Abstract: Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.

Abstract: The invention concerns the use of nicergoline for preventing and/or treating motor neuron diseases.

Abstract: Duplex polynucleotides containing damage or errors are detected with hindered intercalating compounds which are capable of intercalating only in the presence of such damage or error. Conditions characterized by the presence of polynucleotide errors or damage are treated with such compounds that are capable of catalyzing polynucleotide cleavage with light.

Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.

Abstract: The invention concerns the use of nicergoline for treating pyramidal spasticity of neurological diseases involving a pathology of the cerebrospinal tract.

Abstract: Method for mediating the effects of light on melatonin rhythmicity in mammals and a method of mediating circadian rhythms, effected by the administration of a compound or compounds effective at a 5-HT2c serotonin receptor site. By administration of selected doses of the 5-HT2c receptor active compound it is possible to advance or delay circadian rhythms as measured by the rate of melatonin production or moderation of core body temperature rhythms.

Abstract: The invention concerns the use of 1,6-dimethyl-8&bgr;-hydroxymethyl-10&agr;-methoxyergoline for preventing and/or treating motor neuron diseases.

Abstract: The invention concerns the use of nicergoline for treating pyramidal spasticity of neurological diseases involving a pathology of the cerebrospinal tract.

Abstract: The invention provides methods of treating erectile dysfunction comprising the step of placing within the fossa navicularis of the patient an effective erection-inducing amount of a prostaglandin E1 composition of a semi-solid consistency, as well as suitable applicators. The composition comprises prostaglandin E1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N,N-disubstituted amino)-alkanoate ester, an (N,N-disubstituted amino)-alkanol alkanoate, or a mixture of these. The lipophilic compound may be an aliphatic C1 to C8 alcohol, aliphatic C2 to C30 ester, an aliphatic C8 to C30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 7.4.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.

Abstract: The invention relates to novel derivatives of ergoline of the general formula 1 in which R1 together with the two adjacent N atoms is the residue of a diamine and R4 together with the two adjacent carbonyl groups is the residue of a dicarboxylic acid. R2, R3, R6, R7, R8 can be H or an organic radical. R7 and R8 are H or together are a bond. The compounds show a strong antihypertensive effect. These effects moreover occur after intravenous and enteral administration even at dosages in the region of a few &mgr;g/kg (body weight). The compounds can accordingly be used as pharmaceuticals for hypertensive diseases in human medicine.

Abstract: Methods for reducing the incidence and occurrence of dermal lesions in mammals, particularly human patients, who receive chemotherapy treatment and in the course of such treatment are administered liposomal formulations of cytotoxic agents are provided. Cytotoxic agents typically include doxorubicin, cytarabine, epirubicin, daunorubicin, 5-fluorouracil (5-FU) and vinorelbine. Reduction in the incidence and occurrence of dermal lesions in a patient is achieved by administration of a cytoprotective agent.

Abstract: Poly(ADP-ribose) polymerase (“PARP”) inhibitors and methods for treating neurodegenerative diseases, neural tissue damage related to cerebral ischemia and reperfusion injury, and cardiovascular in an animal.

Abstract: The invention concerns the use of nicergoline for treating pyramidal spasticity of neurological diseases involving a pathology of the cerebrospinal tract.

Abstract: The present invention provides for methods for the treatment of fibromyalgia syndrome or chronic fatigue syndrome by the administration of heterocyclic amine-type compounds, substituted phenylazacycloalkane-type compounds, or cabergoline-type compounds, or a salt of any said compound.

Abstract: The invention provides a compound of formula I 1

Abstract: A method for the treatment of Restless Leg Syndrome (RLS), which comprises administering an &agr;2-agonist and a second agent selected from the group consisting of the dopamine agonists, opioids, benzodiazepines and the combination of L-DOPA plus a decarboxylase inhibitor.

Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.

Abstract: Methods and formulations for treating female sexual dysfunction are provided. A pharmaceutical composition formulated so as to contain a selected vasoactive agent is administered to the vagina, vulvar area or urethra of the individual undergoing treatment. Suitable vasoactive agents are vasodilators, including naturally occurring prostaglandins, synthetic prostaglandin derivatives, endothelial-derived relaxation factors, vasoactive intestinal polypeptide agonists smooth muscle relaxants leukotriene inhibitors, and other. The formulations are also useful for preventing the occurrence of yeast infections, improving vaginal muscle tone and tissue health, enhancing vaginal lubrication, and minimizing excess collagen deposition. A clitoral drug delivery device is also provided.

Abstract: The invention concerns the use of nicergoline for preventing and/or treating motor neuron diseases.

Abstract: The present invention relates to a method for the prevention or treatment of a motoneuron disease with a combination of an ergoline chosen from nicergoline and lumilysergol and of riluzole or one of its pharmaceutically acceptable salts.

Abstract: The present invention relates to a method for the prevention or treatment of a motoneuron disease with a combination of an ergoline chosen from nicergoline and lumilysergol and of riluzole or one of its pharmaceutically acceptable salts.

Abstract: A method is provided for delaying the onset of ejaculation in an individual. The method preferably involves administration of an antidepressant drug, a serotonin agonist or antagonist, an adrenergic agonist or antagonist, an adrenergic neurone blocker, or a derivative analog thereof, within the context of an effective dosing regimen. The preferred mode of administration is transurethral; however, the selected active agent may also be delivered via intracavernosal injection or using alternative routes. Pharmaceutical formulations and kits are provided as well.

Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes multiple pain and inflammation inhibitory at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for preemptive inhibition of pain and while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents.

Abstract: A method is provided for delaying the onset of ejaculation in an individual. The method preferably involves administration of an antidepressant drug, a serotonin agonist or antagonist, an adrenergic agonist or antagonist, an adrenergic neurone blocker, or a derivative analog thereof, within the context of an effective dosing regimen. The preferred mode of administration is transurethral; however, the selected active agent may also be delivered via intracavernosal injection or using alternative routes. Pharmaceutical formulations and kits are provided as well.

Abstract: The new use of antagonists of the AMPA receptor complex and its physiologically compatible salts as pharmaceutical agents for prevention and treatment of Parkinson's disease as well as pharmaceutical agents, which contain these compounds, is described.

Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.

Abstract: A method of treating sexual dysfunction comprising administering a therapeutically effective amount of a combination of phentolamine and apomorphine, as well as pharmaceutical compositions and kits useful in those methods, are disclosed.

Abstract: The present invention provides for the use of cabergoline and other agents for the treatment of restless legs syndrome (RLS).

Abstract: Disclosed herein is a method of treating an immune system dysfunction in a mammal by administering a prolactin reducer and a prolactin enhancer at a predetermined time or times.

Abstract: This invention relates to a method for inhibiting the growth of neoplasms, in a mammal having a prolactin profile. This method involves comparing the prolactin profile of the afflicted mammal to a standard prolactin profile for healthy mammals of the same species and sex and adjusting the prolactin profile of the afflicted mammal to conform to or approach the standard prolactin profile for a mammal of the same species and sex of the afflicted mammal, thereby inhibiting the neoplastic growth.

Abstract: The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.

Abstract: This invention relates to methods and compositions for the treatment of migraine headache by administering a combination of a) a migraine-treating amount of an ergot alkaloid and b) an antimigraine-potentiating amount of at least one of dextromethorphan or dextrorphan.

Abstract: The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.

Abstract: A method of treating sexual dysfunction comprising administering a therapeutically effective amount of a combination of phentolamine and apomorphine, as well as pharmaceutical compositions and kits useful in those methods, are disclosed.

Abstract: A process for the long term modification and regulation of lipid and carbohydrate metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes)--by administration (i.e., by oral, sublingual or parenternal administration) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of insulin resistant and insulin sensitive members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can be controlled in humans on a long term basis by such treatment inasmuch as the short term daily administration resets hormonal timing in the neural centers of the brain to produce long term effects.

Abstract: Disclosed are dopamine agonist and opioidergic compositions and methods for their use in the treatment of alcoholism. The invention discloses compounds and therapeutic kits useful in the treatment of alcoholics having the A1 allele of the dopamine receptor D2 gene. Also disclosed are methods of treating alcoholics having the A1/A1 or A1/A2 DRD2 genotype comprising administration of dopamine agonists such as aporphines, ergolines, related compounds, and their analogs, in combination with opioidergic compounds such as naloxone.

Abstract: Disclosed are methods for rectifying or ameliorating abnormal responses of mammalian immune systems, such as rheumatoid arthritis. Also disclosed are methods for modifying normal responses of the mammalian immune system. Further disclosed are methods for accomplishing the foregoing by administering to a mammal a prolactin reducer and/or enhancer at a pre-determined time or times during a 24-hour period that results in modification of the mammal's abnormal prolactin profile so that it approaches or conforms to the prolactin profile of a young, healthy mammal of the same species (or to a standard profile generated from such individuals). Additionally, methods of upregulating or augmenting an immune response in a mammal are disclosed.

Abstract: The present invention provides a method for altering mammalian central and peripheral physiological and pathological functioning which is mediated by serotonin binding to the 5-HT.sub.7 receptor. Specifically, the invention provides a method for antagonizing serotonin binding to the 5-HT.sub.7 receptor.

Abstract: Provided are methods for the regulation and modification of lipid and glucose metabolism by administering to a subject a dopamine D1 agonist, optionally in combination with a dopamine D2 agonist, an alpha-1 adrenergic antagonist, an alpha-2 adrenergic agonist, or a serotonergic inhibitor, or optionally in combination with a dopamine D2 agonist coadministered with at least one of alpha-1 adrenergic antagonist, an alpha-2 adrenergic agonist, or a serotonergic inhibitor, and further administering the subject a serotonin 5HT.sub.1b agonist.

Abstract: Disclosed are methods for treating a disorder to the immune system or an immunodeficiency state which comprise the steps of administering to a patient an effective amount of at least one serotonin agonist and at least one dopamine agonist, where the combination of the serotonin agonist and the dopamine agonist are present in an amount effective to treat the patient's condition, where administration of each of the agents is confined to the time of day during which the administration is capable of adjusting the prolactin profile of the patient to conform or to approach the standard human prolactin profile.

Abstract: The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula ##STR1## where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.

Abstract: A process for the long term modification and regulation of lipid and carbohydrate metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes)--by administration (i.e., by oral, sublingual or parenternal administration) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of insulin resistant and insulin sensitive members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can be controlled in humans on a long term basis by such treatment inasmuch as the short term, daily administration resets hormonal timing in the neural centers of the brain to produce long term effects.

Abstract: A therapeutic package for dispensing to, or for use in dispensing to, a vertebrate being treated for a metabolic condition selected from the group consisting of obesity, insulin resistance, hyperinsulinemia, and hyperglycemia comprising one or more unit doses of bromocriptine and labeling directing the use of the package in the treatment of the metabolic condition in a dosage regimen under which the delivery of the bromocriptine is confined to the period during the day near the time of day at which the serum prolactin concentration of a lean, insulin sensitive vertebrate of the same sex is low, and further directing the use of said package in conjunction with the concomitant administration to the vertebrate of one or more unit doses providing a therapeutically effective amount of a prolactin stimulator in a dosage regimen under which the delivery of the prolactin stimulator is confined to the period during the day after the time at which the serum prolactin concentration of a lean, insulin-sensitive vertebrat

Abstract: Methods for detecting abnormalities in prolactin daily rhythms of a subject are provided. Prolactin levels of a subject are compared to levels of healthy subjects and based on the comparison a determination is made of the adjustments necessary to normalize the subject's daily prolactin rhythm. Also provided are methods for normalizing a subject's daily prolactin rhythm.

Abstract: This invention relates to a method for inhibiting the growth of neoplasms, in a mammal having a prolactin profile. This method involves comparing the prolactin profile of the afflicted mammal to a standard prolactin profile for healthy mammals of the same species and sex and adjusting the prolactin profile of the afflicted mammal to conform to or approach the standard prolactin profile for a mammal of the same species and sex of the afflicted mammal, thereby inhibiting the neoplastic growth.

Abstract: A veterinary method for clinically modifying the behavior of a household pet dog exhibiting a recognized type of canine affective aggression behavior is provided. The veterinary behavior modification method administers at least one preferential serotonin reuptake inhibitor compound to the dog upon one or multiple occasions; and the administration of these compounds will modify clinically the canine affective aggression behavior of the household dog permanently or for an indefinite period of time. This veterinary behavior modification method can be usefully employed as an adjunct to conditioning approaches presently employed and will avoid the need for euthanasia in extreme behavioral circumstances.

Abstract: The present invention is directed to an improvement in a method of weight and/or body-fat reduction comprising a (preferably moderate) reduction in the caloric intake of a subject in need of such treatment in combination with administration to said subject of a prolactin inhibitor. Additionally, the present invention is directed to an improvement in a method for altering and/or resetting prolactin profiles (and thereby controlling one or more metabolic disorders such as obesity, excessive body fat, hyperlipidemia, hyperlipoproteinemia, hyperglycemia, hypercholesterolemia, hyperinsulinemia, insulin resistance, glucose intolerance, and Type II diabetes) comprising administration to a subject in need of such treatment of a prolactin inhibitor at a predetermined time or times during a 24-hour period in combination with a (preferably moderate) reduction of the caloric intake of said subject.

Abstract: A process for the long term modification and regulation of lipid and carbohydrate metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes)--by administration (i.e., by oral, sublingual or parenternal administration) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of insulin resistant and insulin sensitive members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can be controlled in humans on a long term basis by such treatment inasmuch as the short term daily administration resets hormonal timing in the neural centers of the brain to produce long term effects.

Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species. The dopamine agonist is administered at the time of.