JP6338601B2 - ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物 - Google Patents

ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物 Download PDF

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JP6338601B2
JP6338601B2 JP2015559501A JP2015559501A JP6338601B2 JP 6338601 B2 JP6338601 B2 JP 6338601B2 JP 2015559501 A JP2015559501 A JP 2015559501A JP 2015559501 A JP2015559501 A JP 2015559501A JP 6338601 B2 JP6338601 B2 JP 6338601B2
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JP2016513130A5 (enExample
JP2016513130A (ja
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テヘドール， マリア デル マール クアドラド
テヘドール， マリア デル マール クアドラド
フェルナンデス， ラファエル フランコ
フェルナンデス， ラファエル フランコ
オスタ， アナ マリア ガルシア
オスタ， アナ マリア ガルシア
サンタマリーナ， ジュレン オヤルザバル
サンタマリーナ， ジュレン オヤルザバル
グラシア， マリア オブデュリア ラバル
グラシア， マリア オブデュリア ラバル
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フンダシオン パラ ラ インベスティガシオン メディカ アプリカダ
フンダシオン パラ ラ インベスティガシオン メディカ アプリカダ
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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
    • 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
    • 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
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
JP2015559501A 2013-03-01 2014-02-27 ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物 Expired - Fee Related JP6338601B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13382065.4 2013-03-01
EP13382065 2013-03-01
PCT/EP2014/053877 WO2014131855A1 (en) 2013-03-01 2014-02-27 Novel compounds as dual inhibitors of phosphodiesterases and histone deacetylases

Publications (3)

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JP2016513130A JP2016513130A (ja) 2016-05-12
JP2016513130A5 JP2016513130A5 (enExample) 2017-03-30
JP6338601B2 true JP6338601B2 (ja) 2018-06-06

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JP2015559501A Expired - Fee Related JP6338601B2 (ja) 2013-03-01 2014-02-27 ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物

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US (1) US9573956B2 (enExample)
EP (1) EP2961741B1 (enExample)
JP (1) JP6338601B2 (enExample)
CA (1) CA2908482A1 (enExample)
DK (1) DK2961741T3 (enExample)
ES (1) ES2635016T3 (enExample)
WO (1) WO2014131855A1 (enExample)

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US9505767B2 (en) * 2013-09-05 2016-11-29 Genentech, Inc. Pyrazolo[1,5-A]pyrimidin-7(4H)-onehistone demethylase inhibitors
EP3085700B1 (en) * 2013-12-20 2018-10-31 Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China Novel piperidine carboxamide compound, preparation method, and usage thereof
CA2987978C (en) * 2014-06-16 2022-08-16 Fundacion Para La Investigacion Medica Aplicada Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases
JP2017523204A (ja) * 2014-08-04 2017-08-17 ファンダシオン パラ ラ インベスティガシオン メディカ アプリカダＦｕｎｄａｃｉｏｎ Ｐａｒａ Ｌａ Ｉｎｖｅｓｔｉｇａｓｉｏｎ Ｍｅｄｉｃａ Ａｐｌｉｃａｄａ 認知向上のために用いる新規化合物
WO2016120432A1 (en) * 2015-01-30 2016-08-04 Fundación Para La Investigación Médica Aplicada Compounds and methods for anticoagulation therapy
CN104610166B (zh) * 2015-03-10 2017-06-13 山东大学 嘧啶苄基异羟肟酸类组蛋白去乙酰化酶抑制剂及制备方法和应用
HK1249104A1 (zh) 2015-03-13 2018-10-26 Forma Therapeutics, Inc. 作为HDAC8抑制剂的α-肉桂酰胺化合物和组合物
KR102457316B1 (ko) * 2015-06-26 2022-10-20 총킹 디캉 에릴 파마 씨오. 엘티디. 새로운 5형포스포디에스테라아제 억제제 및 그 용도
CN110337437B (zh) 2016-12-28 2023-02-03 达特神经科学有限公司 作为pde2抑制剂的取代的吡唑并嘧啶酮化合物
CN107163052B (zh) * 2017-04-18 2020-08-11 华南农业大学 一种针对多种pde-5抑制剂药物的免疫检测方法
WO2019018562A1 (en) 2017-07-19 2019-01-24 Ideaya Biosciences, Inc. AMIDO COMPOUND AS MODULATORS OF AHR
CN108912029B (zh) * 2017-08-25 2021-10-01 广东东阳光药业有限公司 含氮杂环酰胺衍生物及其用途
KR102794907B1 (ko) 2017-11-27 2025-04-14 다트 뉴로사이언스, 엘엘씨 Pde1 억제제로서의 치환된 푸라노피리미딘 화합물
CN110054625B (zh) * 2018-01-18 2022-01-07 山东大学 N-酰基苯磺酰胺异羟肟酸类Bcl-2、HDAC双靶点抑制剂及制备方法和应用
CN108558890A (zh) * 2018-06-28 2018-09-21 重庆康刻尔制药有限公司 一种西地那非中间体合成方法
CN109824516B (zh) * 2019-03-14 2021-07-23 泰州精英化成医药科技有限公司 一种反式-4-羟基环已烷甲酸叔丁酯的制备方法
CN109810108B (zh) * 2019-03-20 2021-08-06 华东理工大学 2,8-二氮杂-螺-[4,5]-癸烷类嘧啶-异羟肟酸化合物及其用途
US11787812B2 (en) 2020-12-11 2023-10-17 Ildong Pharmaceutical Co., Ltd. Substituted pyrazolo[4,3-d]pyrimidines and imidazo[5,1 -f][1,2,4]triazines as androgen receptor and phosphodiesterase dual inhibitors
KR20240124952A (ko) 2021-12-22 2024-08-19 어거스틴 테라퓨틱스 Hdac6 억제제로서의 화합물 및 이의 용도
CN115417877B (zh) * 2022-09-20 2024-05-14 杭州师范大学 组蛋白去乙酰化酶抑制剂及其制备和在制备抗癌症药物上的应用
CN116375714A (zh) * 2023-03-24 2023-07-04 苏州满元生物科技有限公司 卡巴地那非类药物关键中间体的制备方法

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Publication number Publication date
WO2014131855A1 (en) 2014-09-04
ES2635016T3 (es) 2017-10-02
EP2961741A1 (en) 2016-01-06
EP2961741B1 (en) 2017-04-05
US20160002246A1 (en) 2016-01-07
WO2014131855A9 (en) 2014-11-13
JP2016513130A (ja) 2016-05-12
CA2908482A1 (en) 2014-09-04
DK2961741T3 (en) 2017-07-03
US9573956B2 (en) 2017-02-21

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