CN111051308A - 吡唑并嘧啶pde9抑制剂 - Google Patents

吡唑并嘧啶pde9抑制剂 Download PDF

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Publication number
CN111051308A
CN111051308A CN201880037972.4A CN201880037972A CN111051308A CN 111051308 A CN111051308 A CN 111051308A CN 201880037972 A CN201880037972 A CN 201880037972A CN 111051308 A CN111051308 A CN 111051308A
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CN
China
Prior art keywords
ethyl
pyrimidine
pyrazolo
dihydro
oxo
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.)
Pending
Application number
CN201880037972.4A
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English (en)
Chinese (zh)
Inventor
A·阿拉萨潘
J·M·科克斯
J·S·德本汉姆
郭竹艳
贺家芳
Z·侯赛因
赖中
李德润
孟东方
S·拉格哈范
S·特亚加亚詹
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Merck Sharp and Dohme LLC
Original Assignee
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 LLC filed Critical Merck Sharp and Dohme LLC
Publication of CN111051308A publication Critical patent/CN111051308A/zh
Pending 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)
CN201880037972.4A 2017-06-08 2018-06-06 吡唑并嘧啶pde9抑制剂 Pending CN111051308A (zh)

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
CN111051308A true CN111051308A (zh) 2020-04-21

Family

ID=62779024

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880037972.4A Pending CN111051308A (zh) 2017-06-08 2018-06-06 吡唑并嘧啶pde9抑制剂

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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114773256A (zh) * 2022-03-23 2022-07-22 中国农业大学 一种4-氰基哌啶的合成方法
CN117582909A (zh) * 2024-01-19 2024-02-23 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
CN120329388A (zh) * 2025-04-30 2025-07-18 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

Families Citing this family (5)

* 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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103052639A (zh) * 2010-08-12 2013-04-17 贝林格尔.英格海姆国际有限公司 6-环烷基-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途
CN103459397A (zh) * 2011-02-14 2013-12-18 勃林格殷格翰国际有限公司 6-环丁基-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途

Family Cites Families (36)

* 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
WO2012102405A1 (ja) 2011-01-28 2012-08-02 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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103052639A (zh) * 2010-08-12 2013-04-17 贝林格尔.英格海姆国际有限公司 6-环烷基-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途
CN103459397A (zh) * 2011-02-14 2013-12-18 勃林格殷格翰国际有限公司 6-环丁基-1,5-二氢-吡唑并[3,4-d]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114773256A (zh) * 2022-03-23 2022-07-22 中国农业大学 一种4-氰基哌啶的合成方法
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
CN117582909A (zh) * 2024-01-19 2024-02-23 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
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
CN120329388A (zh) * 2025-04-30 2025-07-18 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
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

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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
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
KR20200013758A (ko) 2020-02-07
MX2019014597A (es) 2020-02-05

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