HRP20210793T1 - Derivati kromana, izokromana i dihidroizobenzofurana kao mglur2-negativni alosterni modulatori, pripravci i njihova uporaba - Google Patents
Derivati kromana, izokromana i dihidroizobenzofurana kao mglur2-negativni alosterni modulatori, pripravci i njihova uporaba Download PDFInfo
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- HRP20210793T1 HRP20210793T1 HRP20210793TT HRP20210793T HRP20210793T1 HR P20210793 T1 HRP20210793 T1 HR P20210793T1 HR P20210793T T HRP20210793T T HR P20210793TT HR P20210793 T HRP20210793 T HR P20210793T HR P20210793 T1 HRP20210793 T1 HR P20210793T1
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- VZWXIQHBIQLMPN-UHFFFAOYSA-N chromane Chemical compound C1=CC=C2CCCOC2=C1 VZWXIQHBIQLMPN-UHFFFAOYSA-N 0.000 title 1
- HEBMCVBCEDMUOF-UHFFFAOYSA-N isochromane Chemical compound C1=CC=C2COCCC2=C1 HEBMCVBCEDMUOF-UHFFFAOYSA-N 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 229940126662 negative allosteric modulator Drugs 0.000 title 1
- SFLGSKRGOWRGBR-UHFFFAOYSA-N phthalane Chemical class C1=CC=C2COCC2=C1 SFLGSKRGOWRGBR-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 57
- 150000003839 salts Chemical class 0.000 claims 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 229960003530 donepezil Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/18—Bridged systems
-
- 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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
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- 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
- A61K31/02—Halogenated hydrocarbons
- A61K31/025—Halogenated hydrocarbons carbocyclic
- A61K31/03—Halogenated hydrocarbons carbocyclic aromatic
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/20—Hypnotics; Sedatives
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- 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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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/22—Bridged ring systems
- C07D221/24—Camphidines
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
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- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Claims (33)
1. Spoj formule (I):
[image]
ili njegov stereoizomer, ili farmaceutski prihvatljiva sol navedenog spoja ili navedenog stereoizomera, naznačen time što:
prsten A je ostatak izabran od:
[image]
i
[image]
u kojima:
R2 je izabran od H, ciklopropil, -(C1-C4)alkil, -(C1-C4)alkil-OH, -(C1-C4)alkil-OCH3, -(C1-C4)haloalkil, -(C1-C4)alkil-O-(C1-C4)haloalkil, -CH(CH3)2, -CH2-O-(C1-C4)haloalkil, -CH(CH3)-O-(C1-C4)haloalkil, -CH2-NH-(C1-C4)haloalkil i -CH2-N(CH3)-(C1-C4)haloalkil,
R2A je izabran od H i metil;
R3 je izabran od H i metil;
R3A je izabran od H i metil;
prsten B je ostatak izabran iz grupe koja se sastoji od fenil, heteroaril, -(C5-C6) cikloalkil, i -(C5-C6) cikloalkenil;
n je 0, 1, 2 ili 3, pod uvjetom da vrijednost n ne prelazi maksimalan broj atoma vodika na prstenu B koji se mogu supstituirati; i
svaki R1 (kada je prisutan) je neovisno izabran iz grupe koja se sastoji od halogen, -CN, -OH, -(C1-C6) alkil,-O-(C1-C6) alkil, -(C1-C6) haloalkil, -O-(C1-C6) haloalkil, ciklopropil, ciklobutil, -NH2, -NH(C1-C6)alkil, -N(C1-C6alkil)2, -C(O)O(C1-C6) alkil, i fenil.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što prsten A je ostatak:
[image]
i formula (I) ima oblik formule (IA):
[image]
3. Spoj prema patentnom zahtjevu 2, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R2 izabran od H, ciklopropil, -CH3, -CH(CH3)2, -CH2-OH, -CH2-OCH3, -CH2F, - CHF2, -CF3, -CH2CH2F, -CH2CHF2, -CH2CF3, -CH2-O-CH2F, -CH2-O-CHF2, -CH(CH3)-O-CH2F, -CH(CH3)-O-CHF2, -CH2-NH-CH2CF3 i -CH2-N(CH3)-CH2CF3;
R2A je izabran od H i metil;
R3 je izabran od H i metil; i
R3A je izabran od H i metil.
4. Spoj prema patentnom zahtjevu 2, ili njegova farmaceutski prihvatljiva sol, naznačen time što R2 i R2A su oba metil; i
R3 i R3A su oba H.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što prsten A je ostatak:
[image]
i formula (I) ima oblik formule (IB):
[image]
6. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što prsten A je ostatak:
[image]
i formula (I) ima oblik formule (IC):
[image]
7. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što prsten A je ostatak:
[image]
i formula (I) ima oblik formule (ID):
[image]
8. Spoj prema bilo kojem od patentnih zahtjeva 1-7, ili njegova farmaceutski prihvatljiva sol, naznačen time što:
prsten B je ostatak izabran iz grupe koja se sastoji od fenil, ciklopentil, cikloheksil, piridinil, pirimidinil, pirazolil, tienil, tiazolil, tiadiazolil, izoksazolil, oksadiazolil i oksazolil;
n je 0, 1, 2, ili 3, pod uvjetom da vrijednost n ne prelazi maksimalan broj atoma vodika na prstenu B koji se mogu supstituirati; i
svaki R1 (kada je prisutan) je neovisno izabran iz grupe koja se sastoji od halogen, -CN, -OH, -(C1-C6) alkil,-O-(C1-C6) alkil, -(C1-C6) haloalkil, -O-(C1-C6) haloalkil, ciklopropil, ciklobutil, -NH2, -NH(C1-C6)alkil, -N(C1-C6alkil)2, -C(O)O(C1-C6) alkil i fenil.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-7, ili njegova farmaceutski prihvatljiva sol, naznačen time što:
prsten B je ostatak izabran iz grupe koja se sastoji od: fenil, pirazolil, piridinil, tienil, izoksazolil, oksadiazolil i oksazolil;
n je 0, 1, ili 2; i
svaki R1 (kada je prisutan) je neovisno izabran iz grupe koja se sastoji od fluoro, kloro, -CH3 i -CHCF2.
10. Spoj prema patentnom zahtjevu 1, koji ima formulu (IA-1):
[image]
ili njegov steroizomer ili farmaceutski prihvatljiva sol navedenog spoja ili navedenog stereoizomera, naznačen time što:
R2 je izabran od H, ciklopropil, -CH3, -CH(CH3)2, -CH2-OH, -CH2-OCH3, -CH2F, - CHF2, -CF3, -CH2CH2F, -CH2CHF2, -CH2CF3, -CH2-O-CH2F, -CH2-O-CHF2, -CH(CH3)-O-CH2F, -CH(CH3)-O-CHF2, -CH2-NH-CH2CF3 i -CH2-N(CH3)-CH2CF3;
R2A je izabran od H i CH3;
R3 je izabran od H i CH3; i
R3A je izabran od H i CH3.
11. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu je navedeni spoj izabran iz grupe koja se sastoji od:
[image]
[image]
[image]
[image]
[image]
[image]
12. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
13. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
14. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
15. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
16. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
17. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
18. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
19. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
20. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
21. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
22. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
23. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
24. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
25. Spoj prema patentnom zahtjevu 1, naznačen time što navedeni spoj ima strukturu:
[image]
pri čemu je navedeni spoj u obliku farmaceutski prihvatljive soli.
26. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv nosač.
27. Kombinacija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegovu farmaceutski prihvatljivu sol ili solvat i jedan, dva, tri ili više drugih terapeutskih sredstava.
28. Spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22 ili 24, ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju Alzheimerove bolesti, blagog kognitivnog oštećenja, shizofrenije, poremećaja raspoloženja ili poremećaja spavanja.
29. Spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegova farmaceutski prihvatljiva sol za uporabu u terapiji.
30. Spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju neurodegenerativnih bolesti ili poremećaja koji pogađaju kogniciju.
31. Spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju Alzheimerove bolesti.
32. Spoj prema bilo kom od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju depresije.
33. Kombinacija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1-12, 14, 16, 18, 20, 22, ili 24, ili njegovu farmaceutski prihvatljivu sol ili solvat i donepezil.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662400150P | 2016-09-27 | 2016-09-27 | |
| EP17781253.4A EP3519416B1 (en) | 2016-09-27 | 2017-09-25 | Chromane, isochromane and dihydroisobenzofuran derivatives as mglur2-negative allosteric modulators, compositions, and their use |
| PCT/US2017/053155 WO2018063955A1 (en) | 2016-09-27 | 2017-09-25 | CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20210793T1 true HRP20210793T1 (hr) | 2021-09-03 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20210793TT HRP20210793T1 (hr) | 2016-09-27 | 2021-05-17 | Derivati kromana, izokromana i dihidroizobenzofurana kao mglur2-negativni alosterni modulatori, pripravci i njihova uporaba |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US10335399B2 (hr) |
| EP (1) | EP3519416B1 (hr) |
| JP (3) | JP6681517B2 (hr) |
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Families Citing this family (6)
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| MA46342B1 (fr) * | 2016-09-27 | 2021-05-31 | Merck Sharp & Dohme | Dérivés de chromane, d'isochromane et de dihydroisobenzofurane en tant que modulateurs allostériques négatifs de mglur2, compositions et leur utilisation |
| AU2019208331B2 (en) | 2018-01-19 | 2024-05-02 | Cytokinetics, Inc. | Dihydrobenzofuran and inden analogs as cardiac sarcomere inhibitors |
| JP7438148B2 (ja) | 2018-06-26 | 2024-02-26 | サイトキネティックス， インコーポレイテッド | 心臓サルコメア阻害剤 |
| BR112021017276A2 (pt) * | 2019-03-01 | 2021-11-09 | Kbp Biosciences Co Ltd | Método para preparar composto tricíclico e intermediário do mesmo |
| BR112023017461A2 (pt) | 2021-03-04 | 2023-09-26 | Cytokinetics Inc | Compostos, composição farmacêutica, métodos de tratamento de doença cardíaca, de uma doença ou afecção associada à cardiomiopatia hipertrófica, de uma doença ou afecção que está associada ao espessamento secundário da parede do ventrículo esquerdo, de uma doença ou afecção associada à pequena cavidade ventricular esquerda e obliteração da cavidade, contração hiperdinâmica do ventrículo esquerdo, isquemia miocárdica ou fibrose cardíaca, de uma doença ou afecção selecionada a partir de distrofias musculares e doenças de armazenamento de glicogênio, e, método de inibição do sarcômero cardíaco |
| WO2023278729A1 (en) * | 2021-06-30 | 2023-01-05 | The General Hospital Corporation | Chromane imaging ligands |
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| US5552437A (en) | 1994-10-27 | 1996-09-03 | Merck Frosst Canada, Inc. | Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis |
| US5576338A (en) | 1995-02-15 | 1996-11-19 | Merck Frosst Canada, Inc. | Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis |
| WO2005014543A1 (ja) | 2003-08-06 | 2005-02-17 | Japan Tobacco Inc. | 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用 |
| EP1934205A4 (en) | 2005-10-05 | 2010-06-02 | Merck Frosst Canada Ltd | SUBSTITUTED QUINOLINES AS INHIBITORS OF LEUCOTRIENE BIOSYNTHESIS |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| US20120040974A1 (en) | 2008-08-18 | 2012-02-16 | Yale University | Mif modulators |
| MX2011011964A (es) * | 2009-05-12 | 2012-02-23 | Janssen Pharmaceuticals Inc | Derivados de 1,2,3-triazolo[4,3-a]piridina y su uso para el tratamiento o prevencion de trastornos neurologicos y psiquiatricos. |
| US8772301B2 (en) | 2009-12-18 | 2014-07-08 | Sunovion Pharmaceuticals, Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| WO2013066736A1 (en) * | 2011-11-03 | 2013-05-10 | Merck Sharp & Dohme Corp. | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| WO2016029454A1 (en) | 2014-08-29 | 2016-03-03 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| US9382208B1 (en) | 2015-01-26 | 2016-07-05 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 2 |
| WO2016149324A1 (en) | 2015-03-16 | 2016-09-22 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 2 |
| JP6471614B2 (ja) | 2015-05-29 | 2019-02-20 | 株式会社リコー | 通信端末、通信システム、通信制御方法、及びプログラム |
| JP2018154554A (ja) | 2015-07-29 | 2018-10-04 | 大日本住友製薬株式会社 | 新規リンカー部位を持つ縮合ピラゾール誘導体およびその医薬用途 |
| MA46342B1 (fr) * | 2016-09-27 | 2021-05-31 | Merck Sharp & Dohme | Dérivés de chromane, d'isochromane et de dihydroisobenzofurane en tant que modulateurs allostériques négatifs de mglur2, compositions et leur utilisation |
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2019
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2020
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2021
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