435 results about "Phosphodiesterase" patented technology

The present invention relates to novel compositions and therapeutic methods for the treatment of pain, in particular neuropathic, ischemic, muscle, arthritic or multiple sclerosis pain. The compositions include a combination of an alpha2-adrenergic agonist or a nitric oxide donor combined with a phosphodiesterase (PDE) or a phosphatidic acid (PA) inhibitor, which have been found to act together synergistically to provide effective treatment for pain, especially when administered topically.

Purine phosphodiesterase 7 (PDE 7) inhibitors of the following formulas

wherein R¹, Z, Y and J are described herein, and analogs thereof are provided which are useful in treated T-cell mediated diseases. R² is defined by the following

• • (a) heteroaryl, or heterocyclo, either of which may be optionally substituted with one to three groups T¹, T², T³;
  • (b) aryl substituted with one to three groups T¹, T², T³ provided that at least one of T¹, T², T³ is other than H; or
  • (c) aryl fused to a heteroaryl or heterocyclo ring wherein the combined ring system may be optionally substituted with one to three groups T¹, T², T³.

PCT No. PCT/US98/23482 Sec. 371 Date Feb. 7, 2000 Sec. 102(e) Date Feb. 7, 2000 PCT Filed Nov. 4, 1998 PCT Pub. No. WO99/26616 PCT Pub. Date Jun. 3, 1999The present invention provides compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of diseases whose treatment benefits from the inhibition of phosphodiesterase (PDE-IV) or Tumor Necrosis Factor (TNF) including asthma, allergic diseases, rheumatoid arthritis, osteoarthritis, septic shock. The compounds provided by this invention have formula (I) wherein R1, R2, R3, R4 are as defined herein.

The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.

Methods of modulating type-I interferon production in a cell are provided. Aspects of the methods include modulating cytosolic cyclic di-adenosine monophosphate (c-di-AMP) activity in the cell in a manner sufficient to modulate type-I interferon production in the cell. Additional aspects of the invention include c-di-AMP activity modulatory compositions, e.g., c-di-AMP, mutant Listeria bacteria, cyclase and/or phosphodiesterase nucleic acid or protein compositions, etc. The subject methods and compositions find use in a variety of applications, including therapeutic applications.

The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Compounds of the formula (I) ##STR1## are useful as inhibitors of cGMP PDE especially Type 5.

The invention relates to therapeutic antisense oligonucleotides directed against genes coding for phosphodiesterase (PDEs) and the use of these in combination. These antisense oligonucleotides may be used as analytical tools and/or as therapeutic agents in the treatment of disease associated with reduced cellular cAMP in a patient, such as inflammatory diseases of the respiratory tract including, for example, asthma, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome, bronchitis, chronic bronchitis, silicosis, pulmonary fibrosis, lung allograft rejection, allergic rhinitis and chronic sinusitis as well as other conditions in which an increase in cyclic AMP or a decrease in PDE levels is beneficial.

The present invention relates to the use of neutral endopeptidase inhibitors (NEPi) and a combination of NEPi and phosphodiesterase type 5 (PDE5) inhibitor for the treatment of male sexual dysfunction, in particular MED.

Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula

wherein R¹, R², Z, J and L are described herein, and analogs thereof are provided which are useful in treating T-cell mediated diseases.

The present invention provides a therapeutic method for treating gastric lesions, including administration to a patient in need thereof of an effective amount of an A_2A adenosine receptor agonist. The A_2A adenosine receptor agonist can be a compound of formula (I) as disclosed herein. The invention further provides a therapeutic method for treating the patient with an A_2A adenosine receptor agonist, optionally, in combination with a Type IV phosphodiesterase (PDE) inhibitor. In one embodiment, the gastric lesions are caused by, or aggravated by, the use of NSAIDS such as, for example, aspirin.

Compounds of general structural formula (I) wherein A represents a 5- or 6-membered heteroaryl group containing at least one heteroatom selected from the group consisting of oxygen, nitrogen, and sulfur, and use of the compounds, and salts and solvates thereof, as therapeutic agents, are disclosed.

Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.

Compounds of the formula

wherein R₁, R₂, R₃, R₄, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.

The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represented by the following formula, its salt or hydrates thereof, and a medicament comprising the same.wherein the ring A is an aromatic hydrocarbon ring which may have a heteroatom, the ring B represents (a) a saturated hydrocarbon ring, (b) an unsaturated hydrocarbon ring, (c) a saturated heterocyclic ring or (d) an unsaturated heterocyclic ring, all of which may have a substituent group.

The invention relates to a method for preparing a mixed-type nucleotide feed additive from yeast cells and applications of the feed additive, which belong to the technical field of the preparation of nucleotide feed additives from yeast cells. The method comprises the steps: using yeast cells as raw materials and combining a homogenization method and a salt method to break yeast cell walls ; separating the yeast cell walls, protein and other insoluble substances by centrifugation and fractional isoelectric crystallization; specially collecting RNA precipitates at special isoelectric points to obtain wet and crude nucleic acid with the purity of 70 percent; dissolving the wet and crude nucleic acid in water, using high-activity phosphodiesterase from malt roots to carry out a high-efficiency directional enzymatic reaction; directly spraying, drying and crushing the solution after the enzymatic reaction to obtain the mixed-type nucleotide feed additive product comprising the protein content lower than 10 percent and four monosomic nucleotides (AMP, GMP, CMP and UMP) larger than 60 percent. After the feed additive is applied to animal feed, the intestinal absorption function of animals can be notably improved, the growth of the animals is stimulated, and the immune function, the antiviral capability and the anti-stress capability of the animals are improved.

The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotirazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.

1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.

The invention relates to a series of derivatives (I) of isopentenyl flavonoid and preparation methods and uses thereof. The pharmacology experiments show that: the compounds can inhibit cGMP specific phosphodiesterase, in particular to selectively inhibiting phosphodiesterase V (PDE5), and have wide application in the treatment and prevention of sexual function trouble and the improvement of vascoconstriction related diseases.