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DOP2002000482A - PDE9 INHIBITORS FOR TREATMENT OF CARDIOVASCULAR DISORDERS - Google Patents

  • ️Sat May 31 2003

DOP2002000482A - PDE9 INHIBITORS FOR TREATMENT OF CARDIOVASCULAR DISORDERS - Google Patents

PDE9 INHIBITORS FOR TREATMENT OF CARDIOVASCULAR DISORDERS

Info

Publication number
DOP2002000482A
DOP2002000482A DO2002000482A DO2002000482A DOP2002000482A DO P2002000482 A DOP2002000482 A DO P2002000482A DO 2002000482 A DO2002000482 A DO 2002000482A DO 2002000482 A DO2002000482 A DO 2002000482A DO P2002000482 A DOP2002000482 A DO P2002000482A Authority
DO
Dominican Republic
Prior art keywords
alkyl
optionally substituted
treatment
pde9 inhibitors
cardiovascular disorders
Prior art date
2001-11-02
Application number
DO2002000482A
Other languages
Spanish (es)
Inventor
Mark Ian Kemp
Anthony Wood
Michael Paul Deninno
Bernadette Hughes
Michael John Palmer
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
2002-10-09
Publication date
2003-05-31
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
2002-10-09 Application filed by Pfizer filed Critical Pfizer
2003-05-31 Publication of DOP2002000482A publication Critical patent/DOP2002000482A/en

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    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
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    • A61P13/10Drugs for disorders of the urinary system of the bladder
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
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    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
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    • A61P17/06Antipsoriatics
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    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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

Abstract

La invención se refiere a los inhibidores PDE9 para el tratamiento de trastornos cardiovasculares. Los inhibidores PDE9 preferidos son compuestos de la fórmula I en los que R1 es H o alquilo C1-6, en el que R1 está unido bien a N1 o N2; R2 es alquilo C16 opcionalmente sustituido con hidroxi o alcoxi; cicloalquilo C3-7, opcionalmente sustituido con alquilo, hidroxi, o alcoxi; un heterociclo saturado de 5-6 miembros opcionalmente sustituido con alquilo, ,hidroxi o alcoxi; het o Ar1 R3 es alquilo c-6 opcionalmente sustituido con 1 ó 2 grupos independientemente seleccionados entre: Ar2 cicloalquilo C3-7, opcionalmente sustituido con alquilo C,6 OAr2 SAr2 NHCO alquilo C,.6 het2 xanteno; y naft1eno.The invention relates to PDE9 inhibitors for the treatment of cardiovascular disorders. Preferred PDE9 inhibitors are compounds of the formula I in which R1 is H or C1-6 alkyl, wherein R1 is well linked to N1 or N2; R2 is C16 alkyl optionally substituted with hydroxy or alkoxy; C3-7 cycloalkyl, optionally substituted with alkyl, hydroxy, or alkoxy; a saturated 5-6 membered heterocycle optionally substituted with alkyl, hydroxy or alkoxy; het or Ar1 R3 is C-6 alkyl optionally substituted with 1 or 2 groups independently selected from: Ar2 C3-7 cycloalkyl, optionally substituted with C alkyl, 6 OAr2 SAr2 NHCO C alkyl, .6 het2 xanthene; and naphthine.

DO2002000482A 2001-11-02 2002-10-09 PDE9 INHIBITORS FOR TREATMENT OF CARDIOVASCULAR DISORDERS DOP2002000482A (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
DOP2002000482A true DOP2002000482A (en) 2003-05-31

Family

ID=27256310

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2002000482A DOP2002000482A (en) 2001-11-02 2002-10-09 PDE9 INHIBITORS FOR 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
EP1575916B1 (en) 2001-08-31 2013-05-22 The Rockefeller University Phosphodiesterase activity and regulation of phosphodiesterase 1-b-mediated signaling in brain
CA2468156A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Azolopyrimidinone compounds and their use
DE10238723A1 (en) 2002-08-23 2004-03-11 Bayer Ag Phenyl substituted pyrazolyprimidines
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
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
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
WO2004099211A1 (en) * 2003-05-09 2004-11-18 Bayer Healthcare Ag 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines
DE102004004142A1 (en) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines
DE10320785A1 (en) 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-arylmethyl substituted pyrazolopyrimidines
DE10328479A1 (en) 2003-06-25 2005-01-13 Bayer Ag 6-arylamino-5-cyano-4-pyrimidinones
MXPA06000794A (en) 2003-07-22 2006-08-23 Astex Therapeutics Ltd 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
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating 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
EP1908765B1 (en) 2005-06-14 2014-10-22 ASKA Pharmaceutical Co., Ltd. Thienopyrimidine derivative
US20080194592A1 (en) * 2005-08-23 2008-08-14 Intra-Cellular Therapies, Inc. Organic Compounds
MX2008015489A (en) 2006-06-06 2009-01-13 Intra Cellular Therapies Inc Organic compounds.
CA2659967C (en) 2006-08-08 2014-05-13 Aska Pharmaceutical Co., Ltd. Quinazoline derivatives
US8299080B2 (en) * 2006-12-13 2012-10-30 Aska Pharmaceutical Co., Ltd. Substituted imidazo[1,5-A] quinoxalines as a PDE9 inhibitor
CN101557826A (en) * 2006-12-13 2009-10-14 Aska制药株式会社 Therapeutic agent for urinary tract disease
EP2129218B1 (en) * 2007-02-16 2016-10-19 Emisphere Technologies, Inc. Compounds having a cyclic moiety and compositions for delivering active agents
SI2152712T1 (en) * 2007-05-11 2012-03-30 Pfizer Amino-heterocyclic compounds
EP2217602B1 (en) * 2007-11-30 2018-08-29 Boehringer Ingelheim International GmbH 1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators for the treatment of cns disorders
MX2010006208A (en) 2007-12-06 2010-12-21 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
EP2334684B1 (en) 2008-09-08 2017-08-02 Boehringer Ingelheim International GmbH Pyrazolopyrimidines and their use for the treatment of cns disorders
MX2011004258A (en) 2008-10-22 2011-06-01 Merck Sharp & Dohme Novel cyclic benzimidazole derivatives useful anti-diabetic agents.
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8697710B2 (en) 2008-12-06 2014-04-15 Intra-Cellular Therapies, Inc. Optionally substituted 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo [3,4-d]pyrimidin-6(7H)-ones
MA32941B1 (en) 2008-12-06 2012-01-02 Intra Cellular Therapies Inc Organic compounds
EP2367428B1 (en) 2008-12-06 2016-04-06 Intra-Cellular Therapies, Inc. Organic compounds
TWI404721B (en) 2009-01-26 2013-08-11 Pfizer Amino-heterocyclic compounds
ES2612954T3 (en) 2009-03-05 2017-05-19 Astellas Pharma Inc. Quinoxaline Compounds
EP2414363B1 (en) 2009-03-31 2014-01-08 Boehringer Ingelheim International GmbH 1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators
WO2011016861A2 (en) 2009-08-05 2011-02-10 Intra-Cellular Therapies, Inc. Novel regulatory proteins and inhibitors
EP2538784B1 (en) 2010-02-25 2015-09-09 Merck Sharp & Dohme Corp. Benzimidazole derivatives useful anti-diabetic agents
EP2590657A4 (en) 2010-05-31 2014-02-12 Intra Cellular Therapies Inc Organic compounds
US9434730B2 (en) 2010-05-31 2016-09-06 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
WO2012004900A1 (en) * 2010-07-09 2012-01-12 Aska Pharmaceutical Co., Ltd. Thienopyrimidine compounds
KR101918909B1 (en) 2010-08-12 2018-11-15 베링거 인겔하임 인터내셔날 게엠베하 6-cycloalkyl-1,5-dihydro-pyrazolo[3,4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors
BR112013005439A2 (en) 2010-09-07 2017-09-19 Astellas Pharma Inc quinoxaline compounds
JP5888237B2 (en) 2010-09-07 2016-03-16 アステラス製薬株式会社 Pyrazoloquinoline compounds
WO2012076435A1 (en) * 2010-12-06 2012-06-14 Glaxo Group Limited Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp - pla2
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
PE20140859A1 (en) 2011-02-25 2014-07-25 Merck Sharp & Dohme NOVELTY DERIVATIVES OF CYCLIC AZABENZIMIDAZOLE USEFUL AS ANTIDIABETIC AGENTS
EP2906562B1 (en) * 2011-10-10 2016-10-05 H. Lundbeck A/S Pde9i with imidazo pyrazinone backbone
AU2013213603B2 (en) 2012-01-26 2017-02-02 H. Lundbeck A/S 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
US9840512B2 (en) 2013-02-22 2017-12-12 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel 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
EP3303339B1 (en) 2015-07-07 2021-01-13 H. Lundbeck A/S Pde9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
EP3558298A4 (en) 2016-12-20 2020-08-05 Merck Sharp & Dohme Corp. ANTIDIABETIC SPIROCHROMAN COMPOUNDS
EP3630113A4 (en) 2017-06-01 2021-02-24 Eisai R&D Management Co., Ltd. PHARMACEUTICAL COMPOSITION, INCLUDING PDE9 INHIBITOR
ES2980131T3 (en) 2017-06-01 2024-09-30 Eisai R&D Man Co Ltd Therapeutic agent for dementia that combines pyrazoloquinoline derivative and donepezil
SG11201909590XA (en) 2017-06-01 2019-11-28 Eisai R&D Man Co Ltd Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine
JP7269875B2 (en) 2017-06-01 2023-05-09 エーザイ・アール・アンド・ディー・マネジメント株式会社 Lewy Body Disease Treatment Agent Containing Pyrazoloquinoline Derivative
KR20210014662A (en) 2018-05-25 2021-02-09 이마라 인크. 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7H-imidazo[1, 5-a]Pyrazin-8-one monohydrate and crystalline form
EP3843737A4 (en) 2018-08-31 2022-06-01 Imara Inc. PDE9 INHIBITORS FOR THE TREATMENT OF SICKLE CELL DISEASE
CN111658653B (en) * 2019-03-08 2022-09-09 药捷安康(南京)科技股份有限公司 Use of phosphodiesterase inhibitors

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

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