ZA200509807B - Imidazole derivatives as glutamate receptor antagonists - Google Patents

Imidazole derivatives as glutamate receptor antagonists Download PDF

Info

Publication number: ZA200509807B
Authority: ZA; South Africa
Prior art keywords: compound; formula; methyl; chloro; pyridine
Prior art date: 2003-06-05

Application number

ZA200509807A

Other languages

English (en)

Inventor

Buettelmann Bernd

Jaeschke Georg

Vieira Eric

Ceccarelli Simona Maria

Porter Richard Hugh Philip

Kolczewski Sabine

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.)

2003-06-05

Filing date

2005-12-02

Publication date

2006-12-27

2005-12-02 Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche

2006-12-27 Publication of ZA200509807B publication Critical patent/ZA200509807B/en

Links

239000003825 glutamate receptor antagonist Substances 0.000 title description 3
150000002460 imidazoles Chemical class 0.000 title description 3
229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title description 3
150000001875 compounds Chemical class 0.000 claims description 172
JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 39
150000003839 salts Chemical class 0.000 claims description 32
238000000034 method Methods 0.000 claims description 30
229910052736 halogen Inorganic materials 0.000 claims description 25
125000000217 alkyl group Chemical group 0.000 claims description 23
239000000203 mixture Substances 0.000 claims description 23
150000002367 halogens Chemical class 0.000 claims description 20
239000003814 drug Substances 0.000 claims description 17
208000002193 Pain Diseases 0.000 claims description 16
239000001257 hydrogen Substances 0.000 claims description 15
229910052739 hydrogen Inorganic materials 0.000 claims description 15
230000001684 chronic effect Effects 0.000 claims description 14
230000002265 prevention Effects 0.000 claims description 14
125000003118 aryl group Chemical group 0.000 claims description 13
238000004519 manufacturing process Methods 0.000 claims description 12
239000000126 substance Substances 0.000 claims description 12
230000001154 acute effect Effects 0.000 claims description 11
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230000036506 anxiety Effects 0.000 claims description 10
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
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108020003175 receptors Proteins 0.000 claims description 10
238000007792 addition Methods 0.000 claims description 9
125000001072 heteroaryl group Chemical group 0.000 claims description 9
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239000002253 acid Substances 0.000 claims description 8
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230000001404 mediated effect Effects 0.000 claims description 8
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125000004093 cyano group Chemical group *C#N 0.000 claims description 6
125000001153 fluoro group Chemical group F* 0.000 claims description 6
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125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
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125000003545 alkoxy group Chemical group 0.000 claims description 4
125000001309 chloro group Chemical group Cl* 0.000 claims description 4
125000000753 cycloalkyl group Chemical group 0.000 claims description 4
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239000000546 pharmaceutical excipient Substances 0.000 claims description 4
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125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
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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
- C07D401/14—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 three or more hetero rings

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Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

ZA200509807A 2003-06-05 2005-12-02 Imidazole derivatives as glutamate receptor antagonists ZA200509807B (en)

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EP03012200		2003-06-05

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ZA200609681A ZA200609681B (en)	2003-06-05	2006-11-21	Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mGlu5 receptor antagonists

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EP (1)	EP1636206B1 (sr)
JP (1)	JP4401384B2 (sr)
KR (1)	KR100778948B1 (sr)
CN (1)	CN100408572C (sr)
AR (1)	AR044478A1 (sr)
AT (1)	ATE377008T1 (sr)
AU (1)	AU2004245208B2 (sr)
BR (1)	BRPI0411095B8 (sr)
CA (1)	CA2527315C (sr)
CL (1)	CL2004001347A1 (sr)
CR (1)	CR8094A (sr)
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DE (1)	DE602004009796T2 (sr)
DK (1)	DK1636206T3 (sr)
EA (1)	EA010577B1 (sr)
EC (1)	ECSP056202A (sr)
ES (1)	ES2294504T3 (sr)
GT (1)	GT200400117A (sr)
HN (1)	HN2004000208A (sr)
HR (1)	HRP20070529T3 (sr)
IL (1)	IL171930A (sr)
MA (1)	MA27881A1 (sr)
MX (1)	MXPA05013149A (sr)
MY (2)	MY137272A (sr)
NO (1)	NO332143B1 (sr)
NZ (1)	NZ543637A (sr)
PA (1)	PA8604101A1 (sr)
PE (1)	PE20050162A1 (sr)
PL (1)	PL1636206T3 (sr)
PT (1)	PT1636206E (sr)
RS (1)	RS53183B (sr)
SI (1)	SI1636206T1 (sr)
TN (2)	TNSN05309A1 (sr)
TW (1)	TWI338007B (sr)
UA (1)	UA80888C2 (sr)
WO (1)	WO2004108701A1 (sr)
ZA (2)	ZA200509807B (sr)

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US7531529B2 (en)	2003-06-05	2009-05-12	Roche Palo Alto Llc	Imidazole derivatives
UA80888C2 (en) *	2003-06-05	2007-11-12	Hoffmann La Roche	Imidazole derivatives as glutmate receptor antagonists
US7452909B2 (en)	2003-09-04	2008-11-18	Hoffman-La Roche Inc.	Imidazole derivatives
NZ551253A (en)	2004-06-01	2010-07-30	Hoffmann La Roche	Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as MGLU5 receptor antagonists
GB0514296D0 (en) *	2005-07-12	2005-08-17	Novartis Ag	Organic compounds
DE102006011574A1 (de)	2006-03-10	2007-10-31	Grünenthal GmbH	Substituierte Imidazo[2,1-b]thiazol-Verbindungen und ihre Verwendung zur Herstellung von Arzneimitteln
MY148217A (en) *	2006-12-21	2013-03-29	Hoffmann La Roche	Polymorphs of a mglur5 receptor antagonist
US8334287B2 (en) *	2009-07-17	2012-12-18	Hoffmann-La Roche Inc.	Imidazoles
US20120039999A1 (en) *	2010-08-11	2012-02-16	Ashish Chatterji	Pharmaceutical compositions of metabotropic glutamate 5 receptor (mglu5) antagonists
US20120040008A1 (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
MY171517A (en) *	2012-10-18	2019-10-16	Hoffmann La Roche	Ethynyl derivatives as modulators of mglur5 receptor activity
WO2014060398A1 (en) *	2012-10-18	2014-04-24	F. Hoffmann-La Roche Ag	Ethynyl derivatives as modulators of mglur5 receptor activity
EP3436009B1 (en) *	2016-03-30	2024-03-06	Sinntaxis AB	Negative allosteric modulators of mglur5 for use in the treatment of mature brain damages.
EP4069685A1 (en) *	2019-12-02	2022-10-12	F. Hoffmann-La Roche AG	Alkynyl-(heteroaryl)-carboxamide hcn1 inhibitors
BR112022024760A2 (pt)	2020-06-05	2023-03-07	Noema Pharma Ag	Métodos de tratamento do complexo de esclerose tuberosa
BR112023001621A2 (pt) *	2020-07-30	2023-04-04	Noema Pharma Ag	Métodos de tratamento de neuralgia trigeminal
EP4658268A1 (en)	2023-02-02	2025-12-10	Noema Pharma AG	Methods of treatment of dravet syndrome

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US4508560A (en)	1981-11-11	1985-04-02	Ciba Geigy Corporation	Certain pyridylacetylene compounds, compositions containing same and herbicidal methods of use
TW544448B (en) *	1997-07-11	2003-08-01	Novartis Ag	Pyridine derivatives
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
WO2002046166A1 (en)	2000-12-04	2002-06-13	F. Hoffmann-La Roche Ag	Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists
WO2003053922A2 (en) *	2001-12-19	2003-07-03	Merck & Co., Inc.	Heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5
JP2006513996A (ja) *	2002-10-24	2006-04-27	メルク　エンド　カムパニー　インコーポレーテッド	代謝調節型グルタミン酸受容体結合用トレーサーとしてのアルキン誘導体
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

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- 2004-06-02 US US10/858,969 patent/US7332510B2/en not_active Expired - Lifetime
- 2004-06-02 PA PA20048604101A patent/PA8604101A1/es unknown
- 2004-06-02 TW TW093115811A patent/TWI338007B/zh not_active IP Right Cessation
- 2004-06-02 PE PE2004000558A patent/PE20050162A1/es active IP Right Grant
- 2004-06-03 GT GT200400117A patent/GT200400117A/es unknown
- 2004-06-03 AR ARP040101908A patent/AR044478A1/es active IP Right Grant
- 2004-06-03 MY MYPI20042150A patent/MY137272A/en unknown
- 2004-06-03 HN HN2004000208A patent/HN2004000208A/es unknown
2005
- 2005-05-27 MY MYPI20052424A patent/MY143353A/en unknown
- 2005-11-13 IL IL171930A patent/IL171930A/en active IP Right Grant
- 2005-11-14 CR CR8094A patent/CR8094A/es unknown
- 2005-11-18 NO NO20055465A patent/NO332143B1/no unknown
- 2005-12-01 TN TNP2005000309A patent/TNSN05309A1/fr unknown
- 2005-12-02 EC EC2005006202A patent/ECSP056202A/es unknown
- 2005-12-02 ZA ZA200509807A patent/ZA200509807B/en unknown
- 2005-12-09 MA MA28648A patent/MA27881A1/fr unknown
2006
- 2006-11-21 ZA ZA200609681A patent/ZA200609681B/xx unknown
- 2006-11-27 TN TNP2006000391A patent/TNSN06391A1/fr unknown
2007
- 2007-10-31 US US11/930,258 patent/US8481548B2/en active Active
- 2007-12-13 US US11/955,421 patent/US7973165B2/en not_active Expired - Lifetime
2008
- 2008-01-11 CY CY20081100047T patent/CY1107856T1/el unknown

Also Published As

Publication number	Publication date
CY1107856T1 (el)	2013-06-19
TNSN06391A1 (fr)	2008-02-22
HK1093070A1 (zh)	2007-02-23
TWI338007B (en)	2011-03-01
US8481548B2 (en)	2013-07-09
CA2527315A1 (en)	2004-12-16
PE20050162A1 (es)	2005-03-22
MA27881A1 (fr)	2006-05-02
HRP20070529T3 (hr)	2008-05-31
SI1636206T1 (sl)	2008-02-29
US20040248888A1 (en)	2004-12-09
ECSP056202A (es)	2006-04-19
EA200501887A1 (ru)	2006-10-27
BRPI0411095A (pt)	2006-07-18
EA010577B1 (ru)	2008-10-30
IL171930A (en)	2010-12-30
DE602004009796T2 (de)	2008-08-28
UA80888C2 (en)	2007-11-12
BRPI0411095B1 (pt)	2018-04-03
MY143353A (en)	2011-04-29
RS53183B (sr)	2014-06-30
DE602004009796D1 (de)	2007-12-13
CN1802367A (zh)	2006-07-12
AR044478A1 (es)	2005-09-14
KR100778948B1 (ko)	2007-11-28
BRPI0411095B8 (pt)	2021-05-25
ATE377008T1 (de)	2007-11-15
NO332143B1 (no)	2012-07-02
PL1636206T3 (pl)	2008-04-30
ES2294504T3 (es)	2008-04-01
AU2004245208B2 (en)	2007-04-26
US7973165B2 (en)	2011-07-05
EP1636206A1 (en)	2006-03-22
GT200400117A (es)	2005-02-07
IL171930A0 (en)	2006-04-10
TW200509920A (en)	2005-03-16
HN2004000208A (es)	2009-02-03
EP1636206B1 (en)	2007-10-31
MY137272A (en)	2009-01-30
PT1636206E (pt)	2008-01-28
NZ543637A (en)	2008-04-30
RS20050892A (sr)	2007-12-31
WO2004108701A1 (en)	2004-12-16
NO20055465L (no)	2005-11-18
CA2527315C (en)	2010-08-10
JP4401384B2 (ja)	2010-01-20
PA8604101A1 (es)	2004-12-16
JP2006526588A (ja)	2006-11-24
US20080119489A1 (en)	2008-05-22
CR8094A (es)	2006-05-30
US7332510B2 (en)	2008-02-19
CL2004001347A1 (es)	2005-05-06
DK1636206T3 (da)	2008-02-11
ZA200609681B (en)	2008-06-25
KR20060057537A (ko)	2006-05-26
US20080103306A1 (en)	2008-05-01
TNSN05309A1 (fr)	2007-07-10
CN100408572C (zh)	2008-08-06
AU2004245208A1 (en)	2004-12-16
MXPA05013149A (es)	2006-03-17

Publication	Publication Date	Title
US7973165B2 (en)	2011-07-05	Imidazole derivatives
AU2004220382B2 (en)	2007-08-02	Imidazol-4-yl-ethynyl-pyridine derivatives
CA2537826C (en)	2012-04-17	Imidazole derivatives
JP4690395B2 (ja)	2011-06-01	ｍＧｌｕ５レセプターアンタゴニストとしてのピリジン−４−エチニル−イミダゾール及びピラゾール
AU2004247368B2 (en)	2007-11-22	Heteroaryl-substituted imidazole derivatives as glutamate receptor antagonists
CA2531210C (en)	2012-05-29	Imidazole derivatives and their use in the treatment of mglur5 receptor mediated disorders
HK1093070B (en)	2009-01-23	Imidazole derivatives as glutamate receptor antagonists