TWI574962B - 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 - Google Patents

作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 Download PDF

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TWI574962B
TWI574962B TW102140742A TW102140742A TWI574962B TW I574962 B TWI574962 B TW I574962B TW 102140742 A TW102140742 A TW 102140742A TW 102140742 A TW102140742 A TW 102140742A TW I574962 B TWI574962 B TW I574962B
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cancer
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compounds
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TW102140742A
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TW201422615A (zh
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習寧
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加拓科學公司
廣東東陽光藥業有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW102140742A 2012-11-14 2013-11-08 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 TWI574962B (zh)

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US201261726139P 2012-11-14 2012-11-14

Publications (2)

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TW201422615A TW201422615A (zh) 2014-06-16
TWI574962B true TWI574962B (zh) 2017-03-21

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US (1) US9926324B2 (enExample)
EP (2) EP2919784B1 (enExample)
JP (1) JP6268183B2 (enExample)
KR (1) KR102148679B1 (enExample)
CN (1) CN104755085B (enExample)
AU (1) AU2013345107B2 (enExample)
BR (1) BR112015006726B1 (enExample)
CA (1) CA2889346C (enExample)
ES (1) ES2661380T3 (enExample)
MY (1) MY180641A (enExample)
RU (1) RU2665036C9 (enExample)
SG (1) SG11201502725TA (enExample)
TW (1) TWI574962B (enExample)
WO (1) WO2014078211A1 (enExample)
ZA (1) ZA201502575B (enExample)

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CN105503877A (zh) 2014-09-24 2016-04-20 和记黄埔医药(上海)有限公司 咪唑并哒嗪类化合物及其用途
SI3233839T1 (sl) * 2014-12-19 2019-12-31 Janssen Pharmaceutica Nv Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta
JP6568588B2 (ja) * 2014-12-19 2019-08-28 ヤンセン ファーマシューティカ エヌ.ベー. PI3Kβ阻害剤としてのイミダゾピリダジン誘導体
JP7149854B2 (ja) * 2016-06-16 2022-10-07 ヤンセン ファーマシューティカ エヌ.ベー. Pi3k beta阻害薬としての二環式ピリジン、ピラジンおよびピリミジン誘導体
WO2018017633A1 (en) 2016-07-21 2018-01-25 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
JP2019534266A (ja) 2016-10-14 2019-11-28 江蘇恒瑞医薬股▲ふん▼有限公司 5員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用
US11629146B2 (en) * 2016-11-28 2023-04-18 Praxis Precision Medicines, Inc. Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of sodium channel activity
CN108164525B (zh) * 2016-12-08 2020-09-08 沈阳药科大学 一种抗肿瘤化合物的制备方法和用途
AU2018209164B2 (en) 2017-01-17 2021-11-04 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
FR3064364A1 (fr) * 2017-03-27 2018-09-28 S.P.C.M. Sa Methode de dosage de polymeres cationiques
PH12022500017A1 (en) 2020-04-29 2023-08-14 De Shaw Res Llc PI3K-a INHIBITORS AND METHODS OF USE THEREOF
WO2023039532A1 (en) * 2021-09-10 2023-03-16 Relay Therapeutics, Inc. Pi3k-alpha inhibitors and methods of use thereof
WO2023220131A2 (en) * 2022-05-10 2023-11-16 Relay Therapeutics, Inc. PI3Kα INHIBITORS AND METHODS OF USE THEREOF
CN120737113B (zh) * 2025-09-03 2025-11-21 湖北师范大学 一种三唑并哒嗪类化合物区域选择性c3-h炔基化的方法

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Publication number Publication date
RU2015116102A (ru) 2017-01-10
RU2665036C9 (ru) 2018-11-12
RU2665036C2 (ru) 2018-08-27
ZA201502575B (en) 2016-11-30
EP2919784A1 (en) 2015-09-23
MY180641A (en) 2020-12-04
BR112015006726B1 (pt) 2021-11-23
AU2013345107A1 (en) 2015-04-30
TW201422615A (zh) 2014-06-16
JP6268183B2 (ja) 2018-01-24
BR112015006726A2 (pt) 2017-08-22
ES2661380T3 (es) 2018-03-28
EP3299019B1 (en) 2019-10-09
CA2889346C (en) 2018-09-25
AU2013345107B2 (en) 2016-02-25
SG11201502725TA (en) 2015-05-28
HK1210956A1 (en) 2016-05-13
EP2919784A4 (en) 2016-07-06
KR20150083833A (ko) 2015-07-20
EP3299019A1 (en) 2018-03-28
CN104755085A (zh) 2015-07-01
JP2015536994A (ja) 2015-12-24
US9926324B2 (en) 2018-03-27
CN104755085B (zh) 2018-05-01
WO2014078211A1 (en) 2014-05-22
KR102148679B1 (ko) 2020-08-27
CA2889346A1 (en) 2014-05-22
US20140134133A1 (en) 2014-05-15
EP2919784B1 (en) 2017-12-20

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