CO6210731A2 - Polimorfos de un antagonista del receptor mglur5 - Google Patents

Polimorfos de un antagonista del receptor mglur5

Info

Publication number
CO6210731A2
CO6210731A2 CO09058653A CO09058653A CO6210731A2 CO 6210731 A2 CO6210731 A2 CO 6210731A2 CO 09058653 A CO09058653 A CO 09058653A CO 09058653 A CO09058653 A CO 09058653A CO 6210731 A2 CO6210731 A2 CO 6210731A2
Authority
CO
Colombia
Prior art keywords
imidazol
fluorophenyl
chloro
dimethyl
pyridine
Prior art date
Application number
CO09058653A
Other languages
English (en)
Inventor
Thomas P Cleary
Alexander Glomme
Olaf Grassmann
Shan-Ming Kuang
Roland Meier
Doreen Miller
Regina Moog
Franziska Rohrer
Jason Yang
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39186951&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO6210731(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CO6210731A2 publication Critical patent/CO6210731A2/es

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Classifications

    • 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
    • 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

Landscapes

  • 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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

1.- Una sal mono-sulfato de la 2-cloro-4-[1-(4-fluor- fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina. 2.- Una sal hemi-sulfato de la 2-cloro-4-[1-(4-fluor-fenil) -2,5-dimetil-1H-imidazol-4-iletinil] -piridina. 3.- Una forma cristalina de la sal mono-sulfato de la 2-cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina caracterizada por lo menos por tres picos elegidos entre los siguientes picos de difracción de rayos X obtenidos con una radiación Cuka a 2? (2-theta (grados) ) = 9,8, 13,4, 14,2, 18,1, 18,9, 19,6, 22,6, 22,9, 25,7, 27,1 y 29,9 (± 0 , 2° 2-theta). 4.- Una forma cristalina de la sal mono-sulfato de la 2-cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina caracterizada por los siguientes picos de difracción de rayos X obtenidos con una radiación Cuka a 2? (2-theta (grados)) = 9,8, 13,4, 14,2, 18,1, 18,9, 19,6, 22,6, 22,9, 25,7, 27,1 y 29,9 (± 0 , 2° 2-theta). 5.- Una forma cristalina de la sal mono-sulfato de la 2-cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina caracterizada por el modelo de difracción de rayos X del material en polvo representado en la figura 1. 6.- Una forma cristalina de la sal mono-sulfato de la 2-cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]-piridina según una cualquiera de las reivindicaciones 1 o de 3 a 5 caracterizada por un espectro infrarrojo que tiene bandas acusadas a 3068, 2730, 2618, 2236, 2213, 1628, 1587, 1569, 1518, 1384, 1374, 1295, 1236, 1168, 1157, 1116, 1064, 1019, 902, 855, 786 y 674 cm-1 (± 3 cm-1). 7.- Una forma cristalina de la sal mono-sulfato de la 2- cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]- piridina según una cualquiera de las reivindicaciones 1 o de 3 a 6 caracterizada por un espectro infrarrojo representado en la figura 2. 8.- Una forma cristalina de la sal mono-sulfato de la 2-cloro-4-[1-(4-fluor-fenil)-2,5-dimetil-1H-imidazol-4-iletinil]- piridina caracterizada por lo menos por tres picos elegidos entre los siguientes picos de difracción de rayos X obtenidos con una radiación Cuka a 2? (2-theta (grados)) = 8,9, 10,2, 14,3, 14,7, 15,4, 17,1, 18,8, 19,5, 20,9, 22,5 y 23,8 (± 0 , 2° theta).
CO09058653A 2006-12-21 2009-06-05 Polimorfos de un antagonista del receptor mglur5 CO6210731A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US87639806P 2006-12-21 2006-12-21

Publications (1)

Publication Number Publication Date
CO6210731A2 true CO6210731A2 (es) 2010-10-20

Family

ID=39186951

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09058653A CO6210731A2 (es) 2006-12-21 2009-06-05 Polimorfos de un antagonista del receptor mglur5

Country Status (33)

Country Link
US (2) US8063076B2 (es)
EP (1) EP2125779B1 (es)
JP (1) JP5405311B2 (es)
KR (1) KR101148580B1 (es)
CN (1) CN101568531B (es)
AR (1) AR064654A1 (es)
AU (1) AU2007336369B2 (es)
BR (1) BRPI0720954A2 (es)
CA (1) CA2673444C (es)
CL (1) CL2007003695A1 (es)
CO (1) CO6210731A2 (es)
CY (1) CY1117810T1 (es)
DK (1) DK2125779T3 (es)
EC (1) ECSP099431A (es)
ES (1) ES2577391T3 (es)
HR (1) HRP20160950T1 (es)
HU (1) HUE029324T2 (es)
IL (1) IL199181A (es)
MA (1) MA31008B1 (es)
MX (1) MX2009006694A (es)
MY (1) MY148217A (es)
NO (1) NO342451B1 (es)
NZ (1) NZ577440A (es)
PE (1) PE20081484A1 (es)
PL (1) PL2125779T3 (es)
PT (1) PT2125779T (es)
RS (1) RS54853B1 (es)
RU (1) RU2460728C2 (es)
SI (1) SI2125779T1 (es)
TW (1) TWI347320B (es)
UA (1) UA96970C2 (es)
WO (1) WO2008074697A1 (es)
ZA (1) ZA200904289B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ577440A (en) 2006-12-21 2011-12-22 Hoffmann La Roche Polymorphs of a mglur5 receptor antagonist
US20120039999A1 (en) * 2010-08-11 2012-02-16 Ashish Chatterji Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists
CA2830458A1 (en) 2011-03-18 2012-09-27 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
CN105899539B (zh) 2014-01-10 2021-11-09 博笛生物科技有限公司 用于免疫疗法的化合物和组合物
CN106943597A (zh) 2016-01-07 2017-07-14 博笛生物科技（北京）有限公司 用于治疗肿瘤的抗-egfr组合
CN118515666A (zh) 2017-04-27 2024-08-20 博笛生物科技有限公司 2-氨基-喹啉衍生物
KR20230027145A (ko) 2020-06-05 2023-02-27 노에마 파르마 아게 결절성 경화증 복합증의 치료 방법
JP2023540849A (ja) * 2020-07-30 2023-09-27 ノエマ ファーマ アクツィエンゲゼルシャフト 三叉神経痛の治療方法

Family Cites Families (20)

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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
US4508560A (en) 1981-11-11 1985-04-02 Ciba Geigy Corporation Certain pyridylacetylene compounds, compositions containing same and herbicidal methods of use
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
DE69025473T2 (de) 1989-06-30 1996-10-17 Du Pont Substituierte imidazole und ihre verwendung als hemmmstoff fur angiotensin ii
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
NZ502463A (en) 1997-08-14 2002-05-31 F 1-Phenyl vinyl substituted imidazole, triazole or tetrazole derivatives useful for controlling or preventing acute or chronic neurological disorders
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
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WO2002046166A1 (en) 2000-12-04 2002-06-13 F. Hoffmann-La Roche Ag Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists
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JP2005516950A (ja) 2001-12-19 2005-06-09 メルク　エンド　カムパニー　インコーポレーテッド 代謝型グルタミン酸受容体−５のヘテロアリール置換イミダゾールモジュレータ
TWI292318B (en) 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
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NZ577440A (en) 2006-12-21 2011-12-22 Hoffmann La Roche Polymorphs of a mglur5 receptor antagonist

Also Published As

Publication number Publication date
WO2008074697A1 (en) 2008-06-26
RU2460728C2 (ru) 2012-09-10
PT2125779T (pt) 2016-07-19
HRP20160950T1 (hr) 2016-10-07
BRPI0720954A2 (pt) 2014-03-18
JP2010513378A (ja) 2010-04-30
DK2125779T3 (en) 2016-07-04
IL199181A (en) 2016-02-29
HUE029324T2 (en) 2017-02-28
US20080312288A1 (en) 2008-12-18
ES2577391T3 (es) 2016-07-14
TWI347320B (en) 2011-08-21
CL2007003695A1 (es) 2008-07-04
US20120035222A1 (en) 2012-02-09
CA2673444A1 (en) 2008-06-26
ECSP099431A (es) 2009-07-31
AU2007336369A1 (en) 2008-06-26
AR064654A1 (es) 2009-04-15
AU2007336369B2 (en) 2013-01-17
PL2125779T3 (pl) 2016-11-30
CY1117810T1 (el) 2017-05-17
EP2125779A1 (en) 2009-12-02
TW200833679A (en) 2008-08-16
CN101568531A (zh) 2009-10-28
NO20092357L (no) 2009-07-15
JP5405311B2 (ja) 2014-02-05
CA2673444C (en) 2015-01-20
RS54853B1 (sr) 2016-10-31
ZA200904289B (en) 2010-04-28
US8063076B2 (en) 2011-11-22
KR20090081026A (ko) 2009-07-27
MA31008B1 (fr) 2009-12-01
MY148217A (en) 2013-03-29
SI2125779T1 (sl) 2016-07-29
CN101568531B (zh) 2013-11-13
RU2009123135A (ru) 2011-01-27
PE20081484A1 (es) 2008-10-18
EP2125779B1 (en) 2016-04-27
KR101148580B1 (ko) 2012-05-24
MX2009006694A (es) 2009-06-30
NO342451B1 (no) 2018-05-22
US8329912B2 (en) 2012-12-11
NZ577440A (en) 2011-12-22
UA96970C2 (en) 2011-12-26

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