AR078929A1 - Composicion que comprende un ester de un prostanoide y un acido carboxilico. metodo para conferir estabilidad acuosa a la anterior y su uso para preparar un medicamento util para tratar un trastorno ocular - Google Patents

Composicion que comprende un ester de un prostanoide y un acido carboxilico. metodo para conferir estabilidad acuosa a la anterior y su uso para preparar un medicamento util para tratar un trastorno ocular

Info

Publication number
AR078929A1
AR078929A1 ARP100104122A ARP100104122A AR078929A1 AR 078929 A1 AR078929 A1 AR 078929A1 AR P100104122 A ARP100104122 A AR P100104122A AR P100104122 A ARP100104122 A AR P100104122A AR 078929 A1 AR078929 A1 AR 078929A1
Authority
AR
Argentina
Prior art keywords
composition
prostanoid
ester
alkyl
treat
Prior art date
Application number
ARP100104122A
Other languages
English (en)
Original Assignee
Allergan Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43503864&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR078929(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Allergan Inc filed Critical Allergan Inc
Publication of AR078929A1 publication Critical patent/AR078929A1/es

Links

Classifications

    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/559—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing hetero atoms other than oxygen
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Una composicion que comprende un éster de un prostanoide, un ácido carboxílico, fosfato de sodio dibásico, cloruro de sodio, un agente solubilizante, y un resto de agua, donde el pH de la composicion se ajusta de aproximadamente 4 a aproximadamente 8. El agonista de prostanoide posee la formula (1) donde: cada uno de Z1 a Z6 es independientemente C, N, O, o S; A es -(CH2)6-, o cis -CH2CH=CH- (CH2)3-, donde 1 o 2 carbonos pueden estar sustituidos con S o O; o A es -(CH2)m-Ar-(CH2)o-, donde Ar es arileno o heteroarileno, la suma de m y o es de 1 a 4, y donde un CH2 puede estar sustituido con S u O; R1 es alquilo, cicloalquilo, oxialquilo, hidroxialquilo, alquenilo, oxialquenilo, o hidroxialquenilo; R2 es alquilo, alquenilo, hidroxilo, haluro, ciano, u oxo; J es alquilo, cicloalquilo, oxialquilo, hidroxialquilo; E es alquilo C1-12, R3, o -Y-R, donde Y es CH2, S, o O, y R3, es arilo o heteroarilo; n es 0 o 1; y donde una línea de guiones representa la presencia o ausencia de un enlace. Un método para conferir estabilidad acuosa a una formulacion que comprende un éster de un agonista de prostanoide, que comprende agregar un ácido carboxílico a la formulacion y, por lo tanto, ajustar el pH de 4 a aproximadamente 8. Uso de la composicion para preparar un medicamento para tratar un trastorno ocular, donde el trastorno es glaucoma o presion intraocular elevada. Reivindicacion 3: La composicion de la reivindicacion 1, caracterizada porque el ácido carboxílico es ácido cítrico. Reivindicacion 12: La composicion de la reivindicacion 9, caracterizada porque R1 es isopropilo o -CH2-CH2-OH. Reivindicacion 13: La composicion de la reivindicacion 9, caracterizada porque el profármaco del agonista de prostanoide posee la formula (2). Reivindicacion 20: La composicion de la reivindicacion 1, caracterizada porque el agente solubilizante es polisorbato 80 o pluronico F127. Reivindicacion 27: El uso de la reivindicacion 25, caracterizado porque el trastorno es glaucoma o presion intraocular elevada.
ARP100104122A 2009-12-09 2010-11-05 Composicion que comprende un ester de un prostanoide y un acido carboxilico. metodo para conferir estabilidad acuosa a la anterior y su uso para preparar un medicamento util para tratar un trastorno ocular AR078929A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26789709P 2009-12-09 2009-12-09

Publications (1)

Publication Number Publication Date
AR078929A1 true AR078929A1 (es) 2011-12-14

Family

ID=43503864

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104122A AR078929A1 (es) 2009-12-09 2010-11-05 Composicion que comprende un ester de un prostanoide y un acido carboxilico. metodo para conferir estabilidad acuosa a la anterior y su uso para preparar un medicamento util para tratar un trastorno ocular

Country Status (16)

Country Link
US (2) US20110136872A1 (es)
EP (1) EP2509582A1 (es)
JP (2) JP5955774B2 (es)
KR (1) KR20120106788A (es)
CN (1) CN102762195B (es)
AR (1) AR078929A1 (es)
AU (1) AU2010328555B2 (es)
CA (1) CA2783707A1 (es)
CL (1) CL2012001545A1 (es)
IL (1) IL220240A0 (es)
MX (1) MX2012006622A (es)
NZ (1) NZ600577A (es)
RU (1) RU2012127869A (es)
SG (1) SG181600A1 (es)
TW (1) TW201138766A (es)
WO (1) WO2011071620A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014035827A1 (en) 2012-08-27 2014-03-06 Allergan, Inc. Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
KR101535825B1 (ko) 2012-09-25 2015-07-10 엘지디스플레이 주식회사 표시장치 및 이의 라인결함 검출방법
TR201902864T4 (tr) * 2014-02-20 2019-03-21 Allergan Inc Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanımı ile azaltılmış merkezi korneal kalınlaşma.
CN111978310A (zh) 2014-10-02 2020-11-24 阿勒根公司 γ-内酰胺的酯前药及其用途

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4994274A (en) * 1989-07-27 1991-02-19 Allergan, Inc. Intraocular pressure reducing 11,15-diacyl prostaglandins and method of using
US5028624A (en) * 1989-07-27 1991-07-02 Allergan, Inc. Intraocular pressure reducing 9,15-diacyl prostaglandins
US5034413A (en) 1989-07-27 1991-07-23 Allergan, Inc. Intraocular pressure reducing 9,11-diacyl prostaglandins
CA2021316C (en) * 1989-07-27 2000-10-24 Ming Fai Chan Intraocular pressure reducing 11-acyl prostaglandins
JP2002521332A (ja) * 1998-07-21 2002-07-16 メルク エンド カムパニー インコーポレーテッド 高眼圧治療用眼薬組成物
ES2357551T3 (es) * 2000-09-13 2011-04-27 Santen Pharmaceutical Co., Ltd. Colirio.
ES2294361T3 (es) * 2002-08-23 2008-04-01 Santen Pharmaceutical Co., Ltd. Colirios estables que contienen latanoprost como principio activo.
PL1759702T3 (pl) * 2004-05-26 2009-06-30 Bayardo Arturo Jimenez Sposób wytwarzania roztworu latanoprostu do oczu oraz roztwór otrzymany tym sposobem
US20050276867A1 (en) * 2004-06-09 2005-12-15 Allergan, Inc. Stabilized compositions comprising a therapeutically active agent and an oxidizing preservative
EP1856042B1 (en) * 2005-03-10 2012-06-27 Allergan, Inc. Substituted gamma lactams as therapeutic agents
JPWO2008096804A1 (ja) * 2007-02-07 2010-05-27 テイカ製薬株式会社 ラタノプロスト含有点眼剤
MX2010011636A (es) * 2008-04-24 2010-11-25 Allergan Inc Gamma lactamas sustituidas como agentes terapeuticos.
EP2127638A1 (en) * 2008-05-30 2009-12-02 Santen Pharmaceutical Co., Ltd Method and composition for treating ocular hypertension and glaucoma

Also Published As

Publication number Publication date
EP2509582A1 (en) 2012-10-17
RU2012127869A (ru) 2014-01-20
AU2010328555A1 (en) 2012-07-05
NZ600577A (en) 2014-10-31
CN102762195A (zh) 2012-10-31
TW201138766A (en) 2011-11-16
AU2010328555B2 (en) 2016-05-26
MX2012006622A (es) 2012-08-15
SG181600A1 (en) 2012-07-30
KR20120106788A (ko) 2012-09-26
JP5955774B2 (ja) 2016-07-20
CA2783707A1 (en) 2011-06-16
US20160220677A1 (en) 2016-08-04
CL2012001545A1 (es) 2012-08-31
JP2016056207A (ja) 2016-04-21
JP2013513606A (ja) 2013-04-22
WO2011071620A1 (en) 2011-06-16
IL220240A0 (en) 2012-07-31
US20110136872A1 (en) 2011-06-09
CN102762195B (zh) 2016-05-18

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