JP2004504360A - 1−(5−tert−ブチル−2−P−トリル−2H−ピラゾール−3−イル)−3−[4−(2−モルホリン−4−イル−エトキシ)−ナフタレン−1−イル]−ウレアの改良された経口製剤 - Google Patents

1−(5−tert−ブチル−2−P−トリル−2H−ピラゾール−3−イル)−3−[4−(2−モルホリン−4−イル−エトキシ)−ナフタレン−1−イル]−ウレアの改良された経口製剤 Download PDF

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JP2004504360A
JP2004504360A JP2002513505A JP2002513505A JP2004504360A JP 2004504360 A JP2004504360 A JP 2004504360A JP 2002513505 A JP2002513505 A JP 2002513505A JP 2002513505 A JP2002513505 A JP 2002513505A JP 2004504360 A JP2004504360 A JP 2004504360A
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Prior art keywords
morpholin
tolyl
ethoxy
tert
butyl
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Pending
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JP2002513505A
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Japanese (ja)
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JP2004504360A5 (enExample
Inventor
カポラ マイケル エル
ジェレグ ジョージ ダブリュー
ウェイ スーザン
Original Assignee
ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド
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Publication of JP2004504360A publication Critical patent/JP2004504360A/ja
Publication of JP2004504360A5 publication Critical patent/JP2004504360A5/ja
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    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nanotechnology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medical Informatics (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2002513505A 2000-07-24 2001-07-11 1−(5−tert−ブチル−2−P−トリル−2H−ピラゾール−3−イル)−3−[4−(2−モルホリン−4−イル−エトキシ)−ナフタレン−1−イル]−ウレアの改良された経口製剤 Pending JP2004504360A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22038700P 2000-07-24 2000-07-24
PCT/US2001/021860 WO2002007772A2 (en) 2000-07-24 2001-07-11 Improved oral dosage formulations

Publications (2)

Publication Number Publication Date
JP2004504360A true JP2004504360A (ja) 2004-02-12
JP2004504360A5 JP2004504360A5 (enExample) 2008-08-28

Family

ID=22823354

Family Applications (1)

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JP2002513505A Pending JP2004504360A (ja) 2000-07-24 2001-07-11 1−(5−tert−ブチル−2−P−トリル−2H−ピラゾール−3−イル)−3−[4−(2−モルホリン−4−イル−エトキシ)−ナフタレン−1−イル]−ウレアの改良された経口製剤

Country Status (6)

Country Link
US (1) US6565880B2 (enExample)
EP (1) EP1305050A2 (enExample)
JP (1) JP2004504360A (enExample)
CA (1) CA2415131A1 (enExample)
MX (1) MXPA02012909A (enExample)
WO (1) WO2002007772A2 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005527615A (ja) * 2002-05-29 2005-09-15 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 ナトリウムチャンネルブロッカーの非経口適用のための新規な製剤

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US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
US6548503B1 (en) 1998-11-04 2003-04-15 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP2298311B1 (en) 1999-01-13 2012-05-09 Bayer HealthCare LLC w-Carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ES2230171T3 (es) 1999-11-23 2005-05-01 Smithkline Beecham Corporation Compuestos 3,4-dihidro-(1h)quinazolin-2-ona como inhibidores de csbp/p38 quinasa.
JP2003514900A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション CSBP/p38キナーゼ阻害剤としての3,4−ジヒドロ−(1H)−キナゾリン−2−オン化合物
DE60023025T2 (de) 1999-11-23 2006-07-13 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
EP1709965A3 (en) 2001-07-11 2006-12-27 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating cytokine mediate diseases
CA2454913A1 (en) * 2001-08-20 2003-02-27 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2h-pryrazol-3-yl)-3-¬4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl|-urea and a cyclodextrin
AU2002366644A1 (en) * 2001-12-11 2003-06-23 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering birb 796 bs
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
US20040110755A1 (en) * 2002-08-13 2004-06-10 Boehringer Ingelheim Pharmaceuticals, Inc. Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
EP1539121A4 (en) 2002-08-29 2008-08-13 Scios Inc METHOD OF REQUESTING OSTEOGENESIS
EP1636585B2 (en) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl ureas with kinase inhibiting activity
CN100584385C (zh) * 2003-07-10 2010-01-27 协和发酵生化株式会社 片剂及其制备方法
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
US7244441B2 (en) 2003-09-25 2007-07-17 Scios, Inc. Stents and intra-luminal prostheses containing map kinase inhibitors
CA2547837A1 (en) * 2003-12-18 2005-07-14 Boehringer Ingelheim Pharmaceuticals, Inc. Polymorph of birb 796, a p38map kinase inhibitor
JP4251298B2 (ja) 2005-07-15 2009-04-08 ソニー株式会社 再生装置および再生方法、プログラム、プログラム格納媒体、データ、記録媒体、記録装置、および、記録媒体の製造方法
CN101026725B (zh) * 2005-07-15 2010-09-29 索尼株式会社 再现设备及再现方法
NZ575394A (en) 2006-10-20 2012-01-12 Icos Corp Compositions of chk1 inhibitors and cyclodextrin
WO2008079629A2 (en) * 2006-12-21 2008-07-03 Boehringer Ingelheim International Gmbh Formulations with improved bioavailability
EP3257862A1 (en) 2016-06-16 2017-12-20 ETH Zürich Fibronectin-binding peptides for use in tumor or fibrosis diagnosis and therapy
ES2927715T3 (es) 2017-10-05 2022-11-10 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 reducen la expresión de dux4 y de los genes que le siguen para el tratamiento de la FSHD

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5464633A (en) * 1994-05-24 1995-11-07 Jagotec Ag Pharmaceutical tablets releasing the active substance after a definite period of time

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA73492C2 (en) * 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
CA2374737C (en) 1999-07-09 2008-02-12 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
US6254888B1 (en) * 2000-01-28 2001-07-03 Boehringer Ingelheim Pharmaceuticals, Inc. Method for coating pharmaceutical dosage forms

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5464633A (en) * 1994-05-24 1995-11-07 Jagotec Ag Pharmaceutical tablets releasing the active substance after a definite period of time

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005527615A (ja) * 2002-05-29 2005-09-15 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 ナトリウムチャンネルブロッカーの非経口適用のための新規な製剤

Also Published As

Publication number Publication date
WO2002007772A3 (en) 2002-10-17
WO2002007772A2 (en) 2002-01-31
US20020031544A1 (en) 2002-03-14
EP1305050A2 (en) 2003-05-02
CA2415131A1 (en) 2002-01-31
MXPA02012909A (es) 2004-05-05
US6565880B2 (en) 2003-05-20

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