NZ606700A - Process for manufacturing dihydropteridinones and intermediates thereof - Google Patents
Process for manufacturing dihydropteridinones and intermediates thereofInfo
- Publication number
- NZ606700A NZ606700A NZ606700A NZ60670011A NZ606700A NZ 606700 A NZ606700 A NZ 606700A NZ 606700 A NZ606700 A NZ 606700A NZ 60670011 A NZ60670011 A NZ 60670011A NZ 606700 A NZ606700 A NZ 606700A
- Authority
- NZ
- New Zealand
- Prior art keywords
- trans
- cyclopropylmethyl
- piperazin
- methoxy
- cyclohexyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 abstract 3
- -1 cyano, hydroxy Chemical group 0.000 abstract 3
- OKNQFIAMWUCAEB-WGSAOQKQSA-N C1(CC1)CN1CCN(CC1)[C@@H]1CC[C@H](CC1)NC(C1=CC(=C(C=C1)[N+](=O)[O-])OC)=O Chemical compound C1(CC1)CN1CCN(CC1)[C@@H]1CC[C@H](CC1)NC(C1=CC(=C(C=C1)[N+](=O)[O-])OC)=O OKNQFIAMWUCAEB-WGSAOQKQSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- PWURRRRGLCVBMX-UHFFFAOYSA-N 3-methoxy-4-nitrobenzoic acid Chemical compound COC1=CC(C(O)=O)=CC=C1[N+]([O-])=O PWURRRRGLCVBMX-UHFFFAOYSA-N 0.000 abstract 1
- YXJAJKBXQHMYLJ-WGSAOQKQSA-N C1=C(N)C(OC)=CC(C(=O)N[C@@H]2CC[C@H](CC2)N2CCN(CC3CC3)CC2)=C1 Chemical compound C1=C(N)C(OC)=CC(C(=O)N[C@@H]2CC[C@H](CC2)N2CCN(CC3CC3)CC2)=C1 YXJAJKBXQHMYLJ-WGSAOQKQSA-N 0.000 abstract 1
- LBYALFWGJOLWMN-HDJSIYSDSA-N C1C[C@@H](N)CC[C@@H]1N1CCN(CC2CC2)CC1 Chemical compound C1C[C@@H](N)CC[C@@H]1N1CCN(CC2CC2)CC1 LBYALFWGJOLWMN-HDJSIYSDSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000003513 alkali Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 239000002585 base Substances 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000005984 hydrogenation reaction Methods 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 239000003586 protic polar solvent Substances 0.000 abstract 1
- SXNJFOWDRLKDSF-STROYTFGSA-N volasertib Chemical compound C1CN([C@H]2CC[C@@H](CC2)NC(=O)C2=CC=C(C(=C2)OC)NC=2N=C3N(C(C)C)[C@@H](C(N(C)C3=CN=2)=O)CC)CCN1CC1CC1 SXNJFOWDRLKDSF-STROYTFGSA-N 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10187194 | 2010-10-12 | ||
| PCT/EP2011/067696 WO2012049153A1 (en) | 2010-10-12 | 2011-10-11 | Process for manufacturing dihydropteridinones and intermediates thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ606700A true NZ606700A (en) | 2015-06-26 |
Family
ID=43902841
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ606700A NZ606700A (en) | 2010-10-12 | 2011-10-11 | Process for manufacturing dihydropteridinones and intermediates thereof |
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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| 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
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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 |
| 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 |
| JP5937087B2 (ja) | 2016-06-22 |
| 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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