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 T02562 Target Info
Target Name Prostaglandin E synthase (PTGES)
Synonyms p53-induced gene 12 protein; PIG12; PGES; PGE synthase; P53-induced apoptosis protein 12; Microsomal prostaglandin E synthase 1; Microsomal glutathione S-transferase 1-like 1; MPGES1; MPGES-1; MGST1L1; MGST1-L1
Target Type Clinical trial Target
Gene Name PTGES
Biochemical Class Intramolecular oxidoreductase
UniProt ID
PTGES_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013153535
Title Tricyclic Compounds As Mpges-1 Inhibitors.
Abstract The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as m PGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D0LY6S Drug Info IC50 < 50 nM Click to Show More [1]
2 D0S2UD Drug Info IC50 < 50 nM [1]
Patent ID WO2012076673
Title 6-Amino-2-Phenylamino-1H-Benzimidazole-5-Carboxamide- Derivatives and Their Use As Microsomal Prostaglandin E2 Synthase-1 Inhibitors.
Abstract This invention relates to compounds of formula (I) their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D07YPE Drug Info IC50 = 1 nM Click to Show More [1]
2 D0ZT9I Drug Info IC50 = 1 nM [1]
Patent ID WO2011048004
Title Inhibitors of The Microsomal Prostaglandin E2 Synthase-1.
Abstract This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7' Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0AH1A Drug Info IC50 = 1 nM Click to Show More [1]
2 D0FX6I Drug Info IC50 = 1 nM [1]
Patent ID WO2016069376
Title Novel Methyl-Piperidine Compounds Useful for Inhibiting Microsomal Prostaglandin E2 Synthase-1.
Abstract The present invention provides compounds of Formula (1), or a pharmaceutically acceptable salt thereof, formula (1), where R, R1, and G are as described herein; methods of preparing the compounds; and use of the compounds to treat pain and/or inflammation associated with arthritis or osteoarthritis.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0XM9M Drug Info IC50 = 1.93 nM [1]
Patent ID WO2015059618
Title Substituted Pyrimidine Compounds As Mpges-1 Inhibitors.
Abstract The present disclosure is directed to substituted pyrimidine compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D0WR0Q Drug Info IC50 < 50 nM [1]
Patent ID WO2014167444
Title Substituted Bicyclic Compounds As Mpges-1 Inhibitors.
Abstract The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D02DXA Drug Info IC50 < 50 nM [1]
Patent ID WO2013186692
Title Triazolone Compounds As Mpges-1 Inhibitors.
Abstract The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D0JH7Q Drug Info IC50 < 50 nM [1]
Patent ID WO2013072825
Title Phtalazinone Derivatives As Mpegs -1 Inhibitors.
Abstract The present patent application is directed to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D00XFM Drug Info IC50 < 50 nM [1]
Patent ID WO2012087771
Title Novel Imidazole-2-Benzamide Compounds Useful for The Treatment of Osteoarthritis.
Abstract The present invention provides compounds of the formula (I) below or pharmaceutical salts thereof, wherein R1, R2 and R3 are as described herein; methods of treating osteoarthritis using the compounds; and a process for preparing the compounds.
Applicant(s) Eli Lilly and Company
Patent ID WO2012022793
Title New Compounds.
Abstract This invention relates to compounds of formula (I) their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0N2DJ Drug Info IC50 = 1 nM [1]
Patent ID WO2011023812
Title Microsomal Prostaglandin E Synthase-1 (Mpges1) Inhibitors.
Abstract A compound of formula (I): as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from inflammatory diseases, nociceptive pain, auto-immune disease, breathing disorders, fever, cancer, inflammation related anorexia, Alzheimer's disease and cardiovascular diseases.
Applicant(s) Wannberg, Johan et al
Representative Drug(s) D0V4FE Drug Info IC50 = 11 nM [1]
Patent ID WO2010100249
Title 3H-Imidazo [4, 5 -C] Pyridine- 6 -Carboxamides As Anti- Inflammatory Agents.
Abstract The present invention relates to compounds of general formula (I) in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0HH5B Drug Info IC50 = 1 nM [1]
Patent ID WO2010034799
Title 3H-Imidaz0 [4, 5-B] Pyridine- 6 -Carboxamides As Anti -Inflammatory Agents.
Abstract There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0C3ZN Drug Info 100% inhibition = 1000 nM [1]
Patent ID WO2010034798
Title 3H-Imidazo [4, 5-C] Pyridine-6-Carboxamides As Anti -Inflammatory Agents.
Abstract There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0BR7G Drug Info 100% inhibition = 10000 nM [1]
Patent ID WO2010034796
Title 1H-Benz Imidazole-5-Carboxamides As Anti-Inflammatory Agents.
Abstract There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0KY1Y Drug Info 100% inhibition = 1000 nM [1]
Patent ID WO2009130242
Title Low Molecular Weight Derivatives and Use Thereof In Treatment of Prostaglandin E Synthase Related Diseases.
Abstract A compound of formula (I) for use as a medicament, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of a disorder selected from pain, fever, inflammation and cancer.
Applicant(s) Novasaid Ab
Representative Drug(s) D0I1GO Drug Info IC50 = 100 nM [1]
Patent ID WO2009103778
Title Compounds and Methods.
Abstract A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from pain, fever, inflammation and cancer.
Applicant(s) Wannberg, Johan et al
Representative Drug(s) D0YO3X Drug Info IC50 = 110 nM [1]
Patent ID WO2009064250
Title Bis-(Sulfonylamino) Derivatives In Therapy 065.
Abstract The invention provides compounds of formula wherein R1, R2 , R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
Applicant(s) Astrazeneca Ab
Representative Drug(s) D07WOT Drug Info IC50 = 3.2 nM [1]
Patent ID WO2016069374
Title Novel Carboxylic Acid Compounds Useful for Inhibiting Microsomal Prostaglandin E2 Synthase-1.
Abstract The present invention provides compounds of Formula 1, or a pharmaceutically acceptable salts, thereof, where R, X, A, E, and G are as described herein, methods of preparing the compounds, and use of the compounds to treat pain and/or inflammation.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D00PHK Drug Info N.A. [1]
Patent ID WO2012161965
Title Novel Imidazole Derivatives Useful for The Treatment of Arthritis.
Abstract The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0F8KE Drug Info N.A. [1]
Patent ID WO2012110860
Title Tricyclic Compounds As Mpges-1 Inhibitors.
Abstract The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase- 1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I).
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D0U9LS Drug Info N.A. [1]
Patent ID WO2012022792
Title 2-(Arylamino)-3H-Imidazo[4,5-B]Pyridine-6-Carboxamide Derivatives and Their Use As Mpges-1 Inhibitors.
Abstract This invention relates to compounds of formula (I) their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7 have meanings given in the description.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0UJ5D Drug Info N.A. [1]
Patent ID WO2010034797
Title 1H-Benzimidazole-5-Carboxamides As Anti-Inflammatory Agents.
Abstract There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0T1UU Drug Info N.A. [1]
Patent ID WO2009117987
Title Use of Boswellia Acids and Synthetic Boswellia Acid Derivatives for Inhibiting Microsomal Prostanglandin E2 Synthase and Cathepsin G.
Abstract The present invention relates to new boswellia acid derivatives. The present invention furthermore relates to the use of preparations with boswellia acid derivatives or synthetic derivatives, especially with boswellia acid derivatives, which are esterified or etherified at the C3-OH function, for inhibiting the induceable microsomal prostaglandin E2 synthase-1 and/or for inhibiting cathepsin G. Furthermore, the invention relates to the use of boswellia acids or synthetic derivatives for the preparation of a drug for the treatment of PGE2- and/or cathepsin G-induced pathological conditions.
Applicant(s) Univ Tuebingen
Patent ID WO2009117985
Title Pirinixic Acid Derivatives As Prostglandin E2 Synthesis Inhibitors for Treating Inflammatory Diseases.
Abstract The invention relates to pirinixic acid derivatives, especially alpha-substituted pirinixic acids and pirinixic acid esters, and the structural derivatives thereof with the following structural formula. The pirinixic acid derivatives inhibit the PGE2 synthesis, especially that of the mPGES-1. The invention also relates to the use of said pirinixic acid derivatives for producing a medicament for treating prostaglandin E2-mediated diseases, especially inflammatory diseases, painful and feverish conditions, cardiovascular events and cancerous diseases associated with an increased inducible microsomal prostaglandin E2 synthesis-1 (mPGES-1) activity or increased prostaglandin E2 synthesis.
Applicant(s) Medeon Pharmaceuticals Gmbh
Representative Drug(s) D0OE9W Drug Info N.A. [1]
Patent ID WO2008071173
Title Preparations for Inhibiting Prostaglandin E2 Synthesis.
Abstract The present invention relates to preparations of acylphloroglucinols, in particular hyperforin and myrtucommulone and derivatives thereof, the provision of these preparations for the therapeutic treatment of inflammatory diseases, painful and feverous conditions and cancer diseases which are accompanied by increased activity of the inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) or increased prostaglandin E2 synthesis, and also the appertaining methods.
Applicant(s) Eberhard Karls University
Representative Drug(s) D0WG5P Drug Info N.A. [1]
Patent ID WO2009146696
Title Use of Indole-3-Carboxylic Esters for Inhibiting Microsomal Prostaglandin E2 Synthase.
Abstract The present invention relates to the use of indole-3-carboxylic esters and derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. More particularly, the invention relates to the use of derivatives of 3...arboxyaryl[g]indole, in particular of 2-aryl- and 2-arylalkylaryl[g]indole-3-carboxylic esters and structural derivatives thereof for inhibiting inducible microsomal prostaglandin E2 synthase-1 and/or for inhibiting 5-lipoxygenase. The invention further relates to the use of indole-3-carboxylic esters for producing a medicament for treatment of PGE2- and/or 5-LO-mediated disorders and pathological states, especially of inflammatory chronic inflammations such as rheumatoid arthritis, osteoarthritis, disorders of the cardiovascular system, asthma, allergic rhinitis, multiple sclerosis, inflammatory skin disorders, osteoporosis and cancer, pain and fever, in which PGE2 and/or 5-LO products are involved.
Applicant(s) Univ Tuebingen
United States Patent and Trademark Office (USPTO)
Patent ID US2013210844
Title Tricyclic Compounds As Mpges-1 Inhibitors.
Applicant(s) Glenmark Pharmaceuticals Sa
Representative Drug(s) D0EB9M Drug Info IC50 < 50 nM [1]
Patent ID US2012309738
Title Novel Compounds.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0I5DE Drug Info IC50 = 1.3 nM [1]
Patent ID US2009163586
Title Bis-Sulfonylamino Derivatives In Therapy 205.
Applicant(s) Astra Zeneca Ab
Representative Drug(s) D0O2DY Drug Info IC50 = 12.2 nM [1]
German Patent and Trade Mark Office (DPMA)
Patent ID DE102009004436
Title Verwendung Einer Tirucallensaure, Einer Luoansaure Oder Einer Robursaure Als Arzneimittel.
Applicant(s) Aureliasan Gbh
Representative Drug(s) D0RM0U Drug Info N.A. [1]
References  Top
REF 1 Microsomal prostaglandin E2 synthase-1 inhibitors: a patent review.Expert Opin Ther Pat. 2017 Sep;27(9):1047-1059.

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