- Amide-based atropisomers in tachykinin NK1-receptor antagonists: Synthesis and antagonistic activity of axially chiral N-benzylcarboxamide derivatives of 2,3,4,5-tetrahydro-6H-pyrido[2,3-b][1,5]oxazocin-6-one
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A series of novel N-benzylcarboxamide derivatives of bicyclic compounds, 3,4-dihydropyrido[3,2-f][1,4]oxazepin-5(2H)-one and 2,3,4,5-tetrahydro-6H- pyrido[2,3-b][1,5]oxazocin-6-one, were synthesized by cyclization of N-benzyl-2-chloro-N-(2-hydroxyethyl)-
- Ishichi, Yuji,Ikeura, Yoshinori,Natsugari, Hideaki
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p. 4481 - 4490
(2007/10/03)
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- HETEROCYCLIC COMPOUNDS, THEIR PRODUCTION AND USE
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A compound represented by the formula: wherein ring M is a heterocyclic ring wherein--X=Yis one of--N=C,--CO--N or--CS--N; Ra and Rb are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, with the proviso that at least one of them is an optionally substituted heterocyclic ring; Ring C is an optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted nitrogen-containing heterocyclic ring; and n is an integer from 1 to 6, or a salt thereof has a tachykinin receptor antagonistic activity in vitro, and is useful for preventing or treating depression, anxiety, manic-depressive illness or psychopathy.
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- DRUGS
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The present invention relates to a medicine which comprises a compound (I) of the formula:[wherein the ring M is a heterocylic ring having -N=Ca and Rb are bound to each other to form the ring A, or they are the same or different each representing a hydrogen atom or a substituent on the ring M;the rings A and B each is an optionally substituted homocycle or heterocycle, and at least one of them is an optionally substituted heterocycle;the ring C is an optionally substituted homocycle or heterocycle;the ring Z is an optionally substituted nitrogen-containing heterocycle; andn is an integer of 1 to 6] or a salt thereof in combination with a drug having an emetic action. The compounds (I) or their salts are useful as anti-emetic drugs. Particularly, vomiting caused by drugs having an emetic action can be inhibited by these compounds rapidly and safely at a low dose.
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- CYCLIC COMPOUNDS, THEIR PRODUCTION AND USE
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Novel compounds of the following general formula or salts thereof. STR1 wherein Ring M is a heterocyclic ring having--N=C ,--CO--N or--CS--N as the partial structure--X . . . Y ; R. sup.a and R. sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.
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