39 results about "Prostaglandins D" patented technology

An object of the present invention is to provide a method of identifying a substance which acts on a newly found second human prostaglandin D2 receptor subtype that differs from the DP receptor, and is useful for treating or preventing various diseases. In order to attain the object, the present invention provides a method of identifying properties of a test substance with respect to a human prostaglandin D receptor, by establishing correlation between the effect of a test substance on human CRTH2 with the effect of the test substance on the human prostaglandin D receptor.

A compound of the formula (I):wherein A is alkylene optionally having an unsaturated bond; R is —C(═O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(═O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.

Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).

Methods for the detection of active lupus nephritis (LN) and worsening renal disease activity and / or active LN in patients diagnosed with systemic lupus erythematosus, using a panel of biomarkers including transferrin (Tf), ceruloplasmin (Cp), alpha-1-acid glycoprotein (AGP1), lipocalin-like prostaglandin D synthetase (L-PGDS), and urinary neutrophil gelatinase associated lipocalin (UNGAL).

The present invention relates to the discovery that PDG2 is the nautral ligand for orphan receptor CRTH2, which interaction, it will now immediately be recognized, is important in the development of valuable pharmaceuticals. The present invention is therefore related to methods for screening for therapeutic compounds useful in the treatment of PGD2-related disorders such as allergy, asthma and inflammation. Appropriate assay methodology is also disclosed.

The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I),wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention relates to a prostaglandin D2 metabolite, derivatives thereof, compositions comprising the metabolite, and an antibody that specially binds to the metabolite. Methods of use are also provided.

Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).

The present invention provides cell lines expressing endogenous PGD2-specific receptors, methods for increasing expression of the receptors and assays utilizing the hereindisclosed cell lines for identifying modulators of the PGD2-specific receptors. Increasing expression of PGD2-specific receptors is achieved by treating the disclosed cell lines with an agent that induces differentiation.

The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I),wherein R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I),wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin D2 (PGD2) receptors, DP-2 (GPR44). Compositions and methods for regulating hair growth include inhibiting hair growth by administering a DP-2 agonist, or stimulating hair growth by administering a DP-2 antagonist.

The present invention provides a benzimidazole compound represented by Formula (I)wherein X1 is oxygen or carbonyl, and R1 is a furan ring having 1 to 3 substituents or a pyrrole ring that may have 1 to 3 substituents; excluding compounds represented by Formula (I) wherein at least one of the substituents is a phosphoric acid group or a phosphoric ester group; or a salt thereof. The benzimidazole compound or salt thereof has excellent prostaglandin synthase inhibitory activity, and is useful as an agent for preventing and / or treating diseases in which prostaglandin D2 or metabolites thereof participates, such as allergic and inflammatory diseases, and as inhibitor for the exacerbation of Alzheimer's disease or cerebral damage.

The present application provides a human gene over-expressing animal, which is a non-human animal carrying a human hematopoietic prostaglandin D2 synthase gene in its somatic cell chromosome and expressing a large amount of human prostaglandin D2 synthase, wherein the animal is one obtained through ontogenesis of a totipotency cell of a non-human animal or offspring of the obtained animal, and the totipotency cell is introduced with said synthase gene. The present application also provides a method of using the transgenic animal for testing in vivo activity of a candidate for anti-allergy medicines, sleep-controlling substances and candidates for anti-obesity.

There are provided a compound for treatment or prevention of brain injury caused by diseases such as cerebrovascular disorder, brain degenerative disease and demyelinating disease and a method for screening the same. Brain injury in which prostaglandin D2 is participated is treated or prevented by inhibition of hematopoietic prostaglandin D synthase induced in microglia cell or macrophage of brain injury area by diseases such as cerebrovascular disorder, brain degenerative disease or demyelinating disease or by inhibition of activation of prostaglandin D receptor expressed in astroglia cell around the injured area. There is also provided a method of testing those pharmaceutical substances using a transgenic mouse in which human hematopoietic prostaglandin D synthase is expressed in large amounts.

The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.

The present invention relates to azaindole acetic acid derivatives of formula (I),wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

Compounds of Formula I: in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and / or IL-13. The Formula I is shown in the description.

The present invention relates to azaindole acetic acid derivatives of formula (I),wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention relates to azaindolle acetic acid derivatives of formula (I),wherein R1 and R2 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I),wherein R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

Methods for the detection of active lupus nephritis (LN) and worsening renal disease activity and / or active LN in patients diagnosed with systemic lupus erythematosus, using a panel of biomarkers including transferrin (Tf), ceruloplasmin (Cp), alpha-1-acid glycoprotein (AGP1), lipocalin-like prostaglandin D synthetase (L-PGDS), and urinary neutrophil gelatinase associated lipocalin (UNGAL).

The invention relates to a method for predicting prognosis of a heart failure patient by using data of an arachidonic acid metabolome in serum. The metabolome products of the arachidonic acid are 14, 15-DHET: 14, 15-dihydroxyeicosatrienoic acid, 14, 15-EET: 14, 15-epoxyeicosatrienoic acid, PGD2: a prostaglandin D2, and 9-HETE: 9-hydroxyeicosatetraenoic acid. Prediction of the prognosis condition of the heart failure patient is to predict the risk of total cause death of the heart failure patient within one year.

A method of treating a hypopigmentary condition in a subject comprising administering to the subject an amount of SOX9 sufficient to treat melanoma is disclosed. The hypopigmentary condition can be a result of surgery, trauma or vitiligo. A method of treating a hyperpigmentary condition in a subject comprising administering to the subject an amount of inhibitor of SOX9 activity sufficient to treat melanoma is disclosed. A method of treating melanoma in a subject comprising administering to the subject an amount of SOX9 sufficient to treat melanoma is disclosed. A method of treating melanoma in a subject comprising increasing the amounts of retinoic acid and SOX9 in the subject by amounts sufficient to treat melanoma. A method of treating melanoma in a subject comprising administering to the subject an amount of prostaglandin D2 (PGD2) and retinoic acid (RA) sufficient to treat cancer. A method of sensitizing a melanoma cell to RA comprising administering to the subject an amount of SOX9 sufficient to decrease PRAME expression. A method of increasing p21 expression in a subject comprising administering to the subject an amount of SOX9 sufficient to increase p21 expression. Methods of screening for compounds that treat hypopigmentary conditions and / or melanoma are provided.

Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and / or IL-13.

The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I),wherein Y, Z, R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.