TW201630907A

TW201630907A - ＴＧＦβＲ拮抗劑

ＴＧＦβＲ拮抗劑 Download PDF

Info

Publication number: TW201630907A
Authority: TW; Taiwan
Prior art keywords: alkyl; hydrogen; pyridin; halogen; independently
Prior art date: 2014-12-22

Application number

TW104142991A

Other languages

English (en)

Chinese (zh)

Inventor

布萊恩Ｅ芬克

玉芬趙

羅伯特Ｍ波里賴瑞

云惠張

敬淳金

穆索尼Ｇ卡茂

安德魯Ｊ提班

Original Assignee

必治妥美雅史谷比公司

Priority date

2014-12-22

Filing date

2015-12-21

Publication date

2016-09-01

2015-12-21 Application filed by 必治妥美雅史谷比公司 filed Critical 必治妥美雅史谷比公司

2016-09-01 Publication of TW201630907A publication Critical patent/TW201630907A/zh

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239000005557 antagonist Substances 0.000 title claims description 25
150000001875 compounds Chemical class 0.000 claims abstract description 195
206010028980 Neoplasm Diseases 0.000 claims abstract description 48
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 25
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 23
201000011510 cancer Diseases 0.000 claims abstract description 21
125000000217 alkyl group Chemical group 0.000 claims description 375
229910052739 hydrogen Inorganic materials 0.000 claims description 226
239000001257 hydrogen Substances 0.000 claims description 226
-1 -NHCOOH Chemical group 0.000 claims description 169
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 123
229910052736 halogen Inorganic materials 0.000 claims description 122
150000002367 halogens Chemical group 0.000 claims description 122
125000004093 cyano group Chemical group *C#N 0.000 claims description 99
125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 87
125000000753 cycloalkyl group Chemical group 0.000 claims description 74
125000003282 alkyl amino group Chemical group 0.000 claims description 71
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 66
125000000623 heterocyclic group Chemical group 0.000 claims description 65
DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 62
150000003839 salts Chemical class 0.000 claims description 59
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 54
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229910052757 nitrogen Inorganic materials 0.000 claims description 39
239000003814 drug Substances 0.000 claims description 37
238000011282 treatment Methods 0.000 claims description 24
125000003342 alkenyl group Chemical group 0.000 claims description 23
125000004433 nitrogen atom Chemical group N* 0.000 claims description 22
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 18
201000010099 disease Diseases 0.000 claims description 18
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 16
125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 15
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125000001072 heteroaryl group Chemical group 0.000 claims description 12
AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical group C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 12
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MWPLVEDNUUSJAV-UHFFFAOYSA-N anthracene Chemical group C1=CC=CC2=CC3=CC=CC=C3C=C21 MWPLVEDNUUSJAV-UHFFFAOYSA-N 0.000 claims description 8
239000003937 drug carrier Substances 0.000 claims description 8
150000001335 aliphatic alkanes Chemical class 0.000 claims description 7
210000004027 cell Anatomy 0.000 claims description 7
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FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 6
SMWDFEZZVXVKRB-UHFFFAOYSA-N anhydrous quinoline Chemical group N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims description 6
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206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 4
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 4
238000004519 manufacturing process Methods 0.000 claims description 4
UKJWABCHVCNLAX-UHFFFAOYSA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-ethoxy-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2OCC)C1=CC(=NC=C1)NC(C)=O)F UKJWABCHVCNLAX-UHFFFAOYSA-N 0.000 claims description 3
208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 3
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 3
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 3
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VRPRBQAJAQCSCW-BMSJAHLVSA-N N-[4-[3-[5-(trideuteriomethoxy)pyridin-2-yl]-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound C(OC=1C=CC(=NC=1)C1=C(NC=2C1=NC=CC=2)C1=CC(=NC=C1)NC(C)=O)([2H])([2H])[2H] VRPRBQAJAQCSCW-BMSJAHLVSA-N 0.000 claims description 2
SDIWHZMLILEDAK-BMSJAHLVSA-N N-[4-[6-chloro-3-[5-(trideuteriomethoxy)pyridin-2-yl]-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound ClC=1C=C2C(=NC=1)C(=C(N2)C1=CC(=NC=C1)NC(C)=O)C1=NC=C(C=C1)OC([2H])([2H])[2H] SDIWHZMLILEDAK-BMSJAHLVSA-N 0.000 claims description 2
MCOHDLNMMNXGOH-UHFFFAOYSA-N N-[4-[6-fluoro-3-(6-methoxypyridin-3-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC=1C=C2C(=NC=1)C(=C(N2)C1=CC(=NC=C1)NC(C)=O)C=1C=NC(=CC=1)OC MCOHDLNMMNXGOH-UHFFFAOYSA-N 0.000 claims description 2
239000013543 active substance Substances 0.000 claims description 2
125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 2
VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical group C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims description 2
229930192474 thiophene Chemical group 0.000 claims description 2
150000002431 hydrogen Chemical group 0.000 claims 49
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208000032839 leukemia Diseases 0.000 claims 2
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BXHURORUSAJJMH-UHFFFAOYSA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-(2-hydroxypropan-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2C(C)(C)O)C1=CC(=NC=C1)NC(C)=O)F BXHURORUSAJJMH-UHFFFAOYSA-N 0.000 claims 1
DYOHQLYHPIZXHG-UHFFFAOYSA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-(hydroxymethyl)-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2CO)C1=CC(=NC=C1)NC(C)=O)F DYOHQLYHPIZXHG-UHFFFAOYSA-N 0.000 claims 1
CDVFGEXFOAGXJO-UHFFFAOYSA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-(methylaminomethyl)-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2CNC)C1=CC(=NC=C1)NC(C)=O)F CDVFGEXFOAGXJO-UHFFFAOYSA-N 0.000 claims 1
OLYCUNOTKFNETC-NSHDSACASA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-[(1S)-1-hydroxyethyl]-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2[C@H](C)O)C1=CC(=NC=C1)NC(C)=O)F OLYCUNOTKFNETC-NSHDSACASA-N 0.000 claims 1
AQUKDYPRJZEQSG-UHFFFAOYSA-N N-[4-[3-[6-(difluoromethyl)pyridin-2-yl]-7-[(dimethylamino)methyl]-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound FC(C1=CC=CC(=N1)C1=C(NC=2C1=NC=CC=2CN(C)C)C1=CC(=NC=C1)NC(C)=O)F AQUKDYPRJZEQSG-UHFFFAOYSA-N 0.000 claims 1
SDIWHZMLILEDAK-UHFFFAOYSA-N N-[4-[6-chloro-3-(5-methoxypyridin-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl]pyridin-2-yl]acetamide Chemical compound ClC=1C=C2C(=NC=1)C(=C(N2)C1=CC(=NC=C1)NC(C)=O)C1=NC=C(C=C1)OC SDIWHZMLILEDAK-UHFFFAOYSA-N 0.000 claims 1
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