1266727-98-3

Upstream product

• 64695-84-7 2-bromo-4,5-difluorobenzoic acid 
• 476620-55-0 (2-bromo-4,5-difluorophenyl)methanol 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 1307796-07-1 tert-butyl (1R,3'R)-3'-(5-{2-[2-(acetylamino)ethyl]phenyl}-4-bromo-3-isoxazolyl)-5,6-difluoro-1'H,3H-spiro[2-benzofuran-1,4'-piperidine]-1'-carboxylate 
• 1307795-04-5 N-[2-(2-(4-bromo-3-[(1R,3'R)-5,6-difluoro-3H-spiro[2-benzofuran-1,4'-piperidin]-3'-yl]-5-isoxazolyl)phenyl)ethyl]acetamide 
• 1266727-99-4 1-tert-butyl 3-ethyl 4-[2-({[tert-butyl(dimethyl)silyl]oxy}methyl)-4,5-difluorophenyl]-5,6-dihydro-1,3(2H)-pyridinedicarboxylate 
• 1360574-65-7 C₂₄H₂₂ClF₅N₂O₃ 
• 1360574-64-6 C₂₉H₃₀ClF₅N₂O₅ 
• 1360574-63-5 C₂₉H₂₈ClF₅N₂O₅ 

Relevant academic research and scientific papers

Renin inhibitors for the treatment of hypertension: Design and optimization of a novel series of spirocyclic piperidines

The discovery and SAR of a novel series of spirocyclic renin inhibitors are described herein. It was found that by restricting the northern aromatic plate to the bioactive conformation through spirocyclization, increase in renin potency and decrease in hE

RENIN INHIBITORS

Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6 -alkyl or C3-6 -cycloalkyl, wherein said C1-6 -alkyl or C3-6 -cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or -(C=O)-, -CH(OH)-, -CH2- or =CH-; U is a bond or -CH2-, or for the case when V is =CH-, U is -CH=; X is =CH-, =CF-, =C(OR3)-, or -C=O-; and Y is =CH-, =CF-, =N-, or for the case when X is -C=O-, Y is -N(R3)-.

SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS

Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH2- or =CH-; U is a bond or -CH2-, or, when V iS =CH-, U is-CH=; X is =CH-, =CF-, =C(OR3)-, or -(C=O)-; and Y is =CH-, =CF-, =N-, or, for the case when X is -(C=O)-, Y is -N(R3)-.