HRP20160532T1 - Agonisti adenozina a1 za liječenje glaukoma i očne hipertenzije - Google Patents
Agonisti adenozina a1 za liječenje glaukoma i očne hipertenzije Download PDFInfo
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- HRP20160532T1 HRP20160532T1 HRP20160532TT HRP20160532T HRP20160532T1 HR P20160532 T1 HRP20160532 T1 HR P20160532T1 HR P20160532T T HRP20160532T T HR P20160532TT HR P20160532 T HRP20160532 T HR P20160532T HR P20160532 T1 HRP20160532 T1 HR P20160532T1
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- hydrogen
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- glaucoma
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- 238000011282 treatment Methods 0.000 title claims 11
- 206010018307 Glaucoma and ocular hypertension Diseases 0.000 title claims 2
- 239000002582 adenosine A1 receptor agonist Substances 0.000 title 1
- 239000001257 hydrogen Substances 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 28
- -1 1-methylpropan-1-yl Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 19
- 208000010412 Glaucoma Diseases 0.000 claims 18
- 238000011321 prophylaxis Methods 0.000 claims 10
- 206010030043 Ocular hypertension Diseases 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 8
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 6
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- 125000003386 piperidinyl group Chemical group 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 2
- 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 claims 2
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 2
- 239000000695 adrenergic alpha-agonist Substances 0.000 claims 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 2
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 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
- 239000002876 beta blocker Substances 0.000 claims 2
- 229940097320 beta blocking agent Drugs 0.000 claims 2
- 230000036772 blood pressure Effects 0.000 claims 2
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000000004 hemodynamic effect Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- DEFJQIDDEAULHB-WUCPZUCCSA-N 2-[[(2s)-2-aminopropanoyl]amino]propanoic acid Chemical compound C[C@H](N)C(=O)NC(C)C(O)=O DEFJQIDDEAULHB-WUCPZUCCSA-N 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- GFYUCCFYFMMXPD-UHFFFAOYSA-N 3-[2-[4-[2-(azetidin-1-yl)-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-3,5-dicyanopyridin-4-yl]phenoxy]ethylamino]propanoic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1=CC(OCCNCCC(=O)O)=CC=C1C1=C(C#N)C(SCC=2N=C(SC=2)C=2C=CC(Cl)=CC=2)=NC(N2CCC2)=C1C#N GFYUCCFYFMMXPD-UHFFFAOYSA-N 0.000 claims 1
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000006302 indol-3-yl methyl group Chemical group [H]N1C([H])=C(C2=C([H])C([H])=C([H])C([H])=C12)C([H])([H])* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004092 methylthiomethyl group Chemical group [H]C([H])([H])SC([H])([H])* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07D401/00—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
- 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
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- C07D413/02—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
- C07D413/12—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 chain containing hetero atoms as chain links
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Claims (12)
1. Spoj s formulom (I)
[image]
u kojoj
A je kisik ili sumpor,
R1 je vodik ili skupina s formulom
[image]
[image]
ili
[image]
u kojoj
# je mjesto spajanja na kisikov-atom,
L1 je ravni (C2-C4)-alkandiil,
L2 je ravni (C1-C3)-alkandiil,
R5 i R8 su isti ili različiti i neovisno odabrani iz skupine koju čine vodik, metil, propan-2-il, propan-1-il, 2-metilpropan-l-il, 1-metilpropan-1-il, butan-1-il, tert-butil, fenil, benzil, p-hidroksibenzil, indol-3-ilmetil, imidazol-4-ilmetil, hidroksimetil, 2-hidroksietil, 1-hidroksietil, merkaptometil, metiltiometil, 2-merkaptoetil, 2-metiltioetil, karbamoilmetil, 2-karbamoiletil, karboksimetil, 2-karboksietil, 4-aminobutan-1-il, 4-amino-3-hidroksibutan-1-il, 3-aminopropan-1-il, 2-aminometil, aminometil, 3-guanidinopropan-1-il, 3-ureidopropan-1-il,
R6 i R9 su neovisno odabrani od vodika ili metila,
R7 je vodik ili (C1-C4)-alkil,
ili
R7 i R5 tvore zajedno s atomima na koje su vezani pirolidinski- ili piperidinski-prsten,
R10 i R11 su isti ili različiti i neovisno su odabrani od vodika ili (C1-C4)-alkila, pri čemu (C1-C4)-alkil može biti supstituiran s jednom skupinom odabranom od hidroksi, (C1-C4)-alkoksi, amino, mono-(C1-C4)-alkilamino ili di-(C1-C4)-alkilamino,
ili
R10 i R8 tvore zajedno s atomima na koje su vezani pirolidinski- ili piperidinski-prsten,
i
R12 je vodik ili hidroksikarbonil,
R2 je vodik ili skupina s formulom -CH2OR1, pri čemu R1 je definiran kao gore,
R3 je vodik, metil ili etil,
R4 je vodik, metil ili etil,
ili
R3 i R4 tvore zajedno s atomom dušika, na koji su vezani, azetidinski-, pirolidinski- ili piperidinski-prsten, pri čemu azetidinski-, pirolidinski- ili piperidinski-prsten može biti supstituiran s jednim ili 2 supstituenta koji su neovisno odabrani iz skupine koju čine fluoro, trifluorometil, metil, etil, metoksi i etoksi,
ili njihove soli, solvati i solvati soli
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
2. Spoj s formulom (I) prema zahtjevu 1 naznačen time da
A je sumpor,
R1 je skupina s formulom
[image]
u kojoj ili
# je mjesto spajanja na kisikov-atom,
L1 je etan-1,2-diil,
R5 je vodik, metil, propan-2-il, 1-metilpropan-1-il, 2-metilpropan-1-il, hidroksilmetil ili 1-hidroksimetil,
R6 je vodik,
R7 je vodik,
R8 je vodik, metil, propan-2-il, 1-metilpropan-1-il, 2-metilpropan-l-il, imidazol-4-ilmetil, hidroksimetil, hidroksietil, 2-karboksietil, 4-aminobutan-1-il ili 2-aminoetil,
R9 je vodik,
R10 je vodik,
R11 je vodik,
ili
R10 i R8 tvore zajedno s atomima na koje su vezani pirolidinski-prsten,
R2 je vodik
R3 je vodik,
R4 je vodik,
ili
R3 i R4 tvore zajedno s atomom dušika, na koji su vezani, azetidinski- pirolidinski- ili piperidinski-prsten,
i njihove soli, solvati i solvati soli,
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
3. Spoj s formulom (I) prema zahtjevu 1 naznačen time da
A je sumpor,
R1 je skupina s formulom
[image]
u kojoj
# je mjesto spajanja na kisikov atom,
R5 je vodik, metil, propan-2-il, 2-metilpropan-l-il, benzil, hidroksimetil ili 1-hidroksietil,
R6 je vodik,
R7 je vodik,
R8 je vodik, metil, propan-2-il, 1-metilpropan-1-il, 2-metilpropan-l-il, imidazol-4-ilmetil, 4-aminobutan-1-il, 2-aminometil, 3-aminopropan-1-il, aminometil ili 3-guanidinopropan-1-il,
R9 je vodik,
R10 je vodik,
R11 je vodik,
R2 je vodik,
R3 je vodik,
R4 je vodik,
i njihove soli, solvati i solvati soli,
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
4. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 3 naznačen time da je odabran iz skupa koji čine:
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-lizil-D-alaninat-dihidroklorid,
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-arginil-D-alaninat-dihidroklorid,
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-lizil-D-valinat-dihidroklorid,
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-arginil-D-valinat-trihidroklorid,
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-lizil-D-fenilalaninat-dihidroklorid,
2-{4-[2-(azetidin-1-il)-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]fenoksi}etil-beta-alaninat-Trifluoroacetat,
2-{4-[2-(azetidin-1-il)-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]fenoksi}etil-L-ornitinat-Bis(trifluoroacetat),
2-{4-[2-(azetidin-1-il)-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]fenoksi}etil-L-lizil-L-alaninat-Bis(trifluoroacetat),
2-{4-[2-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijano-6-(pirolidin-1-il)piridin-4-il]fenoksi}etil-L-alanil-L-alaninat-hidroklorid,
2-{4-[2-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijano-6-(pirolidin-l-il)piridin-4-il]fenoksi}etil-L-isoleucil-L-alaninat-hidroklorid,
2-{4-[2-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijano-6-(pirolidin-1-il)piridin-4-il]fenoksi}etil-glicil-L-leucinat-hidroklorid,
(2S)-3-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-oksazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]fenoksi}propan-1,2-diil-(2S,2'S)-bis(2-{[(2S)-2-aminopropanoil]amino}propanoat)-dihidroklorid
ili njihove soli, solvati i solvati soli,
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
5. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 4 naznačen time da je:
2-{4-[2-amino-6-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijanopiridin-4-il]-fenoksi}etil-L-lizil-D-alaninat-dihidroklorid,
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
6. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 3 naznačen time da je:
[image]
pri čemu
R1 je
[image]
R3 je vodik,
R4 je vodik,
HA je 2 HCl.
za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija.
7. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 6 naznačen time da je za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija bez utjecaja na hemodinamiku, osobito u vezi s krvnim tlakom i brojem otkucaja srca.
8. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 ili 6, za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija, naznačen time da se spoj s formulom (I) primjenjuje topikalno na oko.
9. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 ili 6, naznačen time da je za uporabu u postupku liječenja i/ili profilakse glaukoma, normotenzivnog glaukoma, očne hipertenzije i/ili njihovih kombinacija bez utjecaja na hemodinamiku, osobito u vezi s krvnim tlakom i brojem otkucaja srca, pri čemu se spoj s formulom (I) primjenjuje topikalno na oko.
10. Spoj za uporabu prema zahtjevima 8 i 9, naznačen time da se spoj s formulom (I) daje topikalno, u kombinaciji s najmanje jednim daljnjim aktivnim spojem odabranim iz skupine koju čine alfa adrenergični agonisti, beta blokatori, te inhibitori ugljične anhidraze.
11. Spoj s formulom (I) prema bilo kojem od zahtjeva 1 ili 6 naznačen time da je za liječenje i/ili profilaksu glaukoma i očne hipertenzije kod ljudi i životinja topikalnim davanjem terapijski učinkovite količine najmanje jednog spoja prema bilo kojem od zahtjeva 1 do 6 ili lijek koji sadrži najmanje jedan spoj prema bilo kojem od zahtjeva 1 do 6 u kombinaciji s inertnim, netoksičnim, farmaceutski prihvatljivim aditivom.
12. Spoj za uporabu prema zahtjevu 11 naznačen time da lijek dodatno sadrži najmanje jedan daljnji aktivni spoj odabran iz skupine koju čine alfa adrenergični agonisti, beta blokatori, te inhibitori ugljične anhidraze.
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| EP10175151 | 2010-09-02 | ||
| PCT/EP2011/064829 WO2012028585A1 (en) | 2010-09-02 | 2011-08-29 | Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension |
| EP11752517.0A EP2611415B1 (en) | 2010-09-02 | 2011-08-29 | Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension |
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| US (3) | US20120058983A1 (hr) |
| EP (1) | EP2611415B1 (hr) |
| JP (1) | JP5875585B2 (hr) |
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| AP (1) | AP3413A (hr) |
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| CL (2) | CL2013000599A1 (hr) |
| CR (1) | CR20130094A (hr) |
| CY (1) | CY1117458T1 (hr) |
| DK (1) | DK2611415T3 (hr) |
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| US20160317542A1 (en) | 2013-12-09 | 2016-11-03 | Respira Therapeutics, Inc. | Pde5 inhibitor powder formulations and methods relating thereto |
| KR20160094974A (ko) * | 2013-12-12 | 2016-08-10 | 바이엘 파마 악티엔게젤샤프트 | 신장 질환에 대한 의약으로서의 아데노신 a1 작용제 |
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