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65 results about "EP4 Receptor" patented technology
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Prostaglandin E₂ receptor 4 (EP₄) is a prostaglandin receptor for prostaglandin E2 (PGE₂) encoded by the PTGER4 gene in humans; it is one of four identified EP receptors, the others being EP₁, EP₂, and EP₃, all of which bind with and mediate cellular responses to PGE₂ and also, but generally with lesser affinity and responsiveness, certain other prostanoids (see Prostaglandin receptors). EP₄ has been implicated in various physiological and pathological responses in animal models and humans.
EP4 receptor selective agonists in the treatment of osteoporosis
Owner:PFIZER INC
Treatment of conditions that present with low bone mass by continuous combination therapy with selective prostaglandin ep4 receptor agonists and an estrogen
InactiveUS20070191319A1High cure rateLong bone extension is enhancedBiocideSkeletal disorderPresent methodCarboxylic acid
This invention is directed to methods for treating conditions which present with low bone mass in a patient in need thereof using continuous combination therapy with a synergistically effective combination of an EP4 receptor selective agonist or a pharmaceutically acceptable salt thereof, such as 5-(3-{2S-[3R-hydroxy-4-(3-trifluoromethyl-phenyl)-butyl]-5-oxo-pyrrolidin-1-yl}-propyl)-thiophene-2-carboxylic acid or a pharmaceutically acceptable salt thereof; and an estrogen or a pharmaceutically effective salt thereof, The present methods are useful for treating conditions that present with low bone mass including osteoporosis, osteotomy, osteoporotic fracture, childhood idiopathic bone loss, periodontitis and low bone mass and for enhancing bone healing following facial reconstruction, maxillary reconstruction or mandibular reconstruction, inducing vertebral synostosis, enhancing long bone extension, enhancing the healing rate of a bone graft or a long bone fracture or enhancing prosthetic ingrowth in a patient in need thereof.
Owner:PFIZER INC
Pyridone compound
[Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.
Owner:ASTELLAS PHARMA INC
Ep4 receptor agonists
InactiveUS20060167081A1Elevated intraocular pressureBiocideSenses disorderOsteoblastElevated intraocular pressure
This invention relates to potent selective agonists of the EP, subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK FROSST CANADA INC
Peptides and peptidomimetics useful for inhibiting the activity of prostaglandin F2alpha receptor
The invention relates to compositions which are useful for inhibiting prostaglandin F2αreceptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.
Owner:THERATECHONOLGIES INC +1
1,5-Disubstituted imidazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of eye and bone diseases
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors of formula (I), their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of the patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK FROSST CANADA INC
Selective EP4 receptor antagonistic substance for treatment of cancer
This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
Owner:ASKAT
1,5-distributed pyrrolid-2-one derivatives for use as ep4 receptor agonists in the teatment of eye diseases such as glaucoma
InactiveUS20050239872A1Elevated intraocular pressureBiocideSenses disorderDiseaseElevated intraocular pressure
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors of formula (1), their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of the patient.
Owner:MERCK FROSST CANADA INC
EP4 receptor selective agonists in the treatment of osteoporosis
This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists. This invention is especially directed to those methods wherein the EP4 receptor selective agonist is a compound of Formula I: wherein the variables are as defined in the specification.
Owner:PFIZER INC
EP4 receptor agonist, compositions and methods thereof
ActiveUS20050227969A1Elevated intraocular pressureBiocideSenses disorderOsteoblastElevated intraocular pressure
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK CANADA
Combinations of medicaments, containing PDE4-inhibitors and EP4-receptor-antagonists
The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma.The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1wherein X is SO or SO2, but preferably SO, and whereinR1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
Owner:BOEHRINGER INGELHEIM INT GMBH
Treatment of osteoporsis with EP2/EP4 receptor selective agonists
InactiveUS20010056060A1Reduce the chance of fractureImprove bone formationBiocidePeptide/protein ingredientsBone defectBone healing
This invention is directed to methods and pharmaceutical compositions comprising prostaglandin agonists which are userful to prevent bone loss, restore or augment bone mass and to enhance bone healing including the treatment of conditions which present with low bone mass, such as osteoporosis, and / or bone defects in vertebrates, and particularly mammals, including humans. This invention specifically relates to methods and pharmaceutical compositions comprising combinations of EP.sub.2 receptor selective agonists and EP.sub.4 receptor selective agonists and to methods and pharmaceutical compositions comprising agents which are agonists for both the EP.sub.2 receptor and the EP.sub.4 receptor.
Owner:CAMERON KIMBERLY O +3
Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists
The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
Owner:MERCK CANADA
EP4 Receptor Agonist, Compositions and Methods Thereof
InactiveUS20090270395A1Elevated intraocular pressureOrganic active ingredientsSenses disorderOsteoblastElevated intraocular pressure
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts. The compounds of the present invention are the compounds of Formula (I).
Owner:MERCK & CO INC
EP4 receptor antagonist and PD-1 inhibitor combined and used for treating cancer
The invention provides an EP4 receptor antagonist and a PD-1 inhibitor combined and used for treating cancer. The invention provides the product combination, including a first medicine composition (i)and a second medicine composition (ii), the first medicine composition contains a first active ingredient (a) which is the EP4 receptor antagonist and an acceptable vector on pharmacy, the second medicine composition contains a second active ingredient (b) which is the PD-1 inhibitor, and an acceptable vector on the pharmacy; and the medicine compositions of the first medicine composition and thesecond medicine composition are different, or the same. According to the product combination, malignant tumor can be treated synergistically.
Owner:SHANGHAI YUYAO BIOTECH LTD
Thieno-ring compound and synthesis method and application thereof
The invention discloses a thieno-ring compound as shown in the formula (I), a pharmaceutically acceptable salt, or a hydrate thereof, a composition containing the thieno-ring compound, and a preparation method thereof. The invention also discloses application of the thieno-ring compound as a prostaglandin EP4 receptor antagonist for preventing and treating prostaglandin PGE2 mediated diseases, including malignant tumors, autoimmune diseases, inflammation, pain or osteoarthritis.
Owner:SHANGHAI YUYAO BIOTECH LTD
Combinations of medicaments, containing PDE4-inhibitors and EP4-receptor-antagonists
The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma.The invention relates in particular to those medicament combinations which contain at least one EP4 receptor antagonist (2), in addition to one or more, preferably one, PDE4 inhibitor of general formula 1wherein X is SO or SO2, but preferably SO, and whereinR3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryland wherein R1 and R2 have the meanings given in claim 1, the preparation thereof and the use thereof for the treatment of respiratory complaints.
Owner:BOEHRINGER INGELHEIM INT GMBH
Oxazolidin-2-one and thiazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of glaucoma
InactiveUS20060154899A1Elevated intraocular pressureBiocideSenses disorderOsteoblastElevated intraocular pressure
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK FROSST CANADA INC
EP4 receptor selective agonists in the treatment of osteoporosis
This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists. This invention is especially directed to those methods wherein the EP4 receptor selective agonist is a compound of Formula I: wherein the variables are as defined in the specification.
Owner:PFIZER INC +1
EP4 Receptor Agonist, Compositions and Methods Thereof
InactiveUS20090105234A1Elevated intraocular pressureOrganic active ingredientsSenses disorderIntra ocular pressureElevated intraocular pressure
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK & CO INC
EP4 receptor agonist, compositions and methods thereof
Owner:BILLOT XAVIER +2
Combinations of medicaments, containing PDE4-inhibitors and EP4-receptor- antagonists
The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma.The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1wherein X is SO or SO2, but preferably SO, and whereinR1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
Owner:BOEHRINGER INGELHEIM INT GMBH
Oxazolidin-2-one and thiazolidin-2-one derivatives for use as EP4 receptor agonists in the treatment of glaucoma
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
Owner:MERCK FROSST CANADA INC
Selective ep4 receptor agonistic substance for treatment of cancer
This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
Owner:ASKAT
Methods of treatment with selective EP4 receptor agonists
The present invention provides a method of treating hypertension, liver failure, loss of patency of ductus arteriosus, glaucoma or ocular hypertension in a patient, comprising administering to the patient a therapeutically effective amount of a selective EP4 receptor agonist of Formula Ior a prodrug thereof, a pharmaceutically acceptable salt of the selective EP4 receptor agonist or prodrug or a stereoisomer or diastereomeric mixture of the EP4 receptor agonist, prodrug or salt, wherein the variables X, Z, Q, , and R2 are as defined in the specification.
Owner:PFIZER INC
Triazole compound, synthesis method and application thereof
ActiveCN108929281AHigh guiding valueOrganic active ingredientsOrganic chemistryImmunologic disordersDisease
The invention discloses a triazole compound as shown in a formula I and a formula II, and a pharmaceutical derivative and a hydrate of the triazole compound, a composition containing the triazole compound and a preparation method thereof. The invention also discloses a use of the triazole compound serving as a prostaglandin EP4 receptor antagonist for preventing and treating prostaglandin PGE2 mediated diseases, including malignant tumors, autoimmune diseases, inflammation, pains or osteoarthritis.
Owner:EAST CHINA NORMAL UNIV +1
Triterpenoid compounds and methods of use thereof
ActiveUS9029414B2High expressionSuppress bacterial and allergen-induced inflammationBiocideNervous disorderMedicineEP4 Receptor
Owner:THE HONG KONG UNIV OF SCI & TECH
Triterpenoid compounds and methods of use thereof
ActiveUS20110288169A1High expressionSuppress bacterial and allergen-induced inflammationBiocideNervous disorderMedicineEP4 Receptor
The present invention provides therapeutically active compounds and compositions as receptor antagonists and methods of use thereof. In one aspect, the compounds are useful in modulating pain, inflammation and acute phase reactions by inhibiting the PGE2 receptors including PGE2 EP1, EP2 and EP4 receptors.
Owner:THE HONG KONG UNIV OF SCI & TECH
Use of EP4 receptor antagonists for the treatment of NASH-associated liver cancer
ActiveUS10342785B2Avoid developmentInhibit growthOrganic chemistrySulfonylurea active ingredientsActive agentNK1 receptor antagonist
Owner:ASKAT
4-alkynyl imidazole derivative and medicine comprising same as active ingredient
ActiveUS9593081B2Superior receptor antagonistic actionOrganic active ingredientsNervous disorderAnalgesics drugsDisease
There are provided 4-alkynylimidazole derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof; the derivatives have a superior EP4 receptor antagonistic action and are useful as pharmaceuticals for the treatment of diseases associated with the EP4 receptor, for example, as anti-inflammatory and / or analgesic drugs for inflammatory diseases and diseases that involve various kinds of pains, and further as pharmaceuticals for the treatment of immune diseases that result from inflammations as evoked by tissue destruction due to the activation of Th1 cells and / or Th17 cells:
Owner:KAKEN PHARMA CO LTD
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