AR036339A1 - MEDICINAL FORMULATION CONTAINING AN LTB4 ANTAGONIST - Google Patents

MEDICINAL FORMULATION CONTAINING AN LTB4 ANTAGONIST

Info

Publication number
AR036339A1
AR036339A1 ARP020102604A ARP020102604A AR036339A1 AR 036339 A1 AR036339 A1 AR 036339A1 AR P020102604 A ARP020102604 A AR P020102604A AR P020102604 A ARP020102604 A AR P020102604A AR 036339 A1 AR036339 A1 AR 036339A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
phenyl
alkoxy
formula
Prior art date
Legal status (The legal status 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 status listed.)
Suspension/Interruption
Application number
ARP020102604A
Other languages
Spanish (es)
Inventor
Robert Becker
Bock Thomas Dr
Siglinde Moll
Rene Roscher
Ulrich Roth
Achim Sauer
Karl Weber
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
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 GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR036339A1 publication Critical patent/AR036339A1/en
Suspension/Interruption legal-status Critical Current

Links

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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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

Abstract

Una formulación de medicamento en forma de una tableta que contiene un antagonista de LTB4 de fórmula (1), en donde: A significa un grupo de la fórmula -O-CmH2m-O-(PHE)n- en donde m es un número entero de 2 a 6, n es 0 ó 1, PHE representa un grupo 1,4-fenileno eventualmente sustituido con uno o dos grupos alquilo C1-6; o A significa un grupo de fórmula (2); R1 significa H, OH, CN, COOR10 o CHO; R2 significa H, Br, Cl, F, CF3, CHF2, OH, HSO3-O-, alquilo C1-6, alcoxi C1-6, cicloalquilo C5-7, CONR8R9, arilo, O-arilo, CH2-arilo, CR5R6-arilo o C(CH3)2-R7; R3 significa H, alquilo C1-6, alcoxi C1-6, OH, Cl o F; R4 significa H o alquilo C1-6; R5 significa alquilo C1-4, CF3, CH2OH, COOH o COO(alquilo C1-4); R6 significa H, alquilo C1-4 o CF3; R7 significa CH2OH, COOH, COO(alquilo C1-4), CONR8R9 o CH2NR8R9; R8 significa H, alquilo C1-6, fenilo, fenil-(alquilo C1-6), COR10, COOR10, CHO, CONH2, CONHR10, SO2-(alquilo C1-6), SO2-fenilo, pudiendo estar sustituido una o dos veces el grupo fenilo con Cl, F, CF3, alquilo C1-4, OH y/o alcoxi C1-4; R9 significa H o alquilo C1-6; o R8 y R9 tomados juntos, significan un grupo alquileno C4-6; R10 significa alquilo C1-6, cicloalquilo C5-7, arilo, heteroarilo, aralquilo o heteroaril-(alquilo C1-6); representando los grupos arilo de los radicales R2 y R10 fenilo o naftilo, representando los grupos heteroarilo, pirrol, pirazol, imidazol, furanilo, tienilo, piridina o pirimidina, y pudiendo estar sustituidos en cada caso, una o varias veces, con Cl, F, CF3, alquilo C1-4, OH, HSO3-O- o alcoxi C1-4, así como sus sales por adición de ácidos farmacológicamente aceptables y glucósidos y o-sulfatos; y al menos un coadyuvante farmacológicamente aceptable, caracterizada porque la tableta contiene al menos un agente humectante. Esta formulación farmacéutica, aplicable por vía oral, libera el principio activo de fórmula (1) con relativa rapidez y por completo y, por lo tanto, conduce a una elevada biodisponibilidad de este principio activo. Además, está caracterizada por una buena manipulabilidad durante el proceso de fabricación y permite con ello la preparación técnica de modo reproducible y con calidad invariablemente elevada. Procedimiento para la preparación de las tabletas descriptas más arriba, así como su uso para la preparación de un medicamento destinado al tratamiento o la prevención de la artritis, el asma, las afecciones pulmonares obstructivas crónicas, la psoriasis, la colitis ulcerosa, la enfermedad de Alzheimer, el choque (schock), las lesiones por reperfusión/isquemia, la fibrosis quística, la arterioesclerosis y la esclerosis múltiple.A medicament formulation in the form of a tablet containing an LTB4 antagonist of formula (1), wherein: A means a group of the formula -O-CmH2m-O- (PHE) n- where m is an integer from 2 to 6, n is 0 or 1, PHE represents a 1,4-phenylene group optionally substituted with one or two C1-6 alkyl groups; or A means a group of formula (2); R1 means H, OH, CN, COOR10 or CHO; R2 means H, Br, Cl, F, CF3, CHF2, OH, HSO3-O-, C1-6 alkyl, C1-6 alkoxy, C5-7 cycloalkyl, CONR8R9, aryl, O-aryl, CH2-aryl, CR5R6- aryl or C (CH3) 2-R7; R3 means H, C1-6 alkyl, C1-6 alkoxy, OH, Cl or F; R4 means H or C1-6 alkyl; R5 means C1-4 alkyl, CF3, CH2OH, COOH or COO (C1-4 alkyl); R6 means H, C1-4 alkyl or CF3; R7 means CH2OH, COOH, COO (C1-4 alkyl), CONR8R9 or CH2NR8R9; R8 means H, C1-6 alkyl, phenyl, phenyl- (C1-6 alkyl), COR10, COOR10, CHO, CONH2, CONHR10, SO2- (C1-6 alkyl), SO2-phenyl, and may be substituted once or twice the phenyl group with Cl, F, CF3, C1-4 alkyl, OH and / or C1-4 alkoxy; R9 means H or C1-6 alkyl; or R8 and R9 taken together, mean a C4-6 alkylene group; R10 means C1-6 alkyl, C5-7 cycloalkyl, aryl, heteroaryl, aralkyl or heteroaryl- (C1-6 alkyl); representing the aryl groups of the radicals R2 and R10 phenyl or naphthyl, representing the heteroaryl, pyrrole, pyrazol, imidazole, furanyl, thienyl, pyridine or pyrimidine groups, and may be substituted in each case, once or several times, with Cl, F , CF3, C1-4 alkyl, OH, HSO3-O- or C1-4 alkoxy, as well as their salts by the addition of pharmacologically acceptable acids and glycosides and o-sulfates; and at least one pharmacologically acceptable adjuvant, characterized in that the tablet contains at least one wetting agent. This pharmaceutical formulation, applicable orally, releases the active ingredient of formula (1) relatively quickly and completely and, therefore, leads to a high bioavailability of this active ingredient. In addition, it is characterized by good handling during the manufacturing process and thus allows technical preparation in a reproducible way and with invariably high quality. Procedure for the preparation of the tablets described above, as well as their use for the preparation of a drug intended for the treatment or prevention of arthritis, asthma, chronic obstructive pulmonary conditions, psoriasis, ulcerative colitis, disease of Alzheimer's, shock (schock), reperfusion / ischemia lesions, cystic fibrosis, atherosclerosis and multiple sclerosis.

ARP020102604A 2001-07-14 2002-07-12 MEDICINAL FORMULATION CONTAINING AN LTB4 ANTAGONIST Suspension/Interruption AR036339A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10134377 2001-07-14
DE10206241A DE10206241A1 (en) 2001-07-14 2002-02-15 Drug formulation containing an LTB antagonist

Publications (1)

Publication Number Publication Date
AR036339A1 true AR036339A1 (en) 2004-09-01

Family

ID=7691857

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020102604A Suspension/Interruption AR036339A1 (en) 2001-07-14 2002-07-12 MEDICINAL FORMULATION CONTAINING AN LTB4 ANTAGONIST

Country Status (6)

Country Link
AR (1) AR036339A1 (en)
CO (1) CO5560535A2 (en)
DE (2) DE10206241A1 (en)
PE (1) PE20030255A1 (en)
SA (1) SA03230511A (en)
ZA (1) ZA200309710B (en)

Also Published As

Publication number Publication date
DE50203521D1 (en) 2005-08-04
CO5560535A2 (en) 2005-09-30
PE20030255A1 (en) 2003-04-22
SA03230511A (en) 2005-12-03
ZA200309710B (en) 2004-06-04
DE10206241A1 (en) 2003-01-30

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