DK1368355T3 - Substituerede pyrazolo- og thiazolopyrimidiner som analgetika - Google Patents

Substituerede pyrazolo- og thiazolopyrimidiner som analgetika

Info

Publication number: DK1368355T3
Authority: DK; Denmark
Prior art keywords: alkyl; pyrimidine; pyrazolo; tetrahydro; aryl
Prior art date: 2001-03-14

Application number

DK02729998T

Other languages

Danish (da)

English (en)

Inventor

Martin Fuhr

Adriaan P Ijzerman

Groote Miriam Dissen-De

Matthias Gerlach

Corinna Maul

Utz-Peter Jagusch

Bernd Sundermann

Original Assignee

Gruenenthal Gmbh

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.)

2001-03-14

Filing date

2002-03-13

Publication date

2006-10-09

2001-03-14 Priority claimed from DE2001112197 external-priority patent/DE10112197A1/de

2001-10-29 Priority claimed from DE2001153344 external-priority patent/DE10153344A1/de

2002-03-13 Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh

2006-10-09 Application granted granted Critical

2006-10-09 Publication of DK1368355T3 publication Critical patent/DK1368355T3/da

Links

229940035676 analgesics Drugs 0.000 title 1
239000000730 antalgic agent Substances 0.000 title 1
150000008634 thiazolopyrimidines Chemical class 0.000 title 1
125000000217 alkyl group Chemical group 0.000 abstract 8
125000003118 aryl group Chemical group 0.000 abstract 8
125000000753 cycloalkyl group Chemical group 0.000 abstract 6
125000004981 cycloalkylmethyl group Chemical group 0.000 abstract 5
125000003710 aryl alkyl group Chemical group 0.000 abstract 4
239000003446 ligand Substances 0.000 abstract 4
GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 abstract 3
101150065749 Churc1 gene Proteins 0.000 abstract 3
102100038239 Protein Churchill Human genes 0.000 abstract 3
150000001875 compounds Chemical class 0.000 abstract 3
125000001475 halogen functional group Chemical group 0.000 abstract 3
101150009274 nhr-1 gene Proteins 0.000 abstract 3
-1 thiazolo-pyrimidine compounds Chemical class 0.000 abstract 3
JYDBGFDTBUSKLO-UHFFFAOYSA-N 7-(3,4-dimethoxyphenyl)-2-methylsulfanyl-5-(2-phenylethyl)-1,2,3,3a-tetrahydropyrazolo[1,5-a]pyrimidine-3-carbonitrile Chemical compound C1=C(OC)C(OC)=CC=C1C1=CC(CCC=2C=CC=CC=2)=NC2N1NC(SC)C2C#N JYDBGFDTBUSKLO-UHFFFAOYSA-N 0.000 abstract 2
102000019055 Nucleoside Transport Proteins Human genes 0.000 abstract 2
108010012315 Nucleoside Transport Proteins Proteins 0.000 abstract 2
239000003146 anticoagulant agent Substances 0.000 abstract 2
239000003814 drug Substances 0.000 abstract 2
125000000623 heterocyclic group Chemical group 0.000 abstract 2
125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
150000003839 salts Chemical class 0.000 abstract 2
239000012453 solvate Substances 0.000 abstract 2
GCAJUNZLLXNQQO-UHFFFAOYSA-N 1,2,3,3a-tetrahydropyrazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2NCCC21 GCAJUNZLLXNQQO-UHFFFAOYSA-N 0.000 abstract 1
ONMSTJPALRFZAG-UHFFFAOYSA-N 2,5,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine Chemical compound N1C(C)CC(C)N2N=C(C)C=C21 ONMSTJPALRFZAG-UHFFFAOYSA-N 0.000 abstract 1
SYBNTJUJVKJEDU-UHFFFAOYSA-N 2,5-dimethyl-7-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine Chemical compound N12N=C(C)C=C2NC(C)CC1C1=CC=CC=C1 SYBNTJUJVKJEDU-UHFFFAOYSA-N 0.000 abstract 1
AMBPCUJCEYOPTB-UHFFFAOYSA-N 2-(4-nitrophenyl)-4-phenyl-3,4-dihydro-2h-pyrimido[2,1-b][1,3]benzothiazole Chemical compound C1=CC([N+](=O)[O-])=CC=C1C1N=C(SC=2C3=CC=CC=2)N3C(C=2C=CC=CC=2)C1 AMBPCUJCEYOPTB-UHFFFAOYSA-N 0.000 abstract 1
RRUGGIXQTXGKHI-UHFFFAOYSA-N 2-methyl-5,7-diphenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine Chemical compound N12N=C(C)C=C2NC(C=2C=CC=CC=2)CC1C1=CC=CC=C1 RRUGGIXQTXGKHI-UHFFFAOYSA-N 0.000 abstract 1
HBBDYBGRGJFMAM-UHFFFAOYSA-N 2-methyl-5,7-dipropyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carbonitrile Chemical compound N1C(CCC)CC(CCC)N2N=C(C)C(C#N)=C21 HBBDYBGRGJFMAM-UHFFFAOYSA-N 0.000 abstract 1
CJPCIJLKUZKGER-UHFFFAOYSA-N 4-(4-methylphenyl)-2-(4-nitrophenyl)-3,4-dihydro-2h-pyrimido[2,1-b][1,3]benzothiazole Chemical compound C1=CC(C)=CC=C1C1N2C3=CC=CC=C3SC2=NC(C=2C=CC(=CC=2)[N+]([O-])=O)C1 CJPCIJLKUZKGER-UHFFFAOYSA-N 0.000 abstract 1
101710169336 5'-deoxyadenosine deaminase Proteins 0.000 abstract 1
UVZIQHQSQAMQMA-UHFFFAOYSA-N 5,7-dimethyl-2-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine Chemical compound C1=C2NC(C)CC(C)N2N=C1C1=CC=CC=C1 UVZIQHQSQAMQMA-UHFFFAOYSA-N 0.000 abstract 1
OOXNYFKPOPJIOT-UHFFFAOYSA-N 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-amine;dihydrochloride Chemical compound Cl.Cl.C=12C(N)=NC=NC2=NC(C=2C=NC(=CC=2)N2CCOCC2)=CC=1C1=CC=CC(Br)=C1 OOXNYFKPOPJIOT-UHFFFAOYSA-N 0.000 abstract 1
OTDPOGIOVOHVDX-UHFFFAOYSA-N 5-methyl-7-[3-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carbonitrile Chemical compound N12N=CC(C#N)=C2NC(C)CC1C1=CC=CC(C(F)(F)F)=C1 OTDPOGIOVOHVDX-UHFFFAOYSA-N 0.000 abstract 1
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
102000055025 Adenosine deaminases Human genes 0.000 abstract 1
102100032534 Adenosine kinase Human genes 0.000 abstract 1
108010076278 Adenosine kinase Proteins 0.000 abstract 1
102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 abstract 1
108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 abstract 1
239000002253 acid Substances 0.000 abstract 1
230000000202 analgesic effect Effects 0.000 abstract 1
230000003288 anthiarrhythmic effect Effects 0.000 abstract 1
230000001773 anti-convulsant effect Effects 0.000 abstract 1
230000003178 anti-diabetic effect Effects 0.000 abstract 1
230000036436 anti-hiv Effects 0.000 abstract 1
230000003110 anti-inflammatory effect Effects 0.000 abstract 1
230000000648 anti-parkinson Effects 0.000 abstract 1
230000002682 anti-psoriatic effect Effects 0.000 abstract 1
239000003416 antiarrhythmic agent Substances 0.000 abstract 1
229940127219 anticoagulant drug Drugs 0.000 abstract 1
239000001961 anticonvulsive agent Substances 0.000 abstract 1
239000003472 antidiabetic agent Substances 0.000 abstract 1
229960003965 antiepileptics Drugs 0.000 abstract 1
239000000939 antiparkinson agent Substances 0.000 abstract 1
125000005002 aryl methyl group Chemical group 0.000 abstract 1
238000003556 assay Methods 0.000 abstract 1
230000001966 cerebroprotective effect Effects 0.000 abstract 1
OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical compound C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 abstract 1
239000000824 cytostatic agent Substances 0.000 abstract 1
230000001085 cytostatic effect Effects 0.000 abstract 1
230000000694 effects Effects 0.000 abstract 1
150000004677 hydrates Chemical class 0.000 abstract 1
230000000147 hypnotic effect Effects 0.000 abstract 1
230000005764 inhibitory process Effects 0.000 abstract 1
230000010534 mechanism of action Effects 0.000 abstract 1
239000000203 mixture Substances 0.000 abstract 1
239000003176 neuroleptic agent Substances 0.000 abstract 1
230000000701 neuroleptic effect Effects 0.000 abstract 1
230000000324 neuroprotective effect Effects 0.000 abstract 1
230000001777 nootropic effect Effects 0.000 abstract 1
150000003230 pyrimidines Chemical class 0.000 abstract 1
108020003175 receptors Proteins 0.000 abstract 1
102000005962 receptors Human genes 0.000 abstract 1
230000000241 respiratory effect Effects 0.000 abstract 1
230000002537 thrombolytic effect 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
- A61P11/00—Drugs for disorders of the respiratory 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
- 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
- A61P25/20—Hypnotics; Sedatives
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
- 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
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- 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
- 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
- A61P9/06—Antiarrhythmics
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Engineering & Computer Science (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Pain & Pain Management (AREA)
Psychology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Urology & Nephrology (AREA)
Ophthalmology & Optometry (AREA)
Psychiatry (AREA)
Rheumatology (AREA)
Anesthesiology (AREA)
Immunology (AREA)
Dermatology (AREA)
Hospice & Palliative Care (AREA)
Pulmonology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Plural Heterocyclic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

DK02729998T 2001-03-14 2002-03-13 Substituerede pyrazolo- og thiazolopyrimidiner som analgetika DK1368355T3 (da)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
DE2001112197 DE10112197A1 (de)	2001-03-14	2001-03-14	Substituierte Pyrazolo- und Thiazolopyrimidine
DE2001153344 DE10153344A1 (de)	2001-10-29	2001-10-29	Verwendung von substituierten Pyrazolopyrimidinen als Liganden von Nucleosid-Transport-Proteinen und/oder von Purinorezeptoren

Publications (1)

Publication Number	Publication Date
DK1368355T3 true DK1368355T3 (da)	2006-10-09

Family

ID=26008763

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK02729998T DK1368355T3 (da)	2001-03-14	2002-03-13	Substituerede pyrazolo- og thiazolopyrimidiner som analgetika

Country Status (25)

Country	Link
US (1)	US7135568B2 (el)
EP (2)	EP1637533B1 (el)
JP (1)	JP2004527508A (el)
KR (1)	KR20030082982A (el)
CN (1)	CN1318422C (el)
AT (2)	ATE404568T1 (el)
AU (1)	AU2002302419B2 (el)
BR (1)	BR0208244A (el)
CA (1)	CA2440760C (el)
CY (1)	CY1105507T1 (el)
CZ (1)	CZ20032474A3 (el)
DE (2)	DE50207103D1 (el)
DK (1)	DK1368355T3 (el)
ES (2)	ES2311920T3 (el)
HK (1)	HK1061034A1 (el)
HU (1)	HUP0401211A3 (el)
IL (2)	IL157895A0 (el)
MX (1)	MXPA03008291A (el)
NO (1)	NO20034031L (el)
NZ (2)	NZ528639A (el)
PL (1)	PL364388A1 (el)
PT (1)	PT1368355E (el)
RU (1)	RU2003129060A (el)
SK (1)	SK11542003A3 (el)
WO (1)	WO2002072585A2 (el)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2004017908A2 (en)	2002-08-26	2004-03-04	Takeda Pharmaceutical Company Limited	Calcium receptor modulating compound and use thereof
ATE481402T1 (de) *	2003-02-27	2010-10-15	Palau Pharma Sa	Pyrazolopyridin-derivate
GB0404434D0 (en)	2004-02-27	2004-03-31	Novartis Ag	Organic compounds
WO2005112936A1 (en) *	2004-05-14	2005-12-01	The Regents Of The University Of Michigan	Compositions and methods relating to protein kinase inhibitors
AR050188A1 (es) *	2004-08-03	2006-10-04	Uriach Y Compania S A J	Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen
EP1736475A1 (en) *	2005-06-21	2006-12-27	Ferrer Internacional, S.A.	Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
KR100838692B1 (ko)	2007-07-11	2008-06-16	한국화학연구원	7-(3′,4′-디알콕시페닐)-4,5,6,7-테트라히드로피라졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는천식 및 만성폐쇄성 폐질환을 포함한 염증관련 질환,관절염, 아토피 피부염, 암 및 뇌질환의 치료 및 예방을위한 약제학적 조성물
US8629154B2 (en) *	2008-01-24	2014-01-14	Andrey Alexandrovich Ivashchenko	Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the use thereof
EA017805B1 (ru) *	2008-01-24	2013-03-29	Андрей Александрович ИВАЩЕНКО	2-АЛКИЛАМИНО-3-АРИЛСУЛЬФОНИЛЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
JP2012504663A (ja) *	2008-10-06	2012-02-23	アンドレイ・アレクサンドロビッチ・イワシェンコ	置換された３−アリールスルホニル−ピラゾロ［１，５−ａ］ピリミジン、セロトニン５−ＨＴ６受容体アンタゴニスト、その調製のための方法及び使用
CA2747750A1 (en) *	2008-12-22	2010-07-01	Theodros Asberom	Gamma secretase modulators
JO3407B1 (ar)	2012-05-31	2019-10-20	Eisai R&D Man Co Ltd	مركبات رباعي هيدرو بيرازولو بيريميدين
CN102775412B (zh) *	2012-08-21	2013-05-01	四川大学	一种镇静催眠的化合物及其制备方法和用途
CN102977106B (zh) *	2012-12-12	2014-12-10	中国药科大学	一类具有外周镇痛作用的κ阿片受体激动剂
KR20150131254A (ko) *	2013-03-15	2015-11-24	크로모셀 코포레이션	통증 치료를 위한 소듐 채널 조절자
MX2016002881A (es)	2013-09-10	2016-04-21	Chromocell Corp	Moduladores del canal de sodio para el tratamiento de dolor y diabetes.
US10526323B2 (en)	2015-01-30	2020-01-07	Vanderbilt University	Indazole and azaindazole substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
KR102684436B1 (ko)	2015-10-16	2024-07-15	에자이 알앤드디 매니지먼트 가부시키가이샤	Ep4 길항제
WO2018133835A1 (en) *	2017-01-20	2018-07-26	National Institute Of Biological Sciences, Beijing	Nucleoside analogue regulating mammalian circadian rhythm
SG11201909812VA (en) *	2017-04-27	2019-11-28	Takeda Pharmaceuticals Co	Heterocyclic compound
CN113354644B (zh) *	2020-03-04	2023-07-04	烟台药物研究所	一类用作dpp-iv抑制剂的吡唑并嘧啶结构的化合物及应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4847256A (en) *	1986-10-16	1989-07-11	American Cyanamid Company	4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
EP0264773A1 (en)	1986-10-16	1988-04-27	American Cyanamid Company	4,5-dihydro and 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidines
NZ233641A (en) *	1989-05-16	1992-07-28	Merrell Dow Pharma	Quinoline and thienopyridine derivatives and excitatory amino acid antagonistic pharmaceutical compositions
GB9206266D0 (en) *	1992-03-23	1992-05-06	Merck Sharp & Dohme	Therapeutic agents
FR2717812B1 (fr) *	1994-03-28	1996-05-10	Rhone Poulenc Rorer Sa	Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant.
FR2722786B1 (fr) *	1994-07-20	1996-08-23	Rhone Poulenc Rorer Sa	Derives de 4-hydroxy-3-phenyl-indeno(1,2-b)pyridine-2(1h)- one, leur preparation et les medicaments les contenant
DE4444815A1 (de) *	1994-12-15	1996-06-20	Merck Patent Gmbh	Thienopyridone
JP2003288537A (ja)	2000-09-25	2003-10-10	Everyd.Com:Kk	商品宅配システムおよび方法
DE10112197A1 (de)	2001-03-14	2002-09-19	Gruenenthal Gmbh	Substituierte Pyrazolo- und Thiazolopyrimidine

2002
- 2002-03-13 ES ES05026811T patent/ES2311920T3/es not_active Expired - Lifetime
- 2002-03-13 NZ NZ528639A patent/NZ528639A/en unknown
- 2002-03-13 HU HU0401211A patent/HUP0401211A3/hu unknown
- 2002-03-13 KR KR10-2003-7011953A patent/KR20030082982A/ko not_active Application Discontinuation
- 2002-03-13 CA CA2440760A patent/CA2440760C/en not_active Expired - Fee Related
- 2002-03-13 PL PL02364388A patent/PL364388A1/xx not_active Application Discontinuation
- 2002-03-13 WO PCT/EP2002/002722 patent/WO2002072585A2/de active IP Right Grant
- 2002-03-13 AT AT05026811T patent/ATE404568T1/de not_active IP Right Cessation
- 2002-03-13 MX MXPA03008291A patent/MXPA03008291A/es active IP Right Grant
- 2002-03-13 AU AU2002302419A patent/AU2002302419B2/en not_active Ceased
- 2002-03-13 EP EP05026811A patent/EP1637533B1/de not_active Expired - Lifetime
- 2002-03-13 BR BR0208244-6A patent/BR0208244A/pt not_active Application Discontinuation
- 2002-03-13 CZ CZ20032474A patent/CZ20032474A3/cs unknown
- 2002-03-13 EP EP02729998A patent/EP1368355B1/de not_active Expired - Lifetime
- 2002-03-13 JP JP2002571501A patent/JP2004527508A/ja active Pending
- 2002-03-13 DE DE50207103T patent/DE50207103D1/de not_active Expired - Lifetime
- 2002-03-13 NZ NZ540574A patent/NZ540574A/en unknown
- 2002-03-13 DK DK02729998T patent/DK1368355T3/da active
- 2002-03-13 SK SK1154-2003A patent/SK11542003A3/sk unknown
- 2002-03-13 AT AT02729998T patent/ATE328886T1/de not_active IP Right Cessation
- 2002-03-13 CN CNB028096886A patent/CN1318422C/zh not_active Expired - Fee Related
- 2002-03-13 RU RU2003129060/04A patent/RU2003129060A/ru not_active Application Discontinuation
- 2002-03-13 PT PT02729998T patent/PT1368355E/pt unknown
- 2002-03-13 ES ES02729998T patent/ES2263779T3/es not_active Expired - Lifetime
- 2002-03-13 DE DE50212652T patent/DE50212652D1/de not_active Expired - Lifetime
- 2002-03-13 IL IL15789502A patent/IL157895A0/xx unknown
2003
- 2003-09-11 NO NO20034031A patent/NO20034031L/no not_active Application Discontinuation
- 2003-09-11 IL IL157895A patent/IL157895A/en not_active IP Right Cessation
- 2003-09-12 US US10/660,794 patent/US7135568B2/en not_active Expired - Fee Related
2004
- 2004-06-09 HK HK04104154A patent/HK1061034A1/xx not_active IP Right Cessation
2006
- 2006-07-05 CY CY20061100930T patent/CY1105507T1/el unknown

Also Published As

Publication number	Publication date
HUP0401211A3 (en)	2008-03-28
PL364388A1 (en)	2004-12-13
SK11542003A3 (sk)	2004-07-07
EP1368355A2 (de)	2003-12-10
DE50207103D1 (en)	2006-07-20
JP2004527508A (ja)	2004-09-09
IL157895A0 (en)	2004-03-28
ES2263779T3 (es)	2006-12-16
PT1368355E (pt)	2006-09-29
CY1105507T1 (el)	2010-04-28
HK1061034A1 (en)	2004-09-03
NZ528639A (en)	2005-07-29
NO20034031L (no)	2003-10-21
CN1507447A (zh)	2004-06-23
NZ540574A (en)	2006-11-30
CA2440760A1 (en)	2002-09-19
ATE328886T1 (de)	2006-06-15
DE50212652D1 (de)	2008-09-25
CZ20032474A3 (cs)	2003-12-17
NO20034031D0 (no)	2003-09-11
IL157895A (en)	2009-12-24
RU2003129060A (ru)	2005-04-10
BR0208244A (pt)	2004-03-02
US20040127508A1 (en)	2004-07-01
EP1368355B1 (de)	2006-06-07
EP1637533A1 (de)	2006-03-22
CA2440760C (en)	2010-02-09
EP1637533B1 (de)	2008-08-13
HUP0401211A2 (hu)	2004-10-28
WO2002072585A3 (de)	2003-02-20
KR20030082982A (ko)	2003-10-23
ATE404568T1 (de)	2008-08-15
CN1318422C (zh)	2007-05-30
US7135568B2 (en)	2006-11-14
WO2002072585A2 (de)	2002-09-19
AU2002302419B2 (en)	2007-01-18
ES2311920T3 (es)	2009-02-16
MXPA03008291A (es)	2003-12-11

Publication	Publication Date	Title
DK1368355T3 (da)	2006-10-09	Substituerede pyrazolo- og thiazolopyrimidiner som analgetika
KR950031113A (ko)	1995-12-18	약리학적 활성이 있는 피롤로피리미딘 유도체
IL104244A (en)	1997-07-13	FUNGICIDAL COMPOSITIONS CONTAINING SUBSTITUTED 7-AMINO-1, 2, 4-TRIAZOLO £1, 5-a\| PYRIMIDINE DERIVATIVES AND THEIR PREPARATION
CA2107479A1 (en)	1992-10-23	Pyrazolo[1,5-a]Pyrimidine Derivatives and Anti-Inflammatory Agent Containing the Same
DE3750596D1 (de)	1994-11-03	1,2,3,3a,8,8a-Hexahydro-1,3a,8-Trimethylpyrrolo[2,3-b]indole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel.
AU533295B2 (en)	1983-11-17	Triazolo (4,3-a)pyridines
ATE108792T1 (de)	1994-08-15	Chinindolinderivate, verfahren und zwischenprodukte zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen.
DE69401716D1 (de)	1997-03-20	Imidazo [1,2-a] pyrasin-4-on-derivate welche als ampa und nmda receptor antagonisten dienen
IL109530A0 (en)	1994-08-26	[1,2,4] traizolo [4,3-a] quinoxaline derivatives, pharamceutical compositions containing them and method for their preparation
IL84009A (en)	1992-01-15	1,3,4,16b-tetrahydro-2h,10h-indolo(2,1-c)-pyrazino(1,2-a)(1,4)benzodiazepines,their preparation and pharmaceutical compositions containing them
ATE2431T1 (de)	1983-03-15	2,3-dihydroimidazo (1,2-b) pyridazin-derivate, verfahren zu ihrer herstellung und ihre therapeutische verwendung.
DK298085A (da)	1986-01-03	Pyrrolo(1,2-b)(1,2,5)triazepiner, deres fremstilling og anvendelse som laegemiddel, samt ved fremstillingen anvendelige mellemprodukter
DE69210648D1 (de)	1996-06-20	1,2,4-Triazolo[1,5-a]pyrimidinderivate, Verfahren zu ihrer Herstellung, diese enthaltende Arzneimittel und ihre Verwendung