MXPA02012909A - Formulaciones mejoradas de dosis oral de 1-(5-ter-butil -2-p-tiolil2h -pirazol-3 -il)-3-(4-2 (2-morfolin-4-il -etoxi) -naftalen -1-il) -urea. - Google Patents

Formulaciones mejoradas de dosis oral de 1-(5-ter-butil -2-p-tiolil2h -pirazol-3 -il)-3-(4-2 (2-morfolin-4-il -etoxi) -naftalen -1-il) -urea.

Info

Publication number
MXPA02012909A
MXPA02012909A MXPA02012909A MXPA02012909A MXPA02012909A MX PA02012909 A MXPA02012909 A MX PA02012909A MX PA02012909 A MXPA02012909 A MX PA02012909A MX PA02012909 A MXPA02012909 A MX PA02012909A MX PA02012909 A MXPA02012909 A MX PA02012909A
Authority
MX
Mexico
Prior art keywords
naphthalen
morpholin
pyrazol
tolyl
ethoxy
Prior art date
Application number
MXPA02012909A
Other languages
English (en)
Inventor
Michael L Cappola
Original Assignee
Boehringer Ingelheim Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of MXPA02012909A publication Critical patent/MXPA02012909A/es

Links

Classifications

    • 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]

Abstract

Una formulacion que comprende, y un proceso para preparar, formar mejoradas de dosis oral de 1-(5-ter-butil -2-p-tolil -2H-pirazol-3 -il)-3-[4 -(2-morfolin-4 -il-etoxi)-naftalen-1-il ]-urea, una entidad quimica con propiedades anti-inflamatorias. La granulacion de 1-(5-ter-butil -2-p-tolil-2H -pirazol -3-il)-3-[4 -(2-morfolin-4 -il-etoxi)- naftalen -1-il]-urea dentro de intervalos especificados proporciona disolucion mejorada de 1-(5-ter-butil -2-p-tolil-2H-pirazo l-3-il)-3-[4-(2-morfolin -4il-etoxi)-naftalen -1-il]-urea y biodisponibilidad oral, asi como uniformidad de contenido. La incorporacion en la formulacion del compuesto acuoso, soluble de inclusion capaz de formar un complejo con 1-(5-ter-butil -2-p-tolil-2H-pirazol -3-il)-3-[4-(2 -morfolin- 4-il-etoxi) -naftalen-l-il] -urea, tal como beta-ciclodextrina proporciona estabilidad mejorada de 1-(5-ter-butil -2-p-tolil-2H -pirazo1-3-il) -3-[4-(2-morfolin -4-il-etoxi) -naftalen-l-il] -urea, en particular en ambientes altamente ionicos. Se puede prevenir el despostillado y desintegracion de las tabletas que contienen mas de aproximadamente 10 % de beta-ciclodextrina, al aplicar un recubrimiento polimerico a la superficie de la tableta a una temperatura por abajo de 40°C.4.
MXPA02012909A 2000-07-24 2001-07-11 Formulaciones mejoradas de dosis oral de 1-(5-ter-butil -2-p-tiolil2h -pirazol-3 -il)-3-(4-2 (2-morfolin-4-il -etoxi) -naftalen -1-il) -urea. MXPA02012909A (es)

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 (1)

Publication Number Publication Date
MXPA02012909A true MXPA02012909A (es) 2004-05-05

Family

ID=22823354

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA02012909A MXPA02012909A (es) 2000-07-24 2001-07-11 Formulaciones mejoradas de dosis oral de 1-(5-ter-butil -2-p-tiolil2h -pirazol-3 -il)-3-(4-2 (2-morfolin-4-il -etoxi) -naftalen -1-il) -urea.

Country Status (6)

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

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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
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
US20030118575A1 (en) * 2001-12-11 2003-06-26 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering BIRB 796 BS
MXPA04007832A (es) 2002-02-11 2005-09-08 Bayer Pharmaceuticals Corp Aril-ureas con actividad inhibitoria de angiogenesis.
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
DE10223783A1 (de) * 2002-05-29 2003-12-11 Boehringer Ingelheim Pharma Neue Formulierung zur parenteralen Applikation eines Na-Kanal-Blockers
US20040110755A1 (en) * 2002-08-13 2004-06-10 Boehringer Ingelheim Pharmaceuticals, Inc. Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
WO2004019873A2 (en) 2002-08-29 2004-03-11 Scios Inc. Methods of promoting osteogenesis
CA2526617C (en) 2003-05-20 2015-04-28 Bayer Pharmaceuticals Corporation Diaryl ureas with kinase inhibiting activity
WO2005004923A1 (ja) * 2003-07-10 2005-01-20 Kyowa Hakko Kogyo Co., Ltd. 錠剤およびその製造方法
UA84156C2 (ru) 2003-07-23 2008-09-25 Байер Фармасьютикалс Корпорейшн Фторозамещённая омега-карбоксиарилдифенилмочевина для лечения и профилактики болезней и состояний
WO2005030091A2 (en) 2003-09-25 2005-04-07 Scios Inc. Stents and intra-luminal prostheses containing map kinase inhibitors
JP2007514791A (ja) * 2003-12-18 2007-06-07 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 Ｐ３８ｍａｐキナーゼインヒビターであるｂｉｒｂ７９６の多形
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
KR20110098009A (ko) * 2006-10-20 2011-08-31 이코스 코포레이션 Ｃｈｋ1 억제제와 시클로덱스트린의 조성물
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
LT3691620T (lt) 2017-10-05 2022-09-26 Fulcrum Therapeutics, Inc. P38 kinazės inhibitoriai, sumažinantys dux4 ir pasrovinių genų raišką, skirti fshd gydymui
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

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* 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
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
ES2253233T3 (es) 1999-07-09 2006-06-01 Boehringer Ingelheim Pharmaceuticals Inc. Procedimiento para sintesis de compuestos de urea heteroaril sustituidos.
US6254888B1 (en) * 2000-01-28 2001-07-03 Boehringer Ingelheim Pharmaceuticals, Inc. Method for coating pharmaceutical dosage forms

Also Published As

Publication number Publication date
WO2002007772A3 (en) 2002-10-17
US20020031544A1 (en) 2002-03-14
JP2004504360A (ja) 2004-02-12
EP1305050A2 (en) 2003-05-02
WO2002007772A2 (en) 2002-01-31
US6565880B2 (en) 2003-05-20
CA2415131A1 (en) 2002-01-31

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