHLORO-1- (1-PYRIMIDIN-2-IL-PIPERIDIN-4-IL) -4H ACID DIMETHYLAMINE, 6H-2,3,5,10b-TETRAAZA-BENZO [e] AZULENO-5-SULFONICO, AMONG OTHERS. ALSO REFERS TO A PROCEDURE OF PREPARATION AND INTERMEDIATE COMPOUNDS. A PHARMACEUTICAL FORMULATION THAT CONTAINS THEM. THESE COMPOUNDS SHOW ANTAGONIST ACTIVITY OF VASOPRESSIN AND MAY BE USED IN THE TREATMENT OF DYSMENORRHEA

PE2004000165A 2003-02-19 2004-02-17 TRIAZOLE COMPOUNDS AS VASOPRESSIN ANTAGONISTS PE20050222A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0303852.8A GB0303852D0 (en) 2003-02-19 2003-02-19 Triazole compounds useful in therapy

Publications (1)

Publication Number Publication Date
PE20050222A1 true PE20050222A1 (en) 2005-04-13

Family

ID=9953327

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000165A PE20050222A1 (en) 2003-02-19 2004-02-17 TRIAZOLE COMPOUNDS AS VASOPRESSIN ANTAGONISTS

Country Status (11)

Country Link
CN (1) CN1751047A (en)
AR (1) AR043210A1 (en)
CL (1) CL2004000293A1 (en)
GB (1) GB0303852D0 (en)
GT (1) GT200400020A (en)
NL (1) NL1025527C2 (en)
PA (1) PA8596101A1 (en)
PE (1) PE20050222A1 (en)
TW (1) TW200500367A (en)
UY (1) UY28201A1 (en)
WO (1) WO2004074291A1 (en)

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Also Published As

Publication number Publication date
CL2004000293A1 (en) 2005-01-07
PA8596101A1 (en) 2005-08-04
AR043210A1 (en) 2005-07-20
UY28201A1 (en) 2004-09-30
TW200500367A (en) 2005-01-01
CN1751047A (en) 2006-03-22
GT200400020A (en) 2004-09-21
GB0303852D0 (en) 2003-03-26
WO2004074291A1 (en) 2004-09-02
NL1025527A1 (en) 2004-08-23
NL1025527C2 (en) 2005-03-14

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