| 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 |
[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 |
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[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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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] |
