JP2010536887A5 - - Google Patents
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- Publication number
- JP2010536887A5 JP2010536887A5 JP2010522149A JP2010522149A JP2010536887A5 JP 2010536887 A5 JP2010536887 A5 JP 2010536887A5 JP 2010522149 A JP2010522149 A JP 2010522149A JP 2010522149 A JP2010522149 A JP 2010522149A JP 2010536887 A5 JP2010536887 A5 JP 2010536887A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- group
- aryl
- substituted
- 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
- 125000003118 aryl group Chemical group 0.000 claims 40
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 229910005965 SO 2 Inorganic materials 0.000 claims 18
- -1 substituted Chemical class 0.000 claims 15
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000004953 trihalomethyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 150000002829 nitrogen Chemical class 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 1
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 1
- RHIUXJQWJOLZLD-UHFFFAOYSA-N Cc1cc(nccc2I)c2[s]1 Chemical compound Cc1cc(nccc2I)c2[s]1 RHIUXJQWJOLZLD-UHFFFAOYSA-N 0.000 description 1
- ZDNFKEBLQJTNAY-UHFFFAOYSA-N Cc1cc2nccc(C)c2[s]1 Chemical compound Cc1cc2nccc(C)c2[s]1 ZDNFKEBLQJTNAY-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US96867307P | 2007-08-29 | 2007-08-29 | |
| US60/968,673 | 2007-08-29 | ||
| PCT/CA2008/001538 WO2009026717A1 (en) | 2007-08-29 | 2008-08-28 | Inhibitors of protein tyrosine kinase activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010536887A JP2010536887A (ja) | 2010-12-02 |
| JP2010536887A5 true JP2010536887A5 (enExample) | 2011-10-13 |
| JP5656634B2 JP5656634B2 (ja) | 2015-01-21 |
Family
ID=40386626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010522149A Active JP5656634B2 (ja) | 2007-08-29 | 2008-08-28 | タンパク質チロシンキナーゼ活性の阻害剤 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8404846B2 (enExample) |
| EP (1) | EP2183254B1 (enExample) |
| JP (1) | JP5656634B2 (enExample) |
| KR (1) | KR101556269B1 (enExample) |
| CN (3) | CN109970759A (enExample) |
| AR (1) | AR068066A1 (enExample) |
| AU (1) | AU2008293038B2 (enExample) |
| BR (1) | BRPI0816064B8 (enExample) |
| CA (1) | CA2697795C (enExample) |
| DK (1) | DK2183254T3 (enExample) |
| ES (1) | ES2635131T3 (enExample) |
| IL (1) | IL204192A (enExample) |
| MX (1) | MX2010002427A (enExample) |
| MY (1) | MY156536A (enExample) |
| PL (1) | PL2183254T3 (enExample) |
| RU (1) | RU2495044C2 (enExample) |
| TW (1) | TWI571468B (enExample) |
| WO (1) | WO2009026717A1 (enExample) |
| ZA (1) | ZA201001512B (enExample) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ588355A (en) * | 2008-03-05 | 2012-03-30 | Methylgene Inc | Inhibitors of protein tyrosine kinase activity |
| AU2009303602B2 (en) | 2008-10-14 | 2012-06-14 | Sunshine Lake Pharma Co., Ltd. | Compounds and methods of use |
| KR20110133048A (ko) * | 2009-03-21 | 2011-12-09 | 닝 시 | 아미노 에스테르 유도체, 그의 염 및 이용 방법 |
| US9340555B2 (en) | 2009-09-03 | 2016-05-17 | Allergan, Inc. | Compounds as tyrosine kinase modulators |
| MX2012002591A (es) * | 2009-09-03 | 2012-04-02 | Allergan Inc | Compuestos como moduladores de tirosina cinasas. |
| CN103025740B (zh) * | 2010-04-16 | 2015-07-01 | 梅特希尔基因公司 | 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途 |
| GB201007203D0 (en) | 2010-04-29 | 2010-06-16 | Glaxo Group Ltd | Novel compounds |
| EP2588107A1 (en) | 2010-07-01 | 2013-05-08 | Takeda Pharmaceutical Company Limited | COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET |
| JP2013537918A (ja) * | 2010-09-27 | 2013-10-07 | エクセリクシス， インク． | 去勢抵抗性前立腺癌および骨芽細胞骨転移の治療のためのｍｅｔおよびｖｅｇｆの二元阻害薬 |
| WO2012044574A1 (en) * | 2010-09-27 | 2012-04-05 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases |
| PL2621481T5 (pl) * | 2010-09-27 | 2023-03-13 | Exelixis, Inc. | Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości |
| GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
| CN102827186A (zh) * | 2011-06-16 | 2012-12-19 | 中国科学院上海药物研究所 | 一类吡啶并五元杂环衍生物及其制备方法和用途 |
| AU2012310168B2 (en) | 2011-09-15 | 2015-07-16 | Novartis Ag | 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| CN103626761B (zh) * | 2012-08-24 | 2015-07-29 | 上海医药工业研究院 | 苯并吡啶氮杂卓类化合物及其作为抗肿瘤药物的应用 |
| GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
| GB201314452D0 (en) | 2013-08-13 | 2013-09-25 | Ostara Biomedical Ltd | Embryo implantation |
| TWI672141B (zh) | 2014-02-20 | 2019-09-21 | 美商醫科泰生技 | 投予ｒｏｓ１突變癌細胞之分子 |
| CN107207471B (zh) | 2014-12-02 | 2020-06-26 | 伊尼塔公司 | 用于治疗神经母细胞瘤的组合 |
| ES2764299T3 (es) | 2014-12-09 | 2020-06-02 | Inst Nat Sante Rech Med | Anticuerpos monoclonales humanos contra AXL |
| GB201501302D0 (en) | 2015-01-27 | 2015-03-11 | Ostara Biomedical Ltd | Embryo implantation |
| WO2016135041A1 (en) | 2015-02-26 | 2016-09-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Fusion proteins and antibodies comprising thereof for promoting apoptosis |
| GB201517523D0 (en) | 2015-10-05 | 2015-11-18 | Ostara Biomedical Ltd | Methods and compositions for managing reproduction |
| JP7061068B2 (ja) | 2015-12-18 | 2022-04-27 | イグナイタ インコーポレイテッド | 癌治療のための併用薬 |
| CN108530464B (zh) * | 2017-03-02 | 2020-10-27 | 深圳海王医药科技研究院有限公司 | 一种多靶点激酶抑制剂 |
| CN121401264A (zh) | 2017-07-19 | 2026-01-27 | 伊尼塔公司 | 包括恩曲替尼的药物组合物 |
| US10180422B1 (en) | 2017-08-22 | 2019-01-15 | Scripps Health | Methods of treating a neuroendocrine tumor |
| WO2019077506A1 (en) | 2017-10-17 | 2019-04-25 | Ignyta, Inc. | PHARMACEUTICAL COMPOSITIONS AND SOLID GALENIC FORMS |
| AU2019237715B2 (en) * | 2018-03-08 | 2021-01-28 | Wellmarker Bio Co., Ltd. | Thienopyridine derivatives and pharmaceutical composition comprising same |
| BR112020023746A2 (pt) | 2018-05-23 | 2021-02-17 | Beigene, Ltd. | anticorpo, composição farmacêutica, método para tratar câncer, ácido nucleico isolado, vetor, célula hospedeira, processo para a produção de um anticorpo e reagente de diagnóstico |
| CN109384799B (zh) * | 2018-11-12 | 2020-07-14 | 深圳海王医药科技研究院有限公司 | 一种多靶点激酶抑制剂化合物的晶型a及制备方法和含有其的药物组合物 |
| JP2022554042A (ja) | 2019-09-06 | 2022-12-28 | ウェルマーカー・バイオ・カンパニー・リミテッド | バイオマーカー型治療用組成物 |
| WO2021050580A1 (en) * | 2019-09-10 | 2021-03-18 | Mirati Therapeutics, Inc. | Crystalline form of a multi-tyrosine kinase inhibitor, method of preparation, and use thereof |
| EP4061421A4 (en) * | 2019-11-21 | 2024-05-15 | BeiGene, Ltd. | Treatment of cancer with anti-ox40 antibodies and multi-kinase inhibitors |
| CN114945576B (zh) * | 2020-01-07 | 2023-10-13 | 南京明德新药研发有限公司 | 氘代噻吩并吡啶类化合物 |
| WO2022060831A1 (en) | 2020-09-17 | 2022-03-24 | Mirati Therapeutics, Inc. | Combination therapies |
| TW202302597A (zh) * | 2021-03-10 | 2023-01-16 | 美商米拉蒂醫療公司 | 多重酪胺酸激酶抑制劑之結晶鹽、其製備方法及用途 |
| WO2022240802A1 (en) | 2021-05-10 | 2022-11-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of sitravatinib salts and processes for preparation thereof |
| TW202342426A (zh) * | 2022-02-15 | 2023-11-01 | 大陸商百濟神州（蘇州）生物科技有限公司 | N-[(6-溴吡啶-3-基)甲基]-2-甲氧基乙烷-1-胺鹽及其製備方法 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7019A (en) * | 1850-01-15 | Improvement in obstetrical supporters | ||
| US7000A (en) * | 1850-01-08 | Smut-machine | ||
| WO1997017329A1 (en) | 1995-11-07 | 1997-05-15 | Kirin Beer Kabushiki Kaisha | Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same |
| ATE419239T1 (de) | 2000-10-20 | 2009-01-15 | Eisai R&D Man Co Ltd | Verfahren zur herstellung von 4-phenoxy chinolin derivaten |
| AU2002255284B2 (en) | 2001-04-27 | 2007-10-04 | Kyowa Kirin Co., Ltd. | Quinoline derivative having azolyl group and quinazoline derivative |
| EP2088141A3 (en) | 2001-06-22 | 2009-11-18 | Kirin Pharma Kabushiki Kaisha | Quinoline derivatives and quinazoline derivatives capable of inhibiting autophosphorylation of hepatocyte growth factor receptors, and pharmaceutical composition comprising the same |
| AU2002360489A1 (en) * | 2001-12-07 | 2003-06-23 | The Regents Of The University Of California | Treatment for age-related macular degeneration |
| UA77303C2 (en) * | 2002-06-14 | 2006-11-15 | Pfizer | Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use |
| CL2003002287A1 (es) * | 2002-11-25 | 2005-01-14 | Wyeth Corp | COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS |
| EP2392565B1 (en) | 2003-09-26 | 2014-03-19 | Exelixis, Inc. | c-Met modulators and methods of use |
| AU2005217325B2 (en) | 2004-02-27 | 2007-11-29 | Eisai R & D Management Co., Ltd. | Novel pyridine derivative and pyrimidine derivative (1) |
| US7767689B2 (en) * | 2004-03-15 | 2010-08-03 | Ptc Therapeutics, Inc. | Carboline derivatives useful in the treatment of cancer |
| EP1732543B1 (en) * | 2004-03-15 | 2017-05-10 | PTC Therapeutics, Inc. | Tetracyclic carboline deratives for inhibiting angiogenesis |
| US7173031B2 (en) | 2004-06-28 | 2007-02-06 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| ES2438017T3 (es) * | 2004-07-30 | 2014-01-15 | Methylgene Inc. | Inhibidores de la señalización del receptor del VEGF y del receptor del HGF |
| AU2006229343A1 (en) * | 2005-03-28 | 2006-10-05 | Kirin Pharma Kabushiki Kaisha | Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency |
| JO2787B1 (en) * | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
| DK1904504T3 (da) | 2005-05-20 | 2014-06-23 | Methylgene Inc | Inhibitorer af vegf-receptor- og hgf-receptorsignalering |
| NZ564283A (en) * | 2005-05-20 | 2011-07-29 | Methylgene Inc | Inhibitors of VEGF receptor and HGF receptor signaling |
| TW200740820A (en) * | 2005-07-05 | 2007-11-01 | Takeda Pharmaceuticals Co | Fused heterocyclic derivatives and use thereof |
| TWI377198B (en) | 2005-08-24 | 2012-11-21 | Eisai R&D Man Co Ltd | Novel pyridine derivatives and pyrimidine derivatives (3) |
| EP1989211A2 (en) | 2006-01-30 | 2008-11-12 | Array Biopharma, Inc. | Heterobicyclic thiophene compounds for the treatment of cancer |
| CA2645137A1 (en) | 2006-03-07 | 2007-09-13 | James F. Blake | Heterobicyclic pyrazole compounds and methods of use |
| WO2007107005A1 (en) * | 2006-03-22 | 2007-09-27 | Methylgene, Inc. | Inhibitors of protein tyrosine kinase activity |
| CA2655128A1 (en) | 2006-06-08 | 2007-12-21 | Array Biopharma Inc. | Quinoline compounds and methods of use |
| WO2008049855A2 (en) | 2006-10-27 | 2008-05-02 | Glaxo Group Limited | 7-azaindole derivatives as c-met kinase inhibitors |
| CN103025740B (zh) * | 2010-04-16 | 2015-07-01 | 梅特希尔基因公司 | 蛋白酪氨酸激酶活性的抑制剂及其治疗眼科疾病的用途 |
-
2008
- 2008-08-28 ES ES08800252.2T patent/ES2635131T3/es active Active
- 2008-08-28 BR BRPI0816064A patent/BRPI0816064B8/pt active IP Right Grant
- 2008-08-28 DK DK08800252.2T patent/DK2183254T3/en active
- 2008-08-28 PL PL08800252T patent/PL2183254T3/pl unknown
- 2008-08-28 KR KR1020107006866A patent/KR101556269B1/ko active Active
- 2008-08-28 JP JP2010522149A patent/JP5656634B2/ja active Active
- 2008-08-28 AU AU2008293038A patent/AU2008293038B2/en active Active
- 2008-08-28 WO PCT/CA2008/001538 patent/WO2009026717A1/en not_active Ceased
- 2008-08-28 MX MX2010002427A patent/MX2010002427A/es active IP Right Grant
- 2008-08-28 CN CN201910332646.2A patent/CN109970759A/zh active Pending
- 2008-08-28 CN CN201610143388.XA patent/CN105777776B/zh active Active
- 2008-08-28 CA CA2697795A patent/CA2697795C/en active Active
- 2008-08-28 MY MYPI2010000797A patent/MY156536A/en unknown
- 2008-08-28 RU RU2010111729/04A patent/RU2495044C2/ru active
- 2008-08-28 CN CN2008801139404A patent/CN101932586A/zh active Pending
- 2008-08-28 EP EP08800252.2A patent/EP2183254B1/en active Active
- 2008-08-29 US US12/200,939 patent/US8404846B2/en active Active
- 2008-08-29 AR ARP080103775A patent/AR068066A1/es active IP Right Grant
- 2008-08-29 TW TW097133329A patent/TWI571468B/zh active
-
2010
- 2010-02-25 IL IL204192A patent/IL204192A/en active IP Right Grant
- 2010-03-02 ZA ZA2010/01512A patent/ZA201001512B/en unknown
-
2011
- 2011-12-30 US US13/341,604 patent/US8389541B2/en active Active
-
2013
- 2013-02-14 US US13/767,506 patent/US8846927B2/en active Active
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