AU2017237929B2 - Pyrimidines and variants thereof, and uses therefor - Google Patents

Pyrimidines and variants thereof, and uses therefor Download PDF

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Publication number
AU2017237929B2
AU2017237929B2 AU2017237929A AU2017237929A AU2017237929B2 AU 2017237929 B2 AU2017237929 B2 AU 2017237929B2 AU 2017237929 A AU2017237929 A AU 2017237929A AU 2017237929 A AU2017237929 A AU 2017237929A AU 2017237929 B2 AU2017237929 B2 AU 2017237929B2
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compound
mmol
mixture
formula
added
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AU2017237929A1 (en
Inventor
Anthony P. FORD
Joel R. Gever
Ronald Charles Hawley
Prabha Ibrahim
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Afferent Pharmaceuticals Inc
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Afferent Pharmaceuticals Inc
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50Three nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2017237929A 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor Active AU2017237929B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662313334P 2016-03-25 2016-03-25
US62/313,334 2016-03-25
PCT/US2017/023126 WO2017165255A1 (en) 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor

Publications (2)

Publication Number Publication Date
AU2017237929A1 AU2017237929A1 (en) 2018-09-13
AU2017237929B2 true AU2017237929B2 (en) 2021-04-15

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Family Applications (1)

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AU2017237929A Active AU2017237929B2 (en) 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor

Country Status (11)

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US (2) US10662162B2 (enExample)
EP (1) EP3433258B1 (enExample)
JP (1) JP6902045B2 (enExample)
KR (1) KR102377805B1 (enExample)
CN (1) CN108779119B (enExample)
AU (1) AU2017237929B2 (enExample)
CA (1) CA3018180C (enExample)
MA (1) MA44489A (enExample)
MX (1) MX384368B (enExample)
RU (1) RU2760733C2 (enExample)
WO (1) WO2017165255A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10822311B2 (en) 2016-03-14 2020-11-03 Afferent Pharmaceuticals, Inc. Pyrimidines and variants thereof, and uses therefor
WO2017165255A1 (en) * 2016-03-25 2017-09-28 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor
WO2018116139A1 (en) 2016-12-19 2018-06-28 Novartis Ag New picolinic acid derivatives and their use as intermediates
JP6934945B2 (ja) * 2016-12-20 2021-09-15 アファレント ファーマシューティカルズ インコーポレイテッド P2x3アンタゴニストの結晶塩および多形
CA3076680A1 (en) * 2017-11-01 2019-05-09 Beijing Tide Pharmaceutical Co., Ltd. P2x3 and/or p2x2/3 receptor antagonist, pharmaceutical composition comprising same, and use thereof
CN107778255B (zh) * 2017-11-16 2019-10-25 山东大学 一种二芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法和应用
CN114007620B (zh) * 2019-04-30 2024-08-06 北京泰德制药股份有限公司 二氨基嘧啶类化合物治疗子宫内膜异位相关的疼痛的方法
MX2021013338A (es) * 2019-04-30 2022-01-24 Beijing Tide Pharmaceutical Co Ltd Método para tratar la tos usando un compuesto de diaminopirimidina.
SG11202111907UA (en) * 2019-04-30 2021-11-29 Beijing Tide Pharmaceutical Co Ltd Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof
EP3981765A4 (en) * 2019-06-06 2023-05-31 Beijing Tide Pharmaceutical Co., Ltd. P2X3 AND/OR P2X2/3 RECEPTOR ANTAGONIST, PHARMACEUTICAL COMPOSITION CONTAINING IT AND THEIR USE
CN120058573A (zh) * 2025-04-29 2025-05-30 潍坊学院 一种1-三溴甲基磺酰基萘及其衍生物的合成方法

Citations (7)

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Publication number Priority date Publication date Assignee Title
WO2000059893A1 (en) * 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
WO2005095359A1 (en) * 2004-03-05 2005-10-13 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
WO2007025900A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p3x2/3 modulators
WO2007025899A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2007025925A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2007025901A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2017160569A1 (en) * 2016-03-14 2017-09-21 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor

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US2953567A (en) * 1956-11-23 1960-09-20 Burroughs Wellcome Co 5-phenylmercaptopyrimidines and method
CA2432799C (en) * 2000-12-21 2008-08-19 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SI2343281T1 (sl) * 2006-10-04 2014-06-30 F. Hoffmann-La Roche Ag Postopek za sintezo fenoksi diaminopirimidinskih derivatov
WO2008104472A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
CN101842359A (zh) * 2007-10-31 2010-09-22 日产化学工业株式会社 哒嗪酮化合物和p2x7受体抑制剂
GB2471713A (en) 2009-07-08 2011-01-12 Univ Greenwich 1,2,4-triazine derivatives and their use as sodium channel blockers
TWI637949B (zh) * 2013-06-14 2018-10-11 塩野義製藥股份有限公司 胺基三衍生物及含有其等之醫藥組合物
MX367657B (es) * 2013-08-23 2019-08-30 Afferent Pharmaceuticals Inc Moduladores del receptor p2x3 y p2x2/3 de diaminopiridina para el tratamiento de la tos aguda, sub-aguda o crónica.
US10195198B2 (en) * 2014-07-03 2019-02-05 Afferent Pharmaceuticals, Inc. Methods and compositions for treating diseases and conditions
WO2017165255A1 (en) 2016-03-25 2017-09-28 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor

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WO2000059893A1 (en) * 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
WO2005095359A1 (en) * 2004-03-05 2005-10-13 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
WO2007025900A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p3x2/3 modulators
WO2007025899A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2007025925A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2007025901A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
WO2017160569A1 (en) * 2016-03-14 2017-09-21 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor

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Falco, E. A. et al., 5-Arylthiopyrimidines. I. 2, 4-Diamino derivatives; Journal of Organic Chemistry, 1961, 26, 1143-6. *
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Also Published As

Publication number Publication date
KR20180128015A (ko) 2018-11-30
WO2017165255A1 (en) 2017-09-28
CN108779119A (zh) 2018-11-09
RU2760733C2 (ru) 2021-11-30
MX2018011622A (es) 2019-03-28
US10662162B2 (en) 2020-05-26
JP6902045B2 (ja) 2021-07-14
MA44489A (fr) 2019-01-30
EP3433258A1 (en) 2019-01-30
MX384368B (es) 2025-03-14
RU2018137032A (ru) 2020-04-27
CA3018180C (en) 2024-02-20
JP2019510025A (ja) 2019-04-11
US11230532B2 (en) 2022-01-25
US20200239421A1 (en) 2020-07-30
RU2018137032A3 (enExample) 2020-05-22
KR102377805B1 (ko) 2022-03-22
CN108779119B (zh) 2022-02-08
EP3433258A4 (en) 2019-10-30
EP3433258B1 (en) 2023-07-19
BR112018069105A2 (pt) 2019-01-29
AU2017237929A1 (en) 2018-09-13
US20190055202A1 (en) 2019-02-21
CA3018180A1 (en) 2017-09-28

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