HRP20131052T1 - Agonisti mglu2 - Google Patents
Agonisti mglu2 Download PDFInfo
- Publication number
- HRP20131052T1 HRP20131052T1 HRP20131052AT HRP20131052T HRP20131052T1 HR P20131052 T1 HRP20131052 T1 HR P20131052T1 HR P20131052A T HRP20131052A T HR P20131052AT HR P20131052 T HRP20131052 T HR P20131052T HR P20131052 T1 HRP20131052 T1 HR P20131052T1
- Authority
- HR
- Croatia
- Prior art keywords
- amino
- bicyclo
- hexane
- triazol
- ylsulfanyl
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- -1 (2S)-2-amino-4-methylsulfanylbutanoyl Chemical group 0.000 claims 5
- 208000020016 psychiatric disease Diseases 0.000 claims 5
- BBGHHIUQOKQCBW-LDZWZCGGSA-N (1r,2s,4r,5r,6r)-2-[[(2s)-2-aminopropanoyl]amino]-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(NC(=O)[C@@H](N)C)C(O)=O)C=1N=CNN=1 BBGHHIUQOKQCBW-LDZWZCGGSA-N 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- 125000003440 L-leucyl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])C(C([H])([H])[H])([H])C([H])([H])[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- YSOWRGMLMZQSBX-AVUIYAGVSA-N (1r,2s,4r,5r,6r)-2-amino-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(N)C(O)=O)C1=NN=CN1 YSOWRGMLMZQSBX-AVUIYAGVSA-N 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000011688 Generalised anxiety disease Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- MWECKFISVWUYDM-UHFFFAOYSA-N bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Chemical compound C1CC(C(O)=O)C2C(C(=O)O)C21 MWECKFISVWUYDM-UHFFFAOYSA-N 0.000 claims 2
- KAMXAYSXFKTSBQ-LJTNYMJHSA-N dibenzyl (1r,2s,4r,5r,6r)-2-amino-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylate Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(=O)OCC=1C=CC=CC=1)(N)C(=O)OCC=1C=CC=CC=1)C1=NN=CN1 KAMXAYSXFKTSBQ-LJTNYMJHSA-N 0.000 claims 2
- 208000029364 generalized anxiety disease Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- VNLNXJOMGNCSSS-BTRGJMEFSA-N (1r,2s,4r,5r,6r)-2-[(2-aminoacetyl)amino]-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(NC(=O)CN)C(O)=O)C1=NN=CN1 VNLNXJOMGNCSSS-BTRGJMEFSA-N 0.000 claims 1
- YCQVGZVFFKDBHR-SQARDTNNSA-N (1r,2s,4r,5r,6r)-2-[[(2s)-2-amino-4-methylsulfanylbutanoyl]amino]-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(NC(=O)[C@@H](N)CCSC)C(O)=O)C1=NN=CN1 YCQVGZVFFKDBHR-SQARDTNNSA-N 0.000 claims 1
- SGEXVXMPLDCNCK-OUXKRIEPSA-N (1r,2s,4r,5r,6r)-2-[[(2s)-2-amino-4-methylsulfanylbutanoyl]amino]-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid;hydrochloride Chemical compound Cl.S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(NC(=O)[C@@H](N)CCSC)C(O)=O)C1=NN=CN1 SGEXVXMPLDCNCK-OUXKRIEPSA-N 0.000 claims 1
- FICWTZOQUXUYOK-AHKKVLALSA-N (1r,2s,4r,5r,6r)-2-[[(2s)-2-aminopropanoyl]amino]-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid;azane;hydrate Chemical compound N.O.S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(O)=O)(NC(=O)[C@@H](N)C)C(O)=O)C1=NC=NN1 FICWTZOQUXUYOK-AHKKVLALSA-N 0.000 claims 1
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 claims 1
- 125000003412 L-alanyl group Chemical group [H]N([H])[C@@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 1
- HMEOJPJONKZGEK-LJTNYMJHSA-N bis[(2-fluorophenyl)methyl] (1r,2s,4r,5r,6r)-2-amino-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylate Chemical compound S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(=O)OCC=1C(=CC=CC=1)F)(N)C(=O)OCC=1C(=CC=CC=1)F)C1=NN=CN1 HMEOJPJONKZGEK-LJTNYMJHSA-N 0.000 claims 1
- WBPOLGAZOBOJFC-HZABEZJUSA-N bis[(2-fluorophenyl)methyl] (1r,2s,4r,5r,6r)-2-amino-4-(1h-1,2,4-triazol-5-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylate;hydrochloride Chemical compound Cl.S([C@@H]1C[C@@]([C@@H]2[C@H]([C@@H]21)C(=O)OCC=1C(=CC=CC=1)F)(N)C(=O)OCC=1C(=CC=CC=1)F)C1=NN=CN1 WBPOLGAZOBOJFC-HZABEZJUSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
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
- C07D249/12—Oxygen or sulfur atoms
-
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)
Claims (25)
1. Spoj formule
[image]
,
naznačen time što
R1 je vodik, R2 je vodik i R3 je vodik;
R1 je vodik, R2 je (2S)-2-aminopropanoil, a R3 je vodik;
R1 je vodik, R2 je (2S)-2-amino-4-metilsulfanilbutanoil, a R3 je vodik;
R1 je vodik, R2 je (2S)-2-amino-4-metilpentanoil, a R3 je vodik;
R1 je vodik, R2 je 2-aminoacetil, a R3 je vodik;
R1 je benzil, R2 je vodik, a R3 je benzil; ili
R1 je (2-fluorfenil)metil, R2 je vodik, a R3 je (2-fluorfenil)metil;
ili njegova farmaceutski prihvatljiva sol ili solvat soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što je (1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1R,2S,4R,5R,6R)-2-[[(2S)-2-aminopropanoil]amino]-4-(1H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je hidroklorid (1R,2S,4R,5R,6R)-2-[[(2S)-2-aminopropanoil]amino]-4-(1H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-4-metilsulfanilbutanoil]amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što je (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-4-metilsulfanilbutanoil]amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline hidroklorid.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-4-metil-pentanoil]amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što je (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-4-metil-pentanoil]amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline hidroklorid.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1R,2S,4R,5R,6R)-2-[(2-aminoacetil)amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
11. Spoj u skladu s patentnim zahtjevom 10, naznačen time što je hidroklorid (1R,2S,4R,5R,6R)-2-[(2-aminoacetil)amino]-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je dibenzil-(1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilat, ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 12, naznačen time što je dibenzil-(1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilat.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je bis[(2-fluorfenil)metil]-(1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilat, ili njegova farmaceutski prihvatljiva sol.
15. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je bis[(2-fluorfenil)metil]-(1R,2S,4R,5R,6R)-2-amino-4-(4H-1,2,4-triazol-3-ilsulfanil)biciklo[3.1.0]heksan-2,6-dikarboksilat-hidroklorid.
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je monohidrat monoamonijeve soli (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-1-oksopropil]amino]-4-(4H-1,2,4-triazol-3-iltio)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline.
17. Spoj u skladu s patentnim zahtjevom 1, koji je monohidrat monoamonijeve soli (1R,2S,4R,5R,6R)-2-[[(2S)-2-amino-1-oksopropil]amino]-4-(4H-1,2,4-triazol-3-iltio)biciklo[3.1.0]heksan-2,6-dikarboksilne kiseline u kristalnom obliku, naznačen time što uzorak difrakcije rendgenskih zraka na prahu ima signale na 2θ ± 0,2 koji iznose 18,61 i 21,07.
18. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-17 i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
19. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-17, naznačen time što je namijenjen upotrebi u terapiji.
20. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-17, naznačen time što je namijenjen upotrebi u liječenju psihijatrijskog poremećaja, kojeg se bira iz skupine koju čine bipolarni poremećaj, shizofrenija, depresija i generalizirani anksiozni poremećaj.
21. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 20, naznačeni time što je psihijatrijski poremećaj bipolarni poremećaj.
22. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 20, naznačeni time što je psihijatrijski poremećaj shizofrenija.
23. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 20, naznačeni time što je psihijatrijski poremećaj depresija.
24. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 20, naznačeni time što je psihijatrijski poremećaj generalizirani anksiozni poremećaj.
25. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-17, uz farmaceutski prihvatljivu podlogu i izborno druge terapijske sastojke.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382290 | 2009-12-21 | ||
| US30523910P | 2010-02-17 | 2010-02-17 | |
| PCT/US2010/060371 WO2011084437A1 (en) | 2009-12-21 | 2010-12-15 | Mglu2 agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20131052T1 true HRP20131052T1 (hr) | 2013-12-06 |
Family
ID=42026702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20131052AT HRP20131052T1 (hr) | 2009-12-21 | 2013-11-06 | Agonisti mglu2 |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US8318184B2 (hr) |
| EP (1) | EP2516406B1 (hr) |
| JP (1) | JP5779190B2 (hr) |
| KR (1) | KR101395356B1 (hr) |
| CN (1) | CN102695701B (hr) |
| AR (1) | AR079343A1 (hr) |
| AU (1) | AU2010340039B2 (hr) |
| BR (1) | BR112012017188B1 (hr) |
| CA (1) | CA2784667C (hr) |
| CR (1) | CR20120322A (hr) |
| CY (1) | CY1114880T1 (hr) |
| DK (1) | DK2516406T3 (hr) |
| DO (1) | DOP2012000173A (hr) |
| EA (1) | EA020229B1 (hr) |
| EC (1) | ECSP12011989A (hr) |
| ES (1) | ES2435651T3 (hr) |
| HK (1) | HK1171228A1 (hr) |
| HN (1) | HN2012001160A (hr) |
| HR (1) | HRP20131052T1 (hr) |
| IL (1) | IL220011A (hr) |
| JO (1) | JO2978B1 (hr) |
| MA (1) | MA33824B1 (hr) |
| MX (1) | MX2012007332A (hr) |
| MY (1) | MY160618A (hr) |
| NZ (1) | NZ600305A (hr) |
| PE (1) | PE20121688A1 (hr) |
| PL (1) | PL2516406T3 (hr) |
| PT (1) | PT2516406E (hr) |
| RS (1) | RS53063B (hr) |
| SG (1) | SG181836A1 (hr) |
| SI (1) | SI2516406T1 (hr) |
| TN (1) | TN2012000281A1 (hr) |
| TW (1) | TWI477490B (hr) |
| UA (1) | UA107684C2 (hr) |
| WO (1) | WO2011084437A1 (hr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8722660B2 (en) | 2010-02-17 | 2014-05-13 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| WO2012068041A1 (en) * | 2010-11-18 | 2012-05-24 | Eli Lilly And Company | 4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS |
| TWI520935B (zh) * | 2010-11-18 | 2016-02-11 | 美國禮來大藥廠 | 作為ｍＧｌｕＲ２／３拮抗劑之４－經取代－３－苯基磺醯基甲基－雙環［３.１.０］己烷化合物 |
| SI2721012T1 (sl) | 2011-06-17 | 2016-08-31 | Eli Lilly And Company | Derivati biciklo(3.1.0)heksan-2,6-dikarboksilne kisline kot agonisti mglu2 receptorja |
| AR089718A1 (es) | 2012-02-01 | 2014-09-10 | Lilly Co Eli | AGONISTAS DE mGlu2/3 |
| EP3610890A1 (en) | 2012-11-14 | 2020-02-19 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| ES2748633T3 (es) | 2014-01-21 | 2020-03-17 | Janssen Pharmaceutica Nv | Combinaciones que comprenden moduladores alostéricos positivos del receptor glutamatérgico metabotrópico de subtipo 2 y su uso |
| UA128346C2 (uk) | 2014-01-21 | 2024-06-19 | Янссен Фармацевтика Нв | Комбінації, які містять позитивні алостеричні модулятори або ортостеричні агоністи метаботропного глутаматергічного рецептора 2 підтипу, та їх застосування |
| PL3277270T3 (pl) | 2015-04-01 | 2022-02-14 | Akebia Therapeutics, Inc. | Kompozycje i sposoby leczenia niedokrwistości |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5576323A (en) * | 1993-12-03 | 1996-11-19 | Eli Lilly And Company | Excitatory amino acid receptor antagonists |
| 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 |
| ZA983930B (en) | 1997-05-14 | 1999-11-08 | Lilly Co Eli | Excitatory amino acid receptor modulators. |
| CN1267407C (zh) * | 2001-01-11 | 2006-08-02 | 伊莱利利公司 | 兴奋性氨基酸前体药物 |
| EP1351925A1 (en) * | 2001-01-11 | 2003-10-15 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
| WO2002068380A1 (en) * | 2001-02-22 | 2002-09-06 | Eli Lilly And Company | Synthetic excitatory amino acids |
| PT1517915E (pt) * | 2002-06-11 | 2009-04-09 | Lilly Co Eli | Pró-drogas de amino ácidos de excitação |
| 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 |
| WO2012068041A1 (en) * | 2010-11-18 | 2012-05-24 | Eli Lilly And Company | 4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS |
| TWI520935B (zh) * | 2010-11-18 | 2016-02-11 | 美國禮來大藥廠 | 作為ｍＧｌｕＲ２／３拮抗劑之４－經取代－３－苯基磺醯基甲基－雙環［３.１.０］己烷化合物 |
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