HRP20180315T1 - Čvrsti oblici soli alfa-6-mpeg6-o-hidroksikodona kao opioidni agonisti i njihove upotrebe - Google Patents
Čvrsti oblici soli alfa-6-mpeg6-o-hidroksikodona kao opioidni agonisti i njihove upotrebe Download PDFInfo
- Publication number
- HRP20180315T1 HRP20180315T1 HRP20180315TT HRP20180315T HRP20180315T1 HR P20180315 T1 HRP20180315 T1 HR P20180315T1 HR P20180315T T HRP20180315T T HR P20180315TT HR P20180315 T HRP20180315 T HR P20180315T HR P20180315 T1 HRP20180315 T1 HR P20180315T1
- Authority
- HR
- Croatia
- Prior art keywords
- salt
- salt form
- mpeg6
- hydroxycodone
- mixture
- Prior art date
Links
- 150000003839 salts Chemical group 0.000 title claims 17
- 239000007787 solid Substances 0.000 title claims 3
- 229940127450 Opioid Agonists Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 claims 10
- FEWJPZIEWOKRBE-LWMBPPNESA-N levotartaric acid Chemical class OC(=O)[C@@H](O)[C@H](O)C(O)=O FEWJPZIEWOKRBE-LWMBPPNESA-N 0.000 claims 3
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- -1 monophosphate salt Chemical class 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 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:
- C07D489/02—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 oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
- C07D489/04—Salts; Organic complexes
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Dermatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (16)
1. Čvrsti oblik fosfatne ili D-tartaratne soli α-6-mPEG6-O-hidroksikodona.
2. Oblik soli iz patentnog zahtjeva 1, naznačen time, što je oblik soli neuređeni kristalni oblik.
3. Oblik soli iz patentnog zahtjeva 1, naznačen time, što je oblik soli kristalni oblik.
4. Oblik soli iz bilo kojeg od prethodnih patentnih zahtjeva, naznačen time, što je oblik soli α-6-mPEG6-O-hidroksikodon fosfatna sol.
5. Oblik soli iz patentnog zahtjeva 4, naznačen time, što je α-6-mPEG6-O-hidroksikodon fosfatna sol monofosfatna sol.
6. Oblik soli iz patentnog zahtjeva 1, naznačen time, što je oblik soli α-6-mPEG6-O-hidroksikodon D-tartaratna sol.
7. Čvrsti oblik soli iz patentnog zahtjeva 6, naznačen time, što je α-6-mPEG6-O-hidroksikodon D-tartaratna sol monotartaratna sol.
8. Oblik soli iz bilo kojeg od prethodnih patentnih zahtjeva, naznačen time, što se upotrebljava za liječenje boli kod pacijenata.
9. Oblik soli za upotrebu prema patentnom zahtjevu 8, naznačen time, što je bol umjerena do snažna bol.
10. Farmaceutska smjesa, naznačena time, što sadrži oblik soli iz bilo kojeg od prethodnih patentnih zahtjeva i najmanje jedan farmaceutski prihvatljivi ekscipijent.
11. Farmaceutska smjesa iz patentnog zahtjeva 10, naznačena time, što je farmaceutska smjesa tableta.
12. Farmaceutska smjesa iz patentnog zahtjeva 11, naznačena time, što tableta ima sadržaj oblika soli od 10 do 50 postotaka.
13. Farmaceutska smjesa iz bilo kojeg od patentnih zahtjeva 10 do 12, naznačena time, što smjesa sadrži 5 mg do 1000 mg oblika soli.
14. Farmaceutska smjesa iz bilo kojeg od patentnih zahtjeva 10 do 13, naznačena time, što smjesa sadrži jedan ili više ekscipijenata odabranih iz grupe koja se sastoji od dibaznog kalcijevog fosfata, mikrokristalne celuloze, kroskarmeloze natrija, koloidnog silicijevog dioksida i magnezijevog stearata.
15. Farmaceutska smjesa iz bilo kojeg od patentnih zahtjeva 10 do 14, naznačena time, što se upotrebljava za liječenje boli kod pacijenta.
16. Smjesa za upotrebu prema patentnom zahtjevu 15, naznačena time, što je bol umjerena do snažna bol.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261720259P | 2012-10-30 | 2012-10-30 | |
US201361791894P | 2013-03-15 | 2013-03-15 | |
PCT/US2013/067273 WO2014070745A1 (en) | 2012-10-30 | 2013-10-29 | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
EP13796178.5A EP2914599B1 (en) | 2012-10-30 | 2013-10-29 | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20180315T1 true HRP20180315T1 (hr) | 2018-03-23 |
Family
ID=49674367
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20180315TT HRP20180315T1 (hr) | 2012-10-30 | 2018-02-21 | Čvrsti oblici soli alfa-6-mpeg6-o-hidroksikodona kao opioidni agonisti i njihove upotrebe |
Country Status (23)
Country | Link |
---|---|
US (2) | US9682988B2 (hr) |
EP (2) | EP2914599B1 (hr) |
JP (2) | JP6384964B2 (hr) |
KR (1) | KR20150076175A (hr) |
CN (2) | CN110615796A (hr) |
AU (2) | AU2013338098B2 (hr) |
CA (1) | CA2886276A1 (hr) |
CY (1) | CY1119871T1 (hr) |
DK (1) | DK2914599T3 (hr) |
EA (1) | EA029512B1 (hr) |
ES (1) | ES2651689T3 (hr) |
HK (2) | HK1213549A1 (hr) |
HR (1) | HRP20180315T1 (hr) |
HU (1) | HUE038161T2 (hr) |
IL (1) | IL238529A0 (hr) |
LT (1) | LT2914599T (hr) |
ME (1) | ME02971B (hr) |
MX (1) | MX367773B (hr) |
PL (1) | PL2914599T3 (hr) |
PT (1) | PT2914599T (hr) |
RS (1) | RS56898B1 (hr) |
SI (1) | SI2914599T1 (hr) |
WO (1) | WO2014070745A1 (hr) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10512644B2 (en) * | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
JP6384964B2 (ja) * | 2012-10-30 | 2018-09-05 | ネクター セラピューティクス | オピオイド作動薬としてのα−6−MPEG6−O−ヒドロキシコドンの固体塩およびその使用 |
EP3658121A1 (en) * | 2017-07-27 | 2020-06-03 | Inheris Biopharma, Inc. | Oral tablet formulations |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5800334A (en) | 1993-06-17 | 1998-09-01 | Wilk; Peter J. | Intrapericardial assist device and associated method |
US6096337A (en) | 1996-06-10 | 2000-08-01 | Spireas; Spiridon | Liquisolid systems and methods of preparing same |
ATE462417T1 (de) | 1998-08-13 | 2010-04-15 | Cima Labs Inc | Microemulsionen als feste dosisformen zur oralen verabreichung |
US6342249B1 (en) | 1998-12-23 | 2002-01-29 | Alza Corporation | Controlled release liquid active agent formulation dosage forms |
WO2002081477A1 (fr) * | 2001-03-30 | 2002-10-17 | Toray Industries, Inc. | Derives morphinane 7-substitues et leur utilisation medicinale |
WO2002080918A1 (fr) * | 2001-04-02 | 2002-10-17 | Toray Industries, Inc. | Agent therapeutique ou prophylactique en cas de miction frequente ou d'incontinence urinaire |
EP2939696B1 (en) | 2001-10-18 | 2016-03-09 | Nektar Therapeutics | Polymer conjugates of opioid antagonists |
JP2005053744A (ja) | 2003-08-05 | 2005-03-03 | Dsl Japan Co Ltd | 高吸油性非晶質シリカ粒子 |
US20050245557A1 (en) * | 2003-10-15 | 2005-11-03 | Pain Therapeutics, Inc. | Methods and materials useful for the treatment of arthritic conditions, inflammation associated with a chronic condition or chronic pain |
EP2010539B1 (en) | 2006-04-21 | 2017-06-14 | Nektar Therapeutics | Stereoselective reduction of a morphinone |
EP2620163B1 (en) * | 2007-03-12 | 2017-05-03 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
CN102159249A (zh) | 2008-09-16 | 2011-08-17 | 尼克塔治疗公司 | 具有低滥用潜在性的聚乙二醇化阿片样物质 |
EP2456469A1 (en) * | 2009-07-21 | 2012-05-30 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
WO2011088140A1 (en) * | 2010-01-12 | 2011-07-21 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
JP6034789B2 (ja) * | 2010-09-30 | 2016-11-30 | アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag | 結晶性ナロキソール−peg接合体 |
EP2606879A1 (en) * | 2011-12-21 | 2013-06-26 | Hexal AG | Multiple unit pellet tablet formulation comprising an opioid |
JP6384964B2 (ja) * | 2012-10-30 | 2018-09-05 | ネクター セラピューティクス | オピオイド作動薬としてのα−6−MPEG6−O−ヒドロキシコドンの固体塩およびその使用 |
-
2013
- 2013-10-29 JP JP2015539912A patent/JP6384964B2/ja not_active Expired - Fee Related
- 2013-10-29 MX MX2015005510A patent/MX367773B/es active IP Right Grant
- 2013-10-29 AU AU2013338098A patent/AU2013338098B2/en not_active Ceased
- 2013-10-29 SI SI201330875T patent/SI2914599T1/en unknown
- 2013-10-29 LT LTEP13796178.5T patent/LT2914599T/lt unknown
- 2013-10-29 CA CA 2886276 patent/CA2886276A1/en not_active Abandoned
- 2013-10-29 KR KR1020157010866A patent/KR20150076175A/ko not_active Application Discontinuation
- 2013-10-29 WO PCT/US2013/067273 patent/WO2014070745A1/en active Application Filing
- 2013-10-29 HU HUE13796178A patent/HUE038161T2/hu unknown
- 2013-10-29 EP EP13796178.5A patent/EP2914599B1/en active Active
- 2013-10-29 CN CN201910553996.1A patent/CN110615796A/zh active Pending
- 2013-10-29 ME MEP-2018-48A patent/ME02971B/me unknown
- 2013-10-29 EA EA201590853A patent/EA029512B1/ru not_active IP Right Cessation
- 2013-10-29 PT PT137961785T patent/PT2914599T/pt unknown
- 2013-10-29 PL PL13796178T patent/PL2914599T3/pl unknown
- 2013-10-29 DK DK13796178.5T patent/DK2914599T3/en active
- 2013-10-29 EP EP17186401.0A patent/EP3327022A1/en not_active Withdrawn
- 2013-10-29 RS RS20180190A patent/RS56898B1/sr unknown
- 2013-10-29 ES ES13796178.5T patent/ES2651689T3/es active Active
- 2013-10-29 CN CN201380056619.8A patent/CN104755481A/zh active Pending
- 2013-10-29 US US14/439,473 patent/US9682988B2/en active Active
-
2015
- 2015-04-29 IL IL238529A patent/IL238529A0/en unknown
-
2016
- 2016-02-05 HK HK16101433.5A patent/HK1213549A1/zh not_active IP Right Cessation
-
2017
- 2017-04-26 US US15/498,308 patent/US20170226119A1/en not_active Abandoned
-
2018
- 2018-02-01 CY CY20181100121T patent/CY1119871T1/el unknown
- 2018-02-21 HR HRP20180315TT patent/HRP20180315T1/hr unknown
- 2018-02-22 AU AU2018201297A patent/AU2018201297A1/en not_active Abandoned
- 2018-03-26 JP JP2018058310A patent/JP2018111718A/ja active Pending
- 2018-06-12 HK HK18107623.0A patent/HK1248224A1/zh unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20201967T1 (hr) | Heterociklički spojevi i njihova uporaba | |
NZ593045A (en) | Pharmaceutical dosage form comprising nifedipine or nisoldipine and an angiotensin-ii antagonist and/or a diuretic | |
HRP20180315T1 (hr) | Čvrsti oblici soli alfa-6-mpeg6-o-hidroksikodona kao opioidni agonisti i njihove upotrebe | |
NZ753904A (en) | Compositions and methods for treating anemia | |
HRP20201162T1 (hr) | Farmaceutski sastav koji može uključiti lenalidomid u različitim kristaliničnim modifikacijama | |
RU2011152105A (ru) | Составы таблеток 3-цианохинолина и их применение | |
HRP20191559T1 (hr) | Farmaceutski pripravci za liječenje infekcije bakterijom helicobacter pylori | |
BR112018012870A2 (pt) | métodos e composições para o tratamento de transtornos relacionados à crise | |
RU2012121857A (ru) | Твердые фармацевтические композиции, содержащие ингибитор интегразы | |
MX2015002005A (es) | Combinacion de inhibidor de p13k e inhibidor de c-met. | |
MX2021001905A (es) | Preparacion farmaceutica que tiene excelentes propiedades de disolucion, que contiene esomeprazol y bicarbonato de sodio. | |
PH12015502406A1 (en) | Orally administrable pharmaceutical composition for prevention or treatment of dry eye syndrome, comprising rebamipide or prodrug thereof | |
JP2019529570A5 (hr) | ||
HRP20161796T1 (hr) | Farmaceutski pripravak za primjenu u tretmanu ili prevenciji deficijencije vitamina i minerala kod pacijenata podvrgnutih operaciji želučane premosnice | |
JP2015521647A5 (hr) | ||
RU2015140463A (ru) | Способ лечения недостаточности витамина в12 | |
SA516370446B1 (ar) | تركيبة صيدلانية مستقرة مضادة للدرن في صورة قرص قابل للتشتت يحتوي على حبيبات إيزونيازيد وحبيبات ريفابنتين، وعملية لتحضيرها | |
EA201170583A1 (ru) | Новая композиция для лечения эссенциальной тромбоцитемии | |
JP2015120758A5 (hr) | ||
HRP20150387T1 (hr) | Sol kolina i trometamina od likofelona | |
MX370184B (es) | Composición farmacéutica que comprende fingolimod. | |
HRP20210691T1 (hr) | Farmaceutski oblici doziranja koji sadrže natrij 1-[6-(morfolin-4-il)pirimidin-4-il]-4-(1h-1,2,3-triazol-1-il)-1h-pirazol-5-olat | |
BR112012020415A2 (pt) | composição farmacêutica para a prevenção ou tratamento da osteoartrite | |
MX2016001154A (es) | Composicion farmaceutica anti-tuberculosis estable en una forma de un comprimido recubierto que comprende granulos de isoniazid y granulos de rifapentina y su proceso de preparacion. | |
HRP20171305T1 (hr) | Upotreba odiparcila u liječenju mukopolisaharidoze |