JP2010510215A5 - - Google Patents
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- Publication number
- JP2010510215A5 JP2010510215A5 JP2009537199A JP2009537199A JP2010510215A5 JP 2010510215 A5 JP2010510215 A5 JP 2010510215A5 JP 2009537199 A JP2009537199 A JP 2009537199A JP 2009537199 A JP2009537199 A JP 2009537199A JP 2010510215 A5 JP2010510215 A5 JP 2010510215A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- group
- aliphatic
- fluoro
- cancer
- 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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- 150000001875 compounds Chemical class 0.000 claims description 41
- 125000001931 aliphatic group Chemical group 0.000 claims description 24
- -1 N-methylpyrrolidinyl Chemical group 0.000 claims description 13
- 102000003989 Aurora kinases Human genes 0.000 claims description 11
- 108090000433 Aurora kinases Proteins 0.000 claims description 11
- 125000000623 heterocyclic group Chemical group 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 125000001153 fluoro group Chemical group F* 0.000 claims description 7
- 125000002541 furyl group Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000001544 thienyl group Chemical group 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000001404 mediated effect Effects 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 3
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 3
- 125000003944 tolyl group Chemical group 0.000 claims description 3
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 2
- 102000004000 Aurora Kinase A Human genes 0.000 claims description 2
- 108090000461 Aurora Kinase A Proteins 0.000 claims description 2
- 101150065749 Churc1 gene Proteins 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 102100038239 Protein Churchill Human genes 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 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 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- SRFVRJILPIASPG-UHFFFAOYSA-N 4-[[7-(2-fluoro-6-methoxyphenyl)-9-(1-methylpyrrol-2-yl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C=2N(C=CC=2)C)=C1 SRFVRJILPIASPG-UHFFFAOYSA-N 0.000 description 1
- ZLHFILGSQDJULK-UHFFFAOYSA-N 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 ZLHFILGSQDJULK-UHFFFAOYSA-N 0.000 description 1
- NRJOLMQQQLDIPP-UHFFFAOYSA-N 4-[[9-ethynyl-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C#C)=C1 NRJOLMQQQLDIPP-UHFFFAOYSA-N 0.000 description 1
- 101100167062 Caenorhabditis elegans chch-3 gene Proteins 0.000 description 1
- AIUYVPGHBMKGAC-UHFFFAOYSA-M sodium;4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoate Chemical compound [Na+].C1=C(C([O-])=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 AIUYVPGHBMKGAC-UHFFFAOYSA-M 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85934006P | 2006-11-16 | 2006-11-16 | |
| US60/859,340 | 2006-11-16 | ||
| PCT/US2007/023948 WO2008063525A1 (en) | 2006-11-16 | 2007-11-14 | Compounds for inhibiting mitotic progression |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011187930A Division JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010510215A JP2010510215A (ja) | 2010-04-02 |
| JP2010510215A5 true JP2010510215A5 (enExample) | 2011-10-20 |
| JP5102839B2 JP5102839B2 (ja) | 2012-12-19 |
Family
ID=39315133
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009537199A Active JP5102839B2 (ja) | 2006-11-16 | 2007-11-14 | 有糸分裂進行を阻害するための化合物 |
| JP2011187930A Active JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
| JP2013236439A Pending JP2014055166A (ja) | 2006-11-16 | 2013-11-15 | 有糸分裂進行を阻害するための化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011187930A Active JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
| JP2013236439A Pending JP2014055166A (ja) | 2006-11-16 | 2013-11-15 | 有糸分裂進行を阻害するための化合物 |
Country Status (34)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005243175B2 (en) * | 2004-05-14 | 2011-12-01 | Millennium Pharmaceuticals, Inc. | Compounds and methods for inhibiting mitotic progression by inhibition of Aurora kinase |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| JP5684719B2 (ja) * | 2008-12-05 | 2015-03-18 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | Ｐｌｋ阻害剤としての５，７−ジヒドロ−６ｈ−ピリミド［５、−４ｄ］［１］ベンゾアゼピン−６−チオン |
| RU2535032C2 (ru) | 2008-12-22 | 2014-12-10 | Милленниум Фармасьютикалз, Инк. | Сочетание ингибиторов аврора киназы и анти-cd 20 антител |
| JO3635B1 (ar) * | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| JO3434B1 (ar) * | 2009-07-31 | 2019-10-20 | Millennium Pharm Inc | مركبات صيدلانية لمعالجة السرطان وامراض واضطرابات اخري |
| BR112012020557A8 (pt) * | 2010-02-19 | 2018-01-02 | Millennium Pharm Inc | formas cristalinas de 4-{[9-cloro-7-(2-flúor-6-metoifenil)-5h-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoxibenzoato de sódio |
| US20120107304A1 (en) | 2010-04-27 | 2012-05-03 | Boehringer Ingelheim International Gmbh | Combination therapy in treatment of oncological and fibrotic diseases |
| JP5844358B2 (ja) * | 2010-06-22 | 2016-01-13 | グラクソスミスクライン エルエルシー | ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤 |
| AR086656A1 (es) | 2011-06-03 | 2014-01-15 | Millennium Pharm Inc | Combinacion de inhibidores de mek e inhibidores selectivos de la quinasa aurora a |
| US20130303519A1 (en) * | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
| CN103772391A (zh) * | 2012-10-23 | 2014-05-07 | 杨子娇 | 一类治疗房角狭窄的化合物及其用途 |
| WO2014153509A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase |
| EP3076963A4 (en) | 2013-12-06 | 2017-09-13 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd30 antibodies |
| CA2972076A1 (en) * | 2014-12-23 | 2016-06-30 | Millennium Pharmaceuticals, Inc. | Combination of raf inhibitors and aurora kinase inhibitors |
| WO2017015316A1 (en) | 2015-07-21 | 2017-01-26 | Millennium Pharmaceuticals, Inc. | Administration of aurora kinase inhibitor and chemotherapeutic agents |
| EP3347355B1 (en) | 2015-09-09 | 2022-07-13 | Icahn School of Medicine at Mount Sinai | Heterotricyclic sulfonamides as anti-cancer agents |
| CA2997769A1 (en) | 2015-09-09 | 2017-03-16 | Icahn School Of Medicine At Mount Sinai | Heterocyclic constrained tricyclic sulfonamides as anti-cancer agents |
| US11340215B2 (en) | 2016-02-26 | 2022-05-24 | Japanese Foundation For Cancer Research | Screening method of anticancer agent focused on function of HP1 and evaluation system |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| JP6188986B1 (ja) * | 2017-03-23 | 2017-08-30 | 株式会社ノエビア | 時計遺伝子発現量調整剤及びエラスチン産生促進剤 |
| WO2019195658A1 (en) | 2018-04-05 | 2019-10-10 | Dana-Farber Cancer Institute, Inc. | Sting levels as a biomarker for cancer immunotherapy |
| WO2020049208A1 (es) | 2018-09-09 | 2020-03-12 | Fundacio Privada Institut De Recerca De La Sida - Caixa | Aurora cinasa como diana para tratar, prevenir o curar una infección por vih o sida |
| US20220305048A1 (en) | 2019-08-26 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| EP4504710A1 (en) | 2022-04-07 | 2025-02-12 | Eli Lilly and Company | Process for making a kras g12c inhibitor |
| CA3247183A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | TREATMENT METHOD INCLUDING KRAS G12C INHIBITORS AND AURORA A INHIBITORS |
| EP4547251A1 (en) | 2022-06-30 | 2025-05-07 | Eli Lilly and Company | Kras g12c inhibitor for treating cancer |
| CN121941495A (zh) | 2023-10-03 | 2026-04-28 | 武田药品工业株式会社 | 用于治疗小细胞肺癌的阿立塞替和紫杉醇 |
| WO2025245045A1 (en) | 2024-05-21 | 2025-11-27 | The Regents Of The University Of California | Methods of treating lung cancer |
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| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| AU2005243175B2 (en) * | 2004-05-14 | 2011-12-01 | Millennium Pharmaceuticals, Inc. | Compounds and methods for inhibiting mitotic progression by inhibition of Aurora kinase |
| CN101084214A (zh) | 2004-11-17 | 2007-12-05 | 迈卡纳治疗股份有限公司 | 激酶抑制剂 |
| WO2006070198A1 (en) | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| EA200870117A1 (ru) | 2005-12-23 | 2008-12-30 | Смитклайн Бичам Корпорейшн | Азаиндоловые ингибиторы аурора-киназ |
| US7718648B2 (en) | 2006-08-09 | 2010-05-18 | Millennium Pharmaceuticals, Inc. | Pyridobenzazepine compounds and methods for inhibiting mitotic progression |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
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2007
- 2007-11-09 CL CL200703244A patent/CL2007003244A1/es unknown
- 2007-11-14 ES ES12153134.7T patent/ES2537451T3/es active Active
- 2007-11-14 ZA ZA200903279A patent/ZA200903279B/xx unknown
- 2007-11-14 EA EA200970486A patent/EA015779B1/ru unknown
- 2007-11-14 DK DK07867449.6T patent/DK2086981T3/da active
- 2007-11-14 WO PCT/US2007/023948 patent/WO2008063525A1/en not_active Ceased
- 2007-11-14 MX MX2012011398A patent/MX343391B/es unknown
- 2007-11-14 RS RS20150047A patent/RS53788B1/sr unknown
- 2007-11-14 RS RS20120247A patent/RS52313B/sr unknown
- 2007-11-14 PT PT121531313T patent/PT2497772E/pt unknown
- 2007-11-14 EP EP15155821.0A patent/EP2944639B1/en active Active
- 2007-11-14 SI SI200730975T patent/SI2086981T1/sl unknown
- 2007-11-14 CN CN201310367332.9A patent/CN103483343B/zh active Active
- 2007-11-14 SG SG2011080652A patent/SG176443A1/en unknown
- 2007-11-14 PT PT07867449T patent/PT2086981E/pt unknown
- 2007-11-14 KR KR1020097012501A patent/KR101110458B1/ko active Active
- 2007-11-14 JP JP2009537199A patent/JP5102839B2/ja active Active
- 2007-11-14 NZ NZ597252A patent/NZ597252A/xx unknown
- 2007-11-14 EP EP07867449A patent/EP2086981B1/en active Active
- 2007-11-14 DK DK12153131.3T patent/DK2497772T3/en active
- 2007-11-14 ES ES12153131.3T patent/ES2528793T3/es active Active
- 2007-11-14 CN CN2007800423837A patent/CN101547924B/zh active Active
- 2007-11-14 MX MX2009004670A patent/MX2009004670A/es active IP Right Grant
- 2007-11-14 AU AU2007322046A patent/AU2007322046B2/en active Active
- 2007-11-14 MY MYPI20091846A patent/MY153243A/en unknown
- 2007-11-14 CA CA2669680A patent/CA2669680C/en active Active
- 2007-11-14 UA UAA200906211A patent/UA94129C2/ru unknown
- 2007-11-14 PL PL07867449T patent/PL2086981T3/pl unknown
- 2007-11-14 NZ NZ577042A patent/NZ577042A/en unknown
- 2007-11-14 US US11/985,277 patent/US8026246B2/en active Active
- 2007-11-14 MX MX2012011396A patent/MX348568B/es unknown
- 2007-11-14 SG SG10201503350TA patent/SG10201503350TA/en unknown
- 2007-11-14 EP EP12153131.3A patent/EP2497772B1/en active Active
- 2007-11-14 ES ES07867449T patent/ES2384123T3/es active Active
- 2007-11-14 TW TW096143087A patent/TWI401255B/zh active
- 2007-11-14 EP EP12153134.7A patent/EP2497773B1/en active Active
- 2007-11-14 NZ NZ611898A patent/NZ611898A/en not_active IP Right Cessation
- 2007-11-14 SI SI200731591T patent/SI2497772T1/sl unknown
- 2007-11-14 KR KR1020117022355A patent/KR101342014B1/ko active Active
- 2007-11-14 AT AT07867449T patent/ATE556076T1/de active
- 2007-11-14 PL PL12153131T patent/PL2497772T3/pl unknown
- 2007-11-14 GE GEAP200711309A patent/GEP20125459B/en unknown
- 2007-11-14 HR HRP20120490TT patent/HRP20120490T1/hr unknown
- 2007-11-14 BR BRPI0718803A patent/BRPI0718803B8/pt active IP Right Grant
- 2007-11-16 AR ARP070105104A patent/AR064246A1/es unknown
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2009
- 2009-05-08 CR CR10782A patent/CR10782A/es unknown
- 2009-05-11 IL IL198690A patent/IL198690A0/en active IP Right Grant
- 2009-05-13 NO NO20091864A patent/NO343338B1/no unknown
- 2009-06-12 MA MA31985A patent/MA30988B1/fr unknown
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2011
- 2011-08-25 US US13/217,729 patent/US9988384B2/en active Active
- 2011-08-25 US US13/217,659 patent/US20110312942A1/en not_active Abandoned
- 2011-08-30 JP JP2011187930A patent/JP5452811B2/ja active Active
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2012
- 2012-06-06 CY CY20121100518T patent/CY1112828T1/el unknown
- 2012-10-12 PH PH12012502057A patent/PH12012502057B1/en unknown
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2013
- 2013-11-15 JP JP2013236439A patent/JP2014055166A/ja active Pending
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2014
- 2014-04-04 CR CR20140154A patent/CR20140154A/es unknown
- 2014-10-15 US US14/514,687 patent/US9765076B2/en active Active
- 2014-11-27 CR CR20140544A patent/CR20140544A/es unknown
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2015
- 2015-01-13 HR HRP20150047TT patent/HRP20150047T1/hr unknown
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2018
- 2018-06-01 US US15/996,166 patent/US10836766B2/en active Active
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2020
- 2020-11-16 US US17/099,266 patent/US11958855B2/en active Active
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2024
- 2024-03-07 US US18/598,629 patent/US20240400567A1/en active Pending