AR076836A1 - Inhibidores del canal de potasio medular externo renal - Google Patents

Inhibidores del canal de potasio medular externo renal

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Publication number
AR076836A1
AR076836A1 ARP100101504A AR076836A1 AR 076836 A1 AR076836 A1 AR 076836A1 AR P100101504 A ARP100101504 A AR P100101504A AR 076836 A1 AR076836 A1 AR 076836A1
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Argentina
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group
optionally substituted
independently selected
3alkyl
oxo
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Merck Sharp & Dohme
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Publication of AR076836A1 publication Critical patent/AR076836A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
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    • 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
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
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    • 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
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    • A61P7/10—Antioedematous agents; Diuretics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • C07D487/02—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 two hetero rings
    • C07D487/08—Bridged systems
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    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyrane Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Los compuestos de formula 1 son utiles como diuréticos y natriuréticos y por lo tanto son utiles para la terapia y la profilaxis de trastornos resultantes de una retencion de sales y agua excesiva, incluyendo enfermedades cardiovasculares tales como hipertension e insuficiencia cardiaca cronica y aguda. Reivindicacion 1: Un compuesto que tiene la formula estructural (1) y las sales farmacéuticamente aceptables del mismo, en el que formula (2) representa un anillo heterocíclico seleccionado entre el grupo que consiste en el grupo de formulas (3); Z1 se selecciona entre el grupo que consiste en formulas (4); Z2 se selecciona entre el grupo que consiste en formulas (5); X se selecciona entre el grupo que consiste en -H, -OH, -Oalquilo C1-3, -F, oxo, NH2 y -CH3; Y se selecciona entre el grupo que consiste en -H, -OH, -Oalquilo C1-3, -F, oxo, NH2 y -CH3; cada uno de X1 e Y1 se selecciona independientemente entre el grupo que consiste en -H y -CH3; cada uno de X2 e Y2 es -O-; con la condicion de que cuando X sea oxo entonces X1 esté ausente y cuando Y sea oxo entonces Y1 esté ausente; y con la condicion adicional de que cuando ni X2 ni Y2 estén presentes, entonces al menos uno de X e Y se seleccione entre el grupo que consiste en -OH, -Oalquilo C1-3, -F y oxo; cada uno de R1 y R2 se selecciona independientemente entre el grupo que consiste en -H, -halo, -cicloalquilo C3-6, -OR8, -SR8, -SOR8, -SO2R8, -(CH2)nOR8 y alquilo C1-6 opcionalmente sustituido con 1-3 de -F; uno de R3a y R3b se selecciona entre el grupo que consiste en -CN y -NO2 y el otro es Re; uno de R4a y R4b se selecciona entre el grupo que consiste en -CN y -NO2 y el otro es Rf; cada uno de R5 y R6 se selecciona independientemente entre el grupo que consiste en -H, -alquilo C1-6, -cicloalquilo C3-6, -CF3, -CHF2, -CH2F y -CH2OH; R7 se selecciona entre el grupo que consiste en -H, -CH3, -CF3, -CH2F, -CHF2 y -CH2OH; cada uno de Ra y Rb se selecciona independientemente entre el grupo que consiste en (a) -H, (b) halo, (c) -alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (d) -cicloalquilo C3-6, (e) -Oalquilo C1-3 opcionalmente sustituido con 1-3 de -F, (f) -OR8, (g) -CO2alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (h) -(CH2)nOR8, (i) -SR8 , (j) -SOR8, (k) -SO2R8, (l) -NHCOR8 y (m) -NHSO2R8; cada uno de Rc y Rd se selecciona independientemente entre el grupo que consiste en (a) -H, (b) halo, (c) -alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (d) -cicloalquilo C3-6, (e) -Oalquilo C1-3 opcionalmente sustituido con 1-3 de -F, (f) -OR8, (g) -CO2alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (h) -(CH2)OR8, (i) -SR8, (j) -SOR8, (k) -SO2R8, (l) -NHCOR8 y (m) -NHSO2R8; cada uno de Re y Rf se selecciona independientemente entre el grupo que consiste en (a) -H, (b) halo, (c) -alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (d) -cicloalquilo C3-6, (e) -Oalquilo C1-3 opcionalmente sustituido con 1-3 de -F, (f) -OR8, (g) - CO2alquilo C1-6 opcionalmente sustituido con 1-3 de -F, (h) -(CH2)nOR8 , (i) -SR , (j) -SOR8, (k) -SO2R8, (l) -NHCOR8 y (m) -NHSO2R8; n es un numero entero seleccionado entre 1, 2 y 3; y R8 se selecciona independientemente en cada caso entre el grupo que consiste en - H, -cicloalquilo C3-6 y -alquilo C1-6 opcionalmente sustituido con 1-3 de -F.
ARP100101504 2009-05-06 2010-05-04 Inhibidores del canal de potasio medular externo renal AR076836A1 (es)

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US17584709P 2009-05-06 2009-05-06

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AR076836A1 true AR076836A1 (es) 2011-07-13

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US (2) US8673920B2 (es)
EP (1) EP2427444B1 (es)
JP (2) JP5092068B2 (es)
KR (1) KR101373902B1 (es)
CN (1) CN102459216B (es)
AR (1) AR076836A1 (es)
AU (1) AU2010246269C1 (es)
BR (1) BRPI1014050A2 (es)
CA (1) CA2759399C (es)
CL (1) CL2011002761A1 (es)
CO (1) CO6460758A2 (es)
CR (1) CR20110578A (es)
EA (1) EA021008B1 (es)
EC (1) ECSP11011444A (es)
ES (1) ES2561654T3 (es)
GE (1) GEP20146055B (es)
GT (1) GT201100278A (es)
HN (1) HN2011002933A (es)
IL (1) IL215836A0 (es)
MA (1) MA33342B1 (es)
MX (1) MX337570B (es)
MY (1) MY157525A (es)
NI (1) NI201100193A (es)
NZ (1) NZ596229A (es)
PE (1) PE20120346A1 (es)
SG (1) SG175841A1 (es)
TN (1) TN2011000540A1 (es)
TW (1) TWI408135B (es)
UA (1) UA106611C2 (es)
WO (1) WO2010129379A1 (es)
ZA (1) ZA201108070B (es)

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WO2012058116A1 (en) 2010-10-27 2012-05-03 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2632464B1 (en) 2010-10-29 2015-04-29 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
JP2014513116A (ja) 2011-05-02 2014-05-29 ゾエティス・エルエルシー 抗菌剤として有用な新規セファロスポリン
RU2014110401A (ru) 2011-08-19 2015-09-27 Мерк Шарп И Доум Корп. Ингибиторы внешнего медуллярного калиевого канала почек
WO2013039802A1 (en) * 2011-09-16 2013-03-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US8999990B2 (en) 2011-10-25 2015-04-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US8999991B2 (en) 2011-10-25 2015-04-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013066717A1 (en) * 2011-10-31 2013-05-10 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773351B1 (en) * 2011-10-31 2017-08-23 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9139585B2 (en) 2011-10-31 2015-09-22 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
US9206199B2 (en) 2011-12-16 2015-12-08 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013102935A2 (en) * 2012-01-03 2013-07-11 Council Of Scientific & Industrial Research Cu-MEDIATED ANNULATION FOR THE EFFECTIVE SYNTHESIS OF 3-SUBSTITUTED PHTHALIDES
WO2014015495A1 (en) * 2012-07-26 2014-01-30 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
AR092031A1 (es) 2012-07-26 2015-03-18 Merck Sharp & Dohme Inhibidores del canal de potasio medular externo renal
EP2925322B1 (en) * 2012-11-29 2018-10-24 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2934533B1 (en) 2012-12-19 2017-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2956142B1 (en) 2013-02-18 2017-09-20 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014150132A1 (en) 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2015017305A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp Inhibitors of the renal outer medullary potassium channel
WO2015065866A1 (en) * 2013-10-31 2015-05-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US10000484B2 (en) 2013-12-18 2018-06-19 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassim channel
WO2015096035A1 (en) 2013-12-24 2015-07-02 Merck Sharp & Dohme Corp. Inhibitors of renal outer medullary potassium channel
WO2015103756A1 (en) * 2014-01-09 2015-07-16 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
KR20160001316A (ko) 2014-06-27 2016-01-06 조선대학교산학협력단 3ｄ 조영기술을 이용한 환자 맞춤형 임플란트 모형제작방법
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