Patent NZ-508200-A (NZ)
Title: 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens
Inventor: PICKAR JAMES HARRISON
IPC: A61K31/565
Filed: 1999-05-11
Abstract: A  pharmaceutical composition comprising one  or  more estrogens  and a compound having the structure of formula  I or II. R1  is  selected  from H, OH or the C1-C12 esters  (straight chain or branched) or C1-Cl2 (straight chain or branched  or cyclic)   alkyl  ethers  thereof,  or  halogens;  or   Cl-C4 halogenated  ethers  including  trifluoromethyl  ether   and trichloromethyl ether. R2, R3, R4, R5, and R6 are independently selected from H, OH or  the Cl-Cl2 esters (straight chain or branched) or Cl-Cl2 alkyl   ethers  (straight  chain  or  branched  or   cyclic) thereof,  halogens,  or C1-C4 halogenated  ethers  including trifluoromethyl ether and trichloromethyl ether, cyano,  Cl- C6  alkyl  (straight chain or branched), or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH. X   is   selected   from  H,  C1-C6  alkyl,  cyano,   nitro, trifluoromethyl, halogen; n is 2 or 3; Y is selected from: a) the moiety I: where  R7  and R8 are independently selected from  H,  C1-C6 alkyl,  or phenyl optionally substituted by CN, C1-C6  alkyl (straight  chain or branched), C1-C6 alkoxy (straight  chain or  branched), halogen,-OH,-CF3 or-OCF3; or R7  and  R8  are concatenated together as- (CH2)p-, wherein p is  an  integer of  from  2  to 6, preferably 4 to 6, the ring so formed  is optionally  substituted with 1-3 substituents selected  from C1-C4  alkyl,  trihalomethyl, halogen, phenyl,  nitro,  -CN. Hydroxyl. C1-C4 alkoxy, trihalomethoxy, C1-C4 alkylthio, C1- C4   alkylsulfinyl,   C1-C4  alkylsulfonyl,   hydroxy   (C1- C4)alkyl,  -CO2H, -CONH(C1-C4)alkyl, -NH2, C1-C4 alkylamino, di-(C1-C4)alkylamino,  -NHSO2(C1-C4)alkyl,   and   -NHCO(C1- C4)alkyl. b)  a five-, six-or seven-membered saturated, unsaturated or partially  unsaturated  heterocycle  containing  up  to  two heteroatoms  selected  from-O-, -NH-,-N(C1-C4  alkyl)-,  -N= and   -S(O)m-,  wherein  m  is  an  integer  of  from   0-2, optionally  substituted with 1-3 substituents  independently selected  from  hydroxyl, halo, C1-C4 alkyl,  trihalomethyl, C1-C4alkoxy, trihalomethoxy, C1-C4acyloxy, C1-C4  alkylthio, C1-C4  alkylsulfinyl, C1-C4 alkylsulfonyl,  hydroxy  (C1-C4) alkyl, -C02H, - CN,-CONHR1, -NH2, C1-C4 alkylamino, di- (C1- C4)   alkylamino,-NHS02R1,  -N02,  and   phenyl   optionally substituted  with  1-3  (C1-C4) alkyl,  wherein  R1,  is  as defined above or C1-C6 alkyl; c)  a bicyclic heterocycle containing from 6-12 carbon atoms either bridged or fused and containing up to two heteroatoms selected   from  -O-,-NH-,  N(C1-C4  alkyl)-,  and  -S(O)m-, wherein  m is an integer of from 0-2, optionally substituted with 1-3 substituents independently selected hydroxyl, halo, C1-C4 alkyl, trihalomethyl, C1-C4 alkoxy, trihalomethoxy, C1- C4    alkylthio,C1-C4    acyloxy,    alkylsulfinyl,    C1-C4 alkylsulfonyl,   hydroxy  (C1-C4)  alkyl,-C02H,-CN-,-CONHR1, NH2,  C1-C4  alkylamino,  di  (C1-C4)  alkylamino,-NHS02R,,- NHCOR,,-N02, and phenyl optionally substituted with 1-3 (C1- C4)  alkyl;  or a pharmaceutically acceptable salt  thereof, and a pharmaceutically acceptable carrier or excipient.