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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:
ARP130102534
公开号:
AR092031A1
申请日:
2013.07.16
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
They are inhibitors of Channel romk (kir1.1). The compounds can be used as diuretic and natriuretic agents and / or for Therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and Cardiac conditions associated with excessive retention of Salt and Water. Romk (kir1.1) kir1.1 renal medullary canal of External potassium.Claim 1: a compound having the Structural formula (1) or a pharmaceutically acceptable Salt thereof in the r u00b9 is: H -, Halo - or Oh - or - alkyl c u2081 u208b u2083; M is an integer between zero (Selected r u00b3 u1d47 is absent) and 1 (r u00b3 u1d47 is present); n is a integer s Eleccionado between 1 or 2; R u00b2 is selected independently at each occurrence between H = or (oxo), - Oh,C u2081 u208b u2083 alkyl or alkyl c u2081 u208b u2083, with the condition that when n is 2, then at least a R u00b2 is - H; r u00b3 u1d43 is H = alkyl or cycloalkyl, optionally substituted with c u2083 u208b u2084 or c u2081 u208b u2083 - och u2083 or 1 to 3 - F, with the condition that only one or R u00b2 can be r u00b3 u1d43 = o; R u00b3 u1d47 is H or alkyl c u2081 u208b u2083,R u00b3 u1d47 is absent or when r u00b3 u1d43 IS = o or discontinuous Double when the link is a link or a link or r u00b3 u1d43 Aromatic; and r u00b3 u1d47 are United together with the carbon to which both are United to form ciclopropilo or ciclobutilo; or when n is 1,R u00b2 and r u00b3 u1d43 can be United together with the carbon to which each one is United to form (i) a phenyl ring is Condensed with the pyrrolidine ring and M is Zero, or (ii) a Ring of ciclopropilo condensate with the pyrrolidine ring and M is 1; r u2074 is - H OR = or r u2075 is (A); Halo - H, (b), (c) c u2081 u208b u2083 optionally substituted with alkyl or alkyl c u2081 u208b u2083,(d) - (e) c u2083 u208b u2086 cycloalkyl or Heterocyclic optionally substituted with alkyl c u2081 u208b u2083 or Halo; r u2076 is H or alkyl c u2081 u208b u2083; r u2077 u1d43 is
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