CN103328451B - 降低β-淀粉样物质生成的化合物 - Google Patents

降低β-淀粉样物质生成的化合物 Download PDF

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Publication number
CN103328451B
CN103328451B CN201280006419.7A CN201280006419A CN103328451B CN 103328451 B CN103328451 B CN 103328451B CN 201280006419 A CN201280006419 A CN 201280006419A CN 103328451 B CN103328451 B CN 103328451B
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CN
China
Prior art keywords
dihydro
mmol
pyrimidine
preparation
phenyl
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Expired - Fee Related
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CN201280006419.7A
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English (en)
Chinese (zh)
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CN103328451A (zh
Inventor
K.M.博伊
J.M.古尔农
J.E.玛考
R.E.奥尔森
J.史
洛林.A.汤普森三世
Y-J.吴
L.徐
Y.张
D.S.朱福
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
CN201280006419.7A 2011-01-28 2012-01-26 降低β-淀粉样物质生成的化合物 Expired - Fee Related CN103328451B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161437279P 2011-01-28 2011-01-28
US61/437,279 2011-01-28
PCT/US2012/022665 WO2012103297A1 (en) 2011-01-28 2012-01-26 COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION

Publications (2)

Publication Number Publication Date
CN103328451A CN103328451A (zh) 2013-09-25
CN103328451B true CN103328451B (zh) 2015-06-10

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Country Link
US (1) US8710061B2 (enExample)
EP (1) EP2668168B1 (enExample)
JP (1) JP5908499B2 (enExample)
KR (1) KR20140014152A (enExample)
CN (1) CN103328451B (enExample)
AR (1) AR084944A1 (enExample)
AU (1) AU2012211301B2 (enExample)
BR (1) BR112013018298A2 (enExample)
CA (1) CA2825906A1 (enExample)
EA (1) EA201391097A1 (enExample)
IL (1) IL226677A (enExample)
MX (1) MX2013008699A (enExample)
SG (1) SG191840A1 (enExample)
TW (1) TW201309655A (enExample)
WO (1) WO2012103297A1 (enExample)

Families Citing this family (10)

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Publication number Priority date Publication date Assignee Title
KR102227271B1 (ko) 2013-04-15 2021-03-12 에프엠씨 코포레이션 살진균성 아미드
WO2016080516A1 (ja) * 2014-11-21 2016-05-26 味の素株式会社 Drp1重合阻害剤
US10913744B2 (en) 2015-02-13 2021-02-09 Dana-Farber Cancer Institute, Inc. LRRK2 inhibitors and methods of making and using the same
CN105017046A (zh) * 2015-07-15 2015-11-04 上海博康精细化工有限公司 一种4-环丙胺基丁酸乙酯的制备方法
US10494378B2 (en) * 2015-07-21 2019-12-03 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Fused ring pyrimidine compound, intermediate, and preparation method, composition and use thereof
JP7335242B2 (ja) * 2017-11-27 2023-08-29 エフ. ホフマン-ラ ロシュ アーゲー ピリミジン誘導体
WO2020156445A1 (zh) 2019-01-29 2020-08-06 山东轩竹医药科技有限公司 己酮糖激酶抑制剂及其用途
CN112028839B (zh) * 2020-09-30 2022-04-12 中国海洋大学 一种医药中间体环烷烃并嘧啶二酮化合物的合成方法
TW202317528A (zh) * 2021-06-24 2023-05-01 美商富曼西公司 用於防治無脊椎有害生物的唑類化合物
CN117417302A (zh) * 2023-04-12 2024-01-19 江苏艾迪药业股份有限公司 艾诺韦林的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2226315A1 (en) * 2007-12-28 2010-09-08 Carna Biosciences Inc. 2-aminoquinazoline derivative
CN102548557A (zh) * 2009-07-31 2012-07-04 百时美施贵宝公司 用于降低β-淀粉状蛋白生成的化合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1698627A1 (en) 2000-09-15 2006-09-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
TW201030002A (en) * 2009-01-16 2010-08-16 Bristol Myers Squibb Co Bicyclic compounds for the reduction of beta-amyloid production
US8637525B2 (en) * 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2226315A1 (en) * 2007-12-28 2010-09-08 Carna Biosciences Inc. 2-aminoquinazoline derivative
CN102548557A (zh) * 2009-07-31 2012-07-04 百时美施贵宝公司 用于降低β-淀粉状蛋白生成的化合物

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CA2825906A1 (en) 2012-08-02
AR084944A1 (es) 2013-07-10
US20130030011A1 (en) 2013-01-31
JP5908499B2 (ja) 2016-04-26
TW201309655A (zh) 2013-03-01
AU2012211301A1 (en) 2013-09-19
JP2014503590A (ja) 2014-02-13
US8710061B2 (en) 2014-04-29
EP2668168A1 (en) 2013-12-04
IL226677A (en) 2014-11-30
EA201391097A1 (ru) 2013-11-29
MX2013008699A (es) 2013-08-21
BR112013018298A2 (pt) 2016-11-16
WO2012103297A1 (en) 2012-08-02
EP2668168B1 (en) 2017-03-01
CN103328451A (zh) 2013-09-25
SG191840A1 (en) 2013-08-30
AU2012211301B2 (en) 2016-02-25
KR20140014152A (ko) 2014-02-05

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Termination date: 20170126