JP2015517523A5 - - Google Patents
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- JP2015517523A5 JP2015517523A5 JP2015512735A JP2015512735A JP2015517523A5 JP 2015517523 A5 JP2015517523 A5 JP 2015517523A5 JP 2015512735 A JP2015512735 A JP 2015512735A JP 2015512735 A JP2015512735 A JP 2015512735A JP 2015517523 A5 JP2015517523 A5 JP 2015517523A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- compound
- unsubstituted
- formula
- pharmaceutically acceptable
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 28
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 230000002062 proliferating effect Effects 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 10
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 210000000244 kidney pelvis Anatomy 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 6
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 4
- BPYKTIZUTYGOLE-IFADSCNNSA-N Bilirubin Chemical compound N1C(=O)C(C)=C(C=C)\C1=C\C1=C(C)C(CCC(O)=O)=C(CC2=C(C(C)=C(\C=C/3C(=C(C=C)C(=O)N\3)C)N2)CCC(O)=O)N1 BPYKTIZUTYGOLE-IFADSCNNSA-N 0.000 claims description 4
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 4
- 208000032612 Glial tumor Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims description 4
- 208000034578 Multiple myelomas Diseases 0.000 claims description 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 4
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 4
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 210000000481 breast Anatomy 0.000 claims description 4
- 210000000621 bronchi Anatomy 0.000 claims description 4
- 210000003679 cervix uteri Anatomy 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 4
- CVSVTCORWBXHQV-UHFFFAOYSA-N creatine Chemical compound NC(=[NH2+])N(C)CC([O-])=O CVSVTCORWBXHQV-UHFFFAOYSA-N 0.000 claims description 4
- 210000004696 endometrium Anatomy 0.000 claims description 4
- 210000003238 esophagus Anatomy 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 210000003494 hepatocyte Anatomy 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims description 4
- 210000000867 larynx Anatomy 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 210000004072 lung Anatomy 0.000 claims description 4
- 208000003747 lymphoid leukemia Diseases 0.000 claims description 4
- 210000001672 ovary Anatomy 0.000 claims description 4
- 210000000496 pancreas Anatomy 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 210000002307 prostate Anatomy 0.000 claims description 4
- 210000000664 rectum Anatomy 0.000 claims description 4
- 210000000813 small intestine Anatomy 0.000 claims description 4
- 210000002784 stomach Anatomy 0.000 claims description 4
- 210000001685 thyroid gland Anatomy 0.000 claims description 4
- 239000004382 Amylase Substances 0.000 claims description 2
- 102000013142 Amylases Human genes 0.000 claims description 2
- 108010065511 Amylases Proteins 0.000 claims description 2
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims description 2
- 206010012735 Diarrhoea Diseases 0.000 claims description 2
- 208000010201 Exanthema Diseases 0.000 claims description 2
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 2
- 102000004882 Lipase Human genes 0.000 claims description 2
- 108090001060 Lipase Proteins 0.000 claims description 2
- 239000004367 Lipase Substances 0.000 claims description 2
- 206010027940 Mood altered Diseases 0.000 claims description 2
- 206010028116 Mucosal inflammation Diseases 0.000 claims description 2
- 201000010927 Mucositis Diseases 0.000 claims description 2
- 206010028813 Nausea Diseases 0.000 claims description 2
- 206010029350 Neurotoxicity Diseases 0.000 claims description 2
- 208000003251 Pruritus Diseases 0.000 claims description 2
- 206010044221 Toxic encephalopathy Diseases 0.000 claims description 2
- 235000019418 amylase Nutrition 0.000 claims description 2
- 229960003624 creatine Drugs 0.000 claims description 2
- 239000006046 creatine Substances 0.000 claims description 2
- 201000005884 exanthem Diseases 0.000 claims description 2
- 206010016256 fatigue Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 235000019421 lipase Nutrition 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 230000007510 mood change Effects 0.000 claims description 2
- 230000008693 nausea Effects 0.000 claims description 2
- 230000007135 neurotoxicity Effects 0.000 claims description 2
- 231100000228 neurotoxicity Toxicity 0.000 claims description 2
- 208000004235 neutropenia Diseases 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 206010037844 rash Diseases 0.000 claims description 2
- 210000002966 serum Anatomy 0.000 claims description 2
- 229940124530 sulfonamide Drugs 0.000 claims description 2
- 150000003456 sulfonamides Chemical class 0.000 claims description 2
- 206010043554 thrombocytopenia Diseases 0.000 claims description 2
- 238000011269 treatment regimen Methods 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 206010048832 Colon adenoma Diseases 0.000 claims 1
- 230000004596 appetite loss Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 235000021266 loss of appetite Nutrition 0.000 claims 1
- 208000019017 loss of appetite Diseases 0.000 claims 1
- 208000024051 villous adenoma of colon Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 description 2
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 description 2
- 229960003881 letrozole Drugs 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 210000003800 pharynx Anatomy 0.000 description 2
- 0 CC1/C(/N)=N\C(\*)=C(/c2c(*)c(*)nc(N3CCOCC3)n2)\C(\*)=C(/C)\C1 Chemical compound CC1/C(/N)=N\C(\*)=C(/c2c(*)c(*)nc(N3CCOCC3)n2)\C(\*)=C(/C)\C1 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261647654P | 2012-05-16 | 2012-05-16 | |
| US61/647,654 | 2012-05-16 | ||
| PCT/US2013/040877 WO2013173283A1 (en) | 2012-05-16 | 2013-05-14 | Dosage regimen for a pi-3 kinase inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018003680A Division JP2018108998A (ja) | 2012-05-16 | 2018-01-12 | Ｐｉ−３キナーゼ阻害剤の投与レジメン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015517523A JP2015517523A (ja) | 2015-06-22 |
| JP2015517523A5 true JP2015517523A5 (enExample) | 2016-06-02 |
| JP6381523B2 JP6381523B2 (ja) | 2018-08-29 |
Family
ID=48626588
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512735A Expired - Fee Related JP6381523B2 (ja) | 2012-05-16 | 2013-05-14 | Ｐｉ−３キナーゼ阻害剤の投与レジメン |
| JP2018003680A Pending JP2018108998A (ja) | 2012-05-16 | 2018-01-12 | Ｐｉ−３キナーゼ阻害剤の投与レジメン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018003680A Pending JP2018108998A (ja) | 2012-05-16 | 2018-01-12 | Ｐｉ−３キナーゼ阻害剤の投与レジメン |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US10213432B2 (enExample) |
| EP (1) | EP2849756A1 (enExample) |
| JP (2) | JP6381523B2 (enExample) |
| KR (1) | KR20150009540A (enExample) |
| CN (1) | CN104349779A (enExample) |
| AU (1) | AU2013263043B2 (enExample) |
| BR (1) | BR112014028420A2 (enExample) |
| CA (1) | CA2872526A1 (enExample) |
| CL (1) | CL2014003101A1 (enExample) |
| HK (1) | HK1202435A1 (enExample) |
| IL (1) | IL235567B (enExample) |
| MX (1) | MX360892B (enExample) |
| NZ (1) | NZ700924A (enExample) |
| PH (1) | PH12014502547A1 (enExample) |
| RU (1) | RU2630975C2 (enExample) |
| SG (2) | SG11201406550QA (enExample) |
| TN (1) | TN2014000433A1 (enExample) |
| WO (1) | WO2013173283A1 (enExample) |
| ZA (1) | ZA201407406B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012313888B2 (en) | 2011-09-27 | 2016-03-31 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| KR20150131224A (ko) | 2013-03-14 | 2015-11-24 | 노파르티스 아게 | 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| KR20160095035A (ko) | 2013-12-06 | 2016-08-10 | 노파르티스 아게 | 알파-이소형 선택성 포스파티딜이노시톨 3-키나제 억제제를 위한 투여 요법 |
| WO2016109426A1 (en) * | 2014-12-29 | 2016-07-07 | Verastem, Inc. | Oral dosing regimen of a dual mtor and pi3 inhibitor |
| WO2017009751A1 (en) | 2015-07-15 | 2017-01-19 | Pfizer Inc. | Pyrimidine derivatives |
| KR20180073674A (ko) * | 2015-11-02 | 2018-07-02 | 노파르티스 아게 | 포스파티딜이노시톨 3-키나제 억제제에 대한 투여 요법 |
| WO2018009895A1 (en) * | 2016-07-08 | 2018-01-11 | Autotelic Llc | Methods for trabedersen dosing by auc |
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| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| AU2007228984B2 (en) | 2006-03-22 | 2012-05-03 | Syncore Biotechnology Co., Ltd | Treatment of triple receptor negative breast cancer |
| US8022205B2 (en) | 2006-08-08 | 2011-09-20 | Chugai Seiyaku Kabushiki Kaisha | Pyrimidine derivatives as PI3K inhibitor and use thereof |
| US8222288B2 (en) * | 2006-08-30 | 2012-07-17 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| AU2008213808B2 (en) * | 2007-02-06 | 2011-11-10 | Novartis Ag | PI 3-kinase inhibitors and methods of their use |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| CN101896177A (zh) * | 2007-12-13 | 2010-11-24 | 诺瓦提斯公司 | 用于治疗癌症的治疗剂的组合 |
| WO2009155659A1 (en) * | 2008-06-27 | 2009-12-30 | The University Of Queensland | Combination therapy |
| EP2349984A1 (en) | 2008-10-17 | 2011-08-03 | Merck & Co. | Combination therapy |
-
2013
- 2013-05-14 SG SG11201406550QA patent/SG11201406550QA/en unknown
- 2013-05-14 EP EP13729120.9A patent/EP2849756A1/en not_active Withdrawn
- 2013-05-14 BR BR112014028420A patent/BR112014028420A2/pt not_active Application Discontinuation
- 2013-05-14 CN CN201380025377.6A patent/CN104349779A/zh active Pending
- 2013-05-14 RU RU2014150860A patent/RU2630975C2/ru not_active IP Right Cessation
- 2013-05-14 SG SG10201608469RA patent/SG10201608469RA/en unknown
- 2013-05-14 KR KR1020147031775A patent/KR20150009540A/ko not_active Ceased
- 2013-05-14 CA CA2872526A patent/CA2872526A1/en not_active Abandoned
- 2013-05-14 NZ NZ700924A patent/NZ700924A/en not_active IP Right Cessation
- 2013-05-14 WO PCT/US2013/040877 patent/WO2013173283A1/en not_active Ceased
- 2013-05-14 HK HK15103031.8A patent/HK1202435A1/xx unknown
- 2013-05-14 US US14/400,444 patent/US10213432B2/en active Active
- 2013-05-14 JP JP2015512735A patent/JP6381523B2/ja not_active Expired - Fee Related
- 2013-05-14 MX MX2014013904A patent/MX360892B/es active IP Right Grant
- 2013-05-14 AU AU2013263043A patent/AU2013263043B2/en not_active Ceased
-
2014
- 2014-10-13 ZA ZA2014/07406A patent/ZA201407406B/en unknown
- 2014-10-17 TN TN2014000433A patent/TN2014000433A1/fr unknown
- 2014-11-06 IL IL235567A patent/IL235567B/en not_active IP Right Cessation
- 2014-11-14 PH PH12014502547A patent/PH12014502547A1/en unknown
- 2014-11-14 CL CL2014003101A patent/CL2014003101A1/es unknown
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2018
- 2018-01-12 JP JP2018003680A patent/JP2018108998A/ja active Pending
- 2018-12-21 US US16/230,737 patent/US20190134052A1/en not_active Abandoned
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