JP2013508456A - ヘテロアリール化合物の合成方法および精製方法 - Google Patents

ヘテロアリール化合物の合成方法および精製方法 Download PDF

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Publication number
JP2013508456A
JP2013508456A JP2012536897A JP2012536897A JP2013508456A JP 2013508456 A JP2013508456 A JP 2013508456A JP 2012536897 A JP2012536897 A JP 2012536897A JP 2012536897 A JP2012536897 A JP 2012536897A JP 2013508456 A JP2013508456 A JP 2013508456A
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Prior art keywords
dihydropyrazino
pyrazin
methyl
triazol
pyridin
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Pending
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JP2012536897A
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Japanese (ja)
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JP2013508456A5 (OSRAM
Inventor
ハリス，ロイ，エル．
サピエンザ，ジョン
シェヴリン，グラジエッラ
パパ，パトリック
リー，ブランデン，ギングシー
パッカード，ガリク
ジャオ，ジンジン
ジョーキエル，パトリック，アンソニー
モルテンセン，デボラー
リグズ，ジェニファー
ガンボーア，ファン，アントニオ
ボーシャン，マリー，ジョージ
クレイライン，マッシュー，マイケル
コサレ，モヒット，アトゥル
ペリン−ニンコヴィッチ，ソフィー
パイ，フィリップ
ウェイ−ファ レオン，ウィリアム
エルスナー，ジャン
チャウドリー，アヌスヤ
Original Assignee
シグナル ファーマシューティカルズ， エルエルシー
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Publication of JP2013508456A publication Critical patent/JP2013508456A/ja
Publication of JP2013508456A5 publication Critical patent/JP2013508456A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/16—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of arsenic, antimony, bismuth, vanadium, niobium, tantalum, polonium, chromium, molybdenum, tungsten, manganese, technetium or rhenium
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Materials Engineering (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2012536897A 2009-10-26 2010-10-22 ヘテロアリール化合物の合成方法および精製方法 Pending JP2013508456A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25491709P 2009-10-26 2009-10-26
US61/254,917 2009-10-26
US32848010P 2010-04-27 2010-04-27
US61/328,480 2010-04-27
PCT/US2010/053678 WO2011053518A1 (en) 2009-10-26 2010-10-22 Methods of synthesis and purification of heteroaryl compounds

Related Child Applications (1)

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JP2016148782A Division JP6338622B2 (ja) 2009-10-26 2016-07-28 ヘテロアリール化合物の合成方法および精製方法

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JP2013508456A true JP2013508456A (ja) 2013-03-07
JP2013508456A5 JP2013508456A5 (OSRAM) 2013-11-07

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JP2012536897A Pending JP2013508456A (ja) 2009-10-26 2010-10-22 ヘテロアリール化合物の合成方法および精製方法
JP2016148782A Active JP6338622B2 (ja) 2009-10-26 2016-07-28 ヘテロアリール化合物の合成方法および精製方法

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US (3) US8569494B2 (OSRAM)
EP (2) EP3091021B1 (OSRAM)
JP (2) JP2013508456A (OSRAM)
KR (2) KR20120091240A (OSRAM)
CN (2) CN106117213B (OSRAM)
AR (1) AR078788A1 (OSRAM)
AU (1) AU2010313585B2 (OSRAM)
BR (1) BR112012009751A2 (OSRAM)
CA (1) CA2778615C (OSRAM)
CO (1) CO6541598A2 (OSRAM)
CR (1) CR20120211A (OSRAM)
EC (1) ECSP12011831A (OSRAM)
ES (2) ES2613664T3 (OSRAM)
IL (1) IL219368A (OSRAM)
MX (1) MX341704B (OSRAM)
MY (1) MY177695A (OSRAM)
NI (1) NI201200066A (OSRAM)
NZ (2) NZ618135A (OSRAM)
PH (2) PH12012500825A1 (OSRAM)
RU (1) RU2557242C2 (OSRAM)
SG (1) SG10201500511TA (OSRAM)
WO (1) WO2011053518A1 (OSRAM)
ZA (1) ZA201202959B (OSRAM)

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JP2016516815A (ja) * 2013-04-17 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オンに関する医薬製剤、プロセス、固形形態、及び使用方法
JP2016516819A (ja) * 2013-04-17 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法
JP2016516816A (ja) * 2013-04-17 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
JP2016516821A (ja) * 2013-04-17 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー 癌を治療するためのｔｏｒキナーゼ阻害剤及び５−置換キナゾリノン化合物を含む組合せ療法
JP2016518370A (ja) * 2013-04-17 2016-06-23 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
JP2017511361A (ja) * 2014-04-16 2017-04-20 シグナル ファーマシューティカルズ，エルエルシー １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オンの固体形態、その組成物、及びそれらの使用方法
JP2017511367A (ja) * 2014-04-16 2017-04-20 シグナル ファーマシューティカルズ，エルエルシー １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン及び共形成物を含む固体形態、その組成物及び使用方法

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