CN101547904A - (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
CN101547904A
CN101547904A CNA2007800448088A CN200780044808A CN101547904A CN 101547904 A CN101547904 A CN 101547904A CN A2007800448088 A CNA2007800448088 A CN A2007800448088A CN 200780044808 A CN200780044808 A CN 200780044808A CN 101547904 A CN101547904 A CN 101547904A
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composition
peg
milligrams
randomly
compound
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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
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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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=CN101547904(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
Priority to CN201510368829.1A priority Critical patent/CN105012303A/zh
Publication of CN101547904A publication Critical patent/CN101547904A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/227Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
CNA2007800448088A 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 CN101547904A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510368829.1A 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

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06125443.9 2006-12-05
EP06125443 2006-12-05

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510368829.1A Division 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

Publications (1)

Publication Number Publication Date
CN101547904A true CN101547904A (zh) 2009-09-30

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 After (1)

Application Number Title Priority Date Filing Date
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

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)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
WO2017066926A1 (zh) * 2015-10-20 2017-04-27 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
CN107205945A (zh) * 2015-01-27 2017-09-26 詹森药业有限公司 可分散组合物
CN111888477A (zh) * 2020-09-15 2020-11-06 北京福元医药股份有限公司 一种贝达喹啉药物制剂
US20250083126A1 (en) * 2022-07-07 2025-03-13 Shanghai Jiao Tong University Chiral bimetallic cooperative catalysis system containing chelating ligand and use thereof in asymmetric synthesis of bedaquiline

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CZ2015391A3 (cs) * 2015-06-09 2016-12-21 Zentiva, K.S. Sůl bedaquilinu s kyselinou citronovou
LT3971177T (lt) * 2016-07-20 2024-08-26 Novartis Ag Aminopiridino dariniai ir jų panaudojimas kaip selektyvių alk-2 inhibitorių
RS65207B1 (sr) 2017-07-14 2024-03-29 Janssen Pharmaceutica Nv Formulacije bedakvilina sa dugim delovanjem
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
JP2022516671A (ja) 2019-01-09 2022-03-01 ヤンセン ファーマシューティカ エヌ.ベー. 非結核性抗酸菌症の処置における組合せ
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
EP4243800A1 (en) 2020-11-12 2023-09-20 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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3237575A1 (de) * 1982-10-09 1984-04-12 Dr. Karl Thomae Gmbh, 7950 Biberach Neue orale mopidamolformen
GB8824392D0 (en) * 1988-10-18 1988-11-23 Ciba Geigy Ag Dispersible formulation
TW355683B (en) * 1994-02-17 1999-04-11 Janssen Pharmaceutica Nv Composition containing micronized nebivolol
WO1998018326A1 (en) 1996-10-28 1998-05-07 Department Of The Army, U.S. Government Compounds, compositions and methods for treating antibiotic-resistant infections
CZ341297A3 (cs) * 1996-10-30 1998-05-13 Eli Lilly And Company Způsob zlepšení léčby nebo profylaxe rakoviny prsu
US6819464B2 (en) * 2002-06-19 2004-11-16 Seiko Epson Corporation Optical modulator, optical device and projector
DK2301544T3 (da) * 2002-07-25 2013-01-02 Janssen Pharmaceutica Nv Quinolinderivater som mellemprodukter til mykobakterielle inhibitorer
WO2004050068A1 (en) * 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
ATE390925T1 (de) * 2004-05-28 2008-04-15 Janssen Pharmaceutica Nv Verwendung von substituierten chinolin-derivaten zur behandlung von arzneimittelresistenten mycobakteriellen erkrankungen
WO2006024667A1 (en) * 2004-09-02 2006-03-09 Janssen Pharmaceutica N.V. Furamate of 4-( (4-( (4- (2-cyanoethenyl) -2,6-dimethylphenyl)amino)-2-pyrimidinyl)amino)benzonitrile
JP2006182755A (ja) * 2004-12-24 2006-07-13 Janssen Pharmaceut Nv 潜伏性結核の処置

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107205945A (zh) * 2015-01-27 2017-09-26 詹森药业有限公司 可分散组合物
CN114129526A (zh) * 2015-01-27 2022-03-04 詹森药业有限公司 可分散组合物
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
WO2017066926A1 (zh) * 2015-10-20 2017-04-27 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
CN108349898A (zh) * 2015-10-20 2018-07-31 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
US10196360B2 (en) 2015-10-20 2019-02-05 Zhejiang Hisun Pharmaceutical Co., Ltd. Crystal forms of bedaquiline fumarate and preparation methods therefor
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
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
CN111888477A (zh) * 2020-09-15 2020-11-06 北京福元医药股份有限公司 一种贝达喹啉药物制剂
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
US20250083126A1 (en) * 2022-07-07 2025-03-13 Shanghai Jiao Tong University Chiral bimetallic cooperative catalysis system containing chelating ligand and use thereof in asymmetric synthesis of bedaquiline

Also Published As

Publication number Publication date
AP2009004870A0 (en) 2009-06-30
PT2086940E (pt) 2012-08-09
TWI417098B (zh) 2013-12-01
UA97813C2 (uk) 2012-03-26
EP2086940A1 (en) 2009-08-12
DK2086940T3 (da) 2012-08-20
TW200838527A (en) 2008-10-01
PE20081350A1 (es) 2008-09-18
MY148844A (en) 2013-06-14
MX2009005909A (es) 2009-06-16
AU2007328945A1 (en) 2008-06-12
HRP20120639T1 (hr) 2012-08-31
JP2010511663A (ja) 2010-04-15
US8546428B2 (en) 2013-10-01
JO2973B1 (en) 2016-03-15
ME01456B (me) 2014-04-20
KR20090087020A (ko) 2009-08-14
NO20092535L (no) 2009-08-06
HK1214513A1 (zh) 2016-07-29
EA017091B1 (ru) 2012-09-28
US20100028428A1 (en) 2010-02-04
SI2086940T1 (sl) 2012-09-28
JP5894239B2 (ja) 2016-03-23
CA2668512A1 (en) 2008-06-12
EA200970532A1 (ru) 2009-10-30
RS52408B (sr) 2013-02-28
AU2007328945B2 (en) 2014-04-03
AP2498A (en) 2012-10-19
NO342773B1 (no) 2018-08-06
ZA200903907B (en) 2013-08-28
AR064149A1 (es) 2009-03-18
EA017091B9 (ru) 2014-10-30
ES2387923T3 (es) 2012-10-04
NZ576485A (en) 2012-01-12
CL2007003472A1 (es) 2008-08-22
PL2086940T3 (pl) 2012-10-31
JP2015028049A (ja) 2015-02-12
UY30762A1 (es) 2008-07-03
CN105012303A (zh) 2015-11-04
EP2086940B1 (en) 2012-05-16
BRPI0719693A2 (pt) 2013-12-24
IL199077A (en) 2016-09-29
KR101514700B1 (ko) 2015-04-24
CY1113594T1 (el) 2016-06-22
CA2668512C (en) 2015-03-24
WO2008068231A1 (en) 2008-06-12

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