Listing External IP Records

Title Summary
Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
Patent number
10,000,507
Abstract
The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
Salt forms of ceftolozane
Patent number
10,000,510
Abstract
This disclosure relates to salt forms of ceftolozane, processes for making these salt forms, and compositions comprising the same. Also disclosed are stabilized compositions of ceftolozane. Provided herein are salt forms of ceftolozane, processes for making these salt forms and compositions comprising the same. The salt forms provided herein include ceftolozane bromide, ceftolozane edisylate, ceftolozane mesylate, ceftolozane chloride, ceftolozane sulfate, ceftolozane maleate, ceftolozane phosphate, and ceftolozane ketoglutarate.
Small molecules for the modulation of MCL-1 and methods of modulating cell death, cell division, cell differentiation and methods of treating disorders
Patent number
10,000,511
Abstract
This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
Phosphonate compounds for treatment of medical disorders
Patent number
10,000,516
Abstract
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R.sup.12 or R.sup.13 on the A group is a phosphonate substituent (R.sup.32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
Substituted gemcitabine bicyclic amide analogs and treatment methods using same
Patent number
10,000,521
Abstract
In one aspect, the invention relates to substituted gemcitabine aryl amide analogs, derivatives thereof, and related compounds; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating viral disorders and disorders of uncontrolled cellular proliferation using the compounds and compositions. In certain aspects, the compounds have the following structure: ##STR00001##
Molecule for treating an inflammatory disorder
Patent number
10,000,538
Abstract
The invention provides a L19 source as a medicament, preferably for preventing or treating an inflammatory disorder in an individual.
Double-acylated GLP-1 derivatives
Patent number
10,000,542
Abstract
The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC--(CH.sub.2).sub.x--CO--*, and Chem. 2: HOOC--C.sub.6H.sub.4--O--(CH.sub.2).sub.y--CO--*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *--NH--(CH.sub.2).sub.q--CH[(CH.sub.2).sub.w--NR.sub.1R.sub.2]--CO--*, which is connected at its CO--* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R.sub.1 and R.sub.2 independently represent *--H or *--CH.sub.3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptide and linker intermediates. The derivatives are potent, stable, protracted, and suitable for oral administration.
GAL-1 variants having immuno-modulating properties and methods of using the same
Patent number
10,000,548
Abstract
Galectin-1 polypeptide variants that include a mutation of the histidine residue corresponding to position 52 of the full-length amino acid sequence of native human Gal-1 as shown in SEQ ID NO: 1, the mutation being a substitution of the histidine to tyrosine or asparagine, providing resistance to acidosis otherwise resulting in deactivation of the native human Gal-1. The Galectin-1 polypeptide variants may include one or more additional mutation(s) of the cysteine residue corresponding to a position selected from 2, 16, 88, or combinations thereof of the full-length amino acid sequence of native human Gal-1 as shown in SEQ ID NO: 1, the additional mutation being a substitution of the cysteine to serine, and providing resistance to oxidation.
Single-domain V.sub.HH antibodies directed to norovirus GI.1 and GII.4 and their use
Patent number
10,000,556
Abstract
Isolated V.sub.HH monoclonal antibodies are disclosed that specifically bind to a Norovirus polypeptide. In some embodiments, the Norovirus is a Genogroup I Norovirus or a Genogroup II Norovirus. In other embodiments, the Norovirus is Norwalk or MD2004 virus. In some embodiments, the monoclonal antibodies specifically bind VP1. Also disclosed are compositions including the disclosed antibodies, nucleic acids encoding these antibodies, expression vectors including the nucleic acids, and isolated host cells that express the nucleic acids. The antibodies and compositions disclosed herein can be used for detecting the presence of a Norovirus in a biological sample, or detecting a Norovirus infection. Also disclosed are methods of treating and/or preventing a NoV infection.
Use of annexin A3 as a diagnostic and prognostic biomarker and therapeutic target for treating hepatocellular carcinoma
Patent number
10,000,558
Abstract
Annexin A3 (ANAX3) is utilized as a biomarker for the diagnosis and prognosis of hepatocellular carcinoma (HCC) and the utilization of a monoclonal antibody against ANXA3 or antisense polynucleotide against ANXA3 mRNA for the suppression or treatment of HCC, alone or in combination with other HCC treatment. Monoclonal antibody against ANXA3 can be administered for the suppression of tumor growth, metastasis, and chemoresistance.