MX360667B - Derivados de etinilo como moduladores alostericos del receptor de glutamato metabotropico del subtipo 5 (mglur5). - Google Patents
Derivados de etinilo como moduladores alostericos del receptor de glutamato metabotropico del subtipo 5 (mglur5).Info
- Publication number
- MX360667B MX360667B MX2014004144A MX2014004144A MX360667B MX 360667 B MX360667 B MX 360667B MX 2014004144 A MX2014004144 A MX 2014004144A MX 2014004144 A MX2014004144 A MX 2014004144A MX 360667 B MX360667 B MX 360667B
- Authority
- MX
- Mexico
- Prior art keywords
- hydrogen
- lower alkyl
- cycloalkyl
- attached
- form together
- 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
Abstract
La presente invención se refiere a derivados de etinilo de la fórmula I (ver Fórmula) en la que: U es N o CH, R8 es hidrógeno, halógeno, alquilo inferior o alcoxi inferior; Y es -N(R4)-, -O- o -C(R5R5')-; en las que R4 es hidrógeno o alquilo inferior y R5/R5' son con independencia hidrógeno, hidroxi, alquilo inferior o alcoxi inferior; V es -N(R6)- o -C(R7R7'), en las que R6 es hidrógeno o alquilo inferior y R7/R7' son con independencia entre sí hidrógeno, alquilo inferior, CH2-alcoxi inferior o junto con el átomo de carbono al que están unidos pueden formar un cicloalquilo C3-C6; R1 es fenilo o heteroarilo, que están opcionalmente sustituidos por halógeno, alquilo inferior o alcoxi inferior; m es el número 0 ó 1; en el caso de que m sea 1, R3/R3' son con independencia entre sí hidrógeno, alquilo inferior, CH2-alcoxi inferior o junto con el átomo de carbono al que están unidos pueden formar un cicloalquilo C3-C6 n es el número 0 ó 1; en el caso de que n sea 1, R2/R2' son con independencia entre sí hidrógeno, alquilo inferior, CH2-alcoxi inferior o junto con el átomo de carbono al que están unidos pueden formar un cicloalquilo C3-C6; o si m es el número 1 y n es el número 0, R3yR7 junto con los átomos de carbono a los que están unidos pueden formar un cicloalquilo C4-6;o si m es el número 1 y n es el número 1, R2 y R3 o R3 y R7 junto con los átomos de carbono a los que están unidos pueden formar un cicloalquilo C4-6; o una sal de adición de ácido farmacéuticamente aceptable, una mezcla racémica, o los correspondientes enantiómeros y/o isómeros ópticos y/o estereoisómeros de los mismos. Ahora se ha encontrado que los compuestos de la fórmula general I son moduladores alostéricos del receptor metabotrópico de glutamato del subtipo 5 (Mg1uR5).
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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2014004144A MX2014004144A (es) | 2014-07-28 |
| MX360667B true MX360667B (es) | 2018-11-13 |
Family
ID=46968237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014004144A MX360667B (es) | 2011-10-07 | 2012-10-04 | Derivados de etinilo como moduladores alostericos del receptor de glutamato metabotropico del subtipo 5 (mglur5). |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8969338B2 (es) |
| EP (1) | EP2763977B1 (es) |
| JP (1) | JP5840793B2 (es) |
| KR (1) | KR101637792B1 (es) |
| CN (1) | CN103857668B (es) |
| AR (1) | AR088246A1 (es) |
| AU (1) | AU2012320598B2 (es) |
| BR (1) | BR112014007898A2 (es) |
| CA (1) | CA2850082C (es) |
| CL (1) | CL2014000819A1 (es) |
| CO (1) | CO6900143A2 (es) |
| CR (1) | CR20140094A (es) |
| EA (1) | EA024973B1 (es) |
| EC (1) | ECSP14013296A (es) |
| ES (1) | ES2564884T3 (es) |
| HK (1) | HK1195298A1 (es) |
| IL (1) | IL231783A (es) |
| IN (1) | IN2014CN02478A (es) |
| MX (1) | MX360667B (es) |
| MY (1) | MY170822A (es) |
| PE (1) | PE20141556A1 (es) |
| SG (1) | SG11201401322UA (es) |
| TW (1) | TWI468401B (es) |
| UA (1) | UA110862C2 (es) |
| WO (1) | WO2013050454A1 (es) |
| ZA (1) | ZA201402069B (es) |
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 | |
| 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 |
| DK3049409T3 (en) * | 2013-09-25 | 2017-07-10 | 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 |
| 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 |
| 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 |
| PE20190382A1 (es) | 2016-07-18 | 2019-03-08 | Hoffmann La Roche | Derivados etinilo |
| CN111032659B (zh) * | 2017-08-17 | 2022-09-09 | 豪夫迈·罗氏有限公司 | 用于治疗诸如帕金森病的疾病的咪唑并[1，2-a]咪唑-2-酮衍生物 |
| AR124379A1 (es) | 2020-12-17 | 2023-03-22 | Astrazeneca Ab | N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)-quinolin-4-carboxamidas |
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 |
| 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 |
| WO2008151184A1 (en) * | 2007-06-03 | 2008-12-11 | 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) |
| 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 |
| EP2702050B1 (en) * | 2011-04-26 | 2016-05-18 | F.Hoffmann-La Roche Ag | Pyrazolidin-3-one derivatives |
| HUE025031T2 (en) * | 2011-04-26 | 2016-02-29 | Hoffmann La Roche | Ethinyl derivatives as positive allosteric modulators of MGLUR5 |
-
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 KR KR1020147011355A patent/KR101637792B1/ko active IP Right Grant
- 2012-10-04 SG SG11201401322UA patent/SG11201401322UA/en unknown
- 2012-10-04 AU AU2012320598A patent/AU2012320598B2/en not_active Ceased
- 2012-10-04 WO PCT/EP2012/069599 patent/WO2013050454A1/en active Application Filing
- 2012-10-04 CA CA2850082A patent/CA2850082C/en not_active Expired - Fee Related
- 2012-10-04 BR BR112014007898A patent/BR112014007898A2/pt not_active IP Right Cessation
- 2012-10-04 MY MYPI2014001004A patent/MY170822A/en unknown
- 2012-10-04 JP JP2014533884A patent/JP5840793B2/ja active Active
- 2012-10-04 ES ES12767005.7T patent/ES2564884T3/es active Active
- 2012-10-04 IN IN2478CHN2014 patent/IN2014CN02478A/en unknown
- 2012-10-04 CN CN201280049430.1A patent/CN103857668B/zh active Active
- 2012-10-04 TW TW101136749A patent/TWI468401B/zh not_active IP Right Cessation
- 2012-10-04 MX MX2014004144A patent/MX360667B/es active IP Right Grant
- 2012-10-04 PE PE2014000496A patent/PE20141556A1/es active IP Right Grant
- 2012-10-04 EP EP12767005.7A patent/EP2763977B1/en active Active
- 2012-10-04 EA EA201490722A patent/EA024973B1/ru not_active IP Right Cessation
- 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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| FG | Grant or registration |