64 results about "Phosphodiesterase 4 Inhibitor" patented technology

The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general administration of phosphodiesterase 4 inhibitors and optionally training the animal under conditions sufficient to produce an improvement in performance.

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.

Compounds represented by Formula (I):or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.

The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general administration of phosphodiesterase 4 inhibitors and optionally training the animal under conditions sufficient to produce an improvement in performance.

Compounds of formula (I):wherein n, A, R1, and R2 are defined in the specification, are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for treating certain conditions.

This invention relates to treating respiratory diseases by administering a phosphodiesterase 4 inhibitor in combination with a β agonist and an anti-inflammatory steroid.

Pharmaceutical formulations in the form of inhalable dry powder comprising particles of a phosphodiesterase-4 inhibitor as active ingredient are useful for the prevention and / or treatment of respiratory diseases, such as asthma and COPD.

The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.

The invention discloses novel 3-cyclopropylmethoxy-4-alkoxybenzamide PDE (phosphodiesterase) 4 inhibitors. The inhibitors are compounds represented in a general formula I or a general formula II, prodrugs thereof, pharmaceutically usable salts thereof or solvates thereof, wherein R<1> is independent methyl (Me-) or difluoromethyl (CF2H-); R<2> is independent H, Me or Et; R<3> is independent H, MeO or Cl; CnH(2n+2) is alkyl, and N is larger than or equal to 2; a substance shown in the specification is a substituted benzene ring or pyridine ring; X is C or N; Y is C or N. The novel 3-cyclopropylmethoxy-4-alkoxybenzamide PDE 4 inhibitors have the advantages of high in-vitro enzyme inhibition activity, capability of selective application to PDE4 and good anti-inflammation effect and anti-depression effect.

The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of phosphodiesterase 4 inhibitors.

The invention discloses applications of a novel phosphodiesterase 4 (PDE4) inhibitor ZL-n-91 in preparation of medicines preventing lung cancer proliferation and metastasis. A survivorship curve and in-vitro cell experiments of mice prove that the phosphodiesterase 4 inhibitor ZL-n-91 can significantly inhibit lung cancer cell proliferation and metastasis, indicating that the phosphodiesterase 4 inhibitor ZL-n-91 is expected to be an important target in lung cancer proliferation and metastasis preventing researches, and providing bases for preparing medicines preventing lung cancer proliferation and metastasis. The phosphodiesterase 4 inhibitor ZL-n-91 has a good application prospect.

Pharmaceutical formulations in the form of inhalable dry powder comprising particles of a phosphodiesterase-4 inhibitor as active ingredient are useful for the prevention and / or treatment of respiratory diseases, such as asthma and COPD.

The invention discloses a topical pharmaceutical composition of a phosphodiesterase-4 inhibitor and a preparation method thereof, wherein the topical pharmaceutical composition comprises 0.5 to 10% bymass of apremilast active ingredient, 0.2 to 25% by mass of dimethyl sulfoxide and 65 to 99.3% by mass of a topical pharmaceutical acceptable carrier. The dosage forms of the topical pharmaceutical composition are ointments, creams, gels, coatings, lotions, tinctures, powders and liniments. The invention also discloses the preparation method of the topical pharmaceutical composition and use of the topical pharmaceutical composition. The pharmaceutical composition is not like hormonal drugs which have the side effects to cause adermotrophia after long time of use, and the pharmaceutical composition has no disadvantages such as recurrence after curing, has desired pharmacological activity and less side effects, is stable in quality and convenient to use, is safe and effective in treatment of eczema, and has strong practical application value.

The present invention relates to a phosphodiesterase 4 inhibitor capable of avoiding vomiting. The phosphodiesterase 4 inhibitor is a compound, a prodrug or a solvate represented by DTPM; and the DTPM is named as 1-(4-difluoro methoxy-3-(tetrahydrofuran-3-oxyl) phenyl)-3-dimethyl-1-ketone, and has a chemical formula shown as below. A plurality of experiments have proved that the DTPM has better effect on improvement of learning and memory compared with an existing antidepressant PDE4 inhibitor; in a Beagle dog vomiting effect observation experiment, no obvious vomiting inducing reaction is observed; and the DTPM has an inhibitor intensity 5000 times of that of other PDE4D families. The inhibitor provided by the invention can become a drug for treating depression and Alzheimer's disease and improving the cognitive ability, and capable of effectively reducing and even avoiding adverse reactions like vomiting.

The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the prevention and curative treatment of an inflammatory pulmonary disease.

The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the preventive and curative treatment of an inflammatory pulmonary disease.

The invention discloses a novel pharmaceutical composition for local drug administration with a phosphodiesterase-4 (PDE-4) inhibitor as an active component. The oral gel composition includes commonlyused additives: a gel matrix, a surfactant, a solubilizer, a pH regulator, a flavoring agent, a preservative, a solvent containing water or ethanol, and other ingredients. The composition acts directly on oral lesions, and effectively avoids the gastrointestinal adverse reactions caused by the composition. The preparation method of the local pharmaceutical composition is feasible in commercial production, and the quality of the prepared local pharmaceutical composition is stable, reliable, safe, effective, and convenient to use.

A pharmaceutical or veterinary composition, comprises a first active agent selected from a dehydroepiandrosterone and / or dehydroepiandrosterone-sulfate, or a salt thereof, and a second active agent comprising a phosphodiesterase-4 inhibitor for the treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases. The composition is provided in various formulations and in the form of a kit. The products of this patent are applied to the prophylaxis and treatment of asthma, chronic obstructive pulmonary disease, or other respiratory diseases.

The invention discloses the use of lithospermi naphthoquinone compounds in the preparation of phosphodiesterase 4 inhibitor. The invention also discloses the use of the lithospermi naphthoquinone compounds in the preparation of medicines for treating asthma and chronic obstructive pulmonary diseases, the use in the preparation of medicines for treating inflammatory bowel diseases, the use in the preparation of medicines for treating rheumatoid arthritis, particularly the use in the preparation of medicines for treating ulcerative colitis and Crohn disease. The invention also discloses the medicinal use of one or several of lithospermi extracts.

Pharmaceutical formulations in the form of inhalable dry powder comprising particles of a phosphodiesterase-4 inhibitor as active ingredient are useful for the prevention and / or treatment of respiratory diseases, such as asthma and COPD.

The invention relates to a phosphodiesterase 4 inhibitor apremilast composition and a quality detection method. The apremilast composition is a tablet, comprises lactose, magnesium stearate and otherauxiliary materials, and is used for treating adult patients suffering from active psoriatic arthritis, adult patients suffering from moderate-to-severe plaque psoriasis and suitable for phototherapyor systemic therapy, and adult oral ulcer patients related to Bessel's disease. The quality detection method comprises the step of determining the content of the enantiomer in the tablet, and comprises the following operations: by using a chiral chromatographic column and using n-hexane, isopropanol and the like as mobile phases, in a high performance liquid chromatography system, injecting 5 [mu]l of a system applicable solution into a liquid chromatograph, wherein the peak appearance sequence is enantiomer peaks and apremilast peaks successively, and the separation degree between two peaks is not less than 1.5, and precisely measuring 5 [mu]l of the test solution, injecting the test solution into a liquid chromatograph, recording a chromatogram, and calculating the content of the enantiomer according to an area normalization method if enantiomer peaks exist in the chromatogram of the test solution. The compositions and methods of the present invention exhibit excellent technical effects as described in the specification.

Treatment of varying degrees of cognitive impairment associated with Alzheimer's disease with a combination of a phosphodiesterase 4 inhibitor and an acetylcholinestase inhibitor, including roflumilast and donepezil hydrochloride.

The invention relates to a phosphodiesterase 4 inhibitor capable of avoiding a vomiting reaction. The phosphodiesterase 4 inhibitor is a compound or a pro-drug or a solvate represented by formula (I), wherein R1 is independent methoxyl, bromine and substituted aryl; X is a randomly substituted six-membered heterocycle; Y is -(CH2)n-, -NH(CH2)n- and -NH(CH2)n-O-, wherein n can be any one of 0, 1, 2 or 3; and Z is a randomly substituted aromatic ring or a randomly substituted heteroaromatic ring. The phosphodiesterase 4 inhibitor capable of avoiding the vomiting reaction is a novel biphenyl PDE4D inhibitor which is applicable to treating depression and Alzheimer's disease and improving cognitive competence, and is capable of avoiding a side effect such as the vomiting.

The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.

Compounds of formula (I):wherein n, A, R1, and R2 are defined in the specification, are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for treating certain conditions.

The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general administration of phosphodiesterase 4 inhibitors and optionally training the animal under conditions sufficient to produce an improvement in performance.