AU2014308606B2 - 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
AU2014308606B2
AU2014308606B2 AU2014308606A AU2014308606A AU2014308606B2 AU 2014308606 B2 AU2014308606 B2 AU 2014308606B2 AU 2014308606 A AU2014308606 A AU 2014308606A AU 2014308606 A AU2014308606 A AU 2014308606A AU 2014308606 B2 AU2014308606 B2 AU 2014308606B2
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cough
compound
formula
isopropyl
mmol
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Anthony P. FORD
Bruce G. MCCARTHY
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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
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0043Nose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2014308606A 2013-08-23 2014-08-22 Diaminopyrimidine P2X3 and P2X 2/3 receptor modulators for treatment of acute, sub-acute or chronic cough Active AU2014308606B2 (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

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AU2014308606A1 AU2014308606A1 (en) 2016-03-10
AU2014308606B2 true AU2014308606B2 (en) 2017-08-03

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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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JP6546592B2 (ja) * 2013-08-23 2019-07-17 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 急性、亜急性または慢性の咳を治療するためのジアミノピリミジンp2x3およびp2x2/3受容体モジュレーター
EP3725311A1 (en) 2014-02-10 2020-10-21 Respivant Sciences GmbH Methods for the treatment of lung diseases with mast cell stabilizers
EP3653207A1 (en) 2014-02-10 2020-05-20 Respivant Sciences GmbH Mast cell stabilizers treatment for systemic disorders
WO2017011729A1 (en) 2015-07-16 2017-01-19 Patara Pharma, LLC Combination therapies for the treatment of lung diseases
EP3331522A1 (en) 2015-08-07 2018-06-13 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
HUE061764T2 (hu) * 2015-09-29 2023-08-28 Afferent Pharmaceuticals Inc Diaminopirimidin-P2X3 és P2X2/3 receptor modulátorok felhasználásra köhögés kezelésében
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
US10662162B2 (en) * 2016-03-25 2020-05-26 Afferent Pharmaceuticals, Inc. Pyrimidines and variants thereof, and uses therefor
CN110139646A (zh) 2016-08-31 2019-08-16 瑞思皮万特科学有限责任公司 用于治疗由特发性肺纤维化引起的慢性咳嗽的色甘酸组合物
WO2018067341A1 (en) 2016-10-07 2018-04-12 Patara Pharma, LLC Cromolyn compositions for treatment of pulmonary fibrosis
EP3554504B1 (en) 2016-12-15 2022-10-26 Afferent Pharmaceuticals Inc. Substituted pyrazole-pyrimidines, variants thereof, and uses thereof
RU2021120039A (ru) * 2016-12-20 2021-08-03 Эфферент Фармасьютикалз, Инк. Кристаллические соли и полиморфы антагониста 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
CA3093409A1 (en) 2018-03-15 2019-09-19 Danmir Therapeutics, Llc 3",5"-dialkoxybenzoyl-3'-amino-3'-deoxyadenosine-5'-triphosphates and pharmaceutical uses thereof
CA3096505A1 (en) * 2018-04-23 2019-10-31 Merck Sharp & Dohme Corp. Novel process for synthesis of a phenoxy diaminopyrimidine compound
CA3100096A1 (en) 2018-05-15 2019-11-21 Bayer Aktiengesellschaft 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
JP2021523919A (ja) * 2018-05-15 2021-09-09 バイエル アクチェンゲゼルシャフトBayer Aktiengesellschaft 神経線維感作に関連する疾患を治療するための1,3−チアゾール−2−イル置換ベンズアミド
MX2021000908A (es) 2018-07-23 2021-06-08 Trevi Therapeutics Inc Tratamiento de la tos cronica, la dificultad respiratoria y la disnea.
PL3862000T3 (pl) * 2018-10-05 2024-03-18 Shionogi & Co., Ltd Lek na przewlekły kaszel
WO2020174283A1 (en) 2019-02-25 2020-09-03 Bellus Health Cough Inc. Treatment with p2x3 modulators
US20220211703A1 (en) * 2019-04-30 2022-07-07 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
MX2022002941A (es) 2019-09-19 2022-04-06 Shionogi & Co Cristal de derivado de 1,3,5-triazina o solvato del mismo y metodo para producir el mismo.
MX2022008554A (es) 2020-01-10 2022-08-10 Trevi Therapeutics Inc Metodos de administracion de nalbufina.
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
WO2024080126A1 (ja) 2022-10-12 2024-04-18 ソフトバンクグループ株式会社 情報処理システム、情報処理装置、制御装置及びプログラム

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Also Published As

Publication number Publication date
JP2023002662A (ja) 2023-01-10
HK1222126A1 (zh) 2017-06-23
KR20160052581A (ko) 2016-05-12
CR20160093A (es) 2016-08-26
UA118851C2 (uk) 2019-03-25
CL2018002137A1 (es) 2018-10-05
JP2019112459A (ja) 2019-07-11
US20150057299A1 (en) 2015-02-26
EP3035932A1 (en) 2016-06-29
RU2016105581A (ru) 2017-09-28
EP3865134A1 (en) 2021-08-18
MX367657B (es) 2019-08-30
EP3035932A4 (en) 2017-01-04
JP7210348B2 (ja) 2023-01-23
JP2016528301A (ja) 2016-09-15
MX2016002289A (es) 2016-09-06
US20160263112A1 (en) 2016-09-15
CA2921395C (en) 2022-04-26
NI201600029A (es) 2017-09-22
US9284279B2 (en) 2016-03-15
JP7423725B2 (ja) 2024-01-29
IL244131B (en) 2019-06-30
PH12016500357A1 (en) 2016-05-16
IL244131A0 (en) 2016-04-21
KR102196885B1 (ko) 2020-12-30
JP6546592B2 (ja) 2019-07-17
PE20160431A1 (es) 2016-06-02
CN105682659B (zh) 2019-12-10
CN105682659A (zh) 2016-06-15
US10206922B2 (en) 2019-02-19
SG11201601145RA (en) 2016-03-30
CA2921395A1 (en) 2015-02-26
AU2014308606A1 (en) 2016-03-10
CL2016000400A1 (es) 2017-01-20
CL2018002138A1 (es) 2018-10-05
WO2015027212A1 (en) 2015-02-26
MY195728A (en) 2023-02-07
NZ716977A (en) 2017-09-29
US20170326142A1 (en) 2017-11-16
RU2650118C2 (ru) 2018-04-09
US9724346B2 (en) 2017-08-08

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