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AR059574A1 - Formulaciones farmaceuticas acuosas de ligandos selectivos er-beta - Google Patents

Formulaciones farmaceuticas acuosas de ligandos selectivos er-beta

Info

Publication number
AR059574A1
AR059574A1 ARP070100594A ARP070100594A AR059574A1 AR 059574 A1 AR059574 A1 AR 059574A1 AR P070100594 A ARP070100594 A AR P070100594A AR P070100594 A ARP070100594 A AR P070100594A AR 059574 A1 AR059574 A1 AR 059574A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
hydroxyl
alkenyl
trifluoralkoxy
Prior art date
Application number
ARP070100594A
Other languages
English (en)
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of AR059574A1 publication Critical patent/AR059574A1/es

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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente provee además preparaciones de las formulaciones y usos de éstos. Reivindicacion 1: Una composicion farmacéutica acuosa que comprende: a) un ligando selectivo de ERbeta en una cantidad de desde aproximadamente 0,14 microg/mL hasta aproximadamente 40 mg/mL; b) un componente solubilizante/complejante que comprende desde aproximadamente 0,00021% (p/v) hasta aproximadamente 60% (p/v) de la composicion farmacéutica; y c) un componente opcional de ajusto de pH en una concentracion de desde 8,75 x 10-7 N hasta aproximadamente 1,0 N; donde el ligando selectivo de ERbeta tiene la Formula (1), en la cual: R1 es hidrogeno, hidroxilo, halogeno, alquilo C1-6, trifluoralquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, trifluoralcoxi C1-6, tioalquilo C1-6, sulfoxoalquilo C1-6, sulfonoalquilo C1-6, arilo C6-10, un anillo heterocíclico de 5 o 6-miembros que tiene de 1 a 4 heteroátomos seleccionados de O, N o S, -NO2, -NR5R6, -N(R5)COR6, -CN, -CHFCN, -CF2CN, alquinilo C2-7 o alquenilo C2- 7; donde los restos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R2 y R2a son cada una, independientemente, hidrogeno, hidroxilo, halogeno, alquilo C1-6, alcoxi C1-4, alquenilo C2-7, o alquinilo C2-7, trifluoralquilo C1-6, o trifluoralcoxi C1-6; donde los restos alquilo o alquenilo están sustituidos opcionalmente con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, - COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R3, R3a y R4 son cada una, independientemente, hidrogeno, alquilo C1-6, alquenilo C2-7, alquinilo C2-7, halogeno, alcoxi C1-4, trifluoralquilo C1-6, o trifluoralcoxi C1-6; donde las porciones alquilo o alquenilo están sustituidas con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R5 y R6 son cada una, independientemente, hidrogeno, alquilo C1-6 o arilo C6-10; X es O, S o NR7; y R7 es hidrogeno, alquilo C1-6, arilo C6-10, -COR5, -CO2R5 o -SO2R5; o una sal farmacéuticamente aceptable de éstos; o la Formula (2), en la cual: R11, R12, R13 y R14 son cada una, seleccionados independientemente entre, hidrogeno, hidroxilo, alquilo C1-6, alcoxi C1-6 o halogeno; R15, R16, R17, R18, R19 y R20 son cada una, independientemente, hidrogeno, alquilo C1-6, alquenilo C2-7, alquinilo C2-7, halogeno, alcoxi C1-6, -CN, -CHO, fenilo, o un anillo de 5 o 6-miembros que tiene de 1 a 4 heteroátomos seleccionados entre O, N o S; donde los restos alquilo o alquenilo de R15, R16, R17, R18, R19 o R20 pueden estar sustituidos opcionalmente con hidroxilo, CN, halogeno, trifluoralquilo, trifluoralcoxi, NO2 o fenilo; donde el resto fenilo de R15, R16, R17, R18, R19 o R20 puede estar opcionalmente mono-, di o tri-sustituido con alquilo C1-6, alquenilo C2-7, halogeno, hidroxilo, alcoxi C1-6, CN, -NO2, amino, alquilamino C1-6, dialquilamino C1-6 por grupo alquilo, tio, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alcoxicarbonilo C2-7, alquilcarbonilo C2-7 o benzoílo; y donde por lo menos uno de R11, R12, R13, R14, R17, R18, R19 o R20 es hidroxilo; o una sal farmacéuticamente aceptable de éste.
ARP070100594A 2006-02-14 2007-02-13 Formulaciones farmaceuticas acuosas de ligandos selectivos er-beta AR059574A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US77302806P 2006-02-14 2006-02-14

Publications (1)

Publication Number Publication Date
AR059574A1 true AR059574A1 (es) 2008-04-16

Family

ID=38225453

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100594A AR059574A1 (es) 2006-02-14 2007-02-13 Formulaciones farmaceuticas acuosas de ligandos selectivos er-beta

Country Status (10)

Country Link
US (1) US20070191442A1 (es)
EP (1) EP1984028A2 (es)
JP (1) JP2009526851A (es)
AR (1) AR059574A1 (es)
AU (1) AU2007215131A1 (es)
BR (1) BRPI0707655A2 (es)
CA (1) CA2641116A1 (es)
PE (1) PE20071043A1 (es)
TW (1) TW200800177A (es)
WO (1) WO2007095286A2 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070208069A1 (en) * 2006-03-06 2007-09-06 Wyeth Pharmaceutical formulations of an anhydrous crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
WO2007103877A2 (en) * 2006-03-06 2007-09-13 Wyeth Pharmaceutical formulations of a monohydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
AR059741A1 (es) * 2006-03-06 2008-04-23 Wyeth Corp Formulaciones farmaceuticas liquidas y semisolidas y procedimientos
US20090239920A1 (en) * 2006-11-21 2009-09-24 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080175900A1 (en) * 2006-11-21 2008-07-24 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080175901A1 (en) * 2006-11-21 2008-07-24 Wyeth Pharmaceutical formulations of a crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
US20080241234A1 (en) * 2006-11-21 2008-10-02 Wyeth Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
JP2010516819A (ja) * 2007-01-31 2010-05-20 ワイス エルエルシー 急性肺損傷を治療するためのＥＲβ選択的リガンドの使用
DE102007015169A1 (de) * 2007-03-27 2008-10-02 Universität des Saarlandes Campus Saarbrücken 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020198174A1 (en) * 2001-05-07 2002-12-26 Allergan Sales, Inc. Disinfecting and solubilizing steroid compositions
EP1317270A1 (en) * 2000-09-08 2003-06-11 Pharmacia Italia S.p.A. Exemestane for the treatment of oestrogen-dependent cancers
FR2817750B1 (fr) * 2000-12-11 2003-02-21 Sanofi Synthelabo Composition pharmaceutique de dronedarone pour administration parenterale
UA83620C2 (ru) * 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
US6960607B2 (en) * 2001-12-13 2005-11-01 Wyeth Naphthyl benzoxazoles and benzisoxazoles as estrogenic agents
US6903238B2 (en) * 2001-12-13 2005-06-07 Wyeth Substituted indenones as estrogenic agents
US6884814B2 (en) * 2001-12-13 2005-04-26 Wyeth Phenyl benzisoxazoles as estrogenic agents
US6914074B2 (en) * 2001-12-13 2005-07-05 Wyeth Substituted phenyl naphthalenes as estrogenic agents
TW200301107A (en) * 2001-12-13 2003-07-01 Wyeth Corp Substituted 6H-dibenzo[c,h]chromenes as estrogenic agents
US6774248B2 (en) * 2001-12-18 2004-08-10 Wyeth Substituted 2-phenyl benzofurans as estrogenic agents
US6835745B2 (en) * 2002-01-15 2004-12-28 Wyeth Phenyl substituted thiophenes as estrogenic agents
TW200500065A (en) * 2003-05-21 2005-01-01 Wyeth Corp Antiarthritic combinations
EP1761513A1 (en) * 2004-07-01 2007-03-14 Wyeth Tetracyclic compounds as estrogen ligands
AU2005282554A1 (en) * 2004-09-07 2006-03-16 Wyeth 6H-[1]benzopyrano[4,3-b]quinolines and their use as estrogenic agents
KR20070089921A (ko) * 2004-12-02 2007-09-04 와이어쓰 치환된 벤족사졸의 제형
WO2006060384A2 (en) * 2004-12-02 2006-06-08 Wyeth Formulations of substituted benzoxazoles
WO2006065968A2 (en) * 2004-12-17 2006-06-22 Wyeth The uses of estrogen beta agonists to treat cognitive diseases
BRPI0608154A2 (pt) * 2005-02-16 2016-10-11 Wyeth Corp métodos de tratar ou inibir mucosite, cistite por radiação em um indivíduo, e de tratar pelo menos um sintoma de exposição de um indivíduo a um agente citotóxico ou à radiação, e, composição farmacêutica

Also Published As

Publication number Publication date
US20070191442A1 (en) 2007-08-16
BRPI0707655A2 (pt) 2011-05-10
JP2009526851A (ja) 2009-07-23
WO2007095286A3 (en) 2007-12-13
TW200800177A (en) 2008-01-01
PE20071043A1 (es) 2007-10-23
AU2007215131A1 (en) 2007-08-23
WO2007095286A2 (en) 2007-08-23
CA2641116A1 (en) 2007-08-23
EP1984028A2 (en) 2008-10-29

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