CN104718192B - 作为mglur5受体活性调节剂的乙炔基衍生物 - Google Patents

作为mglur5受体活性调节剂的乙炔基衍生物 Download PDF

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Publication number
CN104718192B
CN104718192B CN201380053660.XA CN201380053660A CN104718192B CN 104718192 B CN104718192 B CN 104718192B CN 201380053660 A CN201380053660 A CN 201380053660A CN 104718192 B CN104718192 B CN 104718192B
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compound
base
compounds
formula
formulas
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Expired - Fee Related
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Chinese (zh)
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CN104718192A (zh
Inventor
乔治·耶施克
洛塔尔·林德曼
安东尼奥·里奇
丹尼尔·吕厄
海因茨·施塔德勒
埃里克·维埃拉
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/22—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Epidemiology (AREA)
CN201380053660.XA 2012-10-18 2013-10-15 作为mglur5受体活性调节剂的乙炔基衍生物 Expired - Fee Related CN104718192B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12188940 2012-10-18
EP12188940.6 2012-10-18
PCT/EP2013/071500 WO2014060398A1 (en) 2012-10-18 2013-10-15 Ethynyl derivatives as modulators of mglur5 receptor activity

Publications (2)

Publication Number Publication Date
CN104718192A CN104718192A (zh) 2015-06-17
CN104718192B true CN104718192B (zh) 2016-08-31

Family

ID=47049067

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CN201380053660.XA Expired - Fee Related CN104718192B (zh) 2012-10-18 2013-10-15 作为mglur5受体活性调节剂的乙炔基衍生物

Country Status (26)

Country Link
US (1) US9227959B2 (enExample)
EP (1) EP2909180B1 (enExample)
JP (1) JP5989250B2 (enExample)
KR (1) KR101684816B1 (enExample)
CN (1) CN104718192B (enExample)
AR (1) AR093042A1 (enExample)
AU (1) AU2013333988B2 (enExample)
BR (1) BR112015006454A8 (enExample)
CA (1) CA2882520A1 (enExample)
CL (1) CL2015000891A1 (enExample)
CO (1) CO7200248A2 (enExample)
CR (1) CR20150144A (enExample)
EA (1) EA025667B1 (enExample)
ES (1) ES2599553T3 (enExample)
IL (1) IL237380A (enExample)
MA (1) MA38012B1 (enExample)
MX (1) MX2015004898A (enExample)
MY (1) MY168937A (enExample)
NZ (1) NZ705144A (enExample)
PE (1) PE20150629A1 (enExample)
PH (1) PH12015500398A1 (enExample)
SG (1) SG11201501392TA (enExample)
TW (1) TWI490208B (enExample)
UA (1) UA114529C2 (enExample)
WO (1) WO2014060398A1 (enExample)
ZA (1) ZA201500856B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2909178B1 (en) * 2012-10-18 2016-10-05 F. Hoffmann-La Roche AG Ethynyl derivatives as modulators of mglur5 receptor activity
JP6603334B2 (ja) 2015-06-03 2019-11-06 エフ．ホフマン−ラ ロシュ アーゲー エチニル誘導体
WO2017053769A1 (en) * 2015-09-25 2017-03-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Triazole derivatives as p2y14 receptor antagonists
ES2897050T3 (es) 2017-12-08 2022-02-28 Boehringer Ingelheim Int Derivados de imidazopiridina y el uso de los mismos como medicamento
MA53898B1 (fr) 2018-10-17 2023-03-31 Boehringer Ingelheim Int Dérivés de 4-pyrazin-2-ylméthyl-morpholine et leur utilisation comme médicament
CN112888684B (zh) 2018-10-17 2023-10-10 勃林格殷格翰国际有限公司 4-嘧啶-5-基甲基-吗啉衍生物及其作为药物的用途
WO2020079042A1 (en) 2018-10-17 2020-04-23 Boehringer Ingelheim International Gmbh 4-pyridinylmethyl-morpholine derivatives and the use thereof as medicament
US12398143B2 (en) 2019-06-04 2025-08-26 Boehringer Ingelheim International Gmbh Imidazopyrazine derivatives and the use thereof as medicament
JP7318015B2 (ja) 2019-06-04 2023-07-31 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 特に抑うつ病性障害の処置のための、ｎｒ２ｂネガティブ調節剤としてのプリン誘導体および医薬としてのその使用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1802367A (zh) * 2003-06-05 2006-07-12 弗·哈夫曼-拉罗切有限公司 作为谷氨酸受体拮抗剂的咪唑衍生物
US20090042855A1 (en) * 2007-06-03 2009-02-12 Conn P Jeffrey BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
WO2011051201A1 (en) * 2009-10-27 2011-05-05 F. Hoffmann-La Roche Ag Positive allosteric modulators (pam)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
CA2689282A1 (en) * 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
WO2013049255A1 (en) * 2011-09-26 2013-04-04 Vanderbilt University Substitued 5-(prop-1-yn-1-yl)picolinamide analogs as allosteric modulators of mglur5 receptors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1802367A (zh) * 2003-06-05 2006-07-12 弗·哈夫曼-拉罗切有限公司 作为谷氨酸受体拮抗剂的咪唑衍生物
US20090042855A1 (en) * 2007-06-03 2009-02-12 Conn P Jeffrey BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
WO2011051201A1 (en) * 2009-10-27 2011-05-05 F. Hoffmann-La Roche Ag Positive allosteric modulators (pam)

Also Published As

Publication number Publication date
JP2015531392A (ja) 2015-11-02
AR093042A1 (es) 2015-05-13
HK1207639A1 (zh) 2016-02-05
IL237380A0 (en) 2015-04-30
IL237380A (en) 2017-02-28
MA38012A1 (fr) 2016-05-31
CN104718192A (zh) 2015-06-17
TWI490208B (zh) 2015-07-01
TW201420571A (zh) 2014-06-01
CR20150144A (es) 2015-04-30
EP2909180A1 (en) 2015-08-26
CL2015000891A1 (es) 2015-09-11
EA025667B1 (ru) 2017-01-30
UA114529C2 (uk) 2017-06-26
EP2909180B1 (en) 2016-10-05
EA201590699A1 (ru) 2015-07-30
AU2013333988A1 (en) 2015-02-26
BR112015006454A8 (pt) 2019-08-20
WO2014060398A1 (en) 2014-04-24
CA2882520A1 (en) 2014-04-24
PH12015500398B1 (en) 2015-04-27
BR112015006454A2 (pt) 2017-07-04
KR20150055044A (ko) 2015-05-20
ES2599553T3 (es) 2017-02-02
PH12015500398A1 (en) 2015-04-27
US20150225385A1 (en) 2015-08-13
JP5989250B2 (ja) 2016-09-07
MA38012B1 (fr) 2016-12-30
KR101684816B1 (ko) 2016-12-20
US9227959B2 (en) 2016-01-05
NZ705144A (en) 2018-09-28
PE20150629A1 (es) 2015-05-11
AU2013333988B2 (en) 2017-03-09
CO7200248A2 (es) 2015-02-27
MY168937A (en) 2019-01-10
ZA201500856B (en) 2016-08-31
SG11201501392TA (en) 2015-05-28
MX2015004898A (es) 2015-07-21

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