[go: up one dir, main page]

PE20151951A1 - Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b - Google Patents

Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b

Info

Publication number
PE20151951A1
PE20151951A1 PE2015002407A PE2015002407A PE20151951A1 PE 20151951 A1 PE20151951 A1 PE 20151951A1 PE 2015002407 A PE2015002407 A PE 2015002407A PE 2015002407 A PE2015002407 A PE 2015002407A PE 20151951 A1 PE20151951 A1 PE 20151951A1
Authority
PE
Peru
Prior art keywords
compounds
heteroaryldihydropyrimidines
prophylaxis
hepatitis
bridges
Prior art date
Application number
PE2015002407A
Other languages
English (en)
Inventor
Lei Guo
taishan Hu
Yimin Hu
Buelent Kocer
Buyu Kou
Gangqin Li
Xianfeng Lin
Haixia Liu
Hong Shen
Houguang Shi
Guolong Wu
Zhisen Zhang
Mingwei Zhou
Wei Zhu
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50733070&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20151951(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20151951A1 publication Critical patent/PE20151951A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08Bridged systems
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La invencion proporciona compuestos novedosos que tienen la formula genera (I): en la que R1, R2, R3 Y R4 son como se definen en la descripcion y en las reivindicaciones, ademas de o sales farmaceuticamente aceptables, o isomeros de tautomeria, o enantiomeros, o diaestereomeros de los mismos. La invencion tambien contiene composiciones que incluyen los compuestos y procedimientos de uso de los compuestos. Donde R1 es alquilo C1-6, R2 es fenilo sustituido, R3 es hidrogeno o alquilo C1-6, R4 es a) o b) Compuestos preferidos son: acido 9-[[4R)-4-(2-cloro-4-fluoro-fenil)-5-metoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidin-6-il]metil]-3-oxa-9-azabiciclo[3.3.1]nonano-7-carboxilico; acido 9-[[4R)-6-(2-cloro-4-fluoro-fenil)-5-metoxicarbonil-2-(4-metil-tiazol-2-il)-3,6-dihidro-pirimidin-4-ilmetil]-3-oxa-9-aza-biciclo[3.3.1]nonano-7-carboxilico
PE2015002407A 2013-05-17 2014-05-16 Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b PE20151951A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2013075815 2013-05-17
CN2014075392 2014-04-15

Publications (1)

Publication Number Publication Date
PE20151951A1 true PE20151951A1 (es) 2015-12-26

Family

ID=50733070

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015002407A PE20151951A1 (es) 2013-05-17 2014-05-16 Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b

Country Status (17)

Country Link
US (2) US9266904B2 (es)
EP (1) EP2997032B1 (es)
JP (1) JP6533217B2 (es)
CN (1) CN105209470B (es)
AU (1) AU2014267198A1 (es)
BR (1) BR112015028873A2 (es)
CA (1) CA2911214A1 (es)
CL (1) CL2015003298A1 (es)
CR (1) CR20150611A (es)
EA (1) EA201592126A1 (es)
MX (1) MX2015015692A (es)
PE (1) PE20151951A1 (es)
PH (1) PH12015502443A1 (es)
SG (1) SG11201509463YA (es)
TW (1) TW201512193A (es)
WO (1) WO2014184328A1 (es)
ZA (1) ZA201507840B (es)

Families Citing this family (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201608528YA (en) 2011-12-21 2016-12-29 Novira Therapeutics Inc Hepatitis b antiviral agents
JP2015533782A (ja) 2012-08-28 2015-11-26 ヤンセン・サイエンシズ・アイルランド・ユーシー スルファモイル−アリールアミド及びb型肝炎の治療のための薬剤としてのその使用
EP2892893B2 (en) * 2012-09-10 2019-10-16 F.Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
EP2961732B1 (en) 2013-02-28 2017-04-12 Janssen Sciences Ireland UC Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
AU2014247138B2 (en) 2013-04-03 2018-06-28 Janssen Sciences Ireland Uc N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
JP6533217B2 (ja) * 2013-05-17 2019-06-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療および予防のための6−架橋ヘテロアリールジヒドロピリミジン類
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
PL3786162T3 (pl) 2013-05-17 2024-04-08 Incyte Holdings Corporation Pochodne bipirazolu jako inhibitory jak
CA2909742C (en) 2013-05-17 2020-08-04 Janssen Sciences Ireland Uc Sulphamoylthiophenamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
ES2774749T3 (es) 2013-07-25 2020-07-22 Janssen Sciences Ireland Unlimited Co Derivados de pirrolamida sustituidos con glioxamida y su uso como medicamentos para el tratamiento de la hepatitis B
JP6452119B2 (ja) 2013-10-23 2019-01-16 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー カルボキサミド誘導体およびb型肝炎の処置のための医薬品としてのその使用
MX2016006564A (es) 2013-11-19 2017-09-12 Sunshine Lake Pharma Co Ltd Compuestos dihidropirimidina y su aplicacion en productos farmaceuticos.
RU2688193C1 (ru) 2013-11-27 2019-05-21 Саншайн Лейк Фарма Ко., Лтд. Процессы приготовления производных дигидропиримидина и их промежуточных соединений
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
KR20160128305A (ko) 2014-02-05 2016-11-07 노비라 테라퓨틱스, 인코포레이티드 Hbv 감염의 치료를 위한 병용 요법
CA2932551A1 (en) 2014-02-06 2015-08-13 Janssen Sciences Ireland Uc Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
JP6306750B2 (ja) * 2014-03-07 2018-04-04 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療および予防のための新規な6−縮合ヘテロアリールジヒドロピリミジン
ES2748029T3 (es) 2014-03-13 2020-03-12 Univ Indiana Res & Tech Corp Moduladores alostéricos de proteína núcleo de hepatitis B
EP3122747B1 (en) 2014-03-28 2020-05-20 North & South Brother Pharmacy Investment Company Limited Dihydropyrimidine compounds and their application in pharmaceuticals
WO2016102438A1 (en) * 2014-12-23 2016-06-30 F. Hoffmann-La Roche Ag Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidine analogues
US10098889B2 (en) 2015-02-07 2018-10-16 Sunshine Lake Pharma Co., Ltd. Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals
EP3722297A1 (en) 2015-03-04 2020-10-14 Gilead Sciences, Inc. Toll-like receptor modulating 4,6-diamino-pyrido[3,2-d]pyrimidine compounds
HRP20200943T1 (hr) * 2015-03-16 2020-09-18 F. Hoffmann - La Roche Ag Kombinirani tretman s agonistom tlr7 i inhibitorom hbv kapside
US10442788B2 (en) 2015-04-01 2019-10-15 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
CN106146327B (zh) * 2015-04-03 2019-03-19 浙江海正药业股份有限公司 一种d-环丝氨酸中间体的合成方法
US10738035B2 (en) 2015-05-13 2020-08-11 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
US10179131B2 (en) 2015-07-13 2019-01-15 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US10301255B2 (en) 2015-07-22 2019-05-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
JP2018525412A (ja) 2015-08-26 2018-09-06 ギリアード サイエンシーズ, インコーポレイテッド 重水素化トール様受容体調節因子
TWI786639B (zh) 2015-09-15 2022-12-11 美商艾森伯利生物科學公司 B型肝炎核心蛋白質調節劑
CN108135979A (zh) * 2015-11-03 2018-06-08 豪夫迈·罗氏有限公司 Hbv衣壳组装抑制剂和干扰素的组合疗法
WO2017108630A1 (en) * 2015-12-21 2017-06-29 F. Hoffmann-La Roche Ag Combination therapy of an hbsag inhibitor and an hbv capsid assembly inhibitor
WO2017136403A1 (en) * 2016-02-02 2017-08-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
AR107633A1 (es) 2016-02-19 2018-05-16 Hoffmann La Roche Procedimiento para la preparación del ácido 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]-3-oxo-5,6,8,8a-tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxílico
CN109069488B (zh) 2016-03-07 2021-09-07 英安塔制药有限公司 乙型肝炎抗病毒剂
EP3848026A1 (en) 2016-04-15 2021-07-14 Novira Therapeutics Inc. Combinations and methods comprising a capsid assembly inhibitor
WO2017198744A1 (en) * 2016-05-20 2017-11-23 F. Hoffmann-La Roche Ag Novel pyrazine compounds with oxygen, sulfur and nitrogen linker for the treatment of infectious diseases
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
AU2017271990B2 (en) 2016-05-27 2019-12-19 Gilead Sciences, Inc. Methods for treating Hepatitis B virus infections using NS5A, NS5B or NS3 inhibitors
SG11201810834WA (en) * 2016-06-10 2018-12-28 Enanta Pharm Inc Hepatitis b antiviral agents
CN109689059A (zh) 2016-08-24 2019-04-26 豪夫迈·罗氏有限公司 Hbv衣壳组装抑制剂和核苷或核苷酸类似物的组合疗法
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
EP3507288B1 (en) 2016-09-02 2020-08-26 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
PT3507276T (pt) 2016-09-02 2022-01-11 Gilead Sciences Inc Compostos moduladores do recetor de tipo toll
WO2018045911A1 (zh) * 2016-09-09 2018-03-15 浙江海正药业股份有限公司 二氢嘧啶类化合物及其制备方法和用途
BR112019004560A2 (pt) 2016-09-13 2019-07-02 Hoffmann La Roche tratamento combinado com agonista de tlr7 e um inibidor de formação de capsídeo de hbv
CA3037151A1 (en) 2016-09-15 2018-03-22 Assembly Biosciences, Inc. Hepatitis b core protein modulators
US10662416B2 (en) 2016-10-14 2020-05-26 Precision Biosciences, Inc. Engineered meganucleases specific for recognition sequences in the hepatitis B virus genome
US11166954B2 (en) 2016-11-18 2021-11-09 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Dihydropyrimidine compound and preparation method and use thereof
CN109790145B (zh) 2016-11-18 2020-09-22 四川科伦博泰生物医药股份有限公司 二氢嘧啶类化合物及其制备方法和用途
TW202510891A (zh) 2017-01-31 2025-03-16 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
SG11201908012SA (en) 2017-03-02 2019-09-27 Assembly Biosciences Inc Cyclic sulfamide compounds and methods of using same
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
CN109111451B (zh) 2017-06-26 2020-08-11 广东东阳光药业有限公司 二氢嘧啶类化合物及其在药物中的应用
WO2019001420A1 (en) 2017-06-27 2019-01-03 Janssen Pharmaceutica Nv HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING INFECTIONS WITH HEPATITIS B VIRUS
KR102891807B1 (ko) 2017-08-22 2025-12-01 길리애드 사이언시즈, 인코포레이티드 치료 헤테로시클릭 화합물
EP3675637A4 (en) 2017-08-28 2021-05-19 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
CA3079557A1 (en) 2017-10-18 2019-04-25 Sunshine Lake Pharma Co., Ltd. Dihydropyrimidine compounds and uses thereof in medicine
WO2019086142A1 (en) 2017-11-02 2019-05-09 Aicuris Gmbh & Co. Kg Novel, highly active pyrazolo-piperidine substituted indole-2-carboxamides active against the hepatitis b virus (hbv)
CN111448199A (zh) 2017-11-02 2020-07-24 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的高活性的氨基-噻唑取代的吲哚-2-甲酰胺
US10723733B2 (en) 2017-12-06 2020-07-28 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
TW201927789A (zh) 2017-12-06 2019-07-16 美商因那塔製藥公司 B型肝炎抗病毒試劑
CN111566120B (zh) 2017-12-20 2023-09-29 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的3’3’环状二核苷酸
US11203610B2 (en) 2017-12-20 2021-12-21 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
WO2019143902A2 (en) 2018-01-22 2019-07-25 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
BR122023022189A2 (pt) 2018-02-16 2024-02-20 Incyte Corporation Usos de inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
US10836769B2 (en) 2018-02-26 2020-11-17 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
WO2019175657A1 (en) 2018-03-14 2019-09-19 Janssen Sciences Ireland Unlimited Company Capsid assembly modulator dosing regimen
WO2019191166A1 (en) 2018-03-29 2019-10-03 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
EP4424328A3 (en) 2018-03-30 2024-12-04 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
US10870691B2 (en) 2018-04-05 2020-12-22 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis B virus protein X
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 2,2,─環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
WO2019211799A1 (en) 2018-05-03 2019-11-07 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide
US11186579B2 (en) 2018-07-06 2021-11-30 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
CA3103987C (en) 2018-07-06 2023-08-01 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
CN108947996B (zh) * 2018-07-12 2022-01-18 山东大学 二氢嘧啶-磺酰胺类衍生物及其制备方法与应用
PT3820572T (pt) 2018-07-13 2023-11-10 Gilead Sciences Inc Inibidores pd-1/pd-l1
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
US11053235B2 (en) 2018-08-09 2021-07-06 Janssen Sciences Ireland Unlimited Company Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases
MX2021003253A (es) 2018-09-21 2021-08-11 Enanta Pharm Inc Heterociclos funcionalizados como agentes antivirales.
CN113195055A (zh) 2018-10-22 2021-07-30 组装生物科学股份有限公司 用于hbv治疗的5元杂芳基甲酰胺化合物
JP7158577B2 (ja) 2018-10-24 2022-10-21 ギリアード サイエンシーズ, インコーポレイテッド Pd-1/pd-l1阻害剤
EP4371987B9 (en) 2018-10-31 2025-11-26 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as hpk1 inhibitors
KR102658602B1 (ko) 2018-10-31 2024-04-19 길리애드 사이언시즈, 인코포레이티드 Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물
ES3023937T3 (en) 2018-10-31 2025-06-03 The Westmead Institute For Medical Res Pharmaceutical compositions for use in treating an hbv or hdv infection
AR117188A1 (es) 2018-11-02 2021-07-21 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb)
AR116947A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas-indol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
US20220009945A1 (en) 2018-11-02 2022-01-13 Aicuris Gmbh & Co. Kg Novel urea 6,7-dihydro-4h-thiazole[5,4-c]pyridines active against the hepatitis b virus (hbv)
AR116948A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb)
AR116946A1 (es) 2018-11-02 2021-06-30 Aicuris Gmbh & Co Kg Derivados de urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb)
UY38434A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activas contra el virus de la hepatitis b (hbv)
SG11202105007TA (en) 2018-11-21 2021-06-29 Enanta Pharm Inc Functionalized heterocycles as antiviral agents
TW202035412A (zh) * 2018-12-20 2020-10-01 比利時商健生藥品公司 雜芳基二氫嘧啶衍生物和治療b型肝炎感染之方法
KR20210130753A (ko) 2019-02-22 2021-11-01 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 Hbv 감염 또는 hbv-유발성 질환의 치료에 유용한 아미드 유도체
US20220143061A1 (en) 2019-03-07 2022-05-12 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
CN113543851B (zh) 2019-03-07 2025-03-18 捷克共和国有机化学与生物化学研究所 2’3’-环二核苷酸及其前药
KR102732006B1 (ko) 2019-03-25 2024-11-20 에프. 호프만-라 로슈 아게 Hbv 코어 단백질 알로스테릭 조절제 화합물의 고체 형태
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
AU2020267015A1 (en) 2019-04-30 2021-12-23 Aicuris Gmbh & Co. Kg Novel indole-2-carboxamides active against the hepatitis B virus (HBV)
WO2020221824A1 (en) 2019-04-30 2020-11-05 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv)
CU20210089A7 (es) 2019-04-30 2022-06-06 Aicuris Gmbh & Co Kg Compuestos derivados de fenil y piridil ureas activas contra el virus de la hepatitis b (vhb)
AU2020266258A1 (en) 2019-04-30 2021-12-23 Aicuris Gmbh & Co. Kg Novel oxalyl piperazines active against the hepatitis B virus (HBV)
AR119732A1 (es) 2019-05-06 2022-01-05 Janssen Sciences Ireland Unlimited Co Derivados de amida útiles en el tratamiento de la infección por vhb o de enfermedades inducidas por vhb
WO2020237025A1 (en) 2019-05-23 2020-11-26 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
BR112021023622A2 (pt) 2019-05-24 2022-04-19 Assembly Biosciences Inc Composições farmaceuticas para o tratamento de hbv
US11236111B2 (en) 2019-06-03 2022-02-01 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US11760755B2 (en) 2019-06-04 2023-09-19 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
CA3140708A1 (en) 2019-06-18 2020-12-24 Helen Horton Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
WO2020263830A1 (en) 2019-06-25 2020-12-30 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
WO2021007488A1 (en) 2019-07-11 2021-01-14 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
CN114174300A (zh) * 2019-07-31 2022-03-11 杨森科学爱尔兰无限公司 二氢嘧啶衍生物及其在治疗hbv感染或hbv诱发疾病中的用途
EP4017476A1 (en) 2019-08-19 2022-06-29 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
US11236108B2 (en) 2019-09-17 2022-02-01 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
CA3149557A1 (en) 2019-09-30 2021-04-08 Scott J. Balsitis Hbv vaccines and methods treating hbv
WO2021113765A1 (en) 2019-12-06 2021-06-10 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
WO2021121363A1 (en) * 2019-12-20 2021-06-24 Janssen Pharmaceutica Nv Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis b infections
WO2021188414A1 (en) 2020-03-16 2021-09-23 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
AR121620A1 (es) 2020-03-20 2022-06-22 Gilead Sciences Inc Profármacos de nucleósidos 4’-c-sustituidos-2-halo-2’-deoxiadenosina y métodos de preparación y uso de los mismos
WO2021216660A1 (en) 2020-04-22 2021-10-28 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
BR112022021419A2 (pt) 2020-04-22 2023-03-07 Assembly Biosciences Inc Compostos de heteroaril carboxamida de 5 membros para o tratamento de hbv
EP4139000A1 (en) 2020-04-22 2023-03-01 Assembly Biosciences, Inc. Pyrazole carboxamide compounds for treatment of hbv
WO2021216661A1 (en) 2020-04-22 2021-10-28 Assembly Biosciences, Inc. Pyrazole carboxamide compounds for treatment of hbv
HRP20241560T1 (hr) 2020-06-02 2025-01-17 Incyte Corporation Postupci za proizvodnju inhibitora jak1
ES3054072T3 (en) 2020-08-07 2026-01-29 Gilead Sciences Inc Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use
WO2022052923A1 (zh) * 2020-09-08 2022-03-17 和博医药有限公司 二氢嘧啶类化合物、其应用
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
IL303238A (en) 2020-12-08 2023-07-01 Incyte Corp Jak1 pathway inhibitors for the treatment of vitiligo
WO2022166923A1 (zh) 2021-02-05 2022-08-11 和博医药有限公司 苯基二氢嘧啶类化合物及其应用
CN113512035B (zh) * 2021-04-26 2023-11-24 山东大学 二氢嘧啶-泊马度胺缀合物及其制备方法与应用
CN113135921B (zh) * 2021-04-26 2022-06-17 山东大学 二氢嘧啶-螺环类衍生物及其制备方法与应用
TW202308610A (zh) 2021-05-03 2023-03-01 美商英塞特公司 用於治療結節性癢疹之jak1途徑抑制劑
JP2024518558A (ja) 2021-05-13 2024-05-01 ギリアード サイエンシーズ, インコーポレイテッド TLR8調節化合物と抗HBV siRNA治療薬との組合せ
US11976072B2 (en) 2021-06-23 2024-05-07 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
EP4359413A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
US11932634B2 (en) 2021-06-23 2024-03-19 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
WO2022271659A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023069545A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023069547A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023069544A1 (en) 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023164186A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164181A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164179A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2023164183A1 (en) 2022-02-25 2023-08-31 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2025043094A1 (en) 2023-08-23 2025-02-27 Assembly Biosciences, Inc. Benzothia(dia)zepine compounds for treatment of hbv and hdv
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
US20250345390A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
US20250345389A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
CN120383543A (zh) * 2025-06-06 2025-07-29 康龙化成手性医药技术(宁波)有限公司 一种4-氟-2-氮杂双环[2.1.1]己烷盐酸盐的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10012823A1 (de) * 2000-03-16 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
DE10013126A1 (de) * 2000-03-17 2001-09-20 Bayer Ag Arzneimittel gegen virale Erkrankungen
WO2006033995A2 (en) 2004-09-16 2006-03-30 Valeant Research And Development Thiazolidin-4-ones having anti-hepatitis b activity
CN101328169B (zh) * 2007-06-18 2011-05-25 张中能 一种乙氧碳酰基-取代噻唑二氢嘧啶
DK2785695T3 (da) * 2011-11-30 2020-08-24 Fhoffmann-La Roche Ag Nye bicykliske dihydroisoquinolin-1-on-derivater
EP2892893B2 (en) * 2012-09-10 2019-10-16 F.Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
JP6533217B2 (ja) * 2013-05-17 2019-06-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療および予防のための6−架橋ヘテロアリールジヒドロピリミジン類
JP6306750B2 (ja) * 2014-03-07 2018-04-04 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療および予防のための新規な6−縮合ヘテロアリールジヒドロピリミジン

Also Published As

Publication number Publication date
TW201512193A (zh) 2015-04-01
PH12015502443A1 (en) 2016-02-22
BR112015028873A2 (pt) 2017-07-25
EA201592126A1 (ru) 2016-05-31
SG11201509463YA (en) 2015-12-30
EP2997032B1 (en) 2018-07-25
US20160122363A1 (en) 2016-05-05
US9266904B2 (en) 2016-02-23
WO2014184328A1 (en) 2014-11-20
CL2015003298A1 (es) 2016-06-17
US9758530B2 (en) 2017-09-12
CN105209470A (zh) 2015-12-30
MX2015015692A (es) 2016-03-04
US20140343032A1 (en) 2014-11-20
HK1219480A1 (zh) 2017-04-07
CA2911214A1 (en) 2014-11-20
JP2016518432A (ja) 2016-06-23
AU2014267198A1 (en) 2015-11-05
ZA201507840B (en) 2017-11-29
JP6533217B2 (ja) 2019-06-19
CR20150611A (es) 2015-12-07
EP2997032A1 (en) 2016-03-23
CN105209470B (zh) 2018-02-06

Similar Documents

Publication Publication Date Title
PE20151951A1 (es) Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b
UY33337A (es) DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS
MX377581B (es) Compuestos antihelmínticos y composiciones y método de uso de los mismos.
UY33961A (es) Compuestos de bis(fuoroalquil)-1,4-benziodiazepinona
PE20142456A1 (es) COMPUESTOS DE OXAZOLIDIN-2-ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
AR082968A1 (es) Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto
ECSP14004812A (es) Triazolopiridinas sustituidas
PE20170203A1 (es) Derivados de nucleosido sustituidos con 4'-difluorometilo como inhibidores de la replicacion de arn de la influeza
CR20170367A (es) Derivados de 1-(het)arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de trpa1
PE20160548A1 (es) Sulfonamidas como moduladores de canales de sodio
BRPI1009333B8 (pt) compostos inibidores de beta-secretase, seus usos, bem como composição farmacêutica
PE20142081A1 (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos
PE20140522A1 (es) Derivados de nucleosidos 2'- sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
PE20150776A1 (es) 6-aminoacido-heteroarildihidropirimidinas para el tratamiento y profilaxis de la infeccion del virus de la hepatitis b
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
PE20151892A1 (es) Compuestos tetraciclicos sustituidos con heterociclo y metodos de uso de los mismos para el tratamiento de enfermedades viricas
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
ECSP055801A (es) Compuestos benzofuránicos, composiciones y métodos para el tratamiento y profilaxis de infecciones virales de hepatitis c y enfermedades asociadas
CR20110013A (es) Derivados de Heteroarilo como Inhibidores de DGAT1
MX2015009602A (es) Piridona amidas como moduladores de canales de sodio.
EA201590453A1 (ru) Конденсированные бициклические производные сульфамоила и их применение в качестве лекарственных препаратов для лечения гепатита b
MX2021011389A (es) Compuestos de imidazolonilquinolina y usos terapeuticos de los mismos.
CR8649A (es) Derivados de formamidina para el tratamiento de enfermedades
CR10356A (es) Derivados de 4-benzilphthalazinona 2-sustituidos como antagonistas de histamina h1 y h3
PE20141380A1 (es) Imidazopiridazinas como inhibidores de quinasa akt

Legal Events

Date Code Title Description
FD Application declared void or lapsed