JP6975511B2 - エチニル誘導体 - Google Patents

エチニル誘導体 Download PDF

Info

Publication number
JP6975511B2
JP6975511B2 JP2018505431A JP2018505431A JP6975511B2 JP 6975511 B2 JP6975511 B2 JP 6975511B2 JP 2018505431 A JP2018505431 A JP 2018505431A JP 2018505431 A JP2018505431 A JP 2018505431A JP 6975511 B2 JP6975511 B2 JP 6975511B2
Authority
JP
Japan
Prior art keywords
methyl
phenyl
phenylethynyl
difluoro
dihydro
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.)
Expired - Fee Related
Application number
JP2018505431A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018522037A5 (enExample
JP2018522037A (ja
Inventor
ヤーシュケ,ゲオルク
オハラ,フィオン
プランシャー,ジャン−マルク
リッチ,アントーニオ
リュエル,ダニエル
フィエイラ,エリック
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2018522037A publication Critical patent/JP2018522037A/ja
Publication of JP2018522037A5 publication Critical patent/JP2018522037A5/ja
Application granted granted Critical
Publication of JP6975511B2 publication Critical patent/JP6975511B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • 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)
JP2018505431A 2015-08-03 2016-08-02 エチニル誘導体 Expired - Fee Related JP6975511B2 (ja)

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 (3)

Publication Number Publication Date
JP2018522037A JP2018522037A (ja) 2018-08-09
JP2018522037A5 JP2018522037A5 (enExample) 2019-09-05
JP6975511B2 true JP6975511B2 (ja) 2021-12-01

Family

ID=53776452

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018505431A Expired - Fee Related JP6975511B2 (ja) 2015-08-03 2016-08-02 エチニル誘導体

Country Status (20)

Country Link
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

Family Cites Families (6)

* 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
CN105579447B (zh) * 2013-09-25 2018-11-13 豪夫迈·罗氏有限公司 乙炔基衍生物
TWI649310B (zh) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
SG11201607010XA (en) * 2014-02-25 2016-09-29 Hoffmann La Roche 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
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
CN107667107B (zh) 2021-05-18
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

Similar Documents

Publication Publication Date Title
JP5840793B2 (ja) Mglur5アロステリック調節因子としてのエチニル誘導体
JP5763094B2 (ja) エチニル誘導体
US9850232B2 (en) Heteroaromatic compounds and their use as dopamine D1 ligands
US10077272B2 (en) Heteroaromatic compounds and their use as dopamine D1 ligands
JP6134441B2 (ja) エチニル誘導体
JP6975511B2 (ja) エチニル誘導体
JP6286577B2 (ja) エチニル誘導体
JP6539749B2 (ja) mGluR4のモジュレーターとしての3−(4−エチニルフェニル)ヘキサヒドロピリミジン−2,4−ジオン誘導体
HK1246790B (zh) 乙炔基衍生物
HK1241881A1 (en) 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4
HK1202544A1 (zh) 芳基乙炔基衍生物
HK1241881B (zh) 作为mglur4的调节剂的3-(4-乙炔基苯基)六氢嘧啶-2,4-二酮衍生物
HK1220200B (zh) 乙炔基衍生物
HK1226404A1 (en) Ethynyl derivatives

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190726

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190726

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200611

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200616

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200915

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210216

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210514

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20211012

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20211104

R150 Certificate of patent or registration of utility model

Ref document number: 6975511

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees