DK2721012T3 - Biclo(3.1.0)hexan-2,6-dicarboxylsyre-derivater som MGLU2-receptoragonist - Google Patents
Biclo(3.1.0)hexan-2,6-dicarboxylsyre-derivater som MGLU2-receptoragonist Download PDFInfo
- Publication number
- DK2721012T3 DK2721012T3 DK12729769.5T DK12729769T DK2721012T3 DK 2721012 T3 DK2721012 T3 DK 2721012T3 DK 12729769 T DK12729769 T DK 12729769T DK 2721012 T3 DK2721012 T3 DK 2721012T3
- Authority
- DK
- Denmark
- Prior art keywords
- hydrogen
- optionally substituted
- pharmaceutically acceptable
- fluorine atoms
- hexane
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/14—Nitrogen atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (13)
1. Forbindelse med formlen
R2 er hydrogen, 2,2-dimethyl-propionyloxymethyl eller benzyl, hvor benzyl er eventuelt substitueret med et til to fluorinatomer, -CrC3-alkyl eventuelt sub-stitueret med 1 til 3 fluorinatomer, eller -CrC3-alkoxy; R3 er hydrogen, 2,2-dimethyl- propionyloxymethyl eller benzyl, hvor benzyl er eventuelt substitueret med et til to fluorinatomer, -CrC3-alkyl eventuelt substitueret med 1 til 3 fluorinatomer, eller -CrC3-alkoxy; R4 er hydrogen, (2S)-2-aminopropanoyl, (2S)-2-amino-4-methylsulfanyl-buta-noyl, (2S)-2-amino-4-methyl-pentanoyl eller 2-aminoacetyl; R5 er -CrC3-alkyl eventuelt substitueret med 1 til 3 fluorinatomer, -NH2 eller cycl o propyl; forudsat, at nar R2 og/eller R3 ikke er hydrogen, er R4 hydrogen; forudsat, at nar R4 ikke er hydrogen, er R2 og/eller R3 hydrogen; og forudsat, at R5 kan vasre hydrogen, nar sulfuratomet er bundet til bicyclo-[3.1.0]hexan-ringsystemet i S-konfigurationen; eller et farmaceutisk accepta-belt salt deraf.
2. Forbindelse ifolge krav 1, hvor
R2 er hydrogen, 2,2-dimethyl-propionyloxymethyl eller benzyl, hvor benzyl er eventuelt substitueret med et til to fluorinatomer, -CrC3-alkyl eventuelt sub-stitueret med 1 til 3 fluorinatomer, eller -CrC3-alkoxy; R3 er hydrogen, 2,2-dimethyl-propionyloxymethyl eller benzyl, hvor benzyl er eventuelt substitueret med et til to fluorinatomer, -CrC3-alkyl eventuelt substitueret med 1 til 3 fluorinatomer, eller -CrC3-alkoxy; R4 er hydrogen, (2S)-2-aminopropanoyl, (2S)-2-amino-4-methylsulfanyl-buta-noyl, (2S)-2-amino-4-methyl-pentanoyl eller 2-aminoacetyl; R5 er -CrC3-alkyl eventuelt substitueret med 1 til 3 fluorinatomer, -NH2 eller cyclopropyl; forudsat, at nar R2 og/eller R3 ikke er hydrogen, er R4 hydrogen; forudsat, at nar R4 ikke er hydrogen, er R2 og/eller R3 hydrogen; eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifolge et af kravene 1 til 2, hvor R2 er hydrogen, 2,2-dimethyl- propionyloxymethyl eller benzyl eventuelt substitueret med et til to fluorinatomer, -CF3 eller -OCH3 ; og R3 er hydrogen, 2,2-dimethyl-propionyloxymethyl eller benzyl eventuelt substitueret med et til to fluorinatomer, -CF3 eller -OCH3; eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifolge et af kravene 1 til 3, hvor R1 er
eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifolge et af kravene 1 til 4, hvor R2 er hydrogen; eller et farma-ceutisk acceptabelt salt deraf.
6. Forbindelse ifolge et af kravene 1 til 5, hvor R3 er hydrogen; eller et farma-ceutisk acceptabelt salt deraf.
7. Forbindelse ifolge et af kravene 1 til 6, hvor R4 er hydrogen; eller et farma-ceutisk acceptabelt salt deraf.
8. Farmaceutisk sammensastning omfattende en forbindelse ifolge et af kravene 1 til 7, eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel basrer, fortyndingsmiddel eller hjaalpestof.
9. Forbindelse ifolge et af kravene 1 til 7, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling.
10. Forbindelse ifolge et af kravene 1 til 7, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af en psykiatrisk lidelse udvalgt fra gruppen bestaende af bipolar lidelse, skizofreni og generaliseret angstlidelse.
11. Forbindelse til anvendelse ifolge krav 10, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af bipolar lidelse.
12. Forbindelse ifolge krav 10, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af skizofreni.
13. Forbindelse ifolge krav 10, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af generaliseret angstlidelse.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11382208 | 2011-06-17 | ||
| US201161522791P | 2011-08-12 | 2011-08-12 | |
| PCT/US2012/041229 WO2012173850A1 (en) | 2011-06-17 | 2012-06-07 | Bicyclo (3.1.0) hexane- 2, 6 -dicarboxylic acid derivatives as mglu2 receptor agonist |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2721012T3 true DK2721012T3 (da) | 2016-08-15 |
Family
ID=47357416
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12729769.5T DK2721012T3 (da) | 2011-06-17 | 2012-06-07 | Biclo(3.1.0)hexan-2,6-dicarboxylsyre-derivater som MGLU2-receptoragonist |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9296710B2 (da) |
| EP (1) | EP2721012B1 (da) |
| JP (1) | JP5945592B2 (da) |
| KR (1) | KR101598679B1 (da) |
| CN (1) | CN103596933B (da) |
| AU (1) | AU2012271024B2 (da) |
| BR (1) | BR112013031928B1 (da) |
| CA (1) | CA2836485C (da) |
| CY (1) | CY1117682T1 (da) |
| DK (1) | DK2721012T3 (da) |
| EA (1) | EA023553B1 (da) |
| ES (1) | ES2587204T3 (da) |
| HR (1) | HRP20160676T1 (da) |
| HU (1) | HUE030171T2 (da) |
| MX (1) | MX2013014802A (da) |
| PL (1) | PL2721012T3 (da) |
| PT (1) | PT2721012T (da) |
| RS (1) | RS54888B1 (da) |
| SI (1) | SI2721012T1 (da) |
| WO (1) | WO2012173850A1 (da) |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993006127A1 (en) | 1991-09-17 | 1993-04-01 | Warner-Lambert Company | Novel amino acid prodrug renin inhibitors |
| US5576323A (en) | 1993-12-03 | 1996-11-19 | Eli Lilly And Company | Excitatory amino acid receptor antagonists |
| US5849525A (en) | 1994-03-09 | 1998-12-15 | Brigham And Women's Hospital, Inc. | Compositions corresponding to a proton-coupled peptide transporter and methods of making and using same |
| IL124487A (en) | 1995-11-16 | 2001-01-11 | Lilly Co Eli | Excitatory amino acid derivatives, their preparation and pharmaceutical compositions containing them |
| US5688826A (en) | 1995-11-16 | 1997-11-18 | Eli Lilly And Company | Excitatory amino acid derivatives |
| GB9605429D0 (en) | 1995-11-16 | 1996-05-15 | Lilly Co Eli | Excitatory amino acid receptor antagonists |
| US5952294A (en) | 1996-07-31 | 1999-09-14 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Peptidyl prodrugs and methods of making and using the same |
| ZA983930B (en) | 1997-05-14 | 1999-11-08 | Lilly Co Eli | Excitatory amino acid receptor modulators. |
| ATE236118T1 (de) | 1998-01-28 | 2003-04-15 | Taisho Pharmaceutical Co Ltd | Fluorhaltige aminosäurederivate |
| DK1110943T3 (da) | 1998-08-31 | 2004-10-11 | Taisho Pharmaceutical Co Ltd | 6-fluorbicyclo[3.1.0]hexanderivater |
| US6716452B1 (en) | 2000-08-22 | 2004-04-06 | New River Pharmaceuticals Inc. | Active agent delivery systems and methods for protecting and administering active agents |
| EP1295865A4 (en) | 2000-06-28 | 2005-06-01 | Taisho Pharmaceutical Co Ltd | NEW DICARBOXYLENE DERIVATIVES |
| US7256217B2 (en) | 2001-01-11 | 2007-08-14 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
| US7038077B2 (en) | 2001-01-11 | 2006-05-02 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
| EP1370519A1 (en) * | 2001-02-22 | 2003-12-17 | Eli Lilly And Company | Synthetic excitatory amino acids |
| US7067507B2 (en) | 2001-06-12 | 2006-06-27 | Pharmacia & Upjohn Company | Macrocycles useful in the treatment of Alzheimer's disease |
| WO2003061698A1 (fr) | 2001-12-27 | 2003-07-31 | Taisho Pharmaceutical Co.,Ltd. | Derives de 6-fluorobicyclo[3.1.0]hexane |
| AU2003218063A1 (en) | 2002-04-03 | 2003-10-20 | Eli Lilly And Company | Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist |
| US20050192273A1 (en) | 2002-04-03 | 2005-09-01 | Johnson Bryan G. | Therapy for psychoses combining an atypical antipsychotic and an mglu2/3 receptor agonist |
| NZ556437A (en) * | 2002-06-11 | 2008-11-28 | Lilly Co Eli | Prodrugs of excitatory amino acids |
| CN101362793A (zh) * | 2002-06-11 | 2009-02-11 | 伊莱利利公司 | 兴奋性氨基酸前药 |
| WO2005000790A1 (ja) * | 2003-06-26 | 2005-01-06 | Taisho Pharmaceutical Co., Ltd. | ２－アミノビシクロ[３．１．０]ヘキサン－２，６－ジカルボン酸誘導体 |
| ES2355144T3 (es) * | 2003-06-26 | 2011-03-23 | Taisho Pharmaceutical Co., Ltd. | Derivado de éster 2-aminobiciclo 3.1.0 hexano-2,6-dicarboxílico. |
| CA2773409C (en) * | 2009-11-18 | 2015-06-16 | Suven Life Sciences Limited | Bicyclic compounds as .alpha.4.beta.2 nicotinic acetylcholine receptor ligands |
| JO2978B1 (en) | 2009-12-21 | 2016-03-15 | ايلي ليلي اند كومباني | MGLU2 aids |
-
2012
- 2012-06-07 US US14/123,768 patent/US9296710B2/en active Active
- 2012-06-07 DK DK12729769.5T patent/DK2721012T3/da active
- 2012-06-07 SI SI201230569A patent/SI2721012T1/sl unknown
- 2012-06-07 EA EA201391700A patent/EA023553B1/ru not_active IP Right Cessation
- 2012-06-07 PT PT127297695T patent/PT2721012T/pt unknown
- 2012-06-07 MX MX2013014802A patent/MX2013014802A/es active IP Right Grant
- 2012-06-07 PL PL12729769T patent/PL2721012T3/pl unknown
- 2012-06-07 HU HUE12729769A patent/HUE030171T2/en unknown
- 2012-06-07 JP JP2014515878A patent/JP5945592B2/ja active Active
- 2012-06-07 BR BR112013031928-3A patent/BR112013031928B1/pt active IP Right Grant
- 2012-06-07 CN CN201280029080.2A patent/CN103596933B/zh active Active
- 2012-06-07 EP EP12729769.5A patent/EP2721012B1/en active Active
- 2012-06-07 KR KR1020137033028A patent/KR101598679B1/ko active IP Right Grant
- 2012-06-07 WO PCT/US2012/041229 patent/WO2012173850A1/en active Application Filing
- 2012-06-07 ES ES12729769.5T patent/ES2587204T3/es active Active
- 2012-06-07 CA CA2836485A patent/CA2836485C/en active Active
- 2012-06-07 AU AU2012271024A patent/AU2012271024B2/en active Active
- 2012-06-07 RS RS20160491A patent/RS54888B1/sr unknown
-
2016
- 2016-06-14 HR HRP20160676TT patent/HRP20160676T1/hr unknown
- 2016-06-24 CY CY20161100570T patent/CY1117682T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2012271024A1 (en) | 2013-11-21 |
| PT2721012T (pt) | 2016-07-27 |
| WO2012173850A1 (en) | 2012-12-20 |
| JP5945592B2 (ja) | 2016-07-05 |
| BR112013031928A2 (pt) | 2016-12-13 |
| SI2721012T1 (sl) | 2016-08-31 |
| KR20140009568A (ko) | 2014-01-22 |
| ES2587204T3 (es) | 2016-10-21 |
| CY1117682T1 (el) | 2017-05-17 |
| PL2721012T3 (pl) | 2017-05-31 |
| AU2012271024B2 (en) | 2015-07-09 |
| EP2721012A1 (en) | 2014-04-23 |
| EA023553B1 (ru) | 2016-06-30 |
| CN103596933A (zh) | 2014-02-19 |
| MX2013014802A (es) | 2014-01-24 |
| KR101598679B1 (ko) | 2016-02-29 |
| JP2014517035A (ja) | 2014-07-17 |
| CA2836485C (en) | 2016-12-13 |
| EP2721012B1 (en) | 2016-05-25 |
| HUE030171T2 (en) | 2017-05-29 |
| CN103596933B (zh) | 2016-03-23 |
| BR112013031928B1 (pt) | 2022-05-24 |
| CA2836485A1 (en) | 2012-12-20 |
| US20140113944A1 (en) | 2014-04-24 |
| EA201391700A1 (ru) | 2014-04-30 |
| HRP20160676T1 (hr) | 2016-07-15 |
| RS54888B1 (sr) | 2016-10-31 |
| US9296710B2 (en) | 2016-03-29 |
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