UA114529C2 - Похідні етинілу як модулятори активності рецептора mglur5 - Google Patents

Похідні етинілу як модулятори активності рецептора mglur5

Info

Publication number
UA114529C2
UA114529C2 UAA201504680A UAA201504680A UA114529C2 UA 114529 C2 UA114529 C2 UA 114529C2 UA A201504680 A UAA201504680 A UA A201504680A UA A201504680 A UAA201504680 A UA A201504680A UA 114529 C2 UA114529 C2 UA 114529C2
Authority
UA
Ukraine
Prior art keywords
modulators
ethynyl derivatives
receptor activity
mglur5 receptor
disease
Prior art date
Application number
UAA201504680A
Other languages
English (en)
Inventor
Гєорг Єшкє
Лотар Ліндеманн
Антоніо Річчі
Даніель Рюхер
Хайнц Штадлєр
Ерік Віейра
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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 Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of UA114529C2 publication Critical patent/UA114529C2/uk

Links

Classifications

    • 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

Abstract

EMBED ISISServer , І Даний винахід належить до похідних етинілу формули (І), де Υ позначає N або СН, R1 позначає фтор- або хлор-, R2 позначає водень або метил, або до їх фармацевтично прийнятної кислотно-адитивної солі. Тепер несподівано виявили, що сполуки загальної формули І є антагоністами метаботропного рецептора глутамату (негативні алостеричні модулятори) для застосування в лікуванні тривожності і болю, депресії, синдрому Мартіна-Белл, розладів аутичного спектра, хвороби Паркінсона і гастроезофагального рефлюксу (GERD).
UAA201504680A 2012-10-18 2013-10-15 Похідні етинілу як модулятори активності рецептора mglur5 UA114529C2 (uk)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
UA114529C2 true UA114529C2 (uk) 2017-06-26

Family

ID=47049067

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201504680A UA114529C2 (uk) 2012-10-18 2013-10-15 Похідні етинілу як модулятори активності рецептора mglur5

Country Status (27)

Country Link
US (1) US9227959B2 (uk)
EP (1) EP2909180B1 (uk)
JP (1) JP5989250B2 (uk)
KR (1) KR101684816B1 (uk)
CN (1) CN104718192B (uk)
AR (1) AR093042A1 (uk)
AU (1) AU2013333988B2 (uk)
BR (1) BR112015006454A8 (uk)
CA (1) CA2882520A1 (uk)
CL (1) CL2015000891A1 (uk)
CO (1) CO7200248A2 (uk)
CR (1) CR20150144A (uk)
EA (1) EA025667B1 (uk)
ES (1) ES2599553T3 (uk)
HK (1) HK1207639A1 (uk)
IL (1) IL237380A (uk)
MA (1) MA38012B1 (uk)
MX (1) MX2015004898A (uk)
MY (1) MY168937A (uk)
NZ (1) NZ705144A (uk)
PE (1) PE20150629A1 (uk)
PH (1) PH12015500398A1 (uk)
SG (1) SG11201501392TA (uk)
TW (1) TWI490208B (uk)
UA (1) UA114529C2 (uk)
WO (1) WO2014060398A1 (uk)
ZA (1) ZA201500856B (uk)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA026941B1 (ru) * 2012-10-18 2017-06-30 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5
PE20180358A1 (es) 2015-06-03 2018-02-21 Hoffmann La Roche Derivados de etinilo
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
US10849907B2 (en) 2017-12-08 2020-12-01 Boehringer Ingelheim International Gmbh Imidazopyridine derivatives and the use thereof as medicament
CN112867508B (zh) 2018-10-17 2023-09-15 勃林格殷格翰国际有限公司 4-吡啶基甲基-吗啉衍生物及其作为药物的用途
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
PE20211278A1 (es) * 2018-10-17 2021-07-19 Boehringer Ingelheim Int Derivados de 4-pirazin-2-ilmetil-morfolina y su uso como medicamento
CN113950478B (zh) 2019-06-04 2024-02-02 勃林格殷格翰国际有限公司 作为nr2b负向调节剂的嘌呤衍生物及其作为药物的用途，特别是用于治疗抑郁病症

Family Cites Families (6)

* 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
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
MX2009013169A (es) * 2007-06-03 2010-04-30 Univ Vanderbilt Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos.
US8853392B2 (en) * 2007-06-03 2014-10-07 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
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

Also Published As

Publication number Publication date
CA2882520A1 (en) 2014-04-24
AU2013333988B2 (en) 2017-03-09
MX2015004898A (es) 2015-07-21
CR20150144A (es) 2015-04-30
NZ705144A (en) 2018-09-28
EA025667B1 (ru) 2017-01-30
JP5989250B2 (ja) 2016-09-07
MY168937A (en) 2019-01-10
ES2599553T3 (es) 2017-02-02
WO2014060398A1 (en) 2014-04-24
AR093042A1 (es) 2015-05-13
TW201420571A (zh) 2014-06-01
BR112015006454A8 (pt) 2019-08-20
IL237380A (en) 2017-02-28
CL2015000891A1 (es) 2015-09-11
US9227959B2 (en) 2016-01-05
KR20150055044A (ko) 2015-05-20
PH12015500398B1 (en) 2015-04-27
CN104718192B (zh) 2016-08-31
PH12015500398A1 (en) 2015-04-27
MA38012A1 (fr) 2016-05-31
EP2909180A1 (en) 2015-08-26
JP2015531392A (ja) 2015-11-02
SG11201501392TA (en) 2015-05-28
BR112015006454A2 (pt) 2017-07-04
IL237380A0 (en) 2015-04-30
AU2013333988A1 (en) 2015-02-26
HK1207639A1 (zh) 2016-02-05
US20150225385A1 (en) 2015-08-13
MA38012B1 (fr) 2016-12-30
PE20150629A1 (es) 2015-05-11
KR101684816B1 (ko) 2016-12-20
CN104718192A (zh) 2015-06-17
EP2909180B1 (en) 2016-10-05
CO7200248A2 (es) 2015-02-27
ZA201500856B (en) 2016-08-31
TWI490208B (zh) 2015-07-01
EA201590699A1 (ru) 2015-07-30

Similar Documents

Publication Publication Date Title
PH12015500398B1 (en) Ethynyl derivatives as modulators of mglur5 receptor activity
MX2014000536A (es) Compuestos de 4-piperidinilo para usarse como inhibidores de tanquirasa.
PH12015502692A1 (en) Ethynyl derivatives as metabotropic glutamate receptor antagonists
PH12015500346A1 (en) Ethynyl derivatives as modulators of mglur5 receptor activity
PH12015500496B1 (en) Ethynyl derivatives as modulators of mglur5 receptor activity
PH12015500261A1 (en) Arylethynyl pyrimidines
MX2015008034A (es) Benzazepinas como ligandos de receptor de serotonina 5-ht2c y usos de las mismas.
PH12017502128A1 (en) Ethynyl derivatives
IL202282A0 (en) Prolinamide-tetrazole derivatives as nk3 receptor antagonists
TH167680B (th) อนุพันธ์เอไทนิลในฐานะโมดูเลเตอร์ของฤทธิ์ของ mglur5 รีเซปเตอร์
TH167680A (th) อนุพันธ์เอไทนิลในฐานะโมดูเลเตอร์ของฤทธิ์ของ mglur5 รีเซปเตอร์