JP2003523389A5 - - Google Patents
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- JP2003523389A5 JP2003523389A5 JP2001561317A JP2001561317A JP2003523389A5 JP 2003523389 A5 JP2003523389 A5 JP 2003523389A5 JP 2001561317 A JP2001561317 A JP 2001561317A JP 2001561317 A JP2001561317 A JP 2001561317A JP 2003523389 A5 JP2003523389 A5 JP 2003523389A5
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- 125000001424 substituent group Chemical group 0.000 description 34
- 239000008194 pharmaceutical composition Substances 0.000 description 30
- 125000003118 aryl group Chemical group 0.000 description 23
- 150000001875 compounds Chemical class 0.000 description 17
- 125000000623 heterocyclic group Chemical group 0.000 description 11
- 206010028980 Neoplasm Diseases 0.000 description 9
- 125000000217 alkyl group Chemical group 0.000 description 9
- 201000011510 cancer Diseases 0.000 description 9
- 229910052736 halogen Inorganic materials 0.000 description 9
- 150000002367 halogens Chemical class 0.000 description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- 229910052757 nitrogen Inorganic materials 0.000 description 8
- 125000003342 alkenyl group Chemical group 0.000 description 5
- 125000000304 alkynyl group Chemical group 0.000 description 5
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 description 4
- 239000004037 angiogenesis inhibitor Substances 0.000 description 4
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- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 3
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- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 3
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- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 3
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
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- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 description 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- IRAUOUBGYSKULF-UHFFFAOYSA-N 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=NC=C2NC(C3=CC4=CC=CC=C4NC3=O)=CC2=C1 IRAUOUBGYSKULF-UHFFFAOYSA-N 0.000 description 1
- FABIXNWMMUTTHQ-UHFFFAOYSA-N 3-(1h-pyrrolo[3,2-b]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=CC=C2NC(C3=CC4=CC=CC=C4NC3=O)=CC2=N1 FABIXNWMMUTTHQ-UHFFFAOYSA-N 0.000 description 1
- VFBIWRXQJRQOHU-UHFFFAOYSA-N 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-quinolin-2-one Chemical compound N1=CC=C2NC(C3=CC4=CC=CC=C4NC3=O)=CC2=C1 VFBIWRXQJRQOHU-UHFFFAOYSA-N 0.000 description 1
- IWHQVGWQVDOGRI-UHFFFAOYSA-N 3-(5-methoxy-1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=CC=C2NC(=O)C(C3=CC=4C=C(N=CC=4N3)OC)=CC2=C1 IWHQVGWQVDOGRI-UHFFFAOYSA-N 0.000 description 1
- MWHFZGLXSQQPEW-UHFFFAOYSA-N 3-(5-methoxy-1h-pyrrolo[3,2-b]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=CC=C2NC(=O)C(C=3NC4=CC=C(N=C4C=3)OC)=CC2=C1 MWHFZGLXSQQPEW-UHFFFAOYSA-N 0.000 description 1
- VJSLZUPGUKJBHM-UHFFFAOYSA-N 3-(5-oxo-1,4-dihydropyrrolo[3,2-b]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=CC=C2NC(=O)C(C=3NC=4C=CC(NC=4C=3)=O)=CC2=C1 VJSLZUPGUKJBHM-UHFFFAOYSA-N 0.000 description 1
- OGGZWELJIMBJTL-UHFFFAOYSA-N 3-(5-oxo-1,6-dihydropyrrolo[2,3-c]pyridin-2-yl)-1h-quinolin-2-one Chemical compound C1=CC=C2NC(=O)C(C3=CC4=CC(NC=C4N3)=O)=CC2=C1 OGGZWELJIMBJTL-UHFFFAOYSA-N 0.000 description 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 description 1
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- 208000026310 Breast neoplasm Diseases 0.000 description 1
- HVXBOLULGPECHP-WAYWQWQTSA-N Combretastatin A4 Chemical compound C1=C(O)C(OC)=CC=C1\C=C/C1=CC(OC)=C(OC)C(OC)=C1 HVXBOLULGPECHP-WAYWQWQTSA-N 0.000 description 1
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- 229940124761 MMP inhibitor Drugs 0.000 description 1
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- 229930012538 Paclitaxel Natural products 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 102000010780 Platelet-Derived Growth Factor Human genes 0.000 description 1
- 108010038512 Platelet-Derived Growth Factor Proteins 0.000 description 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- UIRKNQLZZXALBI-MSVGPLKSSA-N Squalamine Chemical compound C([C@@H]1C[C@H]2O)[C@@H](NCCCNCCCCN)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CC[C@H](C(C)C)OS(O)(=O)=O)[C@@]2(C)CC1 UIRKNQLZZXALBI-MSVGPLKSSA-N 0.000 description 1
- UIRKNQLZZXALBI-UHFFFAOYSA-N Squalamine Natural products OC1CC2CC(NCCCNCCCCN)CCC2(C)C2C1C1CCC(C(C)CCC(C(C)C)OS(O)(=O)=O)C1(C)CC2 UIRKNQLZZXALBI-UHFFFAOYSA-N 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 1
- 206010064930 age-related macular degeneration Diseases 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
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- -1 carboxamide triazole Chemical class 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 229960005537 combretastatin A-4 Drugs 0.000 description 1
- HVXBOLULGPECHP-UHFFFAOYSA-N combretastatin A4 Natural products C1=C(O)C(OC)=CC=C1C=CC1=CC(OC)=C(OC)C(OC)=C1 HVXBOLULGPECHP-UHFFFAOYSA-N 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 229940111134 coxibs Drugs 0.000 description 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 102000006495 integrins Human genes 0.000 description 1
- 108010044426 integrins Proteins 0.000 description 1
- 229940117681 interleukin-12 Drugs 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 206010023841 laryngeal neoplasm Diseases 0.000 description 1
- 210000000867 larynx Anatomy 0.000 description 1
- 201000004962 larynx cancer Diseases 0.000 description 1
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- 208000002780 macular degeneration Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 201000008968 osteosarcoma Diseases 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 229940043138 pentosan polysulfate Drugs 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 229960004622 raloxifene Drugs 0.000 description 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 1
- 201000006845 reticulosarcoma Diseases 0.000 description 1
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- 230000004263 retinal angiogenesis Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 208000007442 rickets Diseases 0.000 description 1
- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
- 229950001248 squalamine Drugs 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 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 description 1
- 229960003433 thalidomide Drugs 0.000 description 1
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical group C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 description 1
- 229960003425 tirofiban Drugs 0.000 description 1
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- 229960000575 trastuzumab Drugs 0.000 description 1
- 208000027930 type IV hypersensitivity disease Diseases 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 description 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18502300P | 2000-02-25 | 2000-02-25 | |
| US60/185,023 | 2000-02-25 | ||
| PCT/US2001/005482 WO2001062251A1 (en) | 2000-02-25 | 2001-02-21 | Tyrosine kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003523389A JP2003523389A (ja) | 2003-08-05 |
| JP2003523389A5 true JP2003523389A5 (https=) | 2008-02-07 |
Family
ID=22679236
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001561317A Withdrawn JP2003523389A (ja) | 2000-02-25 | 2001-02-21 | チロシンキナーゼ阻害薬 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6420382B2 (https=) |
| EP (1) | EP1259235B1 (https=) |
| JP (1) | JP2003523389A (https=) |
| AT (1) | ATE368457T1 (https=) |
| AU (2) | AU2001238575B2 (https=) |
| CA (1) | CA2400875A1 (https=) |
| DE (1) | DE60129672T2 (https=) |
| ES (1) | ES2288928T3 (https=) |
| WO (1) | WO2001062251A1 (https=) |
Families Citing this family (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20010034660A1 (en) * | 2000-02-09 | 2001-10-25 | Heinz Heumann | Goods and services referring by location |
| AU778417B2 (en) * | 2000-02-25 | 2004-12-02 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| EP1313734B1 (en) | 2000-09-01 | 2009-11-11 | Novartis Vaccines and Diagnostics, Inc. | Aza heterocyclic derivatives and their therapeutic use |
| CZ304344B6 (cs) * | 2000-09-11 | 2014-03-19 | Novartis Vaccines & Diagnostics, Inc. | Chinolinonový derivát a jeho použití a farmaceutický prostředek s obsahem tohoto derivátu |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| US20090118139A1 (en) * | 2000-11-07 | 2009-05-07 | Caliper Life Sciences, Inc. | Microfluidic method and system for enzyme inhibition activity screening |
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| ES2266553T3 (es) * | 2001-06-29 | 2007-03-01 | Ab Science | Utilizacion de derivados de la n-fenil-2-pirimidina-amina para tratar las enfermedades inflamatorias. |
| DE60215648T2 (de) | 2001-06-29 | 2007-08-23 | Ab Science | Die verwendung von c-kit hemmer zur behandlung von entzündlichen darmerkrankungen |
| JP2005500041A (ja) * | 2001-06-29 | 2005-01-06 | アブ サイエンス | 強力で選択的かつ非毒性のｃ−ｋｉｔ阻害剤 |
| EP1427379B1 (en) * | 2001-09-20 | 2008-08-13 | AB Science | Use of potent, selective and non toxic c-kit inhibitors for treating interstitial cystitis |
| DE60227701D1 (de) * | 2001-09-20 | 2008-08-28 | Ab Science | Die verwendung von c-kithemmern zur förderung des haarwuchses |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
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| US6822097B1 (en) | 2002-02-07 | 2004-11-23 | Amgen, Inc. | Compounds and methods of uses |
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| US20050256157A1 (en) * | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
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| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| AU2003273675A1 (en) * | 2002-10-09 | 2004-05-04 | Wayne R. Danter | Protein tyrosine kinase inhibitors |
| AU2003290699B2 (en) * | 2002-11-13 | 2009-08-27 | Novartis Vaccines And Diagnostics, Inc. | Methods of treating cancer and related methods |
| AU2004259755A1 (en) * | 2003-07-22 | 2005-02-03 | Janssen Pharmaceutica, N.V. | Quinolinone derivatives as inhibitors of c-fms kinase |
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| CN102225926A (zh) | 2003-11-07 | 2011-10-26 | 诺华疫苗和诊断公司 | 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐 |
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| KR101387985B1 (ko) * | 2005-01-27 | 2014-04-25 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 전이 종양의 치료 |
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| JP5571387B2 (ja) | 2007-01-11 | 2014-08-13 | クリティカル・アウトカム・テクノロジーズ・インコーポレイテッド | 癌の治療のための化合物および方法 |
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| WO2016063122A1 (en) | 2014-10-20 | 2016-04-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for screening a subject for a cancer |
| JP6864953B2 (ja) | 2014-12-09 | 2021-04-28 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | Ａｘｌに対するヒトモノクローナル抗体 |
| 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 |
| US20180201687A1 (en) | 2015-07-07 | 2018-07-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antibodies having specificity to myosin 18a and uses thereof |
| WO2017032867A1 (en) | 2015-08-27 | 2017-03-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting the survival time of patients suffering from a lung cancer |
| WO2017055327A1 (en) | 2015-09-29 | 2017-04-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of endothelial cells in a tissue sample |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5409930A (en) | 1991-05-10 | 1995-04-25 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5578609A (en) | 1994-03-25 | 1996-11-26 | The Dupont Merck Pharmaceutical Company | 2-carbocyclic and 2-heterocyclic quinoline-4-carboxylic acids and salts thereof useful as immunosuppressive agents |
| GB9524104D0 (en) | 1995-11-24 | 1996-01-24 | Smithkline Beecham Spa | Novel compounds |
| CA2254756A1 (en) | 1996-05-20 | 1997-11-27 | Mark Goulet | Antagonists of gonadotropin releasing hormone |
| US6413971B1 (en) | 1996-11-27 | 2002-07-02 | Pfizer Inc | Fused bicyclic pyrimidine derivatives |
| ATE459616T1 (de) | 1998-08-11 | 2010-03-15 | Novartis Ag | Isochinoline derivate mit angiogenesis-hemmender wirkung |
| HRP20020349A2 (en) * | 1999-10-19 | 2004-02-29 | Merck & Co Inc | Tyrosine kinase inhibitors |
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2001
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- 2001-02-21 JP JP2001561317A patent/JP2003523389A/ja not_active Withdrawn
- 2001-02-21 WO PCT/US2001/005482 patent/WO2001062251A1/en not_active Ceased
- 2001-02-21 AT AT01911031T patent/ATE368457T1/de not_active IP Right Cessation
- 2001-02-21 ES ES01911031T patent/ES2288928T3/es not_active Expired - Lifetime
- 2001-02-21 DE DE60129672T patent/DE60129672T2/de not_active Expired - Fee Related
- 2001-02-21 EP EP01911031A patent/EP1259235B1/en not_active Expired - Lifetime
- 2001-02-21 AU AU2001238575A patent/AU2001238575B2/en not_active Ceased
- 2001-02-21 AU AU3857501A patent/AU3857501A/xx active Pending
- 2001-02-21 CA CA002400875A patent/CA2400875A1/en not_active Abandoned
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