- An intra/intermolecular suzuki sequence to benzopyridyloxepines containing geometrically pure exocyclic tetrasubstituted alkenes
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(Chemical Equation Presented) A route to enable the preparation of 5-benzylidenyl-benzopyridyloxepine analogues was developed to continue our research in the field of nuclear hormone receptor modulators. The key steps are1) a syn-stereoselective diboratio
- Carson, Matthew W.,Giese, Matthew W.,Coghlan, Michael J.
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supporting information; experimental part
p. 2701 - 2704
(2009/05/26)
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- Piperazine Heteroaryl Derivatives as Gpr38 Agonists
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The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
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Page/Page column 13
(2009/01/24)
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- PIPERAZINE HETEROARYL DERIVATES AS GPR38 AGONISTS
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The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, (I) wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
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Page/Page column 39
(2010/11/25)
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- ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
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Page/Page column 120-121
(2010/10/20)
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- NOVEL BIAROMATIC COMPOUNDS, INHIBITORS OF THE P2X7-RECEPTOR
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The invention provides compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar1 represents a group (II), (III), (IV) or (V), and A, Ar2, n, R1, R2, R3, R4 and R
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Page/Page column 58-59
(2008/06/13)
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- Application of organolithium compounds in organic synthesis. Part 19. Synthetic strategies based on aromatic metallation. A concise regiospecific synthesis of 3-halogenated picolinic and isonicotinic acids
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The synthesis of the halogenated picolin- and isonicotinalides (3) and (4) via metallation (n-BuLi) of the anilides (1) and (2) and then the reaction of the generated bis-lithiated anilides with halogenating agents (CCl3-CCl3, CH2Br-CH2Br, I2) followed by subsequent acidic hydrolysis of (3) and (4), as a way of regiospecific transformation of picoline and isonicotine acids into their C3-halogenated derivatives, is described.
- Epsztajn,Plotka,Grabowska
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p. 1075 - 1086
(2007/10/03)
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