BR112013001015A2 - método por tratar doenças oftálmicas que usam compostos de inibidor de cinase em formas de prodrug - Google Patents

método por tratar doenças oftálmicas que usam compostos de inibidor de cinase em formas de prodrug

Info

Publication number
BR112013001015A2
BR112013001015A2 BR112013001015A BR112013001015A BR112013001015A2 BR 112013001015 A2 BR112013001015 A2 BR 112013001015A2 BR 112013001015 A BR112013001015 A BR 112013001015A BR 112013001015 A BR112013001015 A BR 112013001015A BR 112013001015 A2 BR112013001015 A2 BR 112013001015A2
Authority
BR
Brazil
Prior art keywords
prodrugs
rock
compounds
ophthalmic diseases
treating ophthalmic
Prior art date
Application number
BR112013001015A
Other languages
English (en)
Inventor
John W Lampe
Paul S Watson
Sammy R Shaver
Original Assignee
Inspire Pharmaceuticals 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
Application filed by Inspire Pharmaceuticals Inc filed Critical Inspire Pharmaceuticals Inc
Publication of BR112013001015A2 publication Critical patent/BR112013001015A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

método por tratar doenças oftalmicas que usam compostos de inibidor de cinase em formas de prodrug. esta invenção é dirigida a profármaco de inibidores de rho cinase (rock). este profármacos são em geral os derivados de éster ou amida dos compostos origem. este profármacos são frequentemente inibidores fracos de rock, porém seus compostos origem têm atividades boas. em instilação nos olhos, o grupo éster ou amida destes profármacos são rapidamente hidrolizados em álcoo, amina, ou ácido, e os profármacos são convertidos nos compostos de base ativos. os profármacos de inibidores de rock fornecem várias vantagens tais como liberação de concentrações mais altas das espécies ativas no sítio alvo e redução de desconforto ocular. a invenção é da mesma forma dirigida a um método de tratar doenças oftálmicas tal glaucoma, conjuntivite alérgica, edema macular, degeneração macular, e blefarite, administrando-se uma quantidade eficaz de um composto de profármaco de rock de fórmula i aos olhos do paciente em necessidade disso.
BR112013001015A 2010-07-27 2011-07-25 método por tratar doenças oftálmicas que usam compostos de inibidor de cinase em formas de prodrug BR112013001015A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36818310P 2010-07-27 2010-07-27
PCT/US2011/045244 WO2012015760A1 (en) 2010-07-27 2011-07-25 Method for treating ophthalmic diseases using kinase inhibitor compounds in prodrug forms

Publications (1)

Publication Number Publication Date
BR112013001015A2 true BR112013001015A2 (pt) 2016-05-24

Family

ID=45530465

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013001015A BR112013001015A2 (pt) 2010-07-27 2011-07-25 método por tratar doenças oftálmicas que usam compostos de inibidor de cinase em formas de prodrug

Country Status (11)

Country Link
US (1) US20130131059A1 (pt)
EP (1) EP2597953A4 (pt)
JP (1) JP2013532689A (pt)
KR (1) KR20130095263A (pt)
CN (1) CN103249305A (pt)
AU (1) AU2011282887A1 (pt)
BR (1) BR112013001015A2 (pt)
CA (1) CA2803689A1 (pt)
MX (1) MX2013001003A (pt)
RU (1) RU2013108641A (pt)
WO (1) WO2012015760A1 (pt)

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GB201107223D0 (en) * 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
CA2857344C (en) 2011-12-21 2019-02-12 Novira Therapeutics, Inc. Hepatitis b antiviral agents
JP6505013B2 (ja) 2012-08-28 2019-04-24 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー スルファモイル−アリールアミド及びｂ型肝炎の治療のための薬剤としてのその使用
JP6205425B2 (ja) * 2012-10-31 2017-09-27 ピーエイチ ファーマ シーオー．，エルティディ． 新規のｒｏｃｋ阻害剤
EP2961405A4 (en) * 2012-12-14 2017-03-29 The Brigham and Women's Hospital, Inc. Methods and assays relating to macrophage differentiation
AU2014222641B2 (en) 2013-02-28 2018-03-15 Janssen Sciences Ireland Uc Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of Hepatitis B
JP6419155B2 (ja) 2013-04-03 2018-11-07 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｎ−フェニル−カルボキサミド誘導体およびｂ型肝炎を治療するための医薬品としてのその使用
CN105050600B (zh) * 2013-04-24 2018-09-28 国立大学法人九州大学 眼底疾病治疗剂
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
US10160743B2 (en) 2013-05-17 2018-12-25 Janssen Sciences Ireland Uc Sulphamoylthiophenamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
LT3024819T (lt) 2013-07-25 2018-06-11 Janssen Sciences Ireland Uc Pirolamido dariniai, turintys glioksamido pakaitų, ir jų panaudojimas kaip vaistų hepatito b gydymui
WO2015041533A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
WO2015059212A1 (en) 2013-10-23 2015-04-30 Janssen R&D Ireland Carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
MX2016009449A (es) 2014-02-05 2016-10-13 Novira Therapeutics Inc Terapia de combinacion para el tratamiento de infecciones por virus de la hepatitis b (vhb).
EP3102572B1 (en) 2014-02-06 2018-10-24 Janssen Sciences Ireland UC Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
JP2018510159A (ja) 2015-03-19 2018-04-12 ノヴィラ・セラピューティクス・インコーポレイテッド アゾカン及びアゾナン誘導体及びｂ型肝炎感染症の治療法
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
AU2016330964B2 (en) 2015-09-29 2021-04-01 Novira Therapeutics, Inc. Crystalline forms of a hepatitis B antiviral agent
AU2017248828A1 (en) 2016-04-15 2018-11-01 Janssen Sciences Ireland Uc Combinations and methods comprising a capsid assembly inhibitor
US10696638B2 (en) 2017-12-26 2020-06-30 Industrial Technology Research Institute Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same
US10973801B2 (en) 2018-03-14 2021-04-13 Janssen Sciences Ireland Unlimited Company Capsid assembly modulator dosing regimen
CA3110661A1 (en) 2018-08-29 2020-03-05 University Of Massachusetts Inhibition of protein kinases to treat friedreich ataxia
CN113454077A (zh) 2019-02-22 2021-09-28 爱尔兰詹森科学公司 用于治疗hbv感染或hbv诱发的疾病的酰胺衍生物
MX2021013594A (es) 2019-05-06 2021-12-10 Janssen Sciences Ireland Unlimited Co Derivados de amida utiles en el tratamiento de la infeccion por vhb o de enfermedades inducidas por vhb.
AU2021259332A1 (en) 2020-04-22 2022-10-27 Atriva Therapeutics Gmbh ROCK inhibitors for use in treating or preventing pulmonary edema

Family Cites Families (7)

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EP1459742B9 (en) * 1998-08-17 2012-05-02 Senju Pharmaceutical Co., Ltd. Agent for prophylaxis and treatment of asthenopia and pseudomyopia
US7217722B2 (en) * 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
EP1866316A2 (en) * 2005-03-25 2007-12-19 Inspire Pharmaceuticals, Inc. Cytoskeletal active compounds, composition and use
US8071779B2 (en) * 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
EP2291077A4 (en) * 2008-06-18 2011-05-25 Inspire Pharmaceuticals Inc METHOD OF MANUFACTURING RHO-KINASE INHIBITOR COMPOUNDS
EP2299820A4 (en) * 2008-06-18 2012-11-14 Inspire Pharmaceuticals Inc OPHTHALMOLOGICAL FORMULATION OF RHO KINASE INHIBITOR COMPOUND
US20090325959A1 (en) * 2008-06-26 2009-12-31 Vittitow Jason L Method for treating ophthalmic diseases using rho kinase inhibitor compounds

Also Published As

Publication number Publication date
EP2597953A1 (en) 2013-06-05
EP2597953A4 (en) 2013-12-25
KR20130095263A (ko) 2013-08-27
RU2013108641A (ru) 2014-09-10
CA2803689A1 (en) 2012-02-02
AU2011282887A1 (en) 2013-02-07
WO2012015760A1 (en) 2012-02-02
JP2013532689A (ja) 2013-08-19
US20130131059A1 (en) 2013-05-23
CN103249305A (zh) 2013-08-14
MX2013001003A (es) 2013-03-07

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Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]