AR093042A1 - Derivados de etinilo - Google Patents

Derivados de etinilo

Info

Publication number
AR093042A1
AR093042A1 ARP130103764A ARP130103764A AR093042A1 AR 093042 A1 AR093042 A1 AR 093042A1 AR P130103764 A ARP130103764 A AR P130103764A AR P130103764 A ARP130103764 A AR P130103764A AR 093042 A1 AR093042 A1 AR 093042A1
Authority
AR
Argentina
Prior art keywords
disease
formula
ethylene derivatives
gerd
stereoisomers
Prior art date
Application number
ARP130103764A
Other languages
English (en)
Inventor
Jaeschke Georg
Lindemann Lothar
Ricci Antonio
Rueher Daniel
Stadler Heinz
Vieira Eric
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR093042A1 publication Critical patent/AR093042A1/es

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

La presente se refiere a derivados de etinilo de la fórmula (1), en la que: Y es N o CH; R¹ es flúor o cloro; R² es hidrógeno o metilo; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a sus correspondientes enantiómeros y/o isómeros ópticos y/o estereoisómeros. Ahora se ha encontrado de modo sorprendente que los compuestos de la fórmula general 1 son antagonistas del receptor de glutamato metabotrópico (moduladores alostéricos negativos) que pueden utilizarse para el tratamiento de la ansiedad y el dolor, la depresión, el síndrome de la X frágil, los trastornos del espectro autista, la enfermedad de Parkinson y la enfermedad del reflujo gastroesofágico (GERD).
ARP130103764A 2012-10-18 2013-10-17 Derivados de etinilo AR093042A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12188940 2012-10-18

Publications (1)

Publication Number Publication Date
AR093042A1 true AR093042A1 (es) 2015-05-13

Family

ID=47049067

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103764A AR093042A1 (es) 2012-10-18 2013-10-17 Derivados de etinilo

Country Status (27)

Country Link
US (1) US9227959B2 (es)
EP (1) EP2909180B1 (es)
JP (1) JP5989250B2 (es)
KR (1) KR101684816B1 (es)
CN (1) CN104718192B (es)
AR (1) AR093042A1 (es)
AU (1) AU2013333988B2 (es)
BR (1) BR112015006454A8 (es)
CA (1) CA2882520A1 (es)
CL (1) CL2015000891A1 (es)
CO (1) CO7200248A2 (es)
CR (1) CR20150144A (es)
EA (1) EA025667B1 (es)
ES (1) ES2599553T3 (es)
HK (1) HK1207639A1 (es)
IL (1) IL237380A (es)
MA (1) MA38012B1 (es)
MX (1) MX2015004898A (es)
MY (1) MY168937A (es)
NZ (1) NZ705144A (es)
PE (1) PE20150629A1 (es)
PH (1) PH12015500398B1 (es)
SG (1) SG11201501392TA (es)
TW (1) TWI490208B (es)
UA (1) UA114529C2 (es)
WO (1) WO2014060398A1 (es)
ZA (1) ZA201500856B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013331782B2 (en) * 2012-10-18 2017-03-09 F. Hoffmann-La Roche Ag Ethynyl derivatives as modulators of mGluR5 receptor activity
PL3303316T3 (pl) 2015-06-03 2020-06-29 F. Hoffmann-La Roche Ag Pochodne etynylu
EP3353161B1 (en) * 2015-09-25 2021-07-21 The United States of America, as represented by the Secretary, Department of Health and Human Services Triazole derivatives as p2y14 receptor antagonists
AU2018379438B2 (en) 2017-12-08 2022-08-18 Boehringer Ingelheim International Gmbh Imidazopyridine derivatives and the use thereof as medicament
MA53898B1 (fr) * 2018-10-17 2023-03-31 Boehringer Ingelheim Int Dérivés de 4-pyrazin-2-ylméthyl-morpholine et leur utilisation comme médicament
TW202035395A (zh) 2018-10-17 2020-10-01 德商百靈佳殷格翰國際股份有限公司 4-嘧啶-5-基甲基-嗎啉衍生物及其作為藥物之用途
TW202035396A (zh) 2018-10-17 2020-10-01 德商百靈佳殷格翰國際股份有限公司 4-吡啶基甲基-嗎啉衍生物及其作為藥物之用途
EP3980401A1 (en) 2019-06-04 2022-04-13 Boehringer Ingelheim International GmbH Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders

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
CN101795689B (zh) * 2007-06-03 2014-11-19 范德比尔特大学 苯甲酰胺mGluR5正性变构调节剂和制备与使用所述调节剂的方法
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
TWI490208B (zh) 2015-07-01
AU2013333988B2 (en) 2017-03-09
UA114529C2 (uk) 2017-06-26
KR101684816B1 (ko) 2016-12-20
AU2013333988A1 (en) 2015-02-26
CL2015000891A1 (es) 2015-09-11
PH12015500398A1 (en) 2015-04-27
CA2882520A1 (en) 2014-04-24
MY168937A (en) 2019-01-10
CR20150144A (es) 2015-04-30
EA201590699A1 (ru) 2015-07-30
NZ705144A (en) 2018-09-28
EA025667B1 (ru) 2017-01-30
PH12015500398B1 (en) 2015-04-27
SG11201501392TA (en) 2015-05-28
BR112015006454A2 (pt) 2017-07-04
EP2909180B1 (en) 2016-10-05
KR20150055044A (ko) 2015-05-20
ES2599553T3 (es) 2017-02-02
MA38012A1 (fr) 2016-05-31
US9227959B2 (en) 2016-01-05
JP5989250B2 (ja) 2016-09-07
WO2014060398A1 (en) 2014-04-24
EP2909180A1 (en) 2015-08-26
MA38012B1 (fr) 2016-12-30
BR112015006454A8 (pt) 2019-08-20
ZA201500856B (en) 2016-08-31
MX2015004898A (es) 2015-07-21
CO7200248A2 (es) 2015-02-27
TW201420571A (zh) 2014-06-01
CN104718192A (zh) 2015-06-17
PE20150629A1 (es) 2015-05-11
US20150225385A1 (en) 2015-08-13
IL237380A0 (en) 2015-04-30
CN104718192B (zh) 2016-08-31
IL237380A (en) 2017-02-28
JP2015531392A (ja) 2015-11-02
HK1207639A1 (zh) 2016-02-05

Similar Documents

Publication Publication Date Title
AR093042A1 (es) Derivados de etinilo
AR080878A1 (es) Derivados heterociclicos de ariletinilo, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de la esquizofrenia y trastornos cognitivos.
AR096824A1 (es) Derivados de etinilo
AR093029A1 (es) Derivados de etilino
ECSP13012990A (es) Derivados de pirazolidin-3-ona
AR093043A1 (es) Derivados de etinilo
CY1118595T1 (el) Αρυλοαιθινυλο πυριμιδινες
AR091764A1 (es) Derivados de ariletinilo
CO2017012260A2 (es) Derivados de etinilo
TH167680B (th) อนุพันธ์เอไทนิลในฐานะโมดูเลเตอร์ของฤทธิ์ของ mglur5 รีเซปเตอร์

Legal Events

Date Code Title Description
FB Suspension of granting procedure