AU2018281131B2 - Pyrazolopyrimidine PDE9 inhibitors - Google Patents

Pyrazolopyrimidine PDE9 inhibitors Download PDF

Info

Publication number
AU2018281131B2
AU2018281131B2 AU2018281131A AU2018281131A AU2018281131B2 AU 2018281131 B2 AU2018281131 B2 AU 2018281131B2 AU 2018281131 A AU2018281131 A AU 2018281131A AU 2018281131 A AU2018281131 A AU 2018281131A AU 2018281131 B2 AU2018281131 B2 AU 2018281131B2
Authority
AU
Australia
Prior art keywords
ethyl
pyrazolo
dihydro
oxo
pyrimidine
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2018281131A
Other languages
English (en)
Other versions
AU2018281131A1 (en
Inventor
Ashok Arasappan
Jason M. Cox
John S. Debenham
Zhuyan Guo
Jiafang He
Zahid Hussain
Zhong LAI
Derun Li
Dongfang Meng
Subharekha Raghavan
Sriram Tyagarajan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of AU2018281131A1 publication Critical patent/AU2018281131A1/en
Application granted granted Critical
Publication of AU2018281131B2 publication Critical patent/AU2018281131B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2018281131A 2017-06-08 2018-06-06 Pyrazolopyrimidine PDE9 inhibitors Ceased AU2018281131B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762516903P 2017-06-08 2017-06-08
US62/516,903 2017-06-08
US201862665840P 2018-05-02 2018-05-02
US62/665,840 2018-05-02
PCT/US2018/036172 WO2018226771A1 (en) 2017-06-08 2018-06-06 Pyrazolopyrimidine pde9 inhibitors

Publications (2)

Publication Number Publication Date
AU2018281131A1 AU2018281131A1 (en) 2019-12-05
AU2018281131B2 true AU2018281131B2 (en) 2022-01-20

Family

ID=62779024

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018281131A Ceased AU2018281131B2 (en) 2017-06-08 2018-06-06 Pyrazolopyrimidine PDE9 inhibitors

Country Status (13)

Country Link
US (2) US10934294B2 (enExample)
EP (1) EP3634964B1 (enExample)
JP (1) JP2020523309A (enExample)
KR (1) KR20200013758A (enExample)
CN (1) CN111051308A (enExample)
AU (1) AU2018281131B2 (enExample)
BR (1) BR112019025813A2 (enExample)
CA (1) CA3064938A1 (enExample)
MA (1) MA53841A (enExample)
MX (1) MX2019014597A (enExample)
RU (1) RU2019144010A (enExample)
TW (1) TW201902898A (enExample)
WO (1) WO2018226771A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10934294B2 (en) * 2017-06-08 2021-03-02 Merck Sharp & Dohme Corp. Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors
WO2020123271A1 (en) * 2018-12-12 2020-06-18 Merck Sharp & Dohme Corp. Cyclobutyl pyrazolopyrimidine pde9 inhibitors
WO2020123272A1 (en) * 2018-12-12 2020-06-18 Merck Sharp & Dohme Corp. Pyrazolopyrimidine pde9 inhibitors
AU2020235187B8 (en) * 2019-03-08 2024-02-08 Transthera Sciences (Nanjing), Inc. Uses of phosphodiesterase inhibitors
WO2021253180A1 (en) * 2020-06-15 2021-12-23 Novartis Ag Methyl (r) -2- (fluoromethyl) -5-oxo-4-phenyl-4, 5, 6, 7-tetrahydro-1h-cyclopenta [b] pyridine-3-carboxylate and methyl (r) -2- (fluoromethyl) -5-oxo-4-phenyl-1, 4, 5, 7-tetrahydrofuro [3, 4-b] pyridine-3-carboxylate as cav1.2 activators
CN114773256B (zh) * 2022-03-23 2024-05-03 中国农业大学 一种4-氰基哌啶的合成方法
CN117582909B (zh) * 2024-01-19 2024-04-02 天津凯莱英医药科技发展有限公司 一种连续生产5-单硝酸异山梨酯的系统和方法
CN120329388B (zh) * 2025-04-30 2025-09-26 中日友好医院(中日友好临床医学研究所) 一种双靶点多肽及其在心衰治疗中的应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2012110440A1 (en) * 2011-02-14 2012-08-23 Boehringer Ingelheim International Gmbh 6 - cyclobutyl - 1, 5 - dihydro - pyrazolo [3, 4-d] pyrimidin- 4 - one derivatives their use as pde9a inhibitors

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE71183B1 (en) 1988-12-27 1997-01-29 Takeda Chemical Industries Ltd Guanidine derivatives their production and insecticides
US5294612A (en) 1992-03-30 1994-03-15 Sterling Winthrop Inc. 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
DE19709877A1 (de) 1997-03-11 1998-09-17 Bayer Ag 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
ES2233685T3 (es) 2000-08-01 2005-06-16 Bayer Healthcare Ag Inhibidores selectivos de pde 2 como medicamentos para mejorar la percepcion.
US6770645B2 (en) 2001-03-16 2004-08-03 Pfizer Inc. Pharmaceutically active compounds
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
HUP0401998A2 (hu) 2001-11-02 2005-01-28 Pfizer Products Inc., PDE9 inhibitorok alkalmazása olyan gyógyszer előállítására, amellyel inzulin-rezisztencia szindróma és 2-es típusú diabétesz kezelhető
DE10238722A1 (de) 2002-08-23 2004-03-11 Bayer Ag Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse
DE10328479A1 (de) 2003-06-25 2005-01-13 Bayer Ag 6-Arylamino-5-cyano-4-pyrimidinone
US8293754B2 (en) 2005-06-14 2012-10-23 Aska Pharmaceutical Co., Ltd. Thienopyrimidine derivatives
CA2914168C (en) 2006-03-28 2018-05-08 Atir Holding S.A. Pyrido[1,2-a]pyrimidin-4-one derivatives and their use in the treatment of sexual disorders
US8101624B2 (en) 2006-08-08 2012-01-24 Aska Pharmaceutical Co., Ltd. Quinazoline derivatives
KR101563103B1 (ko) 2006-12-13 2015-10-23 아스카 세이야쿠 가부시키가이샤 퀴녹살린 유도체
AU2008249750B2 (en) 2007-05-11 2011-07-14 Pfizer Inc. Amino-heterocyclic compounds
US8648085B2 (en) 2007-11-30 2014-02-11 Boehringer Ingelheim International Gmbh 1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders
US9089572B2 (en) 2008-01-17 2015-07-28 California Institute Of Technology Inhibitors of p97
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
JP5453431B2 (ja) 2008-09-08 2014-03-26 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 ピラゾロピリミジン及びｃｎｓ障害の治療のためのそれらの使用
TWI404721B (zh) 2009-01-26 2013-08-11 Pfizer 胺基－雜環化合物
PT2414363E (pt) 2009-03-31 2014-02-26 Boehringer Ingelheim Int Derivados de 1-heterociclil-1,5-di-hidro-pirazolo[3,4- d]pirimidin-4-ona e sua utilização como moduladores de pde9a
TW201118099A (en) 2009-08-12 2011-06-01 Boehringer Ingelheim Int New compounds for the treatment of CNS disorders
JP5990106B2 (ja) 2011-01-28 2016-09-07 佐藤製薬株式会社 縮環化合物
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
EP2906562B1 (en) 2011-10-10 2016-10-05 H. Lundbeck A/S Pde9i with imidazo pyrazinone backbone
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
KR101706216B1 (ko) 2012-04-03 2017-02-13 한화테크윈 주식회사 고밀도 삼차원 영상 재구성 장치 및 방법
WO2014024125A1 (en) 2012-08-08 2014-02-13 Celon Pharma S.A. Pyrazolo[4,3-d]pyrimidin-7(6h)-one derivatives as pde9 inhibitors
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
WO2016191935A1 (en) 2015-05-29 2016-12-08 Merck Sharp & Dohme Corp. 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
WO2016209749A1 (en) 2015-06-25 2016-12-29 Merck Sharp & Dohme Corp. Substituted pyrazolo/imidazolo bicyclic compounds as pde2 inhibitors
WO2017000276A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Bicyclic heterocyclic compounds as pde2 inhibitors
US10376504B2 (en) 2015-07-29 2019-08-13 Merck, Sharp & Dohme Corp. Substituted quinolinones as PDE9 inhibitors
WO2017019724A1 (en) 2015-07-29 2017-02-02 Merck Sharp & Dohme Corp. Phenyl-cyanoquinolinone pde9 inhibitors
WO2017019726A1 (en) 2015-07-29 2017-02-02 Merck Sharp & Dohme Corp. Oxy-cyanoquinolinone pde9 inhibitors
US10934294B2 (en) * 2017-06-08 2021-03-02 Merck Sharp & Dohme Corp. Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2012110440A1 (en) * 2011-02-14 2012-08-23 Boehringer Ingelheim International Gmbh 6 - cyclobutyl - 1, 5 - dihydro - pyrazolo [3, 4-d] pyrimidin- 4 - one derivatives their use as pde9a inhibitors

Also Published As

Publication number Publication date
US11028092B2 (en) 2021-06-08
JP2020523309A (ja) 2020-08-06
BR112019025813A2 (pt) 2020-07-07
US20200140445A1 (en) 2020-05-07
KR20200013758A (ko) 2020-02-07
MX2019014597A (es) 2020-02-05
US10934294B2 (en) 2021-03-02
RU2019144010A3 (enExample) 2021-10-01
EP3634964B1 (en) 2022-02-23
WO2018226771A1 (en) 2018-12-13
TW201902898A (zh) 2019-01-16
AU2018281131A1 (en) 2019-12-05
RU2019144010A (ru) 2021-07-13
CA3064938A1 (en) 2018-12-13
US20180354955A1 (en) 2018-12-13
CN111051308A (zh) 2020-04-21
MA53841A (fr) 2021-09-22
EP3634964A1 (en) 2020-04-15

Similar Documents

Publication Publication Date Title
AU2018281131B2 (en) Pyrazolopyrimidine PDE9 inhibitors
EP3319966B1 (en) Bicyclic heterocyclic compounds as pde2 inhibitors
US10358435B2 (en) Triazolyl pyrimidinone compounds as PDE2 inhibitors
EP2763533A1 (en) Triazolyl pde10 inhibitors
WO2017003894A1 (en) Substituted triazolo bicyclic compounds as pde2 inhibitors
EP3302484B1 (en) 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
WO2012054366A2 (en) Substituted amino-triazolyl pde10 inhibitors
US10647727B2 (en) Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors
EP3894413B1 (en) Pyrazolopyrimidine pde9 inhibitors
US12247031B2 (en) Cyclobutyl pyrazolopyrimidine PDE9 inhibitors

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired