JP2012504628A5 - - Google Patents
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- Publication number
- 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
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- 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 (https=) | 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 (https=) |
| EP (1) | EP2350070A1 (https=) |
| JP (1) | JP2012504628A (https=) |
| AR (1) | AR073524A1 (https=) |
| PA (1) | PA8843901A1 (https=) |
| TW (1) | TW201018685A (https=) |
| UY (1) | UY32153A (https=) |
| WO (1) | WO2010039740A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0617162B8 (pt) * | 2005-10-07 | 2021-05-25 | Exelixis Inc | compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos |
| CN101395155A (zh) * | 2005-10-07 | 2009-03-25 | 埃克塞里艾克西斯公司 | PI3Kα的吡啶并嘧啶酮抑制剂 |
| CN101528231A (zh) | 2006-08-16 | 2009-09-09 | 埃克塞利希斯股份有限公司 | 在癌症的治疗中使用pi3k和mek调控剂 |
| DK2074122T5 (da) * | 2006-09-15 | 2014-03-17 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer |
| JP2010523670A (ja) * | 2007-04-10 | 2010-07-15 | エクセリクシス， インク． | Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法 |
| EP2142543B8 (en) * | 2007-04-11 | 2013-07-03 | Exelixis, Inc. | Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| EP2616442B8 (en) | 2010-09-14 | 2018-10-17 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
| TW201311683A (zh) * | 2011-04-29 | 2013-03-16 | Exelixis Inc | 使用吡啶并嘧啶酮ｐｉ３ｋ／ｍｔｏｒ抑制劑治療淋巴瘤之方法 |
| CN104302294A (zh) | 2011-11-01 | 2015-01-21 | 埃克塞利希斯股份有限公司 | 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺 |
| US20180214452A1 (en) | 2015-03-06 | 2018-08-02 | Korea Advanced Institute Of Science And Technology | COMPOSITION FOR PREVENTION OR TREATMENT OF INTRACTABLE EPILEPSY COMPRISING mTOR INHIBITOR |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| KR20220047247A (ko) | 2019-06-04 | 2022-04-15 | 아르커스 바이오사이언시즈 인코포레이티드 | 2,3,5-삼치환 피라졸로[1,5-a]피리미딘 화합물 |
| CN114901664B (zh) * | 2020-01-10 | 2024-07-02 | 南京再明医药有限公司 | 吡啶酮化合物及应用 |
| US20230165864A1 (en) * | 2020-04-30 | 2023-06-01 | Guangzhou Joyo Pharmatech Co., Ltd | Application of heterocyclic compound |
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 |
| ES2301194T3 (es) | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| KR20020070520A (ko) | 2000-01-27 | 2002-09-09 | 워너-램버트 캄파니 | 신경퇴행성 질병의 치료를 위한 피리도피리미디논 유도체 |
| PL358271A1 (pl) | 2000-03-06 | 2004-08-09 | Warner-Lambert Company | 5-alkilopirydo[2,3-D]pirymidyny jako inhibitory kinazy tyrozyny |
| CN1186324C (zh) | 2000-04-27 | 2005-01-26 | 山之内制药株式会社 | 稠合杂芳基衍生物 |
| MXPA03007623A (es) | 2001-02-26 | 2003-12-04 | Tanabe Seiyaku Co | Derivado de piridopirimidina o naftiridina. |
| EP1408985A4 (en) * | 2001-06-21 | 2006-03-22 | Ariad Pharma Inc | NEW PYRIDOPYRIMIDONE AND ITS USES |
| US7019002B2 (en) | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| KR20040103972A (ko) | 2002-04-19 | 2004-12-09 | 스미스클라인 비참 코포레이션 | 신규 화합물 |
| AU2003232071A1 (en) | 2002-05-06 | 2003-11-17 | Genelabs Technologies, Inc. | 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 |
| WO2005040337A2 (en) | 2003-05-20 | 2005-05-06 | The Regents Of The University Of California | METHODS FOR BINDING AGENTS TO β-AMYLOID PLAQUES |
| BRPI0507852A (pt) | 2004-02-18 | 2007-07-10 | Warner Lambert Co | 2-(piridin-3-ilamino)-pirido[2,3-d]pirimidin-7-onas |
| ATE373659T1 (de) | 2004-05-04 | 2007-10-15 | Warner Lambert Co | Pyrrolylsubstituierte pyrido(2,3-d)pyrimidin-7- one und derivate davon als therapeutische mittel |
| AU2005316668B2 (en) | 2004-12-13 | 2012-09-06 | Millennium Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
| CN101395155A (zh) * | 2005-10-07 | 2009-03-25 | 埃克塞里艾克西斯公司 | PI3Kα的吡啶并嘧啶酮抑制剂 |
| US8247408B2 (en) * | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| DK2074122T5 (da) * | 2006-09-15 | 2014-03-17 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer |
| CN101711249A (zh) * | 2007-04-11 | 2010-05-19 | 埃克塞里艾克西斯公司 | 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 |
-
2009
- 2009-09-29 WO PCT/US2009/058881 patent/WO2010039740A1/en not_active Ceased
- 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 EP EP09737495A patent/EP2350070A1/en not_active Withdrawn
- 2009-09-29 JP JP2011530150A patent/JP2012504628A/ja active Pending
- 2009-09-29 US US12/569,760 patent/US8101622B2/en not_active Expired - Fee Related
- 2009-09-29 UY UY0001032153A patent/UY32153A/es not_active Application Discontinuation
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