WO2007090134A3 - Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma - Google Patents

Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma Download PDF

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Publication number
WO2007090134A3
WO2007090134A3 PCT/US2007/061331 US2007061331W WO2007090134A3 WO 2007090134 A3 WO2007090134 A3 WO 2007090134A3 US 2007061331 W US2007061331 W US 2007061331W WO 2007090134 A3 WO2007090134 A3 WO 2007090134A3
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WO
WIPO (PCT)
Prior art keywords
glaucoma
antagonists
prevention
treatment
vanilloid receptor
Prior art date
Application number
PCT/US2007/061331
Other languages
French (fr)
Other versions
WO2007090134A2 (en
Inventor
Martin B Wax
Iok-Hou Pang
Allan Shepard
Original Assignee
Alcon Mfg Ltd
Martin B Wax
Iok-Hou Pang
Allan Shepard
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 Alcon Mfg Ltd, Martin B Wax, Iok-Hou Pang, Allan Shepard filed Critical Alcon Mfg Ltd
Publication of WO2007090134A2 publication Critical patent/WO2007090134A2/en
Publication of WO2007090134A3 publication Critical patent/WO2007090134A3/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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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

Abstract

Compositions and methods for treating glaucoma and for treating or preventing retina damage resulting from glaucoma with vanilloid receptor-1 antagonist compounds are disclosed.
PCT/US2007/061331 2006-01-31 2007-01-31 Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma WO2007090134A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76374006P 2006-01-31 2006-01-31
US60/763,740 2006-01-31

Publications (2)

Publication Number Publication Date
WO2007090134A2 WO2007090134A2 (en) 2007-08-09
WO2007090134A3 true WO2007090134A3 (en) 2007-11-08

Family

ID=38320607

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/061331 WO2007090134A2 (en) 2006-01-31 2007-01-31 Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma

Country Status (4)

Country Link
AR (1) AR059244A1 (en)
TW (1) TW200738232A (en)
UY (1) UY30120A1 (en)
WO (1) WO2007090134A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2719515C (en) 2008-04-18 2013-11-05 Daewoong Pharmaceutical Co., Ltd. A novel benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and a use thereof
JP2010024219A (en) * 2008-06-18 2010-02-04 Santen Pharmaceut Co Ltd Therapeutic agent for optic nerve disorder
KR101293384B1 (en) 2010-10-13 2013-08-05 주식회사 대웅제약 Novel pyridyl benzoxazine derivatives, pharmaceutical composition comprising the same, and use thereof
AU2020222348B2 (en) 2019-02-15 2023-03-16 Bausch + Lomb Ireland Limited Methods for treating ocular surface pain
JP6994061B2 (en) 2019-02-15 2022-01-14 ノバルティス アーゲー Preparation of 4- (7-hydroxy-2-isopropyl-4-oxo-4H-quinazoline-3-yl) -benzonitrile

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005004866A1 (en) * 2003-06-12 2005-01-20 Euro-Celtique, S.A. Therapeutic agents useful for treating pain

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005004866A1 (en) * 2003-06-12 2005-01-20 Euro-Celtique, S.A. Therapeutic agents useful for treating pain

Non-Patent Citations (17)

* Cited by examiner, † Cited by third party
Title
APPENDINO GIOVANNI ET AL: "Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 312, no. 2, February 2005 (2005-02-01), pages 561 - 570, XP002445729, ISSN: 0022-3565 *
DOHERTY ELIZABETH M ET AL: "Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 1, 13 January 2005 (2005-01-13), pages 71 - 90, XP002445730, ISSN: 0022-2623 *
JETTER MICHELE C ET AL: "N-Isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 12, 21 June 2004 (2004-06-21), pages 3053 - 3056, XP002445727, ISSN: 0960-894X *
LEE JEEWOO ET AL: "Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N'-(4-(methylsulfonylamino)benzyl)thiou rea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 9, 3 May 2004 (2004-05-03), pages 2291 - 2297, XP002445723, ISSN: 0960-894X *
LEE JEEWOO ET AL: "N-(4-(Methylsulfonylamino)benzyl)thiourea analogues as vanilloid receptor antagonists: Analysis of structure-activity relationships for the 'C-Region'.", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 12, no. 2, 15 January 2004 (2004-01-15), pages 371 - 385, XP002445719, ISSN: 0968-0896 *
MCDONNELL MARK E ET AL: "7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 2, 19 January 2004 (2004-01-19), pages 531 - 534, XP002445720, ISSN: 0960-894X *
PARK HYEUNG-GEUN ET AL: "N-4-methansulfonamidobenzyl-n'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 7, 5 April 2004 (2004-04-05), pages 1693 - 1696, XP002445722, ISSN: 0960-894X *
PARK HYEUNG-GEUN ET AL: "N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: Investigation on the role of methanesulfonamido group in antagonistic activity.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 3, 9 February 2004 (2004-02-09), pages 787 - 791, XP002445721, ISSN: 0960-894X *
PARK HYEUNG-GEUN ET AL: "Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor.", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 13, no. 2, 20 January 2003 (2003-01-20), pages 197 - 200, XP002445716, ISSN: 0960-894X *
PARK HYEUNG-GEUN ET AL: "Synthesis of N,N',N''-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 13, no. 4, 24 February 2003 (2003-02-24), pages 601 - 604, XP002445717, ISSN: 0960-894X *
RAMI HARSHAD K ET AL: "Discovery of small molecule antagonists of TRPV1", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 14, 16 July 2004 (2004-07-16), pages 3631 - 3634, XP002445724, ISSN: 0960-894X *
RYU CHONG HYUN ET AL: "Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 7, 5 April 2004 (2004-04-05), pages 1751 - 1755, XP002445726, ISSN: 0960-894X *
SUN Q ET AL: "4-(2-pyridyl)pipereazine-1-carboxamides: potent Vanilloid Receptor 1 antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 13, 20 October 2003 (2003-10-20), pages 3611 - 3616, XP002307277, ISSN: 0960-894X *
SWANSON DEVIN M ET AL: "Identification and biological evaluation of 4-(3-trifluoromethylpyrid in-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)a mide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 6, March 2005 (2005-03-01), pages 1857 - 1872, XP002445733, ISSN: 0022-2623 *
TAFESSE LAYKEA ET AL: "Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 14, no. 22, 15 November 2004 (2004-11-15), pages 5513 - 5519, XP002445725, ISSN: 0960-894X *
TÓTH ATTILA ET AL: "Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.", MOLECULAR PHARMACOLOGY FEB 2004, vol. 65, no. 2, February 2004 (2004-02-01), pages 282 - 291, XP002445728, ISSN: 0026-895X *
XI NING ET AL: "Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 15, no. 23, December 2005 (2005-12-01), pages 5211 - 5217, XP002445734, ISSN: 0960-894X *

Also Published As

Publication number Publication date
WO2007090134A2 (en) 2007-08-09
AR059244A1 (en) 2008-03-19
UY30120A1 (en) 2007-05-31
TW200738232A (en) 2007-10-16

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