- MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
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- NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS
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The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
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- NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS
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The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
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- THIAZOLE AND OXAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
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Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
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Page/Page column 38
(2012/02/03)
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- NEW AMINOTHIAZOLES AS FBPASE INHIBITORS FOR DIABETES
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Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
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- THIAZOLE AND OXAZOLE-SUBSTITUTED ARYLAMIDES
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Compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: R1 is a group of formula A or formula B; and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
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Page/Page column 62
(2008/12/05)
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- 1-Oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides
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Antiallergy and antiulcer agents having the formula (I), STR1 and their pharmaceutically acceptable salts, wherein R1 and R2 taken separately are each hydrogen or lower alkyl; and R1 and R2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), STR2 wherein R1 and R2 are as defined above and R3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R1 and R2 are defined as above, and R3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
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- Antiulcer thiazol-2-ylcarbamoyl-carboxylic acids, esters and amides
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This invention encompasses orally effective antiulcer agents of the formula STR1 wherein X is hydroxy, (C1 -C5)-alkoxy, phenoxy, benzyloxy, or --NH(CH2)n Y wherein n is an integer of value 2 to 4 and Y is di-(C1 -C3)-alkylamino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl; R' and R" when taken together are (C3 -C8)-alkylene, with the proviso that the ring so formed is 5- to 8-membered; R' and R" when taken separately are each independently hydrogen, (C1 -C6)-alkyl or (C5 -C6)-cycloalkyl, with the proviso that when X is other than --NH(CH2)n Y, at least one of R' and R" is other than hydrogen; the pharmaceutically acceptable cationic salts thereof when X is hydroxyl, and the pharmaceutically acceptable anionic salts thereof when X is --NH(CH2)n Y.
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- SYNTHETIC APPLICATIONS OF 2-CHLOROOXIRANES: PREPARATION OF THIAZOLES, DIHYDROTHIAZOLES AND SELENAZOLES
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The reaction of 2-chlorooxiranes 1 with thioamides and thioureas provides access to thiazoles, 4-hydroxy-4,5-dihydrothiazoles and 2-imino-2,3-dihydrothiazoles under mild conditions and excellent yields.With 1 and selenourea, near quantitative yields of se
- Gasteiger, Johann,Herzig, Christian
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p. 2607 - 2611
(2007/10/02)
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