65 results about "EP4 Receptor" patented technology

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.

[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.

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.

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.

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.

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 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 1

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.

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.

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).

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.

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.

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 1

wherein X is SO or SO₂, but preferably SO, and wherein

• R³ denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl
• and wherein R¹ and R² have the meanings given in claim 1,
• the preparation thereof and the use thereof for the treatment of respiratory complaints.

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.

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.

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.

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.

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 I

or 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.