[EN] DUAL-ACTING ANTIHYPERTENSIVE AGENTS<br/>[FR] AGENTS ANTIHYPERTENSIFS À DOUBLE ACTION
申请人:THERAVANCE INC
公开号:WO2009035543A1
公开(公告)日:2009-03-19
The invention relates to compounds having the formula: (I) wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly)
n
, where one of the positions Xaa or Yaa is a bulky, non-electron withdrawing proline derivative. By substituting a proline derivative at either the Xaa or Yaa position in the native collagen helix, the stability of the helix is increased due solely to steric effects relative to prior known collagen-related triple helices. Methods are also disclosed for making the novel collagen mimics.
STABILIZATION OF THE COLLAGEN TRIPLE HELIX BY O-METHYLATION OF HYDROXYPROLINE RESIDUES
申请人:Raines Ronald T.
公开号:US20090264626A1
公开(公告)日:2009-10-22
This invention relates to a collagen polypeptide comprising a tripeptide motif having the formula (ProYaaGly)
n
, where Yaa is an O-methylated amino acid residue and “n” is the number of motif repeats. Preferred O-methylated amino acid residues at the Yaa position include (2S,4R)-4-methoxyproline. Other suitable amino acid residues at that position include O-mono or O-di-halogenated methylproline. Also, disclosed is a method of making a synthetic or a semi-synthetic collagen polypeptide molecule having increased stability relative to natural collagen. The strengthened collagen molecules are suitable for use in biomaterials for the medical field or in leather-related products prepared by the tanning industry.
[EN] ARYL DERIVATIVES FOR TREATING TRPM3 MEDIATED DISORDERS<br/>[FR] DÉRIVÉS D'ARYLE POUR LE TRAITEMENT DE TROUBLES À MÉDIATION PAR TRPM3
申请人:UNIV LEUVEN KATH
公开号:WO2022112345A1
公开(公告)日:2022-06-02
The invention relates to compounds that are useful for the prevention or treatment of TRPM3 mediated disorders, more in particular disorders selected from pain and inflammatory hypersensitivity. The invention also relates to a method for the prevention or treatment of said TRPM3 mediated disorders.
[EN] HETEROCYCLE DERIVATIVES FOR TREATING TRPM3 MEDIATED DISORDERS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES POUR LE TRAITEMENT DE TROUBLES À MÉDIATION PAR TRPM3
申请人:UNIV LEUVEN KATH
公开号:WO2022112352A1
公开(公告)日:2022-06-02
The invention relates to compounds that are useful for the prevention or treatment of TRPM3 mediated disorders, more in particular disorders selected from pain and inflammatory hypersensitivity. The invention also relates to a method for the prevention or treatment of said TRPM3 mediated disorders.