JP2007502789A - 噴霧乾燥された無定形ｂｉｂｎ４０９６、その調製方法及び吸入剤としてのその使用 - Google Patents
噴霧乾燥された無定形ｂｉｂｎ４０９６、その調製方法及び吸入剤としてのその使用 Download PDFInfo
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- JP2007502789A JP2007502789A JP2006523576A JP2006523576A JP2007502789A JP 2007502789 A JP2007502789 A JP 2007502789A JP 2006523576 A JP2006523576 A JP 2006523576A JP 2006523576 A JP2006523576 A JP 2006523576A JP 2007502789 A JP2007502789 A JP 2007502789A
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- 238000002360 preparation method Methods 0.000 title claims abstract description 7
- 108010073488 1-(N(2)-(3,4-dibromo-N-((4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl)carbonyl)tyrosyl)lysyl)-4-(4-pyridinyl)piperazine Proteins 0.000 title 1
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- 229910002651 NO3 Inorganic materials 0.000 claims description 2
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- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000009056 active transport Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- GONOPSZTUGRENK-UHFFFAOYSA-N benzyl(trichloro)silane Chemical compound Cl[Si](Cl)(Cl)CC1=CC=CC=C1 GONOPSZTUGRENK-UHFFFAOYSA-N 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 239000012050 conventional carrier Substances 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000009089 cytolysis Effects 0.000 description 1
- 239000007857 degradation product Substances 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000009246 food effect Effects 0.000 description 1
- 235000021471 food effect Nutrition 0.000 description 1
- 235000019253 formic acid Nutrition 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 239000010514 hydrogenated cottonseed oil Substances 0.000 description 1
- 238000010902 jet-milling Methods 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-L malate(2-) Chemical compound [O-]C(=O)C(O)CC([O-])=O BJEPYKJPYRNKOW-UHFFFAOYSA-L 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- IWYDHOAUDWTVEP-UHFFFAOYSA-M mandelate Chemical compound [O-]C(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-M 0.000 description 1
- 229960002510 mandelic acid Drugs 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000000877 morphologic effect Effects 0.000 description 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N n-hexanoic acid Natural products CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 230000009057 passive transport Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 238000005086 pumping Methods 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 238000004441 surface measurement Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- ZSDSQXJSNMTJDA-UHFFFAOYSA-N trifluralin Chemical compound CCCN(CCC)C1=C([N+]([O-])=O)C=C(C(F)(F)F)C=C1[N+]([O-])=O ZSDSQXJSNMTJDA-UHFFFAOYSA-N 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
Classifications
-
- 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
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE2003138402 DE10338402A1 (de) | 2003-08-18 | 2003-08-18 | Sprühgetrocknetes, amorphes BIBN 4096, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum |
| DE10338402.2 | 2003-08-18 | ||
| PCT/EP2004/009012 WO2005018603A2 (de) | 2003-08-18 | 2004-08-12 | Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen herstellung sowie dessen verwendung als inhalativum |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007502789A true JP2007502789A (ja) | 2007-02-15 |
| JP2007502789A6 JP2007502789A6 (ja) | 2007-05-10 |
| JP2007502789A5 JP2007502789A5 (https=) | 2007-09-27 |
Family
ID=34201781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006523576A Pending JP2007502789A (ja) | 2003-08-18 | 2004-08-12 | 噴霧乾燥された無定形ｂｉｂｎ４０９６、その調製方法及び吸入剤としてのその使用 |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1663149A2 (https=) |
| JP (1) | JP2007502789A (https=) |
| CA (1) | CA2536047A1 (https=) |
| DE (1) | DE10338402A1 (https=) |
| WO (1) | WO2005018603A2 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007502790A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む微粒子、その調製方法及び吸入粉末としてのその使用 |
| JP2012530064A (ja) * | 2009-06-12 | 2012-11-29 | マンカインド コーポレ−ション | 規定された比表面積を有するジケトピペラジン微粒子 |
| JP2018193401A (ja) * | 2013-06-19 | 2018-12-06 | アイキュリス アンチ−インフェクティブ キュアズ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 非晶質レテルモビル及び経口投与のためのその固形医薬製剤 |
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| US9006175B2 (en) | 1999-06-29 | 2015-04-14 | Mannkind Corporation | Potentiation of glucose elimination |
| US6923175B2 (en) | 2002-03-20 | 2005-08-02 | Mannkind Corporation | Inhalation apparatus |
| DE10338407A1 (de) * | 2003-08-18 | 2005-03-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Inhalationspulver enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin |
| ATE486064T1 (de) | 2004-08-20 | 2010-11-15 | Mannkind Corp | Katalyse der diketopiperazinsynthese |
| KR20130066695A (ko) | 2004-08-23 | 2013-06-20 | 맨카인드 코포레이션 | 약물 전달용 디케토피페라진염, 디케토모르포린염 또는 디케토디옥산염 |
| MX373000B (es) | 2005-09-14 | 2020-05-21 | Mannkind Corp | Metodo para formulacion de farmaco basado en el aumento de la afinidad de agentes activos hacia las superficies de microparticulas cristalinas. |
| EP1986679B1 (en) | 2006-02-22 | 2017-10-25 | MannKind Corporation | A method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent |
| CN101827626B (zh) | 2008-06-13 | 2015-03-18 | 曼金德公司 | 干粉吸入器和用于药物输送的系统 |
| US8485180B2 (en) | 2008-06-13 | 2013-07-16 | Mannkind Corporation | Dry powder drug delivery system |
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| TWI532497B (zh) | 2008-08-11 | 2016-05-11 | 曼凱公司 | 超快起作用胰島素之用途 |
| US8314106B2 (en) | 2008-12-29 | 2012-11-20 | Mannkind Corporation | Substituted diketopiperazine analogs for use as drug delivery agents |
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| CA2778698A1 (en) | 2009-11-03 | 2011-05-12 | Mannkind Corporation | An apparatus and method for simulating inhalation efforts |
| CN102985125A (zh) | 2010-06-21 | 2013-03-20 | 曼金德公司 | 干粉药物输送系统和方法 |
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Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5643448B1 (https=) * | 1967-08-08 | 1981-10-13 | ||
| WO2001056581A1 (en) * | 2000-02-04 | 2001-08-09 | Kissei Pharmaceutical Co., Ltd. | Powdered preparation for inhalation and powder inhalant containing the same packed |
| WO2001095885A1 (en) * | 2000-06-16 | 2001-12-20 | Glaxo Group Limited | Dry-powder pharmaceutical formulation for inhalation comprising alpha4-intergrin antagonist |
| WO2003015787A1 (en) * | 2001-08-17 | 2003-02-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Use of bibn4096 in combination with other antimigraine drugs for the treatment of migraine |
| JP2007502792A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−［ｎ２−［３，５−ジブロモ−ｎ−［［４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル］カルボニル］−ｄ−チロシル］−ｌ−リシル］−４−（４−ピリジニル）−ピペラジンを含有する粉末製剤、その吸入粉末としての製造方法及び使用 |
| JP2007502790A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む微粒子、その調製方法及び吸入粉末としてのその使用 |
| JP2007502791A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む新規吸入粉末製剤 |
| JP4085064B2 (ja) * | 2002-02-19 | 2008-04-30 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６の塩を含有する吸入粉末の調製方法 |
| JP4085063B2 (ja) * | 2002-02-20 | 2008-04-30 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６を含有する吸入粉末及びその調製方法 |
-
2003
- 2003-08-18 DE DE2003138402 patent/DE10338402A1/de not_active Withdrawn
-
2004
- 2004-08-12 WO PCT/EP2004/009012 patent/WO2005018603A2/de not_active Ceased
- 2004-08-12 EP EP04764016A patent/EP1663149A2/de not_active Withdrawn
- 2004-08-12 CA CA002536047A patent/CA2536047A1/en not_active Abandoned
- 2004-08-12 JP JP2006523576A patent/JP2007502789A/ja active Pending
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| JPS5643448B1 (https=) * | 1967-08-08 | 1981-10-13 | ||
| WO2001056581A1 (en) * | 2000-02-04 | 2001-08-09 | Kissei Pharmaceutical Co., Ltd. | Powdered preparation for inhalation and powder inhalant containing the same packed |
| WO2001095885A1 (en) * | 2000-06-16 | 2001-12-20 | Glaxo Group Limited | Dry-powder pharmaceutical formulation for inhalation comprising alpha4-intergrin antagonist |
| WO2003015787A1 (en) * | 2001-08-17 | 2003-02-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Use of bibn4096 in combination with other antimigraine drugs for the treatment of migraine |
| JP4085064B2 (ja) * | 2002-02-19 | 2008-04-30 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６の塩を含有する吸入粉末の調製方法 |
| JP4085063B2 (ja) * | 2002-02-20 | 2008-04-30 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６を含有する吸入粉末及びその調製方法 |
| JP2007502792A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−［ｎ２−［３，５−ジブロモ−ｎ−［［４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル］カルボニル］−ｄ−チロシル］−ｌ−リシル］−４−（４−ピリジニル）−ピペラジンを含有する粉末製剤、その吸入粉末としての製造方法及び使用 |
| JP2007502790A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む微粒子、その調製方法及び吸入粉末としてのその使用 |
| JP2007502791A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む新規吸入粉末製剤 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007502790A (ja) * | 2003-08-18 | 2007-02-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む微粒子、その調製方法及び吸入粉末としてのその使用 |
| JP2012530064A (ja) * | 2009-06-12 | 2012-11-29 | マンカインド コーポレ−ション | 規定された比表面積を有するジケトピペラジン微粒子 |
| JP2016028067A (ja) * | 2009-06-12 | 2016-02-25 | マンカインド コーポレイション | 規定された比表面積を有するジケトピペラジン微粒子 |
| JP2018193401A (ja) * | 2013-06-19 | 2018-12-06 | アイキュリス アンチ−インフェクティブ キュアズ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 非晶質レテルモビル及び経口投与のためのその固形医薬製剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1663149A2 (de) | 2006-06-07 |
| WO2005018603A3 (de) | 2005-07-21 |
| CA2536047A1 (en) | 2005-03-03 |
| DE10338402A1 (de) | 2005-03-17 |
| WO2005018603A2 (de) | 2005-03-03 |
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