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公开(公告)号:AU761605B2
公开(公告)日:2003-06-05
申请号:AU2257700
申请日:2000-03-24
Applicant: SERVIER LAB
Inventor: LESIEUR DANIEL , YOUS SAID , DESCAMPS-FRANCOIS CAROLE , LEFOULON FRANCOIS , GUILLAUMET GERALD , VIAUD MAIRE-CLAUDE , BENNEJEAN CAROLINE , DELAGRANGE PHILIPPE , RENARD PIERRE
IPC: C07D339/08 , A61K31/16 , A61K31/165 , A61K31/33 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/437 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P15/18 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , B01J31/24 , C07B61/00 , C07C231/12 , C07C233/18 , C07C233/20 , C07C233/36 , C07C233/60 , C07C233/73 , C07C235/34 , C07C271/16 , C07C275/24 , C07C319/14 , C07C323/42 , C07D209/14 , C07D209/16 , C07D307/68 , C07D307/79 , C07D307/81 , C07D311/58 , C07D319/20 , C07D333/58 , C07D471/04 , C07D519/00 , C07D319/16 , A61K31/4439 , A61K31/444 , C07C233/17 , C07C271/08 , C07C275/22 , C07D209/36 , C07D307/82 , C07D307/83 , C07D307/91 , C07D333/60 , C07D333/64
Abstract: Compounds (I) selected from alkylenedioxybisnaphthalene derivatives and related compounds are new. Compounds of formula (I) other than diethyl 2-acetylamino-2-(5-(3-(2-acetylamino-3-ethoxy-2-ethoxycarbonyl-3-oxopr opyl)-1H-indol-5-ylmethyl)-1H-indol-3-ylmethyl)malonate and N-(2-(5-(3-(2-acetylaminoethyl)-1H-indol-5-ylmethyl)-1H-indol-3-yl)eth yl)acetamide are new. A = NR -C(Q)-R , NR -C(Q)-NR R or C(Q)-NR R ; Q = O or S; R - R = H or R; or NR R = 1-piperazinyl, piperidino or pyrrolidino; R = optionally Q'-substituted 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl or (3-8C cycloalkyl)-(1-6C alkyl); 1-6C polyhaloalkyl; or optionally Q-substituted aryl, aryl(1-6C alkyl), aryl(2-6C alkenyl), heteroaryl, heteroaryl-(1-6C alkyl) or heteroaryl-(2-6C alkenyl); B = NR -C(Q)-R , NR -C(Q)-NR R , C(Q)-NR R , C(Q)-OR , NR -C(Q)-OR or NR R ; G1, G3 = 1-4C alkylene optionally substituted by one or more of OH, COOH, CHO, R, OR, C(O)OR or C(O)R; Cy = a group of formula (i) in which G2 is attached to the benzene ring and G1 or G3 is attached to the other ring, or a group of formula (ii) in which G2 is attached to the D ring and G1 or G3 is attached to the other ring: X, Y' = S, O, C, CH or CH2; R = H, halogen, CF3, OH, COOH, CHO, NH2, NHR, NRR', NHC(O)R, C(O)NHR, R, OR, C(O)R or COOR; R' = R; Z' = S, O, CH, CH2, NH, NSO2-phenyl or NR; D' = a benzene or pyridine ring; G2 = an optionally substituted W1(CH2)nW2(CH2)mW3 group containing no adjacent heteroatoms; W1-W3 = bond, O, S, CH2, CHR, NH or NR; n, m = 0 - 6; Q' = one or more of OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2, 1-6C alkylamino, di(1-6C alkyl)amino and halogen; aryl = naphthyl, phenyl or biphenylyl; heteroaryl = a saturated or unsaturated mono- or bicyclic group containing 5-10 C atoms and 1-3 heteroatoms selected from N, S and O; and Q = OH, COOH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CHO, CN, NO2, NH2, 1-6C alkylamino, di(1-6C alkyl)amino and halogen. Independent claims are also included for the following: (1) a process for preparing (I); and (2) compounds of formula (II) other than N-(2-(5-(2-hydroxyethoxy)-1H-indol-3-yl)ethyl)acetamide. W4 = O, S, NH or NR; and E' = OH or halogen; provided that W4-(CH2)n-W2-(CH2)m is not oxyalkylene when Cy is naphthylene and G1-A is (CH2)2-NR CQR or (CH2)2-NR CQNR R .
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公开(公告)号:FR2830012A1
公开(公告)日:2003-03-28
申请号:FR0112205
申请日:2001-09-21
Applicant: SERVIER LAB
Inventor: LESIEUR DANIEL , BLANC DELMAS ELODIE , BENNEJEAN CAROLINE , CHAVATTE PHILIPPE , GUILLAUMET GERALD , DACQUET CATHERINE , LEVENS NIGEL , BOUTIN JEAN ALBERT , RENARD PIERRE
IPC: A61P3/10 , A61P9/10 , A61P17/06 , A61P19/10 , A61P35/00 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/428
Abstract: Benzothiazolyl derivatives (I), their enantiomers, diastereoisomers, and addition salts with acids and bases. Benzothiazolyl derivatives of formula (I), their enantiomers, diastereoisomers, and addition salts with acids and bases. X = O, S, CH2 or is CH linked to R ; Y = O or S; R and R = H, alkyl, aralkyl, aryloxy, arylalkyloxy, alkoxy, OH, amino, mono- and di-alkylamino; or R +R = oxo, thioxo, or imino; A = alkylene in which one methylene group may be replaced by O, S, or NH, N-alkyl, phenylene or naphthylene; B = alkylene, alkenylene, or alkynylene; D and D' = a benzene or pyridine ring, optionally substituted by 1-3 halo, CN, NO2, R, OR, -S(O)n-R, C(Z)R, -CH(OR)-R', C(Z)OR, NRR', C(Z)NRR', -CR=N-OR, -NR-C(Z)R', -NR-C(Z)OR', and OC(Me)2-COOR; R and R' = H, alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroarylalkyl, cycloalkyl, or cycloalkyl alkyl; Z = O or S; n = 0-2; R and R = H, halo, R, OR, or NRR'; or R +R = 5-6 membered ring that may contain O, N, or S; R = H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylcarbonyl, arylcarbonyl, or heteroaryl carbonyl, all of which may be substituted by one or more R , -CH2CHR R , -CH=CR R , halo, OH, NO2, CN, NH2 or alkoxy; R = -(CH2)t-C(=Z)Z'; t = 0-6; Z' = OR or NRR'; R and R = -C(=Z)Z' Where alkyl, alkoxy, alkylene, alkenyl, alkynyl, alkenylene and alkynylene groups have 1-6 C atoms, cycloalkyl groups have 3-8 C atoms, aryl means phenyl, naphthyl, or biphenyl, optionally partially hydrogenated, heteroaryl groups have one or two rings containing 5-10 members, optionally partially hydrogenated and containing 1-3 O, N and/or S atoms, and the aryl and heteroaryl groups may be substituted by 1-3 groups selected from alkyl, alkoxy, carboxy, formyl, amino, mono- and dialkylamino, ester, amido, NO2, CN, and OC(Me)2COOR.
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公开(公告)号:NO20031043A
公开(公告)日:2003-03-06
申请号:NO20031043
申请日:2003-03-06
Applicant: SERVIER LAB
Inventor: DESCAMPS-FRANCOIS CAROLE , YOUS SAID , LESIEUR DANIEL , GUILLAUMET GERALD , VIAUD MARIE-CLAUDE , COSTA HERVE DA , BENNEJEAN CAROLINE , DELAGRANGE PHILIPPE , RENARD PIERRE
IPC: C07D333/58 , A61K31/235 , A61K31/343 , A61K31/381 , A61K31/4045 , A61K31/437 , A61P3/04 , A61P3/10 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/20 , A61P25/28 , A61P35/00 , C07C231/12 , C07C233/18 , C07C233/60 , C07D209/08 , C07D209/20 , C07D307/68 , C07D307/79 , C07D307/81 , C07D333/54 , C07D471/04 , A61K31/165
CPC classification number: C07D307/79 , C07C233/18 , C07C233/60 , C07C2601/04 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D307/68 , C07D333/54 , C07D471/04
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公开(公告)号:NZ507692A
公开(公告)日:2002-06-28
申请号:NZ50769299
申请日:1999-05-10
Applicant: SERVIER LAB
Inventor: DELAGRANGE PHILIPPE , LESIEUR DANIEL , KLUPSCH FREDERIQUE , GUILLAUMET GERALD , VIAUD MARIE-CLAUDE , LANGLOIS MICHEL , BENNEJEAN CAROLINE , RENARD PIERRE
IPC: C07D295/12 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/27 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/357 , A61K31/381 , A61K31/382 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/437 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/453 , A61K31/454 , A61K31/473 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P3/06 , A61P3/10 , A61P5/02 , A61P9/00 , A61P15/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P35/00 , A61P43/00 , C07C233/36 , C07C233/40 , C07C233/43 , C07C233/62 , C07C233/65 , C07C237/48 , C07C271/20 , C07C271/30 , C07C275/24 , C07C275/40 , C07C311/46 , C07C317/32 , C07C323/40 , C07C323/41 , C07C323/44 , C07C323/62 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/20 , C07D209/60 , C07D209/90 , C07D213/70 , C07D221/08 , C07D221/10 , C07D233/42 , C07D233/84 , C07D235/06 , C07D235/14 , C07D261/20 , C07D295/18 , C07D307/68 , C07D307/77 , C07D307/81 , C07D307/92 , C07D311/58 , C07D311/60 , C07D311/92 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/40 , C07D333/50 , C07D333/56 , C07D333/58 , C07D333/74 , C07D335/06 , C07D335/08 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/06 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/048 , C07D491/052 , C07D493/04 , C07D495/04 , C07D495/14 , C07D521/00 , C07C311/37 , C07D307/85
Abstract: A compound of the general formula R-A-R' for use in the treatment of seasonal affective disorder, sleep disorder, cardiovascular pathologies, insomnia and fatigue resulting from jet-lag, appetite disorders and obesity. Wherein; A represents a ring system of Formula (II), (III) or (IV); R represents a group of formula (V), (VI), (VII) or (VIII); and R' represents a group of Formula (IX), wherein R5 represents a group of Formula X.
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公开(公告)号:DK0708099T3
公开(公告)日:2002-02-11
申请号:DK95402331
申请日:1995-10-19
Applicant: SERVIER LAB
Inventor: LECLERK VERONIQUE , LESIEUR DANIEL , RENARD PIERRE , DEPREUX PATRICK , AIT MANSOUR HAMID , DELAGRANGE PHILIPPE
IPC: A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/41 , A61P3/04 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/28 , A61P35/00 , A61P37/06 , A61P43/00 , C07C233/13 , C07C233/20 , C07C233/60 , C07D307/92 , C07D311/92 , C07D491/04 , C07D491/044 , C07D491/052 , C07D493/04 , C07D495/04 , C07C233/18 , C07C275/22
Abstract: Tricyclic amides of formula (I), their enantiomers, diastereoisomers, and salts are new. R = 1-4C alkylene, opt. substd. by alkyl, OH, alkoxycarbonyl, or COOH; R = H or alkyl; R = a group R which is -C(=X')-(CH2)n-R or a group R which is -C(=X)-NH-(CH2)m -R ; m and n = 0-3; R5, R6 = H, alkyl, alkenyl, alkynyl, cycloalkyl, or di-cycloalkyl-alkyl (all opt. substd.); X, X' = O or S; A = -O-A -; A = 2-5C alkylene, alkenylene, or alkynylene which may be substd. by alkyl, alkoxy, OH and oxo gps.; Y forms, with the benzene ring to which it is attached, a group Y which is naphthalene, benzofuran, or benzothiophene, all of which may be partially hydrogenated, or indole; provided that the substitutions on alkyl, alkenyl, and alkynyl groups are halogen, alkyl, or alkoxy, while the substitution on cycloalkyl and di-cycloalkyl-alkyl groups are alkyl, alkoxy, hydroxy, or oxo. Alkyl, alkoxy, alkenyl and alkynyl groups have up to 6C, and cycloalkyl groups have up to 8C, and may be satd. or unsatd. Intermediates of formula (II) and (VI) are new. Z = a reactive gp.; A = 2-5C alkenyl opt. substd. by 1-6C alkyl.
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公开(公告)号:PT841330E
公开(公告)日:2001-10-30
申请号:PT97402655
申请日:1997-11-06
Applicant: SERVIER LAB
Inventor: LESIEUR DANIEL , RENARD PIERRE , RETTORI MARIE-CLAIRE , NEWMAN-TANCREDI ADRIAN , CAIGNARD DANIEL-HENRI , DEPREUX PATRICK , CARATO PASCAL , BONTE JEAN-PAUL , MILLAN MARK
IPC: A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61P25/00 , A61P25/18 , C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/36 , A61K31/415 , A61K31/54
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公开(公告)号:HK1032042A1
公开(公告)日:2001-07-06
申请号:HK01102647
申请日:2001-04-12
Applicant: SERVIER LAB
Inventor: LESIEUR DANIEL , YOUS SAID , DESCAMPS-FRANCOIS CAROLE , LEFOULON FRANCOIS , GUILLAUMET GERALD , VIAUD MARIE-CLAUDE , BENNEJEAN CAROLINE , DELAGRANGE PHILIPPE , PENARD PIERRE
IPC: C07D339/08 , A61K31/16 , A61K31/165 , A61K31/33 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/437 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P15/18 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , B01J31/24 , C07B61/00 , C07C231/12 , C07C233/18 , C07C233/20 , C07C233/36 , C07C233/60 , C07C233/73 , C07C235/34 , C07C271/16 , C07C275/24 , C07C319/14 , C07C323/42 , C07D209/14 , C07D209/16 , C07D307/68 , C07D307/79 , C07D307/81 , C07D311/58 , C07D319/20 , C07D333/58 , C07D471/04 , C07D519/00 , C07C , C07D , A61K , A61P
Abstract: Compounds (I) selected from alkylenedioxybisnaphthalene derivatives and related compounds are new. Compounds of formula (I) other than diethyl 2-acetylamino-2-(5-(3-(2-acetylamino-3-ethoxy-2-ethoxycarbonyl-3-oxopr opyl)-1H-indol-5-ylmethyl)-1H-indol-3-ylmethyl)malonate and N-(2-(5-(3-(2-acetylaminoethyl)-1H-indol-5-ylmethyl)-1H-indol-3-yl)eth yl)acetamide are new. A = NR -C(Q)-R , NR -C(Q)-NR R or C(Q)-NR R ; Q = O or S; R - R = H or R; or NR R = 1-piperazinyl, piperidino or pyrrolidino; R = optionally Q'-substituted 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl or (3-8C cycloalkyl)-(1-6C alkyl); 1-6C polyhaloalkyl; or optionally Q-substituted aryl, aryl(1-6C alkyl), aryl(2-6C alkenyl), heteroaryl, heteroaryl-(1-6C alkyl) or heteroaryl-(2-6C alkenyl); B = NR -C(Q)-R , NR -C(Q)-NR R , C(Q)-NR R , C(Q)-OR , NR -C(Q)-OR or NR R ; G1, G3 = 1-4C alkylene optionally substituted by one or more of OH, COOH, CHO, R, OR, C(O)OR or C(O)R; Cy = a group of formula (i) in which G2 is attached to the benzene ring and G1 or G3 is attached to the other ring, or a group of formula (ii) in which G2 is attached to the D ring and G1 or G3 is attached to the other ring: X, Y' = S, O, C, CH or CH2; R = H, halogen, CF3, OH, COOH, CHO, NH2, NHR, NRR', NHC(O)R, C(O)NHR, R, OR, C(O)R or COOR; R' = R; Z' = S, O, CH, CH2, NH, NSO2-phenyl or NR; D' = a benzene or pyridine ring; G2 = an optionally substituted W1(CH2)nW2(CH2)mW3 group containing no adjacent heteroatoms; W1-W3 = bond, O, S, CH2, CHR, NH or NR; n, m = 0 - 6; Q' = one or more of OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2, 1-6C alkylamino, di(1-6C alkyl)amino and halogen; aryl = naphthyl, phenyl or biphenylyl; heteroaryl = a saturated or unsaturated mono- or bicyclic group containing 5-10 C atoms and 1-3 heteroatoms selected from N, S and O; and Q = OH, COOH, 1-6C alkoxy, 1-6C alkyl, 1-6C polyhaloalkyl, CHO, CN, NO2, NH2, 1-6C alkylamino, di(1-6C alkyl)amino and halogen. Independent claims are also included for the following: (1) a process for preparing (I); and (2) compounds of formula (II) other than N-(2-(5-(2-hydroxyethoxy)-1H-indol-3-yl)ethyl)acetamide. W4 = O, S, NH or NR; and E' = OH or halogen; provided that W4-(CH2)n-W2-(CH2)m is not oxyalkylene when Cy is naphthylene and G1-A is (CH2)2-NR CQR or (CH2)2-NR CQNR R .
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28.
公开(公告)号:AU3610499A
公开(公告)日:1999-11-29
申请号:AU3610499
申请日:1999-05-10
Applicant: SERVIER LAB
Inventor: LESIEUR DANIEL , KLUPSCH FREDERIQUE , GUILLAUMET GERALD , VIAUD MARIE-CLAUDE , LANGLOIS MICHEL , BENNEJEAN CAROLINE , RENARD PIERRE , DELAGRANGE PHILIPPE
IPC: C07D295/12 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/27 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/357 , A61K31/381 , A61K31/382 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/437 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/453 , A61K31/454 , A61K31/473 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P3/06 , A61P3/10 , A61P5/02 , A61P9/00 , A61P15/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P35/00 , A61P43/00 , C07C233/36 , C07C233/40 , C07C233/43 , C07C233/62 , C07C233/65 , C07C237/48 , C07C271/20 , C07C271/30 , C07C275/24 , C07C275/40 , C07C311/46 , C07C317/32 , C07C323/40 , C07C323/41 , C07C323/44 , C07C323/62 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/20 , C07D209/60 , C07D209/90 , C07D213/70 , C07D221/08 , C07D221/10 , C07D233/42 , C07D233/84 , C07D235/06 , C07D235/14 , C07D261/20 , C07D295/18 , C07D307/68 , C07D307/77 , C07D307/81 , C07D307/92 , C07D311/58 , C07D311/60 , C07D311/92 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/40 , C07D333/50 , C07D333/56 , C07D333/58 , C07D333/74 , C07D335/06 , C07D335/08 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/06 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/048 , C07D491/052 , C07D493/04 , C07D495/04 , C07D495/14 , C07D521/00 , C07C311/37 , C07D307/85
Abstract: The invention concerns compounds of formula (I): R-A-R' wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R 1 , R 2 , R 3 , v and R 4 are as defined in the description; R' represents a -(CH 2 )t-R 5 group wherein t and R 5 are as defined in the description.
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公开(公告)号:AU8021594A
公开(公告)日:1995-06-15
申请号:AU8021594
申请日:1994-12-05
Applicant: SERVIER LAB
Inventor: DEPREUX PATRICK , AIT MANSOUR HAMID , LESIEUR DANIEL , LEFOULON FRANCOIS , RENARD PIERRE , ADAM GERARD , DELAGRANGE PHILIPPE
IPC: A61K31/165 , A61K31/17 , A61K31/18 , A61K31/215 , A61K31/22 , A61P1/00 , A61P3/04 , A61P9/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/12 , C07C233/18 , C07C233/25 , C07C233/31 , C07C233/60 , C07C233/61 , C07C273/18 , C07C275/24 , C07C275/26 , C07C327/42 , C07C327/46 , C07C275/46 , C07C233/05 , C07C233/58 , A61K31/16
Abstract: Naphthalene derivatives of formula (I), their optical isomers and mixtures, and their acid addition salts, are new. X = O or S; R = H, OH, (substd.) alkyl, (substd.) alkoxy; R1 = H or alkyl; R2 = H, (substd.) alkyl, (substd.) alkenyl, (substd.) cycloalkyl, or (substd.) cycloalkyl alkyl or -NHR4; R3 = OH, 2-6C (substd.) alkyl, (substd.) cycloalkyl alkyl, (substd.) alkenyl or alkynyl, R5-alkyl, or -OCO-R6; R4 = (substd.) alkyl, cycloalkyl or cycloalkyl alkyl; R5 = (substd.) pyridyl, phenyl, naphthyl, thienyl, furyl, pyrimidyl, indolyl, benzofuryl, benzothienyl, isoquinolyl, or quinolyl; -CO-R6 = (1-5C) alkyl, cycloalkyl, cycloalkyl (1-5C) alkyl, R5, and R5 - (1-5C) alkyl. Unless indicated otherwise, alkyl, alkenyl, alkynyl and alkoxy groups have up to 6C, cycloalkyl has 3-8C, optional substituents on alkyl, cycloalkyl and alkoxy groups may be one or more halogens, alkyl or alkoxy groups, and optional substituents on R5 may be one or more alkyl, alkoxy, halogen, OH or CF3 groups on the aromatic ring(s).
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公开(公告)号:AU7137591A
公开(公告)日:1991-08-29
申请号:AU7137591
申请日:1991-02-26
Applicant: SERVIER LAB
Inventor: ANDRIEUX JEAN , HOUSSIN RAYMOND , YOUS SAID , GUARDIOLA BEATRICE , LESIEUR DANIEL
IPC: A61K31/165 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4409 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P17/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P35/00 , C07C217/60 , C07C233/17 , C07C233/22 , C07C233/60 , C07C233/73 , C07C237/08 , C07D207/12 , C07D207/27 , C07D209/42 , C07D213/81 , C07D233/60 , C07D241/44 , C07D295/14 , C07D295/15 , C07D333/38 , C07C233/18 , C07C237/06 , A61K31/44 , C07D265/30 , C07D295/145 , C07D233/64 , C07D233/90 , C07D211/76
Abstract: Compounds of the formula: in which: A represents R represents linear or branched lower alkyl, R1 represents hydrogen or linear or branched lower alkyl, and R2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, and medicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.
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