JP2012526772A5 - - Google Patents
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- Publication number
- JP2012526772A5 JP2012526772A5 JP2012510289A JP2012510289A JP2012526772A5 JP 2012526772 A5 JP2012526772 A5 JP 2012526772A5 JP 2012510289 A JP2012510289 A JP 2012510289A JP 2012510289 A JP2012510289 A JP 2012510289A JP 2012526772 A5 JP2012526772 A5 JP 2012526772A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- cancer
- methyl
- 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.)
- Pending
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 24
- 150000001875 compounds Chemical class 0.000 claims description 20
- 230000002062 proliferating effect Effects 0.000 claims description 20
- 201000010099 disease Diseases 0.000 claims description 18
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims description 13
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims description 13
- 239000003623 enhancer Substances 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 9
- 206010022489 Insulin Resistance Diseases 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 208000020816 lung neoplasm Diseases 0.000 claims description 8
- 102000038030 PI3Ks Human genes 0.000 claims description 6
- 108091007960 PI3Ks Proteins 0.000 claims description 6
- 239000008280 blood Substances 0.000 claims description 6
- 210000004369 blood Anatomy 0.000 claims description 6
- 230000005764 inhibitory process Effects 0.000 claims description 6
- 230000037361 pathway Effects 0.000 claims description 6
- BMMXYEBLEBULND-UHFFFAOYSA-N BGT226 free base Chemical compound C1=NC(OC)=CC=C1C1=CC=C(N=CC2=C3N(C=4C=C(C(N5CCNCC5)=CC=4)C(F)(F)F)C(=O)N2C)C3=C1 BMMXYEBLEBULND-UHFFFAOYSA-N 0.000 claims description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 5
- -1 cyano, imidazolyl Chemical group 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 5
- 239000008103 glucose Substances 0.000 claims description 5
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical class CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims description 5
- NKOHRVBBQISBSB-UHFFFAOYSA-N 5-[(4-hydroxyphenyl)methyl]-1,3-thiazolidine-2,4-dione Chemical compound C1=CC(O)=CC=C1CC1C(=O)NC(=O)S1 NKOHRVBBQISBSB-UHFFFAOYSA-N 0.000 claims description 4
- 108010011376 AMP-Activated Protein Kinases Proteins 0.000 claims description 4
- 102000014156 AMP-Activated Protein Kinases Human genes 0.000 claims description 4
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims description 4
- 229940123208 Biguanide Drugs 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 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
- 206010014733 Endometrial cancer Diseases 0.000 claims description 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 102100026715 Serine/threonine-protein kinase STK11 Human genes 0.000 claims description 4
- 101710181599 Serine/threonine-protein kinase STK11 Proteins 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 230000004777 loss-of-function mutation Effects 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000037841 lung tumor Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- JTSLALYXYSRPGW-UHFFFAOYSA-N n-[5-(4-cyanophenyl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NC(C1=C2)=CNC1=NC=C2C1=CC=C(C#N)C=C1 JTSLALYXYSRPGW-UHFFFAOYSA-N 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 238000006029 Jeger synthesis reaction Methods 0.000 claims description 3
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims description 3
- 230000035945 sensitivity Effects 0.000 claims description 3
- 239000012190 activator Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 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 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 238000000034 method Methods 0.000 description 7
- RWGBXAQMUBGGKQ-UHFFFAOYSA-N 4-(trifluoromethyl)pyridin-2-amine Chemical compound NC1=CC(C(F)(F)F)=CC=N1 RWGBXAQMUBGGKQ-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09160440.5 | 2009-05-15 | ||
| EP09160440 | 2009-05-15 | ||
| PCT/EP2010/056538 WO2010130779A2 (en) | 2009-05-15 | 2010-05-12 | COMBINATION OF A PBOSPBOINOSITKLE 3-KSπASE INHIBITOR AND AN ANTIDIABETIC COMPOUND |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012526772A JP2012526772A (ja) | 2012-11-01 |
| JP2012526772A5 true JP2012526772A5 (enExample) | 2013-06-27 |
Family
ID=40983590
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012510289A Pending JP2012526772A (ja) | 2009-05-15 | 2010-05-12 | ホスホイノシチド３−キナーゼ阻害剤および抗糖尿病性化合物の組合せ剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20120059005A1 (enExample) |
| EP (1) | EP2429516A2 (enExample) |
| JP (1) | JP2012526772A (enExample) |
| KR (1) | KR20120096869A (enExample) |
| CN (1) | CN102958518A (enExample) |
| AU (1) | AU2010247397B2 (enExample) |
| BR (1) | BRPI1010979A2 (enExample) |
| CA (1) | CA2760179A1 (enExample) |
| MX (1) | MX2011012201A (enExample) |
| RU (1) | RU2011150619A (enExample) |
| WO (1) | WO2010130779A2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR081060A1 (es) | 2010-04-15 | 2012-06-06 | Bayer Schering Pharma Ag | Procedimiento para preparar 4-{4-[({[4-cloro-3-(trifluorometil)fenil]amino}carbonil)amino]-3-fluorofenoxi}-n-metilpiridin-2-carboxamida |
| CA2813333C (en) * | 2010-10-01 | 2019-01-15 | Novartis Ag | Manufacturing process for pyrimidine derivatives |
| CN112023054A (zh) * | 2013-04-12 | 2020-12-04 | 内德生物系统有限公司 | 癌症的治疗 |
| JP7187035B2 (ja) | 2016-08-03 | 2022-12-12 | アールイーエムディー バイオセラピューティクス，インコーポレイテッド | 癌を治療するためのグルカゴン受容体アンタゴニストとｐｉ３ｋ経路阻害剤との組み合わせ |
| US12324807B2 (en) | 2018-06-01 | 2025-06-10 | Cornell University | Combination therapy for PI3K-associated disease or disorder |
| CN117281814A (zh) * | 2018-07-23 | 2023-12-26 | 豪夫迈·罗氏有限公司 | 用pi3k抑制剂gdc-0077治疗癌症的方法 |
| TW202027736A (zh) * | 2018-10-08 | 2020-08-01 | 瑞士商赫孚孟拉羅股份公司 | 用PI3Kα抑制劑及二甲雙胍治療癌症之方法 |
| BR112022012280A2 (pt) * | 2019-12-20 | 2022-08-30 | Recurium Ip Holdings Llc | Combinações |
| CN120361228B (zh) * | 2025-04-08 | 2025-11-21 | 复旦大学附属妇产科医院 | 一种葡萄糖激酶激活剂与pi3k抑制剂的组合物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004066929A2 (en) * | 2003-01-24 | 2004-08-12 | Bristol-Myers Squibb Company | Cycloalkyl containing anilide ligands for the thyroid receptor |
| WO2007008200A1 (en) * | 2004-07-09 | 2007-01-18 | Prolx Pharmaceuticals Corp. | Wortmannin analogs and methods of using same in combination with chemotherapeutic agents |
| WO2006069186A2 (en) * | 2004-12-22 | 2006-06-29 | The Ohio State Research Foundation | Small molecule bcl-xl/bcl-2 binding inhibitors |
| GB0510390D0 (en) * | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| TW200824678A (en) * | 2006-08-11 | 2008-06-16 | Combinatorx Inc | Methods and compositions for the treatment of neurodegenerative disorders |
| WO2008076447A2 (en) * | 2006-12-15 | 2008-06-26 | Ordway Research Institute | Treatments of therapy-resistant diseases comprising drug combinations |
| EP2231147A2 (en) * | 2007-12-13 | 2010-09-29 | Novartis AG | Combinations of therapeutic agents for treating cancer |
| WO2009155659A1 (en) * | 2008-06-27 | 2009-12-30 | The University Of Queensland | Combination therapy |
| RU2508110C2 (ru) * | 2008-07-11 | 2014-02-27 | Новартис Аг | КОМБИНАЦИЯ (А) ИНГИБИТОРА ФОСФОИНОЗИТ-3-КИНАЗЫ И (Б) МОДУЛЯТОРА ПУТИ Ras/Raf/Mek |
-
2010
- 2010-05-12 RU RU2011150619/02A patent/RU2011150619A/ru not_active Application Discontinuation
- 2010-05-12 WO PCT/EP2010/056538 patent/WO2010130779A2/en not_active Ceased
- 2010-05-12 MX MX2011012201A patent/MX2011012201A/es not_active Application Discontinuation
- 2010-05-12 JP JP2012510289A patent/JP2012526772A/ja active Pending
- 2010-05-12 KR KR1020117027030A patent/KR20120096869A/ko not_active Withdrawn
- 2010-05-12 AU AU2010247397A patent/AU2010247397B2/en not_active Ceased
- 2010-05-12 BR BRPI1010979A patent/BRPI1010979A2/pt not_active IP Right Cessation
- 2010-05-12 CA CA2760179A patent/CA2760179A1/en not_active Abandoned
- 2010-05-12 US US13/319,536 patent/US20120059005A1/en not_active Abandoned
- 2010-05-12 EP EP10718226A patent/EP2429516A2/en not_active Withdrawn
- 2010-05-12 CN CN2010800199053A patent/CN102958518A/zh active Pending
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