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6342633 |
O-benzyl oxime ether derivatives and their use as pesticides
Compounds of the formula I in which Y is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, OH, CN, NO 2 , Si(CH 3 ) 3 , CF 3 or halogen, Z is a group a) R 1 is hydrogen, C 1 -C 4 alkyl, C 2 -C 4...
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6323227 |
Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
This invention relates to compounds of formula ##STR1## which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of...
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6320045 |
Process for the reduction of oxiranyl epothilones to olefinic epothilones
The invention as claimed is directed to a process for making an epothilone having the following structures ##STR1## from ones having an oxiranyl moiety, by reacting a compound having the latter...
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6300353 |
Azoles for treatment of fungal infections
Azole derivatives of the formula I ##STR1## wherein R 14 , R 15 are each independently hydrogen or fluorine, T is a group of the formula: ##STR2## wherein R 9 is pyrrolidinyl or a group...
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6277849 |
N-sulphonyl and N-sulphinyl amino acid amides as microbiocides
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and ...
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6271179 |
Benzylidene pyrazolones, production and use thereof
Benzylidenepyrazolones of the formula I, ##STR1## Useful as herbicides.
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6262094 |
C-21 modified epothilones
The invention is concerned with epothilones in which the thiazole substituent has been modified, with methods for their preparation and with antifungal or therapeutic agents which contain these...
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6251926 |
Oxyiminoalkanoic acid derivatives with hypoglycemic and hypolipidemic activity
This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia,...
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6245790 |
Oxazole compounds useful as PGE2 agonists and antagonists
Azole compounds of the formula: ##STR1## wherein R 1 is lower alkyl substituted with carboxy, etc., R 2 is hydrogen or lower alkyl, R 3 is aryl, etc. R 4 is aryl, etc. Q is ##STR2##...
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6239104 |
Isolation and structural elucidation of the cytostatic linear and cyclo-depsipeptides dolastatin 16, dolastatin 17, and dolastatin 18
Cytostatic linear and cyclo-depsipeptides, "Dolastatin 16", "Dolastatin 18", and "Dolastatin 17", are disclosed which are obtained from Indian Ocean shelless mollusk Dolabella auricularia. Methods...
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6211240 |
O-benzyl oxime ether derivatives and their use as pesticides
Compounds of the formula I ##STR1## in which Y is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, OH, CN, NO 2 , Si(CH 3 ) 3 , CF 3 or halogen, Z is a group a) ##STR2## R 1 is hydrogen, C...
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6197802 |
Fungicidal melithiazole derivatives
Compounds of formula (I), wherein R 1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, alkyloxiranyl, alkanoyl, alkoxycarbonyl, formyl, hydroxyalkyl, alkoxyalkyl,...
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6194448 |
N, N-disubstituted amides that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding;...
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6166051 |
Thiol derivatives with metallopeptidase (ACE/NEP) inhibitory activity
Compounds of formula (I) wherein R, R 1 , R 2 , R 3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active...
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6166023 |
1,5- and 3-O-substituted 1H-indazoles having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments
The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##
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6166004 |
Combinations of HIV protease inhibitors with reverse transcriptase inhibitors
There are described compounds of formula I*, ##STR1## wherein R 1 is lower alkoxycarbonyl, R 2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R 3 is phenyl that is...
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6165944 |
4-(3-heterocyclyl-1-benzoyl) pyrazoles and their use as herbicides
4-(3-Heterocyclyl-1-benzoyl)pyrazoles of the formula I ##STR1## where: R 1 and R 3 are each hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio,...
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6162823 |
LTA.sub.4 hydrolase inhibitors
The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory...
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6160122 |
Process for the preparation of a disubstituted thiazole
A process is disclosed for the preparation of N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)carbon
yl)-amino acid derivatives.
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6156776 |
Diaryl substituted thiazoles useful in the treatment of fungal infections
Disclosed is a novel class of thiazole, thiadiazole, and oxadiazole compounds which are substituted at their nuclear carbons by aromatic moieties. These compounds exhibit antifungal activity...
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6156905 |
Deoxy epothilones and intermediates utilized in the process for preparing epothilones
The invention relates to a process for the production of epothilones and intermediate products within the process. Epothilones A and B are natural substances, which can be produced by...
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6143696 |
Substituted 4-(3-alkenylbenzoyl)pyrazoles
4-(3-Alkenylbenzoyl)pyrazoles of the formula I ##STR1## and agriculturally useful salts thereof; processes for preparing the compounds of the formula I; compositions comprising them; and the use of...
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6140330 |
Thiazole derivative
A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R 1 and R 2 are the same or different and are each H, or lower alkyl, etc.; R 3 is ##STR2## R 4 is H or...
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6140272 |
Substituted 4-benzoyl-pyrazoles
4-Benzoylpyrazoles of the formula I where: A is a group of the formula IIIa, IIIb or IV ##STR1## Q is a pyrazole of the formula II, ##STR2## useful as herbicides.
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6096898 |
One pot synthesis of 1,2,4-triazoles
One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.
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6077864 |
Cyclic sulfone derivatives
A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration,...
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6069162 |
Indolyl and benzofuranyl carboxamides as inhibitors of nitric oxide production
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6048883 |
Heterocyclic compounds as pharmaceutical
This invention provides compounds of formula (I): A 1 --X--(CH 2 ) n --O--A 2 --A 3 --Y.R 2 (I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a...
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6046137 |
Herbicidal heterocyclically substituted benzoylisothiazoles
4-Benzoylisothiazoles of the general formula 1 ##STR1## where the substituents have the following meanings: X is oxygen or sulfur; R 3 is a radical of the general formula 2 ##STR2## where Z and...
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6043282 |
Azinooximethers, processes and intermediate products for manufacturing same, and the uses thereof in combating harmful fungi and pests
Azinooxime ethers of the formula I ##STR1## (X=NOCH 3 , CHOCH 3 , CHCH 3 ; Y=O, NZ, where Z=H, alkyl; R 1 =H, alkyl; R 2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it...
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6043263 |
(2,3-dihydrobenzofuranyl)-thiazoles as phosphodiesterase inhibitors
The invention relates to compounds of the formula (I), wherein R1, R2, R3, R4, R5 and n have the meanings cited in the description said compounds being new effective bronchial therapeutic agents.
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6037365 |
Aminobenzamidinosuccinyl lactone derivatives useful as inhibitors of platelet aggregation
This invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of...
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6037367 |
Substituted-pent-4-ynoic acids
Compounds of formula (I) wherein: R 1 is --(CR 4 R 5 ) n C(O)O(CR 4 R 5 ) m R 6 , --(CR 4 R 5 ) n C(O)NR 4 (CR 4 R 5 ) m R 6 , (CR 4 R 5 ) n O(CR 4 R 5 ) m R 6 , or --(CR 4 R 5 ) r ...
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6020495 |
Stereoselective method for synthesizing dolaphenine
The present invention relates to a method for the stereospecific synthesis of an enantiomer of a chiral amine, wherein the chiral amine has the formula R 1 CH(NH 2 )R 2 . R 1 and R 2 are each...
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6013811 |
Preparation process of benzodifuranone dyes
A process for the preparation of a polycyclic dye of Formula (1) which comprises steps: i) reaction of a compound of formula (2) with a compound of formula (3) or a derivative thereof to form an...
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6007865 |
Reversing the formation of advanced glycosylation endproducts
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent...
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6004988 |
Carboxylic acid derivatives, their preparation and their use
Carboxylic acid derivatives of the formula I ##STR1## here R 1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the...
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5994539 |
Mercapto acyl aminoacid derivatives endowed with dual ACE-NEP inhibitory activity, useful in the treatment of cardiovascular diseases
Compounds of formula ##STR1## wherein R, R 1 , R 2 , R 3 , R 4 , m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain...
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5981559 |
Azole derivative with leukotriene (LTs) antagonizing activity and thromboxane (TX) A.sub.2 antagonizing activity
An azole derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having both of a leukotriene antagonistic effect and a thromboxane A2 antagonistic effect and...
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5977149 |
Dihydrotriazole compounds and their use for controlling fungal plant diseases
Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR 5 ;or CR 14 --, G is C or N; W is O or S; X is OR 1 , S(O) m R 1 or halogen; R 1 , R 2 , and R 5 are...
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5969145 |
Process for the production of epothilones and intermediate products within the process
The invention relates to a process for the production of epothilones and intermediate products within the process. Epothilones A and B are natural substances, which can be produced by...
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5965741 |
Ortho-substituted aromatic ether compounds and their use in pharmaceutical compositions for pain relief
The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R 1 , and R 3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof,...
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5962686 |
N-benzylazolium derivatives
N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;...
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5948779 |
Substituted condensation products of n-benzyl-3-indenyl acetamides with heterocyclic aldehydes
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell...
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5942535 |
a!-Annelated pyrrole derivatives and pharmaceutical use thereof
The present invention relates to heterocyclic compounds of the formula ##STR1## in which R 1 -R 7 , B, a and X have the meanings recited in the specification. These compounds are usable in the...
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5932606 |
Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors
A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as ##STR1## which are useful for inhibiting formation of blood...
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5929248 |
Substituted heteroarylphenyloxazolidinones
The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and...
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5925631 |
Alkylated styrenes as prodrugs to COX-2 inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions...
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5892033 |
Metallic chelating dye
Disclosed is a metal chelate dye which is composed of a metal ion and a ligand that is a methine dye having 2 or more bonding positions capable of coordinate bond to the metal ion at the bonding...
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