PE20050466A1 - HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE TYPE 9 (PDE9) - Google Patents

HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE TYPE 9 (PDE9)

Info

Publication number
PE20050466A1
PE20050466A1 PE2004000413A PE2004000413A PE20050466A1 PE 20050466 A1 PE20050466 A1 PE 20050466A1 PE 2004000413 A PE2004000413 A PE 2004000413A PE 2004000413 A PE2004000413 A PE 2004000413A PE 20050466 A1 PE20050466 A1 PE 20050466A1
Authority
PE
Peru
Prior art keywords
pyrimidin
pyrazole
dihydro
oxo
type
Prior art date
Application number
PE2004000413A
Other languages
Spanish (es)
Inventor
Michael Scott Visser
Andrew Simon Bell
Michael John Palmer
Michael Paul Deninno
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 PE20050466A1 publication Critical patent/PE20050466A1/en

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE LA FORMULA (I), EN DONDE A ES UN RADICAL DE FORMULA (a), (d), (g), ENTRE OTROS; P ES CICLOALQUILO(C3-C5), HETEROCICLOALQUILO(C3-C8), ARILO O HETEROARILO, OPCIONALMENTE SUSTITUIDOS; J ES O, S, -N(R15)-, -N(R15)CO-, -CON(R15)-, ENTRE OTROS; x ES DE 0 A 6; R10 ES -CO2H, -CONR30R31, -NR30R31, O -N(R15)SO2R40; R1 Y R2 SON, INDEPENDIENTEMENTE, H O ALQUILO(C1-C3); R3 ES ALQUILO(C1-C8), CICLOALQUILO(C3-C8), HETEROCICLOALQUIL(C3-C8), METILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 1-{[2-(3-ISOPROPIL-7-OXO-6,7-DIHIDRO-1H-PIRAZOLO[4,3-d]PIRIMIDIN-5-ILMETIL)FENOXI]ACETIL}PIRROLIDINA-2-CARBOXILICO, N-[(1R,2S)-2-(3-ISOPROPIL-7-OXO-6,7-DIHIDRO-1H-PIRAZOLO[4,3-d]PIRIMIDIN-5-ILMETIL)CICLOHEXIL-1-IL]2-PIRROLIDIN-1-IL ACETAMIDA, ESTER METILICO DEL ACIDO 1-{[(1R,2S)-2-(3-ISOPROPIL-7-OXO-6,7-DIHIDRO-1H-PIRAZOLO[4,3-d]PIRIMIDIN-5-ILMETIL)CICLOHEX-1-ILCARBAMOIL]METIL}PIRROLIDINA-2(S)-CARBOXILICO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE FOSFODIESTERASA TIPO 9 ESPECIFICOS DEL MONOFOSFATO CICLICO DE GUANOSINA Y SON UTILES EN EL TRATAMIENTO DE DIABETES TIPO 1 Y TIPO 2, HIPERGLUCEMIA, DISLIPIDEMIA, TOLERANIA A LA GLUCOSA ALTERADA, SINDROME METABOLICO Y/O ENFERMEDAD CARDIOVASCULARREFERS TO COMPOUNDS DERIVED FROM FORMULA (I), WHERE A IS A RADICAL OF FORMULA (a), (d), (g), AMONG OTHERS; P IS CYCLOALKYL (C3-C5), HETEROCICLOALKYL (C3-C8), ARYL OR HETEROARYL, OPTIONALLY SUBSTITUTED; J IS O, S, -N (R15) -, -N (R15) CO-, -CON (R15) -, AMONG OTHERS; x IS FROM 0 TO 6; R10 IS -CO2H, -CONR30R31, -NR30R31, O -N (R15) SO2R40; R1 AND R2 ARE, INDEPENDENTLY, H OR ALKYL (C1-C3); R3 IS ALKYL (C1-C8), CYCLOALKYL (C3-C8), HETEROCICLOALKYL (C3-C8), METHYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: 1 - {[2- (3-ISOPROPYL-7-OXO-6,7-DIHYDRO-1H-PYRAZOLE [4,3-d] PYRIMIDIN-5-ILMETHYL) PHENOXY] ACETYL} PYRROLIDINE-2- CARBOXYL, N - [(1R, 2S) -2- (3-ISOPROPYL-7-OXO-6,7-DIHYDRO-1H-PYRAZOLE [4,3-d] PYRIMIDIN-5-ILMETHYL) CYCLOHEXYL-1-IL] 2-PYRROLIDIN-1-IL ACETAMIDE, ACID METHYL ESTER 1 - {[(1R, 2S) -2- (3-ISOPROPYL-7-OXO-6,7-DIHYDRO-1H-PYRAZOLE [4,3-d] PYRIMIDIN-5-ILMETIL) CYCLOHEX-1-ILCARBAMOIL] METHYL} PYRROLIDINE-2 (S) -CARBOXYL, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS ARE SPECIFIC INHIBITORS OF TYPE 9 PHOSPHODIESTERASE OF CYCLIC GUANOSINE MONOPHOSPHATE AND ARE USEFUL IN THE TREATMENT OF TYPE 1 AND TYPE 2 DIABETES, HYPERGLYCAEMIA, DYSLIPIDEMIA, TOLERANIA A LA GLYCEDULATE / ALTERABLY GLYCEDULATE SYNDROME

PE2004000413A 2003-04-30 2004-04-27 HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE TYPE 9 (PDE9) PE20050466A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US46663903P 2003-04-30 2003-04-30

Publications (1)

Publication Number Publication Date
PE20050466A1 true PE20050466A1 (en) 2005-06-18

Family

ID=33551403

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000413A PE20050466A1 (en) 2003-04-30 2004-04-27 HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE TYPE 9 (PDE9)

Country Status (8)

Country Link
AR (1) AR044119A1 (en)
CL (1) CL2004000901A1 (en)
GT (1) GT200400086A (en)
NL (1) NL1026091C2 (en)
PA (1) PA8601601A1 (en)
PE (1) PE20050466A1 (en)
TW (1) TW200503714A (en)
UY (1) UY28291A1 (en)

Also Published As

Publication number Publication date
UY28291A1 (en) 2004-11-30
NL1026091A1 (en) 2004-11-02
GT200400086A (en) 2005-01-11
CL2004000901A1 (en) 2005-03-18
NL1026091C2 (en) 2005-05-26
AR044119A1 (en) 2005-08-24
TW200503714A (en) 2005-02-01
PA8601601A1 (en) 2005-02-04

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