公开(公告)号：EP1144408A1

公开(公告)日：2001-10-17

申请号：EP00900639.6

申请日：2000-01-21

申请人： PIERRE FABRE MEDICAMENT

发明人： RIEU, Jean-Pierre ,  PATOISEAU, Jean-François ,  JOHN, Gareth ,  LEGRAND, Bruno ,  VERSCHEURE, Yvan

IPC分类号： C07D417/12 ,  C07D413/12 ,  A61K31/54 ,  A61K31/535

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (I) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2-CH(OH)-CH2- radical; R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively; and their pure enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (I) and their possible hydrates.

公开(公告)号：EP0842174B1

公开(公告)日：2001-10-04

申请号：EP96927083.4

申请日：1996-07-25

申请人： PIERRE FABRE MEDICAMENT

发明人： RIEU, Jean-Pierre ,  PATOISEAU, Jean-François ,  JOHN, Gareth, W. ,  LEGRAND, Bruno ,  VALENTIN, Jean-Pierre

IPC分类号： C07D417/12 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  C07D413/12

CPC分类号： C07D413/12 ,  C07D417/12

摘要： Novel substituted N-heterocyclyl-1-aryloxyalkyl-4-piperidineamines of formula (I), wherein each of R1 to R4, which are the same or different, is hydrogen, optionally branched C1-4 alkyl, optionally branched C1-4 alkyloxy, a halo grouping, a nitro grouping, a hydroxy grouping or a trifluoromethyl or trifluoromethoxyl grouping; R5 is hydrogen, optionally branched C1-6 alkyl, optionally branched C7-12 phenylalkyl optionally substituted on the aromatic by one or more radicals having the same definition as R1; W and X are oxygen or sulphur; Y is a C2-6 polymethylene grouping or a radical -CH2-CH(OH)-CH2-; and n is 0 or 1, are disclosed. Pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, are also disclosed. Furthermore, therapeutically acceptable organic or inorganic salts of the compounds of general formula (I), and any hydrates thereof, are disclosed. Finally, a method for preparing the claimed compounds, and their use as drugs, are disclosed.

公开(公告)号：EP1370547B1

公开(公告)日：2004-09-15

申请号：EP02759802.8

申请日：2002-03-20

申请人： PIERRE FABRE MEDICAMENT

发明人： VACHER, Bernard ,  CASTANT-CUISIAT, Florence ,  JOHN, Gareth ,  LEGRAND, Bruno

IPC分类号： C07D327/02 ,  C07C323/22 ,  A61K31/39 ,  A61P9/10

CPC分类号： C07C323/22 ,  C07D327/02

摘要： The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts.

公开(公告)号：EP1143971A1

公开(公告)日：2001-10-17

申请号：EP00900638.8

申请日：2000-01-21

申请人： PIERRE FABRE MEDICAMENT

发明人： PATOISEAU, Jean-François ,  RIEU, Jean-Pierre ,  JOHN, Gareth ,  LEGRAND, Bruno ,  VERSCHEURE, Yvan

IPC分类号： A61K31/445 ,  C07D211/58

CPC分类号： C07D211/58

摘要： The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

公开(公告)号：EP1144408B1

公开(公告)日：2002-09-25

申请号：EP00900639.6

申请日：2000-01-21

申请人： PIERRE FABRE MEDICAMENT

发明人： RIEU, Jean-Pierre ,  PATOISEAU, Jean-François ,  JOHN, Gareth ,  LEGRAND, Bruno ,  VERSCHEURE, Yvan

IPC分类号： C07D417/12 ,  C07D413/12 ,  A61K31/54 ,  A61K31/535

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (I) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2-CH(OH)-CH2- radical; R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively; and their pure enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (I) and their possible hydrates.

公开(公告)号：EP0842174A1

公开(公告)日：1998-05-20

申请号：EP96927083.0

申请日：1996-07-25

申请人： PIERRE FABRE MEDICAMENT

发明人： RIEU, Jean-Pierre ,  PATOISEAU, Jean-François ,  JOHN, Gareth, W. ,  LEGRAND, Bruno ,  VALENTIN, Jean-Pierre

IPC分类号： A61K31 ,  A61P9 ,  C07D413 ,  C07D417

CPC分类号： C07D413/12 ,  C07D417/12

摘要： Novel substituted N-heterocyclyl-1-aryloxyalkyl-4-piperidineamines of formula (I), wherein each of R1 to R4, which are the same or different, is hydrogen, optionally branched C1-4 alkyl, optionally branched C1-4 alkyloxy, a halo grouping, a nitro grouping, a hydroxy grouping or a trifluoromethyl or trifluoromethoxyl grouping; R5 is hydrogen, optionally branched C1-6 alkyl, optionally branched C7-12 phenylalkyl optionally substituted on the aromatic by one or more radicals having the same definition as R1; W and X are oxygen or sulphur; Y is a C2-6 polymethylene grouping or a radical -CH2-CH(OH)-CH2-; and n is 0 or 1, are disclosed. Pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, are also disclosed. Furthermore, therapeutically acceptable organic or inorganic salts of the compounds of general formula (I), and any hydrates thereof, are disclosed. Finally, a method for preparing the claimed compounds, and their use as drugs, are disclosed.

公开(公告)号：EP1143971B1

公开(公告)日：2004-06-02

申请号：EP00900638.8

申请日：2000-01-21

申请人： PIERRE FABRE MEDICAMENT

发明人： PATOISEAU, Jean-François ,  RIEU, Jean-Pierre ,  JOHN, Gareth ,  LEGRAND, Bruno ,  VERSCHEURE, Yvan

IPC分类号： A61K31/445 ,  C07D211/58

CPC分类号： C07D211/58

摘要： The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

公开(公告)号：EP1370547A1

公开(公告)日：2003-12-17

申请号：EP02759802.8

申请日：2002-03-20

申请人： PIERRE FABRE MEDICAMENT

发明人： VACHER, Bernard ,  CASTANT-CUISIAT, Florence ,  JOHN, Gareth ,  LEGRAND, Bruno

IPC分类号： C07D327/02 ,  C07C323/22 ,  A61K31/39 ,  A61P9/10

CPC分类号： C07C323/22 ,  C07D327/02

摘要： The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts.