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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CA
Canada
Prior art keywords
compound
formula
mmol
mixture
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA3018180A
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English (en)
French (fr)
Other versions
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
Original Assignee
Afferent Pharmaceuticals Inc
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Filing date
Publication date
Application filed by Afferent Pharmaceuticals Inc filed Critical Afferent Pharmaceuticals Inc
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
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 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
    • C07D403/02—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

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 (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
AU2017237929B2 (en) 2016-03-25 2021-04-15 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor
CA3044366A1 (en) 2016-12-19 2018-06-28 Novartis Ag New picolinic acid derivatives and their use as intermediates
MX381790B (es) * 2016-12-20 2025-03-13 Afferent Pharmaceuticals Inc Sales cristalinas y polimorfos de un antagonista de p2x3.
CN117186068A (zh) 2017-11-01 2023-12-08 北京泰德制药股份有限公司 P2x3和/或p2x2/3受体拮抗剂、包含其的药物组合物及其用途
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
EP3964505B1 (en) * 2019-04-30 2025-10-15 Beijing Tide Pharmaceutical Co., Ltd. Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof
SG11202111960PA (en) * 2019-04-30 2021-12-30 Beijing Tide Pharmaceutical Co Ltd Method for treating endometriosis-associated pain by using diaminopyrimidine compound
EP3960179B1 (en) * 2019-04-30 2026-03-18 Beijing Tide Pharmaceutical Co., Ltd. Method for treating cough by using diaminopyrimidine compound
US12595261B2 (en) 2019-06-06 2026-04-07 Beijing Tide Pharmaceutical Co., Ltd. P2X3 and/or P2X2/3 receptor antagonist, pharmaceutical composition containing same, and use thereof
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
EP1165522A1 (en) * 1999-04-06 2002-01-02 Krenitsky Pharmaceuticals, Inc. Neurotrophic thio substituted pyrimidines
BR0116493A (pt) * 2000-12-21 2003-09-30 Vertex Pharma Compostos de pirazol úteis como inibidores de proteìna cinase
PT1725540E (pt) * 2004-03-05 2012-11-29 Hoffmann La Roche Diaminopirimidinas como antagonistas de p2x3 e p2x2/3
AU2006286576B2 (en) * 2005-09-01 2012-06-14 F. Hoffmann-La Roche Ag Diaminopyrimidines as P2X3 and P3X2/3 modulators
ES2562056T3 (es) 2005-09-01 2016-03-02 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores P2X3 y P2X2/3
ES2612890T3 (es) * 2005-09-01 2017-05-19 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P2X2/3
SI1924264T1 (sl) * 2005-09-01 2013-12-31 F. Hoffmann-La Roche Ag Diaminopirimidini kot modulatorji p2x3 in p2x2/3
DK2343281T3 (en) * 2006-10-04 2014-03-24 Hoffmann La Roche Process for the Synthesis of Phenoxydiamino-Pyrimidine Derivatives
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
JP5423679B2 (ja) * 2007-10-31 2014-02-19 日産化学工業株式会社 ピリダジノン化合物及びp2x7受容体阻害剤
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
PE20160431A1 (es) * 2013-08-23 2016-06-02 Afferent Pharmaceuticals Inc Moduladores del receptor p2x3 y p2x2/3 de diaminopiridina para el tratamiento de la tos aguda, sub-aguda o cronica
US10195198B2 (en) * 2014-07-03 2019-02-05 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
AU2017237929B2 (en) 2016-03-25 2021-04-15 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor

Also Published As

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

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