Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract: Formula (I) compounds with atypical antipsychotic activity where the meanings of the various groups are as described here below, are endowed with activity characteristic of atypical antipsychotic agents, and therefore are useful as medicaments, particularly for the treatment of schizophrenia, paranoid states, manic-depressive states, affective disorders, social regression, personality regression and hallucinations.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia and dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis wherein A is chosen from B is chosen from wherein the variables R1 to R7, m, n, are as defined herein. A method for treating the above diseases employing the above compounds is also provided.

Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

Abstract: Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.

Abstract: Quinolone carboxylic acid derivatives of formula (I) and pharmaceutically acceptable salts thereof have potent antibacterial activity: wherein, R1 is a C1-4 alkyl group, or phenyl or C3-6 cycloalkyl group optionally substituted with one or more halogens; R2 is H, amino or C1-4 alkyl group; R3 is H, C1-4 alkyl group, or amino, aminomethyl or aminoethyl group optionally substituted with one C1-4 alkyl radical; W is N, CH or CY (Y is halogen, or C1-4 alkyl or C1-4 alkoxy group optionally substituted with one or more halogens); and Pyr represents 2-, 3- or 4-pyridyl group, provided that when W is C, W and R1 are fused together to form COCH2CH(CH3), CCH2CH2CH(CH3), or CSCH2CH(CH3).

Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: The present invention provides plant extracts, isolated alkaloids, synthetic alkaloids and compositions having antitussive activity. In some preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of a genus in the family Stemonaceae. In other preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of the genus Stemona, Croomia, or Stichoneuron. In especially preferred embodiments, the plant extracts and the isolated alkaloids are from the plant Stemona tuberosa. The present invention further provides methods for isolating such plant extracts and alkaloids. In addition, the present invention provides methods for reducing or suppressing coughing by administering plant extracts, alkaloids and compositions having antitussive activity.

Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.

Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.

Abstract: A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.

Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.

Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Abstract: The present invention provides plant extracts, isolated alkaloids, synthetic alkaloids and compositions having antitussive activity. In some preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of a genus in the family Stemonaceae. In other preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of the genus Stemona, Croomia, or Stichoneuron. In especially preferred embodiments, the plant extracts and the isolated alkaloids are from the plant Stemona tuberosa. The present invention further provides methods for isolating such plant extracts and alkaloids. In addition, the present invention provides methods for reducing or suppressing coughing by administering plant extracts, alkaloids and compositions having antitussive activity.

Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salt, solvate and ester thereof, wherein R1 to R4 and n are as defined in the specification. A compound of formula 1 is useful as a pharmaceutical composition for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

Abstract: Novel compounds of formula (I): wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.

Abstract: Compounds of the formula I: 1

Abstract: The present invention provides compounds of formula (I): 1

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides pharmaceutically active compounds of formula I as described herein useful for the treatment of diseases or disorders of the central nervous system.

Abstract: The present invention is a chemical compound of formula (I) 1

Abstract: The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone- 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 1

Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: Benzoazepines of the following formula wherein R1, R1a, R2, R9k, L, Q, X, Y and Z are as described herein, and analogs thereof are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

Abstract: Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.

Abstract: 1

Abstract: A pyridine alcohol derivative represented by General Formula III 1

Abstract: Novel compounds of formula (I): 1

Abstract: The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.

Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.

Abstract: Tricyclic pyridin-2-one analogues which are ligands for GABA.sub.

Abstract: A compound of the formula ##STR1## wherein a, V, X, Y, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, useful in (a) the treatment of myelosuppression including suppression associated with cancer chemotherapy as well as activation of the immune system for the treatment of cancer or (b) prevention and treatment of viral, fungal, bacterial and parasitic infectious diseases.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: The present invention discloses compounds of the formula, or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereofwhereinX and Y together forms .dbd.O, .dbd.S, .dbd.NOR.sup.2, .dbd.CR.sup.3 R.sup.4, .dbd.N--CN, .dbd.N--NR.sup.7 R.sup.8, --(CH.sub.2).sub.m --, or--W'--(CH.sub.2).sub.p --W"--, or one of X and Y is hydrogen and the other is --OR.sup.5, --SR.sup.5, or --NR.sup.5 R.sup.6Z is hydrogen, --COOR.sup.9 ;R.sup.3 and R.sup.4 are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, aryl, arylalkyl, or --(CH.sub.2).sub.q --COOR.sup.2 ;R.sup.2, R.sup.5 and R.sup.6 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, --CO-alkyl, or --SO.sub.2 -alkyl;R.sup.7 and R.sup.8 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl;R.sup.9 is alkyl, alkenyl or alkynyl;R.sup.

Abstract: A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y.sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO-- or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.

Abstract: Compounds based on the benzoxazine ring system are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.

Abstract: Compounds of formula I ##STR1## wherein X is N or C--R.sup.9, Y is N--R.sup.10, CH.sub.2, O, S, SO, SO.sub.2, C.dbd.O or CH--OH,R is H or alkyl,R.sup.1 is heteroaryl,n is 1-5, andR.sup.2 -R.sup.10 are H or various substituents,are useful as inhibitors of protein farnesyl transferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.