JP2013520443A5 - - Google Patents
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- Publication number
- JP2013520443A5 JP2013520443A5 JP2012554085A JP2012554085A JP2013520443A5 JP 2013520443 A5 JP2013520443 A5 JP 2013520443A5 JP 2012554085 A JP2012554085 A JP 2012554085A JP 2012554085 A JP2012554085 A JP 2012554085A JP 2013520443 A5 JP2013520443 A5 JP 2013520443A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- ring
- acceptable salt
- compound according
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 3
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Chemical compound C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 2
- HBEDSQVIWPRPAY-UHFFFAOYSA-N 2,3-dihydrobenzofuran Chemical compound C1=CC=C2OCCC2=C1 HBEDSQVIWPRPAY-UHFFFAOYSA-N 0.000 claims 2
- 201000002847 Cowden syndrome Diseases 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 1
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 claims 1
- 201000007815 Bannayan-Riley-Ruvalcaba syndrome Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000012609 Cowden disease Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 208000007569 Giant Cell Tumors Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 1
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 1
- 208000022010 Lhermitte-Duclos disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- -1 chloro, hydroxyl Chemical group 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- LPAGFVYQRIESJQ-UHFFFAOYSA-N indoline Chemical compound C1=CC=C2NCCC2=C1 LPAGFVYQRIESJQ-UHFFFAOYSA-N 0.000 claims 1
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- VDBNYAPERZTOOF-UHFFFAOYSA-N isoquinolin-1(2H)-one Chemical compound C1=CC=C2C(=O)NC=CC2=C1 VDBNYAPERZTOOF-UHFFFAOYSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 150000003222 pyridines Chemical class 0.000 claims 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 0 CC(*)(C=C(*)C=C1)C=C1N(C1O)C(CC2CC(CCC(*)=O)C2)=NN1*=C Chemical compound CC(*)(C=C(*)C=C1)C=C1N(C1O)C(CC2CC(CCC(*)=O)C2)=NN1*=C 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30670910P | 2010-02-22 | 2010-02-22 | |
| US61/306,709 | 2010-02-22 | ||
| US35758710P | 2010-06-23 | 2010-06-23 | |
| US61/357,587 | 2010-06-23 | ||
| PCT/US2011/025661 WO2011103546A1 (en) | 2010-02-22 | 2011-02-22 | Triazolones as fatty acid synthase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013520443A JP2013520443A (ja) | 2013-06-06 |
| JP2013520443A5 true JP2013520443A5 (enExample) | 2014-03-13 |
| JP5805672B2 JP5805672B2 (ja) | 2015-11-04 |
Family
ID=44483349
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012554085A Expired - Fee Related JP5805672B2 (ja) | 2010-02-22 | 2011-02-22 | 脂肪酸合成酵素阻害剤としてのトリアゾロン類 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8802864B2 (enExample) |
| EP (1) | EP2538787B1 (enExample) |
| JP (1) | JP5805672B2 (enExample) |
| KR (1) | KR20120133386A (enExample) |
| CN (1) | CN102858175A (enExample) |
| AU (1) | AU2011217809A1 (enExample) |
| BR (1) | BR112012020976A2 (enExample) |
| CA (1) | CA2790692A1 (enExample) |
| EA (1) | EA201290822A1 (enExample) |
| ES (1) | ES2509951T3 (enExample) |
| MX (1) | MX2012009720A (enExample) |
| SG (1) | SG183260A1 (enExample) |
| WO (1) | WO2011103546A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2509951T3 (es) * | 2010-02-22 | 2014-10-20 | Glaxosmithkline Llc | Triazolonas como inhibidores de sintasa de ácidos grasos |
| EP2822931B1 (en) * | 2012-03-09 | 2017-05-03 | Inception 2, Inc. | Triazolone compounds and uses thereof |
| SG11201504622PA (en) | 2012-12-20 | 2015-07-30 | Inception 2 Inc | Triazolone compounds and uses thereof |
| US20150329524A1 (en) * | 2013-01-10 | 2015-11-19 | Glaxosmithkline Intellectual Property (No.2) Limited | Fatty acid synthase inhibitors |
| ES2753386T3 (es) | 2013-03-13 | 2020-04-08 | Forma Therapeutics Inc | Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer |
| JP6434522B2 (ja) | 2013-09-05 | 2018-12-05 | ダウ アグロサイエンシィズ エルエルシー | ホウ素化アレーンを生成する方法 |
| CN105579440A (zh) | 2013-09-06 | 2016-05-11 | 因森普深2公司 | 三唑酮化合物及其应用 |
| WO2015095011A1 (en) | 2013-12-17 | 2015-06-25 | Janssen Pharmaceutica Nv | Imidazolin-5-one derivative useful as fasn inhibitors for the treatment of cancer |
| TW201625354A (zh) | 2014-06-16 | 2016-07-16 | 陶氏農業科學公司 | 用於製備氧硼基化芳烴之方法 |
| CN104876917B (zh) * | 2015-06-16 | 2017-09-19 | 上海皓元医药股份有限公司 | 用作脂肪酸合成酶抑制剂的三唑酮的合成方法 |
| WO2016205590A1 (en) | 2015-06-18 | 2016-12-22 | Cephalon, Inc. | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| KR20180026459A (ko) | 2015-06-18 | 2018-03-12 | 세파론, 인코포레이티드 | 1,4-치환된 피페리딘 유도체 |
| TW201722957A (zh) * | 2015-09-15 | 2017-07-01 | 葛蘭素史克智慧財產（第二）有限公司 | 化學化合物 |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
| CN114539193B (zh) * | 2022-01-20 | 2024-08-06 | 安徽普利药业有限公司 | 一种盐酸胺碘酮中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5728834A (en) * | 1996-11-14 | 1998-03-17 | Wyckoff Chemical Company, Inc. | Process for preparation of 4-aryl-1,2,4-triazol-3-ones |
| ATE552236T1 (de) * | 2003-01-14 | 2012-04-15 | Cytokinetics Inc | Verbindungen, zusammensetzungen und verfahren zur behandlung von herzinsuffizienz |
| SE0400850D0 (sv) * | 2004-03-30 | 2004-03-31 | Astrazeneca Ab | Novel Compounds |
| ES2355923T3 (es) * | 2004-08-26 | 2011-04-01 | Pfizer, Inc. | Compuestos de aminoheteroarilo sustituidos con pirazol como inhibidores de proteina quinasa. |
| JP5116687B2 (ja) * | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ［２，１−ｆ］［１，２，４］トリアジン−４−イルアミンＩＧＦ−１Ｒキナーゼ阻害剤 |
| US8236792B2 (en) | 2008-05-23 | 2012-08-07 | Janssen Pharmaceutica Nv | Substituted pyrrolidine amides as modulators of the histamine H3 receptor |
| ES2509951T3 (es) * | 2010-02-22 | 2014-10-20 | Glaxosmithkline Llc | Triazolonas como inhibidores de sintasa de ácidos grasos |
-
2011
- 2011-02-22 ES ES11745417.3T patent/ES2509951T3/es active Active
- 2011-02-22 EP EP11745417.3A patent/EP2538787B1/en active Active
- 2011-02-22 JP JP2012554085A patent/JP5805672B2/ja not_active Expired - Fee Related
- 2011-02-22 EA EA201290822A patent/EA201290822A1/ru unknown
- 2011-02-22 WO PCT/US2011/025661 patent/WO2011103546A1/en not_active Ceased
- 2011-02-22 BR BR112012020976A patent/BR112012020976A2/pt not_active Application Discontinuation
- 2011-02-22 CN CN2011800201452A patent/CN102858175A/zh active Pending
- 2011-02-22 MX MX2012009720A patent/MX2012009720A/es unknown
- 2011-02-22 AU AU2011217809A patent/AU2011217809A1/en not_active Abandoned
- 2011-02-22 CA CA2790692A patent/CA2790692A1/en not_active Abandoned
- 2011-02-22 SG SG2012059291A patent/SG183260A1/en unknown
- 2011-02-22 KR KR1020127024682A patent/KR20120133386A/ko not_active Withdrawn
- 2011-02-22 US US13/579,040 patent/US8802864B2/en not_active Expired - Fee Related
-
2013
- 2013-11-04 US US14/071,093 patent/US9340529B2/en not_active Expired - Fee Related
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