- DOPAMINE D3 RECEPTOR ANTAGONISTS HAVING A BICYCLO MOIETY
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The disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.
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- 2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
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The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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- The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists
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The 5-HT2C receptor has been implicated in the regulation of appetite. As such, small molecule agonists to this receptor may serve as novel therapies to combat obesity. We describe here the identification, synthesis, and SAR of a 5-HT2C/s
- Huck, Bayard R.,Llamas, Luis,Robarge, Michael J.,Dent, Thomas C.,Song, Jianping,Hodnick, William F.,Crumrine, Chris,Stricker-Krongrad, Alain,Harrington, John,Brunden, Kurt R.,Bennani, Youssef L.
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p. 2891 - 2894
(2008/09/20)
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- 2,7-Diazabicyclo[3.3.0]octanes as novel h5-HT(1D) receptor agonists
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The conformational restriction of a (benzylamino)methyl substituted pyrrolidine to form 2,7-diazabicyclo[3.3.0]octanes has led to a series of compounds with high affinity at the h5-HT(1D) receptor as well as dramatically increased concentrations in the hepatic portal vein following oral administration.
- Russell, Michael G. N.,Beer, Margaret S.,Stanton, Josephine A.,Sohal, Bindi,Mortishire-Smith, Russell J.,Castro, Jose L.
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p. 2491 - 2496
(2007/10/03)
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- 7-(1-PYRROLIDINYL)-3-QUINOLONE-AND-NAPHTHYRIDONECARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS AND FEED ADDITIVES
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7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula in which X1 is halogen, X2 is hydrogen, halogen, amino or other radical, R1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical, R2 is hydrogen, alkyl or a dioxolylmethyl radical, R 3 i s A is N, CH, C-halogen, or the like, or forms a bridge with R1, and addition products thereof
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- Preparation of 2,7-diazabicyclo[3.3.0]octanes
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2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula STR1 in which R1, R3, R4, R5, R7 and R8 may be identical or different and in each case denote H, C1 -C5 -alkyl (optionally substituted by halogen, hydroxyl or C1 -C3 -alkoxy), C1 -C3 -alkoxycarbonyl or C6 -C12 -aryl, R4 additionally denotes halogen, R2 and R6 may be identical or different, denote H, C1 -C6 -alkyl, benzyl, C6 -C12 -aryl, C1 -C3 -alkanoyl, benzoyl or C1 -C5 -alkoxycarbonyl, or R2 and R3 together denote a bridge of the structure (CH2)n, n=2-4, CH2 --CHOH--CH2, CH2 --S--CH2 or C(CH3)2 --S--CH2, excluding 2,7-diazabicyclo[3.3.0]octane. Also their preparation by the reaction STR2 Intermediates II are also new.
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