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7449579 |
Detection of electrophilic and nucleophilic chemical agents
A “real time” method for detecting electrophilic and nucleophilic species generally by employing tunable, precursor sensor materials that mimic the physiological interaction of these agents to...
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB
wherein
X 1 and X 2 are each independently N or C—R″ and R 1 , R 2 ,R 3 , R 4 , R 5 , and R 6 are as defined in...
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7365201 |
Process for the preparation of the boron difluoride chelate of quinolone-3-carboxylic acid
A process for the preparation of the boron difluoride chelate of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-qui
nolone carboxylic acid via:
(a) the reaction of...
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7345174 |
Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula:
wherein each of R 1 and R 2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino,...
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7321039 |
Industrial process for preparing tropenol
The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.
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7297704 |
Cycloalkyfused indole, benzothiophene, benzofuran and idene derivatives
The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central...
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RE39762 |
Polyketide synthase enzymes and recombinant DNA constructs therefor
Polyketide compounds of the formula but not including FK-506, FK-520, 18-hydroxy-FK520 and 18-hydroxy-FK-506.
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7053104 |
Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating...
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7038052 |
Process for the synthesis of derivatives of 2, 3-dihydro-1, 4-dioxino- [2, 3-f] quinoline
Methods of preparing compounds of Formula I
are provided.
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7012142 |
Process for preparation of bicyclic and polycyclic molecules
The present application is directed to a method of synthesis of a bicyclic or polycyclic compound of formula I or formula II:
in which E, G, Y, n, m, R, R 1 , R 2 , R 3 , R 6 , R 7 , R 8 and...
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6962942 |
Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and...
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6939877 |
Antidepressant piperidine derivatives of heterocycle-fused benzodioxans
Compounds of the Formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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6911445 |
Antidepressant cycloalkylamine derivatives of heterocycle-fused benzodioxans
Compounds of the formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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6872718 |
Tricyclic dihydrobenzofuran derivatives, process for the preparation thereof and agents
A compound represented by the formula:
wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is...
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6821981 |
Azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino&lsqb 2,3-f&rsqb -quinoline as 5-HT1A antagonists
Compounds of the formula useful for the treatment of disorders, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite,...
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6800637 |
Antidepressant indolealkyl derivatives of heterocycle-fused benzodioxan methylamines
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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6645983 |
Pharmaceutical compositions comprising 4-quinolones for treating cancers
A non-cytotoxic pharmaceutical composition acting on the proliferation of clonogenic cells in malignant tumors and including an efficient amount of a compound selected among the compounds of...
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6642222 |
Pyrano, piperidino, and thiopyrano compounds and methods of use
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder...
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6635759 |
Luminescent 4-trifluoromethyl 1-2-quinolones with long wave UV absorption and the use thereof
The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum...
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6632418 |
Radioligands and their use for identifying potassium channel modulators
The present invention relates to novel radioligands and test methods using those radioligands in screening compounds.
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6605616 |
Quinoline derivatives
The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is methyl, methoxy, fluoro, chloro, bromo, azido,...
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6599915 |
Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxinol&lsqb 2,3f&rsqb quinoline
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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6579881 |
Indoles
A 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 each represent a methine or a...
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6534653 |
3,5-Dioxa-8-aza-tricyclo&lsqb 5.2.1.00,0&rsqb decane-9-methanols, their metal complexes and enantio-selective hydrogenation processes
Compounds of the formula I, in the form of their racemates, mixtures of stereoisomers or mainly pure stereoisomers in which Y is C 1 -C 4 alkylene or —SiR 1 R 2 —; X is a carbon atom and A 1...
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6492513 |
Method for separating analogous organic compounds
The present invention relates to a method for separating a lactone-containing high-molecular weight compound having an alkyl group as its side chain from a lactone-containing high-molecular weight...
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6462038 |
Androgen receptor modulator compounds and methods
Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions...
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6458802 |
Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-dioxino &lsqb 2,3-f&rsqb quinoline
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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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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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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6376670 |
Quinoline-indole antimicrobial agents, uses and compositions related thereto
The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms, via a non-lytic mechanism. Additionally, the present invention provides...
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6277860 |
Furopyridine antibacterials
This invention provides a compound of formula (I): ##STR1## or pharmaceutically acceptable salts thereof, wherein X 1 and X 2 are C or N, respectively; R 1 and R 2 are independently phenyl...
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6207679 |
Antimicrobial agents uses and compositions related thereto
The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical...
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6184228 |
Anti-sickling agents: selection methods and effective compounds
The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands...
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6051711 |
Synthesis of swainsonine salts
A method for synthesizing swainsonine salts and intermediates thereof comprising subjecting a compound of the formula I ##STR1## wherein R 2 and R 2 ' are the same or different and represent...
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5962465 |
Aminomethyl-2,3,8,9-tetrahydro-7H-1,4-dioxino- 2,3-e!-indol-8-ones and derivatives
The compounds of formula I: ##STR1## wherein R 1 and R 2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R 1 and R 2 , taken together, are benzylidene optionally substituted with R 3 ...
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5922878 |
Amino acid derivatives, processes for preparing them and pharmaceutical compositions containing these compounds
The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein the group R 2 is ##STR2## and R 1 , A, G, Y, Z and m...
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5891878 |
Quinolones and their therapeutic use
1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumour Necrosis Factor activity. The compounds of the invention have the...
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5861412 |
Dihydro-isoquinoline compounds and their use as pharmaceuticals
Compound of general formula I ##STR1## wherein A is a benzo or thieno group; R 1 is (C 4 -6)cycloalkyl, (C 4 -6)cycloalkyl-(C 1 -5)alkyl or ##STR2## R 2 , m, R 3 , R 4 , R and u are defined as...
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5827799 |
Compounds and herbicides containing same as active components
An object of the invention is to provide herbicides which are completely selective to crops such as paddy rice, soybeans and cotton and have an excellent herbicidal activity on weeds. The invention...
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5776943 |
Rapamycin metabolites
This invention provides metabolites of rapamycin, the first of which is 41-O-desmethyl rapamycin, having a deprotonated molecular ion detected at a mass to charge ratio of 899, and a characteristic...
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5731321 |
Endothelin receptor antagonists
Novel compounds of the formula I ##STR1## in which --Y--Z--, R 1 , R 2 , R 3 , R 4 and R 5 have the meanings as stated in the specification, and their salts show endothelin receptor antagonist...
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5710169 |
Therapeutic heterocycles
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , Q 4 , and Q 5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are...
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5708005 |
Quinolines, their production and use
A compound of the formula: ##STR1## wherein R 1 represents hydrogen or an optionally substituted hydrocarbon group; R 2 represents an optionally substituted hydrocarbon group, an optionally...
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5703231 |
Process for making antimicrobial compounds
The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A 1 , A 2 and A 3 are independently carbon or nitrogen and R 1 , R 3 ,...
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5576324 |
Quinoline derivatives or salt thereof and remedy for cardiac diseases containing the same
A quinoline derivative represented by general formula (1), a medicinally acceptable salt thereof, and a remedy for cardiac diseases containing the same: ##STR1## [wherein ring A represents a furan,...
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5498717 |
6,7-dialkoxy-3,4-diydroisoquinolin-8-yl compounds
This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the...
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5484925 |
Synthesis of (-)-swainsonine and intermediate compounds employed in such synthesis
Enamides of the formula: ##STR1## wherein each R 2 when taken independently represents alkoxymethyl or arylmethyl and when taken together represent alkylene bridging the oxygen atoms to which they...
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5446164 |
Process for preparing 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ol
This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the...
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5389638 |
Tetrahydroisoquinolines as alpha-2 antagonists and biogenic amine uptake inhibitors
The present invention provides a tetrahydroisoquinoline compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof which is an antagonist for alpha-2 adrenoreceptors and/or...
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5362736 |
Isoquinoline derivatives
Novel isoquinoline derivatives represented by formula (I): ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are as defined in the specification, have an anti-arrhythmic activity and...
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