CN107667107B - 乙炔基衍生物 - Google Patents

乙炔基衍生物 Download PDF

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Publication number
CN107667107B
CN107667107B CN201680029481.6A CN201680029481A CN107667107B CN 107667107 B CN107667107 B CN 107667107B CN 201680029481 A CN201680029481 A CN 201680029481A CN 107667107 B CN107667107 B CN 107667107B
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China
Prior art keywords
methyl
phenyl
phenylethynyl
trione
difluoro
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Expired - Fee Related
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CN201680029481.6A
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English (en)
Chinese (zh)
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CN107667107A (zh
Inventor
乔治·耶施克
菲奥·奥哈拉
让-马克·普朗谢
安东尼奥·里奇
丹尼尔·吕厄
埃里克·维埃拉
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09Geometrical isomers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201680029481.6A 2015-08-03 2016-08-02 乙炔基衍生物 Expired - Fee Related CN107667107B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15179550 2015-08-03
EP15179550.7 2015-08-03
PCT/EP2016/068359 WO2017021384A1 (en) 2015-08-03 2016-08-02 Ethynyl derivatives

Publications (2)

Publication Number Publication Date
CN107667107A CN107667107A (zh) 2018-02-06
CN107667107B true CN107667107B (zh) 2021-05-18

Family

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Family Applications (1)

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CN201680029481.6A Expired - Fee Related CN107667107B (zh) 2015-08-03 2016-08-02 乙炔基衍生物

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US (1) US10011607B2 (enExample)
EP (1) EP3331882B1 (enExample)
JP (1) JP6975511B2 (enExample)
KR (1) KR20180030857A (enExample)
CN (1) CN107667107B (enExample)
AR (1) AR105556A1 (enExample)
AU (1) AU2016302696B2 (enExample)
BR (1) BR112017023951A2 (enExample)
CA (1) CA2983908A1 (enExample)
CL (1) CL2018000278A1 (enExample)
CO (1) CO2017011010A2 (enExample)
IL (1) IL255103B (enExample)
MX (1) MX2018001486A (enExample)
PE (1) PE20180357A1 (enExample)
PH (1) PH12018500247A1 (enExample)
RU (1) RU2722014C9 (enExample)
TW (1) TWI621619B (enExample)
UA (1) UA120888C2 (enExample)
WO (1) WO2017021384A1 (enExample)
ZA (1) ZA201707015B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201513742D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
AU2016302144B2 (en) 2015-08-03 2020-10-08 Bristol-Myers Squibb Company Heterocyclic compounds useful as modulators of TNF alpha
PT3331863T (pt) 2015-08-03 2020-05-22 Glenmark Pharmaceuticals Sa Novos compostos como moduladores de ror gama
TW202039425A (zh) 2018-12-21 2020-11-01 德商馬克專利公司 雙取代炔類衍生物、包含其之藥物組成及組、及用於製備其之製程

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015044075A1 (en) * 2013-09-25 2015-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
WO2015104271A1 (en) * 2014-01-10 2015-07-16 F. Hoffmann-La Roche Ag Ethynyl-imidazolin-2,4-dione derivatives as mglur4 modulators
WO2015128307A1 (en) * 2014-02-25 2015-09-03 F. Hoffmann-La Roche Ag Ethynyl derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010314891A1 (en) * 2009-11-06 2012-06-07 Vanderbilt University Aryl and heteroaryl sulfones as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
EP2702050B1 (en) * 2011-04-26 2016-05-18 F.Hoffmann-La Roche Ag Pyrazolidin-3-one derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015044075A1 (en) * 2013-09-25 2015-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
WO2015104271A1 (en) * 2014-01-10 2015-07-16 F. Hoffmann-La Roche Ag Ethynyl-imidazolin-2,4-dione derivatives as mglur4 modulators
WO2015128307A1 (en) * 2014-02-25 2015-09-03 F. Hoffmann-La Roche Ag Ethynyl derivatives

Also Published As

Publication number Publication date
JP2018522037A (ja) 2018-08-09
CA2983908A1 (en) 2017-02-09
KR20180030857A (ko) 2018-03-26
HK1246790A1 (zh) 2018-09-14
TW201718589A (zh) 2017-06-01
ZA201707015B (en) 2018-11-28
WO2017021384A1 (en) 2017-02-09
BR112017023951A2 (pt) 2018-07-24
PE20180357A1 (es) 2018-02-21
RU2722014C9 (ru) 2020-10-22
CN107667107A (zh) 2018-02-06
UA120888C2 (uk) 2020-02-25
IL255103A0 (en) 2017-12-31
MX2018001486A (es) 2018-03-15
EP3331882A1 (en) 2018-06-13
TWI621619B (zh) 2018-04-21
CL2018000278A1 (es) 2018-07-06
AU2016302696A1 (en) 2017-11-02
JP6975511B2 (ja) 2021-12-01
RU2722014C2 (ru) 2020-05-26
AR105556A1 (es) 2017-10-18
US10011607B2 (en) 2018-07-03
AU2016302696B2 (en) 2020-05-07
CO2017011010A2 (es) 2018-02-09
RU2018105872A3 (enExample) 2019-12-26
IL255103B (en) 2020-01-30
PH12018500247A1 (en) 2018-08-13
US20180127429A1 (en) 2018-05-10
EP3331882B1 (en) 2020-04-29
RU2018105872A (ru) 2019-09-05

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