BR112013026116A2 - derivados etinílicos como moduladores alostéricos positivos de mglur5 - Google Patents
derivados etinílicos como moduladores alostéricos positivos de mglur5Info
- Publication number
- BR112013026116A2 BR112013026116A2 BR112013026116A BR112013026116A BR112013026116A2 BR 112013026116 A2 BR112013026116 A2 BR 112013026116A2 BR 112013026116 A BR112013026116 A BR 112013026116A BR 112013026116 A BR112013026116 A BR 112013026116A BR 112013026116 A2 BR112013026116 A2 BR 112013026116A2
- Authority
- BR
- Brazil
- Prior art keywords
- hydrogen
- mglur5
- positive allosteric
- allosteric modulators
- lower alkyl
- Prior art date
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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P70/00—Climate change mitigation technologies in the production process for final industrial or consumer products
- Y02P70/50—Manufacturing or production processes characterised by the final manufactured product
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02T—CLIMATE CHANGE MITIGATION TECHNOLOGIES RELATED TO TRANSPORTATION
- Y02T10/00—Road transport of goods or passengers
- Y02T10/60—Other road transportation technologies with climate change mitigation effect
- Y02T10/70—Energy storage systems for electromobility, e.g. batteries
Abstract
resumo patente de invenção: "derivados etinílicos como moduladores alostéricos positivos de mglur5". a presente invenção refere-se a derivados etinílicos de fórmula i i em que x é n ou c-r, em que r é hidrogênio ou halogênio; g é n ou ch; com a condição de que no máximo um de g ou x pode ser nitrogênio; r1 é fenila ou piridinila, que são opcionalmente substituídos com halogênio; r2 é hidrogênio, alquil inferior, hidróxi, alcóxi inferior ou c(o)o-benzil; r3,r3', r4, r4', r6, r6' são independentemente um do outro hidrogênio ou alquil inferior; ou r6 e r4 podem formar, junto com o átomo de carbono ao qual eles estão ligados, um anel c4-6-cicloalquil, se m for 0 e n for 1 ou 2; r5 é hidrogênio ou alquil inferior; n é 0, 1 ou 2; m é 0 ou 1; com a condição de que n e m não sejam simultaneamente 0; ou a um sal de adição de ácido farmaceuticamente aceitável, a uma mistura racêmica, ou ao enantiômero do mesmo e/ou isômero óptico e/ou estereoisômero correspondente do mesmo. foi agora surpreendentemente descoberto que os compostos de fórmula geral i são moduladores alostéricos positivos (pam) do receptor de glutamato metabotrópico subtipo 5 (mglur5). eles podem ser usados para o tratamento de esquizofrenia ou de distúrbios cognitivos. 1/1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11163683 | 2011-04-26 | ||
| PCT/EP2012/057335 WO2012146551A1 (en) | 2011-04-26 | 2012-04-23 | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112013026116A2 true BR112013026116A2 (pt) | 2016-12-27 |
Family
ID=46025665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013026116A BR112013026116A2 (pt) | 2011-04-26 | 2012-04-23 | derivados etinílicos como moduladores alostéricos positivos de mglur5 |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8957213B2 (pt) |
| EP (1) | EP2702051B1 (pt) |
| JP (1) | JP5753627B2 (pt) |
| KR (1) | KR101554803B1 (pt) |
| CN (1) | CN103492373B (pt) |
| AR (1) | AR086036A1 (pt) |
| AU (1) | AU2012247653B2 (pt) |
| BR (1) | BR112013026116A2 (pt) |
| CA (1) | CA2829170C (pt) |
| CL (1) | CL2013003056A1 (pt) |
| CO (1) | CO6801734A2 (pt) |
| CR (1) | CR20130475A (pt) |
| CY (1) | CY1116391T1 (pt) |
| DK (1) | DK2702051T3 (pt) |
| EA (1) | EA022019B1 (pt) |
| ES (1) | ES2534090T3 (pt) |
| HK (1) | HK1191330A1 (pt) |
| HR (1) | HRP20150555T1 (pt) |
| HU (1) | HUE025031T2 (pt) |
| IL (1) | IL228835A (pt) |
| MA (1) | MA35133B1 (pt) |
| MX (1) | MX337443B (pt) |
| MY (1) | MY163164A (pt) |
| PE (1) | PE20141169A1 (pt) |
| PL (1) | PL2702051T3 (pt) |
| PT (1) | PT2702051E (pt) |
| RS (1) | RS53903B1 (pt) |
| SG (1) | SG194120A1 (pt) |
| SI (1) | SI2702051T1 (pt) |
| TW (2) | TW201306355A (pt) |
| UA (1) | UA110378C2 (pt) |
| WO (1) | WO2012146551A1 (pt) |
| ZA (1) | ZA201306586B (pt) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025031T2 (en) * | 2011-04-26 | 2016-02-29 | Hoffmann La Roche | Ethinyl derivatives as positive allosteric modulators of MGLUR5 |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| SI2875000T1 (sl) * | 2012-07-17 | 2017-01-31 | F.Hoffmann-La Roche Ag | Ariletinilni derivati |
| NZ703537A (en) * | 2012-10-18 | 2018-06-29 | Hoffmann La Roche | Ethynyl derivatives |
| UA116023C2 (uk) * | 2013-07-08 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як антагоністи метаботропного глутаматного рецептора |
| CN107849006B (zh) | 2015-06-03 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 乙炔基衍生物 |
| CN107580598B (zh) | 2015-07-15 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 作为代谢型谷氨酸受体调节剂的乙炔基衍生物 |
| US10423423B2 (en) * | 2015-09-29 | 2019-09-24 | International Business Machines Corporation | Efficiently managing speculative finish tracking and error handling for load instructions |
| PE20190382A1 (es) | 2016-07-18 | 2019-03-08 | Hoffmann La Roche | Derivados etinilo |
| AU2018347349A1 (en) * | 2017-10-10 | 2020-04-23 | Biogen Inc. | Process for preparing spiro derivatives |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI292318B (en) | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| EP2380889B1 (en) * | 2004-10-07 | 2013-06-26 | Merck Sharp & Dohme Corp. | Thiazolyl MGLUR5 antagonists and methods for their use |
| EP1809620B1 (en) | 2004-11-04 | 2010-12-29 | Addex Pharma SA | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| WO2007137954A1 (en) | 2006-05-31 | 2007-12-06 | F. Hoffmann-La Roche Ag | Aryl-4-ethynyl-isoxazole derivatives |
| WO2008151184A1 (en) * | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US8034806B2 (en) * | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| TW201020245A (en) | 2008-08-20 | 2010-06-01 | Schering Corp | Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
| US8586581B2 (en) | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| HUE025031T2 (en) * | 2011-04-26 | 2016-02-29 | Hoffmann La Roche | Ethinyl derivatives as positive allosteric modulators of MGLUR5 |
-
2012
- 2012-04-23 HU HUE12718153A patent/HUE025031T2/en unknown
- 2012-04-23 AU AU2012247653A patent/AU2012247653B2/en not_active Ceased
- 2012-04-23 CN CN201280019903.3A patent/CN103492373B/zh active Active
- 2012-04-23 RS RS20150192A patent/RS53903B1/en unknown
- 2012-04-23 ES ES12718153.5T patent/ES2534090T3/es active Active
- 2012-04-23 KR KR1020137031119A patent/KR101554803B1/ko active IP Right Grant
- 2012-04-23 JP JP2014506826A patent/JP5753627B2/ja active Active
- 2012-04-23 SG SG2013074810A patent/SG194120A1/en unknown
- 2012-04-23 PL PL12718153T patent/PL2702051T3/pl unknown
- 2012-04-23 BR BR112013026116A patent/BR112013026116A2/pt not_active IP Right Cessation
- 2012-04-23 MY MYPI2013003846A patent/MY163164A/en unknown
- 2012-04-23 PT PT127181535T patent/PT2702051E/pt unknown
- 2012-04-23 SI SI201230199T patent/SI2702051T1/sl unknown
- 2012-04-23 EP EP20120718153 patent/EP2702051B1/en active Active
- 2012-04-23 UA UAA201313475A patent/UA110378C2/uk unknown
- 2012-04-23 US US13/452,973 patent/US8957213B2/en active Active
- 2012-04-23 EA EA201391537A patent/EA022019B1/ru not_active IP Right Cessation
- 2012-04-23 CA CA2829170A patent/CA2829170C/en not_active Expired - Fee Related
- 2012-04-23 MX MX2013011105A patent/MX337443B/es active IP Right Grant
- 2012-04-23 WO PCT/EP2012/057335 patent/WO2012146551A1/en active Application Filing
- 2012-04-23 PE PE2013002401A patent/PE20141169A1/es active IP Right Grant
- 2012-04-23 DK DK12718153T patent/DK2702051T3/en active
- 2012-04-24 AR ARP120101405 patent/AR086036A1/es unknown
- 2012-04-24 TW TW101114538A patent/TW201306355A/zh unknown
- 2012-04-24 TW TW101114577A patent/TWI436993B/zh not_active IP Right Cessation
-
2013
- 2013-08-29 CO CO13205214A patent/CO6801734A2/es active IP Right Grant
- 2013-09-02 ZA ZA2013/06586A patent/ZA201306586B/en unknown
- 2013-09-23 CR CR20130475A patent/CR20130475A/es unknown
- 2013-10-10 IL IL228835A patent/IL228835A/en active IP Right Grant
- 2013-10-22 CL CL2013003056A patent/CL2013003056A1/es unknown
- 2013-11-22 MA MA36462A patent/MA35133B1/fr unknown
-
2014
- 2014-05-09 HK HK14104405.5A patent/HK1191330A1/xx unknown
-
2015
- 2015-01-06 US US14/590,530 patent/US9212171B2/en active Active
- 2015-05-20 CY CY20151100452T patent/CY1116391T1/el unknown
- 2015-05-26 HR HRP20150555TT patent/HRP20150555T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR112013026116A2 (pt) | derivados etinílicos como moduladores alostéricos positivos de mglur5 | |
| BR112014007898A2 (pt) | derivados de etinila como moduladores alostéricos de mglur5 | |
| BR112013021848A2 (pt) | 5-(fenil/piridinil-etinil)-2-piridina/2-pirimidina-carboxamidas como moduladores de mglur5 | |
| MY162998A (en) | Ethynyl derivatives | |
| PE20090655A1 (es) | Derivados de 2-aza-biciclo[2.2.2]octano para prevencion o tratamiento de psicosis | |
| EA200970793A1 (ru) | Модуляторы рецепторов, активируемых пролифераторами пероксисом | |
| BR112015006454A2 (pt) | derivados de etinila como moduladores de atividade de receptor de mglur5 | |
| MY165141A (en) | Pyrazolidin-3-one derivatives | |
| MX2012001799A (es) | Derivados de pirrolidina como antagonistas del receptor de neuroquinona 3 (nk3). | |
| CY1118595T1 (el) | Αρυλοαιθινυλο πυριμιδινες | |
| EA201692404A1 (ru) | Пептиды, выполняющие роль агонистов окситоцина | |
| EA201290610A1 (ru) | Сульфоновые соединения в качестве лигандов 5-htрецептора | |
| BR112015002320A2 (pt) | derivados de etinila como moduladores de atividade de receptor mglur5 | |
| BR112014008078A2 (pt) | derivados de etinila como moduladores do receptor de glutamato metabotrópico | |
| TH146315A (th) | อนุพันธ์เอทธินิลเป็นตัวควบคุมแบบอัลโลสเตอริคบวกของ mglur5 | |
| BR112012032576A2 (pt) | derivados de amino-tropano |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 9A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2622 DE 06/04/2021. |