HRP20110824T1 - Predlijekovi nalmefena - Google Patents
Predlijekovi nalmefena Download PDFInfo
- Publication number
- HRP20110824T1 HRP20110824T1 HR20110824T HRP20110824T HRP20110824T1 HR P20110824 T1 HRP20110824 T1 HR P20110824T1 HR 20110824 T HR20110824 T HR 20110824T HR P20110824 T HRP20110824 T HR P20110824T HR P20110824 T1 HRP20110824 T1 HR P20110824T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- formula
- compound according
- image
- pharmaceutically acceptable
- Prior art date
Links
- WJBLNOPPDWQMCH-MBPVOVBZSA-N Nalmefene Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=C)O)CC1)O)CC1CC1 WJBLNOPPDWQMCH-MBPVOVBZSA-N 0.000 title claims abstract 6
- 229960005297 nalmefene Drugs 0.000 title claims abstract 4
- 239000000651 prodrug Substances 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 28
- 208000007848 Alcoholism Diseases 0.000 claims abstract 4
- 208000026331 Disruptive, Impulse Control, and Conduct disease Diseases 0.000 claims abstract 3
- 208000030990 Impulse-control disease Diseases 0.000 claims abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 201000009032 substance abuse Diseases 0.000 claims abstract 3
- 231100000736 substance abuse Toxicity 0.000 claims abstract 3
- 208000011117 substance-related disease Diseases 0.000 claims abstract 3
- 206010012335 Dependence Diseases 0.000 claims abstract 2
- 208000001613 Gambling Diseases 0.000 claims abstract 2
- 206010034158 Pathological gambling Diseases 0.000 claims abstract 2
- 206010001584 alcohol abuse Diseases 0.000 claims abstract 2
- 208000025746 alcohol use disease Diseases 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims 7
- 239000002253 acid Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 150000001266 acyl halides Chemical class 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000032050 esterification Effects 0.000 claims 1
- 238000005886 esterification reaction Methods 0.000 claims 1
- 238000013265 extended release Methods 0.000 claims 1
- 239000012948 isocyanate Substances 0.000 claims 1
- 150000002513 isocyanates Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 abstract 1
- 238000001311 chemical methods and process Methods 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
- C07D489/08—Oxygen atom
-
- 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
- A61P25/18—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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Spoj, naznačen time, da je prikazan formulom (I) uključujući i njegove bilo koje stereokemijske izomerne oblike, pri čemuR1 je C6-16alkil ili C8-12alkilamino; ili njegova farmaceutski prihvatljiva kisela adicijska sol ili njegov solvat. Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Spoj, naznačen time, da je prikazan formulom (I)
[image]
uključujući i njegove bilo koje stereokemijske izomerne oblike, pri čemu
R1 je C6-16alkil ili C8-12alkilamino;
ili njegova farmaceutski prihvatljiva kisela adicijska sol ili njegov solvat.
2. Spoj prema zahtjevu 1, naznačen time, da R1 je C7alkil, C9alkil, C11alkil ili C15alkil.
3. Spoj prema zahtjevu 1, naznačen time, da R1 je C10alkilamino.
4. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je
[image]
ili
[image]
[image]
ili
[image]
5. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je
[image]
6. Farmaceutski sastav, naznačen time, da sadrži farmaceutski prihvatljiv nosač i terapeutski učinkovitu količinu spoja prema bilo kojem od zahtjeva od 1 do 5.
7. Postupak za dobivanje farmaceutskog sastava prema zahtjevu 6, naznačen time, da je terapeutski učinkovita količina spoja prema bilo kojem od zahtjeva od 1 do 5 blisko pomiješana sa farmaceutski prihvatljivim nosačem.
8. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da se koristi kao lijek.
9. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da se koristi kod liječenja poremećaja zloupotrebe tvari i poremećaja kontroliranja nagona.
10. Spoj prema zahtjevu 9, naznačen time, da se navedeni spoj dostavlja intra-mišićno ili supkutano.
11. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da se koristi za proizvodnju lijeka za liječenje poremećaja zloupotrebe tvari poput zloupotrebe alkohola i ovisnosti o alkoholu, te poremećaja kontroliranja nagona poput patološkog kockanja i ovisnosti o kupovini.
12. Spoj prema zahtjevu 11, naznačen time, da se koristi za proizvodnju lijeka pri čemu se navedeni lijek dostavlja intra-mišićno ili supkutano.
13. Spoj prema zahtjevu 12, naznačen time, da se koristi za proizvodnju lijeka pri čemu navedeni lijek je lijek sa produženim otpuštanjem.
14. Postupak za dobivanje spoja sa formulom (I-a), definiranog kao spoja sa formulom (I), kako je zatraženo u zahtjevu 1, pri čemu R1 predstavlja C6-16alkil, naznačen time da se navedeni spoj može pripremiti pomoću postupaka esterifikacije koji su poznati u stanju tehnike pomoću reakcije nalmefena (II) sa acil halidom sa formulom (III) u prisutnosti baze koja treba preuzeti kiselinu, koja se oslobađa tijekom reakcije,
[image]
ili; ako je poželjno; spoj formule (I-a) pretvara se u farmaceutski prihvatljivu kiselu adicijsku sol, ili suprotno, kisela adicijska sol spoja formule (I-a) pretvara se u oblik slobodne alkalne baze; te ako se želi, pripreme njegovih stereokemijskih izomernih oblika.
15. Postupak za dobivanje spoja sa formulom (I-b), definiranog kao spoja sa formulom (I) pri čemu R1 predstavlja C8-12alkilamino, naznačen time, da se navedeni spoj može pripremiti pomoću reakcije nalmefena (II) sa izocijanatom prema formuli (IV),
[image]
ili; ako se želi; spoj sa formulom (I-b) pretvara se u farmaceutski prihvatljivu adicijsku sol, ili suprotno, kisela adicijska sol spoja formule (I-b) pretvara se u oblik slobodne alkalne baze; te ako se želi, pripreme njegovih stereokemijskih izomernih oblika.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08155094 | 2008-04-24 | ||
| PCT/EP2009/054882 WO2009130272A1 (en) | 2008-04-24 | 2009-04-23 | Nalmefene prodrugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110824T1 true HRP20110824T1 (hr) | 2012-01-31 |
Family
ID=39816976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110824T HRP20110824T1 (hr) | 2008-04-24 | 2011-11-09 | Predlijekovi nalmefena |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8440686B2 (hr) |
| EP (1) | EP2291380B1 (hr) |
| JP (1) | JP6009764B2 (hr) |
| KR (1) | KR101598137B1 (hr) |
| CN (1) | CN102066381A (hr) |
| AT (1) | ATE523512T1 (hr) |
| AU (1) | AU2009239929B2 (hr) |
| CA (1) | CA2722246C (hr) |
| CY (1) | CY1112295T1 (hr) |
| DK (1) | DK2291380T3 (hr) |
| ES (1) | ES2373364T3 (hr) |
| HR (1) | HRP20110824T1 (hr) |
| ME (1) | ME01319B (hr) |
| PL (1) | PL2291380T3 (hr) |
| PT (1) | PT2291380E (hr) |
| RS (1) | RS52041B (hr) |
| RU (1) | RU2495042C2 (hr) |
| SI (1) | SI2291380T1 (hr) |
| WO (1) | WO2009130272A1 (hr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019086017A1 (en) * | 2017-11-03 | 2019-05-09 | Nirsum Laboratories, Inc. | Opioid receptor antagonist prodrugs |
| TW202015684A (zh) * | 2018-06-21 | 2020-05-01 | 景凱生物科技股份有限公司 | 那曲酮、納美芬及其衍生物之前藥 |
| AU2019444588A1 (en) | 2019-05-07 | 2021-12-02 | Nirsum Laboratories, Inc. | Opioid receptor antagonist prodrugs |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4673679A (en) * | 1986-05-14 | 1987-06-16 | E. I. Du Pont De Nemours And Company | Use of prodrugs of 3-hydroxymorphinans to prevent bitter taste upon buccal, nasal or sublingual administration |
| US5086058A (en) * | 1990-06-04 | 1992-02-04 | Alko Ltd. | Method for treating alcoholism with nalmefene |
| JPH06271578A (ja) * | 1993-03-15 | 1994-09-27 | Natl Sci Council | 鎮痛剤ナルブフィン前薬の誘導体 |
| DE69427551T2 (de) * | 1993-03-15 | 2002-05-16 | National Science Council, Taipeh/T'ai-Pei | Nalbuphinester und diese enthaltende Arzneimittel mit verzögerter Wirkstoffabgabe |
| US5869669A (en) * | 1996-07-26 | 1999-02-09 | Penick Corporation | Preparation of 14-hydroxynormorphinones from normorphinone dienol acylates |
| US20030153590A1 (en) * | 2001-08-14 | 2003-08-14 | Oy Contral Pharma Ltd | Method of treating alcoholism or alcohol abuse |
| US20040033253A1 (en) * | 2002-02-19 | 2004-02-19 | Ihor Shevchuk | Acyl opioid antagonists |
| US7759358B2 (en) * | 2003-07-23 | 2010-07-20 | Crooks Peter A | Oral bioavailable prodrugs |
| WO2008101187A2 (en) * | 2007-02-16 | 2008-08-21 | Pharmacofore, Inc. | Pro-drugs of peripheral phenolic opioid antagonists |
| DK2307420T3 (da) * | 2008-04-24 | 2012-02-27 | Janssen Pharmaceutica Nv | Nalmefendiester-prodrugs |
-
2009
- 2009-04-23 DK DK09733923.8T patent/DK2291380T3/da active
- 2009-04-23 RS RS20110534A patent/RS52041B/en unknown
- 2009-04-23 AT AT09733923T patent/ATE523512T1/de active
- 2009-04-23 KR KR1020107025887A patent/KR101598137B1/ko active IP Right Grant
- 2009-04-23 CN CN2009801142933A patent/CN102066381A/zh active Pending
- 2009-04-23 AU AU2009239929A patent/AU2009239929B2/en not_active Ceased
- 2009-04-23 US US12/937,744 patent/US8440686B2/en active Active
- 2009-04-23 PL PL09733923T patent/PL2291380T3/pl unknown
- 2009-04-23 PT PT09733923T patent/PT2291380E/pt unknown
- 2009-04-23 RU RU2010147833/04A patent/RU2495042C2/ru active
- 2009-04-23 CA CA2722246A patent/CA2722246C/en active Active
- 2009-04-23 ME MEP-2011-200A patent/ME01319B/me unknown
- 2009-04-23 JP JP2011505510A patent/JP6009764B2/ja active Active
- 2009-04-23 EP EP09733923A patent/EP2291380B1/en active Active
- 2009-04-23 SI SI200930109T patent/SI2291380T1/sl unknown
- 2009-04-23 ES ES09733923T patent/ES2373364T3/es active Active
- 2009-04-23 WO PCT/EP2009/054882 patent/WO2009130272A1/en active Application Filing
-
2011
- 2011-11-09 HR HR20110824T patent/HRP20110824T1/hr unknown
- 2011-12-06 CY CY20111101207T patent/CY1112295T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009130272A1 (en) | 2009-10-29 |
| DK2291380T3 (da) | 2011-12-05 |
| US20110034502A1 (en) | 2011-02-10 |
| EP2291380B1 (en) | 2011-09-07 |
| ME01319B (me) | 2013-12-20 |
| RU2010147833A (ru) | 2012-05-27 |
| PL2291380T3 (pl) | 2012-02-29 |
| CA2722246A1 (en) | 2009-10-29 |
| AU2009239929B2 (en) | 2014-02-13 |
| KR101598137B1 (ko) | 2016-02-29 |
| US8440686B2 (en) | 2013-05-14 |
| ATE523512T1 (de) | 2011-09-15 |
| SI2291380T1 (sl) | 2012-01-31 |
| JP6009764B2 (ja) | 2016-10-19 |
| CA2722246C (en) | 2016-06-21 |
| KR20110004877A (ko) | 2011-01-14 |
| CN102066381A (zh) | 2011-05-18 |
| CY1112295T1 (el) | 2015-12-09 |
| EP2291380A1 (en) | 2011-03-09 |
| PT2291380E (pt) | 2011-12-22 |
| ES2373364T3 (es) | 2012-02-02 |
| JP2011518805A (ja) | 2011-06-30 |
| AU2009239929A1 (en) | 2009-10-29 |
| RU2495042C2 (ru) | 2013-10-10 |
| RS52041B (en) | 2012-04-30 |
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