JP2019521189A - ドライアイ、眼痛および炎症の処置のためのｔｒｐａ１アンタゴニスト - Google Patents

ドライアイ、眼痛および炎症の処置のためのｔｒｐａ１アンタゴニスト Download PDF

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JP2019521189A
JP2019521189A JP2019520930A JP2019520930A JP2019521189A JP 2019521189 A JP2019521189 A JP 2019521189A JP 2019520930 A JP2019520930 A JP 2019520930A JP 2019520930 A JP2019520930 A JP 2019520930A JP 2019521189 A JP2019521189 A JP 2019521189A
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carbonyl
group
fluoro
pyrazole
trifluoromethyl
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JP2019521189A5 (enExample
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エム．， ハーツ，ジェフリー
エム．， ハーツ，ジェフリー
エー．， ケシッキ，エドワード
エー．， ケシッキ，エドワード
ピー．， ズータ，チャールズ
ピー．， ズータ，チャールズ
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アルゴメディックス，インク．
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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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
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    • 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
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    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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    • A61K9/0048—Eye, e.g. artificial tears
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    • 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
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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
JP2019520930A 2016-07-06 2017-07-06 ドライアイ、眼痛および炎症の処置のためのｔｒｐａ１アンタゴニスト Pending JP2019521189A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662359122P 2016-07-06 2016-07-06
US62/359,122 2016-07-06
PCT/US2017/040976 WO2018009717A1 (en) 2016-07-06 2017-07-06 Trpa1 antagonists for treatment of dry eye, ocular pain and inflammation

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JP2019521189A true JP2019521189A (ja) 2019-07-25
JP2019521189A5 JP2019521189A5 (enExample) 2020-08-20

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JP2019520930A Pending JP2019521189A (ja) 2016-07-06 2017-07-06 ドライアイ、眼痛および炎症の処置のためのｔｒｐａ１アンタゴニスト

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US (1) US20200179357A1 (enExample)
EP (1) EP3481808A4 (enExample)
JP (1) JP2019521189A (enExample)
CA (1) CA3029901A1 (enExample)
IL (1) IL264069A (enExample)
SG (1) SG11201811655SA (enExample)
WO (1) WO2018009717A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11963943B2 (en) 2019-05-03 2024-04-23 Zyus Life Sciences Inc. Formulation for pain management
US12178797B2 (en) 2019-05-03 2024-12-31 Zyus Life Sciences Inc. Formulation for pain management
US12220396B2 (en) 2019-05-03 2025-02-11 Zyus Life Sciences Inc. Formulation for pain management

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2936111C (en) 2014-01-06 2023-03-14 Algomedix, Inc. Trpa1 modulators
WO2020184479A1 (ja) * 2019-03-08 2020-09-17 ロート製薬株式会社 刺激感が抑制された眼科組成物
GR1010012B (el) * 2020-05-12 2021-05-27 Φαρματεν Α.Β.Ε.Ε. Φαρμακευτικο σκευασμα ελευθερο συντηρητικου για οφθαλμικη χορηγηση περιεχον κυκλοσπορινη
IT202100015098A1 (it) 2021-06-09 2022-12-09 Flonext S R L Composto antagonista del canale trpa1 per uso in patologie degenerative della retina
KR20240032924A (ko) * 2021-07-12 2024-03-12 오큐소프트, 인코포레이티드 피부 보습 조성물

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015103060A1 (en) * 2014-01-06 2015-07-09 Algomedix, Inc. Trpa1 modulators

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2331878A1 (en) * 1998-05-14 1999-11-18 G.D. Searle & Co. 1,5-diaryl substituted pyrazoles as p38 kinase inhibitors
EP1620095A4 (en) * 2003-04-24 2009-04-01 Merck & Co Inc HEMMER OF ACT ACTIVITY

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015103060A1 (en) * 2014-01-06 2015-07-09 Algomedix, Inc. Trpa1 modulators

Non-Patent Citations (1)

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Title
NEUROSCIENCE, 2015, VOL.290, PP.204-213, AUTHOR MANUSCRIPT, JPN6021024970, ISSN: 0004731488 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11963943B2 (en) 2019-05-03 2024-04-23 Zyus Life Sciences Inc. Formulation for pain management
US12178797B2 (en) 2019-05-03 2024-12-31 Zyus Life Sciences Inc. Formulation for pain management
US12220396B2 (en) 2019-05-03 2025-02-11 Zyus Life Sciences Inc. Formulation for pain management

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EP3481808A1 (en) 2019-05-15
CA3029901A1 (en) 2018-01-11
EP3481808A4 (en) 2020-07-15
US20200179357A1 (en) 2020-06-11
IL264069A (en) 2019-01-31
SG11201811655SA (en) 2019-01-30

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