BG108166A - Imidazo-pyrimidine derivatives as liigands for gaba receptors - Google Patents

Imidazo-pyrimidine derivatives as liigands for gaba receptors

Info

Publication number: BG108166A
Authority: BG; Bulgaria
Prior art keywords: pyrimidine derivatives; liigands; imidazo; substituted; phenyl ring
Prior art date: 2001-03-21

Application number

BG108166A

Other languages

Bulgarian (bg)

English (en)

Inventor

Mark S. Chambers

Simon C. Goodacre

David J. Hallett

Andrew Jennings

Philip Jones

Richard T. Lewis

Kevin W. Moore

Leslie J. Street

Helen J. Szekeres

Original Assignee

Merck Sharp & Dohme Limited

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.)

2001-03-21

Filing date

2003-09-09

Publication date

2004-09-30

2001-03-21 Priority claimed from GB0107134A external-priority patent/GB0107134D0/en

2001-11-21 Priority claimed from GB0127938A external-priority patent/GB0127938D0/en

2003-09-09 Application filed by Merck Sharp & Dohme Limited filed Critical Merck Sharp & Dohme Limited

2004-09-30 Publication of BG108166A publication Critical patent/BG108166A/xx

Links

102000005915 GABA Receptors Human genes 0.000 title 1
108010005551 GABA Receptors Proteins 0.000 title 1
150000005237 imidazopyrimidines Chemical class 0.000 title 1
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
XKTONDZDILVOOL-UHFFFAOYSA-N 3-phenylimidazo[1,2-a]pyrimidine Chemical class C=1N=C2N=CC=CN2C=1C1=CC=CC=C1 XKTONDZDILVOOL-UHFFFAOYSA-N 0.000 abstract 1
208000019901 Anxiety disease Diseases 0.000 abstract 1
206010010904 Convulsion Diseases 0.000 abstract 1
102000027484 GABAA receptors Human genes 0.000 abstract 1
108091008681 GABAA receptors Proteins 0.000 abstract 1
230000002411 adverse Effects 0.000 abstract 1
230000036506 anxiety Effects 0.000 abstract 1
210000003169 central nervous system Anatomy 0.000 abstract 1
208000010877 cognitive disease Diseases 0.000 abstract 1
230000036461 convulsion Effects 0.000 abstract 1
125000001153 fluoro group Chemical group F* 0.000 abstract 1
125000001072 heteroaryl group Chemical group 0.000 abstract 1
239000003446 ligand Substances 0.000 abstract 1
230000002265 prevention Effects 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
- 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
- A61P25/06—Antimigraine agents
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
- 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
- A61P25/22—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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
- 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
- A61P39/00—General protective or antinoxious 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
- 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

Landscapes

Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
General Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Urology & Nephrology (AREA)
Hospice & Palliative Care (AREA)
Addiction (AREA)
Heart & Thoracic Surgery (AREA)
Rheumatology (AREA)
Cardiology (AREA)
Vascular Medicine (AREA)
Toxicology (AREA)
Otolaryngology (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

BG108166A 2001-03-21 2003-09-09 Imidazo-pyrimidine derivatives as liigands for gaba receptors BG108166A (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GB0107134A GB0107134D0 (en)	2001-03-21	2001-03-21	Therapeutic agents
GB0127938A GB0127938D0 (en)	2001-11-21	2001-11-21	Therapeutic agents
PCT/GB2002/001351 WO2002074772A1 (en)	2001-03-21	2002-03-19	Imidazo-pyrimidine derivatives as ligands for gaba receptors

Publications (1)

Publication Number	Publication Date
BG108166A true BG108166A (en)	2004-09-30

Family

ID=26245875

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
BG108166A BG108166A (en)	2001-03-21	2003-09-09	Imidazo-pyrimidine derivatives as liigands for gaba receptors

Country Status (24)

Country	Link
EP (1)	EP1381606B1 (cs)
JP (1)	JP4409174B2 (cs)
KR (1)	KR20030083001A (cs)
CN (1)	CN1294133C (cs)
AT (1)	ATE299882T1 (cs)
AU (1)	AU2002241138B2 (cs)
BG (1)	BG108166A (cs)
BR (1)	BR0207994A (cs)
CA (1)	CA2461426C (cs)
CZ (1)	CZ20032539A3 (cs)
DE (1)	DE60205101T2 (cs)
EA (1)	EA006234B1 (cs)
EE (1)	EE200300455A (cs)
ES (1)	ES2244752T3 (cs)
HU (1)	HUP0303630A3 (cs)
IL (1)	IL157641A0 (cs)
MX (1)	MXPA03008572A (cs)
NO (1)	NO20034170L (cs)
NZ (1)	NZ527901A (cs)
PE (1)	PE20020970A1 (cs)
PL (1)	PL363804A1 (cs)
SK (1)	SK11672003A3 (cs)
TW (1)	TWI248936B (cs)
WO (2)	WO2002074772A1 (cs)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB0117277D0 (en)	2001-07-16	2001-09-05	Merck Sharp & Dohme	Therapeutic agents
GB0128499D0 (en) *	2001-11-28	2002-01-23	Merck Sharp & Dohme	Therapeutic agents
GB0226462D0 (en) *	2002-11-13	2002-12-18	Merck Sharp & Dohme	Therapeutic agents
ATE350382T1 (de) *	2003-07-25	2007-01-15	Neurogen Corp	Imidazopyrimidine und triazolopyrimidine: benzodiazepinrezeptorliganden
JP5442449B2 (ja)	2006-12-22	2014-03-12	アステックス、セラピューティックス、リミテッド	新規化合物
CN101679408B (zh)	2006-12-22	2016-04-27	Astex治疗学有限公司	作为fgfr抑制剂的双环杂环化合物
GB0720041D0 (en)	2007-10-12	2007-11-21	Astex Therapeutics Ltd	New Compounds
GB0720038D0 (en)	2007-10-12	2007-11-21	Astex Therapeutics Ltd	New compounds
GB0810902D0 (en)	2008-06-13	2008-07-23	Astex Therapeutics Ltd	New compounds
GB0906472D0 (en)	2009-04-15	2009-05-20	Astex Therapeutics Ltd	New compounds
GB0906470D0 (en)	2009-04-15	2009-05-20	Astex Therapeutics Ltd	New compounds
NZ623384A (en) *	2009-10-16	2016-06-24	Melinta Therapeutics Inc	Antimicrobial compounds and methods of making and using the same
JP2013508299A (ja)	2009-10-16	2013-03-07	リブ−エックスファーマシューティカルズ，インコーポレイテッド	抗微生物性化合物および抗微生物性化合物の製造方法および使用方法
JP6274723B2 (ja)	2009-10-16	2018-02-07	メリンタセラピューティクス，インコーポレイテッド	抗微生物性化合物および抗微生物性化合物の製造方法および使用方法
US20150374705A1 (en)	2012-02-14	2015-12-31	Shanghai Institues for Biological Sciences	Substances for treatment or relief of pain
CN102898315B (zh) *	2012-11-05	2015-01-28	上海毕得医药科技有限公司	3-乙炔基-4-氟苯胺的制备方法
MX2016002975A (es)	2013-09-09	2016-10-21	Melinta Therapeutics Inc	Compuestos antimicrobianos y métodos de fabricación y utilización de los mismos.
US9937183B2 (en)	2013-09-09	2018-04-10	Melinta Therapeutics, Inc.	Antimicrobial compounds and methods of making and using the same
WO2016145417A1 (en)	2015-03-11	2016-09-15	Melinta Therapeutics, Inc.	Antimicrobial compounds and methods of making and using the same
WO2017098367A1 (en) *	2015-12-10	2017-06-15	Pfizer Limited	4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain
BR112018015386A2 (pt)	2016-01-27	2019-03-19	Universität Zürich	uso de moduladores de receptor gabaa para tratamento de prurido
US11098047B2 (en)	2016-05-06	2021-08-24	BioVersys AG	Antimicrobials and methods of making and using same
CN112384513A (zh)	2018-04-18	2021-02-19	纽罗塞克医疗公司	Gabaa正变构调节剂化合物、其制备方法和用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5185446A (en) *	1990-09-04	1993-02-09	Neurogen Corporation	Certain cycloalkyl imidazopyrimidines; a new class of gaba brainreceptor ligands
ES2150671T3 (es) *	1995-04-21	2000-12-01	Neurosearch As	Compuesto de bencimidazol y su utilizacion como moduladores del complejo de receptores gaba-a.
PA8535601A1 (es) *	2000-12-21	2002-11-28	Pfizer	Derivados benzimidazol y piridilimidazol como ligandos para gabaa

2002
- 2002-03-12 TW TW091104588A patent/TWI248936B/zh active
- 2002-03-19 ES ES02706976T patent/ES2244752T3/es not_active Expired - Lifetime
- 2002-03-19 WO PCT/GB2002/001351 patent/WO2002074772A1/en not_active Ceased
- 2002-03-19 HU HU0303630A patent/HUP0303630A3/hu unknown
- 2002-03-19 CZ CZ20032539A patent/CZ20032539A3/cs unknown
- 2002-03-19 JP JP2002573781A patent/JP4409174B2/ja not_active Expired - Fee Related
- 2002-03-19 PE PE2002000211A patent/PE20020970A1/es not_active Application Discontinuation
- 2002-03-19 EP EP02706976A patent/EP1381606B1/en not_active Expired - Lifetime
- 2002-03-19 CN CNB028070577A patent/CN1294133C/zh not_active Expired - Fee Related
- 2002-03-19 CA CA2461426A patent/CA2461426C/en not_active Expired - Fee Related
- 2002-03-19 NZ NZ527901A patent/NZ527901A/en unknown
- 2002-03-19 EE EEP200300455A patent/EE200300455A/xx unknown
- 2002-03-19 PL PL02363804A patent/PL363804A1/xx not_active Application Discontinuation
- 2002-03-19 EA EA200301037A patent/EA006234B1/ru not_active IP Right Cessation
- 2002-03-19 IL IL15764102A patent/IL157641A0/xx unknown
- 2002-03-19 BR BR0207994-1A patent/BR0207994A/pt not_active IP Right Cessation
- 2002-03-19 MX MXPA03008572A patent/MXPA03008572A/es unknown
- 2002-03-19 DE DE60205101T patent/DE60205101T2/de not_active Expired - Lifetime
- 2002-03-19 AU AU2002241138A patent/AU2002241138B2/en not_active Ceased
- 2002-03-19 SK SK1167-2003A patent/SK11672003A3/sk not_active Application Discontinuation
- 2002-03-19 KR KR10-2003-7012252A patent/KR20030083001A/ko not_active Withdrawn
- 2002-03-19 AT AT02706976T patent/ATE299882T1/de not_active IP Right Cessation
- 2002-03-19 WO PCT/GB2002/001352 patent/WO2002074773A1/en not_active Ceased
2003
- 2003-09-09 BG BG108166A patent/BG108166A/xx unknown
- 2003-09-19 NO NO20034170A patent/NO20034170L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
DE60205101T2 (de)	2006-05-24
IL157641A0 (en)	2004-03-28
NO20034170D0 (no)	2003-09-19
CZ20032539A3 (en)	2004-03-17
BR0207994A (pt)	2004-03-02
HUP0303630A3 (en)	2005-06-28
KR20030083001A (ko)	2003-10-23
SK11672003A3 (sk)	2004-05-04
ES2244752T3 (es)	2005-12-16
CN1294133C (zh)	2007-01-10
PL363804A1 (en)	2004-11-29
ATE299882T1 (de)	2005-08-15
EP1381606B1 (en)	2005-07-20
CA2461426C (en)	2010-08-03
WO2002074773A1 (en)	2002-09-26
NO20034170L (no)	2003-11-19
PE20020970A1 (es)	2002-11-01
EE200300455A (et)	2003-12-15
JP4409174B2 (ja)	2010-02-03
DE60205101D1 (de)	2005-08-25
EA006234B1 (ru)	2005-10-27
JP2004523584A (ja)	2004-08-05
AU2002241138B2 (en)	2007-09-20
WO2002074772A1 (en)	2002-09-26
EP1381606A1 (en)	2004-01-21
HUP0303630A2 (hu)	2004-03-01
CA2461426A1 (en)	2002-09-26
MXPA03008572A (es)	2003-12-08
CN1498218A (zh)	2004-05-19
NZ527901A (en)	2005-09-30
TWI248936B (en)	2006-02-11
EA200301037A1 (ru)	2004-04-29

Publication	Publication Date	Title
AU1253002A (en)	2002-05-21	Imidazo-triazine derivatives as ligands for gaba receptors
DE60012044D1 (de)	2004-08-12	Imidazopyridinderivate als liganden für gaba-rezeptoren
IL157641A0 (en)	2004-03-28	Imidazo-pyrimidine derivatives as ligands for gaba receptors
DE60207416D1 (de)	2005-12-22	Imidazotriazin-derivate als gaba-rezeptor-liganden
GB0212048D0 (en)	2002-07-03	Therapeutic agents
ATE338758T1 (de)	2006-09-15	Imidazopyrimidin-derivate als liganden für gaba- rezeptoren
ATE371659T1 (de)	2007-09-15	Pyrazolotriazinderivate als gaba-rezeptorliganden
ATE335741T1 (de)	2006-09-15	8-fluorimidazo(1,2-a)pyridin derivative als liganden für gaba rezeptoren
DE60016566D1 (de)	2005-01-13	Triazolopyridazinderivate als liganden für gaba-rezeptoren
YU43800A (sh)	2002-12-10	Triazolo-piridazin derivati kao ligandi za gaba receptore
EA199900164A1 (ru)	2000-04-24	Замещенные производные триазоло-пиридазина в качестве лигандов рецепторов гамк
ATE253066T1 (de)	2003-11-15	Imidazotriazinderivate als gaba rezeptor-liganden
ATE255109T1 (de)	2003-12-15	Imidazopyridinderivate als gaba rezeptor liganden
ATE250062T1 (de)	2003-10-15	Triazolopiridazinederivate als gaba rezeptor- liganden
DE60325865D1 (de)	2009-03-05	Phenylpyridazin derivative als liganden für gaba-rezeptoren
JO2312B1 (en)	2005-09-12	Imidazo-pyrimidine derivatives as associative groups of JABA receptors
WO2005021562A3 (en)	2005-06-16	Phospinite-imidazolines and metal complexes thereof
MXPA02003639A (es)	2004-11-12	Proceso nuevo para la sintesis de (3as)-5, 5-dioxo-2, 3, 3a-4- tetrahidro-1h-pirrolo[2, 1c][1, 2, 4] benzotiadiazina.
CA2260774A1 (en)	1998-02-05	Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
PE44299A1 (es)	1999-05-06	Derivados sustituidos de triazolo-piridacina como ligandos para receptores gaba
CO5050329A1 (es)	2001-06-27	Nuevos derivados de tetrahidroisoquinoleina y procedimientos para su preparacion