公开(公告)号：NO20020262A

公开(公告)日：2002-07-19

申请号：NO20020262

申请日：2002-01-17

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  DIGUARHER THIERRY LE ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS

IPC: C07C317/00 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06

CPC classification number: C07D233/64 ,  A61K31/4164 ,  C07D213/38 ,  C07D401/06

公开(公告)号：FR2819510A1

公开(公告)日：2002-07-19

申请号：FR0100642

申请日：2001-01-18

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS ,  FAUCHERE JEAN LUC ,  ORTUNO JEAN CLAUDE

IPC: A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/55 ,  C07D401/04

Abstract: N-Substituted cyclo (c)-fused bicyclic azepane or azepanone derivatives (I) are new. Bicyclic azepane derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. W = CO or CH2; X = direct bond, alkylene, CO, S(O)n, S(O)n-A1, CO-A1, A1-S(O)n-A1 or A1-CO-A1 (bonded to the ring at the left-hand terminal); A1 = alkylene; n = 0-2; Y = aryl, heteroaryl, cycloalkyl or heterocycloalkyl (all optionally substituted (os) by R6); R1, R2 = H or as for Y; T = CHR3, NR3 or NR3CO (bonded to the ring at the left-hand terminal); R3 = H; or alkyl, aryl, heteroaryl, aralkyl or heteroaralkyl (all os by one or more R5); V = H; or aryl or heteroaryl (both os by one or more R5); A2 = -(CR4R'4)p; p = 0-4 (but not 0 if T = NR3); R4, R'4 = H, alkyl (os by R7), alkenyl, alkynyl or R7; R7 = OR3, NR3R'3, S(O)nR3, CONR3R'3, NR3COR'3, NR3SO2R'3, SO2NR3R'3 or NR3COOR'3; R'3 = as R3; R5 = os aralkyl, os heteroaryl, os heteroaralkyl, os cycloalkylalkyl or os heterocycloalkylalkyl; R6 = halo, =O, OH, CN, NO2, COOH, alkoxycarbonyl, U-R60 or A60-U-R60; A60 = alkylene; U = direct bond, O, NH, S(O)n, NHCO, CONH, SO2NH or NHSO2; R60 = alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl; and B' = an optionally partially hydrogenated aryl or heteroaryl ring (os by one or more of CN, alkyl, alkoxy, OH or halo); alkyl or alkylene moieties have 1-6C; cycloalkyl moieties have 3-8C; heterocycloalkyl moieties are 5-7 membered and contain 1-3 of N, O and S as heteroatom(s); aryl moieties are phenyl or naphthyl; heteroaryl moieties are mono- or bicyclic 5-11 membered systems containing at least one aromatic ring and 1-5 of N, O and S as heteroatom(s); the substituents in os aryl, heteroaryl, aralkyl or heteroaralkyl are one or more of CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part); and the substituents in os cycloalkyl, heterocycloalkyl, cycloalkylalkyl or heterocycloalkylalkyl are one or more of =O, CN, alkylcarbonyl, CONH2 (os by 1 or 2 alkyl) or halo (in the ring part). An Independent claim is included for the preparation of (I).

公开(公告)号：ZA200110517B

公开(公告)日：2002-07-11

申请号：ZA200110517

申请日：2001-12-21

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  BENOIST ALAIN ,  PASTOUREAU PHILIPPE ,  SABATINI MASSIMO ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON

IPC: C07D491/048 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/541 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D405/14 ,  C07D417/14 ,  C07D491/04 ,  C07D ,  A61K

Abstract: 5-Sulfonyl-2-(4-pyridinyl)-benzofuran, benzothiophene or indole derivatives (I), containing a hydroxamic acid function, are new. Benzofuran, benzothiophene or indole derivatives of formula (I) and their isomers, N-oxides and acid or base addition salts are new. R1 = H, halo, 1-6C alkyl or 1-6C alkoxy; X = O, S or NR; R = H or 1-6C alkyl; A = N-hydroxy-carboxamido-substituted tetrahydrofuropyridine, thiomorpholine or tetrahydropyranylmethyl group of formula (i)-(iii); Ra = H, halo, 1-6C alkyl or 1-6C alkoxy; Rb, Rc = H or 1-6C alkyl; and n = 0-2. An Independent claim is also included for the preparation of (I).

公开(公告)号：AT212634T

公开(公告)日：2002-02-15

申请号：AT98402806

申请日：1998-11-13

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  REMOND GEORGES ,  PALADINO JOSEPH ,  ATASSI GHANEM ,  PIERRE ALAIN ,  TUCKER GORDON ,  BONNET JACQUELINE ,  SABATINI MASSIMO

IPC: A61K31/00 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/437 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  A61K31/44 ,  C07D221/00 ,  C07D209/00

Abstract: Tetrahydro carboline derivatives of formula (I) and their preparation from D-tryptophan derivatives. Tetrahydrocarboline derivatives of formula (I) their isomers and their salts m = 1, 2,3, or 4; n and p = 0, 1, 2, 3, or 4; X = O, S, or a simple bond; R1 = H, halogen, 1-6C alkyl or trihaloalkyl, OH, 1-6C alkoxy or trihaloalkoxy; R2, R3, and R4 = H or 1-6C alkyl; R5 = H, halogen,1-6C alkoxy, aryloxy or heteroaryloxy; R6, R7, and R8 = H, 1-6C alkyl, or R6 with N and R7 or R8 form a heterocycle; R9 = -SO3H, -COOR10, -CO-NR11R12, or -NR13R14; R10 = H or 1-6C alkyl; R11 and R12 = H or 1-6C alkyl or form an optionally substituted heterocycle with the N atom; R13 and R14 = H or 1-6C alkyl or form an optionally substituted heterocycle with the N atom

公开(公告)号：PL345101A1

公开(公告)日：2001-12-03

申请号：PL34510199

申请日：1999-06-29

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  CHOLLET ANNE-MARIE ,  LE DIGUARHER THIERRY ,  ATASSI GHANEM ,  BONNET JACQUELINE ,  PIERRE ALAIN ,  SABATINI MASSIMO ,  TUCKER GORDON ,  GUILBAUD NICOLAS

IPC: C07D253/04 ,  A61K31/18 ,  A61K31/197 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/517 ,  A61K31/53 ,  A61K31/535 ,  A61K31/536 ,  A61K31/537 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C233/82 ,  C07C233/83 ,  C07C259/10 ,  C07C311/29 ,  C07D209/48 ,  C07D209/66 ,  C07D231/22 ,  C07D233/72 ,  C07D233/74 ,  C07D237/32 ,  C07D239/96 ,  C07D253/08 ,  C07D265/06 ,  C07D265/16 ,  C07D275/04 ,  C07D275/06 ,  C07D277/20 ,  C07D277/34 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04 ,  A61K31/40 ,  C07D221/14 ,  C07D263/44 ,  C07D265/26

公开(公告)号：HU229343B1

公开(公告)日：2013-11-28

申请号：HU0300181

申请日：2001-03-06

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  PERRON-SIERRA FRANCOISE ,  ATASSI GHANEM ,  TUCKER GORDON ,  SAINT-DIZIER DOMONIQUE

IPC: A61K31/4164 ,  C07D213/74 ,  A61K31/4168 ,  C07D233/24 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/426 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/505 ,  A61K31/55 ,  A61P9/00 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P33/14 ,  A61P35/00 ,  A61P43/00 ,  C07D213/36 ,  C07D223/04 ,  C07D223/12 ,  C07D233/48 ,  C07D233/54 ,  C07D235/10 ,  C07D235/14 ,  C07D235/30 ,  C07D239/14 ,  C07D277/18 ,  C07D277/20 ,  C07D277/42 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

Abstract: Compounds of formula (1):wherein:G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C,T1 represents -CH2-CH2-, -CH=CH- or =CH-CH2-, and T2 is a bond, or T1 represents -CH2- or =CH- and T2 is -CH2-, =CH-,R5 represents -(CH2)m-COOR6,R6 and R6' represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl,A represents -CO-, -CH2-, =CH- or -CH= and W represents -CH-, =C- or -C=, or A represents -CO- or -CH2- and W represents N,X represents -CO-X1-, -CO-NR6-X1-, -NR6-CO-X1-, -O-X1-, -SO2-NR6-X1- or -S(O)n-X1-,Y represents -Y1-, -Y2-Y1- or -Y1-Y2-Y1-, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene,Z represents -Z1-, -Z10-NR6-, and -Z10-NR6-CO-, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroaryl or fused heteroarylheteroaryl, each of which is optionally substituted, or a group,Z2-NR6 or Z2-NR6-CO, Z2 being a group Z1, alkyl or heteroalkyl, andZ10 represents Z1 or an alkyl,its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base,and medicinal products containing the same which are useful as vitronectin receptor antagonists.

公开(公告)号：CA2367306C

公开(公告)日：2006-07-11

申请号：CA2367306

申请日：2002-01-17

Applicant: SERVIER LAB

Inventor： GUILBAUD NICOLAS ,  PIERRE ALAIN ,  LE DIGUARHER THIERRY ,  HICKMAN JOHN ,  DOREY GILBERT ,  CASARA PATRICK ,  TUCKER GORDON

IPC: C07C13/24 ,  C07C317/00 ,  A61K31/015 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/56 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06

Abstract: L'invention concerne de nouveaux composés répondant à la formule formule (I ): dans laquelle X représente une liaison ou un groupement alkylène, CO, S(O)n, *- S(O)n-A1-, *-CO-A1-, -A1-S(O)n-A'1- et -A1-CO-A'1- dans lesquels A1 et A'1, identiques ou différents, représentent un groupement alkylène et n vaut 0, 1 ou 2, le symbole "*" représentant le point de rattachement du groupement au cycloheptène; Y représente un groupement aryle, hétéroaryle, cycloalkyle ou hétérocycloalkyle; R1, R2, R3 et R4 représentent indépendamment l'un de l'autre un atome d'hydrogène ou un groupement aryle, hétéroaryle, cycloalkyle ou hétérocycloalkyle, ou bien R1, R2, R3 et R4, pris deux à deux , forment ensemble une liaison, ou bien R1 et R2, ou R2 et R3 ou R3 et R4, pris deux à deux avec les atomes de carbone auxquels ils sont liés, forment un cycle benzénique fusion né ou un hétérocycle fusionné aromatique ou partiellement hydrogéné; T représente un groupement -CH(R5)-, -N(R5)- ou *-N(R5)CO- dans lesquels R5 représente un atome d'hydrogène ou un groupement alkyle, aryle, hétéroaryle, arylalkyle ou hétéroarylalkyle, le symbole "*" représentant le point de rattachement du groupement au cycloheptène; V représente un atome d'hydrogène ou un groupement aryle ou hétéroaryle; A2 représente un groupement [C(R6)(R'6)]p où p vaut 0, 1, 2, 3 ou 4 lorsque T représente un groupement - CH(R5)- ou *-N(R5)CO- où p vaut 1, 2, 3 ou 4 lorsque T représente un groupement -N(R5)- , et R6 et R'6, identiques ou différents, représentent un atome d'hydrogène ou un groupement alkyle, alkényle, alkynyle, aryle, hétéroaryle, hétérocycloalkyle, arylalkyle éventuellement substitué, hétéroarylalkyle, hétérocycloalkylalkyle, R9 ou alkyle substitué par un groupement R9 où R9 représente un groupement -OR5,-N(R5)(R'5), -S(O)m R5, -CON(R5)(R'5), -N(R5)COR'5, -N(R5)SO2R'5, -SO2N(R5)(R'5), -N(R5)COO(R'5), m étant égal à 0, 1 ou 2, et R'5 prenant toutes les valeurs de R5. L'invention vise également les énantiomères et diastéréoisomères des composés de formule (I), ainsi que leu rs sels -52- d'addition à un acide ou à une base pharmaceutiquement acceptable. Les composés selon l'invention sont utiles à titre de médicaments pour le traitement des maladi es cancéreuses ainsi que pour le traitement de la resténose après angioplastie ou chirurgie vasculaire, et de la neurofibromatose de type I.

公开(公告)号：NO321490B1

公开(公告)日：2006-05-15

申请号：NO20016177

申请日：2001-12-18

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  PIERRE ALAIN ,  PASTOUREAU PHILIPPE ,  TUCKER GORDON ,  SABATINI MASSIMO ,  BENOIST ALAIN ,  HICKMAN JOHN

IPC: C07D491/04 ,  C07D491/048 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/541 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D405/14 ,  C07D417/14

Abstract: 5-Sulfonyl-2-(4-pyridinyl)-benzofuran, benzothiophene or indole derivatives (I), containing a hydroxamic acid function, are new. Benzofuran, benzothiophene or indole derivatives of formula (I) and their isomers, N-oxides and acid or base addition salts are new. R1 = H, halo, 1-6C alkyl or 1-6C alkoxy; X = O, S or NR; R = H or 1-6C alkyl; A = N-hydroxy-carboxamido-substituted tetrahydrofuropyridine, thiomorpholine or tetrahydropyranylmethyl group of formula (i)-(iii); Ra = H, halo, 1-6C alkyl or 1-6C alkoxy; Rb, Rc = H or 1-6C alkyl; and n = 0-2. An Independent claim is also included for the preparation of (I).

公开(公告)号：DE60105001T2

公开(公告)日：2005-08-18

申请号：DE60105001

申请日：2001-03-06

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  PERRON-SIERRA FRANCOISE ,  ATASSI GHANEM ,  TUCKER GORDON ,  SAINT-DIZIER DOMINIQUE

IPC: C07D233/24 ,  A61K31/4164 ,  A61K31/4168 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/426 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/505 ,  A61K31/55 ,  A61P9/00 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P33/14 ,  A61P35/00 ,  A61P43/00 ,  C07D213/36 ,  C07D213/74 ,  C07D223/04 ,  C07D223/12 ,  C07D233/48 ,  C07D233/54 ,  C07D235/10 ,  C07D235/14 ,  C07D235/30 ,  C07D239/14 ,  C07D277/18 ,  C07D277/20 ,  C07D277/42 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

Abstract: Compounds of formula (1):wherein:G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C,T1 represents -CH2-CH2-, -CH=CH- or =CH-CH2-, and T2 is a bond, or T1 represents -CH2- or =CH- and T2 is -CH2-, =CH-,R5 represents -(CH2)m-COOR6,R6 and R6' represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl,A represents -CO-, -CH2-, =CH- or -CH= and W represents -CH-, =C- or -C=, or A represents -CO- or -CH2- and W represents N,X represents -CO-X1-, -CO-NR6-X1-, -NR6-CO-X1-, -O-X1-, -SO2-NR6-X1- or -S(O)n-X1-,Y represents -Y1-, -Y2-Y1- or -Y1-Y2-Y1-, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene,Z represents -Z1-, -Z10-NR6-, and -Z10-NR6-CO-, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroaryl or fused heteroarylheteroaryl, each of which is optionally substituted, or a group,Z2-NR6 or Z2-NR6-CO, Z2 being a group Z1, alkyl or heteroalkyl, andZ10 represents Z1 or an alkyl,its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base,and medicinal products containing the same which are useful as vitronectin receptor antagonists.

公开(公告)号：DK1217002T3

公开(公告)日：2005-01-24

申请号：DK01403333

申请日：2001-12-21

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  HICKMAN JOHN ,  PIERRE ALAIN ,  BENOIST ALAIN ,  PASTOUREAU PHILIPPE ,  SABATINI MASSIMO ,  TUCKER GORDON

IPC: C07D491/048 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/541 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D405/14 ,  C07D417/14 ,  C07D491/04

Abstract: 5-Sulfonyl-2-(4-pyridinyl)-benzofuran, benzothiophene or indole derivatives (I), containing a hydroxamic acid function, are new. Benzofuran, benzothiophene or indole derivatives of formula (I) and their isomers, N-oxides and acid or base addition salts are new. R1 = H, halo, 1-6C alkyl or 1-6C alkoxy; X = O, S or NR; R = H or 1-6C alkyl; A = N-hydroxy-carboxamido-substituted tetrahydrofuropyridine, thiomorpholine or tetrahydropyranylmethyl group of formula (i)-(iii); Ra = H, halo, 1-6C alkyl or 1-6C alkoxy; Rb, Rc = H or 1-6C alkyl; and n = 0-2. An Independent claim is also included for the preparation of (I).