Japanese Patent JPS6158456

B2

Compounds having the formulawherein A when taken individually is hydrogen; B when taken individually is hydroxy or alkanoyloxy having from one to five carbon atoms;A and B when taken together are oxo;R, is hydrogen, benzyl, or R₁' wherein R₁' is alkanoyl having from one to five carbon atoms, P(O) (OH)₂ and mono-and disodium and potassium salts thereof, -CO(CH₂)₂COOH and the sodium and potassium salts thereof, or -CO(CH₂)_pNR₄R₅ wherein p is 0 or an integer from 1 to 4, each of R₄ and R₅ when taken individually is hydrogen or alkyl having from one to four carbon atoms; R₄ and R₅ when taken together with the nitrogen to which they are attached are piperidino, pyrrolo, pyrrolidino, morpholino or N-alkylpiperazino having from one to four carbon atoms in the alkyl group;R₂ when taken individually is hydrogen;R₃ when taken individually is hydrogen, methyl, hydroxy, hydroxymethyl, -OR,' or -CH₂OR₁'; R₂ and R₃ when taken together are oxo, methylene or alkylenedioxy having from two to four carbon atoms;W is hydrogen, pyridyl, orwherein W, is hydrogen, chloro or fluoro;when W is hydrogen, Z is(a) alkylene having from five to thirteen carbon atoms; or(b) -lalk₁)_m-O-(alk₂)_n- wherein each of (alk,) and (alk₂) is alkylene having from one to thirteen carbon atoms; each of m and n is 0 or 1; with the provisos that the summation of carbon atoms in (alk₁) plus (alk₂) is not less than five or greater than thirteen; and at least one of m and n is 1; when W is other than hydrogen, Z is(a) alkylene having from three to eight carbon atoms; or(b) -(elk₁)_m-O-(alk₂)_n- wherein each of (alk₁) and (alk₂) is alkylene having from one to eight carbon atoms; each of m and n is 0 or 1; with the provisos that the summation of carbon atoms in (alk,) plus (alk₂) is not less than three or greater than eight; and at least one of m and n is 1;or a pharmaceutically acceptable acid addition salt of those compounds wherein R, is -CO(CH₂)_pNR₄R₅ and/or W is pyridyl; pharmaceutical compositions containing them, and processes for their preparation. The compounds are particularly useful in the treatment of nausea and as analgesics.

MAIKERU ROSU JONSON
ROORENSU SHEAMAN MERUBIN JUNIAA

JP14772381A

December 11, 1986

September 18, 1981

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PFIZER

A61K31/00; C07D295/08; A61K31/045; A61K31/05; A61K31/085; A61K31/12; A61K31/335; A61K31/357; A61P1/00; A61P25/00; A61P25/04; C07C27/00; C07C39/17; C07C39/23; C07C39/42; C07C41/00; C07C43/196; C07C43/20; C07C43/23; C07C45/00; C07C45/59; C07C45/67; C07C45/69; C07C49/623; C07C49/747; C07C49/753; C07C62/38; C07C67/00; C07C69/035; C07C69/353; C07C229/06; C07D295/14; C07D295/15; C07D317/00; C07D317/72; C07D319/00; C07D319/08; C07D321/00; C07D321/10; C07D405/04; C07D493/06; C07D493/10; C07F9/12

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