JP5937087B2 - ジヒドロプテリジノン及びその中間体を製造する方法 - Google Patents
ジヒドロプテリジノン及びその中間体を製造する方法 Download PDFInfo
- Publication number
- JP5937087B2 JP5937087B2 JP2013533178A JP2013533178A JP5937087B2 JP 5937087 B2 JP5937087 B2 JP 5937087B2 JP 2013533178 A JP2013533178 A JP 2013533178A JP 2013533178 A JP2013533178 A JP 2013533178A JP 5937087 B2 JP5937087 B2 JP 5937087B2
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound represented
- defined above
- alkyl
- cycloalkyl
- 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.)
- Active
Links
- 0 *N1CCNCC1 Chemical compound *N1CCNCC1 0.000 description 2
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
- C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
- C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
- C07D295/033—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic 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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10187194 | 2010-10-12 | ||
| EP10187194.5 | 2010-10-12 | ||
| PCT/EP2011/067696 WO2012049153A1 (en) | 2010-10-12 | 2011-10-11 | Process for manufacturing dihydropteridinones and intermediates thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013539771A JP2013539771A (ja) | 2013-10-28 |
| JP2013539771A5 JP2013539771A5 (https=) | 2014-12-04 |
| JP5937087B2 true JP5937087B2 (ja) | 2016-06-22 |
Family
ID=43902841
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013533178A Active JP5937087B2 (ja) | 2010-10-12 | 2011-10-11 | ジヒドロプテリジノン及びその中間体を製造する方法 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8546566B2 (https=) |
| EP (1) | EP2627656B1 (https=) |
| JP (1) | JP5937087B2 (https=) |
| KR (1) | KR20140005877A (https=) |
| CN (1) | CN103168040A (https=) |
| AU (1) | AU2011315552B2 (https=) |
| BR (1) | BR112013008883A2 (https=) |
| CA (1) | CA2813838A1 (https=) |
| CL (1) | CL2013000730A1 (https=) |
| DK (1) | DK2627656T3 (https=) |
| EA (1) | EA024256B1 (https=) |
| ES (1) | ES2509741T3 (https=) |
| IL (1) | IL224602A (https=) |
| MX (1) | MX2013003994A (https=) |
| NZ (1) | NZ606700A (https=) |
| PH (1) | PH12013500694A1 (https=) |
| PL (1) | PL2627656T3 (https=) |
| WO (1) | WO2012049153A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US7439358B2 (en) | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
| US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
| US20150031699A1 (en) | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
| CN104003989B (zh) * | 2014-05-26 | 2015-11-11 | 苏州明锐医药科技有限公司 | 伏拉塞替及其中间体的制备方法 |
| US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
| CN105646398B (zh) * | 2014-12-05 | 2018-09-07 | 上海医药工业研究院 | N-((1r,4r)-4-(4-(环丙基甲基)哌嗪-1-基)环己基)乙酰胺的制备方法 |
| CN108610343A (zh) * | 2018-06-12 | 2018-10-02 | 杨文思 | 一种用于治疗癌症的表皮生长因子受体抑制剂及其合成方法 |
| JPWO2020130125A1 (ja) | 2018-12-21 | 2021-11-04 | 第一三共株式会社 | 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ |
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| JPH0276860A (ja) | 1987-10-05 | 1990-03-16 | Toyo Jozo Co Ltd | 6−置換アルコキシ−2−オキソ−1,2−ジヒドロキノキサリン誘導体 |
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| JP2008510771A (ja) | 2004-08-27 | 2008-04-10 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用 |
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| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
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| ES2624622T3 (es) | 2008-12-30 | 2017-07-17 | Rigel Pharmaceuticals, Inc. | Inhibidores de pirimidindiamina cinasa |
| JP2013512882A (ja) | 2009-12-07 | 2013-04-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | トリプルネガティブ乳癌の治療に使用するbibw2992 |
| EP2536725B1 (en) | 2010-02-17 | 2015-10-28 | Boehringer Ingelheim International GmbH | Dihydropteridinones, method for production and use thereof |
| US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| US20130131069A1 (en) | 2011-05-13 | 2013-05-23 | Boehringer Ingelheim International Gmbh | Method for treatment of solid malignancies including advanced or metastatic solid malignancies |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
-
2011
- 2011-09-15 US US13/233,066 patent/US8546566B2/en active Active
- 2011-10-11 AU AU2011315552A patent/AU2011315552B2/en not_active Ceased
- 2011-10-11 JP JP2013533178A patent/JP5937087B2/ja active Active
- 2011-10-11 PH PH1/2013/500694A patent/PH12013500694A1/en unknown
- 2011-10-11 NZ NZ606700A patent/NZ606700A/en not_active IP Right Cessation
- 2011-10-11 CA CA2813838A patent/CA2813838A1/en not_active Abandoned
- 2011-10-11 PL PL11767449T patent/PL2627656T3/pl unknown
- 2011-10-11 MX MX2013003994A patent/MX2013003994A/es active IP Right Grant
- 2011-10-11 CN CN2011800493287A patent/CN103168040A/zh active Pending
- 2011-10-11 WO PCT/EP2011/067696 patent/WO2012049153A1/en not_active Ceased
- 2011-10-11 DK DK11767449.9T patent/DK2627656T3/da active
- 2011-10-11 EP EP11767449.9A patent/EP2627656B1/en active Active
- 2011-10-11 ES ES11767449.9T patent/ES2509741T3/es active Active
- 2011-10-11 KR KR1020137009470A patent/KR20140005877A/ko not_active Ceased
- 2011-10-11 EA EA201300443A patent/EA024256B1/ru not_active IP Right Cessation
- 2011-10-11 BR BR112013008883A patent/BR112013008883A2/pt not_active IP Right Cessation
-
2013
- 2013-02-07 IL IL224602A patent/IL224602A/en not_active IP Right Cessation
- 2013-03-18 CL CL2013000730A patent/CL2013000730A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8546566B2 (en) | 2013-10-01 |
| CA2813838A1 (en) | 2012-04-19 |
| IL224602A (en) | 2016-04-21 |
| NZ606700A (en) | 2015-06-26 |
| CL2013000730A1 (es) | 2013-08-09 |
| DK2627656T3 (da) | 2014-09-08 |
| BR112013008883A2 (pt) | 2017-10-10 |
| AU2011315552A1 (en) | 2013-02-21 |
| KR20140005877A (ko) | 2014-01-15 |
| PH12013500694A1 (en) | 2015-06-19 |
| CN103168040A (zh) | 2013-06-19 |
| EA024256B1 (ru) | 2016-08-31 |
| EA201300443A1 (ru) | 2013-11-29 |
| JP2013539771A (ja) | 2013-10-28 |
| US20120238754A1 (en) | 2012-09-20 |
| MX2013003994A (es) | 2013-06-05 |
| WO2012049153A1 (en) | 2012-04-19 |
| EP2627656A1 (en) | 2013-08-21 |
| EP2627656B1 (en) | 2014-08-20 |
| ES2509741T3 (es) | 2014-10-17 |
| PL2627656T3 (pl) | 2015-02-27 |
| AU2011315552B2 (en) | 2015-05-21 |
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