Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T62841 Target Info
Target Name Proteinase activated receptor 2 (PAR2)
Synonyms Thrombin receptor-like 1; Proteinase-activated receptor-2; Proteinase-activated receptor 2; Protease activated receptor 2; PAR-2; GPR11; G-protein coupled receptor 11; Coagulation factor II receptor-like 1
Target Type Clinical trial Target
Gene Name F2RL1
Biochemical Class GPCR rhodopsin
UniProt ID
PAR2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015048245
Title Imidazopyridazines Useful As Inhibitors of The Par-2 Signaling Pathway.
Abstract The present invention relates to compounds useful as inhibitors of the PAR-2 signaling pathway. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of GPCRs in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such GPCRs; and the comparative evaluation of new inhibitors of the PAR-2 signaling pathway. The compounds of this invention have formula I: wherein the variables are as defined herein.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D02SJB Drug Info IC50 = 0.5 nM Click to Show More [1]
2 D0G7KY Drug Info IC50 = 0.7 nM [1]
3 D0UN9X Drug Info IC50 = 1.4 nM [1]
4 D0N3AF Drug Info IC50 = 2 nM [1]
5 D0W9AB Drug Info IC50 = 7.5 nM [1]
Patent ID WO2014020351
Title Receptor Antagonists.
Abstract N-(4-carbamimidoylphenyl)-amide derivatives having utility in therapy as PAR2 receptor antagonists.
Applicant(s) Proximagen Limited
Representative Drug(s) D07HJT Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0AK6L Drug Info IC50 < 1000 nM [1]
3 D0G2EP Drug Info IC50 = 1000 to 10000 nM [1]
4 D0JT0B Drug Info IC50 < 1000 nM [1]
5 D0VN2U Drug Info IC50 < 1000 nM [1]
6 D0WH1K Drug Info IC50 < 1000 nM [1]
Patent ID WO2014020350
Title Par2 Receptor Antagonists.
Abstract Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine.
Applicant(s) Proximagen Limited
Representative Drug(s) D07HJT Drug Info IC50 < 1000 nM Click to Show More [1]
2 D0AK6L Drug Info IC50 < 1000 nM [1]
3 D0G2EP Drug Info IC50 = 1000 to 10000 nM [1]
4 D0JT0B Drug Info IC50 < 1000 nM [1]
5 D0VN2U Drug Info IC50 < 1000 nM [1]
6 D0WH1K Drug Info IC50 < 1000 nM [1]
Patent ID WO2013013273
Title Modulators of Protease Activated Receptors.
Abstract The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for therapies such as metabolic syndrome, obesity, type II diabetes, fibrosis and cardiovascular diseases, whether they are used alone or in combination with other treatment modalities.
Applicant(s) The University of Queensland
Representative Drug(s) D09EIX Drug Info IC50 = 500 nM Click to Show More [1]
2 D0I2RS Drug Info IC50 = 700 nM [1]
Patent ID WO2012101453
Title Protease Activated Receptor 2 (Par2) Antagonists.
Abstract A compound of formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof (I) Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.
Applicant(s) Proximagen Ltd
Representative Drug(s) D04GIJ Drug Info IC50 < 5000 nM Click to Show More [1]
2 D04YKO Drug Info IC50 < 5000 nM [1]
3 D0H1JS Drug Info IC50 < 5000 nM [1]
4 D0S6SJ Drug Info IC50 < 5000 nM [1]
Patent ID WO2012026766
Title Novel Heterocyclic Compound, and Composition for Treating Inflammatory Diseases Using Same.
Abstract The present invention relates to a heterocyclic compound having the effects of treating and preventing inflammatory diseases and healing skin wounds, and particularly, having the effects of restoring.
Applicant(s) Neopharm Co., Ltd
Representative Drug(s) D05VXK Drug Info N.A. Click to Show More [1]
2 D0T6SP Drug Info N.A. [1]
3 D0Z4SW Drug Info N.A. [1]
Patent ID WO2012026765
Title Novel Heterocyclic Compound, and Composition for Treating Inflammatory Diseases Using Same.
Abstract The present invention relates to a heterocyclic compound having the effects of treating and preventing inflammatory diseases and healing skin wounds, and particularly, having the effects of restoring.
Applicant(s) Neopharm Co., Ltd
Representative Drug(s) D05VXK Drug Info N.A. Click to Show More [1]
2 D0T6SP Drug Info N.A. [1]
3 D0Z4SW Drug Info N.A. [1]
Patent ID WO2005030773
Title Novel Pyrazolopyrimidine Derivatives.
Abstract Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof have antipruritic activities and so on and are therefore useful as therapeutic or preventive drugs for allergic diseases, dermatoses and so on wherein R1 is hydroxy, carboxy, or the like; m is an integer of 1 to 3; R2 is alkyl, alkoxy, or the like; n is an integer of 0 to 4; A is a 5- to 8-membered, saturated or unsaturated nitrogenous heterocycle; R3 is haloalkyl or the like; R4 and R5 are each independently hydrogen, halogeno, alkyl, or the like; and X is methine, nitrogen, or the like.
Applicant(s) Dainippon Sumitomo Pharma co., Ltd
Representative Drug(s) D0UD6X Drug Info N.A. [1]
Patent ID WO2013064583
Title Peptides Which Inhibit Activated Receptors and Their Use In Cosmetic or Pharmaceutical Compositions.
Abstract The present invention refers to a peptide of general formula (I) R1-Wn-Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp-Zq-R2, cosmetic compositions which comprises said peptide, method of preparation of said peptides and its use in the treatment and/or prevention of itching, inflammation, pain, diseases and/or disorders of the respiratory airways.
Applicant(s) Lipotec, S.A
Patent ID WO2012139137
Title Pepducin Design and Use.
Abstract Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.
Applicant(s) Tufts Medical Center, Inc
Patent ID WO2012090207
Title Par1 and Par2 C-Tail Peptides and Peptide Mimetics.
Abstract The present invention concerns isolated PAR1 cytoplasmic tail (c-tail) peptides and isolated PAR2 cytoplasmic tail (c-tail) peptides, as well as compositions comprising these peptides, uses thereof and methods of treating various diseases, in particular cancer.
Applicant(s) Hadasit Medical Research Services & Amp; Development Limited
Patent ID WO2012011908
Title Compositions and Methods for Inhibiting Par2 Activation of Keratinocytes.
Abstract A composition for inhibiting PAR2 activation of keratinocytes is disclosed as comprising a vitamin B3 compound, an N-acyl amino acid compound, and a Laminaria Saccharina extract. In one embodiment, the composition for inhibiting PAR2 activation of keratinocytes comprises niacinamide, N-undecylenoyl-L-phenylalanine, and a Laminaria Saccharina extract. In response to the technical problems identified in the background, the present invention may take other forms including methods for inhibiting PAR2 activation of keratinocytes.
Applicant(s) The Procter & Amp; Gamble Company
Patent ID WO2010017086
Title Effectors of Par-2 Activation and Their Use In The Modulation of Inflammation.
Abstract The present invention relates to the recognition that PAR-2 receptors amplify the inflammatory response and that effectors of PAR-2 activation can thus be used to modulate the inflammatory response and thereby impart therapeutic benefit to patients. The invention is particularly directed to the use of PAR-2 effectors in the treatment of inflammation and nociception (pain) caused by inflammation, cancer and injury. The invention is particularly directed to negative effectors of PAR-2 activation, and more particularly to anti-PAR-2 antibodies that are negative effectors of PAR-2 activation.
Applicant(s) Boehringer Ingelheim International Gmbh
United States Patent and Trademark Office (USPTO)
Patent ID US20150038402
Title Modulators of Protease Activated Receptors.
Applicant(s) The University of Queensland
Representative Drug(s) D09EIX Drug Info IC50 = 500 nM Click to Show More [1]
2 D0I2RS Drug Info IC50 = 700 nM [1]
3 D0Y9UV Drug Info N.A. [1]
Patent ID US20120093824
Title High Affinity Human Antibodies To Human Protease-Activated Receptor-2.
Applicant(s) Regeneron Pharmaceuticals Inc
Patent ID US2008470556
Title Nucleic Acids That Encode Antigen Binding Proteins That Bind Par-2.
Applicant(s) Amgen Inc
Patent ID US2008357367
Title Antibodies That Bind Par-2.
Applicant(s) Amgen Inc
Patent ID US2008287872
Title Methods for Treating Inflammatory Conditions Using Antibodies That Bind Par-2.
Applicant(s) Amgen Inc
Patent ID US2007888482
Title Antibodies That Bind Par-2.
Applicant(s) Amgen Inc
Korean Intellectual Property Office (KIPO)
Patent ID KR2015044675
Title Preparation of Benzothiazine-Carboxamides or Related Compounds As Par2 Inhibitors.
Applicant(s) Amorepacific Corp
Representative Drug(s) D0H4SE Drug Info IC50 = 400 nM Click to Show More [1]
2 D0K9QH Drug Info IC50 = 400 to 1000 nM [1]
3 D0Q8MQ Drug Info IC50 = 800 nM [1]
4 D06XWQ Drug Info IC50 = 1000 nM [1]
5 D07OVM Drug Info IC50 = 1000 nM [1]
6 D0P7UB Drug Info IC50 = 1000 nM [1]
Patent ID KR20111130259
Title Quinazoline Derivative As Par-2 Inhibitor, and Method for The Preparation Thereof.
Applicant(s) Neopharm Co., Ltd
Representative Drug(s) D0P2BJ Drug Info IC50 = 8600 nM Click to Show More [1]
2 D0EC3H Drug Info IC50 = 15000 nM [1]
3 D08ZEM Drug Info IC50 = 17000 nM [1]
4 D0CM5P Drug Info IC50 = 34000 nM [1]
Patent ID KR2013034701
Title Par-2 Activating Peptide Derivative with Improved Biostability and Pharmaceutical Composition Containing It.
Applicant(s) Peptron Inc
Representative Drug(s) D07AXK Drug Info N.A. Click to Show More [1]
2 D0D2PU Drug Info N.A. [1]
Patent ID KR2010038919
Title Preparation of Piperazine Derivative As Par-2 (Protease-Activated Receptor 2) Inhibitor.
Applicant(s) Neopharm Co., Ltd
Representative Drug(s) D0LT5Y Drug Info N.A. [1]
Patent ID KR2011118210
Title Peptides with Par-2 Inhibitory Activities for Improving Skin Conditions.
Applicant(s) Enprani Co. Ltd
References  Top
REF 1 Protease activated receptor 2 (PAR2) modulators: a patent review (2010-2015).Expert Opin Ther Pat. 2016;26(4):471-83.

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