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Inhibitors of the renal Outer medullary Potassium Channel
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
申请号:
ARP120103364
公开号:
AR087853A1
申请日:
2012.09.13
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
1. This compound refers to the compound of structural formula (1) and the salt acceptable for drugs as an inhibitor of extracellular spinal potassium (ROMK) channel (kir1.1). Formula compound (1) plays the role of diuresis and natural therapy, thus helping to treat and prevent diseases caused by excessive salt and water consumption, including cardiovascular diseases such as hypertension, chronic and acute heart failure. Claim 1: a compound whose structural formula (1) or pharmaceutically acceptable salt, wherein: b1-zb-es b1-chr 1-8322 -,B -CHR C (O) -B -C (O) -B -CHR CH C (O) -B -OCH C (O) - o B -CH (CH OH) -ZA-A¹ is -CHR²¹CR²R²²-A¹,-CH = CR²-A¹,-C-A1,-S-A1,-CH₂O-A¹,-C (O) CHR -A-O-A1,-NHCHR²-A¹,-CH N (CH) CH CH (OH) -A-CH N (CH) CH (CH OH) -A-CH N (CH) -A-CH₂S-A¹,-CH₂O-A¹,CH S (O) -A-CH₂S (O₂) -A¹ or -NH-A¹;A1 is a compound selected from the preparation group (2);B1 is a compound composed of formula group (3);X is O or S; R¹ is -H, C₁₋₆ alkyl,C₃₋₆ cycloalkyl,CF8323,-OH, F, -CH₂OH, -C (O) OH, -C (O) O-C₁₋₆ alkyl or R alquilo can be attached to R¹³ᵇ by 2-3 carbon atoms or 1-2 carbon atoms and a heteroatom to form a ring; R² is -H, C₁₋₆ alkyl,C₃₋₆ cycloalkyl,CF8323,-OH, F, -CH₂OH, -C (O) OH, -C (O) O-C₁₋₆ or R² alkyl can be attached to R¹³ᵃ by 2-3 carbon atoms or 1-2 carbon atoms and a heteroatom to form a ring; R⁴ is H, -OH, F, -O-C₁₋₆ alkyl or C₁₋₆ alkyl or it can be attached to R⁵ by a bond or by 1-4 carbon atoms, to form a ring; R⁵ is H, -OH, F, -O-C₁₋₆ alkyl or C₁₋₆ alkyl or it can be attached to R⁴ by a bond or by 1-4 carbon atoms to form a ring; R⁶ is -H, C₁₋₆ alkyl,-C (O) O-C₁₋₆ alkyl,-OH, halogen, -OC (O) C₁₋₆ alkyl,-CH₂OH, -CHF₂,-N (C₁₋₆ alkyl) ₂,-C₆H₅,-CF₃ or a 5- or 6-membered heteroaryl ring with 1, 2, 3 or 4 heteroatoms; R¹³ᵃ is -H, C₁₋₆ alkyl,C₃₋₆ cycloalkyl,-Halogen, cf832323,-CH OH CO R-OR¹⁶ᵃ,-SR¹⁶ᵃ,-Cn-3 carbon atom or 1-2 carbon atom or 1-2 carbon atom and heteroatom can be combined to form a carbon-1-2-749191 ring or r8308 can be combined; 3-4 car
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来源网址:
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