BR112018011103A2 - medicamento para tratar a gripe caracterizada por combinação de inibidor de endonuclease dependente de cap e de fármaco antigripe - Google Patents

medicamento para tratar a gripe caracterizada por combinação de inibidor de endonuclease dependente de cap e de fármaco antigripe

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Publication number
BR112018011103A2
BR112018011103A2 BR112018011103-1A BR112018011103A BR112018011103A2 BR 112018011103 A2 BR112018011103 A2 BR 112018011103A2 BR 112018011103 A BR112018011103 A BR 112018011103A BR 112018011103 A2 BR112018011103 A2 BR 112018011103A2
Authority
BR
Brazil
Prior art keywords
hydrogen
influenza
halogen
alkyl
medicine
Prior art date
Application number
BR112018011103-1A
Other languages
English (en)
Japanese (ja)
Inventor
Shishido Takao
NOSHI Takeshi
Yamamoto Atsuko
KITANO Mitsutaka
Original Assignee
Shionogi & Co., Ltd.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Shionogi & Co., Ltd. filed Critical Shionogi & Co., Ltd.
Publication of BR112018011103A2 publication Critical patent/BR112018011103A2/pt

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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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K31/13—Amines
    • 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
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • A—HUMAN NECESSITIES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • 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
    • A61K31/4965—Non-condensed pyrazines
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    • 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
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/66—Phosphorus compounds
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    • A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
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    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7012—Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
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    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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    • 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
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Abstract

um medicamento caracterizado pelo fato de que (a) um composto é representado por meio da fórmula (i): o seu sal farmaceuticamente aceitável, ou um solvato do mesmo, em que p é hidrogênio ou um grupo para formar um profármaco; a1 é cr1ar1b, s ou o; a2 é cr2ar2b, s ou o; a3 é cr3ar3b, s ou o; a4 é cr4ar4b, s ou o; o número de heteroátomos entre os átomos que constituem o anel que consiste em a1, a2, a3, a4, átomo de nitro-gênio adjacente a a1 e o átomo de carbono adjacente a a4 é 1 ou 2; r1a e r1b são hidrogênio, halogênio, alquila ou similar; r2a e r2b são hidrogênio, halogênio, alquila, ou similar; r3a e r3b são hidrogênio, halogênio, alquila, ou similar; r4a são hidrogênio, halogênio, alquila, ou similar; r4b são hidrogênio, halogênio, alquila, ou similar; r3a e r3b podem ser um átomo de carbono adjacente para formar o carbociclo não aromático ou o heterociclo não aromático; n é qualquer um de um número inteiro de 1 a 2; e r1 é ou similares, é combinado com (b) composto(s) o qual possui uma atividade antigripe, o sal farmaceuticamente aceitável do mesmo ou um solvato do mesmo e/ou um anticorpo o qual possui uma atividade antigripe, é útil para o tratamento ou para a prevenção da gripe.
BR112018011103-1A 2015-12-15 2016-12-14 medicamento para tratar a gripe caracterizada por combinação de inibidor de endonuclease dependente de cap e de fármaco antigripe BR112018011103A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2015244492 2015-12-15
JP2015-244492 2015-12-15
PCT/JP2016/087170 WO2017104691A1 (ja) 2015-12-15 2016-12-14 キャップ依存的エンドヌクレアーゼ阻害剤及び抗インフルエンザ薬を組み合わせることを特徴とするインフルエンザ治療用医薬

Publications (1)

Publication Number Publication Date
BR112018011103A2 true BR112018011103A2 (pt) 2018-11-21

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BR112018011103-1A BR112018011103A2 (pt) 2015-12-15 2016-12-14 medicamento para tratar a gripe caracterizada por combinação de inibidor de endonuclease dependente de cap e de fármaco antigripe

Country Status (19)

Country Link
US (1) US11040048B2 (pt)
EP (1) EP3391888B1 (pt)
JP (1) JP6323860B2 (pt)
KR (1) KR102084109B1 (pt)
CN (1) CN108697715A (pt)
AU (1) AU2016374416A1 (pt)
BR (1) BR112018011103A2 (pt)
CA (1) CA3008607A1 (pt)
CL (1) CL2018001618A1 (pt)
CR (1) CR20180356A (pt)
HK (1) HK1254961A1 (pt)
IL (1) IL260025A (pt)
MA (1) MA44080A (pt)
MX (1) MX2018006966A (pt)
PE (1) PE20181516A1 (pt)
RU (1) RU2745071C2 (pt)
SG (2) SG11201804348SA (pt)
WO (1) WO2017104691A1 (pt)
ZA (1) ZA201803246B (pt)

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Publication number Priority date Publication date Assignee Title
US9969794B2 (en) 2012-05-10 2018-05-15 Visterra, Inc. HA binding agents
JP6358639B2 (ja) 2015-04-24 2018-07-18 塩野義製薬株式会社 ６員複素環誘導体およびそれらを含有する医薬組成物
DK3428170T3 (da) * 2015-04-28 2021-03-01 Shionogi & Co Anti-influenza polycyklisk pyridonderivat og prodrug deraf
PL3290424T3 (pl) * 2015-04-28 2023-05-08 Shionogi & Co., Ltd Podstawione policykliczne pochodne pirydonu i ich prolek
CN113717198A (zh) 2016-06-20 2021-11-30 盐野义制药株式会社 用于制备取代多环吡啶酮衍生物及其晶体的方法
SG10201912212XA (en) * 2016-08-10 2020-02-27 Shionogi & Co Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
CN109721615B (zh) * 2017-09-18 2020-12-29 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
BR112020006639A2 (pt) * 2017-10-06 2020-09-24 Shionogi & Co., Ltd. processo estereosseletivo para a preparação de derivados policíclicos substituídos de piridona
TWI795462B (zh) * 2017-11-17 2023-03-11 日商鹽野義製藥股份有限公司 光安定性及溶出性優異的醫藥製劑
CN110041327B (zh) * 2018-01-17 2022-01-21 江西彩石医药科技有限公司 吡啶酮衍生物、其组合物及作为抗流感病毒药物的应用
AU2019210414B2 (en) * 2018-01-17 2021-04-01 Jiangxi Caishi Pharmaceutical Technology Co., Ltd. Pyridone derivative, composition thereof and application thereof as anti-influenza drug
MX2020011130A (es) * 2018-04-24 2022-09-09 Shionogi & Co Forma de dosificacion solida que tiene excelente estabilidad.
KR102501180B1 (ko) 2018-04-24 2023-02-21 시오노기세야쿠 가부시키가이샤 안정성이 우수한 고형 제제
WO2020058745A1 (en) * 2018-09-18 2020-03-26 Shionogi & Co., Ltd. Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof
TWI829785B (zh) * 2018-10-17 2024-01-21 美商共結晶製藥公司 流感病毒複製抑制劑之組合
KR20210091753A (ko) * 2018-11-13 2021-07-22 코크리스탈 파마, 아이엔씨. 인플루엔자 치료제 제형
CN118791481A (zh) * 2018-12-12 2024-10-18 江西彩石医药科技有限公司 吡啶酮衍生物、其组合物及作为抗流感病毒药物的应用
CN111377944A (zh) * 2018-12-25 2020-07-07 广东东阳光药业有限公司 Baloxavir marboxil晶型及其制备方法
CN111410661B (zh) * 2019-01-04 2023-05-05 周雨恬 帽依赖性内切核酸酶抑制剂及其用途
WO2020177715A1 (zh) * 2019-03-05 2020-09-10 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
SG11202109050WA (en) 2019-03-12 2021-09-29 Shionogi & Co Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof in a subject having influenza and a complication risk factor
TWI830882B (zh) * 2019-03-13 2024-02-01 日商塩野義製藥股份有限公司 使用經取代之多環吡啶酮衍生物及其前藥在具有流感及併發症危險因子的個體中治療流感
US20220008429A2 (en) * 2019-03-22 2022-01-13 Shionogi & Co., Ltd. Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof in a subject having influenza and a severe influenza condition
WO2020194024A1 (en) * 2019-03-22 2020-10-01 Shionogi & Co., Ltd. Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof in a subject having influenza and a severe influenza condition
WO2020198329A1 (en) * 2019-03-25 2020-10-01 Visterra, Inc. Compositions and methods for treating and preventing influenza
EP3714889A1 (en) 2019-03-29 2020-09-30 F. Hoffmann-La Roche AG Baloxavir for the prevention of transmission of influenza virus
CN111825699B (zh) * 2019-04-15 2023-02-21 上海复星星泰医药科技有限公司 含硫杂环化合物及其制备方法
TWI841759B (zh) * 2019-07-11 2024-05-11 中國大陸商南京征祥醫藥有限公司 可用於治療流感病毒感染之化合物
US20210069204A1 (en) * 2019-08-13 2021-03-11 F. Hoffmann-La Roche Ag Dosage of baloxavir marboxil for pediatric patients
WO2021038480A1 (en) * 2019-08-27 2021-03-04 Janssen Pharmaceuticals, Inc. Combinations for treating influenza virus
CN115175913B (zh) * 2019-11-13 2023-11-28 南京知和医药科技有限公司 取代的双三环化合物及其药物组合物和用途
CN112920202B (zh) * 2019-12-05 2024-08-09 北京凯因科技股份有限公司 一种帽依赖性蛋白酶抑制剂
CN113045589B (zh) * 2019-12-27 2024-08-23 广东东阳光药业股份有限公司 流感病毒复制抑制剂及其用途
CN112898346B (zh) * 2020-01-23 2023-11-10 南京知和医药科技有限公司 水溶性多环化合物及其药物组合物和用途
WO2021151031A1 (en) * 2020-01-24 2021-07-29 Regeneron Pharmaceuticals, Inc. Protein-antiviral compound conjugates
CN111233891B (zh) * 2020-03-04 2021-05-04 江苏柯菲平医药股份有限公司 一种稠环吡啶酮衍生物及其制备方法和用途
CN113116899B (zh) * 2020-03-06 2022-12-20 广东众生睿创生物科技有限公司 一种用于治疗流感的药物组合物及含有该药物组合物的制剂
CN112578034B (zh) * 2020-11-04 2022-02-11 广东众生睿创生物科技有限公司 一种手性胺小分子及其盐的质量控制方法
WO2022107755A1 (ja) 2020-11-17 2022-05-27 塩野義製薬株式会社 新規アクリジニウム塩およびその製造方法
JP2024054430A (ja) * 2020-12-28 2024-04-17 塩野義製薬株式会社 Ｄｐ１アンタゴニストおよびキャップ依存性エンドヌクレアーゼ阻害剤からなるウイルス性気道感染症治療用医薬
CN114315827A (zh) * 2020-12-28 2022-04-12 维眸生物科技（上海）有限公司 多环吡啶并哒嗪酰胺并含肟碳环衍生物及其用途
JP2024054429A (ja) * 2020-12-28 2024-04-17 塩野義製薬株式会社 Ｄｐ１アンタゴニストおよびノイラミニダーゼ阻害剤からなるウイルス性気道感染症治療用医薬
CN116829153A (zh) * 2021-05-10 2023-09-29 南京征祥医药有限公司 治疗流感化合物的晶型及应用
CN117343079B (zh) * 2022-07-05 2024-08-20 山东如至生物医药科技有限公司 一种新型抗流感病毒化合物及其药物组合物和用途
CN118056834A (zh) * 2022-11-21 2024-05-21 合肥医工医药股份有限公司 稠环吡啶酮衍生物及其制备方法和用途
CN118561867A (zh) * 2024-05-27 2024-08-30 安徽贝克制药股份有限公司 一种帽状依赖性核酸内切酶抑制剂及其制备方法和其应用

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2280435A (en) 1993-07-29 1995-02-01 Merck & Co Inc Anti-viral agent
US5475109A (en) 1994-10-17 1995-12-12 Merck & Co., Inc. Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
CA2634499A1 (en) 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
US8188271B2 (en) 2005-10-27 2012-05-29 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
WO2008099874A1 (ja) * 2007-02-16 2008-08-21 Toyama Chemical Co., Ltd. ピラジン誘導体を含有する医薬組成物およびピラジン誘導体を組み合わせて使用する方法
ES2671550T3 (es) 2009-06-15 2018-06-07 Shionogi & Co., Ltd. Derivado de carbamoilpiridona policíclica sustituida
US9216995B2 (en) 2010-04-12 2015-12-22 Shionogi & Co., Ltd. Pyridone derivative having integrase inhibitory activity
HUE039859T2 (hu) * 2010-09-24 2019-02-28 Shionogi & Co Helyettesített policiklusos karbamoil-piridon-származék prodrug
US8859290B2 (en) 2011-07-22 2014-10-14 Rutgers, The State University Of New Jersey Inhibitors of influenza endonuclease activity and tools for their discovery
US20130102600A1 (en) 2011-10-21 2013-04-25 F. Hoffmann-La Roche Ltd Heteroaryl hydroxamic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
US20130102601A1 (en) * 2011-10-21 2013-04-25 F. Hoffmann-La Roche Ltd Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease
BR112014029006A2 (pt) 2012-05-23 2017-06-27 European Molecular Biology Laboratory derivados de 7-oxo-4,7-di-hidro-pirazolo[1,5-a]pirimidina que são úteis no tratamento, melhora ou prevenção de uma doença viral
US9434745B2 (en) 2012-05-23 2016-09-06 Savira Pharmaceuticals Gmbh 7-oxo-thiazolopyridine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2014023691A1 (en) 2012-08-06 2014-02-13 Savira Pharmaceuticals Gmbh Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
US9573938B2 (en) 2012-09-11 2017-02-21 Rutgers, The State University Of New Jersey Therapeutic hydroxypyridinones, hydroxypyrimidinones and hydroxypyridazinones
US9701638B2 (en) 2012-11-09 2017-07-11 Rutgers, The State University Of New Jersey Therapeutic hydroxyquinolones
CN104903294A (zh) 2013-01-08 2015-09-09 萨维拉制药有限公司 吡啶酮衍生物及其在治疗、改善或预防病毒疾病中的用途
EP2943495B1 (en) 2013-01-08 2016-12-28 Savira Pharmaceuticals GmbH Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
KR20150103672A (ko) * 2013-01-08 2015-09-11 사피라 파르마슈티칼즈 게엠베하 나프티리디논 유도체 및 바이러스성 질환의 치료, 개선 또는 예방에서의 이의 용도
ES2724581T3 (es) 2013-09-12 2019-09-12 Janssen Biopharma Inc Compuestos de piridazinona y usos de los mismos
AU2014318832B2 (en) 2013-09-12 2018-11-29 Janssen Biopharma, Inc. Aza-pyridone compounds and uses thereof
JP2017521424A (ja) 2014-07-07 2017-08-03 ザヴィラ ファーマシューティカルズ ゲーエムベーハー ウイルス疾患の治療、改善又は予防におけるジヒドロピリドピラジン−１，８−ジオン及びそれらの使用
CN107001355A (zh) 2014-07-07 2017-08-01 萨维拉制药有限公司 吡啶并吡嗪化合物和它们在治疗、改善或预防流感中的用途
DK3428170T3 (da) * 2015-04-28 2021-03-01 Shionogi & Co Anti-influenza polycyklisk pyridonderivat og prodrug deraf
PL3290424T3 (pl) * 2015-04-28 2023-05-08 Shionogi & Co., Ltd Podstawione policykliczne pochodne pirydonu i ich prolek
US20170081331A1 (en) 2015-09-18 2017-03-23 F. Hoffmann-La Roche Ag Pyrazolopyrazines and their use in the treatment, amelioration or prevention of a viral disease
WO2017072341A1 (en) 2015-10-30 2017-05-04 F. Hoffmann-La Roche Ag Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2017109088A1 (en) 2015-12-23 2017-06-29 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
JP6806413B2 (ja) 2016-02-03 2021-01-06 塩野義製薬株式会社 多環性ピリドン誘導体およびそのプロドラッグ
US10858366B2 (en) 2016-03-08 2020-12-08 Novartis Ag Tricyclic compounds useful to treat orthomyxovirus infections
WO2017158147A1 (en) 2016-03-18 2017-09-21 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2017158151A1 (en) 2016-03-18 2017-09-21 Savira Pharmaceuticals Gmbh Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
CN113717198A (zh) 2016-06-20 2021-11-30 盐野义制药株式会社 用于制备取代多环吡啶酮衍生物及其晶体的方法
WO2017223231A1 (en) 2016-06-21 2017-12-28 Alios Biopharma, Inc. (s)-8-(benzhydryl )-6-isopropyl-3,5-dioxo- 5, 6,7,8,-tetrahydro-3h-pyrazino-[1,2-b]pyridazin-yl-isobutyrate antiviral agent for use in treating influenza
SG10201912212XA (en) 2016-08-10 2020-02-27 Shionogi & Co Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
JOP20170169A1 (ar) 2016-08-29 2019-01-30 Novartis Ag مركبات بيريدازين ثلاثية الحلقة مندمجة تفيد في علاج العدوى بفيروس أورثوميكسو
JP7034162B2 (ja) 2016-12-15 2022-03-11 サンシャイン・レイク・ファーマ・カンパニー・リミテッド インフルエンザウイルス複製の阻害剤及びその使用
CN108727369B (zh) 2017-04-25 2023-06-09 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
CN108440564B (zh) 2018-04-11 2019-08-06 安帝康（无锡）生物科技有限公司 被取代的多环氨基甲酰基吡啶酮衍生物及其前药

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