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)
  • 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)
  • 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)
  • 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 2006-12-05
EP06125443.9 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) 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)

Families Citing this family (19)

* 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
HUE062481T2 (hu) 2015-01-27 2023-11-28 Janssen Pharmaceutica Nv Diszpergálódó készítmények
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
EP3366676B1 (en) * 2015-10-20 2021-05-26 Zhejiang Hisun Pharmaceutical Co., Ltd Crystalline forms of bedaquiline fumarate and preparation methods therefor
AU2017298187B2 (en) * 2016-07-20 2019-11-14 Novartis Ag Aminopyridine derivatives and their use as selective ALK-2 inhibitors
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
JP7102500B2 (ja) 2017-07-14 2022-07-19 ヤンセン ファーマシューティカ エヌ．ベー． 長時間作用型配合物
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
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
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
CN116406270A (zh) 2020-11-12 2023-07-07 詹森药业有限公司 在治疗非结核分枝杆菌疾病时的贝达喹啉、乙胺丁醇和大环内酯的组合
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

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
IL122025A (en) * 1996-10-30 2003-01-12 Lilly Co Eli Use of raloxifene or pharmaceutically acceptable salts or solvates thereof, in the preparation of a medicament for preventing 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
KR101276571B1 (ko) * 2004-09-02 2013-06-18 얀센 파마슈티카 엔.브이. 4-((4-((4-(2-시아노에텐일)-2,6-디메틸페닐)아미노-2-피리미딘일)아미노)벤조니트릴의 푸마레이트
KR101301573B1 (ko) * 2004-12-24 2013-09-04 얀센 파마슈티카 엔.브이. 잠재성 튜버큐로시스의 치료법

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

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