AR075609A1 - Derivados pirazolicos heterociclicos nitrogenados activadores de guanilatociclasas solubles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares, entre otras. - Google Patents

Derivados pirazolicos heterociclicos nitrogenados activadores de guanilatociclasas solubles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares, entre otras.

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Publication number
AR075609A1
AR075609A1 ARP100100555A ARP100100555A AR075609A1 AR 075609 A1 AR075609 A1 AR 075609A1 AR P100100555 A ARP100100555 A AR P100100555A AR P100100555 A ARP100100555 A AR P100100555A AR 075609 A1 AR075609 A1 AR 075609A1
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AR
Argentina
Prior art keywords
group
substituted
optionally mono
3alkyl
substituents selected
Prior art date
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ARP100100555A
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English (en)
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Merck Sharp & Dohme
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Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of AR075609A1 publication Critical patent/AR075609A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos son utiles para el tratamiento o prevencion de enfermedades cardiovasculares, disfuncion endotelial, disfuncion diastolica, aterosclerosis, hipertension, hipertension pulmonar, angina de pecho, trombosis, reestenosis, infarto de miocardio, apoplejías, insuficiencia cardiaca, hipertonía pulmonar, disfuncion eréctil, asma bronquial, insuficiencia renal cronica, diabetes o cirrosis del hígado. Reivindicacion 1: Un compuesto de formula estructural (1) una sal farmacéuticamente aceptable del mismo, en el que: W se selecciona entre el grupo constituido por CH y N; Z se selecciona entre el grupo constituido por el grupo de formulas (2) y -(CH2)3-NR3R3a; R1 se selecciona entre el grupo constituido por -OH, -Oalquilo C1-6 y -N(R5)2; R2 se selecciona entre el grupo constituido por -perfluoroalquilo C1-2 y -NH2; R3 se selecciona entre el grupo constituido por: 1) -alquilo C1-6 sustituido por 1-3 de -F, 2)-COR4 y 3) -SO2R6; R3a se selecciona entre el grupo constituido por -H; -alquilo C1-3; cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F; y -CH2-cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F; R4 se selecciona entre el grupo constituido por: 1) -H, 2) -alquilo C1-3, 3) -Oalquilo C1-3, 4) -cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F, 5) -CH2-cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F, 6) -Ocicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F, y 7) -N(R5)2; R5 se selecciona independientemente en cada caso entre -H y -alquilo C1-3; R6 se selecciona entre el grupo constituido por -alquilo C1-3, -cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por -CH3 y -F; y -CH2-cicloalquilo C3-6 opcionalmente mono- o di-sustituido por uno o más sustituyentes seleccionados entre el grupo constituido por - CH3 y -F; R7 se selecciona entre el grupo constituido por -H y -CH3; Ra y Rb se seleccionan independientemente en cada caso entre -F, -CI y -alquilo C1-3 opcionalmente sustituido por 1-3 de -F; y Rc y Rd se seleccionan independientemente en cada caso entre -F, -Cl y -alquilo C1-3 opcionalmente sustituido por 1-3 de -F.
ARP100100555A 2009-02-26 2010-02-25 Derivados pirazolicos heterociclicos nitrogenados activadores de guanilatociclasas solubles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares, entre otras. AR075609A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20864809P 2009-02-26 2009-02-26

Publications (1)

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AR075609A1 true AR075609A1 (es) 2011-04-20

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ARP100100555A AR075609A1 (es) 2009-02-26 2010-02-25 Derivados pirazolicos heterociclicos nitrogenados activadores de guanilatociclasas solubles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares, entre otras.

Country Status (15)

Country Link
US (1) US8507512B2 (es)
EP (1) EP2401265B1 (es)
JP (1) JP5411300B2 (es)
KR (1) KR20110133034A (es)
CN (1) CN102414194A (es)
AR (1) AR075609A1 (es)
AU (1) AU2010218224B2 (es)
BR (1) BRPI1008793A2 (es)
CA (1) CA2753434C (es)
CO (1) CO6430463A2 (es)
IL (1) IL214559A0 (es)
MX (1) MX2011008952A (es)
RU (1) RU2011138970A (es)
TW (1) TW201035077A (es)
WO (1) WO2010099054A2 (es)

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WO2010099054A2 (en) 2010-09-02
IL214559A0 (en) 2011-09-27
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CO6430463A2 (es) 2012-04-30
CA2753434A1 (en) 2010-09-02
JP2012519169A (ja) 2012-08-23
US8507512B2 (en) 2013-08-13
MX2011008952A (es) 2011-09-27
JP5411300B2 (ja) 2014-02-12
AU2010218224B2 (en) 2013-06-27
CA2753434C (en) 2014-07-15
WO2010099054A3 (en) 2010-10-21
US20100216764A1 (en) 2010-08-26
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KR20110133034A (ko) 2011-12-09
RU2011138970A (ru) 2013-04-10

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