HRP20180048T1 - Derivati fentanila kao agonisti opioidnih receptora ovisni o ph - Google Patents
Derivati fentanila kao agonisti opioidnih receptora ovisni o ph Download PDFInfo
- Publication number
- HRP20180048T1 HRP20180048T1 HRP20180048TT HRP20180048T HRP20180048T1 HR P20180048 T1 HRP20180048 T1 HR P20180048T1 HR P20180048T T HRP20180048T T HR P20180048TT HR P20180048 T HRP20180048 T HR P20180048T HR P20180048 T1 HRP20180048 T1 HR P20180048T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- pain
- compound according
- image
- inflammation
- Prior art date
Links
- 102000003840 Opioid Receptors Human genes 0.000 title claims 3
- 108090000137 Opioid Receptors Proteins 0.000 title claims 3
- 230000001419 dependent effect Effects 0.000 title 1
- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical class C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 title 1
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 239000003814 drug Substances 0.000 claims 5
- 206010061218 Inflammation Diseases 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000003902 lesion Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 206010006002 Bone pain Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000001272 neurogenic effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Claims (14)
1. Spoj opće Formule I
[image]
,
naznačen time što je jedan od R1, R2, R3, R4 F, a
preostali ostaci na položajima R1, R2, R3, R4 su H.
2. Spoj u skladu s prethodnim patentnim zahtjevom, naznačen time što je spoj Formule II:
[image]
.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj Formule III:
[image]
.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj Formule IV:
[image]
.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj Formule V:
[image]
.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je namijenjenjen upotrebi kao medikament.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je namijenjenjen upotrebi kao medikament u liječenju boli povezane s upalom.
8. Spoj u skladu s prethodnim patentnim zahtjevom namijenjen upotrebi kao medikament, naznačen time što spoj aktivira ciljani opioidni receptor u uvjetima pH povezanog s upalom u upaljenom tkivu, gdje uvjeti pH povezanog s upalom pokazuju vrijednost pH ispod 7.
9. Spoj namijenjen upotrebi kao medikament u skladu s patentnim zahtjevom 8, naznačen time što se navedeni ciljani opioidni receptor bira iz skupine koju čine receptor μ, receptor δ i receptor κ.
10. Spoj namijenjen upotrebi kao medikament u skladu s patentnim zahtjevom 7, naznačen time što se bol povezanu s upalom bira iz skupine koju čine artritis, upala kože, upalna bol u leđima, glavobolja, primjerice neurogena migrena, upalne lezije u središnjem i perifernom živčanom sustavu, primjerice neuropatska bol, bol uzrokovana rakom, poremećaji imunosnog sustava, primjerice HIV/AIDS ili multipla skleroza, traumatska bol, postoperativna bol, upaljeni zglobovi, kirurški zahvat na zubalu, visceralna bol, kostobolja, opeklinska ozljeda i lezije oka.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, i/ili njegove soli, uz najmanje jednu farmaceutski prihvatljivu podlogu.
12. Farmaceutski pripravak u skladu s prethodnim patentnim zahtjevom, naznačen time što sadrži smjesu najmanje 2 spoja formula II, III, IV i/ili V, i/ili njihovih soli.
13. Farmaceutski pripravak u skladu s prethodnim patentnim zahtjevom, naznačen time što sadrži stereoizomernu smjesu spojeva formula II, III, IV i/ili V.
14. Farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 11 do 13, naznačen time što je navedeni pripravak u obliku pogodnom za topikalnu ili oralnu upotrebu.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11178122A EP2559685A1 (en) | 2011-08-19 | 2011-08-19 | Fentanyl derivatives as pH-dependent opioid receptor agonists |
| PCT/EP2012/066071 WO2013026787A1 (en) | 2011-08-19 | 2012-08-17 | Fentanyl derivatives as ph-dependent opioid receptor agonists |
| EP12753447.7A EP2744781B1 (en) | 2011-08-19 | 2012-08-17 | Fentanyl derivatives as ph-dependent opioid receptor agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20180048T1 true HRP20180048T1 (hr) | 2018-03-23 |
Family
ID=46763055
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20180048TT HRP20180048T1 (hr) | 2011-08-19 | 2018-01-10 | Derivati fentanila kao agonisti opioidnih receptora ovisni o ph |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9133120B2 (hr) |
| EP (2) | EP2559685A1 (hr) |
| DK (1) | DK2744781T3 (hr) |
| ES (1) | ES2655646T3 (hr) |
| HR (1) | HRP20180048T1 (hr) |
| HU (1) | HUE037847T2 (hr) |
| NO (1) | NO2744781T3 (hr) |
| PL (1) | PL2744781T3 (hr) |
| PT (1) | PT2744781T (hr) |
| RS (1) | RS56734B1 (hr) |
| WO (1) | WO2013026787A1 (hr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020006563A1 (en) * | 2018-06-29 | 2020-01-02 | Marquette University | Fluorinated compounds as ph-sensitive analgesics |
| CN113292485B (zh) * | 2021-06-08 | 2023-10-27 | 河南大学 | 苄基哌嗪脲类trpv1拮抗和mor激动双靶点药物及制备方法和应用 |
| CN114949220B (zh) * | 2022-01-30 | 2023-09-22 | 浙江大学 | 一种靶向损伤节段背根神经节的pH响应镇痛药及其应用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3923992A (en) * | 1974-05-23 | 1975-12-02 | Univ Mississippi | Analgetic composition and method of use |
| US6677332B1 (en) * | 1999-05-25 | 2004-01-13 | Sepracor, Inc. | Heterocyclic analgesic compounds and methods of use thereof |
-
2011
- 2011-08-19 EP EP11178122A patent/EP2559685A1/en not_active Withdrawn
-
2012
- 2012-08-17 HU HUE12753447A patent/HUE037847T2/hu unknown
- 2012-08-17 ES ES12753447.7T patent/ES2655646T3/es active Active
- 2012-08-17 PL PL12753447T patent/PL2744781T3/pl unknown
- 2012-08-17 WO PCT/EP2012/066071 patent/WO2013026787A1/en active Application Filing
- 2012-08-17 US US14/239,461 patent/US9133120B2/en active Active
- 2012-08-17 PT PT127534477T patent/PT2744781T/pt unknown
- 2012-08-17 DK DK12753447.7T patent/DK2744781T3/en active
- 2012-08-17 EP EP12753447.7A patent/EP2744781B1/en active Active
- 2012-08-17 RS RS20180018A patent/RS56734B1/sr unknown
- 2012-08-17 NO NO12753447A patent/NO2744781T3/no unknown
-
2018
- 2018-01-10 HR HRP20180048TT patent/HRP20180048T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DK2744781T3 (en) | 2018-01-15 |
| EP2744781B1 (en) | 2017-10-11 |
| EP2744781A1 (en) | 2014-06-25 |
| HUE037847T2 (hu) | 2018-09-28 |
| WO2013026787A1 (en) | 2013-02-28 |
| ES2655646T3 (es) | 2018-02-21 |
| RS56734B1 (sr) | 2018-03-30 |
| PT2744781T (pt) | 2018-01-16 |
| PL2744781T3 (pl) | 2018-05-30 |
| NO2744781T3 (hr) | 2018-03-10 |
| US9133120B2 (en) | 2015-09-15 |
| US20140228406A1 (en) | 2014-08-14 |
| EP2559685A1 (en) | 2013-02-20 |
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