Abstract: Compounds comprising a fused tricylic core that modulate HIF-2? activity, pharmaceutical compositions containing these chemical entities, and methods of using these chemical entities for treating diseases associated with HIF-2? activity are described herein.

Abstract: Methods of synthesizing pomalidomide are disclosed. Further, methods of purifying pomalidomide from a reaction mixture are also disclosed.

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

Abstract: The present invention is intended to provide a novel parasiticide, antiprotozoal or other endoparasite control agents which are effective for controlling animal endoparasites that have been impossible to control by conventional ones. Provided is an endoparasite control agent comprising, as an active ingredient, a heterocyclic carboxamide derivative represented by the general formula (I): or a salt thereof.

Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The present invention provides modulators of protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, and cancer, are provided.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade in the alternative complement pathway. The inhibitors of factor D described herein reduce the excessive activation of complement.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

Abstract: Disclosed is a method for preparing avanafil (I) by using cytosine as the starting material. The preparation steps comprise: using cytosine as the raw material, and enabling the cytosine to react with side chain 3-chlorine-4-methoxybenzyl halogen, N-(2-methylpyrimidine) methanamide and S-hydroxymethyl pyrrolidine, to prepare the target product avanafil (I). For the preparation method, the raw material is easily obtained, and the process is simple, economical, and environmentally friendly, so the method meets the requirement of industrial boost.

Abstract: The present invention relates to the a process for total synthesis of flavonoid compounds of general formula I and isomers thereof wherein R1 and R2 is OH; R3?H or The present invention particularly relates to the process for preparation and separation of (2S,3S)-taxifolin-6-C-?-D-glucopyranoside (ulmoside A), (2R,3R)-taxifolin-6-C-?-D-glucopyranoside and taxifolin.

Abstract: The present invention relates to molecules of formula (I) where R1=—SO3H, —PO3H, —PO2(OH)2, —OPO2H2, —NHSO3H, —S(N?H)Me, SH, SR or guanidyl; R?C1-4 alkyl, phenyl or 5 or 6 membered aromatic nitrogen heterocycles; n=1, 2, 3, 4 or 5; X?C=0, C(OH)H, C(OAlk)H, C?S, CH2; Alk=C1-6 alkyl linear, branched or cyclic, optionally hydroxylated or polyhydroxylated; their preparation and use as analgesics and in the treatment of pain induced by chemotherapies.

Abstract: Methods for preparing disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds that correspond to general formula (I) are described. Also described are pharmaceutical compositions that include the compounds, and methods of using the compounds and compositions for the treatment of chemokine-mediated diseases.

Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, Rl to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.

Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: The present application relates to novel aryl- and hetaryl-substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.

Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3 and R4 are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds (referred to herein as “PPDA compounds”) that, inter alia, inhibit (e.g., selectively inhibit) CDK (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.).

Abstract: Methods are disclosed for making 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof.

Abstract: Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt 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: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.

Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to a process for the preparation of 5-fluorotryptophol as well as a process for the preparation of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano-[3,4b]-indol]-4-amine using the 5-fluorotryptophol obtained by said first process. The process according to the invention provides 5-fluorotryptophol in improved yield and purity without the need for chromatographic purification of the product.

Abstract: Carboxamide-substituted xanthene dyes, reactive dyes, and the use of such dyes as a labeling reagent are disclosed. Specifically, a carboxamide-substituted dye of the formula (I) is disclosed.

Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: The present disclosure relates generally to systems, methods, and compounds for therapeutic use against parasitic infections. More particularly, the disclosure relates to anti-parasitic compounds, and methods for making and for using the anti-parasitic compounds, where the anti-parasitic compounds have the general formula: where X, R1, R2, R3, R4, R5, and R6 are defined more fully below.

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

Abstract: The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Abstract: The present invention relates to salt forms of the phosphoinositide 3-kinase (PI3K) inhibitor (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, pharmaceutical compositions comprising the same, and methods of using the salts and compositions for the treatment of PI3K-associated diseases such as cancer.

Abstract: The present invention is related to crystalline forms of (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one which is a PI3K inhibitor useful in the treatment of cancer and other diseases.

Abstract: The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

Abstract: Provided herein are kallikrein modulating compounds, pharmaceutical compositions comprising the same, and uses thereof.

Abstract: Certain embodiments are directed to a composition comprising a complex of the general formula [M(crown ether)(solvent)n][arene?•], wherein M is an alkali metal and method of making the same.

Abstract: Compounds and method of preparation of Si—X and Ge—X compounds (X?N, P, As and Sb) via dehydrogenative coupling between the corresponding unsubstituted silanes and amines (including ammonia) or phosphines catalyzed by metallic catalysts is described. This new approach is based on the catalytic dehydrogenative coupling of a Si—H and a X—H moiety to form a Si—X containing compound and hydrogen gas (X?N, P, As and Sb). The process can be catalyzed by transition metal heterogenous catalysts such as Ru(0) on carbon, Pd(0) on MgO) as well as transition metal organometallic complexes that act as homogeneous catalysts. The —Si—X products produced by dehydrogenative coupling are inherently halogen free. Said compounds can be useful for the deposition of thin films by chemical vapor deposition or atomic layer deposition of Si-containing films.

Abstract: A modified opioid is provided comprising modified morphine molecules, wherein for each morphine molecule, one or more carbon atoms are replaced with silicon atoms. A method is further provided for modifying an opioid comprising morphine molecules, said method comprising the step of replacing one or more carbon atoms with silicon atoms.

Abstract: The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement.

Abstract: The present application relates to methods and compounds for enhancing contrast in magnetic resonance imaging. The methods comprise administering compounds of Formula I(a) or I(b) to a subject and obtaining a magnetic resonance image of the subject. The present application also relates to methods of preparing compounds of the Formula I(a) as well as intermediate compounds used in such a method of preparation.

Abstract: The present invention provides a process for isolating fermentable sugars from the acid hydrolyzate of a material containing cellulose, hemicellulose and lignin, particularly a process which is simple, economical and commercially viable.

Abstract: Sialic acid derivatives of the formula (I)

Abstract: A method for producing a compound represented by Structural Formula (1), including: introducing benzyl group into trehalose to produce at least one of compound represented by Structural Formula 4a and compound represented by Structural Formula 4a?; subjecting at least one of the Structural Formula 4a compound and the Structural Formula 4a? compound to prenylation to produce at least one of compound represented by Structural Formula 3a and compound represented by Structural Formula 3a?; subjecting at least one of the Structural Formula 3a compound and the Structural Formula 3a? compound to sharpless asymmetric dihydroxylation to produce at least one of compound represented by Structural Formula 2a and compound represented by Structural Formula 2a?; and allowing at least one of the Structural Formula 2a compound and the Structural Formula 2a? compound to react with hydrogen in the presence of palladium catalyst to produce the compound represented by Structural Formula (1).

Abstract: The present invention relates to a 5-formylcytosine specific chemical labeling method and related applications in aspects such as sequencing, detection, imaging, and diagnosis. In the method, a condensation reaction occurs between an active methylene group in an active methylene compound containing a side-chain reactive group and an aldehyde group in 5-formylcytosine or a 1-substituted derivative of 5-formylcytosine, and at the same time an intramolecular reaction occurs between the side-chain reactive group of the active methylene compound and a 4-amino group of cytosine to implement ring closing.

Abstract: Disclosed herein, inter alia, are prodrug compositions and methods of using the same for treatment and detection of disease. Specifically, disclosed herein is a compound of formula (I) having spiro-fused 1,2,4-trioxolane and piperidine rings, namely, 1,2,4-trioxa-8-azaspiro[4.5]decane. Also disclosed is a pharmaceutical composition containing the compound and a pharmaceutically acceptable carrier.