AU2007328945B2 - Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol - Google Patents

Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol Download PDF

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Publication number
AU2007328945B2
AU2007328945B2 AU2007328945A AU2007328945A AU2007328945B2 AU 2007328945 B2 AU2007328945 B2 AU 2007328945B2 AU 2007328945 A AU2007328945 A AU 2007328945A AU 2007328945 A AU2007328945 A AU 2007328945A AU 2007328945 B2 AU2007328945 B2 AU 2007328945B2
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alpha
pharmaceutical composition
peg
beta
compound
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AU2007328945A1 (en
Inventor
Wim Albert Alex Aelterman
Anne Faure
Jean Francois Alexandre Lucas Hegyi
Yolande Lydia Lang
Carina Leys
Sigrid Carl Maria Stokbroekx
Peter Jozef Maria Van Remoortere
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2007328945A 2006-12-05 2007-12-03 Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol Active AU2007328945B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06125443.9 2006-12-05
EP06125443 2006-12-05
PCT/EP2007/063186 WO2008068231A1 (en) 2006-12-05 2007-12-03 Fumarate salt of (alpha s, beta r)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

Publications (2)

Publication Number Publication Date
AU2007328945A1 AU2007328945A1 (en) 2008-06-12
AU2007328945B2 true AU2007328945B2 (en) 2014-04-03

Family

ID=37983588

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Application Number Title Priority Date Filing Date
AU2007328945A Active AU2007328945B2 (en) 2006-12-05 2007-12-03 Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

Country Status (34)

Country Link
US (1) US8546428B2 (enExample)
EP (1) EP2086940B1 (enExample)
JP (2) JP2010511663A (enExample)
KR (1) KR101514700B1 (enExample)
CN (2) CN105012303A (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)

Families Citing this family (18)

* 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
FI3250182T3 (fi) * 2015-01-27 2023-06-28 Janssen Pharmaceutica Nv Dispergoituvia koostumuksia
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
RU2018111482A (ru) * 2015-10-20 2019-11-21 Чжэцзян Хисунь Фармасьютикал Ко., Лтд. Кристаллические формы бедаквилин фумарата и способы их получения
DK3971177T3 (da) * 2016-07-20 2024-07-15 Novartis Ag Aminopyridin-derivater og anvendelse deraf som selektive ALK-2-inhibitorer
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
SI3943070T1 (sl) 2017-07-14 2024-03-29 Janssen Pharmaceutica Nv, Dolgo delujoče formulacije bedakilina
JP7654544B2 (ja) * 2018-12-13 2025-04-01 マンカインド コーポレイション ベダキリンの組成物、それらを含む組み合わせ、それらを調製するための方法、それらを含む使用及び治療方法
WO2020144197A1 (en) 2019-01-09 2020-07-16 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
KR20230107275A (ko) 2020-11-12 2023-07-14 얀센 파마슈티카 엔.브이. 비결핵성 마이코박테리아 질환의 치료에서 베다퀼린, 에탐부톨 및 마크롤라이드의 조합물
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (9)

* 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
IL122026A0 (en) * 1996-10-30 1998-03-10 Lilly Co Eli Improvements in or relating to the prophylaxis of breast cancer
US6819464B2 (en) * 2002-06-19 2004-11-16 Seiko Epson Corporation Optical modulator, optical device and projector
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
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004011436A1 (en) * 2002-07-25 2004-02-05 Janssen Pharmaceutica N.V. Quinoline derivatives and their use as mycobacterial inhibitors
US20050148581A1 (en) * 2002-07-25 2005-07-07 Van Gestel Jozef F.E. Novel 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

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BASTIN R. J. et al., "Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities" Organic Process Research & Development, 2000, Vol. 4, pages 427-435 *
BERGE, S. M. et al., "Pharmaceutical Salts", Journal of Pharmaceutical Sciences, 1977, Vol. 66(1), pages 1-19 *
BIGHLEY, L. D. et al.,"Salt forms of Drugs and Absorption", Encyclopedia of Pharmaceutical Technology. Edited by J. Swarbrick & J. O. Boylan, 1995, Vol. 13, pages 453-499 *
CAS RN 845533-86-0, STN Entry Date: 14 March 2005 *
GOULD, P. L., "Salt selection for Basic Drugs", International Journal of Pharmaceutics, 1986, Vol. 33, pages 201-217 *
STAHL, P. H., "Handbook of Pharmaceutical Salts: Properties, Selection and Use". VHCA, Verlag Helvetica Chimica Acta and Wiley-VCH, 2002, appendix pages 329-341 *

Also Published As

Publication number Publication date
EA017091B9 (ru) 2014-10-30
UA97813C2 (uk) 2012-03-26
MX2009005909A (es) 2009-06-16
JP2015028049A (ja) 2015-02-12
CA2668512C (en) 2015-03-24
AP2009004870A0 (en) 2009-06-30
NO20092535L (no) 2009-08-06
US20100028428A1 (en) 2010-02-04
TW200838527A (en) 2008-10-01
KR20090087020A (ko) 2009-08-14
TWI417098B (zh) 2013-12-01
WO2008068231A1 (en) 2008-06-12
HK1214513A1 (zh) 2016-07-29
JO2973B1 (en) 2016-03-15
SI2086940T1 (sl) 2012-09-28
AP2498A (en) 2012-10-19
US8546428B2 (en) 2013-10-01
HRP20120639T1 (hr) 2012-08-31
UY30762A1 (es) 2008-07-03
AR064149A1 (es) 2009-03-18
IL199077A (en) 2016-09-29
KR101514700B1 (ko) 2015-04-24
EA017091B1 (ru) 2012-09-28
EA200970532A1 (ru) 2009-10-30
EP2086940A1 (en) 2009-08-12
ES2387923T3 (es) 2012-10-04
JP5894239B2 (ja) 2016-03-23
MY148844A (en) 2013-06-14
RS52408B (sr) 2013-02-28
AU2007328945A1 (en) 2008-06-12
CA2668512A1 (en) 2008-06-12
PT2086940E (pt) 2012-08-09
ME01456B (me) 2014-04-20
CL2007003472A1 (es) 2008-08-22
NZ576485A (en) 2012-01-12
ZA200903907B (en) 2013-08-28
JP2010511663A (ja) 2010-04-15
CN105012303A (zh) 2015-11-04
DK2086940T3 (da) 2012-08-20
PL2086940T3 (pl) 2012-10-31
EP2086940B1 (en) 2012-05-16
PE20081350A1 (es) 2008-09-18
BRPI0719693A2 (pt) 2013-12-24
NO342773B1 (no) 2018-08-06
CY1113594T1 (el) 2016-06-22
CN101547904A (zh) 2009-09-30

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