WO2005055926A3 - Amelioration of cataracts, macular degeneration and other ophthalmic diseases - Google Patents

Amelioration of cataracts, macular degeneration and other ophthalmic diseases Download PDF

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Publication number
WO2005055926A3
WO2005055926A3 PCT/US2004/039716 US2004039716W WO2005055926A3 WO 2005055926 A3 WO2005055926 A3 WO 2005055926A3 US 2004039716 W US2004039716 W US 2004039716W WO 2005055926 A3 WO2005055926 A3 WO 2005055926A3
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WO
WIPO (PCT)
Prior art keywords
alkyl
alkenyl
macular degeneration
taken together
cataracts
Prior art date
Application number
PCT/US2004/039716
Other languages
French (fr)
Other versions
WO2005055926A2 (en
Inventor
William L Matier
Ghanshyam Patil
Original Assignee
Othera Pharmaceuticals Inc
William L Matier
Ghanshyam Patil
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 Othera Pharmaceuticals Inc, William L Matier, Ghanshyam Patil filed Critical Othera Pharmaceuticals Inc
Priority to AU2004296738A priority Critical patent/AU2004296738A1/en
Priority to CA002546053A priority patent/CA2546053A1/en
Priority to EP04812275A priority patent/EP1689354A4/en
Priority to JP2006541459A priority patent/JP2007527417A/en
Publication of WO2005055926A2 publication Critical patent/WO2005055926A2/en
Priority to IL175498A priority patent/IL175498A0/en
Publication of WO2005055926A3 publication Critical patent/WO2005055926A3/en

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    • 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
    • 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
    • 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
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A61K38/063—Glutathione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61K9/0051—Ocular inserts, ocular implants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula where R1 and R2 are, independently, H or C1 to C3 alkyl ; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl ; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl ; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.
PCT/US2004/039716 2003-11-20 2004-11-22 Amelioration of cataracts, macular degeneration and other ophthalmic diseases WO2005055926A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU2004296738A AU2004296738A1 (en) 2003-11-20 2004-11-22 Amelioration of cataracts, macular degeneration and other ophthalmic diseases
CA002546053A CA2546053A1 (en) 2003-11-20 2004-11-22 Amelioration of cataracts, macular degeneration and other ophthalmic diseases
EP04812275A EP1689354A4 (en) 2003-11-20 2004-11-22 Amelioration of cataracts, macular degeneration and other ophthalmic diseases
JP2006541459A JP2007527417A (en) 2003-11-20 2004-11-22 Improvement of cataracts, macular degeneration and other eye diseases
IL175498A IL175498A0 (en) 2003-11-20 2006-05-09 Pharmaceutical compositions containing n-hydroxypiperidine derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US52380303P 2003-11-20 2003-11-20
US60/523,803 2003-11-20

Publications (2)

Publication Number Publication Date
WO2005055926A2 WO2005055926A2 (en) 2005-06-23
WO2005055926A3 true WO2005055926A3 (en) 2006-12-07

Family

ID=34676585

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/039716 WO2005055926A2 (en) 2003-11-20 2004-11-22 Amelioration of cataracts, macular degeneration and other ophthalmic diseases

Country Status (8)

Country Link
EP (1) EP1689354A4 (en)
JP (1) JP2007527417A (en)
KR (1) KR20070040326A (en)
CN (1) CN101102770A (en)
AU (1) AU2004296738A1 (en)
CA (1) CA2546053A1 (en)
IL (1) IL175498A0 (en)
WO (1) WO2005055926A2 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7589107B2 (en) 2003-05-19 2009-09-15 Othera Holding, Inc. Amelioration of vitrectomy-induced cataracts
US20080312283A1 (en) * 2005-05-26 2008-12-18 Othera Pharmaceuticals, Inc. Use of Hydroxylamine Derivates for Inhibiting Vitrectomy-Induced Cataracts
JP2009527565A (en) * 2006-02-22 2009-07-30 オセラ ホールディングス、インク． Hydroxylamines and derivatives that inhibit complement activation
US20080200405A1 (en) * 2007-02-16 2008-08-21 Ghanshyam Patil Drug Resistance Reversal In Neoplastic Disease
WO2008103613A2 (en) * 2007-02-22 2008-08-28 Othera Holding, Inc. Hydroxylamine compounds and methods of their use
CA2707158A1 (en) * 2007-11-28 2009-06-04 Revision Therapeutics, Inc. Modulators of ocular oxidative stress
EP2080513A1 (en) * 2008-01-16 2009-07-22 Schraermeyer, Ulrich, Prof. Dr. rer. nat Tetrahydropyridoethers for treatment of AMD
CN102988331B (en) * 2012-05-31 2015-02-04 管孝君 Use of 2-mercapto-3-butanol in preparation of anti-lenticular opacity products
JP6302091B2 (en) * 2014-04-30 2018-03-28 ザ・ジョンズ・ホプキンス・ユニバーシティー Dendrimer composition and use thereof in the treatment of eye diseases
JP6342575B2 (en) 2014-08-13 2018-06-13 ザ・ジョンズ・ホプキンス・ユニバーシティー Selective dendrimer delivery to brain tumors
TW201625264A (en) * 2014-10-31 2016-07-16 學校法人慶應義塾 Inhibitor for lens hardness
WO2018201007A2 (en) 2017-04-27 2018-11-01 The Johns Hopkins University Dendrimer compositions for use in angiography
WO2018201124A1 (en) * 2017-04-28 2018-11-01 Case Western Reserve University Antioxidants for use in ophthalmic surgery
CN111615528A (en) 2017-11-10 2020-09-01 约翰霍普金斯大学 Dendrimer delivery systems and methods of use thereof
AU2020396561A1 (en) 2019-12-04 2022-07-14 Ashvattha Therapeutics, Inc. Dendrimer compositions and methods for drug delivery to the eye

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995017900A1 (en) * 1993-12-30 1995-07-06 Arcturus Pharmaceutical Corporation Methods for the treatment of the central nervous system or eye involving pathogenic oxidation pathways
US5981548A (en) * 1994-11-15 1999-11-09 Moreno Paolini N-Hydroxypiperidines as superoxide radicals scavengers
WO2002034262A1 (en) * 2000-10-25 2002-05-02 Giuliani S.P.A. Combination of catechin and quercetin for pharmaceutical or dietary use
US20030109566A1 (en) * 2000-06-29 2003-06-12 Tomiya Mano Remedial agent for optic nerve disease and the like

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5352442A (en) * 1985-07-18 1994-10-04 Proctor Peter H Topical tempo
ATE110954T1 (en) * 1988-01-29 1994-09-15 Peter H Proctor HAIR GROWTH STIMULATION WITH NITROXIDE AND OTHER RADICALS.
WO1997026879A1 (en) * 1996-01-26 1997-07-31 The United States Of America, Represented By The Secretary, Department Of Health And Human Services, The National Institutes Of Health Hydroxylamine compositions for the prevention or retardation of cataracts
KR20060013632A (en) * 2002-05-17 2006-02-13 오쎄라 파마슈티걸즈, 인크. Amelioration of the development of cataracts and other opthalmic diseases

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995017900A1 (en) * 1993-12-30 1995-07-06 Arcturus Pharmaceutical Corporation Methods for the treatment of the central nervous system or eye involving pathogenic oxidation pathways
US5981548A (en) * 1994-11-15 1999-11-09 Moreno Paolini N-Hydroxypiperidines as superoxide radicals scavengers
US20030109566A1 (en) * 2000-06-29 2003-06-12 Tomiya Mano Remedial agent for optic nerve disease and the like
WO2002034262A1 (en) * 2000-10-25 2002-05-02 Giuliani S.P.A. Combination of catechin and quercetin for pharmaceutical or dietary use

Also Published As

Publication number Publication date
IL175498A0 (en) 2008-04-13
KR20070040326A (en) 2007-04-16
EP1689354A4 (en) 2010-07-14
CA2546053A1 (en) 2005-06-23
AU2004296738A1 (en) 2005-06-23
WO2005055926A2 (en) 2005-06-23
EP1689354A2 (en) 2006-08-16
JP2007527417A (en) 2007-09-27
CN101102770A (en) 2008-01-09

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