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PE20030702A1 - PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS - Google Patents

PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS

Info

Publication number
PE20030702A1
PE20030702A1 PE2002001070A PE2002001070A PE20030702A1 PE 20030702 A1 PE20030702 A1 PE 20030702A1 PE 2002001070 A PE2002001070 A PE 2002001070A PE 2002001070 A PE2002001070 A PE 2002001070A PE 20030702 A1 PE20030702 A1 PE 20030702A1
Authority
PE
Peru
Prior art keywords
alkyl
ona
pyrimidin
dihydro
treatment
Prior art date
Application number
PE2002001070A
Other languages
Spanish (es)
Inventor
Michael Paul Deninno
Bernadette Hughes
Anthony Wood
Michael John Palmer
Mark Ian Kemp
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
Priority claimed from GB0126395A external-priority patent/GB0126395D0/en
Priority claimed from GB0130695A external-priority patent/GB0130695D0/en
Priority claimed from GB0216761A external-priority patent/GB0216761D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of PE20030702A1 publication Critical patent/PE20030702A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P27/14—Decongestants or antiallergics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
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    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
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    • A61P9/10—Drugs 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
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    • A61P9/12—Antihypertensives
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE R1 ES H, ALQUILO C1-C6 DONDE R1 SE UNE A N1 O N2; R2 ES ALQUILO C1-C6, CICLOALQUILO C3-C7, HETEROCICLO DE 5-6 MIEMBROS CON ALQUILO, OH, ALCOXI; R3 ES ALQUILO C1-C6 CON Ar2, CICLOALQUILO C3-C7, ENTRE OTROS; Ar2 ES EL GRUPO a CONDE R4, R5, R6 SON H, HALO, FENOXI, FENILO, CF3, CF3, ENTRE OTROS. CUANDO R1 ESTA UNIDO A N1, R1 ES ALQUILO C1-C6 Y R2 ES PROPILO ENTONCE R3 NO ES METILO SUSTITUIDO CON Ar1; R1 ESTA UNIDO A N1, R1 ES ALQUILO C1-C6, R2 ES METILO ENTONCES R3 NO ES ALQUILO C1-C4 SUSTITUIDO CON Ar1. SON COMPUESTOS PREFERIDOS 5-(-3-CLOROBENZIL)-3-ISOPROPIL-1,6-DIHIDRO-PIRAZOL[4,3-d]PIRIMIDIN-7-ONA, 3-ISOPROPIL-5-(2-FENOXIBENZIL)-1,6-DIHIDRO-PIRAZOL[4,3-d]PIRIMIDIN-7-ONA. 3-(3-PIRIDINIL)-5-(-2-BENCILOXIBENZIL)-1,6-DIHIDRO-PIRAZOL[4,3-d]PIRIMIDIN-7-ONA. 3-ISOPROPIL-5-(2-TRIFLUOROMETOXIBENCIL)-1,6-DIHIDRO-PIRAZOL[4,3-d]PIRIMIDIN-7-ONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DE LA FOSFODIESTERASA 9 (PDE9) Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARESREFERS TO COMPOUNDS OF FORMULA I WHERE R1 IS H, C1-C6 ALKYL WHERE R1 JOINS N1 OR N2; R2 IS C1-C6 ALKYL, C3-C7 CYCLOALKYL, 5-6 MEMBER HETERO CYCLE WITH ALKYL, OH, ALCOXY; R3 IS C1-C6 ALKYL WITH Ar2, C3-C7 CYCLOALKYL, AMONG OTHERS; Ar2 IS THE GROUP to COUNT R4, R5, R6 ARE H, HALO, FENOXI, FENILO, CF3, CF3, AMONG OTHERS. WHEN R1 IS BOUND TO N1, R1 IS ALKYL C1-C6 AND R2 IS PROPYL THEN R3 IS NOT METHYL SUBSTITUTED WITH Ar1; R1 IS JOINTED TO N1, R1 IS C1-C6 ALKYL, R2 IS METHYL THEN R3 IS NOT C1-C4 ALKYL REPLACED WITH Ar1. PREFERRED COMPOUNDS ARE 5 - (- 3-CHLOROBENZIL) -3-ISOPROPIL-1,6-DIHYDRO-PIRAZOL [4,3-d] PYRIMIDIN-7-ONA, 3-ISOPROPYL-5- (2-PHENOXIBENZIL) -1, 6-DIHYDRO-PYRAZOLE [4,3-d] PYRIMIDIN-7-ONA. 3- (3-PYRIDINYL) -5 - (- 2-BENZYLOXIBENZIL) -1,6-DIHYDRO-PYRAZOLE [4,3-d] PYRIMIDIN-7-ONA. 3-ISOPROPYL-5- (2-TRIFLUOROMETOXIBENCIL) -1,6-DIHYDRO-PIRAZOLE [4,3-d] PYRIMIDIN-7-ONA, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PROCEDURE FOR THE PREPARATION. THE MENTIONED COMPOUNDS ARE INHIBITORS OF PHOSPHODIESTERASE 9 (PDE9) AND ARE USEFUL FOR THE TREATMENT OF CARDIOVASCULAR DISEASES

PE2002001070A 2001-11-02 2002-10-30 PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS PE20030702A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0126395A GB0126395D0 (en) 2001-11-02 2001-11-02 Pyrazolo[4,3]pyrimidine derivatives and their use in treating disease
GB0130695A GB0130695D0 (en) 2001-12-21 2001-12-21 Pyrazola[4,3]pyrimidine
GB0216761A GB0216761D0 (en) 2002-07-18 2002-07-18 PDE9 Inhibitors for treating cardiovascular disorders

Publications (1)

Publication Number Publication Date
PE20030702A1 true PE20030702A1 (en) 2003-08-21

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PE2002001070A PE20030702A1 (en) 2001-11-02 2002-10-30 PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS

Country Status (14)

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EP (1) EP1440073A1 (en)
JP (1) JP2005511575A (en)
AR (1) AR037329A1 (en)
BR (1) BR0214096A (en)
CA (1) CA2466824A1 (en)
DO (1) DOP2002000482A (en)
HN (1) HN2002000317A (en)
MX (1) MXPA04004171A (en)
PA (1) PA8557401A1 (en)
PE (1) PE20030702A1 (en)
SV (1) SV2004001373A (en)
TW (1) TW200300081A (en)
UY (1) UY27522A1 (en)
WO (1) WO2003037899A1 (en)

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