CN105012303A - (αS,βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐 - Google Patents

(αS,βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐 Download PDF

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Publication number
CN105012303A
CN105012303A CN201510368829.1A CN201510368829A CN105012303A CN 105012303 A CN105012303 A CN 105012303A CN 201510368829 A CN201510368829 A CN 201510368829A CN 105012303 A CN105012303 A CN 105012303A
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CN
China
Prior art keywords
pharmaceutical composition
peg
alpha
active ingredient
methoxy
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.)
Pending
Application number
CN201510368829.1A
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English (en)
Chinese (zh)
Inventor
J.F.A.L.赫格伊
W.A.A.阿尔特曼
Y.L.兰
S.C.M.斯托克布罗克斯
C.利斯
P.J.M.范雷摩尔特尔
A.福雷
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.)
Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37983588&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN105012303(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CN105012303A publication Critical patent/CN105012303A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201510368829.1A 2006-12-05 2007-12-03 (αS,βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐 Pending CN105012303A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06125443.9 2006-12-05
EP06125443 2006-12-05
CNA2007800448088A CN101547904A (zh) 2006-12-05 2007-12-03 (αS，βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNA2007800448088A Division CN101547904A (zh) 2006-12-05 2007-12-03 (αS，βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐

Publications (1)

Publication Number Publication Date
CN105012303A true CN105012303A (zh) 2015-11-04

Family

ID=37983588

Family Applications (2)

Application Number Title Priority Date Filing Date
CNA2007800448088A Pending CN101547904A (zh) 2006-12-05 2007-12-03 (αS，βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐
CN201510368829.1A Pending CN105012303A (zh) 2006-12-05 2007-12-03 (αS,βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CNA2007800448088A Pending CN101547904A (zh) 2006-12-05 2007-12-03 (αS，βR)-6-溴-α-[2-(二甲胺基)乙基]-2-甲氧基-α-1-萘基-β-苯基-3-喹啉乙醇的富马酸盐

Country Status (34)

Country Link
US (1) US8546428B2 (enExample)
EP (1) EP2086940B1 (enExample)
JP (2) JP2010511663A (enExample)
KR (1) KR101514700B1 (enExample)
CN (2) CN101547904A (enExample)
AP (1) AP2498A (enExample)
AR (1) AR064149A1 (enExample)
AU (1) AU2007328945B2 (enExample)
BR (1) BRPI0719693A2 (enExample)
CA (1) CA2668512C (enExample)
CL (1) CL2007003472A1 (enExample)
CY (1) CY1113594T1 (enExample)
DK (1) DK2086940T3 (enExample)
EA (1) EA017091B9 (enExample)
ES (1) ES2387923T3 (enExample)
HK (1) HK1214513A1 (enExample)
HR (1) HRP20120639T1 (enExample)
IL (1) IL199077A (enExample)
JO (1) JO2973B1 (enExample)
ME (1) ME01456B (enExample)
MX (1) MX2009005909A (enExample)
MY (1) MY148844A (enExample)
NO (1) NO342773B1 (enExample)
NZ (1) NZ576485A (enExample)
PE (1) PE20081350A1 (enExample)
PL (1) PL2086940T3 (enExample)
PT (1) PT2086940E (enExample)
RS (1) RS52408B (enExample)
SI (1) SI2086940T1 (enExample)
TW (1) TWI417098B (enExample)
UA (1) UA97813C2 (enExample)
UY (1) UY30762A1 (enExample)
WO (1) WO2008068231A1 (enExample)
ZA (1) ZA200903907B (enExample)

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US20120010216A1 (en) * 2010-07-06 2012-01-12 Brown Arthur M Pharmaceutical compositions containing vanoxerine
CZ2014708A3 (cs) 2014-10-16 2016-04-27 Zentiva, K.S. Soli Bedaquilinu
AU2016212116B2 (en) * 2015-01-27 2021-07-15 Janssen Pharmaceutica Nv Dispersible compositions
CN106279017A (zh) * 2015-05-21 2017-01-04 重庆圣华曦药业股份有限公司 贝达喹啉晶型、组合物及其制备方法
CZ2015391A3 (cs) 2015-06-09 2016-12-21 Zentiva, K.S. Sůl bedaquilinu s kyselinou citronovou
CN108349898B (zh) * 2015-10-20 2021-03-23 浙江海正药业股份有限公司 富马酸贝达喹啉的晶型及其制备方法
PT3971177T (pt) * 2016-07-20 2024-07-30 Novartis Ag Derivados de aminopiridina e a sua utilização como inibidores seletivos de alk-2
CN106316943A (zh) * 2016-07-27 2017-01-11 重庆华邦制药有限公司 富马酸贝达喹啉晶型化合物的精制方法
EP3651736B1 (en) 2017-07-14 2021-06-23 Janssen Pharmaceutica NV Long-acting formulations
US20220023282A1 (en) * 2018-12-13 2022-01-27 Mannkind Corporation Compositions of Bedaquiline, Combinations Comprising Them, Processes for Their Preparation, Uses and Methods of Treatment Comprising Them
US20220062319A1 (en) 2019-01-09 2022-03-03 Janssen Pharmaceutica Nv Combination in the treatment of nontuberculous mycobacterial diseases
WO2020161743A1 (en) * 2019-02-08 2020-08-13 Mylan Laboratories Limited Process for the preparation of bedaquiline fumarate
KR102303635B1 (ko) * 2020-07-01 2021-09-17 동아에스티 주식회사 (1r,2s)-1-(6-브로모-2-메톡시퀴놀린-3-일)-4-디메틸아미노-2-(1-나프틸)-1-페닐-부탄-2-올 및 이의 약제학적으로 허용 가능한 염의 제조방법
CN111888477B (zh) * 2020-09-15 2023-03-07 北京福元医药股份有限公司 一种贝达喹啉药物制剂
US20230346770A1 (en) 2020-11-12 2023-11-02 Janssen Pharmaceutica Nv Combination of bedaquiline, ethambutol and a macrolide in the treatment of nontuberculous mycobacterial diseases
US11793808B2 (en) 2021-02-22 2023-10-24 Mannkind Corp. Compositions of clofazimine, combinations comprising them, processes for their preparation, uses and methods comprising them
WO2023150747A1 (en) 2022-02-07 2023-08-10 Insmed Incorporated Dry powder compositions of bedaquiline and salts and methods of use thereof
WO2023232838A1 (en) 2022-05-31 2023-12-07 Janssen Pharmaceutica Nv Bedaquiline for use in the treatment of leprosy
CN117399070B (zh) * 2022-07-07 2025-06-24 上海交通大学 含有螯合配体的双手性金属协同催化体系及其不对称合成贝达喹啉的应用

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WO2004011436A1 (en) * 2002-07-25 2004-02-05 Janssen Pharmaceutica N.V. Quinoline derivatives and their use as mycobacterial inhibitors
WO2005117875A1 (en) * 2004-05-28 2005-12-15 Janssen Pharmaceutica N.V. Use of substituted quinoline derivatives for the treatment of drug resistant mycobacterial diseases

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Also Published As

Publication number Publication date
RS52408B (sr) 2013-02-28
CA2668512A1 (en) 2008-06-12
ZA200903907B (en) 2013-08-28
CN101547904A (zh) 2009-09-30
HRP20120639T1 (hr) 2012-08-31
AR064149A1 (es) 2009-03-18
JO2973B1 (en) 2016-03-15
ES2387923T3 (es) 2012-10-04
HK1214513A1 (zh) 2016-07-29
NO20092535L (no) 2009-08-06
US8546428B2 (en) 2013-10-01
US20100028428A1 (en) 2010-02-04
IL199077A (en) 2016-09-29
CY1113594T1 (el) 2016-06-22
CA2668512C (en) 2015-03-24
PL2086940T3 (pl) 2012-10-31
NZ576485A (en) 2012-01-12
EA200970532A1 (ru) 2009-10-30
MY148844A (en) 2013-06-14
PT2086940E (pt) 2012-08-09
KR101514700B1 (ko) 2015-04-24
CL2007003472A1 (es) 2008-08-22
TWI417098B (zh) 2013-12-01
AP2498A (en) 2012-10-19
SI2086940T1 (sl) 2012-09-28
EA017091B1 (ru) 2012-09-28
PE20081350A1 (es) 2008-09-18
EP2086940A1 (en) 2009-08-12
AU2007328945B2 (en) 2014-04-03
ME01456B (me) 2014-04-20
TW200838527A (en) 2008-10-01
KR20090087020A (ko) 2009-08-14
BRPI0719693A2 (pt) 2013-12-24
JP2010511663A (ja) 2010-04-15
DK2086940T3 (da) 2012-08-20
EP2086940B1 (en) 2012-05-16
UA97813C2 (uk) 2012-03-26
AP2009004870A0 (en) 2009-06-30
JP5894239B2 (ja) 2016-03-23
AU2007328945A1 (en) 2008-06-12
UY30762A1 (es) 2008-07-03
EA017091B9 (ru) 2014-10-30
WO2008068231A1 (en) 2008-06-12
NO342773B1 (no) 2018-08-06
JP2015028049A (ja) 2015-02-12
MX2009005909A (es) 2009-06-16

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