Patent classifications
C07K5/0827
USE OF ANTI-AGING GLYCOPROTEIN FOR ENHANCING SURVIVAL OF NEUROSENSORY PRECURSOR CELLS
The present disclosure relates to an in vitro method for enhancing engraftment of neurosensory precursor cell comprising the step of contacting an isolated neurosensory precursor cell prior to a transplantation in a subject in need thereof, with a gem-difluorinated C-glycopeptide compound of general formula I, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate thereof: (I).
INHIBITORS OF HEPATITIS C VIRUS
- Kyla Bjornson ,
- Eda Canales ,
- Jeromy J. Cottell ,
- Kapil K. Karki ,
- Ashley A. Katana ,
- Darryl Kato ,
- Tetsuya Kobayashi ,
- John O. Link ,
- Ruben Martinez ,
- Barton W. Phillips ,
- Hyung-Jung Pyun ,
- Michael Sangi ,
- Adam J. Schrier ,
- Dustin Siegel ,
- James G. Taylor ,
- Chinh V. Tran ,
- Teresa A. Trejo Martin ,
- Randall W. Vivian ,
- Zheng-Yu Yang ,
- Jeff Zablocki ,
- Sheila Zipfel
Compounds of Formula I are disclosed
##STR00001##
As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.
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.
NEW DIFLUOROKETAMIDE DERIVATIVES AS HTRA1 INHIBITORS
The invention provides novel compounds having the general formula (I)
##STR00001##
wherein R.sup.1, 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.9, 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.
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.
COATING FOR METAL NANOPARTICLES
The invention relates to a ligand compound having a structure A-B-C, wherein (a) A represents a mono- or polyphosphorylated amino acid linked to part B by its amino group to form an amide bond; B represents (i) a carboxylic acid, and (ii) an amino acid or peptidyl group of 2-10 amino acids, an alkyl or alkenyl group comprising 1-26 carbon atoms, a polyethylene glycol group comprising 1-26 carbon atoms or a combination thereof covalently linked to the carboxylic acid; and C represents a hydrophilic group covalently linked to the group of B (ii) or (b) A represents a mono-or polyphosphorylated amino acid linked to B by its carboxylic acid to form an amide bond; B represents an amino acid or peptidyl group of 2-10 amino acids, an amino substituted alkyl or alkenyl group comprising 1-26 carbon atoms, an amino substituted polyethylene glycol group comprising 1-26 carbon atoms or a combination thereof covalently linked to A by their amino group; C represents a hydrophilic group covalently linked to the group of B. The invention further relates to a coated metal nanoparticle such as super paramagnetic iron oxide nanoparticle (SPIONs) coated with a plurality of the aforementioned ligands and a method of producing thereof.
PEPTIDE DRUG CONJUGATES
The invention provides compounds of formula (I), that are peptidase enhanced cytotoxics. The invention further provides pharmaceutical compositions comprising the compounds, and the use of the compounds or pharmaceutical compositions as a medicament, particularly for use in the treatment or prophylaxis of cancers such as multiple myeloma, osteosarcoma, breast cancer, lung cancer, ovarian cancer, leukaemia and lymphoma.
##STR00001##
MODULATORS OF SORTILIN ACTIVITY
The present invention relates to compounds of formula (I), which are modulators of sortilin activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions where modulation of sortilin activity is beneficial.
Intermediates for macrocyclic compounds
The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n.sub.1, m, p Z.sub.1, Z.sub.2, and Z.sub.3 are as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.