CN101103033B - 作为pde2抑制剂的三唑并酞嗪 - Google Patents

作为pde2抑制剂的三唑并酞嗪 Download PDF

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Publication number
CN101103033B
CN101103033B CN2006800017646A CN200680001764A CN101103033B CN 101103033 B CN101103033 B CN 101103033B CN 2006800017646 A CN2006800017646 A CN 2006800017646A CN 200680001764 A CN200680001764 A CN 200680001764A CN 101103033 B CN101103033 B CN 101103033B
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Prior art keywords
phenyl
alkyl
methoxy
triazolo
phthalazin
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Expired - Fee Related
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CN2006800017646A
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English (en)
Chinese (zh)
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CN101103033A (zh
Inventor
B·施米特
S·维因布伦纳
D·弗洛克兹
R·库尔泽
H·特诺
H·-P·克利
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Takeda GmbH
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Nycomed GmbH
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
CN2006800017646A 2005-01-05 2006-01-04 作为pde2抑制剂的三唑并酞嗪 Expired - Fee Related CN101103033B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP05100045.3 2005-01-05
EP05100045 2005-01-05
EP05100044 2005-01-05
EP05100044.6 2005-01-05
PCT/EP2006/050041 WO2006072615A2 (en) 2005-01-05 2006-01-04 Triazolophthalazines as pde2-inhibitors

Publications (2)

Publication Number Publication Date
CN101103033A CN101103033A (zh) 2008-01-09
CN101103033B true CN101103033B (zh) 2010-08-04

Family

ID=36604687

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2006800017646A Expired - Fee Related CN101103033B (zh) 2005-01-05 2006-01-04 作为pde2抑制剂的三唑并酞嗪

Country Status (15)

Country Link
US (1) US8106047B2 (https=)
EP (1) EP1836207B1 (https=)
JP (1) JP5240899B2 (https=)
KR (1) KR20070095986A (https=)
CN (1) CN101103033B (https=)
AU (1) AU2006204454B2 (https=)
BR (1) BRPI0606379A2 (https=)
CA (1) CA2592007C (https=)
EA (1) EA012505B1 (https=)
ES (1) ES2397080T3 (https=)
IL (1) IL183919A (https=)
MX (1) MX2007008137A (https=)
NO (1) NO20073921L (https=)
NZ (1) NZ555661A (https=)
WO (1) WO2006072615A2 (https=)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005279221C9 (en) * 2004-09-02 2012-08-23 Takeda Gmbh Triazolophthalazines
EP1874775B1 (en) 2005-01-05 2012-10-10 Nycomed GmbH Triazolophthalazines as pde2-inhibitors
BRPI0606379A2 (pt) 2005-01-05 2009-06-23 Nycomed Gmbh triazolftalazinas
PH12012501361A1 (en) 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
US9540379B2 (en) 2011-01-31 2017-01-10 Boehringer Ingelheim International Gmbh (1,2,4)triazolo[4,3-A]quinoxaline derivatives as inhibitors of phosphodiesterases
SG195085A1 (en) 2011-06-07 2013-12-30 Pfizer Pyrazolo[3,4-d]pyrimidine compounds and their use as pde2 inhibitors and/or cyp3a4 inhibitors
MX361539B (es) 2012-04-25 2018-12-10 Takeda Pharmaceuticals Co Compuesto heterociclico nitrogenado.
EP2844660B1 (en) 2012-05-02 2017-11-01 Southern Research Institute Triazolopyridazine compounds, use as inhibitors of the kinase lrrk2, and methods for preparation thereof
EP2873669A4 (en) * 2012-07-13 2015-11-25 Takeda Pharmaceutical HETEROCYCLIC CONNECTION
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
EP2975031A4 (en) 2013-03-14 2017-04-19 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP6427491B2 (ja) 2013-07-03 2018-11-21 武田薬品工業株式会社 複素環化合物
ES2950424T3 (es) 2013-07-03 2023-10-09 Takeda Pharmaceuticals Co Compuesto de amida
EP3091983B1 (en) 2014-01-08 2019-10-02 Intra-Cellular Therapies, Inc. Pharmaceutical compositions comprising a pde-1 inhibitor and a pde-2 inhibitor
CN103694244B (zh) * 2014-01-09 2016-03-30 郑州大学 3,6位取代-1,2,4-三氮唑并[3,4-a]酞嗪类化合物及其制备和用途
DK3134413T3 (da) 2014-04-23 2019-10-14 Dart Neuroscience Cayman Ltd Substituerede [1,2,4]triazolo[1,5-a]pyrimidin-7-yl-forbindelser som pde2-inhibitorer
US10239882B2 (en) 2014-11-05 2019-03-26 Dart Neuroscience (Cayman) Ltd. Substituted 5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine compounds as PDE2 inhibitors
CN107205993B (zh) 2014-12-06 2021-03-09 细胞内治疗公司 有机化合物
US10300064B2 (en) 2014-12-06 2019-05-28 Intra-Cellular Therapies, Inc. Organic compounds
WO2016145614A1 (en) * 2015-03-17 2016-09-22 Merck Sharp & Dohme Corp. Triazolyl pyrimidinone compounds as pde2 inhibitors
WO2016154081A1 (en) 2015-03-26 2016-09-29 Merck Sharp & Dohme Corp. Pyrazolyl pyrimidinone compounds as pde2 inhibitors
WO2016179059A1 (en) 2015-05-05 2016-11-10 Merck Sharp & Dohme Corp. Heteroaryl-pyrimidinone compounds as pde2 inhibitors
WO2016183741A1 (en) 2015-05-15 2016-11-24 Merck Sharp & Dohme Corp. Pyrimidinone amide compounds as pde2 inhibitors
WO2016191935A1 (en) 2015-05-29 2016-12-08 Merck Sharp & Dohme Corp. 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
WO2016192083A1 (en) 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. 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
WO2017000277A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
EP3156405A1 (en) 2015-10-13 2017-04-19 Boehringer Ingelheim International GmbH Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide
AU2018371216B2 (en) 2017-11-23 2024-09-19 Oslo University Hospital Hf Treatment of tachycardia

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FI81350C (fi) 1982-01-18 1990-10-10 Lepetit Spa Analogfoerfarande foer framstaellning av nya, farmakologiskt aktiva 6-substituerade s-triatsolo/3,4-a/ ftalazinderivat.
IT1194310B (it) * 1983-07-12 1988-09-14 Lepetit Spa Derivati triazolo (3,4-a) ftalazinici 3,6-disostituiti
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ES2194205T3 (es) 1996-07-25 2003-11-16 Merck Sharp & Dohme Derivados de triazolo-piridazina sustituidos como ligandos para los receptores gaba.
EP0986562B1 (en) 1997-05-08 2002-08-07 MERCK SHARP & DOHME LTD. Substituted 1,2,4-triazolo 3,4-a]phthalazine derivatives as gaba alpha 5 ligands
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EP1261609B1 (de) * 1999-12-24 2004-11-03 Bayer HealthCare AG Triazolotriazinone und ihre verwendung
GB0028583D0 (en) 2000-11-23 2001-01-10 Merck Sharp & Dohme Therapeutic compounds
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NZ539163A (en) 2002-09-04 2007-03-30 Schering Corp Pyrazolo[1,5-a]pyrimidine compounds useful as cyclin dependent kinase (CDK) inhibitors
US20070179161A1 (en) 2003-03-31 2007-08-02 Vernalis (Cambridge) Limited. Pyrazolopyrimidine compounds and their use in medicine
AU2005279221C9 (en) 2004-09-02 2012-08-23 Takeda Gmbh Triazolophthalazines
BRPI0606379A2 (pt) 2005-01-05 2009-06-23 Nycomed Gmbh triazolftalazinas
EP1874775B1 (en) * 2005-01-05 2012-10-10 Nycomed GmbH Triazolophthalazines as pde2-inhibitors

Also Published As

Publication number Publication date
MX2007008137A (es) 2007-07-19
NZ555661A (en) 2010-11-26
IL183919A0 (en) 2007-10-31
CA2592007A1 (en) 2006-07-13
US8106047B2 (en) 2012-01-31
EA012505B1 (ru) 2009-10-30
WO2006072615A2 (en) 2006-07-13
NO20073921L (no) 2007-07-26
JP2008526717A (ja) 2008-07-24
JP5240899B2 (ja) 2013-07-17
BRPI0606379A2 (pt) 2009-06-23
US20080312225A1 (en) 2008-12-18
EA200701396A1 (ru) 2007-12-28
EP1836207B1 (en) 2012-10-10
AU2006204454B2 (en) 2011-11-10
IL183919A (en) 2011-06-30
CN101103033A (zh) 2008-01-09
EP1836207A2 (en) 2007-09-26
AU2006204454A1 (en) 2006-07-13
WO2006072615A3 (en) 2007-01-04
KR20070095986A (ko) 2007-10-01
CA2592007C (en) 2013-12-10
ES2397080T3 (es) 2013-03-04
HK1116776A1 (en) 2009-01-02

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