Patent classifications
C07K5/123
Phosphatidylinositol-3-kinase inhibitor and pharmaceutical composition
A substance contains a phosphatidylinositol-3-kinase (PI3K) inhibitor including a depsipeptide-class compound represented by formula (1), or a physiologically acceptable salt thereof that combines a PI3K inhibitory effect and an HDAC inhibitory effect to provide an anti-cancer pharmaceutical composition for the treatment of an intractable cancer.
METHOD OF MONOMERISATION OF RECOMBINANT ANTIBODY MOLECULES
The present invention provides method of increasing the percentage of monomer in a composition of recombinantly expressed antibody molecules characterised in that the antibody molecule comprises at least one Fv with specificity for an antigen of interest comprising one VH and one VL wherein said VH and VL are connected directly or indirectly via one or more linkers and are stabilised by a disulfide bond therebetween, said method comprises: a) a conversion step of treating the composition with a denaturant selected from urea and/or Guanidine hydrochloride; b) wherein step a) is performed in the presence of a reducing agent or after treatment with a reducing agent.
Conjugates of RGD peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses
Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.
SELF-ASSEMBLING ULTRASHORT ALIPHATIC CYCLIC PEPTIDES FOR BIOMEDICAL APPLICATIONS
The invention relates to cyclic peptides of 3-9 amino acids comprising 2-7 aliphatic and 0-2 polar amino acids that are capable of self-assembling, wherein said aliphatic amino acids are arranged in decreasing hydrophobicity from N- to C-terminus and at least a portion of the cyclic peptide has to have its amino acids in alternating D- and L-configuration, as well as their use in hydrogels as well as co-gels or co-hydrogels. The hydrogels of the invention may be used in nanomedicine or drug delivery, cell culture or alternatively in electronic devices.
MODULATION OF HEPATITIS B VIRUS CCCDNA TRANSCRIPTION
The present invention provides small molecule inhibitors of hepatitis B virus (HBV) covalently closed circular (ccc) DNA, which are useful as therapeutics in the management of chronic HBV. The compounds of the invention achieve epigenetic modification of the cccDNA, histone modification and histone deacetylase activity inhibition, thus modulating HBV cccDNA. The present invention further provides methods for modulating HBV cccDNA, for treating or preventing HBV in a subject, and for modulating cccDNA transcription of hepatitis B in a subject.
Beta-turn peptidomimetic cyclic compounds for treating dry eye
The present invention relates to methods of treating dry eye using -turn peptidomimetic cyclic compounds or derivatives thereof. The -turn peptidomimetic cyclic compounds can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat dry eye.
PROTEASE INHIBITION
The invention relates to a method for inhibiting an ADAM protease, comprising inhibiting binding to an integrin-binding loop of a disintegrin domain in the ADAM protease. Also provided are cyclic peptides which inhibit binding to an integrin-binding loop of an ADAM protease, as well as associated pharmaceutical compositions, uses and methods of treatment.
Modulation of hepatitis B virus CCCDNA transcription
The present invention provides small molecule inhibitors of hepatitis B virus (HBV) covalently closed circular (ccc) DNA, which are useful as therapeutics in the management of chronic HBV. The compounds of the invention achieve epigenetic modification of the cccDNA, histone modification and histone deacetylase activity inhibition, thus modulating HBV cccDNA. The present invention further provides methods for modulating HBV cccDNA, for treating or preventing HBV in a subject, and for modulating cccDNA transcription of hepatitis B in a subject.
MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS
The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:
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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.
Cyclopeptide and method for preparing the same
A method for preparing a cyclopeptide and a cyclopeptide preparing by the method are disclosed. The method includes the following steps: (a) providing compounds represented by formulas (I-1) and (I-4); (b) performing a reaction between the compounds of formulas (I-1) and (I-4) to obtain a compound represented by formula (I-5); (c) performing a reaction between the compound of formula (I-5) and the compound represented by formula (I-6) to obtain a compound represented by formula (I-7); (d) performing a cyclization reaction of the compound of formula (I-7) with a catalyst of formula (II) and deprotection to obtain a compound represented by formula (III), wherein the compounds of formulas (I-1), (I-4) to (I-7), (III) and the catalyst of formula (II) are as defined in the specification.