JP2012504628A5 - - Google Patents
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- JP2012504628A5 JP2012504628A5 JP2011530150A JP2011530150A JP2012504628A5 JP 2012504628 A5 JP2012504628 A5 JP 2012504628A5 JP 2011530150 A JP2011530150 A JP 2011530150A JP 2011530150 A JP2011530150 A JP 2011530150A JP 2012504628 A5 JP2012504628 A5 JP 2012504628A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- compound
- optionally
- formula
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 45
- 150000003839 salts Chemical class 0.000 claims description 32
- 239000000203 mixture Substances 0.000 claims description 23
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 201000011510 cancer Diseases 0.000 claims description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 239000003085 diluting agent Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 8
- 239000003937 drug carrier Substances 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010014733 Endometrial cancer Diseases 0.000 claims description 6
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 6
- 206010033128 Ovarian cancer Diseases 0.000 claims description 6
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 208000005017 glioblastoma Diseases 0.000 claims description 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 206010038038 rectal cancer Diseases 0.000 claims description 6
- 201000001275 rectum cancer Diseases 0.000 claims description 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 6
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- SVFIZNZDTQAIQG-UHFFFAOYSA-N 2-amino-6-(6-aminopyridin-3-yl)-4-methyl-8-(oxan-4-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2C=NC(N)=CC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOCC1 SVFIZNZDTQAIQG-UHFFFAOYSA-N 0.000 claims description 2
- PPDYHMXJTNTNFD-LLVKDONJSA-N 2-amino-6-(6-aminopyridin-3-yl)-4-methyl-8-[(3r)-oxolan-3-yl]pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2C=NC(N)=CC=2)=CC=2C(C)=NC(N)=NC=2N1[C@@H]1CCOC1 PPDYHMXJTNTNFD-LLVKDONJSA-N 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 0 Cc1nc(N*)nc(N2[C@]3COCC3)c1C=C(c1cnc(*)cc1)C2=O Chemical compound Cc1nc(N*)nc(N2[C@]3COCC3)c1C=C(c1cnc(*)cc1)C2=O 0.000 description 1
- 230000002152 alkylating effect Effects 0.000 description 1
- 210000003679 cervix uteri Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19476108P | 2008-09-30 | 2008-09-30 | |
| US61/194,761 | 2008-09-30 | ||
| PCT/US2009/058881 WO2010039740A1 (en) | 2008-09-30 | 2009-09-29 | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα AND MTOR |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012504628A JP2012504628A (ja) | 2012-02-23 |
| JP2012504628A5 true JP2012504628A5 (enExample) | 2012-11-15 |
Family
ID=41572575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011530150A Pending JP2012504628A (ja) | 2008-09-30 | 2009-09-29 | ＰＩ３ＫαおよびｍＴＯＲのピリドピリミジノン阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8101622B2 (enExample) |
| EP (1) | EP2350070A1 (enExample) |
| JP (1) | JP2012504628A (enExample) |
| AR (1) | AR073524A1 (enExample) |
| PA (1) | PA8843901A1 (enExample) |
| TW (1) | TW201018685A (enExample) |
| UY (1) | UY32153A (enExample) |
| WO (1) | WO2010039740A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2513165T3 (es) * | 2005-10-07 | 2014-10-24 | Exelixis, Inc. | Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa |
| US8044062B2 (en) * | 2005-10-07 | 2011-10-25 | Exelixis, Inc. | Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha |
| JP2010500994A (ja) | 2006-08-16 | 2010-01-14 | エグゼリクシス， インコーポレイテッド | Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法 |
| GEP20115306B (enExample) | 2006-09-15 | 2011-10-10 | Pfizer Prod Inc | |
| UA100979C2 (ru) * | 2007-04-10 | 2013-02-25 | Экселиксис, Инк. | Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака |
| CA2683784A1 (en) * | 2007-04-11 | 2008-10-23 | Exelixis, Inc. | Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| AR080151A1 (es) * | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| TWI642670B (zh) | 2010-09-14 | 2018-12-01 | 伊塞利克斯公司 | Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法 |
| JP6130305B2 (ja) | 2011-02-23 | 2017-05-17 | インテリカイン， エルエルシー | キナーゼ阻害剤の組み合わせおよびそれらの使用 |
| EP2701690A1 (en) * | 2011-04-29 | 2014-03-05 | Exelixis, Inc. | Method of treating lymphoma using pyridopyrimidinone inhibitors of pi3k/mtor |
| PE20141794A1 (es) | 2011-11-01 | 2014-12-17 | Exelixis Inc | N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-quinasa para el tratamiento de neoplasias linfoproliferativas |
| EP3828269B1 (en) | 2015-03-06 | 2023-05-03 | Korea Advanced Institute Of Science And Technology | Composition for prevention or treatment of intractable epilepsy comprising mtor inhibitor |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| AU2020288610A1 (en) | 2019-06-04 | 2022-01-27 | Arcus Biosciences, Inc. | 2,3,5-trisubstituted pyrazolo[1,5-a]pyrimidine compounds |
| WO2021139775A1 (zh) * | 2020-01-10 | 2021-07-15 | 江苏先声药业有限公司 | 吡啶酮化合物及应用 |
| WO2021219101A1 (zh) * | 2020-04-30 | 2021-11-04 | 广州嘉越医药科技有限公司 | 一种含杂环的化合物的应用 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL117923A (en) | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| DE69839338T2 (de) | 1997-02-05 | 2008-07-10 | Warner-Lambert Company Llc | Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation |
| CN1433417A (zh) | 2000-01-27 | 2003-07-30 | 沃尼尔·朗伯公司 | 用于治疗神经变性疾病的吡啶并嘧啶酮衍生物 |
| YU66502A (sh) | 2000-03-06 | 2005-09-19 | Warner-Lambert Company | 5-alkilpirido(2,3-d)pirimidini, inhibitori tirozinkinaza |
| CN100345830C (zh) | 2000-04-27 | 2007-10-31 | 安斯泰来制药有限公司 | 稠合杂芳基衍生物 |
| JP4166991B2 (ja) | 2001-02-26 | 2008-10-15 | 田辺三菱製薬株式会社 | ピリドピリミジンまたはナフチリジン誘導体 |
| US20030100572A1 (en) * | 2001-06-21 | 2003-05-29 | Ariad Pharmaceuticals,Inc. | Novel pyridopyrimidones and uses thereof |
| US7019002B2 (en) | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| MXPA04010267A (es) | 2002-04-19 | 2005-02-03 | Smithkline Beecham Corp | Compuestos novedosos. |
| US20040063658A1 (en) | 2002-05-06 | 2004-04-01 | Roberts Christopher Don | Nucleoside derivatives for treating hepatitis C virus infection |
| JP2004083587A (ja) | 2002-08-06 | 2004-03-18 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| WO2004063195A1 (en) | 2003-01-03 | 2004-07-29 | Sloan-Kettering Institute For Cancer Research | Pyridopyrimidine kinase inhibitors |
| WO2004089930A1 (en) | 2003-04-02 | 2004-10-21 | Imclone Systems Incorporated | 4-fluoroquinolone derivatives and their use as kinase inhibitors |
| JP2007504283A (ja) | 2003-05-20 | 2007-03-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | β−アミロイド斑に作用物質を結合させる方法 |
| JP2007523151A (ja) | 2004-02-18 | 2007-08-16 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | ２−（ピリジン−３−イルアミノ）−ピリド［２，３−ｄ］ピリミジン−７−オン |
| BRPI0510560A (pt) * | 2004-05-04 | 2007-11-20 | Warner Lambert Co | pirido[2,3-d] pirimidin-7-onas pirrolil substituìdas e seus derivados como agentes terapêuticos |
| EP1828186A1 (en) | 2004-12-13 | 2007-09-05 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| US8044062B2 (en) * | 2005-10-07 | 2011-10-25 | Exelixis, Inc. | Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha |
| GEP20115306B (enExample) * | 2006-09-15 | 2011-10-10 | Pfizer Prod Inc | |
| NZ579945A (en) * | 2007-04-11 | 2012-05-25 | Exelixis Inc | Pyrido [2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
-
2009
- 2009-09-29 AR ARP090103759A patent/AR073524A1/es not_active Application Discontinuation
- 2009-09-29 PA PA20098843901A patent/PA8843901A1/es unknown
- 2009-09-29 TW TW098133017A patent/TW201018685A/zh unknown
- 2009-09-29 US US12/569,760 patent/US8101622B2/en not_active Expired - Fee Related
- 2009-09-29 JP JP2011530150A patent/JP2012504628A/ja active Pending
- 2009-09-29 WO PCT/US2009/058881 patent/WO2010039740A1/en not_active Ceased
- 2009-09-29 EP EP09737495A patent/EP2350070A1/en not_active Withdrawn
- 2009-09-29 UY UY0001032153A patent/UY32153A/es not_active Application Discontinuation
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