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PE20120346A1 - Derivados de diazaheterociclos n, n-disustituidos como inhibidores del canal de potasio medular externo renal (romk) - Google Patents

Derivados de diazaheterociclos n, n-disustituidos como inhibidores del canal de potasio medular externo renal (romk)

Info

Publication number
PE20120346A1
PE20120346A1 PE2011001912A PE2011001912A PE20120346A1 PE 20120346 A1 PE20120346 A1 PE 20120346A1 PE 2011001912 A PE2011001912 A PE 2011001912A PE 2011001912 A PE2011001912 A PE 2011001912A PE 20120346 A1 PE20120346 A1 PE 20120346A1
Authority
PE
Peru
Prior art keywords
medular
romk
renal
inhibitors
hydroxy
Prior art date
Application number
PE2011001912A
Other languages
English (en)
Inventor
Alexander Pasternak
Aurash Shahripour
Nardos H Teumelsan
Lihu Yang
Yuping Zhu
Shawn P Walsh
Haifeng Tang
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20120346A1 publication Critical patent/PE20120346A1/es

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    • 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
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • 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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    • 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
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Abstract

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE EL ANILLO CON 2 N ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS; Z1 ES UN COMPUESTO DE FORMULA (z1-i), (z1-ii), ENTRE OTROS; Z2 ES UN COMPUESTO DE FORMULA (z2-i), (z2-ii), ENTRE OTROS, EN DONDE X E Y SON CADA UNO H, OH, -OALQUILO(C1-C3), F, ENTRE OTROS; X1 E Y1 SON CADA UNO H O CH3; R3a, R3b, R4a Y R4b SON CADA UNO CN, NO2, ENTRE OTROS; Ra Y Rb SON CADA UNO H, HALO, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON 1 A 3 DE -F, ENTRE OTROS; R5 Y R6 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-[(1S)-1-HIDROXI-2-{4-[(2R)-2-HIDROXI-2-(4-METIL-1-OXO-1,3-DIHIDRO-2-BENZOFURAN-5-IL)ETIL]PIPERAZIN-1-IL}ETIL]PIRIDIN-3-CARBONITRILO; 5,5'-{PIPERAZINA-1,4-DIILBIS[(1R)-1-HIDROXIETANO-2,1-DIIL]}BIS(4-METIL-2-BENZOFURAN-1(3H)-ONA); 6-[(1R)-1-HIDROXI-2-{4-[(2R)-2-HIDROXI-2-(4-METIL-1-OXO-1,3-DIHIDRO-2-BENZOFURAN-5-IL)ETIL]PIPERAZIN-1-IL}ETIL]-4-METOXIPIRIDIN-3-CARBONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL CANAL DE POTASIO MEDULAR EXTERNO RENAL (ROMK) SIENDO UTILES EN EL TRATAMIENTO DE HIPERTENSION
PE2011001912A 2009-05-06 2010-04-29 Derivados de diazaheterociclos n, n-disustituidos como inhibidores del canal de potasio medular externo renal (romk) PE20120346A1 (es)

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US17584709P 2009-05-06 2009-05-06

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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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