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3,5-Disubstituted 4-fluoroisoxazole, 4,4,5-trifluoroisoxazoline and 4,4-difluoro-5-hydroxyisoxazoline products were obtained from reaction of the corresponding isoxazoles with Selectfluor depending upon the reaction conditions. Although the fluorinations proceeded using conventional heating, microwave (muW) irradiation considerably shortened reaction times and enabled a high yielding one-pot cascade fluorination-cyclization from simple diketone substrates. In addition, a related 4-fluoroisoxazole-3-carboxyamide derivative was synthesized.

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The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

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The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R1 is substituted alkyl or alkoxy each of up to 3 carbon atoms; R2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms; Ar is phenylene or heterocyclene; L is a group of the formula –CO.NH–, –NH.CO–, –CO.NR3 –, –NR3. CO–, –CH=CH–, –CH2 O–, –OCH2, –CH2 S–, –SCH2 –, –CO.CH2 –, –CH2.CO– or –CO.O–, wherein R3 is alkyl of up to 6 carbon atoms; and Y is aryl or heteroaryl or a hydrogenated derivative thereof: or Y is a group of the formula –A–Y1 in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y1 is aryl or heteroaryl or a hydrogenated derivative thereof; or a pharmaceutically-acceptable salt thereof.

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The present invention relates to polycyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 to R4, R7 to R10, Y and A are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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The present invention relates to a diarylethene derivative and a photochromic thin film using the same. More particularly, it relates to a diarylethene derivative and a photochromic thin film having excellent transparency prepared by depositing the same on the surface of a substrate, without crystallization or agglomeration to have effective photochromic property. This method also provides homogenous thin photochromic films with film thickness of a nano meter level and improved processability compared to conventional deposition processes thus, being suitable for coloring change with light repeatedly, optical information recording systems, and optical communication media.

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Provided are a reactive mesogen that may improve display quality of a liquid crystal display, and a liquid crystal composition including the same. The reactive mesogen is represented by the following Formula: where A1, A2, and A3 are each independently a substituted or unsubstituted divalent hydrocarbon ring, or a substituted or unsubstituted divalent heterocycle, L1 and L2 are each independently a direct linkage, ?O?, ?S?, ?CO?, ?COO?, ?OCOO?, ?O(CH2)k1?, ?S(CH2)k1?, ?O(CF2)k1?, ?S(CF2)k1?, ?(CH2)k1?, ?CF2CH2?, ?(CF2)k1?, ?CH?CH?, ?CF?CF?, ?C?C?, ?CH?CH?COO?, or ?(CH2)k1?COO?(CH2)k2?O?, Z1 and Z2 are each independently a direct linkage, ?O?, ?S?, ?CO?, ?COO?, ?OCOO?, ?O(CH2)m1?, ?S(CH2)m1?, ?O(CF2)m1?, ?S(CF2)m1?, ?(CH2)m1?, ?CF2CH2?, ?(CF2)m1?, ?CH?CH?, ?CF?CF?, ?C?C?, ?CH?CH?COO?, ?(CH2)m1?COO?, ?(CH2)m1?COO?(CH2)m2?O?, ?CH?(Sp?Pa)?, ?CH2CH?(Sp?Pa)?, or ?(CH?(Sp?Pa)?CH?(Sp?Pa))?, Pa is a polymerizable group, B is an unsubstituted heterocycle, a substituted or unsubstituted crown ether group, or wherein T1 and T2 are each independently ?OH, ?CH3, ?CF3, ?CHF2, ?CH2F, ?CH2Br, ?CHBr2, ?CHCl2, or ?CH2Cl.

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Compounds of formula (I), wherein X is O, S, NH, OCO, NH-CO, NH-COO, NH-CO-NH, NH-CS or NH-CS-NH; R4 is H, (C1-C3)-alkyl optionally substituted by halogen, or a C-linked heterocyclic radical selected from several possibilities; R1 and R3 are H or F; and R2 is an N-linked or C-linked heterocyclic radical, are useful in the treatment of microbial infections in human or animal body.

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The invention relates to new pyridinyl derivatives of the formula (I) wherein R1 and A are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R 1 , R 2 , R 3 , R 4 , A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollipger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma

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Substituted pteridines for the treatment of inflammatory diseases

The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

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