Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.

Abstract: A wetness sensing system includes a first wetness sensing article; a first signaling device producing a first signal upon sensing wetness in the first wetness sensing article, wherein the first signaling device is compatible with the first wetness sensing article; and a second signaling device producing a second signal upon sensing wetness in the first wetness sensing article, wherein the second signaling device is compatible with the first wetness sensing article. Also, a method for enhancing a wetness sensing system includes producing a wetness sensing absorbent article compatible with at least one component of the wetness sensing system, wherein the wetness sensing system includes as components a wetness sensing article and a first signaling device compatible with the wetness sensing article.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the invention are directed to the use of said [1,4]-benzodiazepine derivatives in therapy based on the capability of said compounds to interfere with the binding of the peptide hormone, vasopressin, to its receptors. In particular as vasopressin V2 receptor antagonists and therefore useful for treating involving increased vascular resistance, cardiac insufficiency, and water retention.

Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.

Abstract: The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

Abstract: The invention is directed to novel [1,4]benzodiazepine compounds useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising [1,4]benzodiazepine compounds of the present invention 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 relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The invention provides compounds of the formula: wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.

Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.

Abstract: Urea derivatives represented by the following general formula (I): which have an agonism of V2 receptor, are useful as agents for the treatment or prevention of diabetes insipidus, nocturia, nocturnal enuresis, overactive bladder or the like.

Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.

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.

Abstract: Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity.

Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines.

Abstract: Compounds having the formula (I), 1

Abstract: Compounds having the following formula:   are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.

Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N- disubstituted fused-heterocyclo amines.

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: There are provided novel compounds of formula (I) ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.

Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.

Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: Compounds ##STR1## are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention 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 and for improving memory encoding.

Abstract: A multi-functional epoxy resin with good high temperature properties allowing prolonged service at temperatures above 120.degree. C. is derived from a precursor of formula (I): ##STR1## in which R.sup.3 to R.sup.8 inclusive are independently selected from hydrogen, C.sub.1 to C.sub.3 alkyl or halo-alkyl and R.sup.9 is hydrogen, alkyl or halogen, and in which n has the value 0, 1 or 2. The precursor (I) may be self-coupled or cross-coupled with precursors of other epoxy compounds of the TGDDM type. Such cross-coupling gives rise to a complex mixture containing not only the mixed product, but also the self-coupled products of each constituent. Regardless of the precise chemical make-up of the mixture, the observed glass transition temperature is higher than for TGDDM resins formed without precursor (I). If the substituent at the R.sup.9 position is alkyl or halogen, oligomer formation is suppressed and a less complex mixture results.

Abstract: A general method is provided for the synthesis of substituted 2,3-dihydro-5-phenyl-1H-1,4-benzodiazepines by the reaction of bis-trifiated-2,5-dihydroxy benzophenones with 1,2-bisaminoethanes, followed by displacement of the 7-trifloxy group.

Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

Abstract: Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.

Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.

Abstract: Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery.

Abstract: The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.

Abstract: New 2-acylaminomethyl-1H-2,3-dihydro-1,4-benzodiazepine compounds are described having the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl or alkenyl radical or the cyclopropylmethyl radical, R.sub.2 is a hydrogen atom, n is 0, 1 or 2, R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl, pyridyl or phenyl radical, R.sub.4 is an optionally substituted furyl, thienyl or, pyrrolyl radical, R.sub.5 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxyl, lower alkylthio, nitro, trifuloromethyl, cyano, amino, lower mono- or dialkylamino, lower monoalkanoylamino, lower N-alkyl-N-alkanoylamino or lower alkanoyloxy radical, and R.sub.6 is a hydrogen atom, or a lower alkyl or lower alkoxy radical or R.sub.5 and R.sub.6 together denote a methylenedioxy or ethylenedioxy radical. The compounds have pharmacological, for example, analgesic, properties.