JP2016509022A5 - - Google Patents
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- JP2016509022A5 JP2016509022A5 JP2015558090A JP2015558090A JP2016509022A5 JP 2016509022 A5 JP2016509022 A5 JP 2016509022A5 JP 2015558090 A JP2015558090 A JP 2015558090A JP 2015558090 A JP2015558090 A JP 2015558090A JP 2016509022 A5 JP2016509022 A5 JP 2016509022A5
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- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- substituted
- halo
- independently
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims description 100
- 229910052739 hydrogen Inorganic materials 0.000 claims description 56
- 239000001257 hydrogen Substances 0.000 claims description 56
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 43
- -1 hydroxy, amino Chemical group 0.000 claims description 30
- 150000001875 compounds Chemical class 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 17
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000002947 alkylene group Chemical group 0.000 claims description 14
- 150000002431 hydrogen Chemical class 0.000 claims description 14
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 14
- 229920006395 saturated elastomer Polymers 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 12
- 125000002883 imidazolyl group Chemical group 0.000 claims description 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 229940124597 therapeutic agent Drugs 0.000 claims description 8
- 229920002472 Starch Polymers 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical group C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
- 239000000730 antalgic agent Substances 0.000 claims description 4
- 230000003474 anti-emetic effect Effects 0.000 claims description 4
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 4
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 4
- 239000000935 antidepressant agent Substances 0.000 claims description 4
- 229940005513 antidepressants Drugs 0.000 claims description 4
- 239000002111 antiemetic agent Substances 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 239000001913 cellulose Substances 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- MMXKVMNBHPAILY-UHFFFAOYSA-N ethyl laurate Chemical compound CCCCCCCCCCCC(=O)OCC MMXKVMNBHPAILY-UHFFFAOYSA-N 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 235000010356 sorbitol Nutrition 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 2
- 229920001817 Agar Polymers 0.000 claims description 2
- 239000005995 Aluminium silicate Substances 0.000 claims description 2
- 241000416162 Astragalus gummifer Species 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 229920002261 Corn starch Polymers 0.000 claims description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 239000001856 Ethyl cellulose Substances 0.000 claims description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 229920002907 Guar gum Polymers 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 240000003183 Manihot esculenta Species 0.000 claims description 2
- 235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 claims description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 235000019483 Peanut oil Nutrition 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 2
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- 235000019486 Sunflower oil Nutrition 0.000 claims description 2
- 229920001615 Tragacanth Polymers 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 2
- 239000008272 agar Substances 0.000 claims description 2
- 235000010419 agar Nutrition 0.000 claims description 2
- 235000010443 alginic acid Nutrition 0.000 claims description 2
- 239000000783 alginic acid Substances 0.000 claims description 2
- 229920000615 alginic acid Polymers 0.000 claims description 2
- 229960001126 alginic acid Drugs 0.000 claims description 2
- 150000004781 alginic acids Chemical class 0.000 claims description 2
- 235000012211 aluminium silicate Nutrition 0.000 claims description 2
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims description 2
- 230000000202 analgesic effect Effects 0.000 claims description 2
- 229940035676 analgesics Drugs 0.000 claims description 2
- 230000001093 anti-cancer Effects 0.000 claims description 2
- 230000001430 anti-depressive effect Effects 0.000 claims description 2
- 229940125683 antiemetic agent Drugs 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 229940041181 antineoplastic drug Drugs 0.000 claims description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 2
- 235000010216 calcium carbonate Nutrition 0.000 claims description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 2
- 235000013539 calcium stearate Nutrition 0.000 claims description 2
- 239000008116 calcium stearate Substances 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 claims description 2
- 235000010980 cellulose Nutrition 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 229920002301 cellulose acetate Polymers 0.000 claims description 2
- 239000004927 clay Substances 0.000 claims description 2
- 229910052570 clay Inorganic materials 0.000 claims description 2
- 235000005687 corn oil Nutrition 0.000 claims description 2
- 239000002285 corn oil Substances 0.000 claims description 2
- 239000008120 corn starch Substances 0.000 claims description 2
- 235000012343 cottonseed oil Nutrition 0.000 claims description 2
- 239000002385 cottonseed oil Substances 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 229960000913 crospovidone Drugs 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 2
- 229920001249 ethyl cellulose Polymers 0.000 claims description 2
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 2
- 229940093471 ethyl oleate Drugs 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 235000011187 glycerol Nutrition 0.000 claims description 2
- 150000002334 glycols Chemical class 0.000 claims description 2
- 239000000665 guar gum Substances 0.000 claims description 2
- 235000010417 guar gum Nutrition 0.000 claims description 2
- 229960002154 guar gum Drugs 0.000 claims description 2
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims description 2
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims description 2
- 229940059904 light mineral oil Drugs 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 2
- 239000002480 mineral oil Substances 0.000 claims description 2
- 235000010446 mineral oil Nutrition 0.000 claims description 2
- 229920001206 natural gum Polymers 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
- 239000004006 olive oil Substances 0.000 claims description 2
- 235000008390 olive oil Nutrition 0.000 claims description 2
- 239000000312 peanut oil Substances 0.000 claims description 2
- 229960000540 polacrilin potassium Drugs 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- WVWZXTJUCNEUAE-UHFFFAOYSA-M potassium;1,2-bis(ethenyl)benzene;2-methylprop-2-enoate Chemical compound [K+].CC(=C)C([O-])=O.C=CC1=CC=CC=C1C=C WVWZXTJUCNEUAE-UHFFFAOYSA-M 0.000 claims description 2
- 229920001592 potato starch Polymers 0.000 claims description 2
- 229920003124 powdered cellulose Polymers 0.000 claims description 2
- 235000019814 powdered cellulose Nutrition 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 239000008159 sesame oil Substances 0.000 claims description 2
- 235000011803 sesame oil Nutrition 0.000 claims description 2
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims description 2
- 239000000377 silicon dioxide Substances 0.000 claims description 2
- 235000012239 silicon dioxide Nutrition 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 235000010413 sodium alginate Nutrition 0.000 claims description 2
- 239000000661 sodium alginate Substances 0.000 claims description 2
- 229940005550 sodium alginate Drugs 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- 235000017550 sodium carbonate Nutrition 0.000 claims description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 2
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims description 2
- 239000003549 soybean oil Substances 0.000 claims description 2
- 235000012424 soybean oil Nutrition 0.000 claims description 2
- 229940032147 starch Drugs 0.000 claims description 2
- 239000008117 stearic acid Substances 0.000 claims description 2
- 235000000346 sugar Nutrition 0.000 claims description 2
- 239000002600 sunflower oil Substances 0.000 claims description 2
- 239000000454 talc Substances 0.000 claims description 2
- 229910052623 talc Inorganic materials 0.000 claims description 2
- 235000012222 talc Nutrition 0.000 claims description 2
- 235000010487 tragacanth Nutrition 0.000 claims description 2
- 239000000196 tragacanth Substances 0.000 claims description 2
- 229940116362 tragacanth Drugs 0.000 claims description 2
- 206010046766 uterine cancer Diseases 0.000 claims description 2
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000034 method Methods 0.000 description 4
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361766439P | 2013-02-19 | 2013-02-19 | |
| US61/766,439 | 2013-02-19 | ||
| PCT/US2014/015938 WO2014130310A1 (en) | 2013-02-19 | 2014-02-12 | Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016509022A JP2016509022A (ja) | 2016-03-24 |
| JP2016509022A5 true JP2016509022A5 (enExample) | 2017-03-16 |
| JP6364028B2 JP6364028B2 (ja) | 2018-07-25 |
Family
ID=50239942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015558090A Active JP6364028B2 (ja) | 2013-02-19 | 2014-02-12 | 選択的エストロゲン受容体ディグレーダーとしてのベンゾチオフェン誘導体およびその組成物 |
Country Status (46)
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE039052T2 (hu) | 2013-02-19 | 2018-12-28 | Novartis Ag | Benzotiofénszármazékok és azok készítményei szelektív ösztrogén receptor lebontóként |
| US10308871B2 (en) * | 2015-02-19 | 2019-06-04 | Jnc Corporation | Liquid crystal compound having benzothiophene, liquid crystal composition and liquid crystal display device |
| TWI708770B (zh) * | 2015-06-08 | 2020-11-01 | 日商捷恩智股份有限公司 | 具有苯并噻吩的液晶性化合物、液晶組成物及液晶顯示元件 |
| ES2935125T3 (es) * | 2015-12-09 | 2023-03-01 | Univ Illinois | Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno |
| US20190142811A1 (en) | 2016-04-01 | 2019-05-16 | Zeno Royalties & Milestones, LLC | Estrogen receptor modulators |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| AR110728A1 (es) * | 2017-01-06 | 2019-04-24 | G1 Therapeutics Inc | Terapia combinada para el tratamiento del cáncer |
| TW201835064A (zh) | 2017-02-10 | 2018-10-01 | 美商G1治療公司 | 苯并噻吩雌激素受體調節劑 |
| EP3709997A1 (en) | 2017-11-16 | 2020-09-23 | Novartis AG | Pharmaceutical combination comprising lsz102 and ribociclib |
| CN111655288A (zh) | 2017-11-16 | 2020-09-11 | 诺华股份有限公司 | 组合疗法 |
| EP3716969A1 (en) | 2017-12-01 | 2020-10-07 | Novartis AG | Pharmaceutical combination comprising lsz102 and alpelisib |
| CN119161384A (zh) | 2018-01-22 | 2024-12-20 | 雷迪厄斯制药公司 | 雌激素受体调节化合物 |
| WO2019157020A1 (en) | 2018-02-06 | 2019-08-15 | The Board Of Trustees Of The University Of Illinois | Substituted benzothiophene analogs as selective estrogen receptor degraders |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| CN112839646A (zh) * | 2018-08-16 | 2021-05-25 | G1治疗公司 | 用于治疗医学疾病的苯并噻吩雌激素受体调节剂 |
| WO2020128972A1 (en) | 2018-12-20 | 2020-06-25 | Novartis Ag | Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives |
| BR112021015672A2 (pt) | 2019-02-15 | 2021-10-05 | Novartis Ag | Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona substituída e usos dos mesmos |
| ES3032659T3 (en) | 2019-02-15 | 2025-07-23 | Novartis Ag | 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| CA3138058A1 (en) | 2019-05-20 | 2020-11-26 | Matthew T. Burger | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| EP3993787A4 (en) | 2019-08-06 | 2023-07-12 | Recurium IP Holdings, LLC | Estrogen receptor modulators for treating mutants |
| KR20220116257A (ko) | 2019-12-20 | 2022-08-22 | 노파르티스 아게 | 골수섬유증 및 골수이형성 증후군을 치료하기 위한, 데시타빈 또는 항 pd-1 항체 스파르탈리주맙을 포함하거나 또는 포함하지 않는, 항 tim-3 항체 mbg453 및 항 tgf-베타 항체 nis793의 조합물 |
| CN111057065B (zh) * | 2019-12-24 | 2021-04-23 | 沈阳药科大学 | 噻吩并嘧啶类化合物的制备方法和用途 |
| CN111646972B (zh) * | 2020-06-12 | 2021-06-29 | 上海皓元医药股份有限公司 | 一种选择性雌激素受体降解剂及其中间体的制备方法 |
| CN115916199A (zh) | 2020-06-23 | 2023-04-04 | 诺华股份有限公司 | 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案 |
| CN116096715A (zh) * | 2020-07-06 | 2023-05-09 | 泰科根公司 | 用于精神障碍或精神增强的有益苯并噻吩组合物 |
| US20230271940A1 (en) | 2020-08-03 | 2023-08-31 | Novartis Ag | Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| CR20230283A (es) | 2020-11-24 | 2023-07-27 | Novartis Ag | Anticuerpos anti-cd48, conjugados de anticuerpo-fármaco, y usos de los mismos |
| WO2022115451A1 (en) | 2020-11-24 | 2022-06-02 | Novartis Ag | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| JP2024502270A (ja) | 2020-12-23 | 2024-01-18 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | エストロゲン受容体調節薬 |
| KR20230170644A (ko) | 2021-02-02 | 2023-12-19 | 르 라보레또레 쎄르비에르 | 선택적 bcl-xl protac 화합물 및 사용 방법 |
| TW202304979A (zh) | 2021-04-07 | 2023-02-01 | 瑞士商諾華公司 | 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途 |
| AR125874A1 (es) | 2021-05-18 | 2023-08-23 | Novartis Ag | Terapias de combinación |
| CN116265458A (zh) * | 2021-12-17 | 2023-06-20 | 中国科学院上海药物研究所 | 苯并噻吩类衍生物、及其制备方法和用途 |
| GB2617173B (en) | 2022-03-31 | 2024-11-20 | Iceye Oy | Detecting and suppressing ambiguities in synthetic aperture radar data and images |
| EP4525926A1 (en) | 2022-05-20 | 2025-03-26 | Novartis AG | Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof |
| JP2025517430A (ja) | 2022-05-20 | 2025-06-05 | ノバルティス アーゲー | Ｅｐｈａ２ ｂｃｌ－ｘｌ阻害剤抗体－薬物コンジュゲートおよびその使用の方法 |
| CN115710248B (zh) * | 2022-11-18 | 2024-06-21 | 南京中医药大学 | 新型选择性雌激素受体下调剂化合物、制备方法及用途 |
| CN120752058A (zh) | 2023-03-10 | 2025-10-03 | 诺华股份有限公司 | panRAS抑制剂抗体-药物缀合物及其使用方法 |
| PY24103486A (es) | 2023-11-22 | 2025-06-06 | Servier Lab | Conjugados de anticuerpo anti-cd74-fármaco y métodos de uso de los mismos |
| TW202539634A (zh) | 2024-04-10 | 2025-10-16 | 瑞士商諾華公司 | Ｐａｎｒａｓ抑制劑及其使用方法 |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH445129A (fr) | 1964-04-29 | 1967-10-15 | Nestle Sa | Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé |
| US3459731A (en) | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
| US3426011A (en) | 1967-02-13 | 1969-02-04 | Corn Products Co | Cyclodextrins with anionic properties |
| US3453257A (en) | 1967-02-13 | 1969-07-01 | Corn Products Co | Cyclodextrin with cationic properties |
| US3453259A (en) | 1967-03-22 | 1969-07-01 | Corn Products Co | Cyclodextrin polyol ethers and their oxidation products |
| JPS6041077B2 (ja) | 1976-09-06 | 1985-09-13 | 喜徳 喜谷 | １，２‐ジアミノシクロヘキサン異性体のシス白金（２）錯体 |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4261989A (en) | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| ZA822247B (en) * | 1981-04-03 | 1983-11-30 | Lilly Co Eli | Benzothiophene compounds and process for preparing them |
| US4418068A (en) | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| US4737323A (en) | 1986-02-13 | 1988-04-12 | Liposome Technology, Inc. | Liposome extrusion method |
| US5266573A (en) | 1989-08-07 | 1993-11-30 | Elf Sanofi | Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| EP0647450A1 (en) | 1993-09-09 | 1995-04-12 | BEHRINGWERKE Aktiengesellschaft | Improved prodrugs for enzyme mediated activation |
| US6756388B1 (en) * | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| US6562862B1 (en) * | 1994-10-20 | 2003-05-13 | Eli Lilly And Company | Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y |
| IL115849A0 (en) | 1994-11-03 | 1996-01-31 | Merz & Co Gmbh & Co | Tangential filtration preparation of liposomal drugs and liposome product thereof |
| US5589482A (en) | 1994-12-14 | 1996-12-31 | Pfizer Inc. | Benzo-thiophene estrogen agonists to treat prostatic hyperplasia |
| US5998441A (en) * | 1995-02-28 | 1999-12-07 | Eli Lilly And Company | Benzothiophene compounds, intermediates, compositions, and methods |
| AR003930A1 (es) * | 1995-02-28 | 1998-09-30 | Lilly Co Eli | Procedimiento para preparar compuestos de 2-fenil-3-fenoxi o feniltio-benzotiofeno y sales farmaceuticamente aceptables, compuestos intermediarios de aplicación exclusiva en dicho procedimiento y metodo para preparar los compuestos intermediarios mencionados |
| US5510357A (en) | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| US6417199B1 (en) | 1995-03-10 | 2002-07-09 | Eli Lilly And Company | 3-benzyl-benzothiophenes |
| DK0842169T3 (da) | 1995-06-26 | 2001-01-29 | Lilly Co Eli | Benzothiophenforbindelser |
| US5731342A (en) | 1996-02-22 | 1998-03-24 | Eli Lilly And Company | Benzothiophenes, formulations containing same, and methods |
| US5827876A (en) * | 1996-04-09 | 1998-10-27 | American Home Products Corporation | Inhibition of bone loss by 3-(4-acrylamidobenzoyl) benzo b!-thiophenes |
| US5886025A (en) | 1997-03-06 | 1999-03-23 | Baylor University | Anti-mitotic agents which inhibit tubulin polymerization |
| ZA982877B (en) | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Treatment of central nervous system disorders with selective estrogen receptor modulators. |
| ZA982818B (en) | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Prevention of breast cancer using selective estrogen receptor modulators. |
| ZA982819B (en) | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Treatment or prophylaxis of prostatic cancer and benign prostatic hyperplasia with selective estrogn receptor modulators. |
| CN1308621A (zh) | 1998-05-12 | 2001-08-15 | 美国家用产品公司 | 用于治疗胰岛素抗性和高血糖的苯基氧代－乙酸 |
| US6166069A (en) | 1998-05-12 | 2000-12-26 | American Home Products Corporation | Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| GB0018891D0 (en) | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
| IL151517A0 (en) | 2000-03-09 | 2003-04-10 | Aventis Pharma Gmbh | Therapeutic uses of ppar mediators |
| US7091240B2 (en) | 2000-03-10 | 2006-08-15 | Oxigene, Inc. | Tubulin binding ligands and corresponding prodrug constructs |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US7425565B2 (en) | 2002-05-09 | 2008-09-16 | Cedars-Sinai Medical Center | Use of benzothiopenes to treat and prevent prostate cancer |
| BR0307544A (pt) | 2002-02-01 | 2004-12-07 | Ariad Gene Therapeutics Inc | Compostos contendo fósforos, componentes e composição bem como, sua utilização através de métodos de tratamentos |
| JP4201716B2 (ja) | 2002-03-05 | 2008-12-24 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害剤 |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| DE60327931D1 (de) | 2002-07-22 | 2009-07-23 | Lilly Co Eli | Selektive östrogenrezeptor modulatoren, die eine phenylsulfonyl-gruppe enthalten |
| ATE407129T1 (de) | 2003-06-10 | 2008-09-15 | Lilly Co Eli | Pentafluoroalkylsulfin-naphthaline und und darauf bezogene modulatoren des östrogenrezeptors |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| WO2005073206A1 (en) * | 2004-01-22 | 2005-08-11 | Eli Lilly And Company | Selective estrogen receptor modulators |
| US20070111988A1 (en) | 2004-01-22 | 2007-05-17 | Eli Lilly And Company | Selective estrogen receptor modulators |
| WO2005073190A1 (en) | 2004-01-29 | 2005-08-11 | Eli Lilly And Company | Selective estrogen receptor modulators |
| KR20200019263A (ko) | 2004-09-02 | 2020-02-21 | 제넨테크, 인크. | 헤지호그 신호전달에 대한 피리딜 억제제 |
| US7998974B2 (en) | 2005-03-03 | 2011-08-16 | Sirtris Pharmaceuticals, Inc. | Fused heterocyclic compounds and their use as sirtuin modulators |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CA2681478A1 (en) | 2007-03-16 | 2008-09-25 | Eli Lilly And Company | Process and intermediates for preparing arzoxifene |
| US20090069380A1 (en) | 2007-09-12 | 2009-03-12 | Protia, Llc | Deuterium-enriched aroxifene |
| AU2008298948B2 (en) | 2007-09-12 | 2014-09-04 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| EP2214675B1 (en) | 2007-10-25 | 2013-11-20 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| CN102477033A (zh) * | 2010-11-23 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途 |
| US9540361B2 (en) | 2010-12-24 | 2017-01-10 | Merck Sharp & Dohme B.V. | N-substituted azetidine derivatives |
| HUE039052T2 (hu) | 2013-02-19 | 2018-12-28 | Novartis Ag | Benzotiofénszármazékok és azok készítményei szelektív ösztrogén receptor lebontóként |
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