CN103649062B - 用于治疗tau病变如阿尔茨海默病的哌嗪噻唑衍生物 - Google Patents

用于治疗tau病变如阿尔茨海默病的哌嗪噻唑衍生物 Download PDF

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Publication number
CN103649062B
CN103649062B CN201280034129.3A CN201280034129A CN103649062B CN 103649062 B CN103649062 B CN 103649062B CN 201280034129 A CN201280034129 A CN 201280034129A CN 103649062 B CN103649062 B CN 103649062B
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China
Prior art keywords
ethyl
phenyl
piperazine
thiadiazol
difluoro
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Expired - Fee Related
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CN201280034129.3A
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English (en)
Chinese (zh)
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CN103649062A (zh
Inventor
赫拉德·格利菲恩
朱塞佩·切切里
马蒂亚斯·内特科文
卡特林·普林森
哈森·拉特尼
马克·罗森斯-伊文思
瓦尔特·维菲安
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reMYND NV
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reMYND NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P25/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
CN201280034129.3A 2011-08-17 2012-08-17 用于治疗tau病变如阿尔茨海默病的哌嗪噻唑衍生物 Expired - Fee Related CN103649062B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11177742.1 2011-08-17
EP11177742 2011-08-17
PCT/EP2012/066136 WO2013024168A1 (en) 2011-08-17 2012-08-17 Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease

Publications (2)

Publication Number Publication Date
CN103649062A CN103649062A (zh) 2014-03-19
CN103649062B true CN103649062B (zh) 2015-10-07

Family

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CN201280034129.3A Expired - Fee Related CN103649062B (zh) 2011-08-17 2012-08-17 用于治疗tau病变如阿尔茨海默病的哌嗪噻唑衍生物

Country Status (9)

Country Link
US (2) US9187440B2 (https=)
EP (1) EP2744798B1 (https=)
JP (1) JP6051218B2 (https=)
CN (1) CN103649062B (https=)
AU (1) AU2012296804B2 (https=)
CA (1) CA2841037C (https=)
ES (1) ES2573299T3 (https=)
PL (1) PL2744798T3 (https=)
WO (1) WO2013024168A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2744798T3 (pl) * 2011-08-17 2016-08-31 Remynd Nv Pochodne tiazolu piperazyny użyteczne w leczeniu tauopatii, takich jak choroba alzheimera
WO2015140130A1 (en) * 2014-03-17 2015-09-24 Remynd Nv Oxadiazole compounds
WO2025104092A1 (en) * 2023-11-13 2025-05-22 Remynd N.V. Modulators of septin 6 for use in the prevention and/or treatment of neurodegenerative disorders

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101137363A (zh) * 2005-01-07 2008-03-05 弗·哈夫曼-拉罗切有限公司 作为甘氨酸转运体1(GlyT-1)抑制剂用于治疗神经学和神经精神病学障碍的[4-(杂芳基)哌嗪-1-基]-(2,5-取代的-苯基)甲酮衍生物
WO2008099210A2 (en) * 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
CN101378757A (zh) * 2006-02-07 2009-03-04 瑞敏德股份有限公司 治疗神经变性疾病的噻二唑衍生物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102004032567A1 (de) 2004-07-05 2006-03-02 Grünenthal GmbH Substituierte 1-Propiolyl-piperazine
EP1705474B1 (en) 2005-03-21 2010-04-28 F.Hoffmann-La Roche Ag Method for determining lipophilicity
PE20070099A1 (es) * 2005-06-30 2007-02-06 Janssen Pharmaceutica Nv N-heteroarilpiperazinil ureas como moduladores de la amida hidrolasa del acido graso
EP2726470B1 (en) * 2011-07-01 2015-04-29 reMynd NV 1,2,4-thiadiazol-5-ylpiperazine derivatives useful in the treatment of neurodegenerative diseases
PL2744798T3 (pl) 2011-08-17 2016-08-31 Remynd Nv Pochodne tiazolu piperazyny użyteczne w leczeniu tauopatii, takich jak choroba alzheimera

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101137363A (zh) * 2005-01-07 2008-03-05 弗·哈夫曼-拉罗切有限公司 作为甘氨酸转运体1(GlyT-1)抑制剂用于治疗神经学和神经精神病学障碍的[4-(杂芳基)哌嗪-1-基]-(2,5-取代的-苯基)甲酮衍生物
CN101378757A (zh) * 2006-02-07 2009-03-04 瑞敏德股份有限公司 治疗神经变性疾病的噻二唑衍生物
WO2008099210A2 (en) * 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions

Also Published As

Publication number Publication date
HK1192848A1 (zh) 2014-09-05
US20140206699A1 (en) 2014-07-24
ES2573299T3 (es) 2016-06-07
US9187440B2 (en) 2015-11-17
CA2841037C (en) 2020-03-31
US9808456B2 (en) 2017-11-07
JP6051218B2 (ja) 2016-12-27
JP2014521737A (ja) 2014-08-28
AU2012296804A1 (en) 2014-01-30
US20160101102A1 (en) 2016-04-14
WO2013024168A1 (en) 2013-02-21
CA2841037A1 (en) 2013-02-21
PL2744798T3 (pl) 2016-08-31
AU2012296804B2 (en) 2017-04-20
CN103649062A (zh) 2014-03-19
EP2744798B1 (en) 2016-03-30
EP2744798A1 (en) 2014-06-25

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