JP2014533284A5 - - Google Patents
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- Publication number
- JP2014533284A5 JP2014533284A5 JP2014541388A JP2014541388A JP2014533284A5 JP 2014533284 A5 JP2014533284 A5 JP 2014533284A5 JP 2014541388 A JP2014541388 A JP 2014541388A JP 2014541388 A JP2014541388 A JP 2014541388A JP 2014533284 A5 JP2014533284 A5 JP 2014533284A5
- Authority
- JP
- Japan
- Prior art keywords
- kinase
- inhibitor
- combination according
- rtk
- item
- 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
Links
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims description 88
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims description 88
- 239000003112 inhibitor Substances 0.000 claims description 53
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims description 38
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims description 38
- 229910052757 nitrogen Inorganic materials 0.000 claims description 31
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 125000003118 aryl group Chemical group 0.000 claims description 17
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- 229940098445 PI3 kinase alpha inhibitor Drugs 0.000 claims description 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 16
- 230000007170 pathology Effects 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 230000001225 therapeutic effect Effects 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 238000009472 formulation Methods 0.000 claims description 4
- 239000006186 oral dosage form Substances 0.000 claims description 4
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 229960004891 lapatinib Drugs 0.000 claims description 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 description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 230000003176 fibrotic effect Effects 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 239000002502 liposome Substances 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 230000002195 synergetic effect Effects 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 49
- -1 heterocycloalkyloxy Chemical class 0.000 description 26
- 125000004122 cyclic group Chemical group 0.000 description 18
- 125000005843 halogen group Chemical group 0.000 description 17
- 150000001408 amides Chemical class 0.000 description 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 16
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 15
- 229910019142 PO4 Inorganic materials 0.000 description 15
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 15
- 125000002252 acyl group Chemical group 0.000 description 15
- 125000004423 acyloxy group Chemical group 0.000 description 15
- 125000003342 alkenyl group Chemical group 0.000 description 15
- 125000003545 alkoxy group Chemical group 0.000 description 15
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 15
- 125000003710 aryl alkyl group Chemical group 0.000 description 15
- 239000004202 carbamide Substances 0.000 description 15
- 125000004404 heteroalkyl group Chemical group 0.000 description 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 15
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 15
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 15
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 15
- 239000010452 phosphate Substances 0.000 description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 15
- 125000000304 alkynyl group Chemical group 0.000 description 14
- 238000000338 in vitro Methods 0.000 description 11
- 238000000021 kinase assay Methods 0.000 description 11
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 10
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 8
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 8
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 description 8
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 description 8
- 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 description 8
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 229910052717 sulfur Inorganic materials 0.000 description 6
- 238000000099 in vitro assay Methods 0.000 description 5
- 230000035772 mutation Effects 0.000 description 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 5
- 229940124530 sulfonamide Drugs 0.000 description 5
- 150000003456 sulfonamides Chemical class 0.000 description 5
- 108091007960 PI3Ks Proteins 0.000 description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 239000002773 nucleotide Substances 0.000 description 3
- 125000003729 nucleotide group Chemical group 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 2
- 206010014733 Endometrial cancer Diseases 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 description 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 1
- 239000002118 L01XE12 - Vandetanib Substances 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 150000001413 amino acids Chemical group 0.000 description 1
- 229960000106 biosimilars Drugs 0.000 description 1
- 238000000423 cell based assay Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960001433 erlotinib Drugs 0.000 description 1
- 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 description 1
- 229960002584 gefitinib Drugs 0.000 description 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 description 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229960000575 trastuzumab Drugs 0.000 description 1
- 229960000241 vandetanib Drugs 0.000 description 1
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161558928P | 2011-11-11 | 2011-11-11 | |
| US61/558,928 | 2011-11-11 | ||
| PCT/US2012/064719 WO2013071264A1 (en) | 2011-11-11 | 2012-11-12 | Combination of kinase inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014533284A JP2014533284A (ja) | 2014-12-11 |
| JP2014533284A5 true JP2014533284A5 (enExample) | 2015-12-24 |
| JP6126615B2 JP6126615B2 (ja) | 2017-05-10 |
Family
ID=48290670
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014541388A Active JP6126615B2 (ja) | 2011-11-11 | 2012-11-12 | キナーゼ阻害剤の組み合わせおよびそれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9682141B2 (enExample) |
| EP (1) | EP2776837A4 (enExample) |
| JP (1) | JP6126615B2 (enExample) |
| CN (1) | CN104204804B (enExample) |
| CA (1) | CA2855666A1 (enExample) |
| HK (1) | HK1202333A1 (enExample) |
| WO (1) | WO2013071264A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9737521B2 (en) | 2012-11-08 | 2017-08-22 | Rhizen Pharmaceuticals Sa | Pharmaceutical compositions containing a PDE4 inhibitor and a PI3 delta or dual PI3 delta-gamma kinase inhibitor |
| CN104177346A (zh) * | 2013-05-21 | 2014-12-03 | 苏州科捷生物医药有限公司 | 喹唑啉类化合物及其用途 |
| IN2014DE00554A (enExample) * | 2014-02-27 | 2015-08-28 | Csir | |
| CN103864800A (zh) * | 2014-04-03 | 2014-06-18 | 定陶县友帮化工有限公司 | 6-氯咪唑并[1,2-b]哒嗪的合成方法 |
| JP6377400B2 (ja) * | 2014-05-08 | 2018-08-22 | 株式会社小糸製作所 | 車両用灯具 |
| WO2016004272A1 (en) | 2014-07-02 | 2016-01-07 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| US20160317438A1 (en) * | 2015-04-29 | 2016-11-03 | Psivida Us, Inc. | Injectable sustained release intraocular device |
| BR112017023762A2 (pt) * | 2015-05-05 | 2018-07-31 | Psivida Us, Inc. | formulações de depósito injetáveis |
| WO2016210345A1 (en) * | 2015-06-25 | 2016-12-29 | The California Institute For Biomedical Research | Composition and methods for inhibiting mammalian sterile 20-like kinase 1 |
| CN105085503A (zh) * | 2015-09-20 | 2015-11-25 | 徐敬媛 | 一种治疗呼吸道感染的药物组合物 |
| WO2018013430A2 (en) | 2016-07-12 | 2018-01-18 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus infection |
| CN106483293A (zh) * | 2016-10-13 | 2017-03-08 | 广州华弘生物科技有限公司 | He4a 临床免疫检测试剂盒及其制备方法 |
| CN106632351A (zh) * | 2016-11-18 | 2017-05-10 | 山东友帮生化科技有限公司 | 6‑溴咪唑并[1,2‑a]吡嗪‑3‑羧酸乙酯的制法 |
| CA2992067C (en) * | 2017-01-17 | 2023-07-04 | Oxiscience Llc | Composition for the prevention and elimination of odors |
| US11337965B2 (en) | 2017-08-25 | 2022-05-24 | Memorial Sloan Kettering Cancer Center | Kinase mutation-associated neurodegenerative disorders |
| US12324807B2 (en) | 2018-06-01 | 2025-06-10 | Cornell University | Combination therapy for PI3K-associated disease or disorder |
| CA3105174A1 (en) * | 2018-06-27 | 2020-01-02 | Reborna Biosciences, Inc. | Prophylactic or therapeutic agent for spinal muscular atrophy |
| MA53921A (fr) | 2018-10-17 | 2022-01-26 | Array Biopharma Inc | Inhibiteurs de protéine tyrosine phosphatase |
| EP3883935A4 (en) | 2018-11-20 | 2022-08-10 | Georgetown University | COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEURODEGENERATIVE, MYODEGENERATIVE AND LYSOSOMA STORAGE DISEASES |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| JP7650243B2 (ja) * | 2019-04-26 | 2025-03-24 | ユニバーシティー オブ ヒューストン システム | 上皮組織の慢性炎症性傷害、化生、異形成、及びがんを治療するための方法ならびに組成物 |
| CN110051859B (zh) * | 2019-06-06 | 2020-06-12 | 鲁南制药集团股份有限公司 | 一种阿昔替尼环糊精包合物 |
| CN111187181B (zh) * | 2019-11-22 | 2023-05-05 | 吉林大学 | 一种2-(4-氨基苯基)-2-甲基丙腈化合物的制备方法 |
| US20240350492A1 (en) | 2020-07-10 | 2024-10-24 | Ting Therapeutics Llc | Methods for the Prevention and Treatment of Hearing Loss |
| US12398156B2 (en) * | 2020-08-21 | 2025-08-26 | 1ST Biotherapeutics, Inc. | Compounds for prevention or treatment of neurodegenerative disorders |
| WO2022056392A1 (en) | 2020-09-14 | 2022-03-17 | EyePoint Pharmaceuticals, Inc. | Bioerodible ocular drug delivery insert and therapeutic method |
| AU2023216951A1 (en) * | 2022-02-08 | 2024-08-15 | Lawrence Livermore National Security, Llc | Compounds having a t-structure formed by at least four cycles for use in the treatment of cancer and other indications |
| WO2024008799A1 (en) * | 2022-07-06 | 2024-01-11 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of proliferative glomerulonephritis |
| TWI866545B (zh) * | 2022-10-20 | 2024-12-11 | 南韓商東亞Ｓｔ股份有限公司 | 氮雜環丁烷基苯并唑化合物及其等作為mer及axl抑制劑的用途 |
| CN116425743B (zh) * | 2022-12-30 | 2025-06-17 | 贵州医科大学 | 一种作为PI3Kα激酶抑制剂的苯并杂环类化合物及其制备方法与应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0607537A2 (pt) * | 2005-04-12 | 2009-09-15 | Elan Pharma Int Ltd | formulações de derivado de quinazolina nanoparticulado |
| MX2008013583A (es) | 2006-04-26 | 2008-10-31 | Genentech Inc | Compuestos del inhibidor de fosfoinositido 3-cinasa y composiciones farmaceuticas que los contienen. |
| UA100979C2 (ru) * | 2007-04-10 | 2013-02-25 | Экселиксис, Инк. | Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака |
| CA2699202C (en) * | 2007-09-12 | 2016-09-27 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| EP2311842A3 (en) | 2008-06-24 | 2011-07-13 | Takeda Pharmaceutical Company Limited | PI3K/M TOR inhibitors |
| GEP201706639B (en) | 2009-08-17 | 2017-03-27 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| US8623604B2 (en) | 2009-09-09 | 2014-01-07 | Quintiles Transnational Corp. | Methods for predicting responsiveness of a cancer cell to an anti-IGFR1 antibody by analysis of mutations in PIK3CA |
-
2012
- 2012-11-12 EP EP12847622.3A patent/EP2776837A4/en not_active Withdrawn
- 2012-11-12 US US14/357,732 patent/US9682141B2/en not_active Expired - Fee Related
- 2012-11-12 CN CN201280066886.9A patent/CN104204804B/zh not_active Expired - Fee Related
- 2012-11-12 WO PCT/US2012/064719 patent/WO2013071264A1/en not_active Ceased
- 2012-11-12 CA CA2855666A patent/CA2855666A1/en not_active Abandoned
- 2012-11-12 JP JP2014541388A patent/JP6126615B2/ja active Active
- 2012-11-12 HK HK15102758.1A patent/HK1202333A1/xx unknown
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