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G - amino butyric acid substituted, processes and Intermediates for their PreparationThat includes a Pharmaceutical Composition and its use in the treatment of diseases mediated by inhibition of NEP
专利权人:
THERAVANCE; INC.
发明人:
HUGHES ADAM,FLEURY MELISSA,GENDRON ROLAND
申请号:
ARP120100547
公开号:
AR085280A1
申请日:
2012.02.17
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
These compounds have neprilisina inhibition activity.Pharmaceutical compositions comprising such Compounds Methods of using such compounds to uses of same in Therapeutics and processes and Intermediates for preparing such compounds.Claim 1: wherein is a compound of formula (1), where R1 is selected from - and - or7 nr8r9 2a is selected from - CH2OH, ch2op (- OR) (OH) 2- ch2oc and (OR) CH (NH2 or 2a R37) taken together with - CH2O - R7 to form cr18r19 - or taken along with R8 to form - CH2O - C (o) - R2B is selected from H and CH3,Or taken together to form 2A - CH2 - or - CH2 -, Z is selected between ch and N X is a heteroaryl C1 - 9 R3 is absent or is selected from h Halo rent C0 - 5 - Oh, - NH2, - C1 alkyl6. NF3 cycloalkyl - C3 - 7 rent C0 or C1 - 2 - alkyl - 6, - C (o) - Rent R20 coor21 C0 - 1 -, - C (o) - NHC (or nr22r23 or R24) = NO2 - - C = N (CH3) (Oh) phenyl optionally substituted with one or two groups SelectOften independently between Halo, - Oh, - CF3, - OCH3, CH3 - NHC (OR)And naftalenilo pyridinyl pirazinilo phenyl pirazolilo optionally substituted with Methyl tiofenilo optionally substituted with Methyl or Halo furanilo and - CH2 - morfolinilo and R3When present,Attached to a carbon Atom R4 is absent or is selected from h Oh alkyl C1 - 6 - 2 - coor35 C1 rent - ch2oc (o) CH (NH2 - och2oc R36) (o) CH (NH2 - och2oc R36) (o) CH3. Ch2op (OR) - CH2 (OH) 2CH (OH) CH2OH [CH - ch (CH3) 2] - NHC (or C1 - 6) or alkyl, phenyl or benzyl pyridinyl and optionally substituted with one or More groups selected from coor35 Halo -, -, - and - OCH3, ocf3, scf3 and R4,When present, joins an atom of carbon or nitrogen R3 and R4 are taken together to form - fenilen - or - (CH2) 1 - 3 - or - fenilen - or - Choh - CH2 - CH2 - is 0 OR 1 R5 is selected from Halo, - CH3,- CF3, and - CN b is 0 or an integer between 1 and 3 each R6 is selected independently between Halo, - Oh, - and - CH3, OCH3, - Cf3 R7 is selected from h, alkyl C1 - 8 3 - aryl - Rent C1 - C6 - 10- Hire C1 - 3 - 9 -
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