KR101637792B1 - Mglur5 알로스테릭 조절체로서의 에틴일 유도체 - Google Patents
Mglur5 알로스테릭 조절체로서의 에틴일 유도체 Download PDFInfo
- Publication number
- KR101637792B1 KR101637792B1 KR1020147011355A KR20147011355A KR101637792B1 KR 101637792 B1 KR101637792 B1 KR 101637792B1 KR 1020147011355 A KR1020147011355 A KR 1020147011355A KR 20147011355 A KR20147011355 A KR 20147011355A KR 101637792 B1 KR101637792 B1 KR 101637792B1
- Authority
- KR
- South Korea
- Prior art keywords
- phenylethynyl
- pyridin
- alkyl
- hydrogen
- alkoxy
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- 0 *C1=[U]C(C#C*)=NC=C1Br Chemical compound *C1=[U]C(C#C*)=NC=C1Br 0.000 description 1
- WRBSLLOTRGATJI-UHFFFAOYSA-N CC(C)(CCN1c(cc2)cnc2C#Cc2ccccc2)OC1=O Chemical compound CC(C)(CCN1c(cc2)cnc2C#Cc2ccccc2)OC1=O WRBSLLOTRGATJI-UHFFFAOYSA-N 0.000 description 1
- ZLZNZOHYIMYNIH-UHFFFAOYSA-N CC(C)(CN1c(cc2)cnc2C#Cc(cc2)ccc2F)N(C)C1=O Chemical compound CC(C)(CN1c(cc2)cnc2C#Cc(cc2)ccc2F)N(C)C1=O ZLZNZOHYIMYNIH-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11184331 | 2011-10-07 | ||
| EP11184331.4 | 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 |
|---|---|
| KR20140077943A KR20140077943A (ko) | 2014-06-24 |
| KR101637792B1 true KR101637792B1 (ko) | 2016-07-07 |
Family
ID=46968237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147011355A Expired - Fee Related KR101637792B1 (ko) | 2011-10-07 | 2012-10-04 | Mglur5 알로스테릭 조절체로서의 에틴일 유도체 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8969338B2 (https=) |
| EP (1) | EP2763977B1 (https=) |
| JP (1) | JP5840793B2 (https=) |
| KR (1) | KR101637792B1 (https=) |
| CN (1) | CN103857668B (https=) |
| AR (1) | AR088246A1 (https=) |
| AU (1) | AU2012320598B2 (https=) |
| BR (1) | BR112014007898A2 (https=) |
| CA (1) | CA2850082C (https=) |
| CL (1) | CL2014000819A1 (https=) |
| CO (1) | CO6900143A2 (https=) |
| CR (1) | CR20140094A (https=) |
| EA (1) | EA024973B1 (https=) |
| EC (1) | ECSP14013296A (https=) |
| ES (1) | ES2564884T3 (https=) |
| IL (1) | IL231783A (https=) |
| IN (1) | IN2014CN02478A (https=) |
| MX (1) | MX360667B (https=) |
| MY (1) | MY170822A (https=) |
| PE (1) | PE20141556A1 (https=) |
| PH (1) | PH12014500775A1 (https=) |
| SG (1) | SG11201401322UA (https=) |
| TW (1) | TWI468401B (https=) |
| UA (1) | UA110862C2 (https=) |
| WO (1) | WO2013050454A1 (https=) |
| ZA (1) | ZA201402069B (https=) |
Families Citing this family (13)
| 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 | |
| MX2015002823A (es) * | 2012-10-18 | 2015-05-15 | Hoffmann La Roche | Derivados de etilinilo como moduladores de la actividad del receptor de glutamato metabotropico 5 (mglur5). |
| UA116023C2 (uk) * | 2013-07-08 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як антагоністи метаботропного глутаматного рецептора |
| EP3049409B1 (en) * | 2013-09-25 | 2017-05-03 | F. Hoffmann-La Roche AG | Ethynyl derivatives |
| LT3303316T (lt) | 2015-06-03 | 2020-05-11 | F. Hoffmann-La Roche Ag | Etinilo dariniai |
| ES2733468T3 (es) | 2015-07-15 | 2019-11-29 | Hoffmann La Roche | Derivados de etinilo como moduladores de los receptores metabotrópicos de glutamato |
| 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 |
| WO2018015235A1 (en) | 2016-07-18 | 2018-01-25 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| JP7364553B2 (ja) * | 2017-08-17 | 2023-10-18 | エフ. ホフマン-ラ ロシュ アーゲー | パーキンソン病等の疾患を処置するためのイミダゾ[1,2-a]イミダゾール-2-オン誘導体 |
| CA3155013A1 (en) * | 2019-10-21 | 2021-04-29 | Ki Ho Lee | Use of imidazopyrimidine or imidazotriazine compound for prevention, alleviation, or treatment of developmental disability |
| CN116745291A (zh) | 2020-12-17 | 2023-09-12 | 阿斯利康(瑞典)有限公司 | N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺 |
| WO2024215771A1 (en) * | 2023-04-11 | 2024-10-17 | Southern Research Institute | Substituted phenyl ethynyl pyrimidines as potent inhibitors of alphaviruses |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011051201A1 (en) | 2009-10-27 | 2011-05-05 | F. Hoffmann-La Roche Ag | Positive allosteric modulators (pam) |
Family Cites Families (12)
| 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 |
| SG185285A1 (en) * | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| 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 |
| PL2702051T3 (pl) * | 2011-04-26 | 2015-08-31 | Hoffmann La Roche | Pochodne etynylu jako pozytywne allosteryczne modulatory 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 MY MYPI2014001004A patent/MY170822A/en unknown
- 2012-10-04 EP EP12767005.7A patent/EP2763977B1/en active Active
- 2012-10-04 KR KR1020147011355A patent/KR101637792B1/ko not_active Expired - Fee Related
- 2012-10-04 ES ES12767005.7T patent/ES2564884T3/es active Active
- 2012-10-04 SG SG11201401322UA patent/SG11201401322UA/en unknown
- 2012-10-04 EA EA201490722A patent/EA024973B1/ru not_active IP Right Cessation
- 2012-10-04 CN CN201280049430.1A patent/CN103857668B/zh not_active Expired - Fee Related
- 2012-10-04 WO PCT/EP2012/069599 patent/WO2013050454A1/en not_active Ceased
- 2012-10-04 IN IN2478CHN2014 patent/IN2014CN02478A/en unknown
- 2012-10-04 PH PH1/2014/500775A patent/PH12014500775A1/en unknown
- 2012-10-04 BR BR112014007898A patent/BR112014007898A2/pt not_active IP Right Cessation
- 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 AU AU2012320598A patent/AU2012320598B2/en not_active Ceased
- 2012-10-04 CA CA2850082A patent/CA2850082C/en not_active Expired - Fee Related
- 2012-10-04 JP JP2014533884A patent/JP5840793B2/ja not_active Expired - Fee Related
- 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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011051201A1 (en) | 2009-10-27 | 2011-05-05 | F. Hoffmann-La Roche Ag | Positive allosteric modulators (pam) |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR101637792B1 (ko) | Mglur5 알로스테릭 조절체로서의 에틴일 유도체 | |
| KR101431367B1 (ko) | 아릴에틴일 유도체 | |
| JP5463420B2 (ja) | ポジティブアロステリックモジュレータ(pam) | |
| KR101554803B1 (ko) | Mglur5의 양성 알로스테릭 조절체로서 에틴일 유도체 | |
| KR101573998B1 (ko) | Mglur5 조절체로서 5-(페닐/피리딘일-에틴일)-2-피리딘/2-피리미딘-카복스아미드 | |
| KR101576343B1 (ko) | 피라졸리딘-3-온 유도체 | |
| KR101656966B1 (ko) | 대사성 글루타메이트 수용체 조절체로서의 에틴일 유도체 | |
| JP6027251B2 (ja) | アリールエチニル誘導体 | |
| NZ621894B2 (en) | Ethynyl derivatives as mglur5 allosteric modulators | |
| HK1195298B (en) | Ethynyl derivatives as mglur5 allosteric modulators | |
| AU2012320509B8 (en) | Ethynyl derivatives as metabotropic glutamate receptor modulators | |
| UA110246C2 (en) | 5- (phenyl /piridinylethinyl) -2-pyridine / 2- pyrimidinecarboxamides as a modulator of mglur5 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
St.27 status event code: A-1-2-D10-D22-exm-PE0701 |
|
| GRNT | Written decision to grant | ||
| PR0701 | Registration of establishment |
St.27 status event code: A-2-4-F10-F11-exm-PR0701 |
|
| PR1002 | Payment of registration fee |
St.27 status event code: A-2-2-U10-U12-oth-PR1002 Fee payment year number: 1 |
|
| PG1601 | Publication of registration |
St.27 status event code: A-4-4-Q10-Q13-nap-PG1601 |
|
| FPAY | Annual fee payment |
Payment date: 20190624 Year of fee payment: 4 |
|
| PR1001 | Payment of annual fee |
St.27 status event code: A-4-4-U10-U11-oth-PR1001 Fee payment year number: 4 |
|
| PC1903 | Unpaid annual fee |
St.27 status event code: A-4-4-U10-U13-oth-PC1903 Not in force date: 20200702 Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE |
|
| PC1903 | Unpaid annual fee |
St.27 status event code: N-4-6-H10-H13-oth-PC1903 Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE Not in force date: 20200702 |
|
| R18-X000 | Changes to party contact information recorded |
St.27 status event code: A-5-5-R10-R18-oth-X000 |