CN102686225A - 杂芳基化合物的合成和纯化方法 - Google Patents

杂芳基化合物的合成和纯化方法 Download PDF

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Publication number
CN102686225A
CN102686225A CN2010800594724A CN201080059472A CN102686225A CN 102686225 A CN102686225 A CN 102686225A CN 2010800594724 A CN2010800594724 A CN 2010800594724A CN 201080059472 A CN201080059472 A CN 201080059472A CN 102686225 A CN102686225 A CN 102686225A
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China
Prior art keywords
ketone
pyrazolo
dihydro
pyrazines
methyl
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Pending
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CN2010800594724A
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Chinese (zh)
Inventor
洛伊·L·哈瑞斯
约翰·塞派泽
格拉茨埃拉·谢乌林
帕特里克·帕佩
布兰登·金格西·李
加里克·帕卡德
赵晶晶
帕特里克·安东尼·约基尔
黛博拉·莫特森
詹尼弗·里格斯
胡安·安东尼奥·甘博亚
玛丽·乔治·彼彻姆斯
马修·迈克尔·克雷莱茵
莫希特·阿塔尔·柯塔尔
索菲·佩兰-宁科维奇
菲利普·派伊
威廉·威-华·莱昂
简·埃尔斯纳
阿纳苏亚·乔杜里
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Signal Pharmaceuticals LLC
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Signal Pharmaceuticals LLC
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Application filed by Signal Pharmaceuticals LLC filed Critical Signal Pharmaceuticals LLC
Priority to CN201610474699.4A priority Critical patent/CN106117213B/zh
Publication of CN102686225A publication Critical patent/CN102686225A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Materials Engineering (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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)
CN2010800594724A 2009-10-26 2010-10-22 杂芳基化合物的合成和纯化方法 Pending CN102686225A (zh)

Priority Applications (1)

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CN201610474699.4A CN106117213B (zh) 2009-10-26 2010-10-22 杂芳基化合物及其合成和纯化方法

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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

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US (3) US8569494B2 (enExample)
EP (2) EP3091021B1 (enExample)
JP (2) JP2013508456A (enExample)
KR (2) KR20120091240A (enExample)
CN (2) CN106117213B (enExample)
AR (1) AR078788A1 (enExample)
AU (1) AU2010313585B2 (enExample)
BR (1) BR112012009751A2 (enExample)
CA (1) CA2778615C (enExample)
CO (1) CO6541598A2 (enExample)
CR (1) CR20120211A (enExample)
EC (1) ECSP12011831A (enExample)
ES (2) ES2751705T3 (enExample)
IL (1) IL219368A (enExample)
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MY (1) MY177695A (enExample)
NI (1) NI201200066A (enExample)
NZ (2) NZ618135A (enExample)
PH (2) PH12012500825A1 (enExample)
RU (1) RU2557242C2 (enExample)
SG (1) SG10201500511TA (enExample)
WO (1) WO2011053518A1 (enExample)
ZA (1) ZA201202959B (enExample)

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CN104744475A (zh) * 2008-10-27 2015-07-01 西格诺药品有限公司 用于与mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的mTOR激酶抑制剂
CN105324381A (zh) * 2013-04-17 2016-02-10 西格诺药品有限公司 有关1-乙基-7-(2-甲基-6-(1H-1,2,4-三唑-3-基)吡啶-3-基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1H)-酮的药物制剂、程序、固体形式和使用方法
CN105339009A (zh) * 2013-04-17 2016-02-17 西格诺药品有限公司 用于治疗癌症的包括tor激酶抑制剂和5-取代喹唑啉酮化合物的组合疗法
CN105339008A (zh) * 2013-04-17 2016-02-17 西格诺药品有限公司 用于治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯酰胺的组合疗法
CN105377260A (zh) * 2013-04-17 2016-03-02 西格诺药品有限公司 用二氢吡嗪并-吡嗪类对癌症的治疗
CN105392499A (zh) * 2013-04-17 2016-03-09 西格诺药品有限公司 用于治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法
CN107474051A (zh) * 2013-05-29 2017-12-15 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
WO2021219090A1 (zh) * 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
WO2022166866A1 (zh) * 2021-02-08 2022-08-11 南京明德新药研发有限公司 二氢吡嗪并吡嗪类大环化合物

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