BRPI0511462A - medicamentos e pró-medicamentos óculo-seletivos - Google Patents

medicamentos e pró-medicamentos óculo-seletivos

Info

Publication number
BRPI0511462A
BRPI0511462A BRPI0511462-4A BRPI0511462A BRPI0511462A BR PI0511462 A BRPI0511462 A BR PI0511462A BR PI0511462 A BRPI0511462 A BR PI0511462A BR PI0511462 A BRPI0511462 A BR PI0511462A
Authority
BR
Brazil
Prior art keywords
alkyl
straight
cycloalkyl
branched
alkoxyalkyl
Prior art date
Application number
BRPI0511462-4A
Other languages
English (en)
Inventor
William L Matier
Ghanshyam Patil
Original Assignee
Othera 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 Othera Pharmaceuticals Inc filed Critical Othera Pharmaceuticals Inc
Publication of BRPI0511462A publication Critical patent/BRPI0511462A/pt

Links

Classifications

    • 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
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C219/14—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/08—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

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

Abstract

MEDICAMENTOS E PRó-MEDICAMENTOS óCULO-SELETIVOS São apresentados compostos da seguinte fórmula, em que R¬ 1¬ E R¬ 2¬ são, cada um independentemente, H,W OU um grupo protetor de fenoxila, e R¬ 4¬ é H ou W, contanto que pelo menos um de R¬ 1¬, R¬ 2¬ e R¬ 4¬ seja W, R¬ 3¬ é hidrogênio, C~ 1~ - C~ 10~ alquila de cadeira linear ou ramificada, cicloalquila, amino, C~ 1~ - C~ 10~ alcóxi, - NHC(=O) R¬ a¬ ou -C (=O) N (H)R¬ a¬; R¬ a¬ é alquila, arila ou heterociclila, Z é -O-, -O(C=O) - ou -NH(C=O) -, em que, quando Z é -O-, R¬ 5¬ é C~ 1~ - C~ 10~ alquila de cadeira linear ou ramificada, cicloalquila, cicloalquila substituída com pelo menos uma C~ 1~ - C~ 10~ alcoxialquila, amino, benzila, tetraidrofuranila, diidrofuranila, furanila, morfolinila, piperidinila, tetraidropiranila, dioxolanila, 2,2- dimetil dioxolanila, dioxanila, pirrolila, pirrolila, pirrolidinila, tetraidrooxazolila, diidrooxazolila, fenila, fenila substituída com C~ 1~ - C~ 10~ alquila, C~ 1~ - C~ 10~ alcóxi ou halo, e W é: , em que casa R¬ 6¬ é independentemente H, C~ 1~ - C~ 10~ alquila de cadeia linear ou ramificada, ou C~ 1~ - C~ 10~ alcoxialquila de cadeia linear ou ramificada, e R¬ 7¬ é alquila, cicloalquila, arila ou aralquila, e em que, quando Z é - O (C=O)-, R¬ 5¬ é C~ 1~ - C~ 10~ alquila de cadeia linear ou ramificada, cicloalquila, cicloalquila substituída com pelo menos um C~ 1~ - C~ 10~ alquila linear ou ramificada, C~ 1~ - C~ 10~ alcoxialquila, amino, benzila, tetraidrofuranila, diidrofuranila, furanila, morfolinila, piperidinila, tetraidropiranila, dioxolanila, 2,2- dimetil dioxolanila, dioxanila, pirrolila, pirrolila, pirrolidinila, tetraidrooxazolila, diidrooxazolila, tenha, fenila substituída com C~ 1~ - C~ 10~ alquila, C~ 1~ - C~ 10~ alcóxi ou halo; e W é: , em que cada R¬ 6¬ é independentemente H, C~ 1~ - C~ 10~ alquila de cadeia linear ou ramificada, ou C~ 1~ - C~ 10~ alcoxialquila de cadeia linear ou ramificada; e R¬ 7¬ é alquila, cicloalquíla, arila ou aralquila; e em que, quando Z é - NH(C=O)-, R¬ 5¬ é C~ 1~ - C~ 10~ alquila de cadeia linear ou ramificada, cicloalquila, cicloalquila substituída com pelo menos uma C~ 1~ - C~ 10~ alquila linear ou ramificada, C~ 1~ - C~ 10~ alcoxialquila, amino, benzila, tetraidrofuranila, diidrofuranila, furanila, morfolinila, piperidinila, tetraidropiranila, dioxolanila, 2,2-ditnetil dioxolanila, dioxanila, pirrolila, pirrolidinila, tetraidrooxazolila, diidrooxazolila, fenila, fenila substituída com C~ 1~ - C~ 10~ alquila, C~ 1~ - C~~ 10~ alcóxi ou halo; e W é: , em que cada R¬ 6¬ é independentemente H, C~ 1~ - C~ 10~ alquila de cadeia linear ou ramificada, ou C~ 1~ - C~ 10~ alcoxialquila de cadeia linear ou ramificada. Também se apresentam métodos de preparação dos compostos, composições farmacêuticas compreendendo os compostos e métodos de tratamento de pacientes pela administração das composições farmacêuticas.
BRPI0511462-4A 2004-05-25 2005-05-24 medicamentos e pró-medicamentos óculo-seletivos BRPI0511462A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US57415704P 2004-05-25 2004-05-25
PCT/US2005/018350 WO2005115375A1 (en) 2004-05-25 2005-05-24 Oculoselective drugs and prodrugs

Publications (1)

Publication Number Publication Date
BRPI0511462A true BRPI0511462A (pt) 2007-12-26

Family

ID=35450641

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0511462-4A BRPI0511462A (pt) 2004-05-25 2005-05-24 medicamentos e pró-medicamentos óculo-seletivos

Country Status (13)

Country Link
US (3) US20070254950A1 (pt)
EP (1) EP1750693A4 (pt)
JP (1) JP2008500359A (pt)
KR (1) KR20070026654A (pt)
CN (1) CN1964711A (pt)
AU (1) AU2005247480A1 (pt)
BR (1) BRPI0511462A (pt)
CA (1) CA2565321A1 (pt)
EA (1) EA012668B1 (pt)
IL (1) IL179336A0 (pt)
NZ (1) NZ551379A (pt)
WO (1) WO2005115375A1 (pt)
ZA (1) ZA200610032B (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
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EA012668B1 (ru) * 2004-05-25 2009-12-30 Отера Холдинг, Инк. Окулоселективные лекарственные средства и пролекарства
JP5198827B2 (ja) * 2007-10-23 2013-05-15 株式会社日本ハイポックス 神経変性疾患治療薬
US8952011B2 (en) 2008-08-01 2015-02-10 Eye Therapies Llc Compositions and methods for the treatment of nasal conditions
US12246013B2 (en) 2008-08-01 2025-03-11 Eye Therapies Llc Vasoconstriction compositions and methods of use
HRP20141047T1 (hr) 2008-08-01 2015-01-02 Eye Therapies Llc Pripravci za sužavanje krvnih žila i metode njihove uporabe
US20100203165A1 (en) 2008-08-01 2010-08-12 Gerald Horn Compositions and methods for treatment of disorders or conditions of the eye
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Also Published As

Publication number Publication date
NZ551379A (en) 2010-11-26
US7678829B2 (en) 2010-03-16
CA2565321A1 (en) 2005-12-08
ZA200610032B (en) 2008-11-26
EA012668B1 (ru) 2009-12-30
US20060019955A1 (en) 2006-01-26
IL179336A0 (en) 2007-03-08
EP1750693A4 (en) 2010-06-02
US20070254950A1 (en) 2007-11-01
EA200602174A1 (ru) 2007-04-27
AU2005247480A1 (en) 2005-12-08
EP1750693A1 (en) 2007-02-14
JP2008500359A (ja) 2008-01-10
KR20070026654A (ko) 2007-03-08
US20100179218A1 (en) 2010-07-15
CN1964711A (zh) 2007-05-16
WO2005115375A1 (en) 2005-12-08

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