CA3018180C - Pyrimidines and variants thereof, and uses therefor - Google Patents

Pyrimidines and variants thereof, and uses therefor Download PDF

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Publication number
CA3018180C
CA3018180C CA3018180A CA3018180A CA3018180C CA 3018180 C CA3018180 C CA 3018180C CA 3018180 A CA3018180 A CA 3018180A CA 3018180 A CA3018180 A CA 3018180A CA 3018180 C CA3018180 C CA 3018180C
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Canada
Prior art keywords
compound
formula
mmol
mixture
alkyl
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CA3018180A
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English (en)
French (fr)
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CA3018180A1 (en
Inventor
Ronald Charles Hawley
Prabha Ibrahim
Anthony P. FORD
Joel R. Gever
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Afferent Pharmaceuticals Inc
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Afferent Pharmaceuticals Inc
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Publication of CA3018180A1 publication Critical patent/CA3018180A1/en
Application granted granted Critical
Publication of CA3018180C publication Critical patent/CA3018180C/en
Active legal-status Critical Current
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Classifications

    • 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
    • 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
    • C07D239/50Three 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)
CA3018180A 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor Active CA3018180C (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
CA3018180A1 CA3018180A1 (en) 2017-09-28
CA3018180C true CA3018180C (en) 2024-02-20

Family

ID=59900805

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3018180A Active CA3018180C (en) 2016-03-25 2017-03-20 Pyrimidines and variants thereof, and uses therefor

Country Status (11)

Country Link
US (2) US10662162B2 (cg-RX-API-DMAC7.html)
EP (1) EP3433258B1 (cg-RX-API-DMAC7.html)
JP (1) JP6902045B2 (cg-RX-API-DMAC7.html)
KR (1) KR102377805B1 (cg-RX-API-DMAC7.html)
CN (1) CN108779119B (cg-RX-API-DMAC7.html)
AU (1) AU2017237929B2 (cg-RX-API-DMAC7.html)
CA (1) CA3018180C (cg-RX-API-DMAC7.html)
MA (1) MA44489A (cg-RX-API-DMAC7.html)
MX (1) MX384368B (cg-RX-API-DMAC7.html)
RU (1) RU2760733C2 (cg-RX-API-DMAC7.html)
WO (1) WO2017165255A1 (cg-RX-API-DMAC7.html)

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
KR102377805B1 (ko) 2016-03-25 2022-03-22 애퍼런트 파마슈티컬스 인크. 피리미딘 및 그의 변이체, 및 그의 용도
AU2017381739B2 (en) 2016-12-19 2020-06-11 Novartis Ag New picolinic acid derivatives and their use as intermediates
US10676444B2 (en) * 2016-12-20 2020-06-09 Afferent Pharmaceuticals, Inc. Crystalline salts and polymorphs of a P2X3 antagonist
US11414444B2 (en) 2017-11-01 2022-08-16 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
KR20220008286A (ko) * 2019-04-30 2022-01-20 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 디아미노피리미딘 화합물을 사용하여 자궁내막증-관련 통증 치료 방법
WO2020221275A1 (zh) * 2019-04-30 2020-11-05 北京泰德制药股份有限公司 二氨基嘧啶类化合物或其水合物的固体形式及其制备方法和用途
US20220211703A1 (en) * 2019-04-30 2022-07-07 Beijing Tide Pharmaceutical Co., Ltd. Method for treating cough by using diaminopyrimidine compound
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
CN120058573B (zh) * 2025-04-29 2025-12-23 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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2953567A (en) * 1956-11-23 1960-09-20 Burroughs Wellcome Co 5-phenylmercaptopyrimidines and method
WO2000059893A1 (en) * 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
EP1345926B1 (en) 2000-12-21 2006-05-17 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2005229331B2 (en) * 2004-03-05 2011-10-13 F. Hoffmann-La Roche Ag Diaminopyrimidines as P2X3 and P2X2/3 antagonists
WO2007025899A1 (en) * 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
EP1924566B1 (en) * 2005-09-01 2016-01-13 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
BRPI0615040A2 (pt) * 2005-09-01 2011-04-26 Hoffmann La Roche diaminopirimidinas como moduladores de p2x3 e p2x2/3
EP1924565B1 (en) * 2005-09-01 2016-09-14 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p3x2/3 modulators
EP2079713B1 (en) * 2006-10-04 2014-04-16 F. Hoffmann-La Roche AG Process for synthesis of phenoxy diaminopyrimidine derivatives
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
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
AU2008319735A1 (en) * 2007-10-31 2009-05-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as P2X7 receptor inhibitors
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
NZ716977A (en) * 2013-08-23 2017-09-29 Afferent Pharmaceuticals Inc Methods of using diaminopyrimidine p2x3 and p2x2/3 receptor modulators for treatment of acute and sub-acute cough, urge to cough and chronic cough, in respiratory diseases
EP3981406A1 (en) * 2014-07-03 2022-04-13 Afferent Pharmaceuticals Inc. Methods and compositions for treating diseases and conditions
US10822311B2 (en) * 2016-03-14 2020-11-03 Afferent Pharmaceuticals, Inc. Pyrimidines and variants thereof, and uses therefor
KR102377805B1 (ko) * 2016-03-25 2022-03-22 애퍼런트 파마슈티컬스 인크. 피리미딘 및 그의 변이체, 및 그의 용도

Also Published As

Publication number Publication date
RU2760733C2 (ru) 2021-11-30
MA44489A (fr) 2019-01-30
CN108779119B (zh) 2022-02-08
US20200239421A1 (en) 2020-07-30
MX2018011622A (es) 2019-03-28
US10662162B2 (en) 2020-05-26
US20190055202A1 (en) 2019-02-21
MX384368B (es) 2025-03-14
EP3433258B1 (en) 2023-07-19
AU2017237929B2 (en) 2021-04-15
JP6902045B2 (ja) 2021-07-14
AU2017237929A1 (en) 2018-09-13
KR102377805B1 (ko) 2022-03-22
JP2019510025A (ja) 2019-04-11
EP3433258A4 (en) 2019-10-30
RU2018137032A3 (cg-RX-API-DMAC7.html) 2020-05-22
EP3433258A1 (en) 2019-01-30
WO2017165255A1 (en) 2017-09-28
RU2018137032A (ru) 2020-04-27
CA3018180A1 (en) 2017-09-28
KR20180128015A (ko) 2018-11-30
BR112018069105A2 (pt) 2019-01-29
US11230532B2 (en) 2022-01-25
CN108779119A (zh) 2018-11-09

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