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)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Pain & Pain Management (AREA)
Psychiatry (AREA)
Addiction (AREA)
Hospice & Palliative Care (AREA)
Urology & Nephrology (AREA)
Rheumatology (AREA)
Cardiology (AREA)
Vascular Medicine (AREA)
Toxicology (AREA)
Heart & Thoracic Surgery (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)	WO2002074773A1 (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
AU2004261591A1 (en) *	2003-07-25	2005-02-10	Neurogen Corporation	Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
US8895745B2 (en)	2006-12-22	2014-11-25	Astex Therapeutics Limited	Bicyclic heterocyclic compounds as FGFR inhibitors
CA2672213C (en)	2006-12-22	2016-02-16	Astex Therapeutics Limited	Bicyclic amine derivatives as protein tyrosine kinase inhibitors
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
GB0906470D0 (en)	2009-04-15	2009-05-20	Astex Therapeutics Ltd	New compounds
GB0906472D0 (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
PH12012500734A1 (en)	2009-10-16	2012-11-26	Melinta Therapeutics Inc	Antimicrobial compounds and methods of making and using the same
MX358697B (es)	2009-10-16	2018-08-31	Melinta Therapeutics Inc	Compuestos antimicrobianos y metodos para fabricar y utilizar los mismos.
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
US9937183B2 (en)	2013-09-09	2018-04-10	Melinta Therapeutics, Inc.	Antimicrobial compounds and methods of making and using the same
JP2016536338A (ja)	2013-09-09	2016-11-24	メリンタセラピューティクス，インコーポレイテッド	抗微生物化合物ならびにそれの製造方法および使用方法
US10947237B2 (en)	2015-03-11	2021-03-16	BioVersys AG	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
JP7115746B2 (ja)	2016-01-27	2022-08-09	ウニヴェルズィテート・ツューリヒ	掻痒の処置のためのｇａｂａａ受容体モジュレーターの使用
WO2017193016A1 (en)	2016-05-06	2017-11-09	Melinta Therapeutics, Inc.	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
TR199701219T1 (xx) *	1995-04-21	1998-03-21	Neurosearch A/S	Benzimidazol bile�ikleri, bu bile�ikleri i�eren ispen�iyar� bile�ikler.
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 AT AT02706976T patent/ATE299882T1/de not_active IP Right Cessation
- 2002-03-19 PE PE2002000211A patent/PE20020970A1/es not_active Application Discontinuation
- 2002-03-19 EA EA200301037A patent/EA006234B1/ru not_active IP Right Cessation
- 2002-03-19 EE EEP200300455A patent/EE200300455A/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 CA CA2461426A patent/CA2461426C/en not_active Expired - Fee Related
- 2002-03-19 KR KR10-2003-7012252A patent/KR20030083001A/ko not_active Withdrawn
- 2002-03-19 NZ NZ527901A patent/NZ527901A/en unknown
- 2002-03-19 CN CNB028070577A patent/CN1294133C/zh not_active Expired - Fee Related
- 2002-03-19 EP EP02706976A patent/EP1381606B1/en not_active Expired - Lifetime
- 2002-03-19 HU HU0303630A patent/HUP0303630A3/hu unknown
- 2002-03-19 DE DE60205101T patent/DE60205101T2/de not_active Expired - Lifetime
- 2002-03-19 JP JP2002573781A patent/JP4409174B2/ja not_active Expired - Fee Related
- 2002-03-19 WO PCT/GB2002/001352 patent/WO2002074773A1/en not_active Ceased
- 2002-03-19 WO PCT/GB2002/001351 patent/WO2002074772A1/en not_active Ceased
- 2002-03-19 PL PL02363804A patent/PL363804A1/xx not_active Application Discontinuation
- 2002-03-19 IL IL15764102A patent/IL157641A0/xx unknown
- 2002-03-19 AU AU2002241138A patent/AU2002241138B2/en not_active Ceased
- 2002-03-19 CZ CZ20032539A patent/CZ20032539A3/cs unknown
- 2002-03-19 SK SK1167-2003A patent/SK11672003A3/sk not_active Application Discontinuation
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
CA2461426A1 (en)	2002-09-26
DE60205101D1 (de)	2005-08-25
IL157641A0 (en)	2004-03-28
JP4409174B2 (ja)	2010-02-03
EP1381606B1 (en)	2005-07-20
BR0207994A (pt)	2004-03-02
PE20020970A1 (es)	2002-11-01
NZ527901A (en)	2005-09-30
HUP0303630A2 (hu)	2004-03-01
CA2461426C (en)	2010-08-03
CN1294133C (zh)	2007-01-10
PL363804A1 (en)	2004-11-29
EA200301037A1 (ru)	2004-04-29
EA006234B1 (ru)	2005-10-27
KR20030083001A (ko)	2003-10-23
WO2002074773A1 (en)	2002-09-26
ES2244752T3 (es)	2005-12-16
NO20034170D0 (no)	2003-09-19
EP1381606A1 (en)	2004-01-21
SK11672003A3 (sk)	2004-05-04
MXPA03008572A (es)	2003-12-08
TWI248936B (en)	2006-02-11
EE200300455A (et)	2003-12-15
DE60205101T2 (de)	2006-05-24
NO20034170L (no)	2003-11-19
CN1498218A (zh)	2004-05-19
ATE299882T1 (de)	2005-08-15
AU2002241138B2 (en)	2007-09-20
CZ20032539A3 (en)	2004-03-17
WO2002074772A1 (en)	2002-09-26
JP2004523584A (ja)	2004-08-05
HUP0303630A3 (en)	2005-06-28

Publication	Publication Date	Title
BG108166A (en)	2004-09-30	Imidazo-pyrimidine derivatives as liigands for gaba receptors
AU1253002A (en)	2002-05-21	Imidazo-triazine derivatives as ligands for gaba receptors
WO2001038326A3 (en)	2002-05-10	Imidazo-pyridine derivatives as ligands for gaba receptors
ATE310002T1 (de)	2005-12-15	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
ATE335741T1 (de)	2006-09-15	8-fluorimidazo(1,2-a)pyridin derivative als liganden für gaba rezeptoren
ATE284403T1 (de)	2004-12-15	Triazolopyridazinderivate als liganden für gaba- rezeptoren
CA2410037A1 (en)	2001-11-29	3-phenyl-imidazo-pyrimidine derivatives as ligands for gaba receptors
BG104671A (en)	2001-05-31	Triazolo-pyridazine derivatives as ligands for gaba receptors
EA199900164A1 (ru)	2000-04-24	Замещенные производные триазоло-пиридазина в качестве лигандов рецепторов гамк
DE60006260D1 (de)	2003-12-04	Imidazotriazinderivate als gaba rezeptor-liganden
ATE255109T1 (de)	2003-12-15	Imidazopyridinderivate als gaba rezeptor liganden
DE69911374D1 (de)	2003-10-23	Triazolopiridazinederivate als gaba rezeptor-liganden
DE60325865D1 (de)	2009-03-05	Phenylpyridazin derivative als liganden für gaba-rezeptoren
TW200609218A (en)	2006-03-16	Bicyclic compounds
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
EA200200378A2 (ru)	2002-10-31	НОВЫЙ СПОСОБ СИНТЕЗА (3aS)-5,5-ДИОКСО-2,3,3а,4-ТЕТРАГИДРО-1H-ПИРРОЛО[2,1-c][1,2,4]БЕНЗОТИАДИАЗИНА
TR200002100T2 (tr)	2000-12-21	GABA reseptörleri için ligandlar olarak triazolo-piridazin türevleri
WO2002060960A3 (en)	2002-10-17	New polymers based on n-carbamyl-n'-dimethylsilyl methyl-piperazine traceless linkers for the solid phase synthesis of phenyl based libraries
WO2001080719A3 (en)	2002-03-28	Methods and composition for the diagnosis of schizophrenia
CO5050329A1 (es)	2001-06-27	Nuevos derivados de tetrahidroisoquinoleina y procedimientos para su preparacion