JP5998145B2 - ピリミジン誘導体の製造プロセス - Google Patents
ピリミジン誘導体の製造プロセス Download PDFInfo
- Publication number
- JP5998145B2 JP5998145B2 JP2013531796A JP2013531796A JP5998145B2 JP 5998145 B2 JP5998145 B2 JP 5998145B2 JP 2013531796 A JP2013531796 A JP 2013531796A JP 2013531796 A JP2013531796 A JP 2013531796A JP 5998145 B2 JP5998145 B2 JP 5998145B2
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- JP
- Japan
- Prior art keywords
- compound
- substituted
- formula
- unsubstituted
- monohydrochloride
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38872110P | 2010-10-01 | 2010-10-01 | |
| US61/388,721 | 2010-10-01 | ||
| US201161494915P | 2011-06-09 | 2011-06-09 | |
| US61/494,915 | 2011-06-09 | ||
| PCT/US2011/053808 WO2012044727A2 (en) | 2010-10-01 | 2011-09-29 | Manufacturing process for pyrimidine derivatives |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246502A Division JP2016106091A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
| JP2015246501A Division JP2016128414A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013541536A JP2013541536A (ja) | 2013-11-14 |
| JP2013541536A5 JP2013541536A5 (enExample) | 2014-11-13 |
| JP5998145B2 true JP5998145B2 (ja) | 2016-09-28 |
Family
ID=44773179
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013531796A Active JP5998145B2 (ja) | 2010-10-01 | 2011-09-29 | ピリミジン誘導体の製造プロセス |
| JP2015246502A Pending JP2016106091A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
| JP2015246501A Pending JP2016128414A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246502A Pending JP2016106091A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
| JP2015246501A Pending JP2016128414A (ja) | 2010-10-01 | 2015-12-17 | ピリミジン誘導体の製造プロセス |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US9181215B2 (enExample) |
| EP (2) | EP2621908A2 (enExample) |
| JP (3) | JP5998145B2 (enExample) |
| KR (2) | KR20130119928A (enExample) |
| CN (3) | CN104987321A (enExample) |
| AR (1) | AR083213A1 (enExample) |
| AU (4) | AU2011308856B2 (enExample) |
| BR (1) | BR112013007123B1 (enExample) |
| CA (1) | CA2813333C (enExample) |
| CL (2) | CL2013000850A1 (enExample) |
| CO (1) | CO6700837A2 (enExample) |
| DK (1) | DK3040333T3 (enExample) |
| EC (1) | ECSP13012596A (enExample) |
| ES (1) | ES2699951T3 (enExample) |
| GT (1) | GT201300080A (enExample) |
| HU (1) | HUE041326T2 (enExample) |
| IL (3) | IL225113A (enExample) |
| LT (1) | LT3040333T (enExample) |
| MX (1) | MX354482B (enExample) |
| MY (1) | MY160785A (enExample) |
| NZ (1) | NZ608285A (enExample) |
| PE (1) | PE20140002A1 (enExample) |
| PH (2) | PH12013500579A1 (enExample) |
| PL (1) | PL3040333T3 (enExample) |
| PT (1) | PT3040333T (enExample) |
| RU (2) | RU2015150728A (enExample) |
| SG (1) | SG188439A1 (enExample) |
| SI (1) | SI3040333T1 (enExample) |
| TW (1) | TWI540133B (enExample) |
| WO (1) | WO2012044727A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140040770A (ko) | 2011-07-01 | 2014-04-03 | 노파르티스 아게 | 암 치료에 사용하기 위한 cdk4/6 억제제 및 pi3k 억제제를 포함하는 조합 요법 |
| PH12014500682A1 (en) | 2011-09-27 | 2014-05-12 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| ES2605638T3 (es) * | 2012-10-23 | 2017-03-15 | Novartis Ag | Proceso Mejorado para fabricar 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| WO2014141104A1 (en) | 2013-03-14 | 2014-09-18 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| US9318944B2 (en) | 2013-04-29 | 2016-04-19 | Rockwell Automation Technologies, Inc. | Methods and apparatus for active front end filter capacitor degradation detection |
| US9294005B2 (en) | 2013-10-01 | 2016-03-22 | Rockwell Automation Technologies, Inc. | Method and apparatus for detecting AFE filter capacitor degradation |
| RU2663999C2 (ru) * | 2013-10-16 | 2018-08-14 | Шанхай Инли Фармасьютикал Ко., Лтд | Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения |
| RU2688665C2 (ru) * | 2014-04-22 | 2019-05-22 | Университет Базель | Новый способ получения производных триазина, пиримидина и пиридина |
| CN105085476B (zh) * | 2014-11-24 | 2018-03-09 | 苏州晶云药物科技有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法 |
| CN107001348B (zh) * | 2014-12-17 | 2019-10-11 | 上海海雁医药科技有限公司 | 2-吗啉-4,6-二取代的嘧啶衍生物、其制法与医药上的用途 |
| US9481665B2 (en) * | 2015-03-13 | 2016-11-01 | Yong Xu | Process for preparing PI3K inhibitor buparsilib |
| EP3273959A1 (en) | 2015-03-25 | 2018-01-31 | Novartis Ag | Pharmaceutical combinations |
| CN105001151B (zh) * | 2015-08-28 | 2017-07-14 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
| CN106543140A (zh) * | 2015-09-21 | 2017-03-29 | 苏州晶云药物科技有限公司 | 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法 |
| PL3978500T3 (pl) * | 2015-12-16 | 2024-03-11 | Genentech, Inc. | Sposób wytwarzania tricyklicznych związków inhibitorów pi3k |
| CN106905294A (zh) * | 2016-07-08 | 2017-06-30 | 苏州科睿思制药有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法 |
| CN107793394A (zh) * | 2017-08-03 | 2018-03-13 | 上海厚璞生物科技有限公司 | 一种生产选择性pi3k抑制剂的系列关键中间体 |
| CN110016142B (zh) * | 2019-04-30 | 2021-08-03 | 合肥工业大学 | 一种含嘧啶硼酸结构的硅油及其制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6124476A (en) | 1998-04-17 | 2000-09-26 | Symyx Technologies, Inc. | Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates |
| CN1735598A (zh) * | 2002-11-11 | 2006-02-15 | 拜耳医药保健股份公司 | 作为ip受体拮抗剂的苯基或杂芳基氨基烷烃衍生物 |
| CA2507100C (en) | 2002-11-21 | 2012-10-09 | Chiron Corporation | 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EP2057140B1 (en) | 2006-08-24 | 2012-08-08 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| MX2009008341A (es) * | 2007-02-06 | 2009-08-12 | Novartis Ag | Inhibidores de cinasa de pi3 y metodos para su uso. |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| JP2012526772A (ja) * | 2009-05-15 | 2012-11-01 | ノバルティス アーゲー | ホスホイノシチド３−キナーゼ阻害剤および抗糖尿病性化合物の組合せ剤 |
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2011
- 2011-09-29 PE PE2013000654A patent/PE20140002A1/es active IP Right Grant
- 2011-09-29 MY MYPI2013000811A patent/MY160785A/en unknown
- 2011-09-29 RU RU2015150728A patent/RU2015150728A/ru unknown
- 2011-09-29 CA CA2813333A patent/CA2813333C/en active Active
- 2011-09-29 PH PH1/2013/500579A patent/PH12013500579A1/en unknown
- 2011-09-29 KR KR1020137011172A patent/KR20130119928A/ko not_active Ceased
- 2011-09-29 AR ARP110103595A patent/AR083213A1/es unknown
- 2011-09-29 NZ NZ608285A patent/NZ608285A/en not_active IP Right Cessation
- 2011-09-29 AU AU2011308856A patent/AU2011308856B2/en active Active
- 2011-09-29 LT LTEP16151719.8T patent/LT3040333T/lt unknown
- 2011-09-29 CN CN201510156027.4A patent/CN104987321A/zh active Pending
- 2011-09-29 DK DK16151719.8T patent/DK3040333T3/da active
- 2011-09-29 PL PL16151719T patent/PL3040333T3/pl unknown
- 2011-09-29 EP EP11767362.4A patent/EP2621908A2/en not_active Withdrawn
- 2011-09-29 RU RU2013120326/04A patent/RU2576619C2/ru active
- 2011-09-29 SI SI201131619T patent/SI3040333T1/sl unknown
- 2011-09-29 ES ES16151719T patent/ES2699951T3/es active Active
- 2011-09-29 MX MX2013003507A patent/MX354482B/es active IP Right Grant
- 2011-09-29 SG SG2013016837A patent/SG188439A1/en unknown
- 2011-09-29 EP EP16151719.8A patent/EP3040333B1/en active Active
- 2011-09-29 HU HUE16151719A patent/HUE041326T2/hu unknown
- 2011-09-29 US US13/825,880 patent/US9181215B2/en active Active
- 2011-09-29 BR BR112013007123-0A patent/BR112013007123B1/pt active IP Right Grant
- 2011-09-29 KR KR1020187032263A patent/KR20180123586A/ko not_active Ceased
- 2011-09-29 PT PT16151719T patent/PT3040333T/pt unknown
- 2011-09-29 CN CN201180047753.2A patent/CN103140479B/zh active Active
- 2011-09-29 JP JP2013531796A patent/JP5998145B2/ja active Active
- 2011-09-29 CN CN201510157366.4A patent/CN104945373A/zh active Pending
- 2011-09-29 WO PCT/US2011/053808 patent/WO2012044727A2/en not_active Ceased
- 2011-09-30 TW TW100135673A patent/TWI540133B/zh active
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2013
- 2013-03-07 IL IL225113A patent/IL225113A/en unknown
- 2013-03-22 CO CO13057091A patent/CO6700837A2/es unknown
- 2013-03-22 GT GT201300080A patent/GT201300080A/es unknown
- 2013-03-28 CL CL2013000850A patent/CL2013000850A1/es unknown
- 2013-04-30 EC ECSP13012596 patent/ECSP13012596A/es unknown
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2014
- 2014-06-19 IL IL233282A patent/IL233282A/en unknown
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2015
- 2015-02-24 AU AU2015200936A patent/AU2015200936A1/en not_active Abandoned
- 2015-02-24 AU AU2015200938A patent/AU2015200938B2/en not_active Ceased
- 2015-03-30 IL IL238046A patent/IL238046A/en not_active IP Right Cessation
- 2015-04-27 CL CL2015001088A patent/CL2015001088A1/es unknown
- 2015-05-06 US US14/705,013 patent/US9359326B2/en not_active Expired - Fee Related
- 2015-07-20 PH PH12015501585A patent/PH12015501585A1/en unknown
- 2015-10-23 AU AU2015246141A patent/AU2015246141B2/en not_active Ceased
- 2015-12-17 JP JP2015246502A patent/JP2016106091A/ja active Pending
- 2015-12-17 JP JP2015246501A patent/JP2016128414A/ja active Pending
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2016
- 2016-05-06 US US15/147,986 patent/US9452994B2/en not_active Expired - Fee Related
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