Patent classifications
C07K5/097
MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS
The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:
##STR00001##
which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
NOVEL COMPOUNDS
The present invention relates to novel compounds which effectively inhibit the melanin synthesis in human melanocytes and are thus suitable for the treatment of senile lentigines, for smoothening skin color irregularities and/or for lightening natural skin color.
Process for preparing compounds having triple activities of thrombolysis, antithrombosis, and radical scavenging
The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: ##STR00001##
wherein the definitions of T, Q, R.sub.1 and R.sub.2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.
Collagen mimics
Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly).sub.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.
Indoline compounds as granzyme B inhibitors
Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B.
Pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the peptide having the ability to inhibit angiotensin-1 converting enzyme as an active ingredient
The present invention relates to a peptide separated from the fraction of oyster enzyme hydrate displaying the ability of suppressing angiotensin converting enzyme (ACE) and a pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the said peptide as an active ingredient. Particularly, the peptide separated from the fraction of the oyster enzyme hydrate of the present invention significantly inhibits ACE activity, and thus brings blood pressure regulating effect and antihypertensive effect. Therefore, the fraction of the oyster enzyme hydrate of the invention or the peptide separated from the same can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of cardiovascular disease.
Process for the Preparation of Cyclic Depsipeptides
Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R.sub.1-R.sub.7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described.
##STR00001##
Pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the peptide having the ability to inhibit angiotensin-1 converting enzyme as an active ingredient
The present invention relates to a peptide separated from the fraction of oyster enzyme hydrolysate displaying the ability of suppressing angiotensin converting enzyme (ACE) and a pharmaceutical composition for the prevention and treatment of cardiovascular disease comprising the said peptide as an active ingredient. Particularly, the peptide separated from the fraction of the oyster enzyme hydrolysate of the present invention significantly inhibits ACE activity, and thus brings blood pressure regulating effect and antihypertensive effect. Therefore, the fraction of the oyster enzyme hydrolysate of the invention or the peptide separated from the same can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of cardiovascular disease.
Humidity-responsive tripeptide crystal
A thin film that has a flexible polymer layer and a peptide layer. The peptide layer is disposed on the flexible polymer layer and has a peptide selected from HYF, DYF and YFD. The thin film reversibly curves with changes in humidity.
Peptide macrocycles against <i>Acinetobacter baumannii</i>
The present invention provides compounds of formula (I) ##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.