patents.google.com

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

  • ️Thu Aug 21 2003

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
2001-11-02
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.)
2001-11-02
Filing date
2002-10-30
Publication date
2003-08-21
2001-11-02 Priority claimed from GB0126395A external-priority patent/GB0126395D0/en
2001-12-21 Priority claimed from GB0130695A external-priority patent/GB0130695D0/en
2002-07-18 Priority claimed from GB0216761A external-priority patent/GB0216761D0/en
2002-10-30 Application filed by Pfizer filed Critical Pfizer
2003-08-21 Publication of PE20030702A1 publication Critical patent/PE20030702A1/en

Links

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
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/16—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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P7/06—Antianaemics
    • 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
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pregnancy & Childbirth (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Toxicology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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

Family

ID=27256310

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001070A PE20030702A1 (en) 2001-11-02 2002-10-30 PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS

Country Status (14)

Country Link
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)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2429132T3 (en) 2001-08-31 2013-11-13 The Rockefeller University Phosphodiesterase activity and regulation of phosphodiesterase 1-B mediated signaling in the brain
JP4467979B2 (en) * 2001-12-06 2010-05-26 メルク・シャープ・エンド・ドーム・コーポレイション Mitotic kinesin inhibitor
DE10238722A1 (en) * 2002-08-23 2004-03-11 Bayer Ag Improving attention, concentration, cognition, learning and/or memory performance, using selective phosphodiesterase 9A inhibitors, preferably 4H-pyrazolo-(3,4-d)-pyrimidin-4-one derivatives
DE10238723A1 (en) * 2002-08-23 2004-03-11 Bayer Ag Phenyl substituted pyrazolyprimidines
DE10238724A1 (en) 2002-08-23 2004-03-04 Bayer Ag New 6-alkyl-1,5-dihydro-4H-pyrazolo-(3,4-d)-pyrimidin-4-ones useful as selective phosphodiesterase 9A inhibitors for improving attention, concentration, learning and/or memory performance
US7141669B2 (en) 2003-04-23 2006-11-28 Pfizer Inc. Cannabiniod receptor ligands and uses thereof
DE10320785A1 (en) 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-arylmethyl substituted pyrazolopyrimidines
WO2004099211A1 (en) * 2003-05-09 2004-11-18 Bayer Healthcare Ag 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines
US8044060B2 (en) 2003-05-09 2011-10-25 Boehringer Ingelheim International Gmbh 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory
DE102004004142A1 (en) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines
DE10328479A1 (en) * 2003-06-25 2005-01-13 Bayer Ag 6-arylamino-5-cyano-4-pyrimidinones
AU2004261459B2 (en) 2003-07-22 2008-06-26 Astex Therapeutics Limited 3, 4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
DE102004001873A1 (en) 2004-01-14 2005-09-29 Bayer Healthcare Ag Cyanopyrimidinone
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
US7067659B2 (en) * 2004-04-23 2006-06-27 Duke University Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (en) 2005-01-21 2007-06-27 Astex Therapeutics Ltd PIPERIDIN ADDITION SALTS 4-IL-ACID AMID 4- (2,6-DICLORO-BENZOILAMINO) 1H-PIRAZOL-3-CARBOXILICO.
DE102005024494A1 (en) * 2005-05-27 2006-11-30 Bayer Healthcare Ag Use of cyanopyrimidines
AU2006258461B2 (en) 2005-06-14 2011-08-25 Aska Pharmaceutical Co., Ltd. Thienopyrimidine derivative
US20080194592A1 (en) * 2005-08-23 2008-08-14 Intra-Cellular Therapies, Inc. Organic Compounds
US9255099B2 (en) 2006-06-06 2016-02-09 Intra-Cellular Therapies, Inc. Pyrazolo[3,4-D]pyrimidine-4,6(5H,7H)-diones as phosphodiesterase 1 inhibitors
ES2581573T3 (en) 2006-08-08 2016-09-06 Aska Pharmaceutical Co., Ltd. Quinazoline derivative
JPWO2008072778A1 (en) * 2006-12-13 2010-04-02 あすか製薬株式会社 Treatment for urinary tract diseases
WO2008072779A1 (en) * 2006-12-13 2008-06-19 Aska Pharmaceutical Co., Ltd. Quinoxaline derivative
US8383852B2 (en) * 2007-02-16 2013-02-26 Emisphere Technologies, Inc. Compounds having a cyclic moiety and compositions for delivering active agents
GEP20125405B (en) * 2007-05-11 2012-02-27 Pfizer Amino-heterocyclic compounds
JP5498392B2 (en) * 2007-11-30 2014-05-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 1,5-Dihydro-pyrazolo [3,4-D] pyrimidin-4-one derivatives and their use as PDE9A modulators for the treatment of CNS disorders
CA2707218A1 (en) 2007-12-06 2009-06-11 Intra-Cellular Therapies, Inc. Organic compounds
UA105362C2 (en) 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
AU2009289240A1 (en) 2008-09-08 2010-03-11 Boehringer Ingelheim International Gmbh Pyrazolopyrimidines and their use for the treatment of CNS disorders
JP5575137B2 (en) 2008-10-22 2014-08-20 メルク・シャープ・アンド・ドーム・コーポレーション Novel cyclic benzimidazole derivatives useful as antidiabetic agents
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
PE20110944A1 (en) 2008-12-06 2012-01-25 Intra Cellular Therapies Inc PYRAZOLO [3,4-d] PYRIMIDINE DERIVATIVES AS PDE1 INHIBITORS
MA32941B1 (en) 2008-12-06 2012-01-02 Intra Cellular Therapies Inc Organic compounds
EA201170768A1 (en) 2008-12-06 2012-05-30 Интра-Селлулар Терапиз, Инк. ORGANIC COMPOUNDS
TWI404721B (en) * 2009-01-26 2013-08-11 Pfizer Amino-heterocyclic compounds
PL2404922T3 (en) 2009-03-05 2017-03-31 Astellas Pharma Inc. Quinoxaline compounds
EA201101395A1 (en) 2009-03-31 2012-06-29 Бёрингер Ингельхайм Интернациональ Гмбх DERIVATIVES 1-HETEROCYCLIL-1,5-DIHYDROPYRAZOLO [3,4D] Pyrimidine-4-OHA AND THEIR APPLICATION AS PDE9A
SG178279A1 (en) 2009-08-05 2012-03-29 Intra Cellular Therapies Inc Novel regulatory proteins and inhibitors
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2575817A4 (en) 2010-05-31 2014-01-08 Intra Cellular Therapies Inc Organic compounds
US9371327B2 (en) 2010-05-31 2016-06-21 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
WO2012004900A1 (en) * 2010-07-09 2012-01-12 Aska Pharmaceutical Co., Ltd. Thienopyrimidine compounds
WO2012020022A1 (en) 2010-08-12 2012-02-16 Boehringer Ingelheim International Gmbh 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors
EP2615096B1 (en) 2010-09-07 2019-08-28 Astellas Pharma Inc. Quinoxaline compound
ES2583528T3 (en) 2010-09-07 2016-09-21 Astellas Pharma Inc. Pyrazoloquinoline compound
PE20140421A1 (en) * 2010-12-06 2014-04-26 Glaxo Group Ltd PYRIMIDINONE-DERIVED COMPOUNDS AS Lp-PLA2 INHIBITORS
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
EA025380B1 (en) 2011-02-25 2016-12-30 Мерк Шарп Энд Домэ Корп. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
US9643970B2 (en) * 2011-10-10 2017-05-09 H. Lundbeck A/S Substituted imidazo [1,5-a]pyrazines as PDE9 inhibitors
SG11201403909RA (en) 2012-01-26 2014-10-30 Lundbeck & Co As H Pde9 inhibitors with imidazo triazinone backbone
RU2015106909A (en) 2012-08-02 2016-09-27 Мерк Шарп И Доум Корп. ANTI-DIABETIC TRICYCLIC COMPOUNDS
CN102786525B (en) 2012-08-08 2014-12-17 中山大学 N-substituted pyrazolo [3, 4-d] pyrimidine ketone compound and preparation method and application thereof
MX2015010935A (en) 2013-02-22 2015-10-29 Merck Sharp & Dohme Antidiabetic bicyclic compounds.
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9546175B2 (en) 2014-08-07 2017-01-17 Intra-Cellular Therapies, Inc. Organic compounds
AU2016289856B2 (en) 2015-07-07 2020-11-26 H. Lundbeck A/S PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. ANTIDIABETIC HETEROCYCLIC COMPOUNDS
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
CA3060183A1 (en) 2017-06-01 2018-12-06 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine
CA3061884A1 (en) 2017-06-01 2019-10-29 Eisai R&D Management Co., Ltd. Lewy body disease therapeutic agent containing pyrazoloquinoline derivative
US11484502B2 (en) 2017-06-01 2022-11-01 Eisai R&D Management Co., Ltd. Pharmaceutical composition comprising PDE9 inhibitor
EP3632439B1 (en) 2017-06-01 2024-03-27 Eisai R&D Management Co., Ltd. Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil
JP2021526134A (en) 2018-05-25 2021-09-30 イマラ インク． 6-[(3S, 4S) -4-methyl-l- (pyrimidine-2-ylmethyl) pyrrolidine-3-yl] -3-tetrahydropyran-4-yl-7H-imidazole [l, 5-A] pyrazine- 8-one monohydrate and crystalline form
AU2019328299B2 (en) * 2018-08-31 2025-02-20 Cardurion Pharmaceuticals, Inc. PDE9 inhibitors for treating sickle cell disease
TWI816026B (en) * 2019-03-08 2023-09-21 大陸商藥捷安康(南京)科技股份有限公司 Phosphodiesterase inhibitor uses and kits

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3939161A (en) * 1973-10-29 1976-02-17 Abbott Laboratories 1,3-Dimethyl- 1H-pyrazolo(4,3-D) pyrimidine-7 (6H)-ones
US4666908A (en) * 1985-04-05 1987-05-19 Warner-Lambert Company 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use
GB9722520D0 (en) * 1997-10-24 1997-12-24 Pfizer Ltd Compounds
DE19838705A1 (en) * 1998-08-26 2000-03-02 Bayer Ag New dihydro- (1,2,3) -triazolo- [4,5-d] pyrimidin-7-ones
IL139457A0 (en) * 1999-11-08 2001-11-25 Pfizer Compounds for the treatment of female sexual dysfunction
WO2002062799A1 (en) * 2001-02-05 2002-08-15 Dr. Reddy's Laboratories Ltd. Aryl substituted alkylcarboxylic acids as hypocholesterolemic agents

Also Published As

Publication number Publication date
SV2004001373A (en) 2004-01-07
HN2002000317A (en) 2003-05-21
PA8557401A1 (en) 2003-11-12
AR037329A1 (en) 2004-11-03
WO2003037899A1 (en) 2003-05-08
TW200300081A (en) 2003-05-16
DOP2002000482A (en) 2003-05-31
MXPA04004171A (en) 2004-09-06
EP1440073A1 (en) 2004-07-28
JP2005511575A (en) 2005-04-28
CA2466824A1 (en) 2003-05-08
BR0214096A (en) 2004-09-28
UY27522A1 (en) 2003-06-30

Similar Documents

Publication Publication Date Title
PE20030702A1 (en) 2003-08-21 PDE9 INHIBITORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS
PE20020506A1 (en) 2002-07-09 PIRAZOLE DERIVATIVES FUSED AS PROTEIN KINASE INHIBITORS
AR054524A1 (en) 2007-06-27 METHODS AND DOSAGE FORMS TO REDUCE THE SIDE EFFECTS OF CARBAMATE COMPOUNDS
PE20040164A1 (en) 2004-05-21 MIMETICS OF GLUCOCORTICOIDS, PROCEDURES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS
DOP2001000271A (en) 2001-11-18 IMIDAZOL COMPOUNDS CONDENSED WITH ARILO OR HETEROARILO AS ANTI-INFLAMMATORY AND ANALGESIC AGENTS.
PE20020753A1 (en) 2002-08-27 HETEROAROMATICS FUSED AS GLUCOKINASE ACTIVATORS
UY26872A1 (en) 2002-01-31 DERIVATIVES OF THE 4- PIRIDINE PHENYL
EA200501265A1 (en) 2006-02-24 DERIVATIVES OF PYRIMIDINE FOR PREVENTION OF HIV INFECTION
PE20020721A1 (en) 2002-10-01 QUINUCLIDINE DERIVATIVES AS ANTIMUSCARINAL AGENTS M3
ECSP034744A (en) 2003-10-28 N-REPLACED N-REPLACED NMDA / NR2B ANTAGONISTS
SE0104334D0 (en) 2001-12-19 Therapeutic agents
NZ511739A (en) 2002-11-26 New esters derived from substituted phenyl-cyclohexyl compounds
WO2002080846A3 (en) 2003-12-04 Epothilone derivatives and methods for making and using the same
ATE302775T1 (en) 2005-09-15 CARBOLINE DERIVATIVES
PE20100737A1 (en) 2010-11-27 NEW COMPOUNDS
PE20030574A1 (en) 2003-07-03 N- [BENZOIL] HETEROARYLSULFONAMIDE AS ANTINEOPLASTIC AGENTS
IL183373A0 (en) 2007-09-20 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof
AR054508A1 (en) 2007-06-27 BENCILPIPERAZINE COMPOSITE, ITS USE TO PREPARE A MEDICINAL PRODUCT, PROCEDURES FOR THE PREPARATION OF SUCH COMPOUND AND INTERMEDIATE COMPOUNDS, SUCH INTERMEDIARY COMPOUNDS, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND PROCEDURE TO PREPARE IT
PE20050587A1 (en) 2005-08-11 DIAZINDOL-DICARBONYL-PIPERAZINYL DERIVATIVES AS ANTIVIRAL AGENTS
RU2009102270A (en) 2010-08-10 THIAZOLYL UREA DERIVATIVES AS PHOSPHATIDYLINOSYTOL-3-KINASE INHIBITORS
DE60214401D1 (en) 2006-10-12 HETERO BICYCLIC CRF ANTAGONISTS
PE20050160A1 (en) 2005-03-26 3-AMINOPYRROLIDINES AS INHIBITORS OF MONOAMINE UPTAKE
AR029005A1 (en) 2003-06-04 STABLE LIQUID FORMATION WITHOUT WATER OR ALMOST WITHOUT WATER FROM REPLACED BENCIMIDAZOLS, PROCESS FOR PREPARATION, USE OF THIS FORMULATION, AND USE OF POLYETHYLENE GLYCOL AND A SODIUM OR POTASSIUM SALT OF AN H +, K + -ATP ASA INHIBITOR
RU2007122406A (en) 2009-01-27 TETRALINE AND INDANA DERIVATIVES AND THEIR APPLICATION AS 5-NT ANTAGONISTS
MY139228A (en) 2009-08-28 Imidazolinylmethyl aralkylsulfonamides

Legal Events

Date Code Title Description
2006-05-23 FD Application declared void or lapsed