BR112015002921A2 - derivados de ariletinila. - Google Patents

derivados de ariletinila.

Info

Publication number
BR112015002921A2
BR112015002921A2 BR112015002921A BR112015002921A BR112015002921A2 BR 112015002921 A2 BR112015002921 A2 BR 112015002921A2 BR 112015002921 A BR112015002921 A BR 112015002921A BR 112015002921 A BR112015002921 A BR 112015002921A BR 112015002921 A2 BR112015002921 A2 BR 112015002921A2
Authority
BR
Brazil
Prior art keywords
derivatives
formula
arylethynyl
mgiur5
autism
Prior art date
Application number
BR112015002921A
Other languages
English (en)
Inventor
Vieira Eric
Jaeschke Georg
Stadler Heinz
Lindemann Lothar
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 BR112015002921A2 publication Critical patent/BR112015002921A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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

Abstract

derivados de ariletinila a presente invenção refere-se a derivados de etinila de fórmula i em que r' é hidrogênio ou halogênio; r2 é c1_3-alquila ou -(ch2)m-0-ch3; n é 2 ou 3; m é 1 ou 2; ou a um sal de adição de ácido far-maceuticamente aceitável, a uma mistura racêmica, ou a seu enantiõ-mero correspondente elou isômero óptico elou estereoisômero dos mesmos. foi descoberto que os compostos de fórmula geral i são mo-duladores alostéricos do receptor metabotrópico de glutamato subtipo 5 (mgiur5) com propriedades melhoradas para o tratamento de es-quizofrenia, doenças cognitivas, síndrome de x frágil ou autismo.
BR112015002921A 2012-08-13 2013-08-06 derivados de ariletinila. BR112015002921A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12180209 2012-08-13
PCT/EP2013/066443 WO2014026880A1 (en) 2012-08-13 2013-08-06 Arylethynyl pyrimidines

Publications (1)

Publication Number Publication Date
BR112015002921A2 true BR112015002921A2 (pt) 2019-07-30

Family

ID=46851291

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015002921A BR112015002921A2 (pt) 2012-08-13 2013-08-06 derivados de ariletinila.

Country Status (36)

Country Link
US (1) US9199971B2 (pt)
EP (1) EP2882742B1 (pt)
JP (1) JP5974179B2 (pt)
KR (1) KR101747005B1 (pt)
CN (1) CN104540815B (pt)
AR (1) AR092097A1 (pt)
AU (1) AU2013304212B2 (pt)
BR (1) BR112015002921A2 (pt)
CA (1) CA2880257C (pt)
CL (1) CL2015000290A1 (pt)
CO (1) CO7180198A2 (pt)
CR (1) CR20150028A (pt)
CY (1) CY1118595T1 (pt)
DK (1) DK2882742T3 (pt)
EA (1) EA025165B1 (pt)
ES (1) ES2601511T3 (pt)
HK (1) HK1207378A1 (pt)
HR (1) HRP20161692T1 (pt)
HU (1) HUE030237T2 (pt)
IL (1) IL237015A (pt)
LT (1) LT2882742T (pt)
MA (1) MA37895B1 (pt)
MX (1) MX358011B (pt)
MY (1) MY170255A (pt)
NZ (1) NZ704858A (pt)
PE (1) PE20150685A1 (pt)
PH (1) PH12015500261B1 (pt)
PL (1) PL2882742T3 (pt)
PT (1) PT2882742T (pt)
RS (1) RS55397B1 (pt)
SG (1) SG11201501055SA (pt)
SI (1) SI2882742T1 (pt)
TW (1) TWI501958B (pt)
UA (1) UA113223C2 (pt)
WO (1) WO2014026880A1 (pt)
ZA (1) ZA201500582B (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY174339A (en) 2012-08-13 2020-04-09 Novartis Ag 1,4-disubstituted pyridazine analogs and methods for treating smn-deficiency-related conditions
NZ703537A (en) * 2012-10-18 2018-06-29 Hoffmann La Roche Ethynyl derivatives
CN107849006B (zh) * 2015-06-03 2020-11-13 豪夫迈·罗氏有限公司 乙炔基衍生物

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
EP1756086B1 (en) * 2004-06-01 2008-06-04 F.Hoffmann-La Roche Ag Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists
EP1809620B1 (en) 2004-11-04 2010-12-29 Addex Pharma SA Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
TW200811157A (en) * 2006-05-05 2008-03-01 Astrazeneca Ab mGluR5 modulators I
WO2008151184A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
WO2009054794A1 (en) * 2007-10-26 2009-04-30 Astrazeneca Ab Amino 1,2,4-triazole derivatives as modulators of mglur5
US8334287B2 (en) * 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
SG186107A1 (en) * 2010-07-09 2013-01-30 Recordati Ireland Ltd Novel spiroheterocyclic compounds as mglu5 antagonists
JPWO2012015024A1 (ja) * 2010-07-29 2013-09-12 大正製薬株式会社 エチニル−ピラゾール誘導体
EP2702050B1 (en) * 2011-04-26 2016-05-18 F.Hoffmann-La Roche Ag Pyrazolidin-3-one derivatives
US20130123254A1 (en) * 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (uk) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
UA110995C2 (uk) * 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
SI2875000T1 (sl) * 2012-07-17 2017-01-31 F.Hoffmann-La Roche Ag Ariletinilni derivati
EA025482B1 (ru) * 2012-09-27 2016-12-30 Ф. Хоффманн-Ля Рош Аг Производные арилэтинила

Also Published As

Publication number Publication date
PT2882742T (pt) 2016-11-16
MA37895B1 (fr) 2017-08-31
HUE030237T2 (en) 2017-04-28
HRP20161692T1 (hr) 2017-02-24
KR20150041132A (ko) 2015-04-15
ES2601511T3 (es) 2017-02-15
IL237015A (en) 2016-11-30
WO2014026880A1 (en) 2014-02-20
RS55397B1 (sr) 2017-04-28
MA37895A1 (fr) 2016-12-30
AU2013304212A1 (en) 2015-02-12
TWI501958B (zh) 2015-10-01
AR092097A1 (es) 2015-03-25
PH12015500261A1 (en) 2015-03-30
UA113223C2 (xx) 2016-12-26
KR101747005B1 (ko) 2017-06-27
MY170255A (en) 2019-07-13
US20150158848A1 (en) 2015-06-11
CR20150028A (es) 2015-02-27
MX2015001599A (es) 2015-05-11
CA2880257C (en) 2020-07-21
PE20150685A1 (es) 2015-05-11
NZ704858A (en) 2018-02-23
SG11201501055SA (en) 2015-03-30
CO7180198A2 (es) 2015-02-09
US9199971B2 (en) 2015-12-01
SI2882742T1 (sl) 2017-01-31
MX358011B (es) 2018-08-02
JP5974179B2 (ja) 2016-08-23
CN104540815A (zh) 2015-04-22
EA201590252A1 (ru) 2015-06-30
DK2882742T3 (en) 2016-12-12
PH12015500261B1 (en) 2015-03-30
ZA201500582B (en) 2016-08-31
CY1118595T1 (el) 2017-07-12
CL2015000290A1 (es) 2015-07-03
AU2013304212B2 (en) 2017-03-09
CA2880257A1 (en) 2014-02-20
JP2015528824A (ja) 2015-10-01
HK1207378A1 (en) 2016-01-29
EP2882742B1 (en) 2016-09-21
CN104540815B (zh) 2016-10-19
EA025165B1 (ru) 2016-11-30
PL2882742T3 (pl) 2017-03-31
LT2882742T (lt) 2016-12-12
EP2882742A1 (en) 2015-06-17
TW201410671A (zh) 2014-03-16

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements