- NITROGEN-CONTAINING 6-MEMBERED CYCLIC COMPOUND
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A novel compound represented by the following general formula (1), or a salt thereof, which has a superior EP4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
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Paragraph 0503-0505
(2020/12/01)
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- COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I) wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
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Paragraph 0314; 0412; 0413
(2018/02/27)
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- FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE
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This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O?X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
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Page/Page column 29
(2008/06/13)
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- Extension of the Heck reaction to the arylation of activated thiophenes
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The direct arylation of activated thiophenes was accomplished in moderate to good yields using a Heck-type reaction with the mixture of Pd(OAc)2 and n-Bu4NBr as a catalytic system. This new arylation method is applied to different derivatives and has proved to be compatible with sensitive functional groups. Furthermore, the substituent nature and position on the thiophene moiety influence the cross coupling. In particular the substitution is regiospecific when the heterocycle is substituted at position 2 with an electron withdrawing group.
- Lavenot,Gozzi,Ilg,Orlova,Penalva,Lemaire
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- Direct thiophene arylation catalysed by palladium
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Direct thiophene arylation using a Heck-type reaction with Pd(OAc)2/NBu4Br as catalytic system is reported. Reactions with 2- and 3-substituted thiophenes have shown that substituent nature and position influence the cross-coupling.
- Gozzi, Christel,Lavenot, Laurence,Ilg, Kerstin,Penalva, Vincent,Lemaire, Marc
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p. 8867 - 8870
(2007/10/03)
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