JP2016522835A5 - - Google Patents
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- JP2016522835A5 JP2016522835A5 JP2016516235A JP2016516235A JP2016522835A5 JP 2016522835 A5 JP2016522835 A5 JP 2016522835A5 JP 2016516235 A JP2016516235 A JP 2016516235A JP 2016516235 A JP2016516235 A JP 2016516235A JP 2016522835 A5 JP2016522835 A5 JP 2016522835A5
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- Prior art keywords
- fluoro
- pyrido
- methylpropyl
- phenyl
- indol
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- 150000001875 compounds Chemical class 0.000 claims 23
- -1 2-fluoro-2-methylpropyl Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 239000011780 sodium chloride Substances 0.000 claims 17
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- DFBDRVGWBHBJNR-BBNFHIFMSA-N (E)-3-[3,5-difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H](N2CC(C)(C)F)C)=C(F)C=C(\C=C\C(O)=O)C=C1F DFBDRVGWBHBJNR-BBNFHIFMSA-N 0.000 claims 1
- STVQFMFTCUMADM-XGMWYDOHSA-N (E)-3-[3,5-difluoro-4-[(1R,3R)-2-[(2S)-3-fluoro-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@@H](C)N2C[C@@H](CF)C)=C(F)C=C(\C=C\C(O)=O)C=C1F STVQFMFTCUMADM-XGMWYDOHSA-N 0.000 claims 1
- AKZLESYLLLKGNZ-MDZDMXLPSA-N (E)-3-[3,5-difluoro-4-[2-(2-fluoro-2-methylpropyl)-3,3-dimethyl-4,9-dihydro-1H-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(CC(C)(F)C)C1C1=C(F)C=C(\C=C\C(O)=O)C=C1F AKZLESYLLLKGNZ-MDZDMXLPSA-N 0.000 claims 1
- XTDHJGCTXMSPCY-RSEBSXLISA-N (E)-3-[3,5-difluoro-4-[2-[(2S)-3-fluoro-2-methylpropyl]-3,3-dimethyl-4,9-dihydro-1H-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(C[C@@H](CF)C)C1C1=C(F)C=C(\C=C\C(O)=O)C=C1F XTDHJGCTXMSPCY-RSEBSXLISA-N 0.000 claims 1
- IOPRLAHXDGSIHG-NAUGMMEESA-N (E)-3-[3-fluoro-4-[2-[(2S)-3-fluoro-2-methylpropyl]-3,3-dimethyl-4,9-dihydro-1H-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(C[C@@H](CF)C)C1C1=CC=C(\C=C\C(O)=O)C=C1F IOPRLAHXDGSIHG-NAUGMMEESA-N 0.000 claims 1
- CLDCRFJRMORRTI-IEGMAYJBSA-N (E)-3-[4-[(1R,3R)-2-[(2S)-3-fluoro-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@@H](C)N2C[C@@H](CF)C)=CC=C(\C=C\C(O)=O)C=C1 CLDCRFJRMORRTI-IEGMAYJBSA-N 0.000 claims 1
- RZLKPYCEHAUODL-SDNWHVSQSA-N (E)-3-[4-[2-(2-fluoro-2-methylpropyl)-3,3-dimethyl-4,9-dihydro-1H-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(CC(C)(F)C)C1C1=CC=C(\C=C\C(O)=O)C=C1 RZLKPYCEHAUODL-SDNWHVSQSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000003078 antioxidant Effects 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-L maleate(2-) Chemical compound [O-]C(=O)\C=C/C([O-])=O VZCYOOQTPOCHFL-UPHRSURJSA-L 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Claims (25)
- R3が水素である、請求項1または2に記載の化合物またはその医薬的に許容される塩。
- R3がメチルである、請求項1または2に記載の化合物またはその医薬的に許容される塩。
- R4が水素であり、R5がフルオロである、請求項1〜4のいずれか一項に記載の化合物またはその医薬的に許容される塩。
- R5が、水素であり、R4が、フルオロである、請求項1〜4のいずれか一項に記載の化合物またはその医薬的に許容される塩。
- 前記化合物が、
(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−((S)−3−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(4−((1R,3R)−2−((S)−3−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(3,5−ジフルオロ−4−(2−((S)−3−フルオロ−2−メチルプロピル)−3,3−ジメチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(3,5−ジフルオロ−4−(2−(2−フルオロ−2−メチルプロピル)−3,3−ジメチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(4−(2−((S)−3−フルオロ−2−メチルプロピル)−3,3−ジメチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(4−(2−(2−フルオロ−2−メチルプロピル)−3,3−ジメチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;
(E)−3−(3−フルオロ−4−(2−((S)−3−フルオロ−2−メチルプロピル)−3,3−ジメチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸;および
(E)−3−[4−[(1R,3R)−1−ジュウテリオ−2−(2−フルオロ−2−メチル−プロピル)−3−メチル−4,9−ジヒドロ−3H−ピリド[3,4−b]インドール−1−イル]−3,5−ジフルオロ−フェニル]プロパ−2−エン酸
から選択される、請求項1に記載の化合物またはそれらの医薬的に許容される塩。 - (E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸である、化合物。
- (E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸のマレイン酸塩である、化合物。
- 2θ=8.4°および10.9°において少なくとも2つの特定のピークを有するX線粉末回折パターンを有する結晶性形態であり、当該ピークは当該値の±0.2°(2θ)の範囲に観測されてもよい、化合物(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸。
- 2θ=8.4°、10.9°、18.3°、24.0°および14.0°において特定のピークを有するX線粉末回折パターンを有する結晶性形態であり、当該ピークは当該値の±0.2°(2θ)の範囲に観測されてもよい、化合物(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸。
- 2θ=8.4°、10.9°、18.3°、24.0°、14.0°、19.0°、14.4°、13.0°、15.3°および20.6°において特定のピークを有するX線粉末回折パターンを有する結晶性形態であり、当該ピークは当該値の±0.2°(2θ)の範囲に観測されてもよい、化合物(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸。
- 実質的に図2で示されるようなXRPDを有する結晶性形態の、化合物(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸。
- 実質的に図8で示されるようなXRPDを有する結晶性形態の、化合物(1R,3R)−1−{4−[(E)−2−カルボキシエテニル]−2,6−ジフルオロフェニル}−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ベータ−カルボリン−2−イウムマレエート。
- 医薬品として使用するための、請求項1〜15のいずれか一項に記載の化合物またはその医薬的に許容される塩。
- ヒトなどの温血動物におけるがんの予防または処置に使用するための、請求項1〜15のいずれか一項に記載の化合物またはその医薬的に許容される塩。
- (E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸、またはその医薬的に許容される塩である、請求項17に記載の化合物またはその医薬的に許容される塩。
- 乳がんまたは婦人科系がんの処置で使用するための、請求項17または18に記載の化合物またはその医薬的に許容される塩。
- 活性成分としての請求項1〜15のいずれか一項に記載の式(I)の化合物またはその医薬的に許容される塩と、少なくとも1つの医薬的に許容される希釈剤またはキャリアーとを含む医薬組成物。
- 少なくとも1つの医薬的に許容される希釈剤またはキャリアーを伴って、(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸、またはその医薬的に許容される塩を含み、組成物中の(R,E)−3−(3,5−ジフルオロ−4−(2−(2−フルオロ−2−メチルプロピル)−3−メチル−4,9−ジヒドロ−3H−ピリド[3,4−b]インドール−2−イウム−1−イル)フェニル)アクリレートの含有量が5%w/w未満である、請求項20の医薬組成物。
- 前記組成物が、抗酸化剤をさらに含み、金属−キレート剤をさらに含んでいてもよい、請求項21に記載の医薬組成物。
- 請求項1〜15のいずれか一項に記載の化合物またはその医薬的に許容される塩と、別の抗腫瘍剤とを含む、がんの処置での使用に好適な組み合わせ。
- 化合物が(E)−3−(3,5−ジフルオロ−4−((1R,3R)−2−(2−フルオロ−2−メチルプロピル)−3−メチル−2,3,4,9−テトラヒドロ−1H−ピリド[3,4−b]インドール−1−イル)フェニル)アクリル酸、またはその医薬的に許容される塩である、請求項23に記載の組み合わせ。
- 追加の抗腫瘍剤がパルボシクリブである、請求項23または24に記載の組み合わせ。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361827951P | 2013-05-28 | 2013-05-28 | |
US61/827,951 | 2013-05-28 | ||
US201361915685P | 2013-12-13 | 2013-12-13 | |
US61/915,685 | 2013-12-13 | ||
PCT/GB2014/051607 WO2014191726A1 (en) | 2013-05-28 | 2014-05-27 | Chemical compounds |
Publications (3)
Publication Number | Publication Date |
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JP2016522835A JP2016522835A (ja) | 2016-08-04 |
JP2016522835A5 true JP2016522835A5 (ja) | 2017-07-13 |
JP6286031B2 JP6286031B2 (ja) | 2018-02-28 |
Family
ID=50841880
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2016516235A Expired - Fee Related JP6286031B2 (ja) | 2013-05-28 | 2014-05-27 | 化合物 |
Country Status (35)
Country | Link |
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US (4) | US9155727B2 (ja) |
EP (2) | EP3360875A1 (ja) |
JP (1) | JP6286031B2 (ja) |
KR (1) | KR20160013198A (ja) |
CN (1) | CN105229004B (ja) |
AP (1) | AP2015008858A0 (ja) |
AU (1) | AU2014272856B2 (ja) |
BR (1) | BR112015029455A8 (ja) |
CA (1) | CA2911859A1 (ja) |
CL (1) | CL2015003491A1 (ja) |
CR (1) | CR20150629A (ja) |
CY (1) | CY1120474T1 (ja) |
DK (1) | DK3004090T3 (ja) |
DO (1) | DOP2015000274A (ja) |
ES (1) | ES2654161T3 (ja) |
HK (1) | HK1222859A1 (ja) |
HR (1) | HRP20171961T1 (ja) |
HU (1) | HUE035738T2 (ja) |
IL (1) | IL242559B (ja) |
LT (1) | LT3004090T (ja) |
ME (1) | ME02892B (ja) |
MX (1) | MX361538B (ja) |
NI (1) | NI201500167A (ja) |
PE (1) | PE20160874A1 (ja) |
PH (1) | PH12015502615A1 (ja) |
PL (1) | PL3004090T3 (ja) |
PT (1) | PT3004090T (ja) |
RS (1) | RS56678B1 (ja) |
RU (1) | RU2664109C2 (ja) |
SG (1) | SG11201509393VA (ja) |
SI (1) | SI3004090T1 (ja) |
TN (1) | TN2015000516A1 (ja) |
TW (1) | TWI653235B (ja) |
UY (1) | UY35590A (ja) |
WO (1) | WO2014191726A1 (ja) |
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