JP4363985B2 - タンパク質キナーゼ阻害剤として有用なインドリン誘導体 - Google Patents
タンパク質キナーゼ阻害剤として有用なインドリン誘導体 Download PDFInfo
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- JP4363985B2 JP4363985B2 JP2003558005A JP2003558005A JP4363985B2 JP 4363985 B2 JP4363985 B2 JP 4363985B2 JP 2003558005 A JP2003558005 A JP 2003558005A JP 2003558005 A JP2003558005 A JP 2003558005A JP 4363985 B2 JP4363985 B2 JP 4363985B2
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- dimethyl
- pharmaceutically acceptable
- pyrrol
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
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- DBABZHXKTCFAPX-UHFFFAOYSA-N probenecid Chemical compound CCCN(CCC)S(=O)(=O)C1=CC=C(C(O)=O)C=C1 DBABZHXKTCFAPX-UHFFFAOYSA-N 0.000 description 1
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- 235000019260 propionic acid Nutrition 0.000 description 1
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- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
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- 208000037803 restenosis Diseases 0.000 description 1
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- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
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- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
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- QHQATUUBFDYJOC-UHFFFAOYSA-N tert-butyl 4-[3-[2,4-dimethyl-5-[(2-oxo-1h-indol-3-ylidene)methyl]-1h-pyrrol-3-yl]propanoyl]piperazine-1-carboxylate Chemical compound CC=1NC(C=C2C3=CC=CC=C3NC2=O)=C(C)C=1CCC(=O)N1CCN(C(=O)OC(C)(C)C)CC1 QHQATUUBFDYJOC-UHFFFAOYSA-N 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Peptides Or Proteins (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US34381301P | 2001-12-27 | 2001-12-27 | |
| US34374601P | 2001-12-27 | 2001-12-27 | |
| PCT/US2002/041252 WO2003057690A1 (en) | 2001-12-27 | 2002-12-20 | Indolinone derivatives useful as protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005514420A JP2005514420A (ja) | 2005-05-19 |
| JP2005514420A5 JP2005514420A5 (https=) | 2005-12-22 |
| JP4363985B2 true JP4363985B2 (ja) | 2009-11-11 |
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| JP2003558005A Expired - Fee Related JP4363985B2 (ja) | 2001-12-27 | 2002-12-20 | タンパク質キナーゼ阻害剤として有用なインドリン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US6686362B2 (https=) |
| EP (1) | EP1458713B1 (https=) |
| JP (1) | JP4363985B2 (https=) |
| KR (1) | KR100965519B1 (https=) |
| CN (1) | CN1290844C (https=) |
| AT (1) | ATE302771T1 (https=) |
| AU (1) | AU2002360753B2 (https=) |
| BR (1) | BR0215360A (https=) |
| CA (1) | CA2470480C (https=) |
| CO (1) | CO5611126A2 (https=) |
| DE (1) | DE60205776T2 (https=) |
| DK (1) | DK1458713T3 (https=) |
| ES (1) | ES2247411T3 (https=) |
| HU (1) | HUP0500111A3 (https=) |
| IL (1) | IL162203A0 (https=) |
| MX (1) | MXPA04006271A (https=) |
| NO (1) | NO327550B1 (https=) |
| NZ (1) | NZ533219A (https=) |
| PL (1) | PL208283B1 (https=) |
| RU (1) | RU2316554C2 (https=) |
| WO (1) | WO2003057690A1 (https=) |
Families Citing this family (31)
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| JP4588447B2 (ja) * | 2002-08-09 | 2010-12-01 | セラヴァンス， インコーポレーテッド | 過剰増殖および関連疾患に関連するオンコキナーゼ融合ポリペプチド、これをコードする核酸、ならびにこれを検出する方法および同定する方法 |
| JP2007509173A (ja) | 2003-10-24 | 2007-04-12 | シエーリング アクチエンゲゼルシャフト | インドリノン誘導体類及び疾病状態、例えば癌の処理へのそれらの使用 |
| US20050171182A1 (en) * | 2003-12-11 | 2005-08-04 | Roger Briesewitz | Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases |
| SE0401790D0 (sv) * | 2004-07-07 | 2004-07-07 | Forskarpatent I Syd Ab | Tamoxifen response in pre- and postmenopausal breast cancer patients |
| US7825244B2 (en) | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| US20060281788A1 (en) | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor |
| KR101443651B1 (ko) | 2005-10-18 | 2014-09-23 | 얀센 파마슈티카 엔.브이. | Ｆｌｔ-3 키나제의 억제 방법 |
| NZ572073A (en) | 2006-04-20 | 2011-09-30 | Janssen Pharmaceutica Nv | Heterocyclic compounds as inhibitors of c-fms kinase |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| BRPI0710548B8 (pt) | 2006-04-20 | 2021-05-25 | Janssen Pharmaceutica Nv | inibidores de c-fms cinase, composição farmacêutica e forma de dosagem farmacêutica |
| CA2663147A1 (en) * | 2006-09-11 | 2008-03-20 | Curis, Inc. | Substituted 2-indolinone as ptk inhibitors containing a zinc binding moiety |
| JO3240B1 (ar) | 2007-10-17 | 2018-03-08 | Janssen Pharmaceutica Nv | c-fms مثبطات كيناز |
| FR2948940B1 (fr) * | 2009-08-04 | 2011-07-22 | Servier Lab | Nouveaux derives dihydroindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US9109227B2 (en) | 2010-01-05 | 2015-08-18 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | FLT3 receptor antagonists for the treatment or the prevention of pain disorders |
| MX2012008083A (es) | 2010-01-12 | 2012-08-15 | Ab Science | Inhibidores de triazol y oxazol quinaza. |
| IN2015DN00659A (https=) | 2012-08-07 | 2015-06-26 | Janssen Pharmaceutica Nv | |
| JP6290884B2 (ja) | 2012-08-07 | 2018-03-07 | ヤンセン ファーマシューティカ エヌ．ベー． | ｃ−ＦＭＳキナーゼ阻害剤の調製プロセス |
| JP6407504B2 (ja) | 2012-09-21 | 2018-10-17 | アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法 |
| BR112015016282A2 (en) | 2013-01-07 | 2017-07-11 | Arog Pharmaceuticals, Inc. | crenolanib for treatment of mutated flt3 proliferative disorders |
| FR3008411B1 (fr) * | 2013-07-12 | 2015-07-03 | Servier Lab | Nouveau sel de la 3-[(3-{[4-(4-morpholinylmethyl)-1h-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1h-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione, sa preparation, et les formulations qui le contiennent |
| US10463658B2 (en) | 2013-10-25 | 2019-11-05 | Videra Pharmaceuticals, Llc | Method of inhibiting FLT3 kinase |
| CN107001283B (zh) | 2014-07-31 | 2021-05-25 | 国家健康与医学研究院 | Flt3受体拮抗剂 |
| EP3254698A1 (en) | 2016-06-08 | 2017-12-13 | Universite De Montpellier | Flt3 receptor inhibitor at low dosage for the treatment of neuropathic pain |
| US12534764B2 (en) | 2016-11-02 | 2026-01-27 | Arog Pharmaceuticals, Inc. | Crenolanib for treating FLT3 mutated proliferative disorders associated mutations |
| BR112019008762A2 (pt) | 2016-11-02 | 2019-07-16 | Arog Pharmaceuticals, Inc. | método para o tratamento de um distúrbio proliferativo mutado em flt3 |
| WO2018211018A1 (en) | 2017-05-17 | 2018-11-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Flt3 inhibitors for improving pain treatments by opioids |
| WO2019057649A1 (en) | 2017-09-19 | 2019-03-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA |
| WO2022019998A1 (en) | 2020-07-20 | 2022-01-27 | Arog Pharmaceuticals, Inc. | Crystal forms of crenolanib and methods of use thereof |
| WO2022090547A1 (en) | 2020-10-30 | 2022-05-05 | Dsm Ip Assets B.V. | Production of carotenoids by fermentation |
| US11969420B2 (en) | 2020-10-30 | 2024-04-30 | Arog Pharmaceuticals, Inc. | Combination therapy of crenolanib and apoptosis pathway agents for the treatment of proliferative disorders |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MC2096A1 (fr) * | 1989-02-23 | 1991-02-15 | Hoffmann La Roche | Pyrroles substitues |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| EA005032B1 (ru) | 1998-05-29 | 2004-10-28 | Сьюджен, Инк. | Пирролзамещенные 2-индолиноны (варианты), фармацевтическая композиция (варианты), способ модулирования каталитической активности протеинкиназы, способ лечения или профилактики нарушения в организме, связанного с протеинкиназой |
| BR9916327A (pt) * | 1998-12-17 | 2001-09-18 | Hoffmann La Roche | Oxindóis de 4-alquenila (e alquinila) como inibidores de cinases dependentes de ciclina, em particular, cdk2 |
| IL143920A0 (en) | 1998-12-31 | 2002-04-21 | Sugen Inc | 3-heteroarylidenyl-2-indolinone derivatives and pharmaceutical compositions containing the same |
| DE19924401A1 (de) | 1999-05-27 | 2000-11-30 | Boehringer Ingelheim Pharma | Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| CA2381821A1 (en) | 1999-08-27 | 2001-03-08 | Boehringer Ingelheim Pharma Kg | Substituted indolinones, their manufacture and their use as medicaments |
| EP1222187B1 (en) | 1999-10-06 | 2004-09-22 | Boehringer Ingelheim Pharmaceuticals Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
| DE19949209A1 (de) | 1999-10-13 | 2001-04-19 | Boehringer Ingelheim Pharma | In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| UA75054C2 (uk) | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу |
| AU2576501A (en) | 1999-12-08 | 2001-06-18 | Advanced Medicine, Inc. | Protein kinase inhibitors |
| SI1255752T1 (sl) * | 2000-02-15 | 2007-12-31 | Pharmacia & Upjohn Co Llc | S pirolom substituirani zaviralci 2-indolinon protein kinaza |
| JP2004502686A (ja) | 2000-06-30 | 2004-01-29 | スージェン・インコーポレーテッド | ４−ヘテロアリール−３−ヘテロアリーリデニル−２−インドリノンおよび蛋白質キナーゼ阻害剤としてのその使用 |
| AU8544901A (en) | 2000-08-18 | 2002-03-04 | Cor Therapeutics Inc | Quinazoline derivatives as kinase inhibitors |
| EP1349852A2 (en) | 2000-12-20 | 2003-10-08 | Sugen, Inc. | 4-(hetero)aryl substituted indolinones |
| JP4588447B2 (ja) | 2002-08-09 | 2010-12-01 | セラヴァンス， インコーポレーテッド | 過剰増殖および関連疾患に関連するオンコキナーゼ融合ポリペプチド、これをコードする核酸、ならびにこれを検出する方法および同定する方法 |
| US20050171182A1 (en) * | 2003-12-11 | 2005-08-04 | Roger Briesewitz | Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases |
-
2002
- 2002-12-20 AT AT02796035T patent/ATE302771T1/de active
- 2002-12-20 PL PL369602A patent/PL208283B1/pl not_active IP Right Cessation
- 2002-12-20 CA CA2470480A patent/CA2470480C/en not_active Expired - Fee Related
- 2002-12-20 DE DE60205776T patent/DE60205776T2/de not_active Expired - Lifetime
- 2002-12-20 BR BR0215360-2A patent/BR0215360A/pt not_active IP Right Cessation
- 2002-12-20 WO PCT/US2002/041252 patent/WO2003057690A1/en not_active Ceased
- 2002-12-20 HU HU0500111A patent/HUP0500111A3/hu unknown
- 2002-12-20 JP JP2003558005A patent/JP4363985B2/ja not_active Expired - Fee Related
- 2002-12-20 EP EP02796035A patent/EP1458713B1/en not_active Expired - Lifetime
- 2002-12-20 US US10/327,385 patent/US6686362B2/en not_active Expired - Lifetime
- 2002-12-20 IL IL16220302A patent/IL162203A0/xx unknown
- 2002-12-20 DK DK02796035T patent/DK1458713T3/da active
- 2002-12-20 AU AU2002360753A patent/AU2002360753B2/en not_active Ceased
- 2002-12-20 KR KR1020047010148A patent/KR100965519B1/ko not_active Expired - Fee Related
- 2002-12-20 MX MXPA04006271A patent/MXPA04006271A/es active IP Right Grant
- 2002-12-20 NZ NZ533219A patent/NZ533219A/en not_active IP Right Cessation
- 2002-12-20 ES ES02796035T patent/ES2247411T3/es not_active Expired - Lifetime
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- 2002-12-20 RU RU2004122918/04A patent/RU2316554C2/ru not_active IP Right Cessation
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2003
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2004
- 2004-07-08 NO NO20042926A patent/NO327550B1/no not_active IP Right Cessation
- 2004-07-22 CO CO04070253A patent/CO5611126A2/es not_active Application Discontinuation
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2006
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