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5880286 |
Acetylation of sterically hindered diamines
A process for acetylating diamines having a sterically hindered amino function and a further, sterically unhindered amino function where the acetylation takes place at the sterically unhindered...
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5863903 |
Use of hydroxy alkyl piperidine and pyrrolidine compounds to treat diabetes
The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.
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5861418 |
Aminobenzoic acid derivatives
To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the...
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5840916 |
Quinoline carboxylic acid derivatives having 7-(4-amino-methyl-3-oxime) pyrrolidine substituent and processes for preparing thereof
The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically the present invention relates to a novel quinoline(naphthyridine)carboxylic...
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5827875 |
Inhibitors of microsomal triglyceride transfer protein and method
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the...
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5814656 |
Selective prevention of organ injury is sepsis and shock using selective release of nitric oxide vulnerable organs
A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically...
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5783576 |
Benzoyl guanidine derivatives, the preparation thereof and their use in pharmaceutical compositions
New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
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5777132 |
Process for the manufacture of 2-aryl-5 perfluoroalkylpyrrole derivatives
There is provided a single step procedure to prepare 2-aryl-5-perfluoroalkylpyrrole derivatives directly from the perfluoroacetylated Strecker reaction product. Said pyrrole derivatives are...
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5773459 |
Urea- and thiourea-type compounds
The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with...
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5723681 |
3,3-(disubstituted)cyclohexan-1-01 dimers and related compounds
The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic...
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5723627 |
Preparation of 7-(3-amino- and 3-amino-methyl-1-pyrrolidinyl)-3-quinolonecarboxylic acids and -naphthridonecarboxylic acids
Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce...
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5721255 |
Substituted benzylamino nitrogen containing non-aromatic heterocycles
The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R 1 , R 2 , R 3 and...
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5703244 |
Process for preparation of chiral 3-amino-pyrrolidine and analogous bicyclic compounds
A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and...
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5686482 |
N-(3-pyrrolidinyl) benzamide derivative
N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D 3 and/or D 4 receptor and are useful as a...
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5631381 |
Process for the preparation of pesticidal 1-(haloaryl) heterocyclic compounds
Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts.
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5618949 |
Process for synthesis of chiral cis- and trans-3-amino-4-substituted pyrrolidine compounds
Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas ##STR2## with the...
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5604252 |
Azanorbornane derivatives
The present invention relates to novel azanorbornane derivatives having the formula ##STR1## wherein R 1 through R 12 are defined as below, and to novel intermediates used in their synthesis. The...
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5576446 |
1-amino-2-(substituted)pyrroles and related compounds
There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as...
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5571925 |
Angiotensin II antagonists
This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
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5554633 |
Substituted amines as tachykinin receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR 9 , where R 9 is...
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5543433 |
Azine-substituted phenylacetic acid derivatives and fungicides containing these
Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH 3 ,...
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5521211 |
Substituted 2-arylpyrroles
Novel substituted 2-arylpyrroles of the formula (I) are described ##STR1## in which R 1 , R 2 , R 3 , R 4 , Ar, Y 1 and Y 2 have the meaning given in the description, as is a process for their...
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5506263 |
Benzyl derivatives and pesticides containing them
Benzyl derivatives of the formula I ##STR1## where A is CH 2 , CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy, B is OH, alkylthio, alkoxy or alkylamino, U, V, W are hydrogen, halogen,...
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5506259 |
β-mercapto-propanamide derivatives useful in the treatment of cardiovascular diseases
Compounds of formula ##STR1## wherein R, R 1 , R 2 , Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as...
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5500422 |
Benzamide derivative
A benzamide derivative represented by the following formula: ##STR1## wherein R 1 represents a hydrogen atom or a lower alkanoyl group; R 2 represents a hydrogen atom or a halogen atom; R 3 ...
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5470921 |
Synthetic polyamides and their salts
A synthetic polyamide of formula I and its salts ##STR1## in which each R 1 independently is selected from hydrogen, carboxyl, amino or a group of formula α -A 1 -R 10 ...
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5466828 |
Chiral 3-cyano-1-substituted-pyrrolidines
Chiral 3-cyanopyrrolidines of the following formula are disclosed, wherein R' is as defined herein. The compounds are useful as intermediates for naphthyridine and quinoline antibiotics. ##STR1##
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5459161 |
Process for the preparation of substituted benzofuran derivatives
Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R 1 and R 2 is hydrogen or halogen and the other is, independently, an amino group or a C 2 -C 4 alkanoyl amino...
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5423998 |
Peroxy carboxylic amino-derivatives
Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R 1 , and R 2 , which may be equal to or different from one...
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5424373 |
Oligomeric cyanoguanidines hardeners for epoxy resins
Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R 1 and R 2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy...
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5420164 |
Cycloalkylurea compounds
A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is...
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5413997 |
Triphenylmethane derivatives
A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
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5414082 |
Method for producing 1-unsubstituted 3-aminopyrroles
A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without...
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5378839 |
Insecticidal, acaricidal and molluscicidal 1-(subsituted)thioalkylpyrroles
There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the...
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5366984 |
Methyl α-arylacrylates substituted by a heterocyclic radical and their use
Methyl α-arylacrylates substituted by a heterocyclic radical and having the general formula ##STR1## where R is alkyl, alkenyl, haloalkyl, cycloalkyl, alkoxy, alkylcarbonyl, alkoxycarbonyl,...
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5366997 |
Oxygen substituted derivatives of nucleophile-nitric oxide adducts as nitric oxide donor prodrugs
There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular...
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5359090 |
Alkoxymethylation of pyrroles
There is provided a safe and effective means of introducing an alkoxymethyl group onto the ring Nitrogen atom of a wide variety of pyrrole compounds via the reaction of the appropriate pyrrole...
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5359088 |
Enantiomerically pure aminopyrrolidine compounds
A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are...
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5347017 |
Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents...
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5326911 |
Process for the preparation of ortho-amides
Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formula M 1 OR 1 (III) where the...
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5324728 |
Naphthoic acid derivative
A naphthoic acid derivative represented by the following general formula or a salt thereof: ##STR1## wherein R 1 , R 2 and R 3 are each independently a hydrogen atom, a halogen atom, a hydroxyl...
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5310938 |
Substituted arylpyrrole compounds
This invention relates to methods and compositions for treating, controlling, preventing and protecting warm-blooded animals from infestation and infection by helminths, acarids and arthropod endo-...
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5300508 |
Method for intercepting activated species of dioxygen
A method for intercepting an activated species of dioxygen by administering an N-substituted pyrrole derivative having the formula: ##STR1## in which: R is an amino acid derivative, a non-protein...
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5296494 |
Pyrrolidine compounds having thromboxane A.sub.2 receptor antagonistic activity and thromboxane A.sub.2 synthase inhibiting activity
Compounds of formula (I): ##STR1## wherein R 1 , R 2 , R 3 , m, n, and R are as defined in the Specification. Medicinal products containing the same are useful in the treatment or prevention of...
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5286741 |
N-oxy- and thioalkylcarbonyloxyalkylpyrrole insecticidal, acaricidal and molluscicidal agents
There are provided N-oxy- and thioalkylcarbonyloxyalkylpyrrole compounds of formula I and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods...
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5286743 |
N-aminoalkylcarbonyloxyalkylpyrrole insecticidal acaricidal and molluscicidal agents
There are provided N-aminoalkylcarbonyloxyalkylpyrrole compounds of formula I ##STR1## and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods...
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5262539 |
Process for the preparation of aromatic amines
Electrophilic aromatic compounds can be reacted with sulphenamides in the presence of bases to form the corresponding aromatic amines.
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5256796 |
Method for the preparation of 2-aryl-5-trifluoromethylpyrrole compounds
There is provided a method for the preparation of 2-aryl-5-trifluoromethylpyrrole compounds via the reaction of an appropriate haloenamine and alkyl trifluoroacetoacetate. The pyrrole compounds...
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5252720 |
Metal complexes of water soluble texaphyrins
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5252747 |
Chiral quinolone intermediates
Chiral compounds having the formulae ##STR1## useful in the synthesis of quinolone intermediates.
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