CA2921395C - Diaminopyrimidine p2x3 and p2x 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough - Google Patents

Diaminopyrimidine p2x3 and p2x 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough Download PDF

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Publication number
CA2921395C
CA2921395C CA2921395A CA2921395A CA2921395C CA 2921395 C CA2921395 C CA 2921395C CA 2921395 A CA2921395 A CA 2921395A CA 2921395 A CA2921395 A CA 2921395A CA 2921395 C CA2921395 C CA 2921395C
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Prior art keywords
compound
alkyl
cough
chronic cough
methoxy
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CA2921395A
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English (en)
French (fr)
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CA2921395A1 (en
Inventor
Anthony P. FORD
Bruce G. MCCARTHY
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Afferent Pharmaceuticals Inc
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Afferent Pharmaceuticals Inc
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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
    • A61K31/495—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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2921395A 2013-08-23 2014-08-22 Diaminopyrimidine p2x3 and p2x 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough Active CA2921395C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361869174P 2013-08-23 2013-08-23
US61/869,174 2013-08-23
PCT/US2014/052389 WO2015027212A1 (en) 2013-08-23 2014-08-22 Diaminopyrimidine p2x3 and p2x 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough

Publications (2)

Publication Number Publication Date
CA2921395A1 CA2921395A1 (en) 2015-02-26
CA2921395C true CA2921395C (en) 2022-04-26

Family

ID=52480919

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2921395A Active CA2921395C (en) 2013-08-23 2014-08-22 Diaminopyrimidine p2x3 and p2x 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough

Country Status (20)

Country Link
US (3) US9284279B2 (enExample)
EP (2) EP3865134A1 (enExample)
JP (3) JP6546592B2 (enExample)
KR (1) KR102196885B1 (enExample)
CN (1) CN105682659B (enExample)
AU (1) AU2014308606B2 (enExample)
CA (1) CA2921395C (enExample)
CL (3) CL2016000400A1 (enExample)
CR (1) CR20160093A (enExample)
IL (1) IL244131B (enExample)
MX (1) MX367657B (enExample)
MY (1) MY195728A (enExample)
NI (1) NI201600029A (enExample)
NZ (1) NZ716977A (enExample)
PE (1) PE20160431A1 (enExample)
PH (1) PH12016500357A1 (enExample)
RU (1) RU2650118C2 (enExample)
SG (1) SG11201601145RA (enExample)
UA (1) UA118851C2 (enExample)
WO (1) WO2015027212A1 (enExample)

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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
JP2017505348A (ja) 2014-02-10 2017-02-16 パタラ ファーマ リミテッド ライアビリティ カンパニー 肺疾患治療のための肥満細胞安定剤
PL3104853T3 (pl) 2014-02-10 2020-05-18 Respivant Sciences Gmbh Leczenie stabilizatorami komórek tucznych zaburzeń ogólnoustrojowych
WO2017011729A1 (en) 2015-07-16 2017-01-19 Patara Pharma, LLC Combination therapies for the treatment of lung diseases
WO2017027387A1 (en) 2015-08-07 2017-02-16 Patara Pharma, LLC Methods for the treatment of mast cell related disorders with mast cell stabilizers
US10265296B2 (en) 2015-08-07 2019-04-23 Respivant Sciences Gmbh Methods for the treatment of systemic disorders treatable with mast cell stabilizers, including mast cell related disorders
CA2998742C (en) * 2015-09-29 2023-08-29 Anthony P. FORD Diaminopyrimidine p2x3 and p2x2/3 receptor modulators for use in the treatment of cough
US9907795B2 (en) * 2016-01-08 2018-03-06 Nerre Therapeutics Limited Method of treatment of chronic cough administering orvepitant in combination with other therapeutic agents
AU2017237929B2 (en) 2016-03-25 2021-04-15 Afferent Pharmaceuticals Inc. Pyrimidines and variants thereof, and uses therefor
JP2019528320A (ja) 2016-08-31 2019-10-10 レシュピファント サイエンシス ゲゼルシャフト ミット ベシュレンクター ハフトゥングＲｅｓｐｉｖａｎｔ Ｓｃｉｅｎｃｅｓ Ｇｍｂｈ 特発性肺線維症による慢性咳の治療のためのクロモリン組成物
EP3522983A4 (en) 2016-10-07 2020-06-03 Respivant Sciences GmbH CROMOLYN COMPOSITION FOR TREATING LUNG FIBROSIS
EP3554504B1 (en) 2016-12-15 2022-10-26 Afferent Pharmaceuticals Inc. Substituted pyrazole-pyrimidines, variants thereof, and uses thereof
MX381790B (es) * 2016-12-20 2025-03-13 Afferent Pharmaceuticals Inc Sales cristalinas y polimorfos de un antagonista de p2x3.
US10111883B1 (en) * 2017-09-18 2018-10-30 Bellus Health Cough Inc. Selective P2X3 modulators
CN108904507A (zh) * 2018-02-11 2018-11-30 赖英杰 P2x3受体调节剂苯并咪唑化合物在制备抗呼吸疾病药物中的应用
CN112004551A (zh) 2018-03-15 2020-11-27 丹米尔治疗有限责任公司 3”,5”-二烷氧基苯甲酰基-3’-氨基-3’-脱氧腺苷-5’-三磷酸及其药物用途
WO2019209607A1 (en) * 2018-04-23 2019-10-31 Merck Sharp & Dohme Corp. Novel process for synthesis of a phenoxy diaminopyrimidine compound
MA52616A (fr) 2018-05-15 2021-03-24 Bayer Ag Benzamides à substitution 1,3-thiazol-2-yl pour le traitement de maladies associées à la sensibilisation de fibres nerveuses
SG11202011010YA (en) * 2018-05-15 2020-12-30 Bayer Ag 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
CN118512451A (zh) * 2018-07-23 2024-08-20 特雷维治疗股份有限公司 慢性咳嗽、呼吸急促和呼吸困难的治疗
CN113164488A (zh) * 2018-10-05 2021-07-23 盐野义制药株式会社 慢性咳嗽治疗用药物
DK3880678T3 (da) 2018-11-13 2025-06-10 Glaxosmithkline Intellectual Property No 3 Ltd Krystallinske former af p2x3-modulator methyl(s)-2-((2-(2,6-difluoro-4-(methylcarbamoyl )phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholin-4-carboxylat
CA3131312A1 (en) 2019-02-25 2020-09-03 Bellus Health Cough Inc. Treatment with p2x3 modulators
EP3960179B1 (en) * 2019-04-30 2026-03-18 Beijing Tide Pharmaceutical Co., Ltd. Method for treating cough by using diaminopyrimidine compound
ES3056709T3 (en) * 2019-04-30 2026-02-24 Beijing Tide Pharmaceutical Co Ltd Salt of diaminopyrimidine compounds, and solid form thereof, preparation method therefor and use thereof
MA56022A (fr) 2019-05-31 2022-04-06 Chiesi Farm Spa Dérivés d'amino quinazoline servant d'inhibiteurs de p2x3
CN117843615A (zh) 2019-09-19 2024-04-09 盐野义制药株式会社 1,3,5-三嗪衍生物或其溶剂合物的晶体及其制造方法
IL294601A (en) 2020-01-10 2022-09-01 Trevi Therapeutics Inc Methods of administration of nalbuphine
CN111635368B (zh) * 2020-06-12 2021-06-29 东莞市东阳光仿制药研发有限公司 一种胺化合物的制备方法
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PT1725540E (pt) * 2004-03-05 2012-11-29 Hoffmann La Roche Diaminopirimidinas como antagonistas de p2x3 e p2x2/3
WO2006012639A2 (en) 2004-07-22 2006-02-02 Duska Scientific Co. Method of diagnosing, monitoring and treating pulmonary diseases
ATE529413T1 (de) * 2005-09-01 2011-11-15 Hoffmann La Roche Verfahren zur synthese von aryloxydiaminopyrimidinen
SI1924264T1 (sl) 2005-09-01 2013-12-31 F. Hoffmann-La Roche Ag Diaminopirimidini kot modulatorji p2x3 in p2x2/3
ES2612890T3 (es) * 2005-09-01 2017-05-19 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P2X2/3
ES2562056T3 (es) 2005-09-01 2016-03-02 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores P2X3 y P2X2/3
DK2343281T3 (en) * 2006-10-04 2014-03-24 Hoffmann La Roche Process for the Synthesis of Phenoxydiamino-Pyrimidine Derivatives
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
JP6124351B2 (ja) * 2012-02-09 2017-05-10 塩野義製薬株式会社 複素環および炭素環誘導体
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
US9222282B2 (en) * 2013-10-11 2015-12-29 Nexkey, Inc. Energy efficient multi-stable lock cylinder

Also Published As

Publication number Publication date
CA2921395A1 (en) 2015-02-26
KR20160052581A (ko) 2016-05-12
NI201600029A (es) 2017-09-22
SG11201601145RA (en) 2016-03-30
KR102196885B1 (ko) 2020-12-30
HK1222126A1 (zh) 2017-06-23
JP7423725B2 (ja) 2024-01-29
CN105682659B (zh) 2019-12-10
JP6546592B2 (ja) 2019-07-17
JP7210348B2 (ja) 2023-01-23
EP3035932A4 (en) 2017-01-04
RU2016105581A (ru) 2017-09-28
JP2016528301A (ja) 2016-09-15
MY195728A (en) 2023-02-07
PH12016500357A1 (en) 2016-05-16
MX2016002289A (es) 2016-09-06
JP2019112459A (ja) 2019-07-11
UA118851C2 (uk) 2019-03-25
CL2016000400A1 (es) 2017-01-20
US10206922B2 (en) 2019-02-19
EP3865134A1 (en) 2021-08-18
US20150057299A1 (en) 2015-02-26
IL244131A0 (en) 2016-04-21
US20160263112A1 (en) 2016-09-15
AU2014308606B2 (en) 2017-08-03
PE20160431A1 (es) 2016-06-02
CR20160093A (es) 2016-08-26
JP2023002662A (ja) 2023-01-10
US9724346B2 (en) 2017-08-08
IL244131B (en) 2019-06-30
WO2015027212A1 (en) 2015-02-26
US20170326142A1 (en) 2017-11-16
CL2018002138A1 (es) 2018-10-05
NZ716977A (en) 2017-09-29
MX367657B (es) 2019-08-30
AU2014308606A1 (en) 2016-03-10
CL2018002137A1 (es) 2018-10-05
EP3035932A1 (en) 2016-06-29
US9284279B2 (en) 2016-03-15
CN105682659A (zh) 2016-06-15
RU2650118C2 (ru) 2018-04-09

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