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JP2002518451A |
Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits...
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JP2002518481A |
Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzh...
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JP2002517488A |
The present invention is directed to a process for the preparation of a compound of formula (X-a):or a pharmaceutically acceptable salt form thereof, wherein:R1 is selected from the group consisting of:C1-5 alkyl substituted with 0-5 R1a...
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JP2002161086A |
To provide a zofimarin derivative useful as a medicament (especially, an antimycotic agent), and a pharmacologically acceptable ester or salt thereof.This new compound is a zofimarin drivative of the general formula (I) (wherein, R1 is f...
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JP3286056B2 |
PURPOSE: To obtain a tricyclic condensed heterocyclic derivative, having excellent inhibiting activities against choline esterases and inhibiting actions on uptake of monoamines and useful as a therapeutic and preventing agent for senile...
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JP3283628B2 |
PURPOSE: To obtain a new compound having action to inhibit a squalene synthetic enzyme and antifungal action and useful in treatment for hypercholesterolemia, coronary arteriosclerotic disease, infection of fungi, etc. CONSTITUTION: A co...
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JP2002512637A |
Compounds, compositions containing compounds, methods of sing compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: or a pharmaceutically acceptable base or acid addition salt, hydrate, ester, ...
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JP2002080468A |
To provide a compound useful for preventing or treating hyperlipemia having cholesterol and triglyceride lowering effects.A compound expressed by the formula [I] [wherein, R1 is a 3-carboxypropyl group or a 1-carboxyethyl group, or a (su...
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JP2002504549A |
Disclosed are compounds of formula (I) or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 represents hydrogen, halogen, hydroxy, alkoxy, alkyl, trifluoromethyl...
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JP3242140B2 |
PURPOSE: To obtain a bactericidal compsn. having an improved effect. CONSTITUTION: A new bactericidal compsn. comprising one or more compound(s) selected from specified 6-aryl-2-(2-'-alkynyl)pyridazinones and/or 6-aryl-2-(2'- alkynyl)-4,...
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JP2001354587A |
To provide a method for inhibiting squalene synthetase, capable of readily selecting a compound inhibiting a squalene synthetase and carrying out drug design by utilizing mutual action of hydrophobic property in active center of squalene...
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JP2001524949A |
This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tis...
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JP2001523223A |
Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
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JP3222891B2 |
The present invention provides dibenzoxazepine compounds of Formula I: which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I i...
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JP2001247478A |
To provide a method for treating a female suffering from FSD (female sexual dysfunction), especially FSAD(female sexual arousal disorder).This pharmaceutical composition comprises an agent capable of potentiating cAMP in the sexual genit...
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JP2001247479A |
To provide a method for treating a female suffering from FSD(female sexual dysfunction), especially FSAD(female sexual arousal disorder).This pharmaceutical composition comprises an agent capable of potentiating cAMP in the sexual genita...
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JP2001514253A |
This invention relates to the seven membered at least one nitrogen containing tricyclic heterocyclic pharmaceutically active compounds which bind to integrins, such as the vitronectin receptor and fibrinogen receptor. Such compounds are ...
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JP2001514256A |
The present invention relates to benzoxazepinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical co...
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JP3208140B2 |
A compound of formula or a pharmaceutically acceptable salt form thereof, is useful as a retrovial protease inhibitor for treating HIV infections.
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JP2001513565A |
Compounds of structural formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, a...
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JP3199752B2 |
Compounds of formula (I), (I) wherein R1 and R2 are independently hydrogen, unsubstituted lower alkyl or lower alkyl substituted by lower alkoxy or lower alkyl thio, or acyl which is unsubstituted or substituted by one or more of lower a...
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JP2001511452A |
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 metasta...
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JP2001213802A |
To provide a method for treating a female having FSD(female sexual dysfunction) especially FSAD(female sexual arousal disorder).This method includes delivery of a medicine capable of increasing cAMP(cyclic adenosine monophosphate) at gen...
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JP2001206855A |
To provide a method for treating a female suffering from FSD(female sexual dysfunction), especially FSAD(female sexual arousal disorder). This method comprises delivering a medical agent capable of potentiating cAMP(cyclic adenosine 5'-m...
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JP3192631B2 |
To obtain the subject medicine having an excellent antagonic effect against Substance P and Neurokinin A and good oral absorption by including a saturated heterocyclic compound as an active ingredient. This medicine, which can be used to...
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JP3191943B2 |
PCT No. PCT/KR98/00023 Sec. 371 Date Jul. 21, 1999 Sec. 102(e) Date Jul. 21, 1999 PCT Filed Feb. 4, 1998 PCT Pub. No. WO98/33779 PCT Pub. Date Aug. 6, 1998The present invention relates to a novel 3-amino-1,2-benzoisoxazole derivatives, r...
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JP3188715B2 |
Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, di...
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JP2001509151A |
Macrocyclic compounds of formula (I) are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting comp...
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JP3170292B2 |
A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
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JP2001506606A |
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:wherein X is O or NR<9 >and R<1>-R<4>, R<6>-R<9>, R<11>, R<12>, R, R, R, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or ...
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JP3166782B2 |
PURPOSE: To provide a new compd. for fungicide, especially useful for agricultural fungicide. CONSTITUTION: The compd. represented by formula I (the ring formed with D-NR1-A is dihydropyridazin-3-one, pyridazin-3-one, etc.; R1 is a lower...
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JP3164584B2 |
A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients: wherein, n is an integer of 2 to 5, R<1> indicates a hydrogen atom, halogen atom, C1 to C4 lower alkyl ...
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JP2001504809A |
The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF- alpha converting enzyme (TACE, tumor necrosis f...
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JP2001502668A |
This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin pr...
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JP3136427B2 |
This invention relates to a compound of formula I wherein p is 1 to 3; R<1> and R<2> each are independently hydrogen or an acyl group R<6>CO-, in which R<6> is C1-6 alkyl, C3-7 cycloalkyl, C2-7 alkenyl, aryl or radical of the formula R<3...
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JP2001501951A |
A method for stimulating bone formation by administering integrin binding compounds which cause the release of osteocalcin from osteoblasts is disclosed.
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JP3121355B2 |
The present invention relates to compounds of the formula Orosco wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and...
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JP3112728B2 |
PURPOSE: To provide a production method suitable for synthesizing a large amount of 2,3,4,5-tetrahydro-1,4-benzoxazepine-3,5-dione which is an intermediate for therapeutic agents for psychopathy in good yield under mild conditions. CONST...
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JP2000511882A |
N-formyl hydroxylamines are provided which have structure (I) wherein R and R<1> are as defined herein and A is a dipeptide derived from an amino acid or is a conformationally restricted dipeptide mimic.
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JP3071824B2 |
Immunoassay methods and reagents for the quantification of total doxepins (i.e., E-doxepin, Z-doxepin, E-desmethyldoxepin, and Z-desmethyldoxepin) in a test sample are disclosed. The quantification of total doxepins is accomplished in an...
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JP3072350B2 |
Chromogenic enzyme substrate compounds comprising a dibenz[b,e] [1,4]oxazepinone or dibenzo[b,e][1,4]thiazepinone nucleus having an enzyme-cleavable group such as a radical of a sugar, carboxylic acid, amino acid, peptide, phosphoric aci...
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JP3050844B2 |
To obtain the subject improved serotonin antagonist that has selective 5-HT1 activity and shows only the minimal action on the β-acceptor by using a specific propanolamine type compound or its salt as an active ingredient. This antagoni...
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JP2000502050A |
This invention relates to macrocyclic molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tis...
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JP2000500132A |
There are provided novel compounds of formula (I), wherein X, R<1>, R<2>, R<3>, R<4> and R<5> are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with proc...
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JP2994220B2 |
PURPOSE: To prepare a heterocyclic 7-membered ring ketone useful as a synthetic intermediate for medicines by carrying out the Dieckmann condensing reaction of a 1,8-dicarboxylic acid ester under specific conditions. CONSTITUTION: The co...
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JPH11322728A |
To obtain a heterocyclic compound useful for physiologically active substances such as agrochemicals and drugs under mild conditions with ease in a high yield, by applying an amide compound as a starting substance. An amide compound of f...
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JP2969207B2 |
PURPOSE: To obtain an oxytocin antagonistic agent, comprising benzoheterocyclic compound as an active ingredient and having suppressing actions on matrical smooth muscles, milk release and synthesis and release of prostaglandins, vasodil...
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JPH11511741A |
Compounds having formula (I) wherein R<1>, R<5>, R<6> and R<7> are hydrogen or certain specified substituents; R<8> and R<9> are independently hydrogen, hydroxy or alkoxy; and X, A and B are independently NR<2>, O, S, SO, SO2, CH=CH or (...
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JPH11209356A |
To obtain a new compound, a non-peptidic compound, having excellent somatostatin receptor agonistic action, and useful as a preventive/therapeutic agent for e.g. diabetes. This compound is shown by formula I [A-ring and B-ring are each a...
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JP2905909B2 |
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