HUE029324T2 - Egy MGLUR5 receptor antagonista polimorf formái - Google Patents
Egy MGLUR5 receptor antagonista polimorf formái Download PDFInfo
- Publication number
- HUE029324T2 HUE029324T2 HUE07857408A HUE07857408A HUE029324T2 HU E029324 T2 HUE029324 T2 HU E029324T2 HU E07857408 A HUE07857408 A HU E07857408A HU E07857408 A HUE07857408 A HU E07857408A HU E029324 T2 HUE029324 T2 HU E029324T2
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- HU
- Hungary
- Prior art keywords
- chloro
- imidazol
- dimethyl
- salt
- pyridine
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
- Az EP 2 125 779 iajstmmszámóeurópai szabadalom igénypontjainak fordítása: 1. t-Któr4-|1 “ΙΦΙυΡΓ^ηΙ^Ι,δ^ίΓηβΙίΙ-Ι Η-i m id ázol «44 letin slj-piridin monoszuifát sójának kristályos formája, amelyre jellemző legalább három csúcs a következő 20 (2fheta (fok)) értékeknél kapói röntgendifekclós csúcsok közül választva, Cur« sugárzás alkalmazása mellett: 9,8, 13,4,14,2, 18,1, 18,9, 19,6, 22,6, 22,9, 25,7,: 27s1 és 29,9 (±0,2° 2theta).
- 2. Az 1, igénypont szerinti 2-klór-4~j1444iyör“feníSh2,5«dlmeíil-1H-imfdazol~4- fetioilj-piridm moeoszeifát sójának kristályos formája, amelyre jellemzők a következő 29 (2thets (fok)} érteteknél kapott röntgendifrakciós csúcsok 0¾¾ sugárzás alkalmazása mellett: 9,3, 13,4, 14,2, 18,1, 18,9, 19,6, 22,8, 22,9, 25,7, 27,1 és 29,9 (±Q,2Ü 2theta).
- 3. Az 1 igénypert szerinti Mlén4«|1>|4^yor~fenil>2,5~dimefik1H4m1dlazol^4*· ileiml|-plridin monoszulfát sójának kristályos formája, amelyre jellemző egy infravörös spektrum, amely éles sávokkal rendelkezik a kővetkezőknél: 3068, 2738, 2618, 2236, 2213, 1828, 1587, 1569, 1518, 1384, 1374, 1298, 1238, 1188, 1157, 1116, 1064 1019, 902, 855, 788 és 674 cm"1 (éi cm'1}.
- 4. Az 1. igénypont szeóntí 2-klór-4-[1~(4-f!uor-fenil)-2,5-dimetil''1H~!mldazol-4- iiefiníllkpindtn monoszulfát sójának kristályos formája, amelyre jellemző legalább bárom csúcs a következő 2i |2theta (fok)) értékeknél kapott röntgendiffrakdós csúcsok közül választva, sugárzás alkalmazása mellett: 8,9, 10,2, 14,3, 14,7, 15,4,17,1,18,8,19,5, 20,9, 22,5 is 23,8 Ít0,2c 2theta). 5. Ä 4. igénypont szerinti 2'-klQr--4-[1-(4őluor-feníi)~2,5''dsmefil“1H»imíőazol-4~ lletinilj-pirídin monoszulfát sójának kdstályös formája, ajfpeïyre je jfimzők a követkézé 20 (2theta (fok)) értékeknél kapott rőntpendiffrakolós csúcsok Curö sugárzás alkalmazása mellett: 8,9, 10,2* 14,3, 14,7, 15,4, 17,1, 18,8, 19,5, 20,9, 22,5 és 23.8 (10,255 2theta). §♦ Az 1. igénypont szerinti 2- kló r~4~[1 ~(4~f íuor-fenii >2,5~d i m etil -1 Η-i m id azoí-4- lletinilj-pirsdin monoszuifát sójának kristályos formája, amelyre jellemző infravörös spektrum ppély éles sávokkal rendelkezik a kővetkezőknél: 3122, 3039, 3003, 2923, |Í63, 2719, 2808, 2231,1822, 1585, 1565,1515, 1439, 1373, 1346, 1224, 1158.
- 7, Az 1. Igénypont szerinti latinlj-pfrídiri monoszuifát sójának kristályos formája, ahol legalább 70% az 1-8. igénypontok bármelyike szerinti kristályos polimorf.
- 8. Gyógyszerészeti készítmény, amely tartalmazza az 1-8. Igénypontok szériái 2-któr~4-[1~f 4-fíuof^S30Í}-2,5“d!metii~i^ monoszulíai sójának kristályos formáját és egy vagy több gyógyszerészetiíeg elfogadható hordozót.
- 9. Eljárás az 1-6, Igénypontok bármelyike szerinti vegyüiat előállítására, amely tartalmazza a kővetkező lépéseket (a) 2~kjor~4-f 1~p-|yor~feo^^^ H~imldazoi~4-iletin:iij--piridin sójának képzése kénsavva! 2-propanolban azt követő spontán kiválással, vagy fbj az £aj lépés termékének átkristáíyosiása sætonstnlbem acetonítril/viz elegyében, metanolban, etanoíban, ízopropanoíban, ecetsavban, i-oktanolban vagy IPA/49% kénsav (10:1 v/v) eíegyében.
- 10, Az 1-8. igénypontok bármelyike szerinti 2-kiór-4-[1-(4iluor-fen:l}-2,5-'dimetii-1H4midazol~4iieintl]-piridin monoszufát sójának kristályos formája terápiásán hatásos anyagként történő alkalmazásra.
- 11, Az 1-6. Igénypontok bármelyike szerinti 2-klór-4-{1-(4-flüor-fenÍ!)-2:6-dímetll-1Η~^Ι03ζο1-·4'·ΙΙβΐ!ηΙ1]-ρΙη0Ιπ monoszulfát sója kristályos -formájának alkalmazása a következők alkotta csoportból választott rendellenességek kezelésére és/vagy megelőzésére szoigáfo gyógyszer előállítására: akut és/vagy krónikus neurológiai rendellenességek, különösen szorongás, vagy a következők kezelésére szolgáló gyógyszer előállításán; krónikus és akut fájdalom, védelem a máj gyógyszer vágy-betegség okozta károsodása, elégtelensége ellen,, vízeieíínkontinencia, elhízás, fragilis X vagy autizmus.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87639806P | 2006-12-21 | 2006-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUE029324T2 true HUE029324T2 (hu) | 2017-02-28 |
Family
ID=39186951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HUE07857408A HUE029324T2 (hu) | 2006-12-21 | 2007-12-11 | Egy MGLUR5 receptor antagonista polimorf formái |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8063076B2 (hu) |
| EP (1) | EP2125779B1 (hu) |
| JP (1) | JP5405311B2 (hu) |
| KR (1) | KR101148580B1 (hu) |
| CN (1) | CN101568531B (hu) |
| AR (1) | AR064654A1 (hu) |
| AU (1) | AU2007336369B2 (hu) |
| BR (1) | BRPI0720954A2 (hu) |
| CA (1) | CA2673444C (hu) |
| CL (1) | CL2007003695A1 (hu) |
| CO (1) | CO6210731A2 (hu) |
| CY (1) | CY1117810T1 (hu) |
| DK (1) | DK2125779T3 (hu) |
| EC (1) | ECSP099431A (hu) |
| ES (1) | ES2577391T3 (hu) |
| HR (1) | HRP20160950T1 (hu) |
| HU (1) | HUE029324T2 (hu) |
| IL (1) | IL199181A (hu) |
| MA (1) | MA31008B1 (hu) |
| MX (1) | MX2009006694A (hu) |
| MY (1) | MY148217A (hu) |
| NO (1) | NO342451B1 (hu) |
| NZ (1) | NZ577440A (hu) |
| PE (1) | PE20081484A1 (hu) |
| PL (1) | PL2125779T3 (hu) |
| PT (1) | PT2125779T (hu) |
| RS (1) | RS54853B1 (hu) |
| RU (1) | RU2460728C2 (hu) |
| SI (1) | SI2125779T1 (hu) |
| TW (1) | TWI347320B (hu) |
| UA (1) | UA96970C2 (hu) |
| WO (1) | WO2008074697A1 (hu) |
| ZA (1) | ZA200904289B (hu) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0720954A2 (pt) | 2006-12-21 | 2014-03-18 | Hoffmann La Roche | Polimorfos de um antagonista de receptor mglur5 |
| US20120039999A1 (en) * | 2010-08-11 | 2012-02-16 | Ashish Chatterji | Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists |
| AU2012232711B2 (en) | 2011-03-18 | 2016-04-28 | Novartis Ag | Combinations of alpha 7 nicotinic acetylcholine receptor activators and mGluR5 antagonists for use in dopamine induced dyskinesia in Parkinson's Disease |
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| GB201317022D0 (en) * | 2013-09-25 | 2013-11-06 | Addex Pharmaceuticals Sa | Polymorphs |
| CN114716555A (zh) | 2014-01-10 | 2022-07-08 | 博笛生物科技有限公司 | 靶向表达egfr的肿瘤的化合物和组合物 |
| CN115252792A (zh) | 2016-01-07 | 2022-11-01 | 博笛生物科技有限公司 | 用于***的抗-egfr组合 |
| CN108794467A (zh) | 2017-04-27 | 2018-11-13 | 博笛生物科技有限公司 | 2-氨基-喹啉衍生物 |
| MX2022015407A (es) | 2020-06-05 | 2023-05-16 | Noema Pharma Ag | Metodos de tratamiento del complejo de esclerosis tuberosa. |
| TW202220649A (zh) * | 2020-07-30 | 2022-06-01 | 瑞士商諾埃瑪製藥公司 | 三叉神經痛之治療方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3303199A (en) | 1963-07-15 | 1967-02-07 | Geigy Chem Corp | Certain imidazolone derivatives and process for making same |
| US3341548A (en) | 1964-04-29 | 1967-09-12 | Hoffmann La Roche | Nitroimidazoles and their preparation |
| DE2035905A1 (de) | 1970-07-20 | 1972-02-03 | Chemische Fabrik Stockhausen & Cie.,4150Krefeld | Imidazolverbindungen und deren Herstellungsverfahren |
| CA1174673A (en) | 1981-02-27 | 1984-09-18 | Walter Hunkeler | Imidazodiazepines |
| EP0079312A3 (de) | 1981-11-11 | 1984-04-25 | Ciba-Geigy Ag | Heterocyclische Acetylenverbindungen |
| US4711962A (en) | 1984-10-18 | 1987-12-08 | Stauffer Chemical Company | Process for selective preparation of ratios of isomers formed on N-substitution of asymmetric imidazoles |
| ATE134368T1 (de) | 1989-06-30 | 1996-03-15 | Du Pont | Substituierte imidazole und ihre verwendung als hemmmstoff fur angiotensin ii |
| TW544448B (en) | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| CN1154489C (zh) | 1997-08-14 | 2004-06-23 | 弗·哈夫曼-拉罗切有限公司 | 抗神经学疾病的杂环乙烯基醚 |
| JP4815083B2 (ja) | 1999-08-31 | 2011-11-16 | メルク・シャープ・エンド・ドーム・コーポレイション | 複素環化合物およびそれの使用方法 |
| JP5154728B2 (ja) | 2000-07-24 | 2013-02-27 | クレニツキー・ファーマシューティカルズ，インコーポレイテッド | 神経栄養活性を有する置換５−アルキニルピリミジン |
| CA2430696C (en) | 2000-12-04 | 2009-01-27 | F. Hoffmann-La Roche Ag | Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists |
| US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
| CA2470612A1 (en) | 2001-12-19 | 2003-07-03 | Merck & Co., Inc. | Heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5 |
| TWI292318B (en) | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| US7091222B2 (en) | 2003-07-03 | 2006-08-15 | Hoffmann-La Roche Inc. | Imidazole derivatives |
| US7452909B2 (en) | 2003-09-04 | 2008-11-18 | Hoffman-La Roche Inc. | Imidazole derivatives |
| DE602005007350D1 (de) * | 2004-06-01 | 2008-07-17 | Hoffmann La Roche | Pyridin-4-yl-ethynylimidazole und -pyrazole als antagonisten des mglu5-rezeptors |
| BRPI0720954A2 (pt) | 2006-12-21 | 2014-03-18 | Hoffmann La Roche | Polimorfos de um antagonista de receptor mglur5 |
-
2007
- 2007-12-11 BR BRPI0720954-1A patent/BRPI0720954A2/pt not_active Application Discontinuation
- 2007-12-11 DK DK07857408.4T patent/DK2125779T3/en active
- 2007-12-11 UA UAA200907474A patent/UA96970C2/ru unknown
- 2007-12-11 JP JP2009541986A patent/JP5405311B2/ja active Active
- 2007-12-11 CA CA2673444A patent/CA2673444C/en active Active
- 2007-12-11 RU RU2009123135/04A patent/RU2460728C2/ru active
- 2007-12-11 PT PT78574084T patent/PT2125779T/pt unknown
- 2007-12-11 AU AU2007336369A patent/AU2007336369B2/en active Active
- 2007-12-11 MY MYPI20092393A patent/MY148217A/en unknown
- 2007-12-11 SI SI200731792A patent/SI2125779T1/sl unknown
- 2007-12-11 EP EP07857408.4A patent/EP2125779B1/en active Active
- 2007-12-11 HU HUE07857408A patent/HUE029324T2/hu unknown
- 2007-12-11 CN CN2007800475969A patent/CN101568531B/zh active Active
- 2007-12-11 RS RS20160461A patent/RS54853B1/sr unknown
- 2007-12-11 WO PCT/EP2007/063721 patent/WO2008074697A1/en active Application Filing
- 2007-12-11 KR KR1020097012810A patent/KR101148580B1/ko active IP Right Grant
- 2007-12-11 PL PL07857408.4T patent/PL2125779T3/pl unknown
- 2007-12-11 NZ NZ577440A patent/NZ577440A/en unknown
- 2007-12-11 ES ES07857408.4T patent/ES2577391T3/es active Active
- 2007-12-11 MX MX2009006694A patent/MX2009006694A/es active IP Right Grant
- 2007-12-14 PE PE2007001802A patent/PE20081484A1/es not_active Application Discontinuation
- 2007-12-17 US US11/957,515 patent/US8063076B2/en active Active
- 2007-12-19 CL CL200703695A patent/CL2007003695A1/es unknown
- 2007-12-19 TW TW096148786A patent/TWI347320B/zh active
- 2007-12-21 AR ARP070105822A patent/AR064654A1/es not_active Application Discontinuation
-
2009
- 2009-06-04 IL IL199181A patent/IL199181A/en active IP Right Grant
- 2009-06-05 CO CO09058653A patent/CO6210731A2/es not_active Application Discontinuation
- 2009-06-15 EC EC2009009431A patent/ECSP099431A/es unknown
- 2009-06-17 MA MA32012A patent/MA31008B1/fr unknown
- 2009-06-18 ZA ZA200904289A patent/ZA200904289B/xx unknown
- 2009-06-19 NO NO20092357A patent/NO342451B1/no unknown
-
2011
- 2011-10-14 US US13/273,266 patent/US8329912B2/en active Active
-
2016
- 2016-07-19 CY CY20161100705T patent/CY1117810T1/el unknown
- 2016-07-26 HR HRP20160950TT patent/HRP20160950T1/hr unknown
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