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AR045959A1 - Derivados de pirazolo- e imidazo-pirimidina - Google Patents

Derivados de pirazolo- e imidazo-pirimidina

Info

Publication number
AR045959A1
AR045959A1 ARP040103565A ARP040103565A AR045959A1 AR 045959 A1 AR045959 A1 AR 045959A1 AR P040103565 A ARP040103565 A AR P040103565A AR P040103565 A ARP040103565 A AR P040103565A AR 045959 A1 AR045959 A1 AR 045959A1
Authority
AR
Argentina
Prior art keywords
hydrogen
unsubstituted
cycloalkyl
alkyl
halogen
Prior art date
Application number
ARP040103565A
Other languages
English (en)
Inventor
Juergen Wichmann
Thomas Johannes Woltering
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR045959A1 publication Critical patent/AR045959A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Otolaryngology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Composiciones farmacéuticas que contienen dichos derivados y a su utilización en la prevención y tratamiento de enfermedades. Reivindicación 1: Un compuesto de la fórmula (1), en la que: A es =C(R4)-; D es =C(R5)-; E es =C(R6)-; o uno de A, D y E es =N-; L es =N- o =C(H)-; M es =C(R7)-, cuando L es =N-; o M es =N-, cuando L es =C(H)-; R1 es -CN, piridinilo sin sustituir, piridinilo sustituido por alquilo C1-4 o el correspondiente N-óxido de piridina; R2 es hidrógeno, halógeno, alquilo C1-4 o cicloalquilo C3-6; R3 es hidrógeno, halógeno, alquilo C1-4 o cicloalquilo C3-6; R4 es hidrógeno, halógeno, alquilo C1-4 sin sustituir o alquilo C1-4 sustituido por flúor, alcoxi C1-4 sin sustituir o alcoxi C1-4 sustituido por flúor, cicloalquilo C3- 6 sin sustituir o cicloalquilo C3-6 sustituido por flúor; R5 es hidrógeno, halógeno, alquilo C1-4 sin sustituir o alquilo C1-4 sustituido por flúor, cicloalquilo C3-6 sin sustituir o cicloalquilo C3-6 sustituido por flúor; R6 es hidrógeno o halógeno; y R7 es hidrógeno, alquilo C1-4 sin sustituir o alquilo C1-4 sustituido por CN, cicloalquilo C3-6 sin sustituir o cicloalquilo C3-6 sustituido por CN, con la condición de que cuando A es =C(R4)-, D es =C(H)-, E es =C(H)-, L es =N-, R1 es - CN, R2 es hidrógeno, R3 es hidrógeno, y a) M es =C(H)-, R4 no es hidrógeno, cloro o metoxi; o b) M es =C(CH3)-, R4 no es hidrógeno, y sus sales de adición farmacéuticamente aceptables.
ARP040103565A 2003-10-03 2004-10-01 Derivados de pirazolo- e imidazo-pirimidina AR045959A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03078075 2003-10-03

Publications (1)

Publication Number Publication Date
AR045959A1 true AR045959A1 (es) 2005-11-16

Family

ID=34486287

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103565A AR045959A1 (es) 2003-10-03 2004-10-01 Derivados de pirazolo- e imidazo-pirimidina

Country Status (20)

Country Link
US (2) US7329662B2 (es)
EP (1) EP1670801B1 (es)
JP (1) JP4551402B2 (es)
KR (2) KR100781469B1 (es)
CN (2) CN101239981B (es)
AR (1) AR045959A1 (es)
AT (1) ATE512148T1 (es)
AU (1) AU2004283801B2 (es)
BR (1) BRPI0414948A (es)
CA (1) CA2540768C (es)
CO (1) CO5680437A2 (es)
ES (1) ES2364753T3 (es)
IL (1) IL174512A0 (es)
MX (1) MXPA06003526A (es)
NO (1) NO20061363L (es)
NZ (1) NZ546037A (es)
RU (1) RU2350616C2 (es)
TW (1) TWI297691B (es)
WO (1) WO2005040171A1 (es)
ZA (1) ZA200602677B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
RU2378277C2 (ru) 2004-06-21 2010-01-10 Ф. Хоффманн-Ля Рош Аг Производные пиразолпиримидина
JP4708438B2 (ja) * 2005-02-11 2011-06-22 エフ.ホフマン−ラ ロシュ アーゲー mGluR2アンタゴニストとしてのピラゾロピリミジン誘導体
CN101180299B (zh) 2005-03-23 2010-12-15 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的乙炔基-吡唑并嘧啶衍生物
BRPI0616571A2 (pt) 2005-09-27 2011-06-21 Hoffmann La Roche oxadiazolil pirazol-piridiminas como antagonistas de mglur2, processo para sua preparação, composição farmacêutica que os contém e uso dos mesmo
EP2178375B1 (en) * 2007-07-20 2014-09-24 Merck Sharp & Dohme Corp. Pyrazoloý1,5-a¨pyrimidine derivatives
CN101671336B (zh) * 2009-09-23 2013-11-13 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途
US9447099B2 (en) * 2011-10-04 2016-09-20 Hoffmann-La Roche Inc. Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine
US20150197503A1 (en) * 2012-07-27 2015-07-16 Bial-Portela & Cª, S.A. Process for the synthesis of substituted urea compounds
MX2015004604A (es) 2012-10-23 2015-10-08 Hoffmann La Roche Antagonistas de los receptores metabotropicos de glutamato 2/3 (mglu2/3) para el tratamiento de los trastornos autistas.
MY182036A (en) 2013-02-21 2021-01-18 Sunshine Lake Pharma Co Ltd Heteroaromatic compounds as pi3 kinase modulators
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法
CN104193745B (zh) * 2014-07-30 2016-09-28 斯芬克司药物研发(天津)股份有限公司 一种咪唑并嘧啶羧酸类化合物及其制备方法
CN107018661B (zh) * 2014-08-01 2020-01-03 詹森药业有限公司 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途
EP3000814A1 (en) 2014-09-26 2016-03-30 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
WO2016087489A1 (en) * 2014-12-03 2016-06-09 Janssen Pharmaceutica Nv Radiolabelled mglur2 pet ligands
TWI713497B (zh) * 2015-02-26 2020-12-21 南韓商愛思開生物製藥股份有限公司 咪唑并嘧啶及咪唑并三衍生物及包含該衍生物之醫藥組成物
AU2016311426B2 (en) 2015-08-26 2021-05-20 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to NTRK
EP3377497A1 (en) * 2015-11-19 2018-09-26 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
EP3389728B1 (en) 2015-12-18 2020-08-05 Janssen Pharmaceutica NV Radiolabelled mglur2/3 pet ligands
PL3389727T3 (pl) 2015-12-18 2021-02-08 Janssen Pharmaceutica Nv RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET
TWI795510B (zh) * 2018-01-17 2023-03-11 英商葛蘭素史密斯克藍智慧財產發展有限公司 PI4KIIIβ抑制劑
WO2025002289A1 (zh) * 2023-06-29 2025-01-02 湖南九典制药股份有限公司 一种吡唑并杂芳基类化合物及其制备方法和应用
CN116836110A (zh) * 2023-06-30 2023-10-03 天津均凯农业科技有限公司 一种2-氨乙基-3-氯-5-三氟甲基吡啶盐酸盐的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ244598A3 (cs) 1996-02-07 1998-10-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidiny jako antagonisty CRF receptoru
NZ333777A (en) * 1996-07-24 2000-07-28 Du Pont Pharm Co (1,5-a) pyrazolo and triazole triazines and pyrimidines
ATE214704T1 (de) * 1997-07-18 2002-04-15 Hoffmann La Roche 5h-thiazolo(3,2-a)pyrimidinderivate
AU4203500A (en) 1999-04-06 2000-10-23 Du Pont Pharmaceuticals Company Pyrazolopyrimidines as crf antagonists
JP4071115B2 (ja) 2001-04-12 2008-04-02 エフ.ホフマン−ラ ロシュ アーゲー mGluR2アンタゴニストIIとしてのジヒドロ−ベンゾ〔b〕〔1,4〕ジアゼピン−2−オン誘導体
GB0128499D0 (en) 2001-11-28 2002-01-23 Merck Sharp & Dohme Therapeutic agents
EP1453815A4 (en) * 2001-11-30 2005-04-06 Merck & Co Inc METABOTROPIC GLUTAMATE RECEPTOR-5 MODULATORS
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine

Also Published As

Publication number Publication date
NO20061363L (no) 2006-04-24
RU2006114749A (ru) 2007-11-20
CN101239981A (zh) 2008-08-13
US7329662B2 (en) 2008-02-12
WO2005040171A8 (en) 2006-08-03
EP1670801B1 (en) 2011-06-08
KR100781469B1 (ko) 2007-12-03
NZ546037A (en) 2008-09-26
TW200528453A (en) 2005-09-01
KR20060089731A (ko) 2006-08-09
IL174512A0 (en) 2006-08-01
KR20070096033A (ko) 2007-10-01
JP4551402B2 (ja) 2010-09-29
AU2004283801B2 (en) 2010-04-22
TWI297691B (en) 2008-06-11
CN1890242A (zh) 2007-01-03
CA2540768A1 (en) 2005-05-06
CO5680437A2 (es) 2006-09-29
RU2350616C2 (ru) 2009-03-27
US20050130992A1 (en) 2005-06-16
WO2005040171A1 (en) 2005-05-06
ATE512148T1 (de) 2011-06-15
ES2364753T3 (es) 2011-09-13
CA2540768C (en) 2011-08-09
US7514443B2 (en) 2009-04-07
CN100522964C (zh) 2009-08-05
AU2004283801A1 (en) 2005-05-06
JP2007507446A (ja) 2007-03-29
ZA200602677B (en) 2007-09-26
EP1670801A1 (en) 2006-06-21
MXPA06003526A (es) 2006-06-08
CN101239981B (zh) 2011-01-19
US20080051421A1 (en) 2008-02-28
BRPI0414948A (pt) 2006-11-07
HK1099302A1 (zh) 2007-08-10

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