HRP20140385T1 - Polimorfni oblici (2s)-(4e)-n-metil-5-[3-(5-izopropoksipiridin)il]-4-penten-2-amin p-hidroksibenzoata u terapiji poremeä†aja središnjeg živäśanog sustava - Google Patents
Polimorfni oblici (2s)-(4e)-n-metil-5-[3-(5-izopropoksipiridin)il]-4-penten-2-amin p-hidroksibenzoata u terapiji poremeä†aja središnjeg živäśanog sustava Download PDFInfo
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- HRP20140385T1 HRP20140385T1 HRP20140385TT HRP20140385T HRP20140385T1 HR P20140385 T1 HRP20140385 T1 HR P20140385T1 HR P20140385T T HRP20140385T T HR P20140385TT HR P20140385 T HRP20140385 T HR P20140385T HR P20140385 T1 HRP20140385 T1 HR P20140385T1
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- FJKROLUGYXJWQN-UHFFFAOYSA-M 4-hydroxybenzoate Chemical compound OC1=CC=C(C([O-])=O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-M 0.000 title claims 3
- 208000015114 central nervous system disease Diseases 0.000 title claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 10
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 8
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 8
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 8
- 208000028017 Psychotic disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 208000010877 cognitive disease Diseases 0.000 claims 5
- 208000035474 group of disease Diseases 0.000 claims 5
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 206010027175 memory impairment Diseases 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 206010065040 AIDS dementia complex Diseases 0.000 claims 3
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 3
- 201000002832 Lewy body dementia Diseases 0.000 claims 3
- 206010036631 Presenile dementia Diseases 0.000 claims 3
- 208000020186 Schizophreniform disease Diseases 0.000 claims 3
- 206010039966 Senile dementia Diseases 0.000 claims 3
- 208000006011 Stroke Diseases 0.000 claims 3
- 201000004810 Vascular dementia Diseases 0.000 claims 3
- 206010013932 dyslexia Diseases 0.000 claims 3
- 208000025688 early-onset autosomal dominant Alzheimer disease Diseases 0.000 claims 3
- 208000022610 schizoaffective disease Diseases 0.000 claims 3
- 201000000980 schizophrenia Diseases 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- 206010012289 Dementia Diseases 0.000 claims 2
- 208000026139 Memory disease Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/65—One oxygen atom attached in position 3 or 5
-
- 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/28—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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Claims (15)
1. Smjesa polimorfa koja sadrži:
a. kristalni polimorf A (2S)-(4E)-N-metil-5-[3-(5-izopropoksipiridin)il]-4-penten-2-amin p-hidroksibenzoata, koji prikazuje obrazac rendgenske difrakcije praha sa karakterističnim maksimumima izraženim u stupnjevima (2-θ) od oko 7.6 i 15.2 i 19.7, i
b. kristalni polimorf B (2S)-(4E)-N-metil-5-[3-(5-izopropoksipiridin)il]-4-penten-2-amin p-hidroksibenzoata, koji prikazuje obrazac rendgenske difrakcije praha sa karakterističnim maksimumima izraženim u stupnjevima (2-θ) od oko 8.0, 9.6 i 16.1.
2. Smjesa, premazahtjevu 1, naznačena time što je relativan odnos polimorfa A prema polimorfu B između 5:95 i 95:5.
3. Smjesa, premazahtjevu 1, naznačena time što polimorf A ima obrazac rendgenske difrakcije praha koji je suštinski isti kao onaj prikazan u tablici 1.
[image]
4. Smjesa, premazahtjevu 1, naznačena time da polimorf B ima obrazac rendgenske difrakcije praha koji je suštinski isti kao onaj prikazan u tabeli 2.
[image]
5. Smjesa, prema bilo kojem od zahtjeva 1 do 4, za primjenu u terapiji.
6. Smjesa, prema zahtjevu 5, za primjenu u postupcima terapije poremećaja središnjeg živčanog sustava.
7. Smjesa, prema zahtjevu 6, naznačena time što je poremećaj izabran iz grupe poremećaja koja obuhvaća poremećaj pamćenja povezan sa starenjem, blagi kognitivni poremećaj, pre-senilnu demenciju (Alzheimerova bolest sa ranim početkom), senilnu demenciju (demencija Alzheimerovog tipa), demenciju sa Levijevim tijelima, vaskularnu demenciju, Alzheimerovu bolest, moždani udar, demenciju uvjetovana SIDA-om, poremećaj smanjene pažnje, deficit pažnje-hiperaktivni poremećaj, disleksiju, šizofreniju, šizofreniformni poremećaj i šizoafektivni poremećaj.
8. Smjesa, prema zahtjevu 6, naznačena time što je poremećaj izabran iz grupe poremećaja koja obuhvaća blagu do umjerenu demenciju Alzheimerovog tipa, poremećaj smanjene pažnje, blagi kognitivni poremećaj i poremećaj pamćenja povezan sa starenjem.
9. Farmaceutska kompozicija koja sadrži smjesu polimorfa A i B, prema bilo kojem od zahtjeva 1 do 4, i jedan ili više farmaceutski prihvatljivih razblaživača, pomoćnih supstanci i/ili inertnih nosača.
10. Farmaceutska kompozicija prema zahtjevu 9, za primjenu u terapiji.
11. Farmaceutska kompozicija prema zahtjevu 9, za primjenu u postupcima terapije poremećaja središnjeg živčanog sustava.
12. Farmaceutska kompozicija prema zahtjevu 11, naznačena time što je poremećaj izabran iz grupe poremećaja koja obuhvaća poremećaj pamćenja povezan sa starenjem, blagi kognitivni poremećaj, pre-senilnu demenciju (Alzheimerova bolest sa ranim početkom), senilnu demenciju (demenciju Alzheimerovog tipa), demenciju sa Levijevim tijelima, vaskularnu demenciju, Alzheimerovu bolest, moždani udar, demenciju uvjetovanu SIDA-om, poremećaj smanjene pažnje, deficit pažnje-hiperaktivni poremećaj, disleksiju, šizofreniju, šizofreniformni poremećaj i šizoafektivni poremećaj.
13. Farmaceutska kompozicija, prema zahtjevu 11, naznačena time što je poremećaj izabran iz grupe poremećaja koja obuhvaća blagu do umjerenu demenciju Alzheimerovog tipa, poremećaj smanjene pažnje, blagi kognitivni poremećaj i poremećaj pamćenja povezan sa starenjem.
14. Uporaba smjese, prema bilo kojem od zahtjeva 1 do 4, u proizvodnji lijekova za terapiju poremećaja središnjeg živčanog sustava.
15. Uporaba prema zahtjevu 14, naznačena time što je poremećaj izabran iz grupe poremećaja koja obuhvaća poremećaj pamćenja povezan sa starenjem, blagi kognitivni poremećaj, pre-senilnu demenciju (Alzheimerova bolest sa ranim početkom), senilnu demenciju (demencija Alzheimerovog tipa), demenciju sa Levijevim tijelima, vaskularnu demenciju, Alzheimerovu bolest, moždani udar, demenciju uvjetovanu SIDA-om, poremećaj smanjene pažnje, deficit pažnje-hiperaktivni poremećaj, disleksiju, šizofreniju, šizofreniformni poremećaj i šizoafektivni poremećaj.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74682106P | 2006-05-09 | 2006-05-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140385T1 true HRP20140385T1 (hr) | 2014-06-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140385TT HRP20140385T1 (hr) | 2006-05-09 | 2014-04-28 | Polimorfni oblici (2s)-(4e)-n-metil-5-[3-(5-izopropoksipiridin)il]-4-penten-2-amin p-hidroksibenzoata u terapiji poremeä†aja središnjeg živäśanog sustava |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US8461344B2 (hr) |
| EP (2) | EP2021326A1 (hr) |
| JP (1) | JP4477097B2 (hr) |
| KR (1) | KR20090005369A (hr) |
| CN (1) | CN101472893A (hr) |
| AR (1) | AR060786A1 (hr) |
| AU (1) | AU2007249485B2 (hr) |
| BR (1) | BRPI0709781A2 (hr) |
| CA (1) | CA2649961A1 (hr) |
| DK (1) | DK2418201T3 (hr) |
| EC (1) | ECSP088876A (hr) |
| ES (1) | ES2460919T3 (hr) |
| HR (1) | HRP20140385T1 (hr) |
| IL (1) | IL194833A0 (hr) |
| MX (1) | MX2008013982A (hr) |
| MY (1) | MY144132A (hr) |
| NO (1) | NO20084567L (hr) |
| NZ (1) | NZ597177A (hr) |
| PL (1) | PL2418201T3 (hr) |
| PT (1) | PT2418201E (hr) |
| RS (1) | RS53286B (hr) |
| RU (1) | RU2440984C2 (hr) |
| SA (1) | SA07280230B1 (hr) |
| SI (1) | SI2418201T1 (hr) |
| TW (1) | TWI389889B (hr) |
| UA (1) | UA96447C2 (hr) |
| UY (1) | UY30330A1 (hr) |
| WO (1) | WO2007134034A1 (hr) |
| ZA (1) | ZA200809284B (hr) |
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| US7459469B2 (en) | 2004-11-10 | 2008-12-02 | Targacept, Inc. | Hydroxybenzoate salts of metanicotine compounds |
| TWI389889B (zh) * | 2006-05-09 | 2013-03-21 | Targacept Inc | （２ｓ）-（４ｅ）-ｎ-甲基-５-〔３-（５-異丙氧基吡啶）基〕-４-戊烯-２-胺之新穎多晶型 |
| CN101528698A (zh) * | 2006-05-09 | 2009-09-09 | 阿斯利康公司 | (2s)-(4e)-n-甲基-5-[3-(5-异丙氧基吡啶)基]-4-戊烯-2-胺的盐形式 |
| AR062860A1 (es) * | 2006-09-15 | 2008-12-10 | Astrazeneca Ab | Combinaciones terapeuticas 482 |
| JP5502494B2 (ja) * | 2007-01-22 | 2014-05-28 | ターガセプト・インコーポレイテッド | メタニコチンアナログの鼻腔内、バッカル、または舌下投与 |
| AU2008282205A1 (en) * | 2007-07-31 | 2009-02-05 | Astrazeneca Ab | Transdermal administration of (2S)-(4E)-N-methyl-5-(3-( 5-isopropoxypyridin)yl)-4-penten-2-amine |
| CN102065845A (zh) * | 2008-06-11 | 2011-05-18 | 阿斯利康(瑞典)有限公司 | 含有(2s)-(4e)-n-甲基-5-(5-异丙氧基吡啶-3-基)-戊-4-烯-2-胺的舌下组合物 |
| WO2010080757A2 (en) * | 2009-01-07 | 2010-07-15 | Astrazeneca Ab | Combinations with an alpha-4beta-2 nicotinic agonist |
| FR2959107B1 (fr) | 2010-04-23 | 2015-03-27 | Oreal | Unite d'application d'un produit cosmetique |
| US8703802B2 (en) * | 2010-05-20 | 2014-04-22 | Targacept, Inc. | Process for the preparation of aryl substituted olefinic amines |
| WO2013184732A1 (en) * | 2012-06-06 | 2013-12-12 | Targacept, Inc. | Crystalline (2s)-(4e)-n-methyl-5-[3-(5-isopropoxypyridin)yl]4-penten-2-amine 1,5-naphthalenedisulfonate |
| KR101579904B1 (ko) | 2014-09-05 | 2016-01-05 | 동신대학교산학협력단 | 마스카라 |
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- 2007-05-07 UY UY30330A patent/UY30330A1/es not_active Application Discontinuation
- 2007-05-07 AR ARP070101972A patent/AR060786A1/es not_active Application Discontinuation
- 2007-05-08 EP EP07783431A patent/EP2021326A1/en not_active Withdrawn
- 2007-05-08 WO PCT/US2007/068446 patent/WO2007134034A1/en active Application Filing
- 2007-05-08 CN CNA2007800168072A patent/CN101472893A/zh active Pending
- 2007-05-08 US US11/745,682 patent/US8461344B2/en not_active Expired - Fee Related
- 2007-05-08 JP JP2009503340A patent/JP4477097B2/ja not_active Expired - Fee Related
- 2007-05-08 SA SA07280230A patent/SA07280230B1/ar unknown
- 2007-05-08 PL PL11167528T patent/PL2418201T3/pl unknown
- 2007-05-08 DK DK11167528.6T patent/DK2418201T3/da active
- 2007-05-08 CA CA002649961A patent/CA2649961A1/en not_active Abandoned
- 2007-05-08 AU AU2007249485A patent/AU2007249485B2/en not_active Ceased
- 2007-05-08 SI SI200731433T patent/SI2418201T1/sl unknown
- 2007-05-08 MX MX2008013982A patent/MX2008013982A/es active IP Right Grant
- 2007-05-08 BR BRPI0709781-6A patent/BRPI0709781A2/pt not_active IP Right Cessation
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- 2007-05-08 ES ES11167528.6T patent/ES2460919T3/es active Active
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- 2007-05-08 EP EP11167528.6A patent/EP2418201B1/en active Active
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- 2007-05-08 KR KR1020087027218A patent/KR20090005369A/ko active IP Right Grant
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- 2008-10-29 ZA ZA200809284A patent/ZA200809284B/xx unknown
- 2008-10-30 NO NO20084567A patent/NO20084567L/no not_active Application Discontinuation
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