JP2010500352A5 - - Google Patents
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- JP2010500352A5 JP2010500352A5 JP2009523802A JP2009523802A JP2010500352A5 JP 2010500352 A5 JP2010500352 A5 JP 2010500352A5 JP 2009523802 A JP2009523802 A JP 2009523802A JP 2009523802 A JP2009523802 A JP 2009523802A JP 2010500352 A5 JP2010500352 A5 JP 2010500352A5
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- JP
- Japan
- Prior art keywords
- ring
- aliphatic
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- independently
- optionally substituted
- Prior art date
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- 125000001931 aliphatic group Chemical group 0.000 claims description 157
- 150000001875 compounds Chemical class 0.000 claims description 135
- 229910052739 hydrogen Inorganic materials 0.000 claims description 102
- 239000001257 hydrogen Substances 0.000 claims description 102
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 70
- 125000000623 heterocyclic group Chemical group 0.000 claims description 66
- 125000001475 halogen functional group Chemical group 0.000 claims description 64
- 125000001424 substituent group Chemical group 0.000 claims description 57
- 229910052799 carbon Inorganic materials 0.000 claims description 52
- 125000004432 carbon atom Chemical group C* 0.000 claims description 50
- 125000001072 heteroaryl group Chemical group 0.000 claims description 49
- 125000002947 alkylene group Chemical group 0.000 claims description 46
- 125000003118 aryl group Chemical group 0.000 claims description 33
- 229910052757 nitrogen Inorganic materials 0.000 claims description 33
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- 150000002431 hydrogen Chemical class 0.000 claims description 24
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 23
- 125000003107 substituted aryl group Chemical group 0.000 claims description 20
- 125000002723 alicyclic group Chemical group 0.000 claims description 16
- 229910052717 sulfur Inorganic materials 0.000 claims description 14
- -1 pyridino Chemical group 0.000 claims description 13
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 11
- 102000003989 Aurora kinases Human genes 0.000 claims description 10
- 108090000433 Aurora kinases Proteins 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 125000000217 alkyl group Chemical group 0.000 claims description 7
- 125000002619 bicyclic group Chemical group 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 125000005605 benzo group Chemical group 0.000 claims description 6
- 125000002883 imidazolyl group Chemical group 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000002950 monocyclic group Chemical group 0.000 claims description 6
- 125000002971 oxazolyl group Chemical group 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
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 125000002393 azetidinyl group Chemical group 0.000 claims description 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-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
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 125000002837 carbocyclic group Chemical group 0.000 claims description 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 2
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 125000005956 isoquinolyl group Chemical group 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000005545 phthalimidyl group Chemical group 0.000 claims description 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 2
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000005493 quinolyl group Chemical group 0.000 claims description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000005505 thiomorpholino group Chemical group 0.000 claims description 2
- 125000004306 triazinyl group Chemical group 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 16
- 239000000203 mixture Substances 0.000 claims 7
- 230000015572 biosynthetic process Effects 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 150000007824 aliphatic compounds Chemical class 0.000 claims 1
- 239000005441 aurora Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 CC(C)C(NC1CCNCC1)=* Chemical compound CC(C)C(NC1CCNCC1)=* 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- 229940123877 Aurora kinase inhibitor Drugs 0.000 description 1
- 239000003719 aurora kinase inhibitor Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83660506P | 2006-08-09 | 2006-08-09 | |
| PCT/US2007/017432 WO2008021038A2 (en) | 2006-08-09 | 2007-08-06 | Pyridobenzazepine compounds and methods for inhibiting mitotic progression |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010500352A JP2010500352A (ja) | 2010-01-07 |
| JP2010500352A5 true JP2010500352A5 (https=) | 2010-09-09 |
Family
ID=39082539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009523802A Pending JP2010500352A (ja) | 2006-08-09 | 2007-08-06 | 有糸分裂の進行を阻止するためのピリドベンゾアゼピン化合物および方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US7718648B2 (https=) |
| EP (1) | EP2054413A2 (https=) |
| JP (1) | JP2010500352A (https=) |
| WO (1) | WO2008021038A2 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2692440A1 (en) * | 2006-07-20 | 2008-01-24 | Cascade Therapeutics Inc. | Tetrahydro-5h-pyrido[2,3-d]azepines as 5-ht2c ligands |
| 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. |
| RU2535032C2 (ru) * | 2008-12-22 | 2014-12-10 | Милленниум Фармасьютикалз, Инк. | Сочетание ингибиторов аврора киназы и анти-cd 20 антител |
| CN102482292B (zh) * | 2009-04-23 | 2017-07-18 | Abbvie 公司 | 5‑ht受体的调节剂和其使用方法 |
| US8518933B2 (en) * | 2009-04-23 | 2013-08-27 | Abbvie Inc. | Modulators of 5-HT receptors and methods of use thereof |
| US8546377B2 (en) * | 2009-04-23 | 2013-10-01 | Abbvie Inc. | Modulators of 5-HT receptors and methods of use thereof |
| 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 |
| CA2788774A1 (en) | 2010-02-19 | 2011-08-25 | Millennium Pharmaceuticals, Inc. | Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoate |
| 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 |
| US20150087687A1 (en) | 2012-03-23 | 2015-03-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| 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 |
| JP2018524292A (ja) | 2015-07-21 | 2018-08-30 | 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． | オーロラキナーゼインヒビターと化学療法剤の投与 |
| US11874276B2 (en) | 2018-04-05 | 2024-01-16 | Dana-Farber Cancer Institute, Inc. | STING levels as a biomarker for cancer immunotherapy |
| US20220305048A1 (en) | 2019-08-26 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| PY2062546A (es) | 2019-10-09 | 2021-09-13 | Biocryst Pharm Inc | Inhibidores del factor d del complemento para administración oral |
| WO2022104206A1 (en) * | 2020-11-13 | 2022-05-19 | Neuron23, Inc. | Kinase modulators and methods of use thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4099012A (en) | 1975-08-28 | 1978-07-04 | Ciba-Geigy Corporation | 2-pyrazolyl-benzophenones |
| US4481142A (en) | 1979-02-07 | 1984-11-06 | Hoffmann-La Roche Inc. | Pyrimido-2-benzazepines |
| CA1138863A (en) | 1979-02-07 | 1983-01-04 | Norman W. Gilman | Benzazepine-derivatives |
| US4469633A (en) | 1980-05-16 | 1984-09-04 | Hoffmann-La Roche Inc. | N-oxides of 5-oxo-1-phenyl-2-benzazepines |
| EP0273697A3 (en) | 1986-12-30 | 1989-11-29 | Merck & Co. Inc. | 2-benzazepines with 5- and 6- membered heterocyclic rings |
| US5166151A (en) | 1988-03-25 | 1992-11-24 | Merck & Co., Inc. | 2-Benzazepines with 5- and 6-membered heterocyclic rings, compositions and medical methods of use thereof |
| US5210082A (en) | 1991-05-16 | 1993-05-11 | Merck & Co., Inc. | 2-benzazepines with 5- and 6-membered heterocyclic rings to treat pain and anxiety disorders |
| US6057329A (en) | 1996-12-23 | 2000-05-02 | Celltech Therapeutics Limited | Fused polycyclic 2-aminopyrimidine derivatives |
| US6277844B1 (en) | 1998-09-14 | 2001-08-21 | Sydney Spector | Compound for selective treatment of malignant cells by inhibiting cell cycle progression, decreasing Bcl2, and increasing apoptosis |
| US6417207B1 (en) | 1999-05-12 | 2002-07-09 | Nitromed, Inc. | Nitrosated and nitrosylated potassium channel activators, compositions and methods of use |
| NZ526472A (en) * | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| JP4364637B2 (ja) | 2001-08-09 | 2009-11-18 | アクテリオン ファーマシューティカルズ リミテッド | 新規なベンゾ縮合へテロ環化合物 |
| 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 |
| ES2540987T3 (es) * | 2004-05-14 | 2015-07-15 | Millennium Pharmaceuticals, Inc. | Métodos para preparar inhibidores de la aurora cinasa |
| US20100160324A1 (en) * | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
-
2007
- 2007-08-06 US US11/890,406 patent/US7718648B2/en active Active
- 2007-08-06 JP JP2009523802A patent/JP2010500352A/ja active Pending
- 2007-08-06 EP EP07836533A patent/EP2054413A2/en not_active Withdrawn
- 2007-08-06 WO PCT/US2007/017432 patent/WO2008021038A2/en not_active Ceased
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