PATENTSCOPE: EN_ALL:nmr AND PA:ucb

2-OXO-1,3-OXAZOLIDINYL IMIDAZOTHIADIAZOLE DERIVATIVES (Fri, 18 Jan 2019)
The present invention relates to 2-oxo-1,3-oxazolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
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2-OXO-1-IMIDAZOLIDINYL IMIDAZOTHIADIAZOLE DERIVATIVES (Fri, 18 Jan 2019)
The present invention relates to 2-oxo-1-imidazolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
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METHOD FOR THE TREATMENT OF IMMUNE THROMBOCYTOPENIA (Fri, 21 Dec 2018)
The disclosure relates to a method of treating or preventing immune (idiopathic) thrombocytopenic purpura (ITP) in a human in need thereof, the method comprising administering to the human in the range of 1 to 5 doses of an anti-FcRn antibody or antigen binding fragment thereof over a treatment period of 1 to 12 weeks, wherein the aggregrate dose in the treatment period is in the range of 1 to 30 mg per kg.
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SPIROCYCLIC INDOLINES AS IL-17 MODULATORS (Fri, 21 Dec 2018)
A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
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FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 02 Nov 2018)
A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 21 Sep 2018)
A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine derivatives, and analogues thereof, being potent modulators of human TNFα activiy, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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ALKOXY BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION (Fri, 03 Aug 2018)
The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
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BICYCLIC BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION (Fri, 03 Aug 2018)
The present invention relates to certain bicyclic bis-heteroaryl compounds of Formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
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BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION (Fri, 03 Aug 2018)
The present invention relates to bis-heteroaryl compounds of formula (I), pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
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(AZA)INDOLE-, BENZOTHIOPHENE-, AND BENZOFURAN-3-SULFONAMIDES (Fri, 06 Jul 2018)
Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
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ANTIBODY FRAMEWORKS FOR REDUCING AGGREGATION OF MULTISPECIFIC ANTIBODIES (Fri, 29 Jun 2018)
The present invention provides a multispecific antibody molecule comprising at least two binding domains each with a variable heavy region VH and a variable light region VL, wherein each binding domain is specific for an antigen and comprises 6 CDRs, characterised in that at least one binding domain comprises a variable heavy region, VHA, having a framework comprising valine at position (5), lysine at position (13), alanine at position (24) and threonine at position (96) with the proviso that CDRH3 in VHA is other than RYYSAMPFAY (SEQ ID NO:29) and a variable light region, VLA, having a framework comprising leucine at position (11) and glutamine at position (103).
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PROTEINS AND USES (Fri, 04 May 2018)
The invention is in the field of protein: protein interactions, in particular the stabilisation of protein: protein interactions. Binding proteins are provided for stabilising the interactions, together with compositions comprising the binding proteins. Methods using the binding proteins are also provided, including targeting of cells and also medical uses.
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9H-PYRROLO-DIPYRIDINE DERIVATIVES (Fri, 09 Feb 2018)
The invention relates to 9H-pyrrolo-dipyridine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
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9H-PYRROLO-DIPYRIDINE DERIVATIVES (Fri, 09 Feb 2018)
The invention relates to 9H-pyrrolo-dipyridine derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
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ANTI-IgE ANTIBODIES (Fri, 15 Dec 2017)
The present invention relates to the area of improved anti-IgE antibodies and antigen binding agents, and compositions thereof, which target IgE, for instance: for use in treating disorders caused by IgE (such as allergic responses, or certain autoimmune responses); and, in particular, disorders caused by the interaction of IgE with the FcεRI receptor. In particular, this invention relates to improved anti-IgE antibodies and antigen binding agents related to novel mutants of omalizumab (Xolair®). The improved anti-IgE antibodies and antigen binding agents of the invention may have improved affinity for IgE and/or an improved interaction with the Cε2 domain of IgE and/or an improved modified epitope on IgE (for instance further involving the Cε2 domain of IgE) and/or the ability to disassociate IgE from the FcεRI receptor for instance at pharmaceutically-relevant concentrations. In one aspect, improved or novel treatments for IgE mediated disorders are disclosed in which IgE is targeted (for instance free IgE and/or IgE complexed with the FcεRI receptor).
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METHODS FOR IDENTIFYING PROTEINS BY USING SYNTHETIC RECEPTORS (Fri, 15 Dec 2017)
The invention relates to oligomeric macrocycles and to uses thereof as receptors for recognition of protein post-translational modifications (PTM) or specific motifs in proteins.
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ANTAGONIST ANTIBODIES THAT T BIND TO HUMAN TGFB1, TGFB2 AND TO TGFB3 AND THEIR USE FOR THE TREATMENT OF LUNG FIBROSIS (Fri, 15 Dec 2017)
The present disclosure relates to TGF-beta antibodies and binding fragments thereof, DNA encoding the same, host cells comprising said DNA and methods of expressing the antibody or binding fragment in a host cell. The disclosure also extends to pharmaceutical compositions comprising the antibody or a binding fragment thereof and use of the antibody, binding fragment and compositions comprising the same in treatment of various diseases including fibrosis.
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AFFINITY ENGINEERED SERUM PROTEIN CARRIER BINDING DOMAIN (Fri, 10 Nov 2017)
The present disclosure relates to a method of modulating the half-life of a binding domain specific to a serum carrier protein by mutating the sequence and a modulated binding domain specific to a serum carrier protein.
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TETRAHYDROISOQUINOLINE DERIVATIVES (Fri, 20 Oct 2017)
The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), wherein G represents a fused heterocyclic system selected from the groups represented by formula (G1), (G2), (G3), (G4), (G5), and (G6), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.
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FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 06 Oct 2017)
A series of substituted fused pentacyclic benzimidazole derivatives,and analogues thereof,being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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