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)
  • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (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) EP3035932A4 (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)

Families Citing this family (28)

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CR20160093A (es) * 2013-08-23 2016-08-26 Afferent Pharmaceuticals Inc Moduladores del receptor p2x3 y p2x2/3 de diaminopiridina para el tratamiento de la tos aguda, sub aguda o cronica
CN106535889A (zh) 2014-02-10 2017-03-22 帕塔拉制药有限责任公司 用于治疗肺疾病的肥大细胞稳定剂
CA2938994A1 (en) 2014-02-10 2015-08-13 Patara Pharma, LLC Inhalable formulations of sodium cromolyn with improved bioavailability
WO2017011729A1 (en) 2015-07-16 2017-01-19 Patara Pharma, LLC Combination therapies for the treatment of lung diseases
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
EP3331522A1 (en) 2015-08-07 2018-06-13 Patara Pharma LLC Methods for the treatment of mast cell related disorders with mast cell stabilizers
PT3355889T (pt) 2015-09-29 2023-04-26 Afferent Pharmaceuticals Inc Moduladores de recetores de diaminopirimidina p2x3 e p2x2/3 para utilização no tratamento da tosse
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
CA3018180C (en) * 2016-03-25 2024-02-20 Ronald Charles Hawley Pyrimidines and variants thereof, and uses therefor
EP3506893A4 (en) 2016-08-31 2020-01-22 Respivant Sciences GmbH CROMOLYN COMPOSITIONS FOR THE TREATMENT OF CHRONIC COUGH DUE TO IDIOPATHIC PULMONAL FIBROSIS
AU2017339366A1 (en) 2016-10-07 2019-04-11 Respivant Sciences Gmbh 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
US10676444B2 (en) * 2016-12-20 2020-06-09 Afferent Pharmaceuticals, Inc. Crystalline salts and polymorphs of a P2X3 antagonist
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
IL277024B (en) 2018-03-15 2022-09-01 Danmir Therapeutics Llc 3" ,5" -dialkoxybenzoyl-3'-amino-3'-deoxyadenosine-5'-triphosphates and pharmaceutical uses thereof
AU2019257606B2 (en) * 2018-04-23 2025-01-30 Msd Werthenstein Biopharma Gmbh Novel process for synthesis of a phenoxy diaminopyrimidine compound
JP2021523201A (ja) 2018-05-15 2021-09-02 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
KR20210009341A (ko) 2018-05-15 2021-01-26 바이엘 악티엔게젤샤프트 신경 섬유 감작과 연관된 질환의 치료를 위한 1,3-티아졸-2-일 치환된 벤즈아미드
IL318587A (en) * 2018-07-23 2025-03-01 Trevi Therapeutics Inc Treatment of chronic cough, shortness of breath and wheezing
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
CN114008027B (zh) * 2019-04-30 2024-02-20 北京泰德制药股份有限公司 二氨基嘧啶类化合物的盐、其固体形式及其制备方法和用途
SG11202111877TA (en) * 2019-04-30 2021-11-29 Beijing Tide Pharmaceutical Co Ltd Method for treating cough by using diaminopyrimidine compound
US12312327B2 (en) 2019-09-19 2025-05-27 Shionogi & Co., Ltd. Crystal of 1,3,5-triazine derivative or solvate thereof and method for producing same
CA3166928A1 (en) 2020-01-10 2021-07-15 Trevi Therapeutics, Inc. Methods of administering 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
CN120019423A (zh) 2022-10-12 2025-05-16 软银集团股份有限公司 信息处理系统、信息处理装置、控制装置及程序

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ES2391636T3 (es) 2004-03-05 2012-11-28 F. Hoffmann-La Roche Ag Diaminopirimidinas como antagonistas de P2X3 y P2X2/3
EP1773405A4 (en) 2004-07-22 2011-10-05 Duska Scient Co METHOD FOR DIAGNOSIS, MONITORING AND TREATMENT OF LUNG DISEASES
KR101012926B1 (ko) * 2005-09-01 2011-02-09 에프. 호프만-라 로슈 아게 Ｐ2ｘ3 및 ｐ2ｘ2/3 조정자로서의 다이아미노피리미딘
WO2007025901A1 (en) 2005-09-01 2007-03-08 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
CN101253158B (zh) 2005-09-01 2013-07-10 弗·哈夫曼-拉罗切有限公司 合成芳氧基二氨基嘧啶类化合物的方法
ES2612890T3 (es) * 2005-09-01 2017-05-19 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P2X2/3
JP5128603B2 (ja) 2006-10-04 2013-01-23 エフ．ホフマン−ラ ロシュ アーゲー フェノキシジアミノピリミジン誘導体の合成方法
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
US9550763B2 (en) * 2012-02-09 2017-01-24 Shionogi & Co., Ltd. Heterocyclic ring and carbocyclic derivative
CR20160093A (es) 2013-08-23 2016-08-26 Afferent Pharmaceuticals Inc Moduladores del receptor p2x3 y p2x2/3 de diaminopiridina para el tratamiento de la tos aguda, sub aguda o cronica
US9133647B2 (en) * 2013-10-11 2015-09-15 Nexkey, Inc. NFC or BLE based contactless lock with charge monitoring of its energy storage

Also Published As

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

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