Abstract: The present invention relates to a compound of formula (I): wherein R1 is R3-IPU and R2 is the acyloxy residue of diclofenac or naproxen, and specified by the following structures (A) wherein OH—R3-IPU is selected from (B) and R4 and R5 may be the same or different selected from (C) and salts, solvates and hydrates thereof.

Abstract: Process for purifying N-alkylpyrrolidones which due to a previous use comprise at least one of the impurities of the formula I or II where R is hydrogen or a C1-C20-alkyl group, wherein a basic compound is added to the N-alkylpyrrolidone to be purified and the temperature of the mixture is at least 80° C. not more than 20 minutes after addition of the basic compound and N-alkylpyrrolidone is distilled off from the mixture obtained.

Abstract: The invention relates to a tenofovir prodrug and pharmaceutical uses thereof. In particular, the invention relates to a compound as shown in general formula (I): and its isomer, pharmaceutically acceptable salt, hydrate or solvate, as well as their uses in preparing drugs for treating viral infectious diseases, especially HIV infection, hepatitis B, or diseases caused by hepatitis B virus, wherein the definition of each substituent in the general formula (I) is as defined in the specification.

Abstract: A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R2CH2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.

Abstract: A process for the continuous preparation of adiponitrile by hydrocyanation of 3-pentenenitrile is described, wherein a) 3-pentenenitrile is hydrocyanated to give a reaction output comprising adiponitrile, b) in a work-up 1, a mixture comprising cis-2-methyl-2-butenenitrile and cis-2-pentenenitrile is separated off as overhead product from the reaction output from the reactor R1 in a first distillation apparatus, c) the mixture comprising cis-2-methyl-2-butenenitrile and cis-2-pentenenitrile from step b) is continuously isomerized in the presence of aluminum oxide as catalyst in a reactor R2 to give a product mixture comprising 3-pentenenitrile, d) cis-2-methyl-2-butenenitrile is separated off as overhead product from the reaction output from the reactor R2 in a distillation apparatus in a work-up 2 and discharged.

Abstract: Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl]-4-(trifluoromethyl)-benzamide.

Abstract: The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.

Abstract: Provided herein are pharmaceutical compositions, which comprise a 1,2,4-oxadiazole benzoic acid or a pharmaceutically acceptable salt thereof. Further provided herein are certain pharmaceutically acceptable salts of a 1,2,4-oxadiazole benzoic acid and methods for making the same. Further provided herein are methods of treating or preventing a disease associated with a nonsense mutation or a premature stop codon, comprising administering such pharmaceutical compositions or pharmaceutically acceptable salts to a patient having a disease associated with a nonsense mutation or a premature stop codon.

Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.

Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.

Abstract: Disclosed are compounds, for example, compounds of formula I, wherein R, R0, R1-R8, n, X, Y, Y?, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.

Abstract: Imidazolone and pyrazolone derivatives of formula (I) described herein exhibit human neutrophil elastase inhibitory properties and are useful for the therapy of diseases and conditions in which HNE is implicated.

Abstract: Described herein are analogs of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogs having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.

Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula: Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exacerbated respiratory disorders and urological disorders.

Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.

Abstract: O/W-emulsion-type topical pharmaceutical compositions including a retinoid are described. Also described, is a topical pharmaceutical composition including by way of an active pharmaceutical ingredient, a retinoid in a physiologically acceptable composition. Preparation methods and the use of the same in dermatology are also described.

Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: A polymer comprising one or more optionally substituted repeat units of formula (I): (I) wherein each Ar1 independently represents a substituted or unsubstituted aromatic or heteroaromatic group; each Ar2 independently represents a substituted or unsubstituted aromatic or heteroaromatic group; n and m in each occurrence is at least 1; and R1 and R2 are substituents wherein R1 and R2 are different.