Abstract: The invention provides an oral dosage form comprising (i) an amount of oxycodone and (ii) an amount of buprenorphine, wherein the weight ratio of the amount of buprenorphine to the amount of oxycodone is greater than 1:40 calculated with the amount of buprenorphine in the dosage form expressed as the equimolar amount of buprenorphine base (Mw=467.64 g/mol) in mg, and the amount of oxycodone in the dosage form expressed as the equimolar amount of oxycodone hydrochloride (Mw=351.82 g/mol) in mg. The invention also provides combinations of an opioid agonist and buprenorphine for use to treat pain, wherein the combination achieves a reduction of adverse pharmacodynamic responses (such as, respiratory depression), compared with a corresponding stand-alone opioid therapy. The invention also includes methods of treatment and dosage forms thereof comprising such combinations.

Abstract: The present invention provides a method for producing an aromatic nitrile compound, the method comprising a dehydration reaction wherein a desired compound can be selectively obtained with high yield while suppressing the generation of by-products during the regeneration of an aromatic amide compound into the corresponding aromatic nitrile compound. In addition, the present invention realizes a method for efficiently producing a carbonate ester by applying the abovementioned production method to a method for producing a carbonate ester. The above are achieved by means of a method for producing an aromatic nitrile compound involving a dehydration reaction wherein an aromatic amide compound is dehydrated, the method having a contact step for bringing the aromatic amide compound into contact with a catalyst in a gas phase during the dehydration reaction.

Abstract: The present invention relates to a novel and improved process for preparing (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4?-(trifluo-romethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of the formula (I) and to novel crystalline forms of it, which is i.a. the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), furthermore the present invention relates to a novel and selective crystallization process for preparation of the pseudopolymorphic form monohydrate I (I-M-I) or the pseudopolymorphic form monohydrate II (I-M-II), preferably monohydrate I of formula (I-M-I) and to pharmaceutical compositions comprising monohydrate I of formula (I-M-I) and to its use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiopulmonary and cardiovascular diseases.

Abstract: The present invention sets forth a salt of an aldose reductase inhibitor shown in formula A-N. The salt being able to be prepared as a crystal form, having notably improved solubility relative to the compound of formula A, having lower hygroscopicity allowing for stable existence, and thus being more easily made into a medicine than are the formula A compound or other salts.

Abstract: The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

Abstract: An organic molecule is disclosed having: one first chemical moiety with a structure of formula I: and one second chemical moiety with a structure of formula II: wherein the first chemical moiety is linked to the second chemical moiety via a single bond; and one third chemical moiety with a structure of Formula III: wherein the first chemical moiety is linked to the third chemical moiety via a single bond.

Abstract: Provided is a catalyst for amide compound hydrogenation characterized in that rhodium and molybdenum are supported on hydroxyapatite, the catalyst for amide compound hydrogenation providing a catalyst that can promote a reduction reaction that converts an amide compound into an amine compound, can be used under moderate conditions, and has durability that allows repeated use thereof while retaining high activity. Also provided is a method for producing an amine compound, the method being characterized by including bringing an amide compound into contact with the catalyst for amide compound hydrogenation to cause hydrogenation, thereby producing an amine compound.

Abstract: Compounds of formula (Ia) and/or formula (Ib), are disclosed wherein R1 and R3 are independently selected from the group consisting of H, halogen, alkyl, fluorinated or partly fluorinated alkyl, and heteroaryl, R2 is selected from the group consisting of halogen, fluorinated and partly fluorinated alkyl, R4 and R5 are independently selected from the group consisting of halogen, alkyl, fluorinated or partly fluorinated alkyl, alkenyl, alkinyl, alkoxy, aryl, and heteroaryl, Z is independently selected from the group consisting of CH2, CHR6 or CR7R8, with R6, R7 and R8 independently selected from the group consisting of H, halogen, alkyl, alkoxy, aryl, and heteroaryl, wherein n is independently 1, 2 or 3, U, V and W of formula (Ia) independently form an aryl ring or a heteroaryl ring, and T, U, V and W of formula (Ib) form an aryl ring or a heteroaryl ring.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: Disclosed are compounds of Formula (I) pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PNPT2 inhibition.

Abstract: A compound of Formula I: wherein: X1-X8 are each independently C or N, wherein two adjacent X1-X8 are carbon-fused to a structure of Formula II: X9-X12 are each independently C or N; A1, A2, and A3 are each independently selected from the group consisting of O, S, Se, N, NR, CR, CRR?, SiR, SiRR?, GeR, and GeRR?, with at least one of A1 and A2 being N or NR; each occurrence of is independently a single bond or a double bond, wherein one occurrence of is a single bond and one occurrence of is a double bond; each of RA, RB, and RC independently represents zero, mono, or up to a maximum allowed substitution to its associated ring; each of occurrence R, R?, RA, RB, and RC is independently a hydrogen or a substituent selected from the group consisting of Formula III, Formula IV, Formula V, Formula VI, Formula VII, Formula VIII, Formula IX, deuterium, halogen, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, boryl, alkenyl, cycloalkenyl, heteroalkenyl, a

Abstract: An object of the present invention is to provide a novel compound represented by the following Formula 1 that is useful as a material for an organic electronic device, particularly, an organic EL device, particularly as a light emitting material, and an organic electronic device using the same, particularly, an organic EL device: wherein R1 to R10 are described herein.

Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: A method for producing a first vadadustat intermediate represented by the following formula (3) comprising reacting a compound represented by the following formula (1) with glycine or a glycine derivative represented by the following formula (2) or a salt of the glycine or the glycine derivative in the presence of carbon monoxide. The method produces a vadadustat intermediate through a clean reaction with high atom conversion efficiency.

Abstract: The present invention relates to a boron hydroxyl-containing organic compound having a structural formula shown in formula I. The present invention also relates to a method for preparing the boron hydroxyl-containing organic compound and use thereof in an organic electronic device, particularly an organic light-emitting diode. The present invention further relates to an organic electronic device, particularly an organic light-emitting diode, including the boron hydroxyl-containing organic compound according to the present invention and use thereof in display and lighting technology. By optimizing the structure of the device and altering the concentration of the boron hydroxyl-containing organic compound in the substrate, the optimal device performance can be achieved so as to produce an OLED device with high efficiency, high brightness and high stability, which provides a better material option for use in full-color display and lighting.

Abstract: The present invention is related to methods of stabilizing an ophthalmic drug by adding a surfactant and a viscosity enhancer to the ophthalmic drug to create a composition wherein the composition has a viscosity of about 25 centipoise or less at a shear rate of 1/1000 per second at 25 degrees Celsius and a viscosity of about 70 centipoise or more at shear rate of 1 per second at 25 degrees Celsius, filling the composition into a container; and storing the container at a temperature from about 2 degrees Celsius to about 25 degrees Celsius. The present invention is further directed to a container prepared by the methods of the present invention.

Abstract: A related substance of linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline, 4,4?-(2-methylpropane-1,3-diyl)bis(2-(chloromethyl)quinazoline) and a method for synthesizing the related substance (impurity) by reacting 2-(chloromethyl)-4-methylquinazoline with acetaldehyde under an alkaline condition and a purification method are provided. The preparation method is simple and convenient to operate, short in reaction time, high in product purity, and high in yield. The synthesized related substance can be used for qualitative and quantitative analysis of the linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline and API impurities of linagliptin, so that the medication safety of the linagliptin is improved.

Abstract: The invention provides methods of chemical synthesis of the pharmacological agent 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate, also called CV-8972. The methods entail formation of a free base form of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethanol, also called CV-8814, as intermediate without producing a salt form of CV-8814.

Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.

Abstract: The present invention belongs to the pharmaceutical field, and provides the pharmaceutically acceptable salts of the compound (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine and the crystalline forms thereof, the solvates and the crystalline forms thereof, the pharmaceutical compositions comprising the same as well as the methods of preparing the same and the use thereof.