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7312223 |
Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure
derivatives, and formulations thereof, and processes for...
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7192962 |
Xanthine phosphodiesterase V inhibitor polymorphs
Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4
-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit...
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7135475 |
Amide substituted xanthine derivatives
The present invention is a 1,3,8 substituted xanthine derivative of formula I
or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are as defined in the specification.
...
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7098217 |
3,7-dihydro-purine-2,6-dione derivatives as CRF receptor ligands
3,7-Dihydro-purine-2,6-dione derivatives of Formula (I) are provided
wherein R 1 , R 2 , R 3 and R 4 are herein defined for use as CRF receptor ligands in the treatment of disorders...
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7053096 |
Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in...
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6878715 |
Therapeutic compounds for inhibiting interleukin-12 signals and method for using same
Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations...
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6855736 |
Molecular target of neurotoxicity
The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterization and/or treatment (or management) of neuro...
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6780865 |
Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in...
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6774130 |
Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same
Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations...
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6693106 |
Pentoxifylline, pioglitazone and metformin are inhibitors of formation of advanced glycation endproducts (AGE's)
Pentoxifylline, pioglitazone and metformin have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. The...
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6649600 |
Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A 1 receptor. Adenosine A 1 antagonists can be usefull...
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6608069 |
Phenyl xanthine derivatives
The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl,...
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6605600 |
Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A 1 receptor. Adenosine A 1 antagonists can be useful...
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6586478 |
Methods and compositions for improving sleep
Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.
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6558660 |
Method for regulating IL-10 with IL-9, and applications thereof
The invention involves the recognition of IL-9 as a molecule involved in induction of IL-10. Administration of IL-9 leads to protection against conditions where IL-10 production is warranted, such...
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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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6469017 |
Method of inhibiting interleukin-12 signaling
A method for blocking IL-12 signaling by administration of the following compound: wherein, R 1 is H, CH 3 , sulfate, phosphate, or salt thereof; R 2 is alkyl (C 1-12 ), alkoxyalkyl (C 1-11 ),...
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6423719 |
Method for treating benign prostate hyperplasia
A method of treating and/or preventing renal dysfunction in a patient, such as renal colic or contrast nephropathy by administering to a patient, a compound of the formula: is described herein....
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6420374 |
Use of xanthines as immunosuppressants and to inhibit allograft reactions
A family of compounds effective in suppressing lymphocyte activation is comprised of 7-(oxoalkyl)1,3-dialkyl xanthines, other than denbufylline, of the formula in which R 1 and R 2 are the...
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6413976 |
Compositions and method for decreasing neuropathic pain
Compositions containing propentofylline, and methods for treating neuropathic pain with such compositions, are disclosed.
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6399624 |
Method and composition for inhibiting post-surgical adhesions
A method and compositions for reducing post-surgical adhesion formation/reformation in mammals following surgical injury to a body cavity or organs situated therein. The aqueous compositions...
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6372740 |
2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof
2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted...
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6337325 |
Combined preparation for the therapy of immune diseases
A combination preparation comprising a compound which has a phosphodiesterase-inhibiting action, and a compound which reduces the biologically effective intracellular Ca 2+ content, is suitable...
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6329381 |
Heterocyclic compounds
The present invention relates to a heterocyclic compound of the following general formula (I): ##STR1## wherein X is sulfur atom, oxygen atom or --NR 3 -- (R 3 may form a heterocyclic ring or...
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6316458 |
Method of enhancing insulin action
A category of hydroxyalkyl-substituted xanthines are useful in treating patients suffering from disorders associated with impaired glucose metabolism or impaired insulin function. Use of these...
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6313131 |
Method of kidney treatment
A method of treating and/or preventing renal dysfunction in a patient, such as renal colic or contrast nephropathy by administering to a patient, a compound of the formula: ##STR1## is described...
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6294541 |
Purine derivatives having phosphodiesterase IV inhibition activity
A compound of the formula: ##STR1## wherein R 3 represent a C 1 -8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO 2 H, NOH, NOCONH 2 , or...
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6248746 |
3-(arylalkyl) xanthines
With the above and other objects in view, the present invention comprises compounds having the general formula (I): ##STR1## wherein: R 1 is a C 2 -8 alkyl, C 2 -8 alkenyl, C 2 -8 alkynyl, C 3...
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6204270 |
Ophthalmic and mucosal preparations
A composition to treat mucosal disorders includes a therapeutically effective quantity of an anti-TNF-α agent and a mucoadhessive delivery system.
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6187780 |
Assymetrically substituted xanthine derivatives having adenosine A1 antagonistic activity
Asymmetrically substituted xanthine derivatives having adenosine A 1 antagonistic activity. These are useful as pharmaceuticals. Exemplary are: (a)...
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6166024 |
Use of topical azathioprine and thioguanine to treat colorectal adenomas
A method is provided to reduce the recurrence of colorectal adenomas following endoscopic removal by topically administering to the colon an effective amount of azathioprine thioguanine or a...
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6133274 |
Hydroxyl-containing bicyclic compounds
Disclosed are therapeutic compounds having the formula: (R)j-(core moiety), including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one...
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6127355 |
High molecular weight polymer-based prodrugs
The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety; X is an electron withdrawing group; Y and Y' are independently...
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6075029 |
Xanthine modulators of metabolism of cellular P-450
A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These...
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6057328 |
Method for treating hyperoxia
Disclosed are methods for treating conditions resulting from hyperoxia or mechanical ventilation comprising the administration of a compound of the formula: ##STR1## wherein R 1 is a substantially...
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6020337 |
Electronegative-substituted long chain xanthine compounds
Therapeutic compounds, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, having a formula: ##STR1## wherein R 0 is selected from the group...
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6010711 |
Methods, articles and compositions for the pharmacologic inhibition of bone resorption with phosphodiesterase inhibitors
A class of active agents, and articles and compositions containing them and methods for treating human patients with them, which inhibit bone resorption of all types. This class of active agents...
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5968940 |
Retinoids and methods of use of same
New purine retinoid compounds according to the formula: ##STR1## wherein R is a purine derivative, and pharmaceutical compositions thereof, are provided which exhibit cancer-inhibiting activity.
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5965564 |
Enantiomerically pure hydroxylated xanthine compounds
There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an ω-1 alcohol of a straight chain alkyl (C 5 -8) substituted at the 1-position...
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5958932 |
Substitutes O.sup.6 -benzylguanines, compositions, and methods of using same
The present invention provides AGT inactivating compounds such as substituted O 6 -benzylguanines of the formula ##STR1## wherein, for example, R 1 is amino, hydroxy, or alkylamino, R 2 is...
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5958413 |
Use of antibodies to TNF or fragments derived thereof and xanthine derivatives for combination therapy and compositions therefor
A combined preparation for simultaneous combined, simultaneous separate, or sequential use in the therapy of prophylaxis of disorders associated with undesirable high levels of TNF, e.g. septic or...
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5891904 |
Use of inhibitors of phosphodiesterase IV
The invention relates to the use of inhibitors of phosphodiesterase IV for the modulation of the motility and peristalsis of the hollow organs of the urogenital and gastrointestinal tract.
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5861405 |
S-substituted 1,3,7-trialkyl-xanthine derivatives
The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A 2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the...
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5861396 |
Purin-6-one derivatives
Purin-6-one derivatives are prepared by acylating appropriately substituted imidazole carboxamides and then cyclizing to give the purines. The purin-6-one derivatives are suitable as active...
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5859017 |
Method for inhibiting mast cell and basophil activation
In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is...
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5856115 |
Assay for identification therapeutic agents
There is disclosed a method for screening for inhibitors of cellular second messenger signaling regulated by lysophosphatidic acid acyl transferase (LPAAT) and phosphatidic acid phosphohydrolase...
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5840729 |
Xanthine derivatives as adenosine A1 receptor antagonists
A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative.
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5792772 |
Enatiomerically pure hydroxylated xanthine compounds
There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an ω-1 alcohol of a straight chain alkyl (C 5 -8) substituted at the 1-position...
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5780476 |
Hydroxyl-containing xanthine compounds
Disclosed are therapeutic compounds having the formula: (R)j - (core moiety), including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from...
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5763446 |
Use of pentoxifylline and other tumor necrosis factor blockers for the treatment of aids-associated optic neuropathy and other central nervous system diseases
In accordance with the present invention, methods are provided for the treatment of visual loss and other neurological dysfunctions in AIDS patients employing agents capable of blocking TNF...
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