HRP20120733T1 - Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, njezini kristalni oblici, njihovo dobivanje i upotreba u terapiji - Google Patents
Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, njezini kristalni oblici, njihovo dobivanje i upotreba u terapiji Download PDFInfo
- Publication number
- HRP20120733T1 HRP20120733T1 HRP20120733AT HRP20120733T HRP20120733T1 HR P20120733 T1 HRP20120733 T1 HR P20120733T1 HR P20120733A T HRP20120733A T HR P20120733AT HR P20120733 T HRP20120733 T HR P20120733T HR P20120733 T1 HRP20120733 T1 HR P20120733T1
- Authority
- HR
- Croatia
- Prior art keywords
- nonane
- carboxylate
- bromophenyl
- diazabicyclo
- fumarate salt
- Prior art date
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- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 title claims 17
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 title 1
- RXLOZRCLQMJJLC-UHFFFAOYSA-N ssr-180,711 Chemical compound C1=CC(Br)=CC=C1OC(=O)N1C(CC2)CCN2CC1 RXLOZRCLQMJJLC-UHFFFAOYSA-N 0.000 claims 13
- 239000003814 drug Substances 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 238000010521 absorption reaction Methods 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000002329 infrared spectrum Methods 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- -1 2,4-dibromophenyl-1,4-diazabicyclo[3.2.2]nonane-4-carboxylate Chemical compound 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims 1
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
Classifications
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/24—Antidepressants
-
- 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
- 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
- A61P25/34—Tobacco-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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (14)
1. Spoj, naznačen time što je fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata.
2. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 1, naznačena time što je u obliku kristalnog polimorfa I, čiji difraktogram rendgenskih zraka na prahu sadrži najmanje tri od sljedećih karakterističnih linija:
[image]
3. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 2, naznačena time što joj infracrveni spektar pokazuje najmanje tri od sljedećih karakterističnih apsorpcijskih vrpci:
[image]
4. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 2, naznačena time što joj je talište 176 °C ± 2 °C, te čija srednja vrijednost entalpije je 107 J/g ± 2 J/g.
5. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 1, naznačena time što je u obliku kristalnog polimorfa II, čiji difraktogram rendgenskih zraka na prahu sadrži najmanje tri od sljedećih karakterističnih linija:
[image]
6. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 5, naznačena time što joj infracrveni spektar pokazuje najmanje tri od sljedećih karakterističnih apsorpcijskih vrpci:
[image]
7. Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u skladu s patentnim zahtjevom 5, naznačena time što joj je talište 175 °C ± 2 °C, te čija srednja vrijednost entalpije je 109 J/g ± 2 J/g.
8. Postupak dobivanja fumaratne soli 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, oblik I, naznačen time što 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilat u obliku slobodne baze reagira s fumarnom kiselinom u otapalu.
9. Postupak dobivanja fumaratne soli 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, oblik II, naznačen time što fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, oblik I, se stavlja u kontakt s fumaratnom solju 2,4-dibromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata u otapalu.
10. Medikament, naznačen time što sadrži fumaratnu sol 4-bromfenil 1,4-diazabiciklo[3.2.2]nonan4-karboksilata.
11. Farmaceutski pripravak, naznačen time što kao aktivnu tvar sadrži fumaratnu sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, a također i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
12. Upotreba fumaratne soli 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, naznačena time što je navedena sol namijenjena pripravi medikamenta namijenjenog liječenju ili sprječavanju poremećaja povezanih s disfunkcijom nikotinskih receptora.
13. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što je namijenjena pripravi medikamenta namijenjenog liječenju ili sprječavanju poremećaja radnih funkcija povezanih s Alzheimerovom bolešću.
14. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što je namijenjena pripravi medikamenta namijenjenog liječenju ili sprječavanju kognitivnog poremećaja povezanog sa shizofrenijom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0802995A FR2931823B1 (fr) | 2008-06-02 | 2008-06-02 | Sel de fumarate du 1,4-diazabicyclo°3.2.2!nonane-carboxylate de 4-bromophenyle, ses formes cristallines, leur preparation et leur utilisation en therapeutique |
PCT/FR2009/051039 WO2009156678A2 (fr) | 2008-06-02 | 2009-06-02 | Sel de fumarate du 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate de 4-bromophenyle, ses formes cristallines, leur préparation et leur utilisation en therapeutique |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120733T1 true HRP20120733T1 (hr) | 2012-10-31 |
Family
ID=40254482
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120733AT HRP20120733T1 (hr) | 2008-06-02 | 2012-09-13 | Fumaratna sol 4-bromfenil-1,4-diazabiciklo[3.2.2]nonan-4-karboksilata, njezini kristalni oblici, njihovo dobivanje i upotreba u terapiji |
Country Status (12)
Country | Link |
---|---|
US (1) | US8569289B2 (hr) |
EP (1) | EP2300473B1 (hr) |
JP (1) | JP2011522016A (hr) |
CY (1) | CY1113134T1 (hr) |
DK (1) | DK2300473T3 (hr) |
ES (1) | ES2389589T3 (hr) |
FR (1) | FR2931823B1 (hr) |
HR (1) | HRP20120733T1 (hr) |
PL (1) | PL2300473T3 (hr) |
PT (1) | PT2300473E (hr) |
SI (1) | SI2300473T1 (hr) |
WO (1) | WO2009156678A2 (hr) |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2791678B1 (fr) | 1999-03-30 | 2001-05-04 | Synthelabo | Derives de 1,4-diazabicyclo [3.2.2] nonane-4-carboxylates et -carboxamides, leur preparation et leur application en therapeutique |
ES2275808T3 (es) * | 2001-02-06 | 2007-06-16 | Pfizer Products Inc. | Composiciones farmaceuticas para el tratamiento de trastornos del snc y otros trastornos. |
EP1987033B1 (en) * | 2006-02-14 | 2010-08-25 | NeuroSearch A/S | Diazabicycloalkane derivatives and their medical use |
US7589076B2 (en) | 2006-05-18 | 2009-09-15 | Pgx Health, Llc | Substituted aryl piperidinylalkynyladenosines as A2AR agonists |
-
2008
- 2008-06-02 FR FR0802995A patent/FR2931823B1/fr not_active Expired - Fee Related
-
2009
- 2009-06-02 WO PCT/FR2009/051039 patent/WO2009156678A2/fr active Application Filing
- 2009-06-02 JP JP2011512184A patent/JP2011522016A/ja active Pending
- 2009-06-02 PL PL09769519T patent/PL2300473T3/pl unknown
- 2009-06-02 PT PT09769519T patent/PT2300473E/pt unknown
- 2009-06-02 SI SI200930332T patent/SI2300473T1/sl unknown
- 2009-06-02 ES ES09769519T patent/ES2389589T3/es active Active
- 2009-06-02 EP EP09769519A patent/EP2300473B1/fr active Active
- 2009-06-02 DK DK09769519.1T patent/DK2300473T3/da active
-
2010
- 2010-12-01 US US12/958,016 patent/US8569289B2/en active Active
-
2012
- 2012-09-13 HR HRP20120733AT patent/HRP20120733T1/hr unknown
- 2012-09-20 CY CY20121100865T patent/CY1113134T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
JP2011522016A (ja) | 2011-07-28 |
WO2009156678A2 (fr) | 2009-12-30 |
DK2300473T3 (da) | 2012-10-01 |
PL2300473T3 (pl) | 2012-11-30 |
US20110130389A1 (en) | 2011-06-02 |
ES2389589T3 (es) | 2012-10-29 |
WO2009156678A3 (fr) | 2010-05-14 |
FR2931823A1 (fr) | 2009-12-04 |
FR2931823B1 (fr) | 2012-08-17 |
PT2300473E (pt) | 2012-09-11 |
EP2300473A2 (fr) | 2011-03-30 |
SI2300473T1 (sl) | 2012-10-30 |
US8569289B2 (en) | 2013-10-29 |
CY1113134T1 (el) | 2016-04-13 |
EP2300473B1 (fr) | 2012-06-20 |
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