Patent classifications
C07K5/097
Water-soluble peptide fluorescence material
A water-soluble peptide fluorescence material having a structure of formula (I): ##STR00001## In formula (I), n is an integer greater than or equal to 1, R.sub.1 is independently selected from hydrogen or a nitrogen-containing functional group, R.sub.2 is independently selected from hydrogen or alkyl, and A.sub.1 is polymerized by at least one amino acid monomer and having a structure of formula (II): ##STR00002## In formula (II), m is an integer greater than or equal to 1, and R.sub.3 in each, of the amino acid monomers of A.sub.1 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl, A.sub.2 is OR.sub.5 or N(R.sub.4).sub.2, and R.sub.4 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, guanidinylalkyl, monoglycosyl, biglycosyl, or oligosaccharyl, and R.sub.5 is hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl.
METHODS OF TREATING DEPRESSION AND OTHER RELATED DISEASES
The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.
FAP-ACTIVATED PROTEASOME INHIBITORS FOR TREATING SOLID TUMORS
Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
Methods of treating depression and other related diseases
The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.
TRIFLUOROMETHYLPROPANAMIDE DERIVATIVES AS HTRA1 INHIBITORS
The invention provides novel compounds having the general formula (I)
##STR00001##
wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.3, R.sup.8, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.
PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
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.
Substrates and inhibitors of prolyl oligopeptidase and methods of use thereof
Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.
Compounds for enzyme inhibition
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
GELATINASE INHIBITORS AND USE THEREOF
New gelatinase inhibitors, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy and/or prophylaxis of conditions wherein inhibition of gelatinases is useful such as epilepsy, schizophrenia, Alzheimer disease, autism (in particular associated to fragile X syndrome), mental retardation, mood disorders such as bipolar disorders, depression, vascular diseases such as ischemic stroke and atherosclerosis, inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease, drug addiction, neuropathic pain, lung diseases such as asthma and chronic obstructive pulmonary disease, cancer and sepsis.
NOVEL LIGANDS FOR PREVENTION OF NEUROTOXICITY OF THE ALZHEIMER'S DISEASE RELATED AMYLOID-BETA PEPTIDE
The present invention relates to the field of molecular biochemistry and medicine, and in particular to ligands comprising modified amino acid residues, targeting the amyloid- peptide associated with Alzheimer's disease for prevention of aggregation, neurotoxicity and use thereof as drugs for treatment of Alzheimer's disease.