Methods for manufacturing tetranor-prostaglandin d, j, e, a and f metabolites

The present invention generally relates to synthetic methods for preparing tetranor-prostaglandin D, J, E, A, and F metabolites.

MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES

Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin Dmediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS). 160.-. (canceled)62. A compound of claim 61 , wherein Yis S.63. A compound of claim 62 , wherein W is a covalent bond.64. A pharmaceutical composition comprising a compound of claim 61 , or an equivalent thereof.65. A method of treating a disease or condition mediated at least in part by prostaglandin Dproduced by H-PGDS claim 61 , in a subject in need of such treatment claim 61 , comprising administering to the subject a therapeutically effective amount of a compound of .66. The method of wherein the disease or condition is allergy or allergic inflammation.67. The method of wherein the disease or condition is asthma.68. The method of wherein the disease or condition is Duchenne muscular dystrophy.69. A pharmaceutical composition comprising a compound of claim 61 , and a second pharmacologically active compound. The present invention claims priority from U.S. Provisional Application No. 61/098,942 filed Sep. 22, 2008 entitled “Multiheterocyclic Compounds for the Treatment of Allergy, Inflammation, and Immune Disorders.”Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin Dmediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).Allergic and inflammatory disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD), allergic conjunctivitis, and atopic dermatitis affect roughly one-fifth of the world population. Symptoms arising from antigenic challenge, including bronchoconstriction, bronchial hyperactivity, sneezing, nasal discharge, and nasal ...

MULTIHETEROARYL COMPOUNDS AS INHIBITORS OF H-PGDS AND THEIR USE FOR TREATING PROSTAGLANDIN D2 MEDIATED DISEASES

Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin Dmediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS). 169.-. (canceled)73. A compound of claim 72 , wherein Yis N.74. A compound of claim 73 , wherein:{'sup': 1', '3', '4', '5, 'each X, X, X, and Xis hydrogen;'}{'sup': '2', 'Xis hydrogen or fluoro;'}{'sup': '6', 'each Ris independently hydrogen, methyl, or trifluoromethyl;'}n is 0, 1, or 2;{'sup': '1', 'Zis phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, piperidin-4-yl, piperidin-3-yl, piperidin-3(R)-yl, piperidin-3(S)-yl, piperidin-2-yl, piperidin-2(R)-yl, piperidin-2(S)-yl, pyrrolidin-3-yl, pyrrolidin-3(R)-yl, pyrrolidin-3(S)-yl, pyrrolidin-2-yl, pyrrolidin-2(R)-yl, pyrrolidin-2(S)-yl, or azetidin-3-yl;'}{'sub': 2', 'q, 'the nitrogen atom of a piperidinyl, a pyrrolidinyl, or a azetidinyl ring is substituted with —(CH)Q;'}q is 0, 1, or 2;{'sub': 1', '6', '2', '3', '3', '6', '3', '6', '3', '6', '2, 'sup': 3', '3', '4', '5, 'Q is hydrogen, (C-C)-alkyl, —CHCF, (C-C)-alkenyl, (C-C)-alkynyl, (C-C)-cycloalkyl, phenyl, naphthyl, C(O)R, COR, C(O)NRR, a three- to six-membered heterocycle, or a five- to ten-membered heteroaryl;'}{'sup': '3', 'sub': 1', '6', '3', '6', '3', '6', '2', 'm', '3', '6', '2', 'm', '2', 'm, 'Ris hydrogen, (C-C)-alkyl, trifluoromethyl, (C-C)-alkenyl, (C-C)-alkynyl, (CH)(C-C)-cycloalkyl, (CH)phenyl, or (CH)-(five- to ten-membered heteroaryl); and'}m is 0, 1, or 2.75. A compound of claim 74 , wherein:{'sup': '1', 'Zis phenyl, 2-pyridyl, 3-pyridyl, or 4-pyridyl; and'}{'sup': '1', 'wherein said phenyl or pyridyl rings of Zare optionally substituted with one or two of any one or combination of the following: halo, hydroxy, methoxy, methyl, or trifluoromethyl.'}76. A compound of claim 75 , wherein:{'sup': '1', 'Zis phenyl; and'}{'sup': '1', 'wherein said phenyl ring ...

2-Aryl-5-heteroaryl pyridine and pyrimidine derivatives as pharmaceutical active agents

Prostaglandin e1 and e2 analogs for the treatment of various medical conditions

A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.

Prostaglandin e1 and e2 analogs for the treatment of various medical conditions

A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.

DERIVATIVES OF 5- (1H-IMIDAZOL-5-IL) -2-PHENYLPYRIMIDINE, AS INHIBITORS OF PROSTAGLANDIN D HEMATOPOYETIC SYNTHASE

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE R1 ES ALQUILO C1-C6, CICLOALQUILO C3-C6, FENILO, 2-PIRIDILO, 3-PIRIDILO, ENTRE OTROS; R2 ES FENILO, 3-FLUOROFENIL, 2-PIRIDIL, PIRIDIN, ENTRE OTROS; W ES ENLACE COVALENTE, O, S, SO, SO2, CO, NH, ENTRE OTROS; Y1, Y2 E Y3 FORMAN JUNTO AL N UN ANILLO DE PREFERENCIA PIRIMIDIN; U1, U2, U3, U4 FORMAN UN ANILLO DE PREFERENCIA 4-IL-OMIDAZOL, 3-PIRAZOL, OXAZOL. SON COMPUESTOS PREFERIDOS: ACIDO-2-(2-FENILPIRIMIDINA-5-IL)TIAZOL-4-CARBOXILICO; FENIL-(5-(2-(PIRIDIN-3-IL)-1H-IMIDAZOL-5-IL)PIRIMIDINA-2-IL)METANONA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE PROSTAGLANDINA D HEMATOPOYETICA (H-PGDS) UTILES EN EL TRATAMIENTO Y PREVENCION DE ENFERMEDADES Y AFECCIONES MEDIADAS POR PROSTAGLANDINA D2 REFERRING TO A COMPOUND OF FORMULA I, WHERE R1 IS C1-C6 ALKYL, C3-C6 CYCLOALKYL, PHENYL, 2-PYRIDYL, 3-PYRIDYL, AMONG OTHERS; R2 IS PHENYL, 3-FLUOROPHENIL, 2-PYRIDYL, PYRIDIN, AMONG OTHERS; W IS COVALENT LINK, O, S, SO, SO2, CO, NH, AMONG OTHERS; Y1, Y2 AND Y3 TOGETHER FORM A PIRIMIDIN PREFERENCE RING; U1, U2, U3, U4 FORM A PREFERENCE RING 4-IL-OMIDAZOLE, 3-PYRAZOLE, OXAZOLE. THE PREFERRED COMPOUNDS ARE: ACID-2- (2-PHENYLPYRIMIDINE-5-IL) THIAZOL-4-CARBOXYL; PHENYL- (5- (2- (PYRIDIN-3-IL) -1H-IMIDAZOL-5-IL) PYRIMIDINE-2-IL) METHANONE; AMONG OTHERS. SUCH COMPOUNDS ARE INHIBITORS OF HEMATOPOYETIC PROSTAGLANDIN D (H-PGDS) USEFUL IN THE TREATMENT AND PREVENTION OF DISEASES AND CONDITIONS MEDIATED BY PROSTAGLANDIN D2

Methods for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin d synthase

An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N- terminus of the enzyme.

Methods for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin d synthase

An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N- terminus of the enzyme.

Methods for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin d synthase

An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N- terminus of the enzyme.

Method for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin d synthase

An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N-terminus of the enzyme.

Methods for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin D synthase

Methods for assaying compounds or agents for ability to displace potent ligands of hematopoietic prostaglandin d synthase

An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N- terminus of the enzyme.

Methods for manufacturing tetranor-prostaglandin D, J, E, A and F metabolites

The present invention generally relates to synthetic methods for preparing tetranor-prostaglandin D, J, E, A, and F metabolites.

Methods for manufacturing tetranor-prostaglandin d, j, e, a and f metabolites

The present invention generally relates to synthetic methods for preparing tetranor-prostaglandin D, J, E, A, and F metabolites.

Methods for manufacturing tetranor-prostaglandin d, j, e, a and f metabolites

The present invention generally relates to synthetic methods for preparing tetranor-prostaglandin D, J, E, A, and F metabolites.

Prostaglandin e1 and e2 analogs for the treatment of various medical conditions

A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.

Prostaglandin e1 and e2 analogs for the treatment of various medical conditions

A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.