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7622478 |
1-nitroacridine/tumor inhibitor compositions
The invention is directed to 1-nitroacridine derivative(s)/tumor inhibitor(s) compositions as well as methods for using said compositions for inhibiting or preventing tumor growth, particularly,...
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7511064 |
Derivatives of 4-(thio- or selenoxanthene-9-ylidene)-piperidine or acridine and its use as a selective 5-HT2B receptor antagonist
The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament...
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7423046 |
3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
Compounds of formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meaning indicated in the description, are novel effective PDE4 inhibitors.
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7388017 |
Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds,...
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7354928 |
Small molecule inhibitors targeted at Bcl-2
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X L . In particular, the present invention provides non-peptide cell permeable small...
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7312209 |
Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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7312082 |
Crystal structure of G-quadruplex containing a potassium ion
The present invention relates to a crystal structure of G-quadruplexes and its use. The invention provides a crystal of an intramolecular G-quadruplex structure having a hexagonal space group P6,...
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7300930 |
Therapeutic acridone and acridine compounds
The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond...
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7141581 |
Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating...
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7094378 |
Method and apparatus for inactivation of biological contaminants using photosensitizers
Methods and apparatuses for treating fluids to inactivate microorganisms which may be present therein, said fluid containing one or more components selected from the group consisting of protein,...
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7084106 |
Application of a viral complement inhibitory protein in the treatment and diagnosis of Alzheimer's Disease
The present invention provides a novel treatment for senile dementia (Alzheimer's Type), comprising administering an anti-complement protein to a patient in need of such treatment in an amount...
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7041674 |
Carbamic acid esters with anticholinergic activity
A compound of formula 1
wherein X − , A, R 1 , R 2 , R 3 , and R 4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in...
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7030133 |
Inhibitors of formation of advanced glycation endproducts (AGEs)
The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is...
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7030132 |
Method of improving bioavailability of orally administered drugs, a method of screening for enhancers of such bioavailability and novel pharmaceutical compositions for oral delivery of drugs
A method for increasing the systemic exposure of cells selected from tumor cells and normal cells to an orally administered pharmaceutically active compound, wherein a bioenhancer comprising an...
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6998405 |
Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use
Compounds of the general formula I
wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings...
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6974821 |
Methods for treating neuropsychiatric disorders
The invention provides methods for treating neuropsychiatric disorders such as schizophrenia, Alzheimer's Disease, autism, depression, benign forgetfulness, childhood learning disorders, closed...
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6956043 |
Pharmaceutical compositions comprising 33-epi-chloro-33-desoxy-ascomycin solid dispersions
A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.
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6906081 |
Use of dual H3/M2 antagonists in the treatment of cognition deficit disorders
This invention relates to a method of treating cognition deficit disorders comprising administering to a mammal in need of such treatment an effective amount of a dual histamine H 3 receptor...
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6884802 |
6-heteroarylphenanthridines
Compounds of formula 1, in which Het is an unsubstituted or R6- and/or R7-substituted pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl,...
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6867197 |
Method of targeting conjugate molecules to mitochondria
The present invention relates to genetic mutations in mitochondrial cytochrome c oxidase genes that segregate with Alzheimer's disease (AD). The invention provides methods for detecting such...
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6831086 |
Process for the inactivation of viruses with the aid of acridine derivatives
The invention relates to the use of acridine or acridine derivatives, preferably in combination with benzalkonium chloride, for the inactivation of enveloped or nonenveloped viruses. The process...
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6821983 |
5-(9-acridinylamino)-toluidine compounds
This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.
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6803373 |
Method, compositions and kits for increasing the oral bioavailability of pharmaceutical agents
A combination of 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7
,-dimethoxy-2-isoquinolinyl)ethyl]pheny]-4-acridinecarboxami
de or a salt thereof and paclitaxel and its analogs or...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6683087 |
Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use
Compounds of the general formula I and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical...
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6680282 |
4-Quinolinol derivatives and agrohorticultural bactericides containing the same as active ingredient
A new agricultural and horticultural fungicide having an excellent control effect is provided. 4-Quinolinol derivatives represented by the following formula: or agriculturally and...
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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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6630481 |
Viologen linked acridine based molecule and process for the preparation thereof
The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or...
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6599535 |
Pharmaceutical compositions
A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.
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6589961 |
9-alkylamino-1-nitroacridine derivatives
The invention is directed to novel 9-hydroxyalkylamino-, 9-alkoxyalkylamino-1-nitroacridine derivatives. Methods of preparation, pharmaceutical compositions comprising said derivatives and their...
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6541483 |
Acridone-derived compounds useful as antineoplastic and antiretroviral agents
The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as...
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6521635 |
Inhibition of MXR transport by acridine derivatives
This invention provides methods that are useful for inhibiting a MXR transporter in a cell overexpressing a MXR gene but not overexpressing a Pgp gene by contacting the cell with an acridine...
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6514988 |
Condensed-ring thiophene derivatives, their production and use
A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or...
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6514987 |
Frangible compounds for pathogen inactivation
Compounds and methods for inactivating pathogens in materials are described, including compositions and methods for inactivating pathogens in biological materials such as red blood cell...
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6486170 |
Phospholipase A2 inhibitors as mediators of gene expression
A signaling pathway is identified that involves the activation of phospholipase A2 and protein kinase C in human cells, which in turn confers x-ray induction of the tumor necrosis factor α (TNF)...
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6479504 |
Antagonism of immunostimulatory CpG-oligonucleotides by 4-aminoquinolines and other weak bases
The present invention relates generally to the field of immunology. More particularly it concerns compositions and methods for inhibiting stimulation of the immune system. The compounds and methods...
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6469047 |
Tyrosine derivatives
The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
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6420377 |
Covalent conjugates of topoisomerase I and topoisomerase II inhibitors
The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: T I —L—T II (I) wherein: T I ...
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6413984 |
8-(heterocyclylmethyl)quinoline derivatives for treating urinary incontinence
The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being...
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6410219 |
Treating blood or blood products with compounds which have a mustard, azirdinium or aziridine group and a nucleic acid binding group
Methods and compositions for treating pathogens in material are described, including methods of decontaminating human fluids prior to processing in the clinical laboratory and methods for...
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6303593 |
3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of...
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6281225 |
Inhibiting proliferation of arterial smooth muscle cells
The present invention provides methods for inhibiting restenosis at a site of vascular recanalization. The methods include intravascular administration of a reactive acridine compound to the site...
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6262081 |
Composition for and method of treating neurological disorders
The invention relates to a method of treating neurological disorders associated with neurotransmitter deficit in a mammal comprising administering to the mammal a therapeutically effective amount...
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6248750 |
9-hydroxyamino tetrahydroacridine and related compounds
There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl,...
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6242459 |
Substituted bis-acridines and related compounds as CCR5 receptor ligands, anti-inflammatory agents and anti-viral agents
This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment...
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6221877 |
Substituted 4-phthalimidocarboxanilides as inhibitors of purine salvage phosphoribosyltransferases
The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
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6214816 |
Heterocyclic compounds
The compounds are N-substituted azaheterocyclic compounds of formula I ##STR1## wherein R 1 and R 2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C 1 -6 -alkyl or C 1 -6 -alkoxy;...
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6194403 |
Tacrine derivatives for treating Alzheimer's disease
A series of tacrine derivatives has be synthesized and disclosed. These tacrine derivatives were claimed to be new and be useful for the treatment of Alzheimer's disease alone or in combination...
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6187787 |
Bis(9-aminoacridine) DNA intercalating agents having antitumor activity
A series of bis-acridinyl DNA intercalating agents with anticancer cell activity represented by formula (I), where Z is a linear arrangement of multiple aromatic rings, containing at least three...
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6177441 |
Treating red blood cell solutions with anti-viral agents
Methods and compositions for treating pathogens in material are described, including methods of decontaminating human fluids prior to processing in the clinical laboratory and methods for...
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