BR112014007898A2 - derivados de etinila como moduladores alostéricos de mglur5 - Google Patents
derivados de etinila como moduladores alostéricos de mglur5Info
- Publication number
- BR112014007898A2 BR112014007898A2 BR112014007898A BR112014007898A BR112014007898A2 BR 112014007898 A2 BR112014007898 A2 BR 112014007898A2 BR 112014007898 A BR112014007898 A BR 112014007898A BR 112014007898 A BR112014007898 A BR 112014007898A BR 112014007898 A2 BR112014007898 A2 BR 112014007898A2
- Authority
- BR
- Brazil
- Prior art keywords
- lower alkyl
- hydrogen
- cycloalkyl
- attached
- lower alkoxy
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
resumo patente de invenção: "derivados de etinila como moduladores alostéricos de mglur5". a presente invenção refere-se aos derivados de etinila de fórmula (i) em que u é n ou ch, r8 é hidrogênio, halogênio, alquila inferior ou alcóxi inferior; y é -n(r4)-, -o- ou -c(r5r5')-; em que r4 é hidrogênio ou alquila inferior e r5/r5' são independentemente hidrogênio, hidróxi, alquila inferior ou alcóxi inferior; v é -n(r6)- ou -c(r7r7'), em que r6 é hidrogênio ou alquila inferior e r7/r7' são, independentemente um do outro, hidrogênio, alquila inferior, ch2-alcóxi inferior, ou podem formar, juntamente com o átomo de carbono ao qual eles são ligados, uma c3-c6-cicloalquila; r1 é fenila ou heteroarila, que são opcionalmente substituídas por halogênio, alquila inferior ou alcóxi inferior; m é 0 ou 1; no caso m é 1, r3/r3' são, independentemente um do outro, hidrogênio, alquila inferior, ch2-alcóxi inferior, ou podem formar, juntamente com o átomo de carbono ao qual eles são ligados, uma c3-c6-cicloalquila; n é 0 ou 1; no caso n é 1, r2/r2' são independentemente um do outro hidrogênio, alquila inferior, ch2-alcóxi inferior ou podem formar, juntamente com o átomo de carbono ao qual eles são ligados, uma c3-c6-cicloalquila; ou se m for 1 e n for 0, r3 e r7 poderão formar, juntamente com os átomos de carbono ao qual eles são ligados, uma c4-6-cicloalquila; ou se m for 1 e n for 1, r2 e r3 ou r3 e r7 poderão formar, juntamente com os átomos de carbono ao qual eles são ligados, uma c4-6-cicloalquila; ou um sal de adição de ácido farmaceuticamente aceitável, uma mistura racêmica, ou seu enantiômero e/ou isômero ótico e/ou estereoisômero do mesmo. contatou-se que os compostos de formula geral i, são moduladores alostéricos do receptor subtipo 5 de glutamato metabotrópico 5 (mglur5).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11184331 | 2011-10-07 | ||
| PCT/EP2012/069599 WO2013050454A1 (en) | 2011-10-07 | 2012-10-04 | Ethynyl derivatives as mglur5 allosteric modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112014007898A2 true BR112014007898A2 (pt) | 2017-04-04 |
Family
ID=46968237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112014007898A BR112014007898A2 (pt) | 2011-10-07 | 2012-10-04 | derivados de etinila como moduladores alostéricos de mglur5 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8969338B2 (pt) |
| EP (1) | EP2763977B1 (pt) |
| JP (1) | JP5840793B2 (pt) |
| KR (1) | KR101637792B1 (pt) |
| CN (1) | CN103857668B (pt) |
| AR (1) | AR088246A1 (pt) |
| AU (1) | AU2012320598B2 (pt) |
| BR (1) | BR112014007898A2 (pt) |
| CA (1) | CA2850082C (pt) |
| CL (1) | CL2014000819A1 (pt) |
| CO (1) | CO6900143A2 (pt) |
| CR (1) | CR20140094A (pt) |
| EA (1) | EA024973B1 (pt) |
| EC (1) | ECSP14013296A (pt) |
| ES (1) | ES2564884T3 (pt) |
| HK (1) | HK1195298A1 (pt) |
| IL (1) | IL231783A (pt) |
| IN (1) | IN2014CN02478A (pt) |
| MX (1) | MX360667B (pt) |
| MY (1) | MY170822A (pt) |
| PE (1) | PE20141556A1 (pt) |
| SG (1) | SG11201401322UA (pt) |
| TW (1) | TWI468401B (pt) |
| UA (1) | UA110862C2 (pt) |
| WO (1) | WO2013050454A1 (pt) |
| ZA (1) | ZA201402069B (pt) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| CA2879489A1 (en) * | 2012-10-18 | 2014-04-24 | F.Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mglur5 receptor activity |
| UA116023C2 (uk) * | 2013-07-08 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як антагоністи метаботропного глутаматного рецептора |
| MA38885B1 (fr) * | 2013-09-25 | 2018-11-30 | Hoffmann La Roche | Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4) |
| AU2016273751B2 (en) | 2015-06-03 | 2020-04-02 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| JP6761821B2 (ja) | 2015-07-15 | 2020-09-30 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 代謝性グルタミン酸受容体モジュレーターとしてのエチニル誘導体 |
| CN106632243B (zh) * | 2015-10-28 | 2019-03-15 | 华领医药技术（上海）有限公司 | 吡咯烷衍生物 |
| SG11201811829QA (en) | 2016-07-18 | 2019-02-27 | Hoffmann La Roche | Ethynyl derivatives |
| EP3668873B1 (en) | 2017-08-17 | 2021-06-30 | F. Hoffmann-La Roche AG | Imidazo[1,2-a]imidazol-2-one derivatives for the treatment of diseases such as parkinson's disease |
| US20240101549A1 (en) | 2020-12-17 | 2024-03-28 | Astrazeneca Ab | N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)-quinoline-4-carboxamides |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3213780B2 (ja) | 1993-12-21 | 2001-10-02 | キヤノン株式会社 | 光学活性化合物、これを含有する液晶組成物、該液晶組成物を用いた液晶素子並びにこれらを用いた表示方法、表示装置 |
| JPH09151179A (ja) | 1995-11-30 | 1997-06-10 | Canon Inc | 光学活性化合物、これを含む液晶組成物、それを有する液晶素子、それらを用いた液晶装置及び表示方法 |
| US6410728B1 (en) | 2000-08-31 | 2002-06-25 | Abbott Laboratories | Oxazolidinone chemotherapeutic agents |
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals 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 |
| NZ581817A (en) | 2007-06-03 | 2012-05-25 | Univ Vanderbilt | 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) |
| 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 |
| US8772300B2 (en) * | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
| CA2829171C (en) * | 2011-04-26 | 2019-02-26 | F. Hoffmann-La Roche Ag | Pyrazolidin-3-one derivatives |
| KR101554803B1 (ko) * | 2011-04-26 | 2015-09-21 | 에프. 호프만-라 로슈 아게 | Mglur5의 양성 알로스테릭 조절체로서 에틴일 유도체 |
-
2012
- 2012-04-10 UA UAA201404621A patent/UA110862C2/uk unknown
- 2012-09-27 US US13/628,136 patent/US8969338B2/en active Active
- 2012-10-04 BR BR112014007898A patent/BR112014007898A2/pt not_active IP Right Cessation
- 2012-10-04 KR KR1020147011355A patent/KR101637792B1/ko active IP Right Grant
- 2012-10-04 WO PCT/EP2012/069599 patent/WO2013050454A1/en active Application Filing
- 2012-10-04 ES ES12767005.7T patent/ES2564884T3/es active Active
- 2012-10-04 JP JP2014533884A patent/JP5840793B2/ja active Active
- 2012-10-04 EA EA201490722A patent/EA024973B1/ru not_active IP Right Cessation
- 2012-10-04 TW TW101136749A patent/TWI468401B/zh not_active IP Right Cessation
- 2012-10-04 MY MYPI2014001004A patent/MY170822A/en unknown
- 2012-10-04 AU AU2012320598A patent/AU2012320598B2/en not_active Ceased
- 2012-10-04 PE PE2014000496A patent/PE20141556A1/es active IP Right Grant
- 2012-10-04 MX MX2014004144A patent/MX360667B/es active IP Right Grant
- 2012-10-04 EP EP12767005.7A patent/EP2763977B1/en active Active
- 2012-10-04 CA CA2850082A patent/CA2850082C/en not_active Expired - Fee Related
- 2012-10-04 CN CN201280049430.1A patent/CN103857668B/zh active Active
- 2012-10-04 IN IN2478CHN2014 patent/IN2014CN02478A/en unknown
- 2012-10-04 SG SG11201401322UA patent/SG11201401322UA/en unknown
- 2012-10-05 AR ARP120103716A patent/AR088246A1/es unknown
-
2014
- 2014-02-26 CR CR20140094A patent/CR20140094A/es unknown
- 2014-02-28 CO CO14043450A patent/CO6900143A2/es active IP Right Grant
- 2014-03-20 ZA ZA2014/02069A patent/ZA201402069B/en unknown
- 2014-03-27 IL IL231783A patent/IL231783A/en active IP Right Grant
- 2014-04-03 CL CL2014000819A patent/CL2014000819A1/es unknown
- 2014-04-07 EC ECSP14013296 patent/ECSP14013296A/es unknown
- 2014-07-08 HK HK14106907.3A patent/HK1195298A1/zh unknown
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Legal Events
| Date | Code | Title | Description |
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| 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 |
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| 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. |
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| 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: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2640 DE 10-08-2021 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |