CN106413402B - 乙型肝炎核心蛋白变构调节剂 - Google Patents

乙型肝炎核心蛋白变构调节剂 Download PDF

Info

Publication number
CN106413402B
CN106413402B CN201580024580.0A CN201580024580A CN106413402B CN 106413402 B CN106413402 B CN 106413402B CN 201580024580 A CN201580024580 A CN 201580024580A CN 106413402 B CN106413402 B CN 106413402B
Authority
CN
China
Prior art keywords
mmol
reaction
tlc
compound
group
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201580024580.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN106413402A (zh
Inventor
W.W.特纳
L.D.阿诺德
H.马格
A.兹洛特尼克
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Indiana University Research and Technology Corp
Assembly Biosciences Inc
Original Assignee
Indiana University Research and Technology Corp
Assembly Biosciences Inc
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 Indiana University Research and Technology Corp, Assembly Biosciences Inc filed Critical Indiana University Research and Technology Corp
Priority to CN201910710699.3A priority Critical patent/CN110437153A/zh
Publication of CN106413402A publication Critical patent/CN106413402A/zh
Application granted granted Critical
Publication of CN106413402B publication Critical patent/CN106413402B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/20—Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/38—[b, e]- or [b, f]-condensed with six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02—Seven-membered rings
    • C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D281/14—[b, e]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02—Seven-membered rings
    • C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D281/16—[b, f]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201580024580.0A 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂 Expired - Fee Related CN106413402B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201910710699.3A CN110437153A (zh) 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461952467P 2014-03-13 2014-03-13
US61/952,467 2014-03-13
US201462010025P 2014-06-10 2014-06-10
US62/010,025 2014-06-10
PCT/US2015/020444 WO2015138895A1 (en) 2014-03-13 2015-03-13 Hepatitis b core protein allosteric modulators

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201910710699.3A Division CN110437153A (zh) 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂

Publications (2)

Publication Number Publication Date
CN106413402A CN106413402A (zh) 2017-02-15
CN106413402B true CN106413402B (zh) 2020-10-30

Family

ID=54072461

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201580024580.0A Expired - Fee Related CN106413402B (zh) 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂
CN201910710699.3A Pending CN110437153A (zh) 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201910710699.3A Pending CN110437153A (zh) 2014-03-13 2015-03-13 乙型肝炎核心蛋白变构调节剂

Country Status (23)

Country Link
US (3) US10183936B2 (enExample)
EP (3) EP3116316B1 (enExample)
JP (2) JP6602311B2 (enExample)
KR (1) KR102363174B1 (enExample)
CN (2) CN106413402B (enExample)
AP (1) AP2016009477A0 (enExample)
AU (2) AU2015229174B2 (enExample)
CA (1) CA2942533C (enExample)
CL (1) CL2016002269A1 (enExample)
DK (1) DK3116316T3 (enExample)
DO (1) DOP2016000233A (enExample)
ES (1) ES2748029T3 (enExample)
HR (1) HRP20191444T1 (enExample)
HU (1) HUE046567T2 (enExample)
IL (3) IL247575B (enExample)
MX (2) MX363600B (enExample)
PH (2) PH12016501762B1 (enExample)
PL (1) PL3116316T3 (enExample)
PT (1) PT3116316T (enExample)
RS (1) RS59430B1 (enExample)
SG (2) SG10202001506UA (enExample)
WO (1) WO2015138895A1 (enExample)
ZA (1) ZA201606209B (enExample)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037918B1 (ru) 2011-12-21 2021-06-07 Новира Терапьютикс, Инк. Противовирусные агенты против гепатита в
HK1208465A1 (en) 2012-08-28 2016-03-04 Janssen Sciences Ireland Uc Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
DK2961732T3 (en) 2013-02-28 2017-07-10 Janssen Sciences Ireland Uc SULFAMOYLARYLAMIDS AND USE THEREOF AS MEDICINES TO TREAT HEPATITIS B
WO2014161888A1 (en) 2013-04-03 2014-10-09 Janssen R&D Ireland N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
RS57999B1 (sr) 2013-05-17 2019-01-31 Janssen Sciences Ireland Uc Derivati sulfamoiltiofenamida i njihova primena kao lekovi za tretman hepatitisa b
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
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
KR102290189B1 (ko) 2013-10-23 2021-08-17 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 카르복스아미드 유도체 및 ｂ형 간염 치료용 의약으로서의 이의 용도
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9169212B2 (en) 2014-01-16 2015-10-27 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
DK3102572T3 (en) 2014-02-06 2019-02-04 Janssen Sciences Ireland Uc SULFAMOYLPYRROLAMIDE DERIVATIVES AND THEIR USE AS MEDICINES TO TREAT HEPATITIS B
MX363600B (es) 2014-03-13 2019-03-28 Univ Indiana Res & Tech Corp Moduladores alostericos de proteina nucleo de hepatitis b.
WO2016149581A1 (en) 2015-03-19 2016-09-22 Novira Therapeutics, Inc. Azocane and azonane derivatives and methods of treating hepatitis b infections
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
SG10201913958QA (en) * 2015-07-15 2020-03-30 Agency Science Tech & Res Modulation of hepatitis b virus replication
TWI721016B (zh) 2015-09-15 2021-03-11 美商艾森伯利生物科學公司 B型肝炎核心蛋白質調節劑
HK1259410A1 (zh) 2015-09-29 2019-11-29 诺维拉治疗公司 乙型肝炎抗病毒剂的晶体形式
EP3442524A2 (en) 2016-04-15 2019-02-20 Novira Therapeutics Inc. Combinations and methods comprising a capsid assembly inhibitor
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
ES2989988T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros heterorocíclicos para la degradación de proteínas diana
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
US10987360B2 (en) 2016-09-15 2021-04-27 Assembly Biosciences, Inc. Hepatitis B core protein modulators
NZ752250A (en) * 2016-10-03 2025-10-31 Sigilon Therapeutics Inc Compounds, devices, and uses thereof
US10821103B2 (en) 2016-11-07 2020-11-03 Arbutus Biopharma Corporation Substituted pyridinone-containing trycyclic compounds, and methods using same
CN106632177A (zh) * 2016-12-05 2017-05-10 万特制药(海南)有限公司 雷美替胺中间体的制备方法
PL3587420T3 (pl) * 2017-02-23 2021-10-11 Fujian Cosunter Pharmaceutical Co., Ltd. Związek tricykliczny i jego zastosowania
ES2898217T3 (es) 2017-03-02 2022-03-04 Assembly Biosciences Inc Compuestos de sulfamida cíclica y métodos de uso de los mismos
AU2018236188B2 (en) * 2017-03-13 2022-01-27 Assembly Biosciences, Inc. Process for making hepatitis B core protein modulators
MA49014A (fr) 2017-03-21 2020-02-05 Arbutus Biopharma Corp Dihydroindène-4-carboxamides substitués, leurs analogues et procédés d'utilisation correspondant
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
KR20200030584A (ko) 2017-07-21 2020-03-20 앤타바이오 에스에이에스 화합물
CN111527087A (zh) 2017-11-02 2020-08-11 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吡唑并-哌啶取代的吲哚-2-甲酰胺
GEP20227373B (en) 2017-11-02 2022-04-25 Aicuris Gmbh & Co Kg Novel, highly active amino-thiazole substituted indole-2-carboxamides active against the hepatitis b virus (hbv)
EA202092171A1 (ru) 2018-03-14 2020-12-01 Янссен Сайенсиз Айрлэнд Анлимитед Компани Схема дозирования модулятора сборки капсида
US12318393B2 (en) 2018-05-03 2025-06-03 Emory University Modulators of orphan nuclear receptors for NASH and other metabolic disorders
CN110627752B (zh) * 2018-06-25 2021-08-17 新发药业有限公司 一种3-氨甲基四氢呋喃的制备方法
CN108863884B (zh) * 2018-07-26 2020-07-03 南京富润凯德生物医药有限公司 一种用dast试剂作为消除试剂合成共轭硝基烯取代系列衍生物的方法
TWI869058B (zh) 2018-07-27 2025-01-01 加拿大商愛彼特生物製藥公司 經取代四氫環戊[c]吡咯、經取代二氫吡咯，其類似物及使用其之方法
TWI742419B (zh) * 2018-08-23 2021-10-11 大陸商福建廣生堂藥業股份有限公司 三并環類化合物的晶型及其應用
PY1991603A (es) 2018-11-02 2020-09-17 Aicuris Gmbh & Co Kg Nueva 6,7-dihidro-4h-pirazolo [1,5-a] pirazina indole -2-carboxamidas 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)
UY38437A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (hbv)
UY38435A (es) 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas urea 6,7-dihidro-4h-pirazol[1,5-a] pirazinas activas contra el virus de la hepatitis b (vhb)
TW202415643A (zh) 2018-12-12 2024-04-16 加拿大商愛彼特生物製藥公司 經取代之芳基甲基脲類及雜芳基甲基脲類、其類似物及其使用方法
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
MA55020A (fr) 2019-02-22 2021-12-29 Janssen Sciences Ireland Unlimited Co Dérivés d'amide utiles dans le traitement d'une infection par le virus de l'hépatite b ou de maladies induites par le virus de l'hépatite b
BR112021021580A2 (pt) 2019-04-30 2022-01-04 Aicuris Gmbh & Co Kg Fenil e piridil ureias inovadoras ativas contra o vírus da hepatite b (hbv)
JP2022533007A (ja) 2019-04-30 2022-07-21 アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト Ｂ型肝炎ウイルス（ｈｂｖ）に対し活性な新規のインドリジン－２－カルボキサミド
BR112021021652A2 (pt) 2019-04-30 2021-12-21 Aicuris Gmbh & Co Kg Oxalil piperazinas inovadoras ativas contra o vírus da hepatite b (hbv)
EP3962914A1 (en) 2019-04-30 2022-03-09 AiCuris GmbH & Co. KG Novel indole-2-carboxamides active against the hepatitis b virus (hbv)
BR112021021454A2 (pt) 2019-05-06 2021-12-21 Janssen Sciences Ireland Unlimited Co Derivados de amida úteis no tratamento da infecção por hbv ou doenças induzidas por hbv
BR112021023622A2 (pt) * 2019-05-24 2022-04-19 Assembly Biosciences Inc Composições farmaceuticas para o tratamento de hbv
CN110526878A (zh) * 2019-09-16 2019-12-03 成都睿智化学研究有限公司 一种2-(噁唑基)乙胺的制备方法
CN111072551A (zh) * 2019-12-30 2020-04-28 上海睿瓦科技有限公司 催化氢化一步法制取哌啶胺的方法
CN121248511A (zh) * 2020-04-22 2026-01-02 组装生物科学股份有限公司 用于治疗hbv的5元杂芳基甲酰胺化合物
CN113135848A (zh) * 2021-04-26 2021-07-20 深圳市华先医药科技有限公司 一种巯基烯酯类化合物的制备方法
CN113636960A (zh) * 2021-08-24 2021-11-12 上海皓元医药股份有限公司 一种2-(氯磺酰基)环己烷-1-烯甲酸乙酯衍生物的制备方法
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法
CN115353479A (zh) * 2022-07-27 2022-11-18 常州琦诺生物科技有限公司 一种5-溴-2-碘嘧啶的制备方法
WO2024089216A1 (en) 2022-10-27 2024-05-02 Syngenta Crop Protection Ag Novel sulfur-containing heteroaryl carboxamide compounds
WO2025069039A1 (en) * 2023-09-28 2025-04-03 Rajaram Samant An in situ process for the preparation of primary amine compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992019277A1 (en) * 1991-05-02 1992-11-12 The Wellcome Foundation Limited Antiviral dibenzothiazepinone derivatives
WO2013006394A1 (en) * 2011-07-01 2013-01-10 Institute For Hepatitis And Virus Research Sulfamoylbenzamide derivatives as antiviral agents against hbv infection

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1480553A (en) * 1976-06-03 1977-07-20 Pfizer Ltd Tricyclic sulphonamides
JPS58225074A (ja) 1982-06-25 1983-12-27 Chugai Pharmaceut Co Ltd ジベンゾオキサゼピン誘導体
US5512563A (en) * 1993-07-29 1996-04-30 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US20070208166A1 (en) * 2003-10-24 2007-09-06 Exelixis, Inc. Tao Kinase Modulators And Method Of Use
DE102004004928A1 (de) 2004-01-31 2005-08-18 Bayer Healthcare Ag Dibenzoxazepine II
CA2625423A1 (en) * 2005-10-17 2007-04-26 Acadia Pharmaceuticals Inc. Cb-1 modulating compounds and their use
US20070105835A1 (en) 2005-11-07 2007-05-10 Kazantsev Aleksey G Compositions and methods for modulating poly(ADP-ribose) polymerase activity
US20100022509A1 (en) 2006-06-07 2010-01-28 Fahey Robert C Inhibitors of MshC and Homologs Thereof, and Methods of Identifying Same
WO2008118141A2 (en) 2006-10-17 2008-10-02 Acadia Pharmaceuticals Inc. Use of cannabinoid modulating compounds in combination with other therapeutic compounds for adjunctive therapy
AU2009274255A1 (en) 2008-07-23 2010-01-28 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the plasmodial surface anion channel as antimalarials
CN104530079B (zh) * 2009-12-18 2017-10-20 北京凯因科技股份有限公司 C型肝炎病毒复制的新型抑制剂
WO2012045194A1 (en) 2010-10-09 2012-04-12 Abbott Laboratories Benzodiazepinones as fak inhibitors for treatment of cancer
WO2013010069A1 (en) 2011-07-13 2013-01-17 Indiana University Research And Technology Corporation Modified viral structural protein with antiviral activity
AU2013207205B2 (en) 2012-01-06 2017-02-02 Janssen Sciences Ireland Uc 4,4-disubstituted-1,4-dihydropyrimidines and the use thereof as medicaments for the treatment of Hepatitis B
SG11201501360TA (en) 2012-08-28 2015-03-30 Janssen Sciences Ireland Uc Fused bicyclic sulfamoyl derivatives and the use thereof as medicaments for the treatment of hepatitis b
HK1208465A1 (en) 2012-08-28 2016-03-04 Janssen Sciences Ireland Uc Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
JP6113285B2 (ja) 2012-09-10 2017-04-12 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及び予防用の６−アミノ酸ヘテロアリールジヒドロピリミジン
EP2917184A4 (en) 2012-11-09 2016-06-29 Univ Indiana Res & Tech Corp ALTERNATIVE USES FOR HBV ARRANGEMENT EFFECTORS
CA2892606A1 (en) 2012-12-06 2014-06-12 Baruch S. Blumberg Institute Functionalized benzamide derivatives as antiviral agents against hbv infection
US9938236B2 (en) 2012-12-27 2018-04-10 Drexel University Antiviral agents against HBV infection
RU2519546C1 (ru) 2013-01-16 2014-06-10 Общество С Ограниченной Ответственностью "Биоинтегратор" (Ооо "Биоинтегратор") КОНЪЮГАТЫ И МАЛЫЕ МОЛЕКУЛЫ, ВЗАИМОДЕЙСТВУЮЩИЕ С РЕЦЕПТОРОМ CD16а
DK2961732T3 (en) 2013-02-28 2017-07-10 Janssen Sciences Ireland Uc SULFAMOYLARYLAMIDS AND USE THEREOF AS MEDICINES TO TREAT HEPATITIS B
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
EP3943087A1 (en) 2013-03-15 2022-01-26 Celgene CAR LLC Heteroaryl compounds and uses thereof
WO2014161888A1 (en) 2013-04-03 2014-10-09 Janssen R&D Ireland N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
RS57999B1 (sr) 2013-05-17 2019-01-31 Janssen Sciences Ireland Uc Derivati sulfamoiltiofenamida i njihova primena kao lekovi za tretman hepatitisa b
WO2014184328A1 (en) 2013-05-17 2014-11-20 F. Hoffmann-La Roche Ag 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
BR112015031903A8 (pt) 2013-06-19 2019-12-31 Seragon Pharmaceuticals Inc composto, sal farmaceuticamente aceitável, composição farmacêutica e uso de um composto
US9550742B2 (en) * 2013-07-29 2017-01-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services 11-OXO-10,11-dihydrodibenzo[B,F][1,4]thiazepine S-oxide derivatives and their use as dopamine D2 receptor antagonists
MX363600B (es) 2014-03-13 2019-03-28 Univ Indiana Res & Tech Corp Moduladores alostericos de proteina nucleo de hepatitis b.
WO2015189035A1 (en) 2014-06-10 2015-12-17 Basf Se Substituted [1,2,4]triazole and imidazole compounds as fungicides
TWI721016B (zh) 2015-09-15 2021-03-11 美商艾森伯利生物科學公司 B型肝炎核心蛋白質調節劑
US10811219B2 (en) 2018-08-07 2020-10-20 Applied Materials Israel Ltd. Method for evaluating a region of an object

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992019277A1 (en) * 1991-05-02 1992-11-12 The Wellcome Foundation Limited Antiviral dibenzothiazepinone derivatives
WO2013006394A1 (en) * 2011-07-01 2013-01-10 Institute For Hepatitis And Virus Research Sulfamoylbenzamide derivatives as antiviral agents against hbv infection

Non-Patent Citations (18)

* Cited by examiner, † Cited by third party
Title
no 20885138;无;《NCBI Database》;20071205 *
no 20885146;无;《NCBI Database》;20071205 *
no 20885149;无;《NCBI Database》;20071205 *
no 20885150;无;《NCBI Database》;20071205 *
no 20885151;无;《NCBI Database》;20071205 *
no 23734106;无;《NCBI Database》;20080220 *
no 23797169;无;《NCBI Database》;20080220 *
no 3576843;无;《NCBI Database》;20050909 *
no 4097179;无;《NCBI Database》;20050913 *
no 4119171;无;《NCBI Database》;20050913 *
no 4152425;无;《NCBI Database》;20050913 *
no 4163918;无;《NCBI Database》;20050913 *
no 4163919;无;《NCBI Database》;20050913 *
no 4167865;无;《NCBI Database》;20050913 *
no 4338109;无;《NCBI Database》;20050914 *
no 4577044;无;《NCBI Database》;20050915 *
no 46260649;无;《NCBI Database》;20100721 *
no 53384785;无;《NCBI Database》;20111013 *

Also Published As

Publication number Publication date
EP3607950A2 (en) 2020-02-12
JP2019151650A (ja) 2019-09-12
US20230019129A1 (en) 2023-01-19
EP3116316A4 (en) 2018-05-23
CA2942533C (en) 2020-12-08
CA2942533A1 (en) 2015-09-17
JP6602311B2 (ja) 2019-11-06
US20170015658A1 (en) 2017-01-19
SG10202001506UA (en) 2020-04-29
PH12016501762B1 (en) 2023-01-11
HRP20191444T1 (hr) 2019-11-29
AU2019203754A1 (en) 2019-06-20
MX2019003525A (es) 2019-07-08
WO2015138895A1 (en) 2015-09-17
AU2015229174A1 (en) 2016-09-22
PH12016501762A1 (en) 2017-02-06
AU2015229174B2 (en) 2019-04-11
AP2016009477A0 (en) 2016-09-30
US10947224B2 (en) 2021-03-16
US10183936B2 (en) 2019-01-22
HUE046567T2 (hu) 2020-03-30
US20180273521A1 (en) 2018-09-27
NZ723972A (en) 2021-08-27
IL247575B (en) 2020-05-31
JP2017518959A (ja) 2017-07-13
SG11201607268UA (en) 2016-09-29
MX2016011800A (es) 2017-04-27
ZA201606209B (en) 2019-04-24
PH12021553231A1 (en) 2023-01-23
CN106413402A (zh) 2017-02-15
PT3116316T (pt) 2019-09-30
CN110437153A (zh) 2019-11-12
IL273132B (en) 2021-05-31
KR102363174B1 (ko) 2022-02-15
EP3607950A3 (en) 2020-03-18
MX363600B (es) 2019-03-28
IL247575A0 (en) 2016-11-30
IL273132A (en) 2020-04-30
KR20160135747A (ko) 2016-11-28
CL2016002269A1 (es) 2017-08-18
IL282391A (en) 2021-06-30
PL3116316T3 (pl) 2020-03-31
ES2748029T3 (es) 2020-03-12
RS59430B1 (sr) 2019-11-29
EP3116316A1 (en) 2017-01-18
EP3116316B1 (en) 2019-07-10
EP3974426A1 (en) 2022-03-30
DK3116316T3 (da) 2019-08-19
DOP2016000233A (es) 2016-12-30

Similar Documents

Publication Publication Date Title
CN106413402B (zh) 乙型肝炎核心蛋白变构调节剂
JP7150903B2 (ja) Ｂ型肝炎ウイルスコアタンパク質モジュレーター
US10987360B2 (en) Hepatitis B core protein modulators
HK40072544A (en) Hepatitis b core protein allosteric modulators
HK40023225A (en) Hepatitis b core protein allosteric modulators
BR112016020895B1 (pt) Moduladores alostéricos da proteína do núcleo da hepatite b, seus usos, e composição farmacêutica
HK1231697B (en) Hepatitis b core protein allosteric modulators
HK1231697A1 (en) Hepatitis b core protein allosteric modulators
OA18052A (en) Hepatitis B core protein allosteric modulators.
NZ723972B2 (en) Hepatitis b core protein allosteric modulators

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20201030