CN102428084B - 化合物 - Google Patents

化合物 Download PDF

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Publication number
CN102428084B
CN102428084B CN201080021866.0A CN201080021866A CN102428084B CN 102428084 B CN102428084 B CN 102428084B CN 201080021866 A CN201080021866 A CN 201080021866A CN 102428084 B CN102428084 B CN 102428084B
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CN
China
Prior art keywords
alkyl
optionally
group
replaces
phenyl
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CN201080021866.0A
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English (en)
Chinese (zh)
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CN102428084A (zh
Inventor
爱德华·贾尔斯·麦基弗
埃拉·斯米利亚尼奇
丹尼丝·贾米拉·哈丁
乔安妮·霍夫
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Life Arc Co
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Medical Research Council Technology
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Publication date
Priority claimed from GB0904746A external-priority patent/GB0904746D0/en
Priority claimed from GB0912238A external-priority patent/GB0912238D0/en
Priority claimed from GBGB1001418.1A external-priority patent/GB201001418D0/en
Application filed by Medical Research Council Technology filed Critical Medical Research Council Technology
Publication of CN102428084A publication Critical patent/CN102428084A/zh
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Publication of CN102428084B publication Critical patent/CN102428084B/zh
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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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65611—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system (X = CH2, O, S, NH) optionally with an additional double bond and/or substituents, e.g. penicillins and analogs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201080021866.0A 2009-03-19 2010-03-19 化合物 Active CN102428084B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
GB0904746.5 2009-03-19
GB0904746A GB0904746D0 (en) 2009-03-19 2009-03-19 Compounds
US16202409P 2009-03-20 2009-03-20
US61/162,024 2009-03-20
GB0912238.3 2009-07-14
GB0912238A GB0912238D0 (en) 2009-07-14 2009-07-14 Compounds
GB1001418.1 2010-01-28
GBGB1001418.1A GB201001418D0 (en) 2010-01-28 2010-01-28 Compounds
PCT/GB2010/000498 WO2010106333A1 (en) 2009-03-19 2010-03-19 Compounds

Publications (2)

Publication Number Publication Date
CN102428084A CN102428084A (zh) 2012-04-25
CN102428084B true CN102428084B (zh) 2016-05-18

Family

ID=42226628

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080021866.0A Active CN102428084B (zh) 2009-03-19 2010-03-19 化合物

Country Status (13)

Country Link
US (2) US20100317646A1 (enExample)
EP (1) EP2408772B1 (enExample)
JP (1) JP5732036B2 (enExample)
KR (1) KR101700229B1 (enExample)
CN (1) CN102428084B (enExample)
AU (1) AU2010224693B2 (enExample)
CA (1) CA2754605C (enExample)
CL (1) CL2011002267A1 (enExample)
IL (1) IL215147A0 (enExample)
MX (1) MX2011009807A (enExample)
PE (1) PE20120506A1 (enExample)
RU (1) RU2011142182A (enExample)
WO (1) WO2010106333A1 (enExample)

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GB201008134D0 (en) * 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
GB201015949D0 (en) 2010-09-22 2010-11-03 Medical Res Council Technology Compounds
EP2632260A4 (en) * 2010-10-29 2015-06-17 Merck Sharp & Dohme LEUCINREICH REPEAT KINASE ENZYME ACTIVITY
WO2012118679A1 (en) 2011-02-28 2012-09-07 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2012135631A1 (en) * 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
SG194216A1 (en) * 2011-04-21 2013-11-29 Origenis Gmbh Heterocyclic compounds as kinase inhibitors
AU2012258977A1 (en) 2011-05-23 2014-01-16 Imago Pharmaceuticals, Inc. Inhibitors of LRRK2 kinase activity
CN102558174B (zh) * 2011-08-23 2014-03-19 天津市斯芬克司药物研发有限公司 一种全新吡唑并[4,3-c]吡啶化合物的发明及其合成方法
EP2760453B1 (en) * 2011-09-30 2016-05-25 Ipsen Pharma S.A.S. Macrocyclic lrrk2 kinase inhibitors
GB201204985D0 (en) 2012-03-21 2012-05-02 Genentech Inc Compounds
WO2013182612A1 (en) 2012-06-07 2013-12-12 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
EP3255049A1 (en) * 2012-06-29 2017-12-13 Pfizer Inc Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
WO2014026330A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014060113A1 (en) 2012-10-19 2014-04-24 Origenis Gmbh Novel kinase inhibitors
CA2887887C (en) * 2012-10-31 2020-08-25 Raqualia Pharma Inc. Pyrazolopyridine derivatives as ttx-s blockers
CA2889572C (en) * 2012-11-08 2019-03-05 Pfizer Inc. Heteroaromatic compounds as dopamine d1 ligands
US9045477B2 (en) * 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2014150981A1 (en) * 2013-03-15 2014-09-25 Elan Pharmaceuticals, Llc Inhibitors of lrrk2 kinase activity
TW201533043A (zh) * 2013-04-18 2015-09-01 Lundbeck & Co As H 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物
TW201534597A (zh) * 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
WO2015026683A1 (en) * 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
EP3083618B1 (en) 2013-12-17 2018-02-21 Pfizer Inc Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
WO2015162518A1 (en) 2014-04-25 2015-10-29 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
CA2948587C (en) 2014-05-14 2018-07-17 Pfizer Inc. Pyrazolopyridines and pyrazolopyrimidines
WO2016036586A1 (en) * 2014-09-03 2016-03-10 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
EP3350178B1 (en) 2015-09-14 2021-10-20 Pfizer Inc. Novel imidazo [4,5-c]quinoline and imidazo [4,5-c][1,5]naphthyridine derivatives as lrrk2 inhibitors
JP6797219B2 (ja) * 2016-06-15 2020-12-09 スーチョウ ヤバオ ファーマスーティカル アールアンドディー カンパニー リミテッド 置換三環式複素環化合物及びその用途
JP6728503B2 (ja) 2017-02-24 2020-07-22 テグ−キョンプク メディカル イノベーション ファウンデーション 血液脳関門を通過することができる化合物を有効成分として含有する脳腫瘍の予防または治療用薬学的組成物
EP3737680A1 (en) 2018-01-08 2020-11-18 F. Hoffmann-La Roche AG Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors
KR101990738B1 (ko) * 2018-07-24 2019-06-19 재단법인 대구경북첨단의료산업진흥재단 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물
US20230024438A1 (en) * 2019-12-04 2023-01-26 Arcus Biosciences, Inc. Inhibitors of hif-2alpha
BR112022026105A2 (pt) 2020-06-22 2023-01-17 Hoffmann La Roche Compostos, composições farmacêuticas, método para o tratamento ou prevenção de adenocarcinoma pulmonar, uso de compostos e invenção
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WO2023160652A1 (zh) * 2022-02-25 2023-08-31 苏州亚宝药物研发有限公司 取代的稠环化合物及其药物组合物、制备方法和用途

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WO2006077319A1 (fr) * 2005-01-19 2006-07-27 Aventis Pharma S.A. Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation

Also Published As

Publication number Publication date
WO2010106333A1 (en) 2010-09-23
KR20110128925A (ko) 2011-11-30
KR101700229B1 (ko) 2017-01-26
CA2754605A1 (en) 2010-09-23
EP2408772A1 (en) 2012-01-25
RU2011142182A (ru) 2013-04-27
EP2408772B1 (en) 2015-07-01
IL215147A0 (en) 2011-12-29
US20100317646A1 (en) 2010-12-16
AU2010224693B2 (en) 2016-07-28
CL2011002267A1 (es) 2012-05-11
MX2011009807A (es) 2011-09-29
CN102428084A (zh) 2012-04-25
CA2754605C (en) 2018-04-17
JP5732036B2 (ja) 2015-06-10
PE20120506A1 (es) 2012-05-14
US20170320870A1 (en) 2017-11-09
JP2012520861A (ja) 2012-09-10
AU2010224693A1 (en) 2011-09-15

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Address after: London, England

Patentee after: Life arc company

Address before: London, England

Patentee before: Medical Res Council Technology