CN106459060B - 作为磷酸二酯酶10a抑制剂的稠合的三唑衍生物 - Google Patents

作为磷酸二酯酶10a抑制剂的稠合的三唑衍生物 Download PDF

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Publication number
CN106459060B
CN106459060B CN201580025963.XA CN201580025963A CN106459060B CN 106459060 B CN106459060 B CN 106459060B CN 201580025963 A CN201580025963 A CN 201580025963A CN 106459060 B CN106459060 B CN 106459060B
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base
dimethyl
compound
triazol
pyrazine
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CN106459060A (zh
Inventor
拉法尔·莫茨兹斯基佩特科斯基
卢卡什·博雅斯基
马切伊·维乔雷克
雅各布·马耶尔
瑟尔维亚·亚诺夫斯卡
米科拉伊·马特洛克
马乌戈热塔·博罗科斯卡
菲利普·斯特凡尼亚克
莫妮卡·拉姆帕斯卡普日贝什
克日什托夫·杜比尔
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Celon Pharma SA
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Celon Pharma SA
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Lubricants (AREA)
CN201580025963.XA 2014-05-19 2015-05-14 作为磷酸二酯酶10a抑制剂的稠合的三唑衍生物 Active CN106459060B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PL408251A PL408251A1 (pl) 2014-05-19 2014-05-19 Skondensowane pochodne triazolu jako inhibitory fosfodiesterazy 10A
PLP.408251 2014-05-19
PCT/IB2015/053549 WO2015177688A1 (en) 2014-05-19 2015-05-14 Fused triazole derivatives as phosphodiesterase 10a inhibitors

Publications (2)

Publication Number Publication Date
CN106459060A CN106459060A (zh) 2017-02-22
CN106459060B true CN106459060B (zh) 2019-04-05

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US (1) US10138245B2 (enExample)
EP (1) EP3145930B1 (enExample)
JP (1) JP6455947B2 (enExample)
KR (1) KR102404650B1 (enExample)
CN (1) CN106459060B (enExample)
AU (1) AU2015263013B2 (enExample)
CA (1) CA2946258C (enExample)
DK (1) DK3145930T3 (enExample)
EA (1) EA030330B9 (enExample)
ES (1) ES2688084T3 (enExample)
HR (1) HRP20181027T1 (enExample)
HU (1) HUE039847T2 (enExample)
MX (1) MX367647B (enExample)
PL (2) PL408251A1 (enExample)
PT (1) PT3145930T (enExample)
SI (1) SI3145930T1 (enExample)
WO (1) WO2015177688A1 (enExample)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
WO2017007301A1 (en) * 2015-07-06 2017-01-12 Universiti Sains Malaysia Compound and method for inhibiting sirtuin activities
KR102587382B1 (ko) * 2016-04-29 2023-10-12 솔루스첨단소재 주식회사 유기 발광 화합물 및 이를 이용한 유기 전계 발광 소자
CN111410657B (zh) * 2019-01-08 2024-05-21 北京鼎材科技有限公司 一种发光材料及其应用
WO2025160629A1 (en) * 2024-01-31 2025-08-07 Certa Therapeutics Pty Ltd Proton sensing gpcr modulators
US20250276984A1 (en) * 2024-02-20 2025-09-04 Iambic Therapeutics, Inc. Solid state forms of her2 inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013003298A2 (en) * 2011-06-29 2013-01-03 Bristol-Myers Squibb Company Inhibitors of pde10

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2694983A1 (en) * 2007-07-17 2009-01-22 Combinatorx, Incorporated Treatments of b-cell proliferative disorders
TWI501965B (zh) * 2008-06-20 2015-10-01 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之新穎苯基咪唑衍生物
US8410117B2 (en) * 2010-03-26 2013-04-02 Hoffmann-La Roche Inc. Imidazopyrimidine derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013003298A2 (en) * 2011-06-29 2013-01-03 Bristol-Myers Squibb Company Inhibitors of pde10

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Classification of scaffold-hopping approaches;Hongmao Sun et al.;《Drug Discovery Today》;20120430;第17卷(第7-8期);310-324 *
Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors;Antonio Dore et al.;《European Journal of Medicinal Chemistry》;20140707;第84卷;181-193 *

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Publication number Publication date
CA2946258C (en) 2023-06-06
MX367647B (es) 2019-08-29
EA030330B1 (ru) 2018-07-31
EP3145930B1 (en) 2018-07-04
JP2017521364A (ja) 2017-08-03
US10138245B2 (en) 2018-11-27
CA2946258A1 (en) 2015-11-26
PL3145930T3 (pl) 2018-11-30
US20170114064A1 (en) 2017-04-27
KR20170005860A (ko) 2017-01-16
DK3145930T3 (en) 2018-09-24
CN106459060A (zh) 2017-02-22
KR102404650B1 (ko) 2022-06-02
JP6455947B2 (ja) 2019-01-23
HUE039847T2 (hu) 2019-02-28
MX2016015180A (es) 2017-03-23
WO2015177688A1 (en) 2015-11-26
ES2688084T3 (es) 2018-10-30
PL408251A1 (pl) 2015-11-23
AU2015263013B2 (en) 2018-10-04
PT3145930T (pt) 2018-10-11
EA030330B9 (ru) 2018-09-28
HRP20181027T1 (hr) 2018-08-24
AU2015263013A1 (en) 2016-11-17
EA201692264A1 (ru) 2017-04-28
EP3145930A1 (en) 2017-03-29
SI3145930T1 (sl) 2018-10-30

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