JP6746569B2 - 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶 - Google Patents

嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶 Download PDF

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JP6746569B2
JP6746569B2 JP2017518552A JP2017518552A JP6746569B2 JP 6746569 B2 JP6746569 B2 JP 6746569B2 JP 2017518552 A JP2017518552 A JP 2017518552A JP 2017518552 A JP2017518552 A JP 2017518552A JP 6746569 B2 JP6746569 B2 JP 6746569B2
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glyceryl
compound
crystal
cftr
glycerol
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JP2017530175A5 (enExample
JP2017530175A (ja
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マルク・シュトローマイアー
ジョン・ピー・シーザー・ジュニア
パトリック・レイモンド・コネリー
マジェド・ファワズ
エドゥアルド・ルス−ルシス
ブライアン・アール・マクレイン
アレス・メデク
ミャオ・ハイ
クワメ・ウィレドゥ・ンティ−アダエ
イン・ピン
ユエガン・ジャン
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Vertex Pharmaceuticals Inc
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Vertex 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/225—Polycarboxylic acids
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12—Acetic acid esters
    • C07C69/18—Acetic acid esters of trihydroxylic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
    • C07C69/30—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/34—Esters of acyclic saturated polycarboxylic acids having an esterified carboxyl group bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52—Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/533—Monocarboxylic acid esters having only one carbon-to-carbon double bond
    • C07C69/58—Esters of straight chain acids with eighteen carbon atoms in the acid moiety
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52—Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/587—Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017518552A 2014-10-07 2015-10-07 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶 Active JP6746569B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462060828P 2014-10-07 2014-10-07
US62/060,828 2014-10-07
PCT/US2015/054577 WO2016057730A1 (en) 2014-10-07 2015-10-07 Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator

Publications (3)

Publication Number Publication Date
JP2017530175A JP2017530175A (ja) 2017-10-12
JP2017530175A5 JP2017530175A5 (enExample) 2018-11-15
JP6746569B2 true JP6746569B2 (ja) 2020-08-26

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JP2017518552A Active JP6746569B2 (ja) 2014-10-07 2015-10-07 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶

Country Status (12)

Country Link
US (1) US9701639B2 (enExample)
EP (1) EP3204358B1 (enExample)
JP (1) JP6746569B2 (enExample)
KR (1) KR20170063954A (enExample)
CN (1) CN107250113B (enExample)
AU (1) AU2015330923B2 (enExample)
CA (1) CA2963945C (enExample)
ES (1) ES2702288T3 (enExample)
IL (1) IL251623B (enExample)
MX (1) MX370450B (enExample)
RU (1) RU2749213C2 (enExample)
WO (1) WO2016057730A1 (enExample)

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WO2007079139A2 (en) 2005-12-28 2007-07-12 Vertex Pharmaceuticals, Inc. Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
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PL2578571T3 (pl) 2007-11-16 2016-03-31 Vertex Pharma Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP
ES2604555T3 (es) 2007-12-07 2017-03-07 Vertex Pharmaceuticals Incorporated Procedimiento para producir ácidos cicloalquilcarboxiamido-piridinabenzoicos
KR20160040745A (ko) 2007-12-07 2016-04-14 버텍스 파마슈티칼스 인코포레이티드 3-(6-(1-(2,2-디플루오로벤조[ｄ][1,3]디옥솔-5-일)사이클로프로판카복스아미도)-3-메틸피리딘-2-일)벤조산의 고체 형태
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AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
WO2015073231A1 (en) 2013-11-12 2015-05-21 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases
KR102447581B1 (ko) 2014-04-15 2022-09-28 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물
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RU2749213C2 (ru) 2014-10-07 2021-06-07 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе
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US10570115B2 (en) 2016-09-30 2020-02-25 Vertex Pharmaceuticals Incorporated Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
HRP20201946T1 (hr) 2016-12-09 2021-01-22 Vertex Pharmaceuticals Incorporated Modulator regulatora transmembranske provodljivosti cistične fibroze, farmaceutski sastavi, postupci liječenja, i postupak za dobivanje modulatora
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US11517564B2 (en) 2017-07-17 2022-12-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
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MA51039A (fr) 2017-12-08 2020-10-14 Vertex Pharma Procédés pour préparer des modulateurs du régulateur de la conductance transmembranaire de la mucoviscidose
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
MD3752510T2 (ro) 2018-02-15 2023-06-30 Vertex Pharma Macrociclii ca modulatori ai regulatorului conductanței transmembranare în fibroza chistică, compoziții farmaceutice ale acestora, utilizarea lor în tratamentul fibrozei chistice, și procedeu pentru fabricarea acestora
EP3774825A1 (en) 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
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CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
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CN116410131B (zh) * 2021-12-31 2025-09-23 山东新时代药业有限公司 米力农药物共晶体及其制备方法

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