Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH?CH?, CH?2, ? or Cy, X is trivalent straight-chain alkylene (3–10C) or trivalent straight-chain 1-alkenylene (3–10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is ?2CH; and is otherwise trivalent straight-chain alkylene (5–10C) or trivalent straight-chain 1-alkenylene (5–10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1–6C); and n is 0–5; wherein each ? and Cy independently may optionally be substituted by alkyl (1–6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1–4C), or two substituents may form a 5–7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: Methods for treatment of depression or other affective mood disorders, such as bipolar manic depression or seasonal affective disorder, are disclosed by administration to a subject suffering or susceptible to same, of therapeutically effective diarylpiperazine compounds as herein described.

Abstract: The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.

Abstract: A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.

Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.

Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.

Abstract: A novel amorphous form of cetirizine and processes for making the amorphous form as well as compositions, pharmaceutical compositions, and methods utilizing the crystalline form are described.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: The present invention provides pharmaceutical compositions including a sedating antihistamine and a stimulant, and methods of use thereof. The stimulant reduces the sedation caused by the antihistamine, thereby allowing potent, but sedating, antihistamines to be used effectively.

Abstract: The present invention is directed to a pharmaceutical composition and method for treatment of rhinitis and cold like symptoms, the composition includes a non-steroidal anti-inflammatory drug (NSAID), a decongestant and an antihistamine preferably in a multi-layer tablet comprising an immediate release layer and an extended release layer to optimize the delivery profile and match the duration of biological action of the multiple active agents.

Abstract: This invention features a method for modulating human N-type calcium channel &agr;1B+SFVG subunit activity.

Abstract: The present invention includes methods of treating allergic skin conditions and disorders by combined administration of an histamine H1 receptor antagonist and a histamine H3 receptor antagonist.

Abstract: A pharmaceutical composition comprising a tiotropium salt; and an antihistamine, optionally together with a pharmaceutically acceptable excipient, the tiotropium salt and the antihistamine optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of respiratory tract diseases.

Abstract: Compounds of the formula 1

Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

Abstract: The present invention relates to crystalline and amorphous forms of dextrorotatory dihydrochloride salt of cetirizine, the process for the preparation thereof and compositions containing the same. The invention also relates to the crystalline and amorphous forms of levorotatory dihydrochloride salt of cetirizine, the process for the preparation thereof and compositions containing the same. Both crystalline and amorphous salt forms of cetirizine dihydrochloride are suitable for pharmaceutical purposes in the treatment of allergies, including ailments such as chronic and acute allergic rhinitis, allergic conjunctivitis, pruritus, urticaria and the like.

Abstract: Methods and pharmaceutical compositions employing (+) cetirizine, (−) cetirizine, or racemic cetirizine, or a pharmaceutically acceptable salt thereof, and a leukotriene inhibitor, or a pharmaceutically acceptable salt thereof, or decongestant for the treatment, management, and/or prevention of inflammation, asthma or symptoms thereof, allergic disorders such as allergic rhinitis, and dermatitis.

Abstract: The present invention concerns a tablet comprising two distinct segments. More particularly the invention relates to combinations of two pharmaceutical substances and methods of treatment of allergic disorders.

Abstract: The present invention relates to compositions and methods of treatment for cardioprotection through the use of non-peptidic delta opioid receptor agonist compound(s) that mediate cardioprotective effects of ischemic preconditioning. The compounds are used to reduce injury associated with ischemia and reperfusion of cardiac tissue. Further, the compounds may be used in solutions preserving the viability of an isolated organ.

Abstract: The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

Abstract: Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R6, R7, A and Z have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as a process for the preparation of such compounds and intermediate products of this process.

Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1-C6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.

Abstract: The present invention provides a combination of (a) a histamine H1 receptor antagonist and (b) an antagonist that is at least 10-fold selective for the histamine H4 receptor as compared to the histamine H3 receptor; and an antagonist that is at least 10-fold selective for the histamine H4 receptor as compared to the histamine H3 receptor: and compositions and uses thereof.

Abstract: The present invention relates to the amorphous form of levocetirizine dihydrochloride. The present invention also relates to the process for the preparation of the amorphous form of levocetirizine dihydrochloride. The amorphous form of levocetirizine dihydrochloride is suitable for pharmaceutical purposes in the treatment of allergies, including ailments such as chronic and acute allergic rhinitis, allergic conjunctivitis, pruritus, urticaria and the like.

Abstract: Nitric acid salts with medicines active in the respiratory system pathology treatment.

Abstract: The present invention relates to the delivery of antidepressants through an inhalation route. Specifically, it relates to aerosols containing an antidepressant that are used in inhalation therapy. In a method aspect of the present invention, an antidepressant is administered to a patient through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises an antidepressant to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles with less than 5% antidepressant degradation products. In a kit aspect of the present invention, a kit for delivering an antidepressant through an inhalation route to a mammal is provided which comprises: a) a thin coating of an antidepressant composition and b) a device for dispensing said thin coating as a condensation aerosol.

Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula 1

Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula 1

Abstract: A composition of an antitussive, a decongestant, and diphenhydramine as an antihistamine to treat upper respiratory and oral pharyngeal congestion and related symptoms in a patient. In addition to providing antihistamine effects, diphenhydramine also provides effects as an anti-cholinergic, an analgesic, an antitussive, and an analgesic adjuvant.

Abstract: Disclosed are methods of preventing or treating cardiac arrhythmia comprising administering to a mammal in need thereof, such as a human, an effective amount of vanoxerine (GBR 12909) or a pharmaceutically acceptable salt, derivative or metabolite thereof.

Abstract: Compositions and methods for treating VKC, GPC, AKC and allergic conjunctivitis with H1 antagonists and ocularly safe steroids are disclosed.

Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula 1

Abstract: Methods of treating and managing cancer are disclosed, which comprise the administration of an antihistaminic agents or structurally/functionally related to compound, optionally in combination with one or more additional anti-cancer agents. Pharmaceutical compositions, including single unit dosage forms, and kits useful in the treatment and management of cancer are disclosed. Also disclosed is a method of determining effectiveness of a cancer treatment.

Abstract: The subject invention provides methods for the treatment of ASD and/or PTSD comprising the administration of a dose of an SSRI taken soon after a trauma (for example, less than 48 hours and before the onset of ASD.

Abstract: A drug, affecting the hyperactivated immunologic effector cells, comprising (I) a Ca-antagonist and (II) an agent, reducing the intracellular cAMP/cGMP-ratio, is being described. In addition, a drug, affecting the hyperactivated immunologic effector cells, consisting of (I) an agent, eliminating the hyperactivated effector cells and (II) alloreactive cells with predetermined cell death, is being described.

Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

Abstract: A method for the treatment, prevention and amelioration of colds and/or cough in a subject in need of such treatment, prevention and amelioration, comprises administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and one or more colds and cough active ingredient. Compositions, pharmaceutical compositions and kits for practicing the method are also disclosed.

Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.

Abstract: The present invention relates to a method for preventing the onset of asthma which comprises administering to a patient a therapeutically effective amount of cetirizine, an individual optical isomer thereof or a pharmaceutically acceptable salt thereof.

Abstract: Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-1a and/or MCP-1 on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissue.

Abstract: Compositions and methods for treating a glomerular disorder. Compositions and methods comprise a cytochrome P450 inhibitor. Preferred inhibitors inhibit a cytochrome P450 2B family member. Compositions and methods reduce proteinuria associated with a glomerular disorder, such as, minimal change nephrotic syndrome.

Abstract: Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.

Abstract: Compositions and methods for treatment of a urinary tract dysfunction by administering to a subject in need of such treatment a pharmaceutical composition including a delta opioid receptor agonist in an amount effective to reduce the effects of the urinary tract dysfunction. The compositions may further include an additional active agent that is used to treat urinary tract dysfunctions, e.g., alpha-adrenergic agonists, anticholinergics, alpha-adrenergic antagonists and tricyclic antidepressants.

Abstract: The invention relates to a rapidly disintegrating oral antihistamine dosage formulation and method of preparing the rapidly disintegrating formulation wherein the formulation is designed to dissolve in the buccal cavity of the patient.

Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a PDE IV inhibitor in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a PDE IV inhibitor and an anxiolytic agent or antidepressant.

Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

Abstract: A palatable chewable tablet is described herein for oral administration of cetirizine dihydrochloride. The formulation is made more palatable by incorporating a combination of a grape flavoring agent with a vanilla flavoring agent.

Abstract: A pharmacological composition includes an anti-histaminic in spray formulation that reduces symptomatic skin itching of skin without substantially eliciting weight gain or sedation in the patient when the composition is sprayed onto the area of skin at a dosage of at least 10 mg/ml over a period of at least 10 applications. Particularly contemplated anti-histaminic include hydroxyzine and ketotifen.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.