公开(公告)号：US20240400575A1

公开(公告)日：2024-12-05

申请号：US18798430

申请日：2024-08-08

Applicant: Universitat De Barcelona

Inventor： Sandra Codony Gisbert ,  Carlos Galdeano Cantador ,  Rosana Leiva Martínez ,  Andreea Larisa Turcu ,  Elena Valverde Murillo ,  Santiago Vázquez Cruz

IPC: C07D493/08 ,  C07C271/56 ,  C07C275/26 ,  C07C335/14 ,  C07D211/26 ,  C07D211/32 ,  C07D211/60 ,  C07D277/64 ,  C07D313/00

Abstract: The present invention relates to soluble epoxide hydrolase (sEH) inhibitors of formula (1) to processes for their obtention and to their therapeutic indications.

公开(公告)号：US20200079786A1

公开(公告)日：2020-03-12

申请号：US15746791

申请日：2016-07-25

Applicant: UNIVERSITAT DE BARCELONA

Inventor： Santiago Vázquez Cruz ,  Elena Valverde Murillo ,  Rosana Leiva Martínez ,  Manuel Vázquez Carrera ,  Sandra Codony Gisbert

IPC: C07D493/08

Abstract: N-(2-oxaadamantan-1-yl)ureas of formula I, where R3 is H, C1-C3 alkyl, cyclohexyl or phenyl; R is —[CH2]n—Y; n is 0-15; in —[CH2]n— 0-n/3 of the methylene groups are optionally replaced by non adjacent oxygen atoms; and Y is a 3- or 4-substituted phenyl, a 3- or 4-substituted cyclohexyl, a N-substituted piperidin-4-yl, a N-substituted piperidin-3-yl, a di- or tri-fluorosubstituted phenyl, 4-chloro-3-trifluoromethylphenyl, 3-chloro-4-trifluoromethylphenyl, 4-fluoro-3-trifluoromethylphenyl, or 3-fluoro-4-trifluoromethylphenyl; have epoxide hydrolase (sEH) inhibitory activities similar to those of their N-(adamantan-1-yl)urea analogs. Thus, compounds I are useful as API for the treatment of sEH mediated diseases. Besides, in general, compounds I have higher water solubilities and lower melting points, what make them more promising from the point of view of pharmacokinetics and formulation.