CN106905324B - 具有咪唑并吡嗪酮骨架的pde9抑制剂 - Google Patents

具有咪唑并吡嗪酮骨架的pde9抑制剂 Download PDF

Info

Publication number
CN106905324B
CN106905324B CN201710247417.1A CN201710247417A CN106905324B CN 106905324 B CN106905324 B CN 106905324B CN 201710247417 A CN201710247417 A CN 201710247417A CN 106905324 B CN106905324 B CN 106905324B
Authority
CN
China
Prior art keywords
substituted
compound
mmol
400mhz
formula
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.)
Active
Application number
CN201710247417.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN106905324A (zh
Inventor
N.斯文斯特鲁普
K.B.西蒙森
L.K.拉斯穆森
K.朱尔
M.兰格加尔德
K.文
Y.王
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.)
H Lundbeck AS
Original Assignee
H Lundbeck AS
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 H Lundbeck AS filed Critical H Lundbeck AS
Priority to CN201710247417.1A priority Critical patent/CN106905324B/zh
Publication of CN106905324A publication Critical patent/CN106905324A/zh
Application granted granted Critical
Publication of CN106905324B publication Critical patent/CN106905324B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201710247417.1A 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂 Active CN106905324B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710247417.1A CN106905324B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2011001692 2011-10-10
CN201710247417.1A CN106905324B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂
CN201280076285.6A CN104703987B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201280076285.6A Division CN104703987B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂

Publications (2)

Publication Number Publication Date
CN106905324A CN106905324A (zh) 2017-06-30
CN106905324B true CN106905324B (zh) 2018-09-25

Family

ID=47019007

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201710247417.1A Active CN106905324B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂
CN201280076285.6A Active CN104703987B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201280076285.6A Active CN104703987B (zh) 2011-10-10 2012-10-09 具有咪唑并吡嗪酮骨架的pde9抑制剂

Country Status (15)

Country Link
US (2) US9643970B2 (enExample)
EP (2) EP2906562B1 (enExample)
JP (1) JP2015531401A (enExample)
CN (2) CN106905324B (enExample)
AU (2) AU2012323085B2 (enExample)
BR (1) BR112015007731B1 (enExample)
CA (1) CA2886885C (enExample)
HK (1) HK1211023A1 (enExample)
IL (2) IL237836A (enExample)
IN (1) IN2015DN02829A (enExample)
MA (1) MA37958B1 (enExample)
MX (2) MX381326B (enExample)
SG (1) SG11201502728WA (enExample)
TN (1) TN2015000100A1 (enExample)
WO (1) WO2013053690A1 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2015DN02829A (enExample) * 2011-10-10 2015-09-11 Lundbeck & Co As H
CR20160395A (es) 2014-02-13 2016-12-20 Incyte Corp Ciclopropilaminas como inhibidores de lsd1
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
ES2672797T3 (es) 2014-02-13 2018-06-18 Incyte Corporation Ciclopropilaminas como inhibidores de LSD1
MY183499A (en) 2014-02-13 2021-02-22 Incyte Corp Cyclopropylamines as lsd1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
TW201629064A (zh) 2014-10-10 2016-08-16 H 朗德貝克公司 作爲pde1抑制劑之三唑並吡酮
MA51438A (fr) 2015-04-03 2021-04-14 Incyte Corp Composés hétérocycliques utilisés en tant qu'inhibiteurs de lsd1
JO3627B1 (ar) * 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
EP4335497A3 (en) * 2015-07-07 2024-05-01 H. Lundbeck A/S Pde9 inhibitor with imidazo pyrazinone backbone for treatment of peripheral diseases
TW201717948A (zh) * 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
SG10202001219UA (en) 2015-08-12 2020-03-30 Incyte Corp Salts of an lsd1 inhibitor
JP6877423B2 (ja) * 2015-11-09 2021-05-26 アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag がんの処置において有用なジヒドロイミダゾピラジノン誘導体
TWI729109B (zh) 2016-04-12 2021-06-01 丹麥商H 朗德貝克公司 作爲PDE1抑制劑的1,5-二氫-4H-吡唑并[3,4-d]嘧啶-4-酮和1,5-二氫-4H-吡唑并[4,3-c]吡啶-4-酮
CR20180553A (es) 2016-04-22 2019-02-01 Incyte Corp Formulaciones de un inhibidor de lsd1
CA3025586A1 (en) * 2016-07-06 2018-01-11 Imara, Inc. Pde9 inhibitors for treatment of peripheral diseases
CN109843884B (zh) 2016-10-18 2022-03-04 H.隆德贝克有限公司 作为pde1抑制剂的咪唑并吡嗪酮、吡唑并嘧啶酮和吡唑并吡啶酮
RS60716B1 (sr) 2016-10-28 2020-09-30 H Lundbeck As Kombinovane terapije koje obuhvataju imidazopirazinone za lečenje psihijatrijskih i/ili kognitivnih poremećaja
MX2019004859A (es) 2016-10-28 2019-06-20 H Lundbeck As Tratamientos de combinacion que comprenden la administracion de imidazopirazinonas.
CN110325535A (zh) * 2017-02-27 2019-10-11 詹森药业有限公司 经哌啶、吗啉或哌嗪取代的作为oga抑制剂的[1,2,4]-三唑[1,5-a]-嘧啶基衍生物
MX2019014049A (es) * 2017-05-26 2020-07-28 Imara Inc Metodos de fabricacion y uso de inhibidores de pde9.
KR20200013758A (ko) 2017-06-08 2020-02-07 머크 샤프 앤드 돔 코포레이션 피라졸로피리미딘 pde9 억제제
US11147275B2 (en) 2017-11-23 2021-10-19 Basf Se Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi
MX2020012636A (es) 2018-05-25 2021-01-29 Imara Inc Formas de monohidrato y cristalinas de 6-[(3s,4s)-4-metil-1-(pirim idin-2- ilmetil)pirrolidin-3-il]-3-tetrahidropiran-4-il-7h-imidazo [1,5-a]pirazin-8- ona.
WO2019243528A1 (en) * 2018-06-20 2019-12-26 Janssen Pharmaceutica Nv Oga inhibitor compounds
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
BR112021003686A2 (pt) 2018-08-31 2021-05-18 Imara Inc. inibidores de pde9 para tratar doença falciforme
JP2022527630A (ja) * 2019-04-05 2022-06-02 イマラ インク. 鎌状赤血球症を治療するためのpde9阻害剤
TW202108585A (zh) * 2019-05-07 2021-03-01 美商伊馬拉公司 用於治療地中海型貧血之pde9抑制劑
WO2022036111A1 (en) * 2020-08-13 2022-02-17 Imara Inc. Methods and compositions for treating sickle cell disease

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003037899A1 (en) * 2001-11-02 2003-05-08 Pfizer Limited Pde9 inhibitors for treating cardiovascular disorders
WO2004096811A1 (en) * 2003-04-30 2004-11-11 Pfizer Products Inc. Pde9 inhibitors for treating type 2 diabetes, metabokic syndrome, and cardiovascular disease
CN101557826A (zh) * 2006-12-13 2009-10-14 Aska制药株式会社 泌尿系统疾病的治疗药
WO2012040230A1 (en) * 2010-09-20 2012-03-29 Envivo Pharmaceuticals, Inc. Imidazotriazinone compounds

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL135462A0 (en) 1997-11-12 2001-05-20 Bayer Ag 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
WO2000043392A2 (de) 1999-01-20 2000-07-27 Arzneimittelwerk Dresden Gmbh Verwendung von imidazo[1,5-a]-pyrido[3,2-e]-pyrazinonen als arzneimittel
PL370599A1 (en) 2001-11-02 2005-05-30 Pfizer Products Inc. Treatment of insulin resistance syndrome and type 2 diabetes with pde9 inhibitors
GB2388111A (en) 2002-05-01 2003-11-05 Bayer Ag Novel imidazotriazinone compounds
BRPI0416118A (pt) 2003-10-31 2007-01-02 Pfizer Prod Inc inibição da fosfodiesterase 9 como tratamento para estados relacionados com a obesidade
US7709468B2 (en) 2005-09-02 2010-05-04 Abbott Laboratories Imidazo based heterocycles
TW200815436A (en) * 2006-05-30 2008-04-01 Elbion Ag 4-amino-pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
WO2008029589A1 (en) 2006-09-08 2008-03-13 Tokuyama Corporation Method and equipment for producing group-iii nitride
EP2489667B1 (en) 2006-12-13 2015-04-15 ASKA Pharmaceutical Co., Ltd. Quinoxaline derivative
GEP20125405B (en) 2007-05-11 2012-02-27 Pfizer Amino-heterocyclic compounds
DE102007032349A1 (de) 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
TWI404721B (zh) 2009-01-26 2013-08-11 Pfizer 胺基-雜環化合物
WO2011028820A1 (en) 2009-09-02 2011-03-10 Concert Pharmaceuticals, Inc. Substituted derivatives of bicyclic [4.3.0] heteroaryl compounds
CA2861795C (en) 2011-10-07 2018-12-04 Eisai R&D Management Co., Ltd. Pyrazoloquinoline derivative
IN2015DN02829A (enExample) * 2011-10-10 2015-09-11 Lundbeck & Co As H
CN107082783B (zh) 2012-01-26 2019-03-22 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
EP2828262A4 (en) 2012-03-19 2015-09-23 Forum Pharmaceuticals Inc IMIDAZOTRIAZINONVERBINDUNGEN

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003037899A1 (en) * 2001-11-02 2003-05-08 Pfizer Limited Pde9 inhibitors for treating cardiovascular disorders
WO2004096811A1 (en) * 2003-04-30 2004-11-11 Pfizer Products Inc. Pde9 inhibitors for treating type 2 diabetes, metabokic syndrome, and cardiovascular disease
CN101557826A (zh) * 2006-12-13 2009-10-14 Aska制药株式会社 泌尿系统疾病的治疗药
WO2012040230A1 (en) * 2010-09-20 2012-03-29 Envivo Pharmaceuticals, Inc. Imidazotriazinone compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy;Patrick R. Verhoest,等;《J.Med.Chem.》;20091117;第52卷(第24期);7946-7949页 *

Also Published As

Publication number Publication date
BR112015007731A2 (pt) 2017-07-04
US9993477B2 (en) 2018-06-12
MX381326B (es) 2025-03-12
MA37958A1 (fr) 2017-11-30
MX370433B (es) 2019-12-13
CN104703987A (zh) 2015-06-10
AU2017201873A1 (en) 2017-04-06
CA2886885C (en) 2019-07-16
MX2019014982A (es) 2020-02-24
US20170173018A1 (en) 2017-06-22
US20150274736A1 (en) 2015-10-01
AU2012323085A1 (en) 2015-04-02
US9643970B2 (en) 2017-05-09
MA37958B1 (fr) 2018-10-31
MX2015004422A (es) 2015-10-15
AU2017201873C1 (en) 2018-08-02
IL253448A0 (en) 2017-09-28
AU2012323085B2 (en) 2017-03-09
WO2013053690A1 (en) 2013-04-18
BR112015007731B1 (pt) 2022-05-31
EP3121178B1 (en) 2018-09-19
EP3121178A1 (en) 2017-01-25
SG11201502728WA (en) 2015-05-28
IL237836A (en) 2017-07-31
JP2015531401A (ja) 2015-11-02
AU2017201873B2 (en) 2018-03-29
TN2015000100A1 (en) 2016-06-29
EP2906562A1 (en) 2015-08-19
HK1211023A1 (zh) 2016-05-13
EP2906562B1 (en) 2016-10-05
CN106905324A (zh) 2017-06-30
CN104703987B (zh) 2017-05-03
IN2015DN02829A (enExample) 2015-09-11
CA2886885A1 (en) 2013-04-18

Similar Documents

Publication Publication Date Title
CN106905324B (zh) 具有咪唑并吡嗪酮骨架的pde9抑制剂
JP7005582B2 (ja) ブルトン型チロシンキナーゼ(btk)インヒビターとしての多フルオロ置換化合物
US10626129B2 (en) Heteroaryl inhibitors of PDE4
JP6955482B2 (ja) Tnfアルファの修飾因子として有用なヘテロ環化合物
CN103917525B (zh) Lrrk2激酶活性的抑制剂
JP2022524974A (ja) Tyk2阻害剤およびその使用
JP2022542540A (ja) isoQC及び/又はQC酵素の阻害剤としてのN-置換-3,4-(縮合5-環)-5-フェニル-ピロリジン-2-オン化合物
TW201315727A (zh) 尿嘧啶衍生物及其醫藥用途
CN110997652B (zh) 哌啶酮甲酰基肽2受体激动剂
JP2018531993A (ja) Alkおよびsrpk阻害剤ならびに使用方法
IL293107A (en) Adenosine receptor antagonist compounds
TWI790810B (zh) Ret激酶抑制劑
TW202423921A (zh) 稠合的雜雙環抗病毒劑
WO2022253081A1 (zh) 氧化膦衍生物及其制备方法和应用
HK40096740A (zh) 杂芳基甲酰胺化合物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant