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7605168 |
PDE4B inhibitors
Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and structural information for...
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7531672 |
Preparation of heterocyclic ketones
The present invention relates to a process for preparing heterocyclic ketones of the formulae (I) and (la), by reacting a heterocyclic compound of the formula (II), with an α, β-unsaturated...
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7365061 |
2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor...
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7226942 |
2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor...
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7223786 |
2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor...
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7214704 |
2-Amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor...
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7199148 |
Broadspectrum substituted oxindole sulfonamide HIV protease inhibitors
The present invention concerns the compounds having the formula
N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R 1 and R 8 each are...
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7078535 |
Method for the production of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1h-pyrrolizin-5-ylacetic acid
The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrr
olizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole...
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6936632 |
Fused pyrrole compounds, pharmaceutical agents containing the same, and the use thereof
The present invention relates to fused pyrrole compounds of the formula 1.
in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl.
These compounds are in particular...
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6930190 |
Process for the preparation of heterocyclic pentalene derivatives
A process for preparing heterocyclic pentalene derivative having formula (I): wherein w is a sulfur atom (S), an oxygen atom (O) or a NR or PR group, wherein R is an hydrocarbon group; R 1 , R 2 ,...
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6878738 |
Anti-inflammatory oxo derivatives and hydroxy derivatives of pyrrolizines, and their pharmaceutical use
The present invention relates to compounds of the formula I
in which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8...
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6559319 |
Synthesis of compounds useful in the manufacture of ketorolac
A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound...
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6548532 |
Indolecarboxylic compounds for treating seborrhea and complications thereof
Indolecarboxylic acid compounds and derivatives thereof are useful for treating seboarhea and the dermatitides associated therewith, especially acne and/or blackheads and/or comedones.
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6541507 |
Indolecarboxylic compounds for inducing/stimulating hair growth and/or retarding hair loss
Indolecarboxylic acid compounds and derivatives thereof, notably 4,6-dimethoxyindole-2-carboxylic acid and derivatives thereof, are especially useful for inducing/stimulating mammalian hair growth...
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6448243 |
1,4-substituted cyclic amine derivatives
A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or...
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6433199 |
Quinone derivatives
The invention relates to a quinone derivative of the following formula: which is capable of converting into two alkylating agents upon bioreduction. Substituents A, B, C, and D are as described...
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6417371 |
Process for preparing 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl-acetic acid
The present invention relates to a process process for the preparation of the compound of the formula I where the compound of the formula III is reacted with oxalyl chloride and the product...
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6395766 |
Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition
Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl,...
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6391917 |
Dialkyl ureas as calcitonin mimetics
Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of...
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6323344 |
Preparation of ketorolac
5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula ##STR1## where R 1 is alkyl and R 2 is optionally substituted phenyl; and the method for their preparation and their conversion...
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6218419 |
Aminoiminoquinone and aminoquinone alkaloid compounds and methods of use
The subject application concerns novel compounds with useful biological properties. For example, these compounds can be used as antinflammatory, anti-proliferative, immunomodulatory, and/or...
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5969133 |
Bioreductive cytotoxic agents
A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive...
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5958943 |
A!-anellated pyrrole derivatives and their use in pharmacology
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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5952316 |
2-amino-1,3-propanediol compound and immunosuppressant
2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted...
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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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5925770 |
Certain fused pyrrolecarboxanilides; a new class of gaba brain receptor ligands
The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted...
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5684160 |
3-aminopyrroles, methods for their synthesis and for their pharmaceutical use
The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive...
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5580888 |
Styryl derivatives as anti-inflammatory agents
Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR 1 , wherein R 1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R 6 )--,...
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5543423 |
Amino acid derivatives with improved multi-drug resistance activity
The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical...
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5523306 |
Amino acid derivatives cyclized at the C-terminal
Novel α-substituted Trp dipeptoid derivatives cyclized at the C-terminal useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as...
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5516784 |
Anti-HIV (AIDS) agents
Compounds of formula ##STR1## wherein Ar, W, Z, Q, R 1 , U, and T are as set forth herein, are described. These compounds are active as agents against retroviruses and in particular against HIV.
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5484944 |
Certain fused pyrrolecarboxanilides and their use as GABA brain receptor ligands
The present invention encompasses structures of the formula I: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or...
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5482942 |
(3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants
This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to...
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RE34918 |
Azaazulene compounds which are useful as antiallergic and antiinflammatory agents
An azaazulene derivative having the general formula (I): ##STR1## wherein R 1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond...
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5354891 |
Method of producing aromatic amine derivatives
Disclosed is a method for producing aromatic amine derivatives in a high yield at a low price, which comprises inducing an aromatic hydroxamic acid derivative to undergo a rearrangement reaction...
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5017213 |
1-phenylpyrroles
Herbicidal 1-phenylpyrroles of the formula ##STR1## wherein each R 1 represents methyl or together form a tetramethylene group, R 2 represents hydrogen, C 1 -6 alkyl, cyclopropylmethyl, C 1 -4...
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4853149 |
Heterocyclic liquid crystal compounds
Heterocyclic liquid crystal compounds containing the structural element ##STR1## wherein M is H, CN,, NCS, halogen or an alkyl group with 1-5 C atoms, X is CR 4 or N, Y is CHR 4 , O, S or NR...
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4737519 |
Substituted naphthalenes, indoles, benzofurans, and benzothiophenes as lipoxygenase inhibitors
The present invention provides certain novel substituted naphthalenes, indoles, benzofurans, and benzothiophenes of Formula I which are useful as inhibitors of leukotriene biosynthesis and as...
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4736043 |
Process for the preparation of indole derivatives
The present invention provides a process for the preparation of 4-hydroxyindole derivatives of the general formula: ##STR1## in which R 1 is a hydrogen atom or an alkyl radical containing up to 6...
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4666934 |
Prostaglandin analogs
The compound 6,9-deepoxy-6,9-(phenylimino)-Δ 6 ,8 -prostaglandin I 1 , potassium salt and compositions thereof.
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4521606 |
5-Indolyl substituted aminoethanols
Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and...
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4496742 |
Analogs of 5,6-dihydro PGI.sub.2
Novel structural analogues of 5,6-dihydro PGI 2 of the formula: ##STR1## and the corresponding 10,11-didehydro-11-deoxy derivatives are useful as antiallergy agents.
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4442291 |
1,2,3,4,4a,7-Hexahydro-6,8-dimethoxy-2-methyl isoquinoline
The present invention is directed to a compound having the formula ##STR1## which is used as an intermediate in the preparation of octahydro-1H-pyrrolo[2,3-g]isoquinolines.
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4383112 |
Chiral amino-alcohol complexes
Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C * is an asymmetric carbon atom, R 1 and R 2 , which may be the same or different...
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4344943 |
6-Chloro- or 6-bromo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids and derivatives thereof
Novel 5-aroyl-6-chloro- or 6-bromo-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-7-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts...
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4336202 |
1,3-Cyclohexanedione derivatives
Novel cyclohexanone derivatives of general formula: ##STR1## (wherein R 1 is a hydrocarbon group of 1 to 15 carbon atoms) and new cyclohexanone derivatives of general formula: ##STR2## (wherein R...
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4316850 |
Tertiary aminoacids
New α-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.
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4294759 |
Structural analogues of 5,6,-dihydro PG.sub.1
Novel structural analogues of 5,6-dihydro PGI 1 of the formula: ##STR1## useful as antiallergy agents.
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4260762 |
Octahydro-1H-pyrrolo[2,3-g]isoquinolines
Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 and X are as hereinafter set forth, are described.
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4087539 |
5-(2-Furoyl)-, 5-(2-thenoyl)-, 5-(3-furoyl)- and 5-(3-thenoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid derivatives and process for the production thereof
Novel 5-substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxy
lic acid compounds represented by the formulas ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof,...
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