SK602004A3 - Selective estrogen receptor modulators - Google Patents

Selective estrogen receptor modulators Download PDF

Info

Publication number: SK602004A3
Authority: SK; Slovakia
Prior art keywords: phenyl; acryloyl; diphenylbut; enyl; benzocyclohepten
Prior art date: 2001-08-11

Application number

SK60-2004A

Other languages

English (en)

Slovak (sk)

Inventor

Robert Kaltenbach

Simon Robinson

George Trainor

Original Assignee

Bristol Myers Squibb Pharma Co

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2001-08-11

Filing date

2002-08-09

Publication date

2004-11-03

2002-08-09 Application filed by Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co

2004-11-03 Publication of SK602004A3 publication Critical patent/SK602004A3/sk

Links

239000000333 selective estrogen receptor modulator Substances 0.000 title abstract 2
229940095743 selective estrogen receptor modulator Drugs 0.000 title abstract 2
150000001875 compounds Chemical class 0.000 claims abstract 19
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 3
OGYFWYWYSDLODF-UHFFFAOYSA-N 3-[4-[6-(3-methoxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound COC1=CC=CC(C=2CCCC3=CC=CC=C3C=2C=2C=CC(C=CC(O)=O)=CC=2)=C1 OGYFWYWYSDLODF-UHFFFAOYSA-N 0.000 claims abstract 2
208000024172 Cardiovascular disease Diseases 0.000 claims abstract 2
206010009944 Colon cancer Diseases 0.000 claims abstract 2
208000001132 Osteoporosis Diseases 0.000 claims abstract 2
210000000481 breast Anatomy 0.000 claims abstract 2
208000029742 colonic neoplasm Diseases 0.000 claims abstract 2
201000010099 disease Diseases 0.000 claims abstract 2
238000000034 method Methods 0.000 claims abstract 2
230000002611 ovarian Effects 0.000 claims abstract 2
239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
230000002062 proliferating effect Effects 0.000 claims abstract 2
125000000217 alkyl group Chemical group 0.000 claims 19
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 18
125000003647 acryloyl group Chemical group O=C([*])C([H])=C([H])[H] 0.000 claims 15
-1 1,2-diphenylbut-1-enyl Chemical group 0.000 claims 12
229910052736 halogen Inorganic materials 0.000 claims 7
150000002367 halogens Chemical class 0.000 claims 7
150000003839 salts Chemical class 0.000 claims 6
125000003118 aryl group Chemical group 0.000 claims 4
AVBPHICCYHJMGI-UHFFFAOYSA-N 3-[4-(6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1C2=CC=C(O)C=C2CCC1C1=CC=CC=C1 AVBPHICCYHJMGI-UHFFFAOYSA-N 0.000 claims 3
125000004122 cyclic group Chemical group 0.000 claims 3
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
125000001424 substituent group Chemical group 0.000 claims 3
CEPMBESUVXXFST-UHFFFAOYSA-N 3-chloropropane-1-sulfonic acid Chemical compound OS(=O)(=O)CCCCl CEPMBESUVXXFST-UHFFFAOYSA-N 0.000 claims 2
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
239000003814 drug Substances 0.000 claims 2
102000015694 estrogen receptors Human genes 0.000 claims 2
108010038795 estrogen receptors Proteins 0.000 claims 2
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
238000004519 manufacturing process Methods 0.000 claims 2
HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 2
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
229910052760 oxygen Inorganic materials 0.000 claims 2
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
KJUGUADJHNHALS-UHFFFAOYSA-N 1H-tetrazole Substances C=1N=NNN=1 KJUGUADJHNHALS-UHFFFAOYSA-N 0.000 claims 1
SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 1
NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 1
125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims 1
QYQLHEFQTFTQBQ-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(2,2,2-trifluoroethylsulfonyl)prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)CC(F)(F)F)=CC=1)C1=CC=CC=C1 QYQLHEFQTFTQBQ-UHFFFAOYSA-N 0.000 claims 1
NKECFBWSUIUYDO-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(3-methoxyphenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=C(OC)C=CC=2)=CC=1)C1=CC=CC=C1 NKECFBWSUIUYDO-UHFFFAOYSA-N 0.000 claims 1
HVHNEXHHAZREHQ-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(3-methylphenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=C(C)C=CC=2)=CC=1)C1=CC=CC=C1 HVHNEXHHAZREHQ-UHFFFAOYSA-N 0.000 claims 1
VYNZFCGMLQOZDG-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(3-nitrophenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=C(C=CC=2)[N+]([O-])=O)=CC=1)C1=CC=CC=C1 VYNZFCGMLQOZDG-UHFFFAOYSA-N 0.000 claims 1
YVLSIRHQEWZRGE-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(3-piperidin-1-ylpropylsulfonyl)prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)CCCN2CCCCC2)=CC=1)C1=CC=CC=C1 YVLSIRHQEWZRGE-UHFFFAOYSA-N 0.000 claims 1
CTEFJDOTNOIAHQ-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(4-hydroxyphenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(O)=CC=2)=CC=1)C1=CC=CC=C1 CTEFJDOTNOIAHQ-UHFFFAOYSA-N 0.000 claims 1
HNRVOGXJOPLJGL-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(4-methoxyphenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(OC)=CC=2)=CC=1)C1=CC=CC=C1 HNRVOGXJOPLJGL-UHFFFAOYSA-N 0.000 claims 1
IMVZCSRJYFUIQZ-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(4-methylphenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(C)=CC=2)=CC=1)C1=CC=CC=C1 IMVZCSRJYFUIQZ-UHFFFAOYSA-N 0.000 claims 1
GTABCCZDUGDYFJ-UHFFFAOYSA-N 3-[4-(1,2-diphenylbut-1-enyl)phenyl]-n-(4-nitrophenyl)sulfonylprop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(=CC=2)[N+]([O-])=O)=CC=1)C1=CC=CC=C1 GTABCCZDUGDYFJ-UHFFFAOYSA-N 0.000 claims 1
VOMLGXZBDWYBIS-UHFFFAOYSA-N 3-[4-(2-hydroxy-6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC=CC=2)CCCC2=CC(O)=CC=C12 VOMLGXZBDWYBIS-UHFFFAOYSA-N 0.000 claims 1
DWZGVAIMLSLJDP-UHFFFAOYSA-N 3-[4-(2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1C2=CC=CC=C2CCC1C1=CC=CC=C1 DWZGVAIMLSLJDP-UHFFFAOYSA-N 0.000 claims 1
DJGWIZOTHKHHNF-UHFFFAOYSA-N 3-[4-(2-phenyl-3,4-dihydronaphthalen-1-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC=CC=2)CCC2=CC=CC=C12 DJGWIZOTHKHHNF-UHFFFAOYSA-N 0.000 claims 1
USJSCWFJJVGBLR-UHFFFAOYSA-N 3-[4-(3-phenyl-2h-chromen-4-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC=CC=2)COC2=CC=CC=C12 USJSCWFJJVGBLR-UHFFFAOYSA-N 0.000 claims 1
QOFIWTNKODZDDI-UHFFFAOYSA-N 3-[4-(6-phenyl-6,7,8,9-tetrahydro-5h-benzo[7]annulen-5-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1C2=CC=CC=C2CCCC1C1=CC=CC=C1 QOFIWTNKODZDDI-UHFFFAOYSA-N 0.000 claims 1
QIJCDIPDKQCNKF-UHFFFAOYSA-N 3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]-n-(3-piperidin-1-ylpropylsulfonyl)prop-2-enamide Chemical compound C=1C=C(C=2C3=CC=CC=C3CCCC=2C=2C=CC=CC=2)C=CC=1C=CC(=O)NS(=O)(=O)CCCN1CCCCC1 QIJCDIPDKQCNKF-UHFFFAOYSA-N 0.000 claims 1
XOWVSXCPJHZAFV-UHFFFAOYSA-N 3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]-n-(trifluoromethylsulfonyl)prop-2-enamide Chemical compound C1=CC(C=CC(=O)NS(=O)(=O)C(F)(F)F)=CC=C1C1=C(C=2C=CC=CC=2)CCCC2=CC=CC=C12 XOWVSXCPJHZAFV-UHFFFAOYSA-N 0.000 claims 1
YNLAGWQYJSLLKX-UHFFFAOYSA-N 3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC=CC=2)CCCC2=CC=CC=C12 YNLAGWQYJSLLKX-UHFFFAOYSA-N 0.000 claims 1
XZUBDZHCNRIWOS-UHFFFAOYSA-N 3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]propanoic acid Chemical compound C1=CC(CCC(=O)O)=CC=C1C1=C(C=2C=CC=CC=2)CCCC2=CC=CC=C12 XZUBDZHCNRIWOS-UHFFFAOYSA-N 0.000 claims 1
QGBWGAQQCWRTGZ-UHFFFAOYSA-N 3-[4-[2-hydroxy-6-(3-hydroxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=C(O)C=CC=2)CCCC2=CC(O)=CC=C12 QGBWGAQQCWRTGZ-UHFFFAOYSA-N 0.000 claims 1
CUEDGSYJWAZEJR-UHFFFAOYSA-N 3-[4-[2-hydroxy-6-(4-hydroxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC(O)=CC=2)CCCC2=CC(O)=CC=C12 CUEDGSYJWAZEJR-UHFFFAOYSA-N 0.000 claims 1
TZSSUVDZZHPSGR-UHFFFAOYSA-N 3-[4-[6-(3-hydroxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=C(O)C=CC=2)CCCC2=CC=CC=C12 TZSSUVDZZHPSGR-UHFFFAOYSA-N 0.000 claims 1
LIIHHGGXUUOGRQ-UHFFFAOYSA-N 3-[4-[6-(4-hydroxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound C1=CC(C=CC(=O)O)=CC=C1C1=C(C=2C=CC(O)=CC=2)CCCC2=CC=CC=C12 LIIHHGGXUUOGRQ-UHFFFAOYSA-N 0.000 claims 1
CHBZIFFFVRUBIV-UHFFFAOYSA-N 3-[4-[6-(4-methoxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]prop-2-enoic acid Chemical compound C1=CC(OC)=CC=C1C(CCCC1=CC=CC=C11)=C1C1=CC=C(C=CC(O)=O)C=C1 CHBZIFFFVRUBIV-UHFFFAOYSA-N 0.000 claims 1
KFAVIVQWHYMDFQ-UHFFFAOYSA-N 4-[3-[4-(1,2-diphenylbut-1-enyl)phenyl]prop-2-enoylsulfamoyl]benzoic acid Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(=CC=2)C(O)=O)=CC=1)C1=CC=CC=C1 KFAVIVQWHYMDFQ-UHFFFAOYSA-N 0.000 claims 1
125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
KEULONSVUWYVQN-UHFFFAOYSA-N 5-[2-[4-(1,2-diphenylbut-1-enyl)phenyl]ethenyl]-1-methyltetrazole Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC=2N(N=NN=2)C)=CC=1)C1=CC=CC=C1 KEULONSVUWYVQN-UHFFFAOYSA-N 0.000 claims 1
DKYNYUWRQMEDEM-UHFFFAOYSA-N 5-[2-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]ethenyl]-2h-tetrazole Chemical compound C=1C=CC=CC=1C=1CCCC2=CC=CC=C2C=1C(C=C1)=CC=C1C=CC1=NN=NN1 DKYNYUWRQMEDEM-UHFFFAOYSA-N 0.000 claims 1
FODCKXYZNKVJIS-UHFFFAOYSA-N 5-[2-[4-[6-(3-methoxyphenyl)-8,9-dihydro-7h-benzo[7]annulen-5-yl]phenyl]ethenyl]-2h-tetrazole Chemical compound COC1=CC=CC(C=2CCCC3=CC=CC=C3C=2C=2C=CC(C=CC=3NN=NN=3)=CC=2)=C1 FODCKXYZNKVJIS-UHFFFAOYSA-N 0.000 claims 1
208000024827 Alzheimer disease Diseases 0.000 claims 1
206010006187 Breast cancer Diseases 0.000 claims 1
208000026310 Breast neoplasm Diseases 0.000 claims 1
201000009273 Endometriosis Diseases 0.000 claims 1
BZORFPDSXLZWJF-UHFFFAOYSA-N N,N-dimethyl-1,4-phenylenediamine Chemical compound CN(C)C1=CC=C(N)C=C1 BZORFPDSXLZWJF-UHFFFAOYSA-N 0.000 claims 1
206010033128 Ovarian cancer Diseases 0.000 claims 1
206010061535 Ovarian neoplasm Diseases 0.000 claims 1
206010060862 Prostate cancer Diseases 0.000 claims 1
208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
206010046543 Urinary incontinence Diseases 0.000 claims 1
208000002495 Uterine Neoplasms Diseases 0.000 claims 1
206010046798 Uterine leiomyoma Diseases 0.000 claims 1
125000003342 alkenyl group Chemical group 0.000 claims 1
125000005466 alkylenyl group Chemical group 0.000 claims 1
125000000304 alkynyl group Chemical group 0.000 claims 1
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
239000003937 drug carrier Substances 0.000 claims 1
CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
201000010260 leiomyoma Diseases 0.000 claims 1
208000002780 macular degeneration Diseases 0.000 claims 1
125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
LZHOIXIYYSOEBY-UHFFFAOYSA-N n-(2-chlorophenyl)sulfonyl-3-[4-(1,2-diphenylbut-1-enyl)phenyl]prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C(=CC=CC=2)Cl)=CC=1)C1=CC=CC=C1 LZHOIXIYYSOEBY-UHFFFAOYSA-N 0.000 claims 1
CKGBJUCVHGGUHM-UHFFFAOYSA-N n-(4-chlorophenyl)sulfonyl-3-[4-(1,2-diphenylbut-1-enyl)phenyl]prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(Cl)=CC=2)=CC=1)C1=CC=CC=C1 CKGBJUCVHGGUHM-UHFFFAOYSA-N 0.000 claims 1
OTWLVXIFIXJCQJ-UHFFFAOYSA-N n-(4-cyanophenyl)sulfonyl-3-[4-(1,2-diphenylbut-1-enyl)phenyl]prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC(=CC=2)C#N)=CC=1)C1=CC=CC=C1 OTWLVXIFIXJCQJ-UHFFFAOYSA-N 0.000 claims 1
ZQEDOISJASRUIF-UHFFFAOYSA-N n-(benzenesulfonyl)-3-[4-(1,2-diphenylbut-1-enyl)phenyl]prop-2-enamide Chemical compound C=1C=CC=CC=1C(CC)=C(C=1C=CC(C=CC(=O)NS(=O)(=O)C=2C=CC=CC=2)=CC=1)C1=CC=CC=C1 ZQEDOISJASRUIF-UHFFFAOYSA-N 0.000 claims 1
PJKUTLRSVQYWFS-UHFFFAOYSA-N n-(benzenesulfonyl)-3-[4-(2-phenyl-3,4-dihydronaphthalen-1-yl)phenyl]prop-2-enamide Chemical compound C=1C=C(C=2C3=CC=CC=C3CCC=2C=2C=CC=CC=2)C=CC=1C=CC(=O)NS(=O)(=O)C1=CC=CC=C1 PJKUTLRSVQYWFS-UHFFFAOYSA-N 0.000 claims 1
BQLJYHFUIIPZGG-UHFFFAOYSA-N n-(benzenesulfonyl)-3-[4-(3-phenyl-2h-chromen-4-yl)phenyl]prop-2-enamide Chemical compound C=1C=C(C=2C3=CC=CC=C3OCC=2C=2C=CC=CC=2)C=CC=1C=CC(=O)NS(=O)(=O)C1=CC=CC=C1 BQLJYHFUIIPZGG-UHFFFAOYSA-N 0.000 claims 1
NUVFTMVWAUGNPW-UHFFFAOYSA-N n-(benzenesulfonyl)-3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]prop-2-enamide Chemical compound C=1C=C(C=2C3=CC=CC=C3CCCC=2C=2C=CC=CC=2)C=CC=1C=CC(=O)NS(=O)(=O)C1=CC=CC=C1 NUVFTMVWAUGNPW-UHFFFAOYSA-N 0.000 claims 1
YDLLWRPKJFTDLJ-UHFFFAOYSA-N n-methylsulfonyl-3-[4-(3-phenyl-2h-chromen-4-yl)phenyl]prop-2-enamide Chemical compound C1=CC(C=CC(=O)NS(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)COC2=CC=CC=C12 YDLLWRPKJFTDLJ-UHFFFAOYSA-N 0.000 claims 1
JMOWFWKQINJIOZ-UHFFFAOYSA-N n-methylsulfonyl-3-[4-(6-phenyl-8,9-dihydro-7h-benzo[7]annulen-5-yl)phenyl]prop-2-enamide Chemical compound C1=CC(C=CC(=O)NS(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)CCCC2=CC=CC=C12 JMOWFWKQINJIOZ-UHFFFAOYSA-N 0.000 claims 1
UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
239000001301 oxygen Substances 0.000 claims 1
210000002307 prostate Anatomy 0.000 claims 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
230000001225 therapeutic effect Effects 0.000 claims 1
KAKQVSNHTBLJCH-UHFFFAOYSA-N trifluoromethanesulfonimidic acid Chemical compound NS(=O)(=O)C(F)(F)F KAKQVSNHTBLJCH-UHFFFAOYSA-N 0.000 claims 1
208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
206010046766 uterine cancer Diseases 0.000 claims 1
208000010579 uterine corpus leiomyoma Diseases 0.000 claims 1
201000007954 uterine fibroid Diseases 0.000 claims 1
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
229920002554 vinyl polymer Polymers 0.000 claims 1
MKYQPGPNVYRMHI-UHFFFAOYSA-N Triphenylethylene Chemical group C=1C=CC=CC=1C=C(C=1C=CC=CC=1)C1=CC=CC=C1 MKYQPGPNVYRMHI-UHFFFAOYSA-N 0.000 abstract 1
208000035475 disorder Diseases 0.000 abstract 1
229940011871 estrogen Drugs 0.000 abstract 1
239000000262 estrogen Substances 0.000 abstract 1
230000002265 prevention Effects 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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SK60-2004A 2001-08-11 2002-08-09 Selective estrogen receptor modulators SK602004A3 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US31146601P	2001-08-11	2001-08-11
PCT/US2002/025394 WO2003016270A2 (en)	2001-08-11	2002-08-09	Selective estrogen receptor modulators

Publications (1)

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SK602004A3 true SK602004A3 (en)	2004-11-03

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SK60-2004A SK602004A3 (en)	2001-08-11	2002-08-09	Selective estrogen receptor modulators

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US (3)	US6927224B2 (et)
EP (1)	EP1417169A2 (et)
JP (1)	JP2005528320A (et)
AU (1)	AU2002323098A1 (et)
BG (1)	BG108561A (et)
CZ (1)	CZ2004220A3 (et)
EE (1)	EE200400061A (et)
HU (1)	HUP0500573A2 (et)
PL (1)	PL374215A1 (et)
SK (1)	SK602004A3 (et)
WO (1)	WO2003016270A2 (et)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPS6180731A (ja) *	1984-09-28	1986-04-24	Toshiba Corp	管球の製造方法
PE20020354A1 (es)	2000-09-01	2002-06-12	Novartis Ag	Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
EP1667955A2 (en)	2003-07-28	2006-06-14	SmithKline Beecham Corporation	Cycloalkylidene compounds as modulators of the estrogen receptor
EP1692127B1 (en) *	2003-10-08	2008-07-02	Smithkline Beecham Corporation	Triphenylethylene compounds as selective estrogen receptor modulators
CA2581316C (en)	2004-09-21	2013-09-10	Novogen Research Pty Ltd	Substituted chroman derivatives, medicaments and use in therapy
US8080675B2 (en)	2004-09-21	2011-12-20	Marshall Edwards, Inc.	Chroman derivatives, medicaments and use in therapy
US7208526B2 (en) *	2005-05-20	2007-04-24	Hoffmann-La Roche Inc.	Styrylsulfonamides
EP2048126A1 (de) *	2007-10-11	2009-04-15	Bayer Schering Pharma AG	Benzocycloheptanderivate als selektiv wirksame Estrogene
BRPI0818637A2 (pt)	2007-10-16	2015-04-07	Repros Therapeutics Inc	Métodos de tratamento de sintoma da síndrome metabólica, de glicose em jejum prejudicada, da síndrome metabólica e de redução de níveis de glicose em, jejum em sujeito com hipogonadismo hipogonadotrófico secundário ou idiopático
US20090215733A1 (en) *	2008-02-26	2009-08-27	Michael Charles Scally	Therapy for the prophylaxis or treatment of adverse body composition changes and/or decreased muscle strength after androgen or gnrh analogue intake
WO2010107474A1 (en) *	2009-03-16	2010-09-23	The Research Foundation Of State University Of New York	Antiestrogens for breast cancer therapy
RS56042B1 (sr)	2010-06-10	2017-09-29	Seragon Pharmaceuticals Inc	Modulatori estrogenih receptora i njihove upotrebe
US8853423B2 (en)	2010-06-17	2014-10-07	Seragon Pharmaceuticals, Inc.	Indane estrogen receptor modulators and uses thereof
DE102010030538A1 (de)	2010-06-25	2011-12-29	Bayer Schering Pharma Aktiengesellschaft	6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
GB2483736B (en) *	2010-09-16	2012-08-29	Aragon Pharmaceuticals Inc	Estrogen receptor modulators and uses thereof
EP2635273B1 (en)	2010-11-01	2020-01-08	MEI Pharma, Inc.	Isoflavonoid compositions and methods for the treatment of cancer
DE102011087987A1 (de)	2011-12-08	2013-06-13	Bayer Intellectual Property Gmbh	6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
WO2013090829A1 (en)	2011-12-14	2013-06-20	Aragon Pharmaceuticals, Inc.	Estrogen receptor modulators and uses thereof
JP2015508825A (ja)	2012-02-29	2015-03-23	レプロスセラピューティクスインコーポレイティド	アンドロゲン欠乏症を治療するための併用療法
US9499538B2 (en)	2012-03-20	2016-11-22	Seragon Pharmaceuticals, Inc.	Estrogen receptor modulators and uses thereof
WO2014008159A1 (en) *	2012-07-03	2014-01-09	The University Of North Carolina At Chapel Hill	Selective estrogen receptor degraders for treatment of tamoxifen resistant tumors
MX2015011132A (es) *	2013-03-14	2015-11-30	Seragon Pharmaceuticals Inc	Moduladores policiclicos del receptor de estrogenos y sus usos.
CN104211695B (zh) *	2013-06-04	2017-04-12	中国医学科学院医药生物技术研究所	一组胺甲酰基苯磺酰类化合物的用途
CN116139125A (zh)	2015-02-02	2023-05-23	梅制药公司	联合治疗
CN105061316B (zh) *	2015-07-17	2017-12-22	苏州大学	稠环类化合物、制备方法和用途
KR20240142622A (ko)	2015-10-01	2024-09-30	올레마 파마슈티컬스 인코포레이티드	테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물
EP3373967B9 (en)	2015-11-10	2023-10-04	Paracrine Therapeutics AB	Treatment of er-negative breast cancer with an pdgf-cc inhibitor and an anti estrogen
EA034994B1 (ru) *	2016-02-15	2020-04-15	Санофи	6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов
ES3039455T3 (en)	2016-11-17	2025-10-21	Sanofi Sa	Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
EP3434272A1 (en)	2017-07-25	2019-01-30	Sanofi	Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
WO2019023621A1 (en) *	2017-07-28	2019-01-31	Yale University	ANTICANCER DRUGS AND METHODS OF MAKING AND USING THEM
US20210094899A1 (en) *	2017-07-28	2021-04-01	Recurium Ip Holdings, Llc	Acrylic acid analogs
CN111032627B (zh) *	2017-09-25	2023-10-20	罗欣健康科技发展(北京)有限公司	一种雌激素受体抑制剂的晶型及其制备方法
SG11202006942WA (en) *	2018-01-22	2020-08-28	Radius Pharmaceuticals Inc	Estrogen receptor-modulating compounds
EP3759086A1 (en) *	2018-02-27	2021-01-06	Artax Biopharma Inc.	Chromene derivatives as inhibitors of tcr-nck interaction
BR112021003440A2 (pt)	2018-09-07	2021-05-18	Sanofi	sais de 6-(2,4-diclorofenil)-5-[4-[(3s)-1-(3-fluoropropil) pirrolidin-3-il]oxifenil]-8,9-di-hidro-7h-benzo[7]anuleno-2-carboxilato de metila e seu processo de preparação
KR20220034129A (ko)	2019-07-07	2022-03-17	올레마 파마슈티컬스 인코포레이티드	에스트로겐 수용체 길항제 요법
EP4037768B1 (en)	2019-10-01	2023-10-11	Sanofi	Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof
AU2020399168A1 (en)	2019-12-09	2022-07-28	Sanofi	Crystalline form of a 7H-benzo[7]annulene-2-carboxylic acid derivative
TW202146007A (zh)	2020-02-27	2021-12-16	法商賽諾菲公司	包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合
TW202233572A (zh)	2020-10-19	2022-09-01	法商賽諾菲公司	新穎之經取代的6,7-二氫-5h-苯並[7]輪烯衍生物，其製備方法及其治療用途
WO2022084280A1 (en)	2020-10-19	2022-04-28	Sanofi	Substituted 6,7-dihydro-5h-benzo[7]annulene compounds and their derivatives, processes for their preparation and therapeutic uses thereof
TW202313558A (zh) *	2021-07-08	2023-04-01	大陸商勤浩醫藥(蘇州)有限公司	一類苯并七元環類化合物及其應用
US20240368121A1 (en) *	2021-08-20	2024-11-07	Biotheryx, Inc.	Estrogen receptor degraders, pharmaceutical compositions thereof, and their therapeutic applications
CN117362142B (zh) *	2023-10-09	2025-12-26	奥锐特药业股份有限公司	环己烯衍生物的不对称催化氢化方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5681835A (en) *	1994-04-25	1997-10-28	Glaxo Wellcome Inc.	Non-steroidal ligands for the estrogen receptor
DE69840126D1 (de)	1997-08-15	2008-11-27	Univ Duke	Verfahren zur prophylaxis oder behandlung von östrogen-abhängigen krankheiten
FR2778404B1 (fr)	1998-05-06	2000-06-30	Hoechst Marion Roussel Inc	Derives du dihydro ou tetrahydronaphtalene, et les compositions pharmaceutiques les renfermant
AU7896100A (en)	1999-10-14	2001-04-23	Endorecherche Inc.	Selective estrogen receptor modulators in the treatment or reduction of the riskof acquiring hypertension, cardiovascular diseases, and insulin resistance
US6528681B2 (en)	2000-04-05	2003-03-04	Bristol-Meyers Squibb Pharma Company	Halogenated triphenylethylene derivatives as selective estrogen receptor modulators
US6417394B2 (en) *	2000-04-05	2002-07-09	Bristol Myers Squibb Pharma Company	Specific salt forms of triphenylethylene derivatives as selective estrogen receptor modulators

2002
- 2002-08-09 PL PL02374215A patent/PL374215A1/xx not_active Application Discontinuation
- 2002-08-09 EE EEP200400061A patent/EE200400061A/et unknown
- 2002-08-09 HU HU0500573A patent/HUP0500573A2/hu unknown
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- 2002-08-09 SK SK60-2004A patent/SK602004A3/sk not_active Application Discontinuation
- 2002-08-09 EP EP02757058A patent/EP1417169A2/en not_active Withdrawn
- 2002-08-09 AU AU2002323098A patent/AU2002323098A1/en not_active Abandoned
- 2002-08-09 US US10/216,253 patent/US6927224B2/en not_active Expired - Lifetime
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- 2004-02-03 BG BG108561A patent/BG108561A/bg unknown
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US6927224B2 (en)	2005-08-09
US20050267183A1 (en)	2005-12-01
HUP0500573A2 (hu)	2005-11-28
WO2003016270A2 (en)	2003-02-27
CZ2004220A3 (cs)	2004-06-16
US20030105148A1 (en)	2003-06-05
US7323587B2 (en)	2008-01-29
EP1417169A2 (en)	2004-05-12
JP2005528320A (ja)	2005-09-22
WO2003016270A3 (en)	2003-11-06
BG108561A (bg)	2005-04-30
EE200400061A (et)	2004-04-15
US20050245602A1 (en)	2005-11-03
AU2002323098A1 (en)	2003-03-03
US7045540B2 (en)	2006-05-16
PL374215A1 (en)	2005-10-03

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US7323587B2 (en)	2008-01-29	Selective estrogen receptor modulators
CN110028403B (zh)	2020-08-11	一种合成丁二酸类化合物的方法
US6528681B2 (en)	2003-03-04	Halogenated triphenylethylene derivatives as selective estrogen receptor modulators
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US6417394B2 (en)	2002-07-09	Specific salt forms of triphenylethylene derivatives as selective estrogen receptor modulators
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RU2407741C2 (ru)	2010-12-27	Способ получения кандесартана
EP0338895A1 (fr)	1989-10-25	Nouveaux dérivés hétéroarotinoides, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent
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AU2001253191A1 (en)	2002-01-10	Specific salt forms of triphenylethylene derivatives as selective estrogen receptor modulators
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CH650255A5 (fr)	1985-07-15	Derives d'imidazole, leur procede de preparation et composition pharmaceutique les contenant.
CN107868069A (zh)	2018-04-03	7‑羟基‑8‑甲基‑6‑硝基‑2‑氧‑2h‑苯并吡喃‑3‑羧酸的制备工艺
CN103183604A (zh)	2013-07-03	维达洛芬的制备方法
Snyder et al.	1946	The Preparation of Unsymmetrical Diaryl Amines. 5-Phenylamino-6-methoxy-8-(3-diethylaminopropylamino)-quinoline1
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JP2740959B2 (ja)	1998-04-15	スレオ―３―（３，４―ジアルコキシフェニル）セリン誘導体の選択的製造方法
JP3030347B2 (ja)	2000-04-10	モノアルキル化法
FR2575470A1 (fr)	1986-07-04	Derives amines de n-imidazolylmethyl-diphenylazomethines, leur preparation et leur application en therapeutique
JPS62181244A (ja)	1987-08-08	４〔４−（４−クロロフエニル）ブトキシ〕フエニルメチルアミン誘導体とその酸付加塩及びその製造方法