- 1,3 DI-SUBSTITUTED CYCLOBUTANE OR AZETIDINE DERIVATIVES AS HEMATOPOIETIC PROSTAGLANDIN D SYNTHASE INHIBITORS
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A compound of formula (I), wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 227-228
(2018/04/27)
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- 10,11-Methanodibenzosuberane derivatives
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10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: STR1 wherein: A is --CH2 --CH2 --, --CH2 --CHRa --CH2 --, or --CH2 --CHRa --CHRb --CH2 --, where one of Ra or Rb is H, OH, or lower acyloxy, and the other is H; R1 is H, F, Cl or Br; R2 is H, F, Cl or Br; and R3 is heteroaryl or phenyl optionally substituted with F, Cl, Br, CF3, CN, NO2 or OCHF2 ; and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.
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- A SIMPLE CONVENIENT METHOD FOR PREPARATION OF DIFLUOROMETHYL ETHERS USING FLUOROSULFONYLDIFLUOROACETIC ACID AS A DIFLUOROCARBENE PRECURSOR
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In the presence of catalytic amounts of sodium sulfate or cuprous iodide, a variety of alkyl and aryl difluoromethyl ethers were synthesized in moderate yields by the reaction of the corresponding alcohols and phenols with fluorosulfonyldifluoroacetic acid (1) in acetonitrile under mild conditions.Fluorosulfonyldifluoroacetate anion (5) is believed to readily eliminate SO2, CO2 and F(1-), thus liberating CF2:; insertion of difluorocarbene into O-H bonds and its capture by fluorode ion then result in the formation of ethers and by-product CF3H, respectively.
- Chen, Qing-Yun,Wu, Sheng-Wen
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p. 433 - 440
(2007/10/02)
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- Fluoroalkoxy substituted benzimidazoles useful as gastric acid secretion inhibitors
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Dialkoxypyridines of formula I STR1 wherein R1 is 1-3C-alkyl which is completely or predominantly substituted by fluorine, or a chlorodifluoromethyl radical and R1' is hydrogen, halo, trifluoromethyl, 1-3C-alkyl, or 1-3C-alkoxy which is optionally completely or predominantly substituted by fluorine, or R1 and R1', together with the oxygen atom to which R1 is bonded, are 1-2C-alkylenedioxy, which is optionally completely or partly substituted by fluorine, or chlorotrifluoroethylenedioxy, R3 is 1-3C-alkoxy, one of R2 and R4 is 1-3C-alkoxy and the other is a hydrogen atom or 1-3C-alkyl and n is 0 or 1, and salts thereof are new compounds with a pronounced protective action on the stomach. Processes for preparing these compounds, medicaments containing them and their use, as well as intermediate compounds and their use for preparing the subject dialkoxypyridines, are disclosed.
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- Picoline derivative useful as gastric acid secretion inhibitors
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Picoline derivatives of the formula I STR1 wherein the substituents have the meanings given in the description, and their salts are new compounds having a pronounced protective action on the stomach.
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