ME02427B - Derivati 1-heterociklil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona i njihovo korišćenje kao pde9a modulatori - Google Patents
Derivati 1-heterociklil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona i njihovo korišćenje kao pde9a modulatoriInfo
- Publication number
- ME02427B ME02427B MEP-2016-75A MEP7516A ME02427B ME 02427 B ME02427 B ME 02427B ME P7516 A MEP7516 A ME P7516A ME 02427 B ME02427 B ME 02427B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- group
- compound according
- pharmaceutically acceptable
- acceptable salts
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims 26
- -1 4-pyridyl- Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 206010012289 Dementia Diseases 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 239000011737 fluorine Substances 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 5
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 5
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 5
- 229910052794 bromium Inorganic materials 0.000 claims 5
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 239000000460 chlorine Substances 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 208000028698 Cognitive impairment Diseases 0.000 claims 3
- 208000006011 Stroke Diseases 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 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 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004810 Vascular dementia Diseases 0.000 claims 1
- 201000008485 Wernicke-Korsakoff syndrome Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000001652 frontal lobe Anatomy 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000028252 learning or memory Effects 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 208000021090 palsy Diseases 0.000 claims 1
- 230000008447 perception Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000000542 thalamic effect Effects 0.000 claims 1
- 208000018726 traumatic encephalopathy Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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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
-
- 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
- A61P25/28—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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
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- Psychiatry (AREA)
- Cardiology (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pulmonology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (19)
1. Jedinjenje prema opštoj formuli IgdjeHc je odabran između grupe od tetrahidropiranila, tetrahidrofuranila, piperidinila, pirolidinila;R1 je odabran između grupe od fenila, 2-, 3- i 4-piridil-, ciklopropil, ciklobutil, ciklopentil, cikloheksil, etil, 1- i 2-propil, 1- i 2-butil-, 1-, 2- i 3-pentil-, tetrahidrofuranil i tetrahidropiranil,pri čemu ove grupe mogu opciono biti supstituisane sa jednim ili više supstituenata nezavisno jedan od drugoga odabrani iz grupe koja se sastoji od fluora, hlora, broma, joda, okso, NC-, C1-6-alkil-O-, C1-6-alkil-, CF3O-, i CF3-;R2 nezavisno od bilo kog drugog R2 je odabran iz grupe od H- i C1-6-alkil-,i u slučaju da je R2 vezan za azot koji je član prstena Hc, ovaj R2 će biti nezavisan od bilo kog drugog R2: H-, C1-6-alkil-CO-, C1-6-alkil-O-CO-, C1-6-alkil-, fenil-CO-, fenil-O-CO-, (C1-6-alkil)2N-CO-, gdje prethodno navedeni članovi mogu opciono biti supstituisani nezavisno jedan od drugoga sa jednim ili više supstituenata fluora;R3 je odabran iz grupe od H-, hidroksi i C1-6-alkil-O-, pri čemu C1-6-alkil-O- može opciono biti supstituisan sa jednim ili više fluora, hlora, broma i HO-;R4 i R5 nezavisno jedan od drugoga je odabran iz grupe od H-, fluora, i metila;x je 0, 1, 2, 3 ili 4; y je 0, ili 1;i njegove farmaceutski prihvatljive soli.
2. Jedinjenje prema zahtjevu 1, gdje Hc je odabran iz grupe od 3- ili 4-piperidinila i 3- pirolidinila; R1 je odabran iz grupe od fenil, 2-, 3- i 4-piridil-, ciklopropil, ciklobutil, ciklopentil, cikloheksil, etil, 1- i 2-propil, 1- i 2-butil-, 1-, 2- i 3-pentil-, tetrahidrofuranil i tetrahidropiranil, pri čemu ove grupe mogu opciono biti supstituisane sa jednim ili više supstituenata nezavisno odabrani između grupe koja se sastoji od fluora, hlora, broma, joda, okso, NC-, C1-6-alkil-O-, C1-6-alkil-, CF3O-, i CF3-; R2 nezavisno od bilo kog drugog R2 je odabran iz grupe od H- i C1-6-alkil-, i u slučaju R2 je vazan za azot koji je član prstena Hc, ovaj R2 će biti nezavisan od bilo kog drugog R2: H-, C1-6-alkil-CO-, C1-6-alkil-O-CO-, C1-6-alkil-, fenil-CO-, fenil-O-CO-, (C1-6-alkil)2N-CO-, gdje prethodno navedeni članovi mogu opciono biti supstituisani nezavisno jedan od drugoga sa jednim ili više supstituenata fluora; R3 je odabran iz grupe od H-, hidroksi i C1-6-alkil-O-, pri čemu C1-6-alkil-O- može opciono biti supstituisan sa jednim ili više fluora, hlora, broma i HO-; R4 i R5 nezavisno jedan od drugog je odabran iz grupe od H-, fluora, i metila; x je 0, 1, 2, 3 ili 4; y je 0, ili 1; i njegove farmaceutski prihvatljive soli.
3. Jedinjenje prema zahtjevu 1, gdje Hc je odabran iz grupe od 3- ili 4-tetrahidropiranila i 3-tetrahidrofuranila, R1 je odabran iz grupe od fenil, 2-, 3- i 4-piridil-, ciklopropil, ciklobutil, ciklopentil, cikloheksil, etil, 1- i 2-propil, 1- i 2-butil-, 1-, 2- i 3-pentil-, tetrahidrofuranil i tetrahidropiranil, pri čemu ove grupe mogu opciono biti supstituisane sa jednim ili više supstituenata nezavisno odabrani između grupe koja se sastoji od fluora, hlora, broma, joda, okso, NC-, C1-6-alkil-O-, C1-6-alkil-, CF3O-, i CF3-; R2 nezavisno od bilo kog drugog R2 je odabran iz grupe od H- i C1-6-alkil-, gdje prethodno navedena(e) C1-6-alkil-grupa(e) mogu opciono biti supstituisane nezavisno jedna od druge sa jednim ili više fluoro supstituenata; R3 je odabran iz grupe od H-, hidroksi i C1-6-alkil-O-, pri čemu C1-6-alkil-O- može opciono biti supstituisan sa jednim ili više fluora, hlora, broma i HO-; R4 i R5 nezavisno jedan od drugog je odabran iz grupe od H-, fluora, i metila; x je 0, 1, 2, 3 ili 4; y je 0, ili 1; i njegove farmaceutski prihvatljive soli.
4. Jedinjenje prema zahtjevu 1 odabran između grupe koja se sastoji od i i svaki njegovi stereoizomeri ili tautomeri ili solvati ili svake njegove farmaceutski prihvatljive soli.
5. Jedinjenje prema bilo kom od zahtjeva 1, 3 i 4, gdje jedinjenje je ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
6. Jedinjenje prema bilo kom od zahtjeva 1, 3 i 4, gdje jedinjenje je ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
7. Jedinjenje prema bilo kom od zahtjeva 1, 3 i 4, gdje jedinjenje je ili njegovi stereoizomeri ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
8. Jedinjenje prema bilo kom od zahtjeva 1, 2 i 4, gdje jedinjenje je ili njegovi stereoizomeri ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
9. Jedinjenje prema bilo kom od zahtjeva 1, 2 i 4, gdje jedinjenje je ili njegovi stereoizomeri ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
10. Jedinjenje prema bilo kom od zahtjeva 1, 3 i 4, gdje jedinjenje je ili njegovi stereoizomeri ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
11. Jedinjenje prema bilo kom od zahtjeva 1, 2 i 4, gdje jedinjenje je ili njegovi tautomeri ili njegovi solvati ili njegove farmaceutski prihvatljive soli.
12. Jedinjenje prema bilo kom od zahtjeva 1 do 11 za korišćenje kao medikament.
13. Jedinjenje prema bilo kom od zahtjeva 1 do 11 za korišćenje u liječenju oboljenja koje je povezano sa inhibicijom PDE9.
14. Jedinjenje prema bilo kom od zahtjeva 1 do 11 za korišćenje u liječenju, poboljšanju ili prevenciji kognitivnog oštečenja koje je povezano sa percepcijom, koncentracijom, spoznajom, učenjem ili pamćenjem.
15. Jedinjenje prema zahtjevu 14, za korišćenje u liječenju, poboljšanju ili prevenciji kognitivnog oštečenja koje je povezano sa oštečenjima u učenju i pamćenju, a koje je povezano sa godinama, gubitkom pamćenja, a koje je povezano sa godinama, vaskularne demencije, kraniocerebralne traume, moždanog udara, demencije koja se dešava posle moždanog udara (post moždana demencija), post-traumatične demencije, opšteg gubitka koncentracije, gubitka koncentracije kod dece usled učenja i problema sa pamćenjem, Alzheimerove bolesti, Lewy telesne demencije, demecije sa degeneracijom frontalnog režnja, uključujući Pickov sindrom, Parkinsonove bolesti, progresivne nuklearne paralize, demencije sa kortikobasalnom degeneracijom, amiotropske lateralne skleroze (ALS), Huntingtonove bolesti, multipla sklerozom, talamitske degeneracije, Creutzfeld-Jacob demencije, HIV demencije, šizofrenije sa demencijom ili Korsakoffa psihoze.
16. Jedinjenje prema bilo kom od zahtjeva 14 ili 15 za korišćenje u liječenju Alzheimerove bolesti.
17. Jedinjenje prema bilo kom od zahtjeva 14 ili 15 za korišćenje u liječenju kognitivnog oštečenja koje je povezano sa Alzheimerovom bolešću.
18. Farmaceutska kompozicija koja sadrži jedinjenje prema bilo kom od zahtjeva 1 do 11 i farmaceutski nosač.
19. Kombinacija jedinjenja prema bilo kom od zahtjeva 1 do 11 sa drugim aktivnim agensom za korišćenje u liječenju Alzheimerove bolesti.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08153987 | 2008-04-02 | ||
| EP09727328.8A EP2300478B1 (en) | 2008-04-02 | 2009-04-01 | 1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators |
| PCT/EP2009/053907 WO2009121919A1 (en) | 2008-04-02 | 2009-04-01 | 1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02427B true ME02427B (me) | 2016-09-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-75A ME02427B (me) | 2008-04-02 | 2009-04-01 | Derivati 1-heterociklil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona i njihovo korišćenje kao pde9a modulatori |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8623879B2 (me) |
| EP (1) | EP2300478B1 (me) |
| JP (1) | JP5391264B2 (me) |
| KR (1) | KR101623762B1 (me) |
| CN (1) | CN101983199B (me) |
| AR (1) | AR071577A1 (me) |
| AU (1) | AU2009232017B2 (me) |
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