HRP20120639T1 - Fumaratna sol (alfa s, beta r)-6-bromo-alfa-[2-(dimetilamino)etil]-2-metoksi-alfa-1-naftalenil-beta-fenil-3-kinolinetanola - Google Patents
Fumaratna sol (alfa s, beta r)-6-bromo-alfa-[2-(dimetilamino)etil]-2-metoksi-alfa-1-naftalenil-beta-fenil-3-kinolinetanola Download PDFInfo
- Publication number
- HRP20120639T1 HRP20120639T1 HRP20120639TT HRP20120639T HRP20120639T1 HR P20120639 T1 HRP20120639 T1 HR P20120639T1 HR P20120639T T HRP20120639T T HR P20120639TT HR P20120639 T HRP20120639 T HR P20120639T HR P20120639 T1 HRP20120639 T1 HR P20120639T1
- Authority
- HR
- Croatia
- Prior art keywords
- alpha
- compound
- beta
- mixture obtained
- wetting agent
- Prior art date
Links
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 title claims abstract 5
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- 238000002360 preparation method Methods 0.000 claims 8
- 239000000080 wetting agent Substances 0.000 claims 7
- 239000011230 binding agent Substances 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 206010062207 Mycobacterial infection Diseases 0.000 claims 5
- 239000004480 active ingredient Substances 0.000 claims 5
- 208000027531 mycobacterial infectious disease Diseases 0.000 claims 5
- 238000002156 mixing Methods 0.000 claims 4
- 239000007884 disintegrant Substances 0.000 claims 3
- 239000000314 lubricant Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000011248 coating agent Substances 0.000 claims 2
- 238000000576 coating method Methods 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 238000007580 dry-mixing Methods 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 238000005469 granulation Methods 0.000 claims 2
- 230000003179 granulation Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 238000007873 sieving Methods 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 238000005507 spraying Methods 0.000 claims 2
- VPDAGUVEZGEHJJ-UHFFFAOYSA-N 2-quinolin-2-ylethanol Chemical compound C1=CC=CC2=NC(CCO)=CC=C21 VPDAGUVEZGEHJJ-UHFFFAOYSA-N 0.000 claims 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- -1 sorbitan fatty acid ester Chemical class 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
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
- 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
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)
- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120639T1 true HRP20120639T1 (hr) | 2012-08-31 |
Family
ID=37983588
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120639TT HRP20120639T1 (hr) | 2006-12-05 | 2012-08-06 | Fumaratna sol (alfa s, beta r)-6-bromo-alfa-[2-(dimetilamino)etil]-2-metoksi-alfa-1-naftalenil-beta-fenil-3-kinolinetanola |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US8546428B2 (da) |
| EP (1) | EP2086940B1 (da) |
| JP (2) | JP2010511663A (da) |
| KR (1) | KR101514700B1 (da) |
| CN (2) | CN101547904A (da) |
| AP (1) | AP2498A (da) |
| AR (1) | AR064149A1 (da) |
| AU (1) | AU2007328945B2 (da) |
| BR (1) | BRPI0719693A2 (da) |
| CA (1) | CA2668512C (da) |
| CL (1) | CL2007003472A1 (da) |
| CY (1) | CY1113594T1 (da) |
| DK (1) | DK2086940T3 (da) |
| EA (1) | EA017091B9 (da) |
| ES (1) | ES2387923T3 (da) |
| HK (1) | HK1214513A1 (da) |
| HR (1) | HRP20120639T1 (da) |
| IL (1) | IL199077A (da) |
| JO (1) | JO2973B1 (da) |
| ME (1) | ME01456B (da) |
| MX (1) | MX2009005909A (da) |
| MY (1) | MY148844A (da) |
| NO (1) | NO342773B1 (da) |
| NZ (1) | NZ576485A (da) |
| PE (1) | PE20081350A1 (da) |
| PL (1) | PL2086940T3 (da) |
| PT (1) | PT2086940E (da) |
| RS (1) | RS52408B (da) |
| SI (1) | SI2086940T1 (da) |
| TW (1) | TWI417098B (da) |
| UA (1) | UA97813C2 (da) |
| UY (1) | UY30762A1 (da) |
| WO (1) | WO2008068231A1 (da) |
| ZA (1) | ZA200903907B (da) |
Families Citing this family (16)
| 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 |
| EP3250182B1 (en) | 2015-01-27 | 2023-04-26 | 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 |
| KR102106318B1 (ko) * | 2015-10-20 | 2020-05-06 | 쯔지앙 하이썬 파머슈티컬 컴퍼니, 리미티드 | 베다퀼린 푸마레이트의 결정형 및 그의 제조방법 |
| WO2018014829A1 (en) * | 2016-07-20 | 2018-01-25 | 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 |
| KR20210113628A (ko) | 2019-01-09 | 2021-09-16 | 얀센 파마슈티카 엔.브이. | 비결핵성 마이코박테리아 질환의 치료에서의 조합물 |
| 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 |
| WO2022101244A1 (en) | 2020-11-12 | 2022-05-19 | 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)
| 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 |
| JP2001503411A (ja) | 1996-10-28 | 2001-03-13 | ディパートメント オブ ジ アーミー，ユー．エス．ガバメント | 抗生物質耐性感染症の処置のための化合物、組成物および方法 |
| 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 |
| EP1527050B1 (en) * | 2002-07-25 | 2010-04-07 | Janssen Pharmaceutica N.V. | Quinoline derivatives and their use as mycobacterial inhibitors |
| AU2002350719A1 (en) * | 2002-11-29 | 2004-06-23 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
| KR20130024969A (ko) * | 2004-05-28 | 2013-03-08 | 얀센 파마슈티카 엔.브이. | 약물 내성 마이코박테리아 질환 치료를 위한 치환된 퀴놀린 유도체의 용도 |
| AU2005279157B2 (en) * | 2004-09-02 | 2011-07-14 | Janssen Pharmaceutica N.V. | Fumarate of 4-[[4-[[4- (2-cyanoethenyl) -2,6-dimethylphenyl]amino)-2-pyrimidinyl)amino]benzonitrile |
| BG66437B1 (bg) * | 2004-12-24 | 2014-07-31 | Janssen Pharmaceutica N.V. | Използване на хинолинови съединения за лечение на латентна туберкулоза |
-
2007
- 2007-03-12 UA UAA200904218A patent/UA97813C2/uk unknown
- 2007-12-02 JO JO2007511A patent/JO2973B1/en active
- 2007-12-03 AP AP2009004870A patent/AP2498A/xx active
- 2007-12-03 CL CL200703472A patent/CL2007003472A1/es unknown
- 2007-12-03 JP JP2009539724A patent/JP2010511663A/ja active Pending
- 2007-12-03 KR KR1020097011043A patent/KR101514700B1/ko active IP Right Grant
- 2007-12-03 SI SI200730984T patent/SI2086940T1/sl unknown
- 2007-12-03 PT PT07847697T patent/PT2086940E/pt unknown
- 2007-12-03 RS RS20120336A patent/RS52408B/en unknown
- 2007-12-03 BR BRPI0719693-8A2A patent/BRPI0719693A2/pt not_active Application Discontinuation
- 2007-12-03 CN CNA2007800448088A patent/CN101547904A/zh active Pending
- 2007-12-03 MY MYPI20092284A patent/MY148844A/en unknown
- 2007-12-03 US US12/515,986 patent/US8546428B2/en active Active
- 2007-12-03 AU AU2007328945A patent/AU2007328945B2/en active Active
- 2007-12-03 NZ NZ576485A patent/NZ576485A/en unknown
- 2007-12-03 MX MX2009005909A patent/MX2009005909A/es active IP Right Grant
- 2007-12-03 ME MEP-2012-95A patent/ME01456B/me unknown
- 2007-12-03 EP EP07847697A patent/EP2086940B1/en active Active
- 2007-12-03 WO PCT/EP2007/063186 patent/WO2008068231A1/en active Application Filing
- 2007-12-03 EA EA200970532A patent/EA017091B9/ru active Protection Beyond IP Right Term
- 2007-12-03 CA CA2668512A patent/CA2668512C/en active Active
- 2007-12-03 CN CN201510368829.1A patent/CN105012303A/zh active Pending
- 2007-12-03 PL PL07847697T patent/PL2086940T3/pl unknown
- 2007-12-03 ES ES07847697T patent/ES2387923T3/es active Active
- 2007-12-03 DK DK07847697.5T patent/DK2086940T3/da active
- 2007-12-04 TW TW096146000A patent/TWI417098B/zh active
- 2007-12-05 PE PE2007001719A patent/PE20081350A1/es active IP Right Grant
- 2007-12-05 UY UY30762A patent/UY30762A1/es active IP Right Grant
- 2007-12-05 AR ARP070105442A patent/AR064149A1/es not_active Application Discontinuation
-
2009
- 2009-06-02 IL IL199077A patent/IL199077A/en active IP Right Grant
- 2009-06-04 ZA ZA2009/03907A patent/ZA200903907B/en unknown
- 2009-07-06 NO NO20092535A patent/NO342773B1/no unknown
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2012
- 2012-08-06 HR HRP20120639TT patent/HRP20120639T1/hr unknown
- 2012-08-13 CY CY20121100734T patent/CY1113594T1/el unknown
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2014
- 2014-09-19 JP JP2014191134A patent/JP5894239B2/ja active Active
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2016
- 2016-03-04 HK HK16102481.4A patent/HK1214513A1/zh unknown
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