JP2010523669A5 - - Google Patents
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- JP2010523669A5 JP2010523669A5 JP2010503043A JP2010503043A JP2010523669A5 JP 2010523669 A5 JP2010523669 A5 JP 2010523669A5 JP 2010503043 A JP2010503043 A JP 2010503043A JP 2010503043 A JP2010503043 A JP 2010503043A JP 2010523669 A5 JP2010523669 A5 JP 2010523669A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkenyl
- hydrogen
- independently
- alkylene
- 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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- 238000011282 treatment Methods 0.000 claims description 19
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 125000000217 alkyl group Chemical group 0.000 claims 70
- 229910052739 hydrogen Inorganic materials 0.000 claims 64
- 239000001257 hydrogen Substances 0.000 claims 64
- 125000003342 alkenyl group Chemical group 0.000 claims 61
- 150000002431 hydrogen Chemical class 0.000 claims 55
- 125000003545 alkoxy group Chemical group 0.000 claims 24
- 238000000034 method Methods 0.000 claims 22
- 125000001475 halogen functional group Chemical group 0.000 claims 21
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 20
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 20
- 239000002246 antineoplastic agent Substances 0.000 claims 19
- 229940127089 cytotoxic agent Drugs 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000003282 alkyl amino group Chemical group 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 18
- 125000001188 haloalkyl group Chemical group 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 125000004663 dialkyl amino group Chemical group 0.000 claims 16
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 16
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 14
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 13
- 125000004438 haloalkoxy group Chemical group 0.000 claims 13
- -1 hydroxy, cyano, amino Chemical group 0.000 claims 13
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 13
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 12
- 125000004103 aminoalkyl group Chemical group 0.000 claims 12
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 125000004043 oxo group Chemical group O=* 0.000 claims 9
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 7
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 7
- DTXOCJGLLMAFBX-UHFFFAOYSA-N oxo-[[1-[2-[[4-(oxoazaniumylmethylidene)pyridin-1-yl]methoxy]ethoxymethyl]pyridin-4-ylidene]methyl]azanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1COCCOCN1C=CC(=C[NH+]=O)C=C1 DTXOCJGLLMAFBX-UHFFFAOYSA-N 0.000 claims 5
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 5
- 229960002930 sirolimus Drugs 0.000 claims 5
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 3
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 3
- 229930012538 Paclitaxel Natural products 0.000 claims 3
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 3
- 229960004562 carboplatin Drugs 0.000 claims 3
- 229960001433 erlotinib Drugs 0.000 claims 3
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 3
- 238000001794 hormone therapy Methods 0.000 claims 3
- 229960004891 lapatinib Drugs 0.000 claims 3
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 3
- 229960001592 paclitaxel Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 3
- 229960000575 trastuzumab Drugs 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 229940122815 Aromatase inhibitor Drugs 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 229940123237 Taxane Drugs 0.000 claims 2
- 125000005090 alkenylcarbonyl group Chemical group 0.000 claims 2
- 125000003302 alkenyloxy group Chemical group 0.000 claims 2
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 2
- 125000002431 aminoalkoxy group Chemical group 0.000 claims 2
- 239000003886 aromatase inhibitor Substances 0.000 claims 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 2
- 125000000262 haloalkenyl group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical group [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 2
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007279 Carcinoid tumour of the gastrointestinal tract Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical group O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas 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
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 229960002932 anastrozole Drugs 0.000 claims 1
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 229960000255 exemestane Drugs 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 238000009169 immunotherapy Methods 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- XMBWDFGMSWQBCA-RNFDNDRNSA-M iodine-131(1-) Chemical compound [131I-] XMBWDFGMSWQBCA-RNFDNDRNSA-M 0.000 claims 1
- 229960003881 letrozole Drugs 0.000 claims 1
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical group C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 description 2
- 238000000692 Student's t-test Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92316407P | 2007-04-11 | 2007-04-11 | |
| US60/923,164 | 2007-04-11 | ||
| PCT/US2008/004570 WO2008127594A2 (en) | 2007-04-11 | 2008-04-08 | Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013228684A Division JP2014074031A (ja) | 2007-04-11 | 2013-11-01 | Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010523669A JP2010523669A (ja) | 2010-07-15 |
| JP2010523669A5 true JP2010523669A5 (https=) | 2013-05-16 |
| JP5726515B2 JP5726515B2 (ja) | 2015-06-03 |
Family
ID=39864581
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010503043A Active JP5726515B2 (ja) | 2007-04-11 | 2008-04-08 | Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 |
| JP2013228684A Pending JP2014074031A (ja) | 2007-04-11 | 2013-11-01 | Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013228684A Pending JP2014074031A (ja) | 2007-04-11 | 2013-11-01 | Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法 |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US8481001B2 (https=) |
| EP (1) | EP2139483B9 (https=) |
| JP (2) | JP5726515B2 (https=) |
| KR (1) | KR101586774B1 (https=) |
| CN (2) | CN103202842A (https=) |
| AU (1) | AU2008239668B2 (https=) |
| BR (1) | BRPI0810208A2 (https=) |
| CA (1) | CA2684056A1 (https=) |
| CO (1) | CO6140024A2 (https=) |
| CR (1) | CR11099A (https=) |
| CY (1) | CY1114608T1 (https=) |
| DK (1) | DK2139483T3 (https=) |
| EA (1) | EA019064B1 (https=) |
| EC (1) | ECSP099723A (https=) |
| ES (1) | ES2438998T3 (https=) |
| GT (1) | GT200900263A (https=) |
| HR (1) | HRP20131081T1 (https=) |
| IL (1) | IL201211A (https=) |
| MA (1) | MA31335B1 (https=) |
| ME (1) | ME00937B (https=) |
| MX (1) | MX2009010929A (https=) |
| MY (1) | MY150797A (https=) |
| NI (1) | NI200900184A (https=) |
| NZ (1) | NZ580009A (https=) |
| PL (1) | PL2139483T3 (https=) |
| PT (1) | PT2139483E (https=) |
| RS (1) | RS53020B (https=) |
| SI (1) | SI2139483T1 (https=) |
| SV (1) | SV2009003390A (https=) |
| TN (1) | TN2009000399A1 (https=) |
| UA (1) | UA98141C2 (https=) |
| WO (1) | WO2008127594A2 (https=) |
| ZA (1) | ZA200906765B (https=) |
Families Citing this family (28)
| 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 |
| 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 |
| WO2010053182A1 (ja) * | 2008-11-10 | 2010-05-14 | 協和発酵キリン株式会社 | キヌレニン産生抑制剤 |
| DE102009049679A1 (de) | 2009-10-19 | 2011-04-21 | Merck Patent Gmbh | Pyrazolopyrimidinderivate |
| 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 |
| EP2590654B1 (en) | 2010-07-09 | 2016-12-21 | Exelixis, Inc. | Combinations of kinase inhibitors for the treatment of cancer |
| EP2616442B8 (en) | 2010-09-14 | 2018-10-17 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| BR112013009643A2 (pt) | 2010-10-20 | 2016-07-19 | Merck Serono S A Geneva | método para preparar n-(3-amino-quinoxalin-2-il)-sulfonamidas substituídas e seus intermediários n-(3-cloo-quinoxalin-2-il)-sulfonamidas |
| DE102010048800A1 (de) * | 2010-10-20 | 2012-05-10 | Merck Patent Gmbh | Chinoxalinderivate |
| DE102010049595A1 (de) | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
| WO2012065057A2 (en) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors and methods of their use |
| KR20140077911A (ko) * | 2011-09-14 | 2014-06-24 | 엑셀리시스, 인코포레이티드 | 암의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제 |
| JP2014528451A (ja) * | 2011-10-04 | 2014-10-27 | ギリアード カリストガ エルエルシー | Ｐｉ３ｋの新規キノキサリン阻害剤 |
| WO2013056067A1 (en) | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| KR20140096035A (ko) * | 2011-10-28 | 2014-08-04 | 노파르티스 아게 | 위장 기질 종양을 치료하는 방법 |
| 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 |
| WO2013067306A1 (en) * | 2011-11-02 | 2013-05-10 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers |
| CA2860051A1 (en) * | 2011-12-27 | 2013-07-04 | Kadmon Corporation, Llc | Methods for treatment of breast cancer nonresponsive to trastuzumab |
| CN103467482B (zh) | 2012-04-10 | 2017-05-10 | 上海璎黎药业有限公司 | 稠合嘧啶类化合物，其制备方法，中间体，组合物和应用 |
| WO2014028479A1 (en) | 2012-08-13 | 2014-02-20 | Envoy Therapeutics, Inc. | Quinoxaline derivatives as gpr6 modulators |
| US9745321B2 (en) | 2013-09-30 | 2017-08-29 | Shanghai Yingli Pharmaceutical Co., Ltd | Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof |
| NZ718487A (en) | 2013-10-16 | 2020-01-31 | Shanghai Yingli Pharm Co Ltd | Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof |
| JP6526034B2 (ja) | 2014-02-14 | 2019-06-05 | 武田薬品工業株式会社 | Ｇｐｒ６のピリドピラジンモジュレーター |
| US9950194B2 (en) | 2014-09-09 | 2018-04-24 | Mevion Medical Systems, Inc. | Patient positioning system |
| WO2019119206A1 (en) * | 2017-12-18 | 2019-06-27 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| WO2023220131A2 (en) * | 2022-05-10 | 2023-11-16 | Relay Therapeutics, Inc. | PI3Kα INHIBITORS AND METHODS OF USE THEREOF |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004064734A2 (en) * | 2003-01-17 | 2004-08-05 | Threshold Pharmaceuticals, Inc. | Combination therapies for the treatment of cancer |
| AU2006283846B2 (en) * | 2005-08-26 | 2012-04-05 | Merck Serono Sa | Pyrazine derivatives and use as PI3K 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 |
| 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 |
| 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 |
| NZ578229A (en) * | 2007-02-22 | 2012-02-24 | Merck Serono Sa | Quinoxaline compounds and use thereof |
| 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 |
| JP4623164B2 (ja) * | 2008-08-21 | 2011-02-02 | セイコーエプソン株式会社 | プロジェクタ |
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