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AR082661A1 - 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
AR082661A1
AR082661A1 ARP110102892A ARP110102892A AR082661A1 AR 082661 A1 AR082661 A1 AR 082661A1 AR P110102892 A ARP110102892 A AR P110102892A AR P110102892 A ARP110102892 A AR P110102892A AR 082661 A1 AR082661 A1 AR 082661A1
Authority
AR
Argentina
Prior art keywords
heteroatoms
alkyl
positions
optionally substituted
cycloalkyl
Prior art date
Application number
ARP110102892A
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English (en)
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Biolab Sanus Farmaceutica Ltda
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Publication date
Application filed by Biolab Sanus Farmaceutica Ltda filed Critical Biolab Sanus Farmaceutica Ltda
Publication of AR082661A1 publication Critical patent/AR082661A1/es

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

Abstract

Describe 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-dibenzodioxol-5-il)-1-(1H-indol-3-il)-7-metil-6,7-dihidro[1,3]oxazolo[3,4-a]pirazin-5,8-diona, su enantiómero (S)-3-(1,3-dibenzodioxol-5-il)-1-(1H-indol-3-il)-7-metil-6,7-dihidro[1,3]oxazolo[3,4-a]pirazin-5,8-diona. 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 la disfunción eréctil y trastornos tratables con inhibidor de PDE-5.Reivindicación 1: Un compuesto de la fórmula (1) o sus sales, solvatos o hidratos; en donde R1 es un grupo aromático, opcionalmente condensado, opcionalmente sustituido con RB en una o más posiciones; un grupo heteroaromático que contiene uno o más heteroátomos, opcionalmente sustituido con RB o un grupo indol en una o más posiciones; un alquenil C1-6-carbonilo, opcionalmente sustituido con RB en una o más posiciones; un aromático bicíclico, opcionalmente sustituido con RB en una o más posiciones o un heteroaromático bicíclico que contiene uno o más heteroátomos, opcionalmente sustituido con RB en una o más posiciones; RB es un halógeno, hidroxilo, nitrógeno, ciano, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-3, arilalquilo C1-3 o heteroarilalquilo C1-3; R2 es un grupo aromático que contiene uno o más heteroátomos, un grupo heteroaromático que contiene uno o más heteroátomos o grupos metileno-3,4-dioxifenilo o uno aromático bicíclico que contiene uno o más heteroátomos o grupos metileno-3,4-dioxifenilo; R3 es hidrógeno, halógeno, haloalquilo C1-6, heteroalquilo C1-3, o alquilo C1-3; y R4 es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-3, arilalquilo C1-3 o heteroarilalquilo C1-3.
ARP110102892A 2010-08-13 2011-08-09 DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO[3,4-a]PIRAZIN-5,8-DIONA AR082661A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37348310P 2010-08-13 2010-08-13

Publications (1)

Publication Number Publication Date
AR082661A1 true AR082661A1 (es) 2012-12-26

Family

ID=45023415

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102892A AR082661A1 (es) 2010-08-13 2011-08-09 DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO[3,4-a]PIRAZIN-5,8-DIONA

Country Status (20)

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)
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
CN114751905A (zh) * 2014-09-12 2022-07-15 生物实验萨纽斯药物有限公司 新的吡啶并嘧啶衍生物化合物、其药物组合物及其用途
MX2021015425A (es) * 2019-07-15 2022-02-21 Biolab Sanus Farmaceutica Ltda Estereoisomeros del compuesto 3-(benzo[d][1,3]dioxol-5-il)-7-(1-hi droxipropano-2-il)-1-(1h-indol-3-il)-6,7-dihidro-3h-oxazol[3,4-a] pirazina-5,8-diona y su uso como antitumoral y inhibidor de la enzima fosfodiesterasa.

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996026940A1 (en) 1995-03-01 1996-09-06 Kyowa Hakko Kogyo Co., Ltd. Imidazoquinazoline derivatives
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.
CA2445189C (en) 2001-06-21 2009-02-17 Lilly Icos Llc Carboline derivatives as pdev inhibitors
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.
CA2562251C (en) 2004-04-07 2009-04-28 Pfizer Inc. Pyrazolo'4,3-d pyrimidines
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
RU2013110795A (ru) 2014-09-20
EP2603512A4 (en) 2014-07-16
CL2013000434A1 (es) 2013-06-07
RU2581831C2 (ru) 2016-04-20
CA2807872C (en) 2018-07-24
WO2012019254A1 (en) 2012-02-16
KR101871856B1 (ko) 2018-06-28
MX2013001692A (es) 2013-03-18
DK2603512T3 (en) 2016-04-04
BR112013003225A2 (pt) 2016-06-07
EP2603512A1 (en) 2013-06-19
ECSP13012486A (es) 2013-04-30
BR112013003225B1 (pt) 2021-03-30
PL2603512T3 (pl) 2016-09-30
HUE027903T2 (hu) 2016-11-28
KR20130109110A (ko) 2013-10-07
US8338432B2 (en) 2012-12-25
UY33535A (es) 2011-12-01
HK1184786A1 (zh) 2014-01-30
CN103108878A (zh) 2013-05-15
ES2565493T3 (es) 2016-04-05
CO6680703A2 (es) 2013-05-31
MX347632B (es) 2017-05-04
US20120040988A1 (en) 2012-02-16
CN103108878B (zh) 2016-01-27
JP5940535B2 (ja) 2016-06-29
JP2013533290A (ja) 2013-08-22
EP2603512B1 (en) 2015-12-30
IL224683A (en) 2016-03-31
CA2807872A1 (en) 2012-02-16

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