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BRPI0616264B8 - composto 7-[2-[4-(6-flúor-3-metil-1,2-benzissoxazol-5- il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c]-pirimidin-5-amina, e, composição farmacêutica - Google Patents

composto 7-[2-[4-(6-flúor-3-metil-1,2-benzissoxazol-5- il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c]-pirimidin-5-amina, e, composição farmacêutica

Info

Publication number
BRPI0616264B8
BRPI0616264B8 BRPI0616264A BRPI0616264A BRPI0616264B8 BR PI0616264 B8 BRPI0616264 B8 BR PI0616264B8 BR PI0616264 A BRPI0616264 A BR PI0616264A BR PI0616264 A BRPI0616264 A BR PI0616264A BR PI0616264 B8 BRPI0616264 B8 BR PI0616264B8
Authority
BR
Brazil
Prior art keywords
benzisoxazol
triazol
pyrazol
pyrimidin
propynyl
Prior art date
Application number
BRPI0616264A
Other languages
English (en)
Inventor
D Boyle Craig
E Lachowicz Jean
Chackalamannil Samuel
G Shah Unmesh
Original Assignee
Merck Sharp & Dohme
Schering Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37487759&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0616264(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme, Schering Corp filed Critical Merck Sharp & Dohme
Publication of BRPI0616264A2 publication Critical patent/BRPI0616264A2/pt
Publication of BRPI0616264B1 publication Critical patent/BRPI0616264B1/pt
Publication of BRPI0616264B8 publication Critical patent/BRPI0616264B8/pt

Links

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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/14—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
    • A61P25/18—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
    • A61P25/24—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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

7-[2-[4-(6-flúor-3-m eti l-1 ,2-benzissoxazol-5-il)-1-piperazinil]etil]-2-(1 -propinil)-7h-pirazol-[4,3-e]-[1 ,2,4]-triazol-[1 ,5-c]-pirimidin-5-amina. a presente invenção refere-se a composto que tem a fórmula estrutural i, ou um sal farmaceuticamente aceitável do mesmo, é descrito, bem como seu uso no tratamento de doenças do sistema nervoso central, em particular mal de parkinson, síndrome extra- piramidal, síndrome das pernas inquietas e distúrbio de hiperatividade com déficit de atenção, composições farmacêuticas compreendendo-os e combinações com outros agentes.
BRPI0616264A 2005-09-23 2006-09-21 composto 7-[2-[4-(6-flúor-3-metil-1,2-benzissoxazol-5- il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c]-pirimidin-5-amina, e, composição farmacêutica BRPI0616264B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US72002705P 2005-09-23 2005-09-23
US60/720,027 2005-09-23
PCT/US2006/037003 WO2007038284A1 (en) 2005-09-23 2006-09-21 7-[2-[4-(6-FLUORO-3-METHYL-1,2-BENZISOXAZOL-5-YL)-1-PIPERAZINYL]ETHYL]-2-(1-PROPYNYL)-7H-PYRAZOLO-[4,3-e]-[1,2,4]-TRIAZOLO-[1,5-c]-PYRIMIDIN-5 AMINE

Publications (3)

Publication Number Publication Date
BRPI0616264A2 BRPI0616264A2 (pt) 2011-06-14
BRPI0616264B1 BRPI0616264B1 (pt) 2020-12-22
BRPI0616264B8 true BRPI0616264B8 (pt) 2021-05-25

Family

ID=37487759

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0616264A BRPI0616264B8 (pt) 2005-09-23 2006-09-21 composto 7-[2-[4-(6-flúor-3-metil-1,2-benzissoxazol-5- il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c]-pirimidin-5-amina, e, composição farmacêutica

Country Status (30)

Country Link
US (2) US7572802B2 (pt)
EP (1) EP1937687B1 (pt)
JP (1) JP4808779B2 (pt)
KR (1) KR101396614B1 (pt)
CN (2) CN102716131B (pt)
AR (1) AR056080A1 (pt)
AT (1) ATE503759T1 (pt)
AU (1) AU2006294633B8 (pt)
BR (1) BRPI0616264B8 (pt)
CA (1) CA2623047C (pt)
CY (1) CY1111921T1 (pt)
DE (1) DE602006021042D1 (pt)
DK (1) DK1937687T3 (pt)
EC (1) ECSP088297A (pt)
ES (1) ES2361856T3 (pt)
HR (1) HRP20110466T1 (pt)
IL (1) IL190275A (pt)
MY (1) MY146429A (pt)
NO (1) NO341760B1 (pt)
NZ (1) NZ566737A (pt)
PE (1) PE20070521A1 (pt)
PL (1) PL1937687T3 (pt)
PT (1) PT1937687E (pt)
RS (1) RS51702B (pt)
RU (1) RU2417997C2 (pt)
SG (1) SG165419A1 (pt)
SI (1) SI1937687T1 (pt)
TW (1) TWI335329B (pt)
WO (1) WO2007038284A1 (pt)
ZA (1) ZA200802550B (pt)

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NZ527142A (en) 2003-07-23 2006-03-31 Douglas Pharmaceuticals Ltd A stable suspension formulation
US7691869B2 (en) 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
AU2010222289B2 (en) 2009-03-13 2013-07-11 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
WO2011017299A2 (en) 2009-08-07 2011-02-10 Schering Corporation PROCESS FOR PREPARING A 2-ALKYNYL SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE
WO2011101861A1 (en) 2010-01-29 2011-08-25 Msn Laboratories Limited Process for preparation of dpp-iv inhibitors
JP5843869B2 (ja) * 2010-09-24 2016-01-13 アドヴィナス・セラピューティックス・リミテッド アデノシン受容体拮抗薬としての縮合三環化合物
WO2012135083A1 (en) * 2011-03-31 2012-10-04 Merck Sharp & Dohme Corp. METABOLITES OF 7-(2-(4-(6-FLUORO-3-METHYLBENZO[d]ISOXAZOL-5-YL)PIPERAZIN-1-YL)ETHYL)-2-(PROP-1-YNYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS
WO2014101113A1 (en) * 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Piperazine-substituted 7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
WO2014101120A1 (en) 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
WO2014128882A1 (ja) * 2013-02-21 2014-08-28 医療法人 和楽会 不安うつ病の治療薬
WO2015027431A1 (en) 2013-08-29 2015-03-05 Merck Sharp & Dohme Corp. 2,2-difluorodioxolo a2a receptor antagonists
US10590086B2 (en) 2014-11-03 2020-03-17 Iomet Pharma Ltd. Pharmaceutical compound
WO2016089796A1 (en) * 2014-12-04 2016-06-09 Merck Sharp & Dohme Corp. Formulation inhibiting effects of low acid environment
CN106543095B (zh) * 2016-09-23 2019-03-05 江苏大学 一种基于2-羟基苯乙酮肟及其衍生物一锅制备苯并异噁唑的方法
EP3723754A4 (en) 2017-12-13 2021-05-19 Merck Sharp & Dohme Corp. IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST
CN110742893B (zh) * 2018-07-23 2024-04-05 百济神州(北京)生物科技有限公司 A2a受体拮抗剂治疗癌症的方法
CN113329791A (zh) 2018-11-30 2021-08-31 默沙东公司 作为腺苷受体拮抗剂的9-取代的氨基三唑并喹唑啉衍生物、药物组合物及其用途

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SE462170B (sv) 1987-10-27 1990-05-14 Aahlstrom Corp Avlaegsnande av loesta och kolloidala makromolekylaera organiska aemnen ur effluenter
IT1264901B1 (it) 1993-06-29 1996-10-17 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina
WO1995003806A1 (en) 1993-07-27 1995-02-09 Kyowa Hakko Kogyo Co., Ltd. Remedy for parkinson's disease
IT1275420B (it) 1995-06-02 1997-08-05 Schering Plough S P A Metodo per misurare l'affinita' di legame al recettore a2a dell'adenosina di componenti di interesse farmacologico mediante l'uso del ligando triziato (3h)-sch 58261
IT1277392B1 (it) 1995-07-28 1997-11-10 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina
DE19604919A1 (de) * 1996-02-01 1997-08-07 Schering Ag Neue 2,3-Benzodiazepinderivate, deren Herstellung und Verwendung als Arzneimittel
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Also Published As

Publication number Publication date
CA2623047C (en) 2013-04-23
RU2008115239A (ru) 2009-10-27
AU2006294633A1 (en) 2007-04-05
CN102716131A (zh) 2012-10-10
KR20080047423A (ko) 2008-05-28
PL1937687T3 (pl) 2011-09-30
TW200730531A (en) 2007-08-16
AR056080A1 (es) 2007-09-19
BRPI0616264B1 (pt) 2020-12-22
CA2623047A1 (en) 2007-04-05
AU2006294633A8 (en) 2012-03-29
CN101273045A (zh) 2008-09-24
AU2006294633B8 (en) 2012-03-29
ECSP088297A (es) 2008-04-28
ES2361856T3 (es) 2011-06-22
DK1937687T3 (da) 2011-07-18
AU2006294633B2 (en) 2012-03-01
PE20070521A1 (es) 2007-07-13
ZA200802550B (en) 2009-06-24
RS51702B (sr) 2011-10-31
TWI335329B (en) 2011-01-01
KR101396614B1 (ko) 2014-05-16
JP2009509959A (ja) 2009-03-12
WO2007038284A1 (en) 2007-04-05
US8389532B2 (en) 2013-03-05
MY146429A (en) 2012-08-15
BRPI0616264A2 (pt) 2011-06-14
NO341760B1 (no) 2018-01-15
JP4808779B2 (ja) 2011-11-02
ATE503759T1 (de) 2011-04-15
EP1937687A1 (en) 2008-07-02
RU2417997C2 (ru) 2011-05-10
IL190275A0 (en) 2009-09-22
US7572802B2 (en) 2009-08-11
CN102716131B (zh) 2014-04-23
HRP20110466T1 (hr) 2011-08-31
HK1119681A1 (en) 2009-03-13
US20090270432A1 (en) 2009-10-29
NZ566737A (en) 2011-09-30
US20070072867A1 (en) 2007-03-29
DE602006021042D1 (de) 2011-05-12
CY1111921T1 (el) 2015-11-04
EP1937687B1 (en) 2011-03-30
SG165419A1 (en) 2010-10-28
NO20081924L (no) 2008-05-22
CN101273045B (zh) 2012-02-01
IL190275A (en) 2014-06-30
PT1937687E (pt) 2011-06-01
SI1937687T1 (sl) 2011-07-29

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