JP2005519908A5 - - Google Patents
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- Publication number
- JP2005519908A5 JP2005519908A5 JP2003562099A JP2003562099A JP2005519908A5 JP 2005519908 A5 JP2005519908 A5 JP 2005519908A5 JP 2003562099 A JP2003562099 A JP 2003562099A JP 2003562099 A JP2003562099 A JP 2003562099A JP 2005519908 A5 JP2005519908 A5 JP 2005519908A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- methyl
- formula
- pharmaceutically acceptable
- acceptable salt
- 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
- 150000001875 compounds Chemical class 0.000 claims 34
- 150000003839 salts Chemical class 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- 125000004430 oxygen atom Chemical group O* 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- -1 pyrrolidino, piperidyl Chemical group 0.000 claims 6
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 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 5
- 241001465754 Metazoa Species 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- HWZPPDMBLZOREF-UHFFFAOYSA-N n-[4-(hydroxymethyl)-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]-4-[(4-methylpiperazin-1-yl)methyl]benzamide Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(CO)=CC=2)C=C1 HWZPPDMBLZOREF-UHFFFAOYSA-N 0.000 claims 1
- PIHXYGAKULHFPS-UHFFFAOYSA-N n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]-4-[(3-oxopiperazin-1-yl)methyl]benzamide Chemical compound C1=C(NC=2N=C(C=CN=2)C=2C=NC=CC=2)C(C)=CC=C1NC(=O)C(C=C1)=CC=C1CN1CCNC(=O)C1 PIHXYGAKULHFPS-UHFFFAOYSA-N 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0201508.9A GB0201508D0 (en) | 2002-01-23 | 2002-01-23 | Organic compounds |
| PCT/EP2003/000613 WO2003062220A1 (en) | 2002-01-23 | 2003-01-22 | N-oxyde of n-phenyl-2-pyrimidine-amine derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008208640A Division JP5027076B2 (ja) | 2002-01-23 | 2008-08-13 | N−フェニル−2−ピリミジン−アミン誘導体のn−オキシド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005519908A JP2005519908A (ja) | 2005-07-07 |
| JP2005519908A5 true JP2005519908A5 (enExample) | 2005-12-22 |
| JP4213595B2 JP4213595B2 (ja) | 2009-01-21 |
Family
ID=9929594
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003562099A Expired - Fee Related JP4213595B2 (ja) | 2002-01-23 | 2003-01-22 | N−フェニル−2−ピリミジン−アミン誘導体のn−オキシド |
| JP2008208640A Expired - Fee Related JP5027076B2 (ja) | 2002-01-23 | 2008-08-13 | N−フェニル−2−ピリミジン−アミン誘導体のn−オキシド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008208640A Expired - Fee Related JP5027076B2 (ja) | 2002-01-23 | 2008-08-13 | N−フェニル−2−ピリミジン−アミン誘導体のn−オキシド |
Country Status (15)
| Country | Link |
|---|---|
| US (5) | US7557105B2 (enExample) |
| EP (3) | EP2194049B1 (enExample) |
| JP (2) | JP4213595B2 (enExample) |
| KR (2) | KR100778163B1 (enExample) |
| CN (2) | CN100467461C (enExample) |
| AT (1) | ATE380807T1 (enExample) |
| BR (1) | BR0307058A (enExample) |
| CA (1) | CA2474104C (enExample) |
| DE (1) | DE60318013T2 (enExample) |
| ES (2) | ES2294293T3 (enExample) |
| GB (1) | GB0201508D0 (enExample) |
| IL (2) | IL162979A (enExample) |
| MX (1) | MXPA04007130A (enExample) |
| PT (2) | PT2194049E (enExample) |
| WO (1) | WO2003062220A1 (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60126997T2 (de) * | 2000-10-20 | 2007-10-25 | Eisai R&D Management Co., Ltd. | Stickstoff-enthaltende aromatische ringverbindungen zur behandlung von tumorerkrankungen |
| GB0201508D0 (en) * | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| WO2004110452A1 (en) * | 2003-06-13 | 2004-12-23 | Novartis Ag | 2-aminopyrimidine derivatives as raf kinase inhibitors |
| US8969379B2 (en) * | 2004-09-17 | 2015-03-03 | Eisai R&D Management Co., Ltd. | Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7=methoxy-6-quinolinecarboxide |
| GB0512091D0 (en) * | 2005-06-14 | 2005-07-20 | Novartis Ag | Organic compounds |
| JP5066446B2 (ja) * | 2005-08-01 | 2012-11-07 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質の効果を予測する方法 |
| JP4989476B2 (ja) | 2005-08-02 | 2012-08-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質の効果を検定する方法 |
| WO2007052849A1 (ja) * | 2005-11-07 | 2007-05-10 | Eisai R & D Management Co., Ltd. | 血管新生阻害物質とc-kitキナーゼ阻害物質との併用 |
| GEP20105074B (en) * | 2005-12-21 | 2010-09-10 | Novartis Ag | Pyrimidinyl aryl urea derivatives being fgf inhibitors |
| JP5190361B2 (ja) * | 2006-05-18 | 2013-04-24 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 甲状腺癌に対する抗腫瘍剤 |
| EP2068835A2 (en) * | 2006-09-01 | 2009-06-17 | Teva Pharmaceutical Industries Ltd. | Imatinib compositions |
| KR20090061055A (ko) * | 2006-10-26 | 2009-06-15 | 시코르, 인크. | 결정질 및 비결정질 이매티닙 염기, 이매티닙 메실레이트 및 이들의 제조 방법 |
| EP1988089A1 (en) * | 2006-10-26 | 2008-11-05 | Sicor, Inc. | Imatinib base, and imatinib mesylate and processes for preparation thereof |
| CN101225085B (zh) * | 2007-01-17 | 2011-09-21 | 天津天士力集团有限公司 | 苯基呋咱氮类一氧化氮供体型2-苯胺嘧啶衍生物、其制备方法、含有该化合物的组合物及其用途 |
| WO2008093855A1 (ja) | 2007-01-29 | 2008-08-07 | Eisai R & D Management Co., Ltd. | 未分化型胃癌治療用組成物 |
| CN101245061B (zh) * | 2007-02-13 | 2012-09-19 | 天津天士力集团有限公司 | N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺类一氧化氮供体型衍生物,制备方法及其用途 |
| US7550591B2 (en) | 2007-05-02 | 2009-06-23 | Chemagis Ltd. | Imatinib production process |
| TWI433677B (zh) * | 2007-06-04 | 2014-04-11 | Avila Therapeutics Inc | 雜環化合物及其用途 |
| EP2166860B1 (en) | 2007-06-07 | 2016-09-21 | Intra-Cellular Therapies, Inc. | Novel heterocycle compounds and uses thereof |
| US8367686B2 (en) | 2007-06-07 | 2013-02-05 | Intra-Cellular Therapies, Inc. | Heterocycle compounds and uses thereof |
| EP2081556A1 (en) * | 2007-09-25 | 2009-07-29 | Teva Pharmaceutical Industries Ltd. | Stable imatinib compositions |
| EP2218712B1 (en) * | 2007-11-09 | 2015-07-01 | Eisai R&D Management Co., Ltd. | Combination of anti-angiogenic substance and anti-tumor platinum complex |
| JP5399926B2 (ja) * | 2008-01-29 | 2014-01-29 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管阻害物質とタキサンとの併用 |
| JP2011515685A (ja) * | 2008-03-26 | 2011-05-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 基質結合ビーズを長期間保存する方法 |
| CN101417995B (zh) * | 2008-11-21 | 2012-06-06 | 陈依军 | 苯氧基嘧啶衍生物及其制备方法和用途 |
| WO2011021597A1 (ja) | 2009-08-19 | 2011-02-24 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | キノリン誘導体含有医薬組成物 |
| BR112012032462A2 (pt) | 2010-06-25 | 2016-11-08 | Eisai R&D Man Co Ltd | agente antitumoral empregando compostos que, em combinação, têm efeito inibidor de quinase. |
| US8962650B2 (en) | 2011-04-18 | 2015-02-24 | Eisai R&D Management Co., Ltd. | Therapeutic agent for tumor |
| ES2705950T3 (es) | 2011-06-03 | 2019-03-27 | Eisai R&D Man Co Ltd | Biomarcadores para predecir y valorar la capacidad de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib |
| CN104755463A (zh) | 2012-12-21 | 2015-07-01 | 卫材R&D管理有限公司 | 非晶态形式的喹啉衍生物及其生产方法 |
| JP6411379B2 (ja) | 2013-05-14 | 2018-10-24 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | レンバチニブ化合物に対する子宮内膜がん対象の応答性を予測及び評価するためのバイオマーカー |
| CN103588754B (zh) * | 2013-11-04 | 2015-05-27 | 遵义医学院 | 伊马替尼的制备方法 |
| DK3524595T3 (da) | 2014-08-28 | 2022-09-19 | Eisai R&D Man Co Ltd | Quinolinderivat af høj renhed og fremgangsmåde til fremstilling deraf |
| DK3263106T3 (da) | 2015-02-25 | 2024-01-08 | Eisai R&D Man Co Ltd | Fremgangsmåde til undertrykkelse af bitterhed af quinolinderivat |
| WO2016140717A1 (en) | 2015-03-04 | 2016-09-09 | Merck Sharp & Dohme Corp. | Combination of a pd-1 antagonist and a vegfr/fgfr/ret tyrosine kinase inhibitor for treating cancer |
| US11369623B2 (en) | 2015-06-16 | 2022-06-28 | Prism Pharma Co., Ltd. | Anticancer combination of a CBP/catenin inhibitor and an immune checkpoint inhibitor |
| MX381976B (es) | 2015-08-20 | 2025-03-13 | Eisai R&D Man Co Ltd | Agente terapéutico contra tumores. |
| WO2018147275A1 (ja) | 2017-02-08 | 2018-08-16 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 腫瘍治療用医薬組成物 |
| CA3061888A1 (en) | 2017-05-16 | 2018-11-22 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
| CN107573322A (zh) * | 2017-09-06 | 2018-01-12 | 南京优科生物医药研究有限公司 | 伊马替尼双氮氧化物、其制备方法和用途 |
| CN109761970B (zh) * | 2019-01-26 | 2020-06-09 | 中国药科大学 | 一种蛋白靶向降解嵌合分子、制备方法及应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4607041A (en) * | 1983-04-27 | 1986-08-19 | Fisons Plc | Antihypertensive 2-phenyl Hantzsch dihydropyridines |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (enExample) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| DE4444288A1 (de) * | 1994-12-13 | 1996-06-20 | Rainer Dr Med Etzel | Verwendung von Weihrauch zur Behandlung der Alzheimer-Krankheit |
| NZ302926A (en) * | 1995-02-28 | 1998-10-28 | Hoechst Marion Roussel Inc | Composition for use as antihistamines comprising piperidinoalkanol derivatives and inert ingredients |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| ITMI992711A1 (it) * | 1999-12-27 | 2001-06-27 | Novartis Ag | Composti organici |
| GB0022438D0 (en) * | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| GB0201508D0 (en) * | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| US7279576B2 (en) * | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
-
2002
- 2002-01-23 GB GBGB0201508.9A patent/GB0201508D0/en not_active Ceased
-
2003
- 2003-01-22 CN CNB038027089A patent/CN100467461C/zh not_active Expired - Fee Related
- 2003-01-22 PT PT101504421T patent/PT2194049E/pt unknown
- 2003-01-22 CA CA2474104A patent/CA2474104C/en not_active Expired - Fee Related
- 2003-01-22 AT AT03731700T patent/ATE380807T1/de active
- 2003-01-22 ES ES03731700T patent/ES2294293T3/es not_active Expired - Lifetime
- 2003-01-22 MX MXPA04007130A patent/MXPA04007130A/es active IP Right Grant
- 2003-01-22 PT PT03731700T patent/PT1470120E/pt unknown
- 2003-01-22 WO PCT/EP2003/000613 patent/WO2003062220A1/en not_active Ceased
- 2003-01-22 EP EP10150442.1A patent/EP2194049B1/en not_active Expired - Lifetime
- 2003-01-22 EP EP07101787A patent/EP1783126A3/en not_active Withdrawn
- 2003-01-22 ES ES10150442.1T patent/ES2503734T3/es not_active Expired - Lifetime
- 2003-01-22 BR BR0307058-1A patent/BR0307058A/pt not_active IP Right Cessation
- 2003-01-22 JP JP2003562099A patent/JP4213595B2/ja not_active Expired - Fee Related
- 2003-01-22 KR KR1020047011382A patent/KR100778163B1/ko not_active Expired - Fee Related
- 2003-01-22 DE DE60318013T patent/DE60318013T2/de not_active Expired - Lifetime
- 2003-01-22 EP EP03731700A patent/EP1470120B1/en not_active Expired - Lifetime
- 2003-01-22 US US10/502,291 patent/US7557105B2/en not_active Expired - Fee Related
- 2003-01-22 KR KR1020077011065A patent/KR20070058019A/ko not_active Withdrawn
- 2003-01-22 CN CNA200910002666XA patent/CN101468984A/zh active Pending
-
2004
- 2004-07-12 IL IL162979A patent/IL162979A/en unknown
-
2008
- 2008-08-13 JP JP2008208640A patent/JP5027076B2/ja not_active Expired - Fee Related
-
2009
- 2009-06-04 US US12/478,082 patent/US20090239879A1/en not_active Abandoned
-
2010
- 2010-05-17 US US12/781,430 patent/US20100222362A1/en not_active Abandoned
- 2010-10-03 IL IL208399A patent/IL208399A/en unknown
-
2011
- 2011-07-05 US US13/176,289 patent/US20110294820A1/en not_active Abandoned
-
2014
- 2014-07-14 US US14/330,404 patent/US20140323494A1/en not_active Abandoned
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