MX347632B - Derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazin-5,8-diona. - Google Patents

Derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazin-5,8-diona.

Info

Publication number
MX347632B
MX347632B MX2013001692A MX2013001692A MX347632B MX 347632 B MX347632 B MX 347632B MX 2013001692 A MX2013001692 A MX 2013001692A MX 2013001692 A MX2013001692 A MX 2013001692A MX 347632 B MX347632 B MX 347632B
Authority
MX
Mexico
Prior art keywords
oxazolo
pyrazine
dione
dihydro
pde
Prior art date
Application number
MX2013001692A
Other languages
English (en)
Other versions
MX2013001692A (es
Inventor
Franz Keppler Artur
Luiz Sacurai Sérgio
Eduardo Da Costa Touzarim Carlos
Henrique Zaim Márcio
De Nucci Gilberto
Original Assignee
Biolab Sanus Farmacêutica Ltda *
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 Biolab Sanus Farmacêutica Ltda * filed Critical Biolab Sanus Farmacêutica Ltda *
Publication of MX2013001692A publication Critical patent/MX2013001692A/es
Publication of MX347632B publication Critical patent/MX347632B/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/04Drugs for disorders of the urinary system for urolithiasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D503/00Heterocyclic compounds containing 4-oxa-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. oxapenicillins, clavulanic acid derivatives; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D503/02Preparation
    • C07D503/04Preparation by forming the ring or condensed ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención describes una serie de derivados de 6, 7-dihidro-3H-oxazolo[3, 4-a]pirazin-5, 8-diona, sus mezclas, sus sales farmacéuticamente aceptables, que son inhibidores de PDE-5, que poseen propiedades vasodilatadoras y efectos de relajación. En particular, el derivado (R)-3-(1, 3-benzodioxol-5-il)-1-(1H-ind ol-3-il)-7-metil-6, 7-dihidro[1, 3joxazolo[3, 4-a]pirazin-5, 8-diona, su enantiómero (S)-3-(1, 3-benzodioxol-5-il)-1-(1 H-indol-3-il)-7-metil-6, 7-dihidro[1, 3]oxazolo[3,4-a]pirazin-5, 8-diona. La presente invención describe, además, procesos para la preparación de dichos compuestos, composiciones farmacéuticas que los contienen, así como usos como inhibidores de la enzima fosfodiesterasa de tipo 5 (PDE-5) en el tratamiento de te disfunción eréctil y trastornos tratables con inhibidor de PDE-5.
MX2013001692A 2010-08-13 2011-08-02 Derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazin-5,8-diona. MX347632B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37348310P 2010-08-13 2010-08-13
PCT/BR2011/000255 WO2012019254A1 (en) 2010-08-13 2011-08-02 Derivatives of 6, 7-dihydro-3h-oxazolo [3, 4-a] pyrazine-5, 8- dione

Publications (2)

Publication Number Publication Date
MX2013001692A MX2013001692A (es) 2013-03-18
MX347632B true MX347632B (es) 2017-05-04

Family

ID=45023415

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013001692A MX347632B (es) 2010-08-13 2011-08-02 Derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazin-5,8-diona.

Country Status (21)

Country Link
US (1) US8338432B2 (es)
EP (1) EP2603512B1 (es)
JP (1) JP5940535B2 (es)
KR (1) KR101871856B1 (es)
CN (1) CN103108878B (es)
AR (1) AR082661A1 (es)
BR (1) BR112013003225B1 (es)
CA (1) CA2807872C (es)
CL (1) CL2013000434A1 (es)
CO (1) CO6680703A2 (es)
DK (1) DK2603512T3 (es)
EC (1) ECSP13012486A (es)
ES (1) ES2565493T3 (es)
HK (1) HK1184786A1 (es)
HU (1) HUE027903T2 (es)
IL (1) IL224683A (es)
MX (1) MX347632B (es)
PL (1) PL2603512T3 (es)
RU (1) RU2581831C2 (es)
UY (1) UY33535A (es)
WO (1) WO2012019254A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33535A (es) * 2010-08-13 2011-12-01 Biolab Sanus Farmaceutuca Limitada Derivados de 6,7-dihidro-3h-oxazolo[3,4]pirazin-5,8-diona
AR099523A1 (es) * 2014-02-24 2016-07-27 Biolab Sanus Farmacêutica Ltda Compuestos derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazina-5,8-diona
MX2017003067A (es) * 2014-09-12 2017-06-14 Biolab Sanus Farmacêutica Ltda Nuevos compuestos derivados de piridopirimidinas.
KR20220035048A (ko) * 2019-07-15 2022-03-21 바이오랩 세너스 팔마씨우티카 엘티디에이. 화합물 3-(벤조[d][1,3]디옥솔-5-일)-7-(1-하이드록시프로판-2-일)-1-(1H-인돌-3-일)-6,7-디하이드로-3H-옥사졸[3,4-a]피라진-5,8-디온의 입체이성질체 및 항종양제 및 포스포디에스테라제 효소 억제제로서의 이의 용도

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996026940A1 (fr) 1995-03-01 1996-09-06 Kyowa Hakko Kogyo Co., Ltd. Derives d'imidazoquinazoline
GB9514464D0 (en) * 1995-07-14 1995-09-13 Glaxo Lab Sa Medicaments
MXPA03011082A (es) * 2001-06-05 2004-07-08 Lilly Icos Llc Derivados de pirazino-1',2': 1,6-prirido-3,4-b-indol-1,4-diona.
DE60213798T2 (de) 2001-06-21 2007-08-16 Lilly Icos Llc, Wilmington Carbolinderivate als pdev inhibitoren
AR045950A1 (es) 2003-10-09 2005-11-16 Speedel Experimenta Ag Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos.
DK1742950T3 (da) 2004-04-07 2009-03-16 Pfizer Ltd Pyrazolo-[4,3-D]-pyrimidiner
RU2418590C2 (ru) * 2006-04-04 2011-05-20 Донг-А Фарматех Ко. Лтд. Средство для предупреждения и лечения гиперплазии предстательной железы, содержащее производное пиразолопиримидинона
BRPI0903803B1 (pt) * 2009-09-30 2019-07-09 Biolab Sanus Farmacêutica Ltda. Composto, processo de preparação, composição farmacêutica e uso dos compostos
UY33535A (es) * 2010-08-13 2011-12-01 Biolab Sanus Farmaceutuca Limitada Derivados de 6,7-dihidro-3h-oxazolo[3,4]pirazin-5,8-diona

Also Published As

Publication number Publication date
WO2012019254A1 (en) 2012-02-16
CO6680703A2 (es) 2013-05-31
MX2013001692A (es) 2013-03-18
HUE027903T2 (hu) 2016-11-28
CA2807872A1 (en) 2012-02-16
CL2013000434A1 (es) 2013-06-07
JP2013533290A (ja) 2013-08-22
ES2565493T3 (es) 2016-04-05
AR082661A1 (es) 2012-12-26
KR20130109110A (ko) 2013-10-07
CN103108878A (zh) 2013-05-15
BR112013003225A2 (pt) 2016-06-07
EP2603512A4 (en) 2014-07-16
CN103108878B (zh) 2016-01-27
UY33535A (es) 2011-12-01
ECSP13012486A (es) 2013-04-30
IL224683A (en) 2016-03-31
KR101871856B1 (ko) 2018-06-28
RU2581831C2 (ru) 2016-04-20
RU2013110795A (ru) 2014-09-20
US8338432B2 (en) 2012-12-25
CA2807872C (en) 2018-07-24
JP5940535B2 (ja) 2016-06-29
EP2603512A1 (en) 2013-06-19
PL2603512T3 (pl) 2016-09-30
US20120040988A1 (en) 2012-02-16
EP2603512B1 (en) 2015-12-30
DK2603512T3 (en) 2016-04-04
HK1184786A1 (zh) 2014-01-30
BR112013003225B1 (pt) 2021-03-30

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