Abstract: By using a bioluminescence, a method for detection of a monovalent cation is provided and the method is a high sensitive and simple method. According to the present invention, an amino acid sequence of symplectin and a base sequence encoding the protein are provided. Symplectin is a photoprotein derived from Symplectoteuthis oualaniensis (okinawan squid). By using the photoprotein of the present invention, a monovalant cation can be detected by luminescence in the presence of a chromophore.

Abstract: This invention provides compounds of formula I, 1

Abstract: Novel fused indazoles and indoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.

Abstract: Chemical compounds of formula (I): 1

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

Abstract: Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.

Abstract: Compounds having the formula (I), 1

Abstract: Chemical compounds of formula (I): 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention is directed to compounds of the wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.

Abstract: 1,4,7,10-Tetraazacyclodecane, a precursor for the synthesis of macrocylic chelating agents for metal ions such as gadolinium, is prepared efficiently as a highly pure product on an industrial scale.

Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

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

Abstract: A compound of the formula 1

Abstract: The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R4b, R5, R6, R7, R8, R9, n, and X are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep and sexual disorders, migraine and other conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1] or polycyclic azaamide nucleus. Pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The invention relates to compound of formula (I): 1

Abstract: This invention concerns compounds of formula 1

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

Abstract: This application is directed to a compound of Formula I wherein a, X, R1, R2, R3 and R4 are as defined herein, useful in the treatment of respiratory, allergic, rheumatoid, body weight regulation, inflammatory and central nervous system disorders such as asthma, chronic obstructive pulmonary disease, adult respiratory diseases syndrome, shock, fibrosis, pulmonary hypersensitivity, allergic rhinitis, atopic dermatitis, psoriasis, weight control, rheumatoid arthritis, cachexia, Crohn's disease, ulcerative colitis, arthritic conditions and other inflammatory diseases, depression, multi-infarct dementia and AIDS.

Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C.

Abstract: Methods are provided for making Anagrelide base from 2,3-dichlorobenzaldehyde. A method is also provided for making an intermediate compound ethyl N-(2,3-dichloro-6-nitrobenzyl)glycine from 2,3-dichlorobenzaldehyde and for reducing the glycine compound using either SnCl2 or a specially defined catalyst. A cyclization method to form Anagrelide base from the corresponding iminoquinazoline compound is further provided.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein.

Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.

Abstract: Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such as bronchial asthma and atopic dermatitis; therapeutic agents for inflammatory diseases such as chronic rheumatoid arthritis; therapeutic agents for autoimmune diseases such as ulcerative colitis and nephritis; and as anti-AIDS drugs.

Abstract: Novel compounds of the following general formula or salts thereof. wherein Ring M is a heterocyclic ring having —N═C<, —CO—N< or —CS—N< as the partial structure —X{overscore (— — — — — — — — —)} Y<; Ra and Rb are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Abstract: The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): 1

Abstract: The invention relates to the use of pyrido[3,2-e]-pyrazinones of formula 1 as inhibitors of phosphodiesterase 5 for the treatment of erectile dysfunction (impotence).

Abstract: Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke.

Abstract: By using a bioluminescence, a method for detection of a monovalent cation is provided and the method is a high sensitive and simple method. According to the present invention, an amino acid sequence of symplectin and a base sequence encoding the protein are provided. Symplectin is a photoprotein derived from Symplectoteuthis oualaniensis (okinawan squid). By using the photoprotein of the present invention, a monovalant cation can be detected by luminescence in the presence of a chromophore.

Abstract: The compound of the formula (I): wherein all the symbols are meaning the same as descriptions of the specification; and salts thereof. The compounds of the formula (I) have inhibitory activity of adhesion molecules expression, and are useful for prevention and/or treatment of inflammation, rheumatoid arthritis, allergies, asthma, atopic dermatitis, psoriasis, suppression of ischemia reperfusion injury, nephritis, hepatitis, multiple sclerosis, ulcerative colitis, adult respiratory distress syndrome (ARDS), suppression of transplant rejection, sepsis, diabetes, autoimmune diseases, tumor metastasis, arteriosclerosis and AIDS.

Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.

Abstract: The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering a growth hormone secretagogue, a prodrug thereof or a pharmaceutically acceptable salt of said secretagogue or said prodrug.

Abstract: The present invention provides a compound of formula I 1

Abstract: Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.

Abstract: A compound of the formula 1

Abstract: This invention provides compounds of formula I, 1

Abstract: This invention encompasses compounds of the formula: and the pharmaceutically acceptable non-toxic salts thereof wherein R1, R2, R3, R4, X, and W are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: Tricyclic compound of the formula: wherein ring A is a nitrogen-containing heterocyclic ring, having two nitrogen atoms as the hetero-atoms, which is optionally substituted with oxo or thioxo; ring Q may optionally be substituted; Y is an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted mecapto group, excluding for methyl group as Y; R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof, having excellent PDGF-inhibiting activities, antihypertensive activities, activities of ameliorating renal diseases and activities of lowering lipid level.

Abstract: A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative bacteria including &bgr;-lactamase producing bacteria. In particular, it has higher antimicrobial activity against methicilline-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and imipenem-resistant Pseudomonas aeruginosa than the existing onium salt type cephem derivatives and hence is very useful as a therapeutic agent for infectious diseases derived from various pathogenic bacteria. wherein X represents CH or N, R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or cycloalkyl; any one of R2, R3, R4, and R5 represents R6R7NSO2NH—C1-6 alkyl where R6 and R7, which may be the same or different, represent a hydrogen atom or C1-6 alkyl; and n is 0 or 1.

Abstract: Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.

Abstract: Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.

Abstract: Imidazo[1,2-a]quinoxalin-4-amines derivatives of formula (I) ##STR1## are described, and salt thereof active as adenosine antagonists and a process for their preparation and pharmaceutical compositions containing them as therapeutically active compounds for psychiatric and neurological disorders of the central nervous system.

Abstract: Imidazoloquinoxalinones of the formula ##STR1## where R.sup.1 -R.sup.5, A and B have the meanings stated in the description, and their preparation are described. The novel substances are suitable for controlling diseases.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders are disclosed.

Abstract: The present invention relates to [1,2,4]triazolo[4,3-a]quinoxalinone compounds of the formula ##STR1## wherein R.sup.1 is POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.7 is trifluoromethyl, and R.sup.6, R.sup.8 and R.sup.9 independently are piperidino, piperazinyl, morpholino, or thiomorpholino, which rings are optionally substituted with one or more of phenyl or C.sub.1-6 -alkyl and phenyl optionally being substituted with C.sub.1-6 -alkoxy; and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Novel heterocyclo-substituted imidazopyrazines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.