HRP20171415T4 - Heterociklični spojevi za liječenje neuroloških i psiholoških poremećaja - Google Patents
Heterociklični spojevi za liječenje neuroloških i psiholoških poremećaja Download PDFInfo
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- HRP20171415T4 HRP20171415T4 HRP20171415TT HRP20171415T HRP20171415T4 HR P20171415 T4 HRP20171415 T4 HR P20171415T4 HR P20171415T T HRP20171415T T HR P20171415TT HR P20171415 T HRP20171415 T HR P20171415T HR P20171415 T4 HRP20171415 T4 HR P20171415T4
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- 208000012902 Nervous system disease Diseases 0.000 title claims 2
- 230000000926 neurological effect Effects 0.000 title claims 2
- 208000020016 psychiatric disease Diseases 0.000 title claims 2
- 208000025966 Neurological disease Diseases 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 7
- 125000001931 aliphatic group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 238000013268 sustained release Methods 0.000 claims 2
- 239000012730 sustained-release form Substances 0.000 claims 2
- 125000006686 (C1-C24) alkyl group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 1
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000004688 alkyl sulfonyl alkyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000005110 aryl thio group Chemical group 0.000 claims 1
- 125000005164 aryl thioalkyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- -1 arylsulfonylalkyl Chemical group 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 1
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- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A61P25/20—Hypnotics; Sedatives
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- 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
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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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
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- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
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- C07D401/14—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 three or more hetero rings
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- C07D413/10—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 linked by a carbon chain containing aromatic rings
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
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Claims (18)
1. Spoj predstavljen formulom V:
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ili njegovi geometrijski izomeri, enantiomeri, diastereomeri, racemati, farmaceutski prihvatljive soli i solvati navedenog,
gdje
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predstavlja jednostruku ili dvostruku vezu;
w je 4;
R5 je izabran od -CH(R10)-OC(O)OR20, -CH(R10)-OC(O)R20, -CH(R10)-OC(O)NR20R21,
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i
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gdje z je 1, 2, 3, 4, 5, 6 ili 7;
svako R20 i R21 je neovisno izabrano od vodika, alifatika, supstituiranog alifatika, arila ili supstituiranog arila;
svako x i y je neovisno cijeli broj između 0 i 30,
gdje su R100, R101 i R103 neovisno izabrani od vodika, halogena, izborno supstituiranog C1-C8 alkila, izborno supstituiranog C2-C8 alkenila, izborno supstituiranog C2-C8 alkinila, izborno supstituiranog C3-C8 cikloalkila, izborno supstituiranog C1-C8 alkoksi, izborno supstituiranog C1-C8 alkilamino i izborno supstituiranog C1-C8 arila;
R105, R106 i R107 su neovisno izabrani od vodika, halogena, izborno supstituiranog C1-C24 alkila, izborno supstituiranog C2-C24 alkenila, izborno supstituiranog C2-C24 alkinila, izborno supstituiranog C3-C24 cikloalkila, izborno supstituiranog C1-C24 alkoksi, izborno supstituiranog C1-C24 alkilamino i izborno supstituiranog C1-C24 arila;
R10 je vodik, halogen, alifatik, supstituirani alifatik, aril ili supstituirani aril; i
gdje "supstituiran" označava zamjenu jednog ili više vodikovih radikala u danoj strukturi radikalom naznačenog supstituenta izabranog od halo, alkil, alkenil, alkinil, aril, heterociklil, tiol, alkiltio, ariltio, alkiltioalkil, ariltioalkil, alkilsulfonil, alkilsulfonilalkil, arilsulfonilalkil, alkoksi, ariloksi, aralkoksi, aminokarbonil, alkilaminokarbonil, arilaminokarbonil, alkoksikarbonil, ariloksikarbonil, haloalkil, amino, trifluorometil, cijano, nitro, alkilamino, arilamino, alkilaminoalkil, arilaminoalkil, aminoalkilamino, hidroksi, alkoksialkil, karboksialkil, alkoksikarbonilalkil, aminokarbonilalkil, acil, aralkoksikarbonil, karboksilne kiseline, sulfonske kiseline, sulfonila, fosfonske kiseline, heteroarila, heterociklika i alifatika.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je R5 izabran od:
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i
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3. Spoj prema patentnom zahtjevu 1, naznačen time što je R5 izabran od:
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pri čemu, svaki x i y je neovisno cijeli broj između 0 i 30, i R105, R106 i R107 su kao što je definirano u patentnom zahtjevu 1.
4. Spoj prema patentnom zahtjevu 1, naznačen time što je R5 izabran iz tabele 1:
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5. Spoj prema patentnom zahtjevu 1, naznačen time što je R5 izabran iz tabele 2, 3 ili 4:
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6. Spoj prema patentnom zahtjevu 1, koji ima formulu:
[image]
ili
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ili njihovi geometrijski izomeri, enantiomeri, diastereomeri, racemati, farmaceutski prihvatljive soli i solvati navedenog:
gdje je R5 izabran iz tabele 1:
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7. Spoj prema patentnom zahtjevu 1 izabran iz tabele A ili B i geometrijski izomeri, enantiomeri, diastereomeri, racemati, farmaceutski prihvatljive soli i solvati navedenog:
Tabela A
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Tabela B
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8. Spoj prema patentnom zahtjevu 1, formule:
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ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 1, formule:
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1, formule:
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema patentnom zahtjevu 1, formule:
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ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-11 za uporabu u liječenju neurološkog ili psihijatrijskog poremećaja.
13. Spoj za upotrebu prema patentnom zahtjevu 12, naznačen time što je navedeni poremećaj shizofrenija.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-11 za uporabu u postupku za produženu isporuku spoja formule XXIII-V:
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gdje je w kao što je definirano u patentnom zahtjevu 1; pri čemu je, nakon primjene kod pacijenta, oslobađanje spoja formule XXIII-V produženo oslobađanje.
15. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što produženo oslobađanje obuhvaća terapeutski efikasnu količinu navedenog spoja formule XXIII-V u krvotoku pacijenta tijekom perioda od najmanje oko 36 sati nakon primjene spoja prema bilo kojem od patentnih zahtjeva 1 do 11.
16. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što je navedeni spoj formule XXIII-V prisutno u krvotoku pacijenta tijekom perioda odabranog od: najmanje 7, 15, 30, 60, 75 ili 90 dana.
17. Spoj za uporabu prema patentnom zahtjevu 16, naznačen time što se spoj primjenjuje injekcijom.
18. Farmaceutski pripravak koji sadrži terapeutski efikasnu količinu spoja prema bilo kojem od patentnih zahtjeva 1-11 i jedan ili više farmaceutski prihvatljivih nosača ili ekscipijenasa.
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