Abstract: The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl.

Abstract: Processes for preparing pyridinecarboxamide derivatives are provided. In particular, process for preparing pyridinecarboxamide derivatives represented by general formula (I) are provided, wherein the substituents of the formula (I) are defined in the specification.

Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein L and R1 to R5 are as described herein, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.

Abstract: Crystalline form S1 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 10.7±0.2, 16.2±0.2, 19.9±0.2, 22.1±0.2, 24.7±0.2, and 25.9±0.2 degrees two-theta, crystalline form S2 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 16.4±0.2, 24.9±0.2, and 26.2±0.2 degrees two-theta, and processes of making thereof are provided.

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

Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.

Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.

Abstract: The present invention provides a single step process for the synthesis of furfuryl ethyl ether comprises refluxing the reaction mixture of furfuryl alcohol, ethanol and catalyst at temperature in the range of 80 to 120° C. for the period in the range of 3 to 7 hrs to afford furfuryl ethyl ether. The catalyst used in present invention is Zr incorporated SBA-15. Further, the conversion of furfuryl alcohol is in the range of 60 to 90%. The selectivity of reaction towards furfuryl ethyl ether is in the range of 85 to 95%.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

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: The present invention relates to polymorphic forms of compound 1 or 1a and processes for preparing compound 1 and 1a polymorphs, which are useful as antifungal agents. In particular, the invention seeks to provide a new methodology for preparing polymorphs of compound 1 and substituted derivatives thereof.

Abstract: Novel processes are disclosed for manufacture of N-(3-(5-(4-chlorophenyl)-l H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (I), wherein no protection-deprotection sequences or halogenation steps are required and use of palladium catalysts is minimized.

Abstract: A novel technique with which it is possible to suppress chemical degradation of a compound represented by general formula (1) or a salt thereof in an aqueous liquid formulation containing a compound represented by general formula (1) or a salt thereof. A method for suppressing the generation of a compound represented by general formula (2) or a salt thereof including containing a compound represented by general formula (1) or a salt thereof and a magnesium compound in an aqueous liquid formulation.

Abstract: The invention discloses a class of compounds for treating or preventing hyperuricemia or gout, which is a compound shown in general formula (I) or a pharmaceutically acceptable salt. These compounds and their pharmaceutically acceptable salts in the invention are useful for the promotion of uric acid excretion to treat or prevent hyperuricemia or gout.

Abstract: Disclosed herein is an improved process for preparation of Lenalidomide and crystalline polymorphic forms thereof.

Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.

Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.

Abstract: The present disclosure provides a process for preparing (1S,2S)-2-fluoro-N-(6-(4-methylpyridin-3-yl)benzo[d]thiazol-2-yl) cyclopropanecarboxamide or a salt thereof, such as the compound of Formula (I), comprising: reacting Compound 1 as a starting material with Compound 2 in the presence of Pd(dppf)Cl2 and 1,4-dioxane to form Compound 3; reacting Compound 3 with Compound 4 in the presence of HATU and DIPEA to produce Compound 5; and reacting Compound 5 with hydrochloric acid to produced Formula (I).

Abstract: The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C1-C6 alkyl, and C1-C6 alkoxy, and R1 is C1-C6 alkyl or C1-C6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R2 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.