113 results about "PDE4 Inhibitors" patented technology

Disclosed are: a safe and highly effective prophylactic/ameliorating or therapeutic agent for NASH; and a method for using the agent. The prophylactic/ameliorating or therapeutic agent for NASH comprises a combination of at least one component selected from the group consisting of ω3PUFAs, a pharmaceutically acceptable salt thereof and an ester thereof and a PDE4 inhibitor as active ingredients.

The present invention is directed to the use of a PDE4 inhibitor and a glucocorticoid to treat peripheral B-cell neoplasms. In particular, the present invention provides a method of treating individuals (e.g. patients) diagnosed with peripheral B-cell leukemias by administering pharmaceutical compositions comprising Type 4 cyclic adenosine monophosphate phosphodiesterase inhibitors and a glucocorticoid. Preferably, the combination of the PDE4 inhibitor and the glucocorticoid has a synergistic effect on apoptosis such that the level of apoptosis induced is greater than the level that would be expected by simply adding a PDE4 inhibitor to a glucocorticoid.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The invention describes the use of a PDE4 inhibitor in combination with BH4 or a BH4 derivative for the prevention and/or treatment of respiratory diseases.

The present invention relates to a combination of therapeutic agents useful in the treatment of obstructive airways and other inflammatory diseases comprising (I) a PDEIV inhibitor that is therapeutically effective in the treatment of said diseases when administered by inhalation; together with (II) an anti-cholinergic agent comprising a member selected from the group consisting of tiotropium and derivatives thereof that is therapeutically effective in the treatment of said diseases when administered by inhalation; as well as to a method of treating said obstructive airways and other inflammatory diseases comprising administering to said mammal by inhalation a therapeutically effective amount of said combination of therapeutic agents; and a pharmaceutical composition comprising a pharmaceutically acceptable carrier together with said combination of therapeutic agents; and a package containing a pharmaceutical composition for insertion into a device capable of simultaneous or sequential delivery of said pharmaceutical composition in the form of an aerosol or dry powder dispersion to said mammal, where said device is a metered dose inhaler or a dry powder inhaler. It is preferred that said anti-cholinergic agent component be tiotropium bromide.

An aqueous pharmaceutical preparation for administration of a slightly soluble PDE4 inhibitor is described.

Methods of treating, preventing and/or managing hematological cancers are disclosed. Specific methods encompass the administration of a PDE4 inhibitor alone or in combination with a second active agent. The invention further relates to methods of treating leukemias and lymphomas which comprise the administration of a PDE4 inhibitor. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma.

The invention particularly relates to those drug combinations which, 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,

contain at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.

The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.

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

Through carrying out in-depth study on selaginella pulvinata extracts, the fact that selaginella pulvinata extracts have a significant anti-inflammatory activity is found. By using a multi-column chromatography separation technology and a semi-preparation high-performance liquid chromatography separation method, compounds (DZJB1-6) with a 9,9-diphenyl-1-(2-phenyleth-1-ynyl)-9H-fluorene new skeleton structure are extracted and separated, and named as selaginpulvilinsA-f (structure (I) thereof is as shown in the specification). The six compounds extracted and separated from selaginella pulvinata are subjected to structural modification, and then a series of compounds are obtained. The compounds can significantly inhibit the activity of type-4 phosphodiesterase (PDE4), and can be used for preparing PDE4 inhibitors, and treating asthma, chronic obstructive pneumonia, inflammations, and the like. According to the invention, a new structure is provided for the development of PDE4 inhibitors.

This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.

The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

This invention relates to the treatment of varying degrees of cognitive impairment associated with, for example, aging, Alzheimer's disease, schizophrenia with low dose administration of a PDE4 inhibitor, specifically roflumilast.

The invention relates to the novel identification of inhibitors of phosphodiesterase type 4 (“PDE4”) as agents which can reverse inhibition of neural regeneration in the mammalian central and peripheral nervous system. The invention provides compositions and methods using agents that can reverse the inhibitory effects on neural regeneration by regulating PDE4 expression. A composition comprising at least one PDE4 inhibitor in an amount effective to inhibit PDE4 activity in a neuron when administered to an animal is provided. Methods for regulating (e.g., promoting) neural growth or regeneration in the nervous system, methods for treating injuries or damage to nervous tissue or neurons, and methods for treating neural degeneration associated with disorders or diseases, comprising the step of administering to an animal a composition comprising a therapeutically effective amount of an agent which inhibits phosphodiesterase IV activity in a neuron are provided.

The present invention relates to a compound according to formula (I); wherein X1, X2, X3, X4 and X5 independently of each other represent -CH- or N; or X3, X4 and X5 independently of each other represent -CH- or N, and Xi and X2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, -CH2-C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hyd rates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

A composition for accelerating fracture healing, which comprises a PDE4 inhibitor as an active ingredient, specifically a composition comprising a PDE4 inhibitor and a biocompatible and biodegradable polymer is provided, which composition, when formulated into a form suitable for local administration such as microsphere preparation, can provide a pharmaceutical composition showing an excellent effect in the early healing of bone fracture. The said composition is useful in the healing of refractory fracture of elderly people and diabetic or osteoporosis patients.

A composition for regenerative treatment of cartilage disease, which comprises a PDE4 inhibitor as an active ingredient, specifically a composition comprising a PDE4 inhibitor and a biocompatible and biodegradable polymer is provided, which composition, when formulated into a form suited to administer locally to affected cartilage region, such as microsphere preparation, can provide a pharmaceutical composition showing an excellent effect in regenerative treatment of cartilage.