Abstract: Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the etiological agent for coronavirus disease 2019 (COVID-19), has emerged as an ongoing global pandemic. Presently, there are no clinically approved vaccines nor drugs for COVID-19. Hence, there is an urgent need to accelerate the development of effective antivirals. One or more members of the 8-Hydroxyquinoline and Benzylamine structural classes inhibited SARS-CoV-2 infection induced cytopathic effect in vitro, inhibited the exopeptidase activity of angiotensin converting enzyme 2 (ACE2), and disrupted the binding between ACE2 and the Spike protein of SARS-CoV-2. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.

Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.

Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane -1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-ffuorophenyl)cyclopropane-1,1-dicarboxamide.

Abstract: Compounds and methods for treating or preventing a neurodegenerative disease, disorder or condition associated with the overall activity of hsp90 but not with the ATPase activity of hsp90, including peripheral neuropathy, such as peripheral neuropathy caused by chemotherapy or diabetes, disorders 5 of the central nervous system, such as Alzheimer's disease and Parkinsons disease, and motor neuron diseases, such as amyotrophic lateral sclerosis (ALS), in a subject are provided.

Abstract: Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases.

Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.

Abstract: The present invention relates to a series of compounds useful for effecting purification, in particular for use in purification of synthetic peptides and proteins. The compounds of the invention are particularly efficient at securely anchoring peptides or proteins to a surface and allowing the peptide or protein to become uniformly orientated, thus ensuring that substantially all of the peptide or protein is available for molecular binding to a substrate.

Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.

Abstract: Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).

Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: Embodiments of the present disclosure provide for BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of making BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of using BHQ-conjugates and protected BHQ-conjugate precursor compounds, and the like.

Abstract: Provided herein is a novel mTOR-comprising complex, mT-ORC3, which comprises mTOR and the Ets transcription factor TEL2. Specific mTORC3 binding agents and modulating agents are provided, along with kits and methods for the detection of mTORC3. Methods of modulating the activity of mTORC3 or modulating cell growth and/or survival are also provided. Further provided are methods for screening for mTORC3 binding agents and for mTORC3 modulating agents. Various methods of diagnosis and treatment are further provided.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, (phosphoryloxy)methyl, and 8-carbamates derivatives thereof are described that exhibit iron chelation, neuroprotective, neurorestorative, apoptotic and/or selective MAO-AB inhibitory activities.

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.

Abstract: The present invention relates to a series of compounds useful for effecting purification, in particular for use in purification of synthetic peptides and proteins. The compounds of the invention are particularly efficient at securely anchoring peptides or proteins to a surface and allowing the peptide or protein to become uniformly orientated, thus ensuring that substantially all of the peptide or protein is available for molecular binding to a substrate.

Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/o

Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.

Abstract: Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, and analysis of molecular chaperone activity.

Abstract: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2).

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments

Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention is administered to a subject.

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: The invention provides potent quinolinol-based BoNT/A small-molecule inhibitors of botulinum neurotoxins, in particular of Clostridium botulinum serotype A neurotoxins. The invention also provides methods of using these small-molecule inhibitors to inhibit infections by Clostridium botulinum, as well as, methods of preventing infections by Clostridium botulinum through materials that may be ingested.

Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.

Abstract: Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I).

Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.

Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.

Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

Abstract: The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.