PATENTSCOPE: EN_ALL:nmr AND PA:roche

DEVICES FOR SAMPLE ANALYSIS USING EPITACHOPHORESIS (Fri, 17 May 2019)
The present disclosure generally relates to devices for effecting epitachophoresis. Epitachophoresis may be used to effect sample analysis, such as by selective separation, detection, extraction, and/ or pre-concentration of target analytes such as, for example, DNA, RNA, and/or other biological molecules. Said target analytes may be collected following epitachophoresis and used for desired downstream applications and further analysis.
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TRIFAB-CONTORSBODY (Fri, 10 May 2019)
Herein is reported a multispecific antibody comprising two circular fusion polypeptides each of them comprising a VH/VL-pair and thereby a first and a second binding site, whereby a third VH/VL-pair and thereby a third binding site is formed by the associated of the two circular fusion polypeptides.
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METHOD FOR IN VIVO GENERATION OF MULTISPECIFIC ANTIBODIES FROM MONOSPECIFIC ANTIBODIES (Fri, 10 May 2019)
Herein is reported a method for the generation of multispecific antibodies directly on the cell-surface at the site of action by a half-antibody exchange reaction between two 2/3-IgGs or two 2/3-BiFabs destabilized in one half by asymmetric perturbing mutations fostering the generation of correctly assembled full length bi-or multi-specific antibodies. The method is performed in the absence hinge region disulfide bonds in the starting 2/3-IgGs or 2/3-BiFabs.
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BICYCLIC SULFONES AND SULFOXIDES AND METHODS OF USE THEREOF (Fri, 10 May 2019)
Provided are compounds having the general formula I: wherein R1, R B1, RB2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds. The compounds of formula (I) are inhibitors of RIP1 kinase and thus useful in the treatmemt of inflammatory, neurodegenerative and other disorders.
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THE COMPBODY - A MULTIVALENT TARGET BINDER (Fri, 10 May 2019)
Herein is reported a multimeric fusion polypeptide comprising five monomeric fusion polypeptides each comprising at least a Fab fragment and a COMP-domain of SEQ ID NO: 01 or a functional fragment thereof.
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DIAGNOSTIC AND THERAPEUTIC METHODS FOR CANCER (Fri, 10 May 2019)
The present invention provides diagnostic methods, therapeutic methods, and compositions for the treatment of cancer (e.g., a bladder cancer (e.g., UC, e.g., mUC), a kidney cancer, a lung cancer, a liver cancer, an ovarian cancer, a pancreatic cancer, a colorectal cancer, or a breast cancer). The invention is based, at least in part, on the discovery that expression levels of one or more biomarkers described herein in a sample from an individual having cancer can be used in methods of identifying an individual having a cancer who may benefit with an anti-cancer therapy that includes an immunotherapy (e.g., a PD-L1 axis binding antagonist such as an anti-PD-L1 antibody (e.g., atezolizumab)) and a suppressive stromal antagonist (e.g., a TGF-β antagonist), methods for selecting a therapy for an individual having cancer, methods of treating an individual having cancer, methods for assessing a response or monitoring the response of an individual to treatment with an anti-cancer therapy that includes an immunotherapy (e.g., a PD-L1 axis binding antagonist such as an anti-PD-L1 antibody (e.g., atezolizumab)) and a suppressive stromal antagonist (e.g., a TGF-β antagonist), and related kits, anti-cancer therapies, and uses.
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BICYCLIC COMPOUNDS FOR USE AS RIP1 KINASE INHIBITORS (Fri, 19 Apr 2019)
The invention provides novel compounds having the general formula (I) or pharmaceutically acceptable salts thereof, wherein RA, RB1, RB2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds as RIP1 kinase inhibitors.
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PIPERAZINE DERIVATIVES AS MAGL INHIBITORS (Fri, 19 Apr 2019)
The invention provides new heterocyclic compounds having general Formula (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, X, Y1 and Y2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
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CRYSTALLINE FORMS OF DIAZABICYCLOOCTANE DERIVATIVES AND PRODUCTION PROCESS THEREOF (Fri, 05 Apr 2019)
The present invention relates to crystalline forms of a diazabicyclooctane derivative represented by Compound I, the process for producing the same and methods for using the same: (I).
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MULTI-CYCLIC AROMATIC COMPOUNDS AS FACTOR D INHIBITORS (Fri, 29 Mar 2019)
Multi-cyclic aromatic compounds and methods of use as Factor D modulators are described herein.
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PROCESS FOR THE PREPRATION OF 7-(4,7-DIAZASPIRO[2.5]OCTAN-7-YL)-2-(2,8-DIMETHYLIMIDAZO[1,2-B]PYRIDAZIN-6-YL)PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES (Fri, 29 Mar 2019)
The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)pyrido[l,2-a]pyrimidin-4-one derivatives useful pharmaceutically active compounds.
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CYCLIC PEPTIDE ANTIBIOTICS (Fri, 22 Mar 2019)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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DIHYDROQUINOLINONES (Fri, 08 Mar 2019)
The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.
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NOVEL PHARMACEUTICAL COMPOSITIONS FOR BASIC OR NEUTRAL, LOW MOLECULAR WEIGHT COMPOUNDS (Fri, 22 Feb 2019)
The present invention provides novel, solid or liquid pharmaceutical preparations comprising a basic or neutral, low molecular weight active pharmaceutical ingredient and the polymer Eudragit® EPO, optionally together with additional pharmaceutically acceptable excipients.The present preparations are for oral or topical administration.
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ANTI-CD8 ANTIBODIES AND USES THEREOF (Fri, 15 Feb 2019)
Provided are anti-CD8 antibodies that bind human CD8 and do not stimulate or inhibit the activation of CD8+ T cells. Also provided are nucleic acids encoding such anti-CD8 antibodies, vectors comprising such nucleic acids, host cells comprising same, and methods of making such anti-CD8 antibodies. Also provided are anti-CD8 antibodies conjugated to a detectable label. Provided are methods of using such anti-CD8 antibodies to detect CD8+ T cells in a subject, monitor disease progress in a subject having cancer, and monitor treatment progress in a subject having cancer.
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THREE-DIMENSIONAL STRUCTURE-BASED HUMANIZATION METHOD (Fri, 08 Feb 2019)
Herein is reported a method for the humanization of non-human antibodies using a structure-based scoring matrix. With the scoring matrix it is possible to determine (the requirement for and) the suitability of specific (back)mutations of amino acid residues at defined positions of a selected human germline sequence. The scoring matrix takes into account the topology, the three-dimensional structure and the interactions of the respective residue and change. Thereby the influence on antigen binding of a specific amino acid residue change can be determined.
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BICYCLIC KETONE COMPOUNDS AND METHODS OF USE THEREOF (Fri, 18 Jan 2019)
The invention provides novel compounds having the general formula (I): (I) wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
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MULTIPLE COUPLING & OXIDATION METHOD (Fri, 04 Jan 2019)
The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers and methods of synthesis of stereodefined oligonucleotides using said monomer. Herein are disclosed oligonucleotide enhanced synthesis methods where within a single elongation cycle there are repeated coupling and oxidation steps. The method results in an enhanced yield and higher purity of stereodefined phosphorothioate oligonucleotides
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ISOINDOLINONE DERIVATIVES AS IRAK4 MODULATORS (Fri, 28 Dec 2018)
Compounds of Formula (0), and stereoisomers and pharmaceutically acceptable salts thereof, as well as methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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BENZOFURANS AS IRAK4 MODULATORS (Fri, 28 Dec 2018)
Compounds of Formula (0), and stereoisomers and pharmaceutically acceptable salts thereof, as well as methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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