HRP20130213T1 - Spojevi morfinana - Google Patents
Spojevi morfinana Download PDFInfo
- Publication number
- HRP20130213T1 HRP20130213T1 HRP20130213AT HRP20130213T HRP20130213T1 HR P20130213 T1 HRP20130213 T1 HR P20130213T1 HR P20130213A T HRP20130213A T HR P20130213AT HR P20130213 T HRP20130213 T HR P20130213T HR P20130213 T1 HRP20130213 T1 HR P20130213T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- quinidine
- therapeutic agent
- Prior art date
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- INAXVFBXDYWQFN-XHSDSOJGSA-N morphinan Chemical class C1C2=CC=CC=C2[C@]23CCCC[C@H]3[C@@H]1NCC2 INAXVFBXDYWQFN-XHSDSOJGSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 11
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 239000000203 mixture Substances 0.000 claims abstract 9
- LOUPRKONTZGTKE-LHHVKLHASA-N quinidine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-LHHVKLHASA-N 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 7
- GJHKWLSRHNWTAN-UHFFFAOYSA-N 1-ethoxy-4-(4-pentylcyclohexyl)benzene Chemical compound C1CC(CCCCC)CCC1C1=CC=C(OCC)C=C1 GJHKWLSRHNWTAN-UHFFFAOYSA-N 0.000 claims 6
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 6
- 239000002552 dosage form Substances 0.000 claims 6
- 229960004482 quinidine sulfate Drugs 0.000 claims 6
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 claims 5
- 229960001404 quinidine Drugs 0.000 claims 5
- 238000004806 packaging method and process Methods 0.000 claims 4
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 229960002870 gabapentin Drugs 0.000 claims 3
- 208000004296 neuralgia Diseases 0.000 claims 3
- 208000021722 neuropathic pain Diseases 0.000 claims 3
- 229960002085 oxycodone Drugs 0.000 claims 3
- 102100031265 Chromodomain-helicase-DNA-binding protein 2 Human genes 0.000 claims 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- 101000777079 Homo sapiens Chromodomain-helicase-DNA-binding protein 2 Proteins 0.000 claims 2
- 101000880945 Homo sapiens Down syndrome cell adhesion molecule Proteins 0.000 claims 2
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 abstract 1
- 239000000018 receptor agonist Substances 0.000 abstract 1
- 229940044601 receptor agonist Drugs 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
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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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/49—Cinchonan derivatives, e.g. quinine
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- 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
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
-
- 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
- A61P11/14—Antitussive agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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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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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- 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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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
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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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- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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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
- C07D221/28—Morphinans
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D471/08—Bridged systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Addiction (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Toxicology (AREA)
- Nutrition Science (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
Claims (21)
1. Spoj formule I:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
R1 se izabire između CH3, CH2D, CHD2, CD3, CHF2, i CF3; i
R2 se izabire između CH3, CH2D, CHD2, i CD3;
uz uvjet da kada R1 je CH3, tada R2 nije CH3;
za uporabu u liječenju bolesnika koji pati od ili koji je podložan dijabetičkoj neuropatskoj boli.
2. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, gdje R1 je CD3 i R2 je CH3.
3. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, gdje R1 je CD3, i R2 nije CH3.
4. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od prethodnih zahtjeva, gdje je svaki atom, koji nije označen kao deuterij, prisutan kao svoj prirodni većinski izotop.
5. Smjesa bez pirogena koja sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od prethodnih zahtjeva i prihvatljivi nosač, za uporabu u liječenju bolesnika koji pati od ili koji je podložan dijabetičkoj neuropatskoj boli.
6. Smjesa prema zahtjevu 5 oblikovana za farmaceutsku primjenu i gdje je nosač farmaceutski prihvatljivi nosač.
7. Smjesa prema zahtjevu 5 ili 6, dalje sadrži drugo terapijsko sredstvo izabrano između kinidina, kinidin sulfata, oksikodona, i gabapentina.
8. Smjesa prema zahtjevu 7, gdje je drugo terapijsko sredstvo kinidin sulfat.
9. Zasebni dozirni oblici:
(i) spoja, njegove farmaceutski prihvatljive soli ili smjese prema bilo kojem od zahtjeva 1-6; i
(ii) drugog terapijskog sredstva izabranog između kinidina, kinidin sulfata, oksikodona i gabapentina,
gdje su taj spoj, njegova farmaceutski prihvatljiva sol ili smjesa i drugo terapijsko sredstvo međusobno povezani.
10. Zasebni dozirni oblici prema zahtjevu 9, gdje je drugo terapijsko sredstvo kinidin sulfat.
11. Pakiranje koje sadrži zasebne dozirne oblike prema zahtjevu 9 ili 10.
12. Zasebni dozirni oblici ili pakiranje prema bilo kojem od zahtjeva 9-11, gdje je to drugo sredstvo za istodobnu primjenu.
13. Zasebni dozirni oblici ili pakiranje prema bilo kojem od zahtjeva 9-11, je to drugo sredstvo za posebnu primjenu.
14. Smjesa, zasebni dozirni oblici ili pakiranje prema bilo kojem od zahtjeva 7-13, koji sadrže 10-60 mg spoja Formule I ili njegove farmaceutski prihvatljive soli, i 2.5-30 mg kinidina.
15. Uporaba spoja formule I:
[image]
ili njegove farmaceutski prihvatljive soli, gdje:
R1 se izabire između CH3, CH2D, CHD2, CD3, CHF2, i CF3; i
R2 se izabire između CH3, CH2D, CHD2, i CD3;
uz uvjet da kada R1 je CH3, tada R2 nije CH3;
u proizvodnji lijeka za liječenje dijabetičke neuropatske boli.
16. Uporaba prema zahtjevu 15, gdje R1 je CD3 i R2 je CH3.
17. Uporaba prema zahtjevu 15, gdje R1 je CD3, i R2 nije CH3..
18. Uporaba prema bilo kojem od zahtjeva 15-17, gdje je svaki atom, koji nije označen kao deuterij, prisutan kao svoj prirodni većinski izotop.
19. Uporaba prema bilo kojem od zahtjeva 15-18, zajedno s drugim terapijskim sredstvom koje se izabire između kinidina, kinidin sulfata, oksikodona i gabapentina.
20. Uporaba prema zahtjevu 19, gdje je drugo terapijsko sredstvo kinidin sulfat.
21. Uporaba prema zahtjevu 19 ili 20, gdje je doza spoja Formule I ili njegove farmaceutski prihvatljive soli 10-60 mg, i doza kinidina je 2.5-30 mg.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US91513007P | 2007-05-01 | 2007-05-01 | |
US91666207P | 2007-05-08 | 2007-05-08 | |
US97600407P | 2007-09-28 | 2007-09-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20130213T1 true HRP20130213T1 (hr) | 2013-04-30 |
Family
ID=47290415
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120317AT HRP20120317T1 (hr) | 2007-05-01 | 2012-04-11 | Spojevi morfinana |
HRP20130213AT HRP20130213T1 (hr) | 2007-05-01 | 2013-03-11 | Spojevi morfinana |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120317AT HRP20120317T1 (hr) | 2007-05-01 | 2012-04-11 | Spojevi morfinana |
Country Status (15)
Country | Link |
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US (5) | US7973049B2 (hr) |
EP (4) | EP2345653B1 (hr) |
JP (8) | JP4944244B2 (hr) |
CN (3) | CN101687868B (hr) |
AT (1) | ATE546449T1 (hr) |
AU (1) | AU2008247818B2 (hr) |
CA (2) | CA2685723C (hr) |
DK (3) | DK2345653T3 (hr) |
ES (2) | ES2401892T3 (hr) |
HK (3) | HK1140755A1 (hr) |
HR (2) | HRP20120317T1 (hr) |
MX (3) | MX2009011958A (hr) |
PL (4) | PL2152709T3 (hr) |
PT (2) | PT2345653E (hr) |
WO (1) | WO2008137474A1 (hr) |
Families Citing this family (176)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008022285A1 (en) * | 2006-08-16 | 2008-02-21 | Auspex Pharmaceuticals, Inc. | Preparation and utility of opioid analgesics |
HUE063526T2 (hu) | 2007-05-01 | 2024-01-28 | Concert Pharmaceuticals Ind Inc | Morfinvegyületek |
PT2345653E (pt) | 2007-05-01 | 2013-04-01 | Concert Pharmaceuticals Inc | Compostos de morfinano |
AU2009293123B2 (en) | 2008-09-19 | 2013-12-19 | Concert Pharmaceuticals Inc. | Morphinan compounds |
HUE028956T2 (en) * | 2008-10-30 | 2017-01-30 | Concert Pharmaceuticals Inc | A combination of morphine compounds and an antidepressant for the treatment of pseudobulbar effects |
WO2011009020A2 (en) | 2009-07-16 | 2011-01-20 | Mallinckrodt Inc. | Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers |
US20110206780A1 (en) * | 2010-01-06 | 2011-08-25 | Auspex Pharmaceuticals, Inc. | Morphinan modulators of nmda receptors, sigma1 receptors, sigma2 receptors, and/or a3b4 nicotinic receptors |
MX2012008721A (es) | 2010-02-16 | 2012-08-17 | Pfizer | (r)-4-((4-((4-(tetrahidrofuran-3-iloxi)benzo[d]isoxazol-3-iloxi)m etil) tetrahidro-2h-piran-4-ol, un agonista pacial de receptores 5-ht4. |
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