Abstract: The present disclosure provides antibody-drug conjugate (ADC) structures, which include a camptothecine or a camptothecine derivative linked to a polypeptide (e.g., an antibody) through a linker. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.

Abstract: The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

Abstract: Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.

Abstract: The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.

Abstract: An 8-((4-hydroxy-3-methoxyphenyl)diazenyl) naphthalene-1,3-disulfonic acid compound, its synthesis, and its use as an antioxidant agent.

Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

Abstract: This discloses that compounds of Formula 1 have antifibrotic properties. In particular, this discloses a pharmaceutical composition including one or more compounds of Formula 1 and methods of using compounds of Formula 1 in fibrosis treatment and inhibiting type 1 collagen synthesis.

Abstract: The present invention relates to methods of treating a human patient suffering from brain injury. These method may comprise (starting) administering to a selected patient within a time period of ?12 hours or within a time period of >12 hours after the occurrence of the brain injury a therapeutically effective amount of a biopterin compound such as 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin. The invention also relates to methods of increasing the value of the extended Glasgow Outcome Scale (eGOS) of patients suffering from brain injury, thereby improving the condition of the patient.

Abstract: A compound of Formula (I) is provided: where the variables are defined herein.

Abstract: The present invention discloses a 1,4-sulfur-bridged polycyclic compound containing dihydrobenzofuran structure which has a structural formula (I). A preparation method is also disclosed which includes the steps of: dissolving 2-nitrobenzofuran (II) and 5H-thiazolone (III) in an organic solvent; then adding molecular sieve and chiral catalyst, stirring and allowing reaction at room temperature under argon protection until the reaction is completed; and carrying out separation and purification to obtain a 1,4-sulfur-bridged polycyclic compound (I) containing dihydrobenzofuran structure. The polycyclic compounds of the present invention have a substructure of dihydrobenzofuran and 1,4-thiopiperidinone. The application of the compound for the preparation of antitumor drugs is also disclosed, which has a good potential value in antitumor drug research. The preparation method has the advantages of novelty, simplicity, simple operation, mild reaction conditions, high yield and high stereoselectivity, and etc.

Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.

Abstract: Compounds of formula (I), wherein A, R, W, Q, n, and m have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Abstract: Disclosed herein, inter alia, are trioxolane compounds and methods of using the same for treatment and detection of diseases.

Abstract: The present disclosure relates generally to compounds and compositions, intermediates, processes for their preparation, and their use as kinase inhibitors.

Abstract: The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof. wherein each symbol is as defined in the specification.

Abstract: Methods of treating a patient having an organic acidemia or a defect in mitochondria chain oxidation are provided. The methods comprise treating the patient with an effective amount of a mitochondria-targeting reactive oxygen species scavenger.

Abstract: Crystalline 4-chloro-N-(4-(morpholinomethyl)phenyl)benzamide, crystalline 4-chloro-N-(4-(morpholinomethyl)phenyl)benzamide hydrochloride, methods of preparing the crystalline compounds, pharmaceutical compositions containing the crystalline compounds, and methods of treatment using the crystalline compounds are disclosed.

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

Abstract: A liquid drug formulation comprising clonidine and midazolam. The amount of clonidine is in the range of 5.0-50 ?g/ml. The amount of midazolam is in the range of 0.5-10 mg/ml. The liquid drug formulation could be in the form of a syrup. The liquid drug formulation could be provided in a multi-use container or a single-use dispenser. Also disclosed is a method of inducing sedation in a patient using the liquid drug formulation.

Abstract: Compositions and methods useful in slowing, inhibiting, or regressing the progression of myopia, while minimizing pupil dilation and light sensitivity are provided herein. Provided compositions can include a muscarinic receptor antagonist and a miotic agent.