KR20200013758A - 피라졸로피리미딘 pde9 억제제 - Google Patents

피라졸로피리미딘 pde9 억제제 Download PDF

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Publication number
KR20200013758A
KR20200013758A KR1020207000123A KR20207000123A KR20200013758A KR 20200013758 A KR20200013758 A KR 20200013758A KR 1020207000123 A KR1020207000123 A KR 1020207000123A KR 20207000123 A KR20207000123 A KR 20207000123A KR 20200013758 A KR20200013758 A KR 20200013758A
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KR
South Korea
Prior art keywords
ethyl
pyrimidine
pyrazolo
oxo
carbonitrile
Prior art date
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Withdrawn
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KR1020207000123A
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English (en)
Korean (ko)
Inventor
아쇽 아라사판
제이슨 엠. 콕스
존 에스. 디벤햄
주얀 구아
지아팡 헤
자히드 후세인
종 라이
더룬 리
동팡 멩
수바레카 라가반
스리람 티아가라잔
Original Assignee
머크 샤프 앤드 돔 코포레이션
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Publication of KR20200013758A publication Critical patent/KR20200013758A/ko
Withdrawn legal-status Critical Current

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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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
KR1020207000123A 2017-06-08 2018-06-06 피라졸로피리미딘 pde9 억제제 Withdrawn KR20200013758A (ko)

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 (1)

Publication Number Publication Date
KR20200013758A true KR20200013758A (ko) 2020-02-07

Family

ID=62779024

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020207000123A Withdrawn KR20200013758A (ko) 2017-06-08 2018-06-06 피라졸로피리미딘 pde9 억제제

Country Status (13)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230022982A (ko) * 2020-06-15 2023-02-16 노파르티스 아게 Cav1.2 활성제로서의 메틸 2-(플루오로메틸)-5-옥소-4-페닐-4,5,6,7-테트라하이드로-1h-시클로펜타[b]피리딘-3-카르복실레이트 및 메틸 2-(플루오로메틸)-5-옥소-4-페닐-1,4,5,7-테트라하이드로푸로[3,4-b]피리딘-3-카르복실레이트

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2019144010A (ru) * 2017-06-08 2021-07-13 Мерк Шарп И Доум Корп. Пиразолопиримидиновые ингибиторы pde9
EP3893881B1 (en) * 2018-12-12 2024-10-09 Merck Sharp & Dohme LLC Cyclobutyl pyrazolopyrimidine pde9 inhibitors
WO2020123272A1 (en) * 2018-12-12 2020-06-18 Merck Sharp & Dohme Corp. Pyrazolopyrimidine pde9 inhibitors
SG11202109781QA (en) 2019-03-08 2021-10-28 Transthera Sciences Nanjing Inc Uses of phosphodiesterase inhibitors
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

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE960441L (en) 1988-12-27 1990-06-27 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
WO2002009713A2 (de) 2000-08-01 2002-02-07 Bayer Aktiengesellschaft Selektive pde 2-inhibitoren als arzneimittel zur verbesserung der wahrnehmung
US6770645B2 (en) 2001-03-16 2004-08-03 Pfizer Inc. Pharmaceutically active compounds
EP1444009A1 (en) 2001-11-02 2004-08-11 Pfizer Products Inc. Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
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
WO2006135080A1 (ja) 2005-06-14 2006-12-21 Aska Pharmaceutical Co., Ltd. チエノピリミジン誘導体
EP2010505B1 (en) 2006-03-28 2012-12-05 Atir Holding S.A. Heterocyclic compounds and uses thereof in the treatment of sexual disorders
AU2007282678B2 (en) 2006-08-08 2012-09-27 Aska Pharmaceutical Co., Ltd. Quinazoline derivative
CA2671980C (en) 2006-12-13 2015-05-05 Aska Pharmaceutical Co., Ltd. Quinoxaline derivatives
PT2152712E (pt) 2007-05-11 2012-02-29 Pfizer Compostos amino-heterocíclicos
JP5498392B2 (ja) 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−ジヒドロ−ピラゾロ[3,4−d]ピリミジン−4−オン誘導体及びcns障害の治療のためのpde9aモジュレーターとしてのそれらの使用
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
PE20120505A1 (es) 2009-03-31 2012-05-09 Boehringer Ingelheim Int Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a
AR077859A1 (es) 2009-08-12 2011-09-28 Boehringer Ingelheim Int Compuestos para el tratamiento de trastornos del snc
AP2012006631A0 (en) * 2010-08-12 2012-12-31 Boehringer Ingelheim Int 6-Cycloalkyl-1, 5-dihydro-pyrazolo[3,4-D] pyrimidin-4-one derivatives and their use as PDE9A inhibitors
WO2012102405A1 (ja) 2011-01-28 2012-08-02 佐藤製薬株式会社 縮環化合物
US20130040971A1 (en) * 2011-02-14 2013-02-14 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of cns disorders
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
SG11201502728WA (en) 2011-10-10 2015-05-28 Lundbeck & Co As H 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
US10647727B2 (en) 2015-06-25 2020-05-12 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
US10370336B2 (en) 2015-07-29 2019-08-06 Merck Sharp & Dohme Corp. Phenyl-cyanoquinolinone PDE9 inhibitors
WO2017019723A1 (en) 2015-07-29 2017-02-02 Merck Sharp & Dohme Corp. Aza-cyanoquinolinone pde9 inhibitors
WO2017019726A1 (en) 2015-07-29 2017-02-02 Merck Sharp & Dohme Corp. Oxy-cyanoquinolinone pde9 inhibitors
RU2019144010A (ru) * 2017-06-08 2021-07-13 Мерк Шарп И Доум Корп. Пиразолопиримидиновые ингибиторы pde9

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230022982A (ko) * 2020-06-15 2023-02-16 노파르티스 아게 Cav1.2 활성제로서의 메틸 2-(플루오로메틸)-5-옥소-4-페닐-4,5,6,7-테트라하이드로-1h-시클로펜타[b]피리딘-3-카르복실레이트 및 메틸 2-(플루오로메틸)-5-옥소-4-페닐-1,4,5,7-테트라하이드로푸로[3,4-b]피리딘-3-카르복실레이트

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Publication number Publication date
US11028092B2 (en) 2021-06-08
US10934294B2 (en) 2021-03-02
BR112019025813A2 (pt) 2020-07-07
RU2019144010A (ru) 2021-07-13
AU2018281131B2 (en) 2022-01-20
US20180354955A1 (en) 2018-12-13
RU2019144010A3 (https=) 2021-10-01
EP3634964B1 (en) 2022-02-23
US20200140445A1 (en) 2020-05-07
CN111051308A (zh) 2020-04-21
WO2018226771A1 (en) 2018-12-13
MA53841A (fr) 2021-09-22
TW201902898A (zh) 2019-01-16
CA3064938A1 (en) 2018-12-13
EP3634964A1 (en) 2020-04-15
JP2020523309A (ja) 2020-08-06
AU2018281131A1 (en) 2019-12-05
MX2019014597A (es) 2020-02-05

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