AU2015321654B2 - Heterocyclic compounds and use thereof - Google Patents

Heterocyclic compounds and use thereof Download PDF

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AU2015321654B2
AU2015321654B2 AU2015321654A AU2015321654A AU2015321654B2 AU 2015321654 B2 AU2015321654 B2 AU 2015321654B2 AU 2015321654 A AU2015321654 A AU 2015321654A AU 2015321654 A AU2015321654 A AU 2015321654A AU 2015321654 B2 AU2015321654 B2 AU 2015321654B2
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compound
alkyl
heteroaryl
aryl
heterocycloalkyl
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AU2015321654A1 (en
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Yu-Sheng Chao
Chiung-Tong Chen
Jiing-Jyh Jan
Kak-Shan Shia
Lun Kelvin Tsou
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National Health Research Institutes
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
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  • Rheumatology (AREA)
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AU2015321654A 2014-09-22 2015-09-21 Heterocyclic compounds and use thereof Active AU2015321654B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462053389P 2014-09-22 2014-09-22
US62/053,389 2014-09-22
PCT/US2015/051143 WO2016048861A2 (en) 2014-09-22 2015-09-21 Heterocyclic compounds and use thereof

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AU2015321654A1 AU2015321654A1 (en) 2017-04-06
AU2015321654B2 true AU2015321654B2 (en) 2019-10-31

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US (2) US9862703B2 (enExample)
EP (1) EP3197885B1 (enExample)
JP (1) JP6615207B2 (enExample)
KR (1) KR102509431B1 (enExample)
CN (1) CN107207465B (enExample)
AU (1) AU2015321654B2 (enExample)
BR (1) BR112017005713B1 (enExample)
CA (1) CA2962329C (enExample)
ES (1) ES2849998T3 (enExample)
RU (1) RU2704008C2 (enExample)
TW (1) TWI598348B (enExample)
WO (1) WO2016048861A2 (enExample)

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AU2018208366B2 (en) * 2017-01-10 2020-12-17 National Health Research Institutes Heterocyclic compounds and use thereof
EA202090595A1 (ru) * 2017-09-08 2020-06-29 Дзе Борд Оф Трастиз Оф Дзе Лелэнд Стэнфорд Джуниор Юниверсити Ингибиторы enpp1 и способы модуляции иммунного ответа
EP3842435A4 (en) 2018-09-20 2022-05-11 Hanmi Pharm. Co., Ltd. NOVEL SULFONAMIDE DERIVATIVE WITH FUSED PYRIMIDINE FRAMEWORK WITH INHIBITING ACTIVITY ON EPIDERMAL GROWTH FACTOR RECEPTOR MUTATIONS
MX2021009269A (es) * 2019-02-01 2021-08-24 Univ Leland Stanford Junior Inhibidores de enpp1 y metodos para modular una respuesta inmunitaria.
CN111961034A (zh) 2019-05-20 2020-11-20 浙江同源康医药股份有限公司 用作ret激酶抑制剂的化合物及其应用
CN111138417B (zh) * 2019-12-18 2021-03-23 浙江工业大学 一种三氮唑修饰的5-氟-2,4-嘧啶二胺类化合物及其应用
WO2023014611A1 (en) * 2021-08-02 2023-02-09 Yeh, Teng-Kuang Pyrimidine compounds and use thereof
KR20250093507A (ko) * 2022-11-07 2025-06-24 고쿠리츠 다이가쿠 호진 교토 다이가쿠 퀴나졸린 유도체
TW202435887A (zh) 2023-03-01 2024-09-16 瑞士商諾華公司 用於治療疾病或障礙的氫喹唑啉衍生物

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CAS Registry Number 744986-10-5; STN Entry Date 15 September 2004; 2,4-di(piperazin-1-yl)-6-thiomorpholinopyrimidine-5-carbonitrile *
CAS Registry Number 746594-35-4; STN Entry Date 17 September 2004; 1,1'-(pyrimidine-2,4-diylbis(piperazine-4,1-diyl))bis(2-chloroethan-1-one) *
CAS Registry Number 747351-91-3; STN Entry Date 17 September 2004; 6-(4-formylpiperazin-1-yl)-2-(piperazin-1-yl)pyrimidine-4-carbonitrile *
CAS Registry Number 923221-53-8; STN Entry Date 26 February 2007; (4-(4-methyl-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl)piperazin-1-yl)(phenyl)methanone *
COWDEN, W. B. et. al., "Pyrimidine N-Oxides. II* The synthesis of some amino- and imino-pyrimidine N-oxides and related compounds", Aust. J. Chem., (1979), vol. 32, pages 2049 - 2057 *
LEE, O et. al., "Electrophillic condensation of pyrimidines with cyclic ketones", Tetrahedron Letters, (1997), vol. 38., no. 36, pages 6401 - 6404 *
POPOVA, L. M. et al., "Synthesis and properties of 2,4-disubstituted 6- fluoropyrimidines", Russian Journal of Organic Chemistry, (1996), vol. 32, no. 9, pages 1424 - 1428 *

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