Abstract: Provided herein are compounds and methods for treating a disorder associated with aberrant A? peptide levels, including Alzheimer's disease.

Abstract: Provided herein are methods of treating inflammation or neuropathic pain using an effective dose of a monoacylglycerol lipase inhibitor or a composition thereof.

Abstract: The present invention covers substituted 6-(1H-pyrazol-1-yl)pyrimidin-4-amine compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular and renal diseases, as a sole agent or in combination with other active ingredients.

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy and Y are defined herein, which are suitable for the treatment of diseases related to BTK, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

Abstract: The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.

Abstract: Provided herein are methods of using KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.

Abstract: There are described compounds of formula (I): and there use as a medicament in the treatment of conditions involving abnormal activation and/or malfunction of the of the hedgehog pathway, such as cancer, fibrosis and chronic graft-versus-host disease (cGVHD).

Abstract: Herein disclosed are compounds, compositions, kits, and methods of treating cancers using 7-azaindolyl furanone/thiophene derivatives. These derivatives inhibit serine-threonine kinase Cdc7, a recognized anticancer target affecting DNA replication. Further, the compounds disclosed herein possess potent inhibitory activity in the presence of adenosine triphosphate (ATP), demonstrate significant kinase selectivity, and offer advantages over known Cdc7 inhibitors with prolonged half-life and inhibitory effects.

Abstract: The present invention relates to novel integrin antagonists of Formula I and their use as a medicament, in particular for inhibiting neovascularization.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of the compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Described herein are 2-amino-quinoline derivatives that are agonists of toll-like receptors 7 and 8 (TLR7/8), pharmaceutical compositions, and methods of use of the compounds and compositions to treat various diseases, such as viral, cancer, and allergic diseases, in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.

Abstract: The present invention relates to a five-membered heteroaryl ring bridged ring derivative, a preparation method therefor and the medical use thereof. In particular, the present invention relates to a new five-membered heteroaryl ring bridged ring derivative as shown in formula (I), a preparation method therefor and a pharmaceutical composition comprising the derivative, and the use thereof as a therapeutic agent, in particular as a TGF-? inhibitor, and the use in the preparation of a drug for treating, preventing or reducing cancers mediated by the over-expression of TGF-?, wherein the definition of each substituent in the general formula (I) is the same as defined in the description.

Abstract: In one aspect, the invention provides compounds of Formula I Formula Ia, Formula Ib, Formula Ic, and Formula Id and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula Ia, Formula Ib, Formula Ic, or Formula Id. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease, diabetes bone loss, and cancer, using a compound of Formula I, Formula Ia, Formula Ib, Formula Ic, or Formula Id.

Abstract: The present invention provides compounds of Formula (1): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The application relates to a process for the synthesis of a Near Infra-Red (NIR) fluorescent probe which is a cRGD-Cy5.5 conjugate of formula (I) known as DA364 comprising an aza-bicycloalkane based cyclic peptide labelled with a Cy5.5 dye moiety and used in the guided surgery of tumors and pathologic regions.

Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Abstract: The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

Abstract: The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.

Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.

Abstract: Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example Alzheimer's disease.

Abstract: The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation, A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of Nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of Naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

Abstract: The present specification provides a compound of Chemical Formula 1, and an organic light emitting device including the same. The compound provides a low driving voltage, high light emission efficiency and a long lifetime of the organic light emitting device.

Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

Abstract: The present invention relates to novel substituted [5,6]cyclic-4(3H)-pyrimidinone compounds of formula (I) and their preparation methods. (I) In particular, the present invention relates to novel substituted [5,6]cyclic-4(3H)-pyrimidinone compounds useful as inhibitors of protein kinases, specifically CDC7 (cell division cycle 7) inhibitors.

Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.

Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, R6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The invention provides synthetic intermediates and synthetic processes that are useful for preparing the antibacterial agent TXA709:

Abstract: The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.

Abstract: The present invention relates to a process for preparing optically active compounds of formula X and intermediates thereof, wherein the variables of compound of formula X are as defined in the claims or the description.

Abstract: The present invention provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula: wherein A3 is CR3A, CR3AR3B, N or NR3C; R3A, R3B, R4A and R4B are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted non-aromatic carbocyclyl; R3C is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic carbocyclyl; ring T1 is substituted or unsubstituted nitrogen-containing non-aromatic heterocycle; R1 is a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; R2 is each independently substituted or unsubstituted alkyl or the like: n is 1 or 2; R3 is substituted or unsubstituted aromatic carbocyclyl or the like; R4 is a hydrogen atom or a carboxy protecting group.

Abstract: Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.

Abstract: Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

Abstract: A phosphorescent chemosensor based on A Gold(I) complex stabilized in an aqueous polymer media. The complex exhibits strong red emission (?max ˜690 nm) in solutions and is sensitive to sub-ppm/nM levels of silver ions. On addition of silver salt to the polymer-complex, a bright-green emissive adduct with peak maximum within 475-515 nm is developed. The silver adduct exhibits a four-fold increase in quantum yield (0.19±0.02) compared to polymer-complex alone (0.05±0.01), along with a corresponding increase in phosphorescence lifetime. The polymer-complex also exhibits sensitivity to higher concentrations (e.g., >1 mM) of other metal ions such as Tl+, Pb2+, and Gd3+. The sensing methodology is simple, fast, and convenient, and the results can be detected by the naked eye. Addition of EDTA restores the red emission of the complex. The complex can distinguish between silver ions and silver nanoparticles and can be used to remediate silver ions from the environment.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: The present invention relates to solid forms of a substituted benzoxaborole compound, specifically crystalline forms of a compound of formula I, compositions comprising crystalline forms of the compound of formula (I), and methods of their use.

Abstract: The present disclosure provides cyclic silyl ethers of the formula: and salts thereof. The cyclic silyl ethers may be useful as monomers for preparing polymers. Also described herein are polymers prepared by polymerizing a cyclic silyl ether and optionally one or more additional monomers. The polymers may be degradable (e.g., biodegradable). One or more O—Si bonds of the polymers may be the degradation sites. Also described herein are compositions and kits including the cyclic silyl ethers or polymers; methods of preparing the polymers; and methods of using the polymers, compositions, and kits.

Abstract: The invention provides a mixture M containing compound A which contains at least one hydrogen atom bound directly to Si, compound B which contains at least one carbon-carbon multiple bond, compound C which contains at least one cationic Si(II) group and compound D which contains at least one alkoxy group bound directly to silicon, and also a method for hydrosilylating the mixture M, wherein the mixture M is heated.

Abstract: The present invention relates to novel polymerizable multivinylaminosilanes which are useful as branching agents for synthetic and natural rubber. The compounds of the invention can be used as such in the polymerization of conjugated diene monomers, optionally together with aromatic vinyl monomers, thus producing polymers, specifically elastomeric polymers, which can favorably be used in rubber articles such as tires.

Abstract: The present disclosure relates to a perovskite that includes A1-xA?xBX3, where A is a first cation, A? is a second cation, B is a third cation, X is a first anion, and 0<x?1. In some embodiments of the present disclosure, the perovskite may further include a second anion (X?) such that the perovskite includes A1-xA?xB(X1-zX?z)3, where 0<z?1. In some embodiments of the present disclosure, the perovskite may further include a fourth cation (A*) such that the perovskite includes A1-x-yA?xA*yB(X1-zX?z)3, where 0<y?1. In some embodiments of the present disclosure, the perovskite may further include a fifth cation (B?) such that the perovskite includes A1-x-yA?xA*yB1-aB?a(X1-zX?z)3, where 0<a?1.

Abstract: Provided herein are compounds useful for the treatment of cancer.

Abstract: Methods for the synthesis of a polyoxometalate compounds include heating a metal precursor in the presence of an organic salt. The polyoxometalate compounds produced herein display high photoluminescence quantum yields and photoluminescence maximums in the blue and/or violet regions of the electromagnetic spectrum.

Abstract: A metal complex of formula (I): M(L1)x(L2)y (I) wherein: M is a second or third row transition metal; L1 in each occurrence is independently a light-emitting ligand; L2 is an auxiliary ligand; x is at least 1; y is at least 1; each L1 is a group of formula (IIa) or (IIb): wherein R1-R10 are each independently H or a substituent with the proviso at least one of R3, R5 and R9 of at least one L1 is a group of formula —(Ar)p wherein Ar in each occurrence is independently an aryl or heteroaryl group that may be unsubstituted or substituted with one or more substituents, and p is at least 2.

Abstract: Provided are an organometallic compound and an organic light-emitting device including the same.

Abstract: A raw material for forming a thin film, comprising a compound represented by General Formula (1) below. (in the formula, R1 represents a linear or branched alkyl group having 1 to 5 carbon atoms, R2 represents hydrogen or a linear or branched alkyl group having 1 to 5 carbon atoms, R3 and R4 each independently represent a linear or branched alkyl group having 1 to 5 carbon atoms, A represents an alkanediyl group having 1 to 4 carbon atoms and M represents copper, iron, nickel, cobalt or manganese.

Abstract: The invention relates to a new method of preparing oligomannuronic diacids, important bioactives. The method utilizes oligomannuronic acids as starting materials and the target substances are obtained by acid degradation and active hypobromous acid oxidation steps. The method of preparing oligomannuronic diacids according to the invention employs moderate reaction conditions, has few side reactions, does not need further purification, achieves a yield of more than 90%, or even more than 95%, and is suitable for production with an on-line continuous reactor device, with reaction processes easy to implement automatic control.

Abstract: Novel steviol glycoside compounds characterized by a first group of four glucopyranose residues attached via the number 13 carbon (C13) of the steviol moiety and a second group of two or three glucopyranose residues attached via the number 19 carbon (C19) of the steviol moiety are described, and exemplified by compounds 1-4. These compounds can be present in a composition with other steviol glycosides (e.g., Reb D and Reb M) to enhance their solubilities. Accordingly, the novel compounds can facilitate the preparation of aqueous compositions having a higher concentration of steviol glycosides. A steviol glycoside composition including one or more of compounds 1-4 can be used as a sweetener composition to sweeten other compositions (sweetenable compositions) such as foods, beverages, medicines, oral hygiene compositions, nutraceuticals, and the like.