102 results about "Histamine receptor" patented technology

Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H₄ receptor, including allergic rhinitis.

2-Aminopyrimidine compounds are described, which are useful as H₄ receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H₄ receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.

Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I

wherein R¹, R², R³, R⁴, R⁵, R⁶, A, X, Y and Z are as defined in the specification.

Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H₃ receptor and/or serotonin transporter modulators useful in the treatment of histamine H₃ receptor- and/or serotonin-mediated diseases.

The present invention relates, in general, to a method of preventing or delaying the onset of Alzheimer's disease and related neurodegenerative disorders. The invention also relates to a method of treating Alzheimer's disease and related neurodegenerative disorders so as to ameliorate the further progress of symptoms. The methods involve the administration of a non-steroidal anti-inflammatory agent and/or a histamine H2 receptor blocking agent. According to indication, the present method can be applied to individuals who are currently asymptomatic but at risk of developing Alzheimer's disease, to individuals who have mild cognitive symptoms that may either denote an incipient prodrome of Alzheimer's disease or represent early symptoms (prodromal stage), or to individuals who have a clinical diagnosis of Alzheimer's disease.

The present invention relates, inter alia, to novel piperazines of the following formula:

to the use of these compounds in the preparation of pharmaceutical compositions, to pharmaceutical compositions comprising the compounds, and to methods of treatment employing these compounds or compositions. The compounds show a high and selective binding affinity for the histamine H3 receptor, indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases or disorders related to the histamine H3 receptor.

The present invention relates to substituted heterocyclic compounds of Formula I or XI:

or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine II4 receptor inhibitors useful in the treatment of histamine II4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

The invention provides a rupatadine fumarate compound which has dual effects of antihistamine and antagonistic platelet activating factor (PAF). According to the research, allergy and inflammatory diseases are multi-factor complex processes caused by generation and release of various different media; histamine is the most inflammatory medium appearing in allergy early symptom, and the disease symptoms including sneezing, rhinocnesmus, tearing, running nose, skin itch, wheal and the like are mostly caused by histamine H1 receptor. And PAF also can cause bronchial constriction and increased permeability of the vessel, so that running nose, nasal congestion, wheal and itch are caused; meanwhile, the PAF is also a main cause of asthma. The antiallergic drug which is clinically used only has an antihistamine activity effect, but does not have a PAF antagonistic effect.

The present invention relates to compounds and methods which may be useful as inhibitors of HiR and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.

Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

This invention relates to a transdermal drug formulation that includes a pharmaceutically suitable carrier; an effective amount of a therapeutic agent; and a histamine type 4 receptor (“H4R”) agonist, as well as a transdermal vaccine formulation that includes a pharmaceutically suitable carrier; an effective amount of an antigen or antigen-encoding nucleic acid molecule present in the carrier, and optionally one or more adjuvants; and an H4R agonist. The present invention also relates to transdermal delivery device including such formulations and methods of administering such formulations. The present invention also relates to methods of enhancing epithelial barrier formation in a patient involving administering to the patient at a site of epithelial disruption an amount of a formulation that comprises an H4R antagonist. The present invention also relates to a method of inhibiting pathogen infection or local spread of infection in the epithelia using an H4R antagonist, an H1R antagonist, or a combination thereof.

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases

This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain pyrazole derivatives, their salts and solvates. These compounds have H₃ histamine receptor binding activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H₃ receptor modulation is beneficial.

The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently —(C₁—C₇) alkyl (optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence —H, -halogen, or —CH₃.

The invention discloses a method utilizing phage antibody library to screen human histamine receptor 4 (HR4) epitope mimic peptide and a vaccine construction method thereof. A phage random dodecapeptide library is utilized to screen one polypeptide section, and the amino acid sequence of the polypeptide section is FNKWMDCLSVTH. The provided method utilizes a phage random dodecapeptide library technology to screen the polypeptide sequence of HR4 epitope mimic peptide; ELISA identifies the affinity of phage monoclone on HR4 mono-antibody, then sequencing is carried out to obtain one polypeptide sequence, which is names as PT1; the targeting result of phage positive clone is further identified to indicate that phage positive clone can specifically combine the human HR4 monoclonal antibody; the human HR4 monoclonal antibody specific polypeptide can be obtained through screening; thus the HR4 epitope mimic peptide vaccine can be constructed; and the vaccine on the basis of HR4 mimic epitope can be used to treat allergic rhinitis in clinic, can also be applied to the research on HR4 antagonist, and provides primary experimental references for the construction of HR4 antagonist.

The present invention discloses novel compounds of Formula I

or pharmaceutically acceptable salts thereof, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical. compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.

The invention relates to the field of pharmaceutical chemistry and in particular relates to a class of compounds (I) with dual antagonistic activity of histamine H1 and H4 receptors. Pharmacodynamic experiments prove that the compounds disclosed by the invention have dual antagonistic effects of the histamine H1 and H4 receptors. The compounds disclosed by the invention have obvious anti-allergicactivity, can further inhibit inflammatory factor release and achieve anti-inflammatory actions.

To clarify histamine receptor H3 protein function in vivo, the present inventors constructed a nonhuman higher animal in which the expression of a histamine receptor H3 gene was artificially inhibited. As a result, the present inventors found that this nonhuman higher animal showed increased body weight, food intake, blood insulin level, or blood leptin level compared with a control. Thus, the present inventors found that abnormalities in the histamine receptor H3 protein relate to diseases characterized by changes in body weight or food intake, and this has made it possible to screen drugs for treatment or prevention of these diseases, and to examine these diseases.