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7615638 |
Synthesis of grossularines-1 and analogs thereof and method of use
In one embodiment of the present invention, a synthesis of grossularine-1 and N,N-didesmethylgrossularine-1 2 and analogs thereof based on a novel oxidative dimerization-electrocyclization...
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7550477 |
Inhibitors of checkpoint kinases
The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods...
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7501435 |
Inhibitors of checkpoint kinases
The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory...
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7291627 |
Dihydroimidazo[5.1-a]-beta-carboline derivatives, method for their preparation, and their application as a drug
The invention concerns dihydroimidazo[ 5,1 -a]-β-carboline compounds of general formula (I)
wherein in particular, R 1 , R 2 , R 3 , R 4 , R 6 and R 7 , identical or different, independently...
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7144843 |
Pest controllers
An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention...
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7138408 |
HIV integrase inhibitors, pharmaceutical compositions and methods for their use
Beta-carboline hydroxamic acid compounds represented by formula (I)
are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to...
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7026482 |
Process for preparing imidazoquinolinamines
A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the...
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7001912 |
HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use
Beta-carboline hydroxamic acid compounds represented by formula (I)
are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to...
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6967215 |
Tetrahydrocarbazoles, a process for the preparation of those compounds, and the use thereof
Tetrahydrocarbazoles of formula
where Q is —SO 2 —; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein,...
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6960585 |
Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders,
wherein X, Y 1 , Y 2 , and R 2- 4 are as...
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6927292 |
Tricyclic epoxides
The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation...
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6858620 |
Condensed pyridoindole derivatives
Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed
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6852727 |
Benzimisazo[4,5-f]isoquinolinone derivatives
Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma,...
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6809096 |
Phenanthroline-7-one derivatives and their therapeutic uses
A pharmaceutical composition including an efficient amount of a compound selected among the compounds of formulae (I) and (Ia). The compounds have interesting cytotoxic properties leading to a...
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6747039 |
Aza-benzothiopyranoindazoles with antitumor activity
The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and...
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6720420 |
Photochromic oxazine compounds and methods for their manufacture
The present invention provides oxazine compounds having aromatic, heteroaromatic, or aliphatic substituents at the 2 position of the oxazine moiety. Additionally, a one pot method with excellent...
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6664260 |
Heterocyclic ether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and heterocyclyl or heteroaryl functionality at the 1-position are useful as immune response modifiers. The compounds...
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6586595 |
Process to prepare (5R)-(methylamino)-5, 6-dihydro-4H-imidazo&lsqb 4,5,1-ij&rsqb -quinolin-2(1H)-one
The present invention is an improved prosess to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-
2(1H)-one the compound of formula (VII)
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6562964 |
Heterocyclic compounds as inhibitors of rotamase enzymes
Compounds of the formula (I): wherein A, Y, R, X, R 1 , R 2 , R 3 and R 4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore...
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6541484 |
Pyrazolo-pyridine derivatives as ligands for GABA receptors
A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom...
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6476021 |
Compounds having cGMP-PDE inhibitory effect
Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same;...
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6469021 |
Non-peptide antagonists of GLP-1 receptor and methods of use
Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical...
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6451809 |
Oxo-pyridoimidazole-carboxamides: GABA brain receptor ligands
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof where R 1 -R 4 and A are defined herein, which compounds are highly selective agonists,...
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6384045 |
Tricyclic and tetracyclic pyrones
This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone...
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6355802 |
Process to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo&lsqb 4,5,1-ij&rsqb -quinolin-2(1h)-one
The present invention is an improved prosess to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-
2(1H)-one the compound of formula (VII).
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6353107 |
1-alkoxy-polyallkyl-piperidine derivatives and their use as polymerization regulators
The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G 1 , G 2 , G 3 , G 4 are independently C 1 -C 6 alkyl with the...
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6218400 |
Treatment method using a cGMP-Specific PDE inhibitor
A compound of formula ##STR1## and salts and solvates thereof, wherein R 0 , R 1 , and R 2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor...
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6153645 |
Heterocycles as antimicrobial agents
Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit...
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6127368 |
Anellated β-carbolines
Compounds of formula I ##STR1## are described, as well as the process for their production and their use in pharmaceutical agents.
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6110910 |
Carbocyclic heterocyclic fused-ring quinolinecarboxylic acids useful as immunosuppressive agents
This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such...
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6107304 |
Thieno[2,3-b]pyrazolo[3,4-d]pyridine-3-ones to enhance erythropoiesis
Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also...
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6043373 |
Heterocycle-fused thiazole derivatives
A thiazole compound represented by general formula (I), wherein R is hydrogen atom, a hydroxy group, a straight or branched C 1 -C 6 lower alkyl group, a C 1 -C 4 lower alkoxy group, phenyl...
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5935969 |
Pyrido-thiopyrandoinazoles with antitumor activity
This invention is directed to compounds of formula (I) wherein one of X, Y, Z or T is nitrogen (N--) and the others are CH--; these compounds have been shown to have antitumor activity. ##STR1##
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5908933 |
Certain 4H- 1!benzopyrano 3,4-b!pyridine derivatives and their corresponding 6,7-b! and 7,8-b! ring isomers
The present invention relates to novel coumarin quinolone carboxylic acids wherein the pyridone system is fused in 3,4-, 6,7- and 7,8-positions of the coumarin system, of the general formula I...
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5874441 |
Carbocyclic and hetertocyclic fused-ring quinolinecarboxylic acids useful as immunosuppressive agents
This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such...
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5861411 |
4-Acylaminopyridine derivative
A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for...
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5856107 |
Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein
The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further...
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5807882 |
Anthracene compounds useful in treating certain cancers
A compound of formula (I): ##STR1## in which R 1 , R 2 , X and Y are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or...
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5741908 |
Process for reparing imidazoquinolinamines
A process for preparing 1H-imidazo 4,5-c!quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo 4,5-c!tetrazolo 1,5-a!quinoline with triphenylphosphine and hydrolyzing the...
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5693811 |
Process for preparing tetrahdroimidazoquinolinamines
A process for preparing 6, 7, 8, 9-tetrahydro-1H-imidazo 4,5-c!quinolin-4-amines is disclosed. The process involves the reduction of a 1H-imidazo 4,5-c!quinolin-4-amine or of a 6H-imidazo...
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5622913 |
(2-imidazolin-2-yl) fused heteropyridine compounds intermediates for the preparation of and use of said compounds as herbicidal agents
There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and...
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5604246 |
2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones
This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino...
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5597832 |
Tetracyclic compounds as dopamine agonists
A tetracyclic compound of the formula: ##STR1## wherein A and the atoms to which it is attached and the optional double bond represent a mono- or di-heterocyclic ring selected from: ##STR2##...
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5596097 |
Hetero-annulated indazoles
This invention is directed to heteroannulated indazoles namely to 2,5-disubstituted quinolino-, isoquinolino-, phthalazino-, and quinoxalino- annulated indazole-6(2H)-ones and related mono...
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5585496 |
Catalytic preparation of condensation products of formaldehyde
A process for the catalytical preparation of condensation products of formaldehyde, in which formaldehyde or a formaldehyde-forming compound is caused to undergo reaction using a catalyst which has...
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5585382 |
Polycyclic and heterocyclic chromophores for bis-imide tumoricidals
Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R 1 , R 2 , R 3 , R 9 and R 10 are independently selected from the group H, C 1 -C 4 alkyl,...
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5512564 |
Tricyclic thiazole and oxazole derivatives and pharmaceutical agents containing them
The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be...
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5512590 |
5,6-dihydro-4h-imidazo 2',1':2,3!imidazo- 4,5,1-ij!quinoline and 4,5-dihydroimidazo- 1,2-a!pyrolo 1,2,3-cd!benzimidazole derivatives, their preparation and application in therapeutics
The invention discloses compounds formula (I) ##STR1## in which n represents the number 1 or 2, X represents a hydrogen atom or indicates that the phenyl ring to which it is attached is substituted...
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5508289 |
Bis-acridone chemotherapeutic derivatives
The present invention provides an anticancer compound having the structure: ##STR1## wherein R is --H, --CH 3 , or --C 2 H 5 ; R1 and R2 are independently --H, --OH, --NH 2 , --OCH 3 , --C(CH 3 )...
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5508422 |
Addition products of triazolium salts
A process for the catalytical preparation of condensation products of formaldehyde, in which formaldehyde or a formaldehyde-forming compound is caused to undergo reaction using a catalyst which has...
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