CN102119163A - 二氮杂咔唑和使用方法 - Google Patents

二氮杂咔唑和使用方法 Download PDF

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Publication number
CN102119163A
CN102119163A CN2009801313072A CN200980131307A CN102119163A CN 102119163 A CN102119163 A CN 102119163A CN 2009801313072 A CN2009801313072 A CN 2009801313072A CN 200980131307 A CN200980131307 A CN 200980131307A CN 102119163 A CN102119163 A CN 102119163A
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China
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alkyl
compound
formula
groups
heterocyclyl
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Pending
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CN2009801313072A
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Chinese (zh)
Inventor
黑兹尔·J·戴克
查尔斯·埃尔伍德
伊曼纽拉·甘西亚
刘易斯·J·加扎德
西蒙·C·古达克里
塞缪尔·S·金茨
约瑟夫·P·利西卡托斯
卡勒姆·麦克劳德
卡伦·威廉斯
陈慧芬
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Genentech Inc
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Genentech Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41066724&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102119163(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of CN102119163A publication Critical patent/CN102119163A/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
    • C07D471/12—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
    • 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
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN2009801313072A 2008-06-11 2009-06-10 二氮杂咔唑和使用方法 Pending CN102119163A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US6074608P 2008-06-11 2008-06-11
US61/060,746 2008-06-11
US14800109P 2009-01-28 2009-01-28
US61/148,001 2009-01-28
PCT/US2009/003492 WO2009151598A1 (en) 2008-06-11 2009-06-10 Diazacarbazoles and methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201410302026.1A Division CN104059066A (zh) 2008-06-11 2009-06-10 二氮杂咔唑和使用方法

Publications (1)

Publication Number Publication Date
CN102119163A true CN102119163A (zh) 2011-07-06

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CN2009801313072A Pending CN102119163A (zh) 2008-06-11 2009-06-10 二氮杂咔唑和使用方法
CN201410302026.1A Pending CN104059066A (zh) 2008-06-11 2009-06-10 二氮杂咔唑和使用方法

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Country Status (20)

Country Link
US (3) US8501765B2 (https=)
EP (2) EP2706059A1 (https=)
JP (2) JP5599784B2 (https=)
KR (1) KR101710732B1 (https=)
CN (2) CN102119163A (https=)
AR (1) AR072092A1 (https=)
AU (1) AU2009258124C1 (https=)
BR (1) BRPI0909954A2 (https=)
CA (1) CA2725754C (https=)
CL (1) CL2010001415A1 (https=)
DK (1) DK2300475T3 (https=)
ES (1) ES2529361T3 (https=)
IL (1) IL209754A0 (https=)
MX (1) MX2010013627A (https=)
PE (2) PE20110365A1 (https=)
PH (1) PH12013502369A1 (https=)
RU (2) RU2515972C2 (https=)
TW (2) TWI466886B (https=)
WO (1) WO2009151598A1 (https=)
ZA (1) ZA201008483B (https=)

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CN102365282A (zh) * 2009-03-24 2012-02-29 赛诺菲 9H-吡咯并[2，3-b：5，4-c’]二吡啶氮杂咔啉衍生物、其制备方法及其治疗用途
CN102503959A (zh) * 2011-10-25 2012-06-20 南方医科大学 一种稠三环类化合物及其制备方法、以及含该类化合物的药物组合物及其应用
CN102791711A (zh) * 2009-12-16 2012-11-21 霍夫曼-拉罗奇有限公司 1,7-二氮杂咔唑和其在治疗癌症中的用途
CN107118207A (zh) * 2017-05-22 2017-09-01 苏州东南药业股份有限公司 一类cdk抑制剂的制备方法
CN113227077A (zh) * 2018-12-13 2021-08-06 英特维特国际股份有限公司 一种制备1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺的方法

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TWI466886B (zh) * 2008-06-11 2015-01-01 Genentech Inc 二氮雜咔唑及使用方法
AR072084A1 (es) * 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
FR2950891B1 (fr) * 2009-10-06 2012-11-09 Sanofi Aventis Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique
RU2017127088A (ru) 2010-11-16 2019-02-04 Эррэй Биофарма Инк. Комбинация ингибиторов чекпойнт-киназы 1 и ингибиторов киназы wee 1
JP6073910B2 (ja) * 2011-11-09 2017-02-01 キャンサー・リサーチ・テクノロジー・リミテッド ５−（ピリジン−２−イル−アミノ）−ピラジン−２−カルボニトリル化合物及びその治療使用
EP2793882A4 (en) 2011-12-22 2015-04-29 Threshold Pharmaceuticals Inc ADMINISTRATION OF HYPOXIA-ACTIVATED PRODRUGS IN COMBINATION WITH CHK1 INHIBITORS FOR THE TREATMENT OF CANCER
JP6182593B2 (ja) 2012-04-20 2017-08-16 アドヴィーナス セラピューティクス リミテッド 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途
EP2671881A1 (en) 2012-06-07 2013-12-11 Syngenta Participations AG. Pesticidally active pyridyl- and pyrimidyl- substituted thiazole derivatives
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
WO2015069489A1 (en) 2013-11-06 2015-05-14 Merck Patent Gmbh Predictive biomarker for hypoxia-activated prodrug therapy
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
CN113015526A (zh) * 2018-09-19 2021-06-22 豪夫迈·罗氏有限公司 螺环2,3-二氢-7-氮杂吲哚化合物及其用途
WO2020072675A1 (en) 2018-10-02 2020-04-09 Northwestern University Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c)
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
US12168662B1 (en) 2023-12-15 2024-12-17 King Faisal University Pyrido[4′,3′:4,5]pyrrolo[2,3-c][2,7]naphthyridines compounds as CK2 inhibitors
US12129252B1 (en) 2024-02-15 2024-10-29 King Faisal University Pyrrolo[2,3-c][2,6]naphthyridine-8-carboxylic acids as CK2 inhibitors

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CN107118207B (zh) * 2017-05-22 2020-10-02 苏州东南药业股份有限公司 一类cdk抑制剂的制备方法
CN113227077A (zh) * 2018-12-13 2021-08-06 英特维特国际股份有限公司 一种制备1-[(3r,4s)-4-氰基四氢吡喃-3-基]-3-[(2-氟-6-甲氧基-4-吡啶基)氨基]吡唑-4-甲酰胺的方法

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