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7273864 |
Compositions and methods for inducing osteogenesis
The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: ...
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7256196 |
Purine cytokine inhibitors
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian...
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7238700 |
A2B adenosine receptor antagonists
Disclosed are novel A 2B adenosine receptor antagonists of Formula I:
A compound of the formula:
wherein:
R 1 is optionally substituted alkyl or a group —Y-Z, in which Y is...
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7217702 |
Selective antagonists of A2A adenosine receptors
Selective antagonists of A 2A adenosine receptors like those of formula I are provided, wherein Y forms a ring.
The novel A 2A blockers are useful for the treatment of Parkinsons disease and...
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7189730 |
A2A adenosine receptor antagonists
Disclosed are novel A 2A adenosine receptor antagonists of the formula:
wherein:
R 1 is optionally substituted aryl or optionally substituted heteroaryl; R 2 is optionally substituted...
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7157449 |
Medicament for the treatment of diseases caused by parasitic protozoa
The present invention relates to the use of an inhibitor of CTP synthetase, such as a glutamine analogue, and a substance capable of suppressing toxic effects thereof in vivo, in the manufacture of...
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7087589 |
Methanocarba cycloakyl nucleoside analogues
The present invention provides novel nucleoside and nucleotide derivatives that are useful agonists or antagonists of P1 or P2 receptors. For example, the present invention provides a compound of...
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7045525 |
Use of (R)-peniciclovir triphosphate for the manufacture of a medicament for the treatment of viral diseases
A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of...
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7008948 |
Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV:
wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or...
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6969720 |
Biaryl substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of...
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6958344 |
Pyrimidine compounds and their use as modulators of chemokine receptor activity
The invention provides certain heterocyclic compounds, processes, and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy; in formula (I),...
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6958324 |
Inosine compounds and their use for treating or preventing an inflamation or a reperfusion disease
Inosine compounds, compositions comprising an inosine compound and methods for treating or preventing an inflammation disease or a reperfusion disease comprising administering an effective amount...
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6926763 |
Purine and isosteric antibacterial compounds
The invention features compounds of the formula:
or a pharmaceutically acceptable salt thereof, wherein A is CR 2 and B is N; wherein n is 0-3; wherein R 1 is (CH 2 ) m —{(G) o —(CH 2 )...
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6924271 |
3-β-D-ribofuranosylthiazolo[4-5-d]pyridimine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention...
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6911460 |
Antiviral agents and methods of treating viral infections
The present invention relates to methods of treating viral or fungal infections using 3-aminopyridine-2-carboxyaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde...
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6790841 |
2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents
Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of...
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6734187 |
Purine derivatives and medicaments comprising the same as active ingredient
Purine derivatives represented by the following formula and salts thereof: wherein R 1 represents a C 1 -C 4 alkyl group or difluoromethyl group; R 2 represents tetrahydrofuranyl group, a C 1...
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6620796 |
Combinatorial library synthesis and pharmaceutically active compounds produced thereby
The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications,...
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6589950 |
Purine derivatives inhibitors of tyrosine protein kinase SYK
Disclosed are compounds of the formula in free or salt form, wherein X, R 1 , R 2 , R 3 , and R 4 are as defined in the specification, their preparation and their use as pharmaceuticals,...
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6440979 |
Aryl isoguanines
Disclosed are compounds having formula (II): wherein: Q 3 , Q 6a , Q 6b and Q 8 are independently a bond, C 1-8 alkylene, C 2-8 alkenylene and C 2-8 alkynylene, and R 3 , R 6a , R 6b and R...
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6417180 |
Zinc finger-reactive antimicrobial compounds
The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such...
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6376501 |
Type 2 helper T cell-selective immune response suppressors
The present invention relates to a type 2 helper T cell-selective immune response inhibitor, an immune response regulator and an anti-allergic agent, individually comprising, as an active...
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6303618 |
Cyclin dependent kinase inhibiting purine derivatives
Method of treating a tumour or other cell proliferation disorder which comprises administering an effective amount of a purine compound which inhibits cyclic dependent kinase activity. Novel purine...
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6258809 |
6-aryloxy and arylthiopurines
Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by...
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6110923 |
Method for treating cancer using novel substituted purinyl derivatives with immunomodulating activity
The present invention covers a method of treatment of cancer, in particular, colon carcinoma, comprising the step of administering the compound N2-(6-dimethylamino...
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6107300 |
Arylamino fused pyrimidines
Corticotropin releasing factor (CRF) antagonists of formula I or formula II: ##STR1## and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
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6087366 |
Use of flavopiridol or a pharmaceutically acceptable salt thereof for inhibiting cell damage or cell death
Flavopiridol and its salts are used to inhibit neuronal cell damage or neuronal cell death.
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6080746 |
Methods and compositions for the prophylaxis and treatment of cytomegalovirus infections
Methods and compositions for preventing or treating cytomegalovirus infections by the use of carbocyclic analogues of purine and pyrimidine nucleosides.
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6054441 |
Oxypurine nucleosides and their congeners, and acyl derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The...
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6043228 |
O.sup.6 -substituted guanine derivatives, a process for their preparation and their use in treating tumor cells
O 6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR', wherein X is O or S, R" and R"' are alkyl, or substituted...
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6043223 |
Enhanced opening of abnormal brain tissue capillaries
Improved compositions and methods for increasing permeability of abnormal brain tissue to pharmaceutical agents. Cyclic GMP specific phosphodiesterase inhibitors are combined with bradykinin or a...
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6028076 |
Purine derivative
This invention relates to novel purine derivatives of formula (I): ##STR1## where R 2 and R 9 are hydrocarbon groups, R 6 is an amino group and R 8 is a hydroxyl, or acyloxy group. These purine...
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6015573 |
Nucleoside phosphate therapy for viral infection
Compositions for topical use in herpes virus infections comprising anti-herpes nucleoside analogue phosphate esters, such as acyclovir monophosphate and acyclovir diphosphate, which show increased...
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6001840 |
Methods of treatment of viral infections using carbocyclic deoxyguanosine analogs
Method for prophylaxis and treatment of a viral infection characterized by the administration of a composition comprising a substantial molar excess of the D-stereoisomer of 2'CdG over the...
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5990118 |
Purine compounds and xanthine oxidase inhibitors
Purine or triazolopurine compounds are disclosed represented by formula (I) or (II): ##STR1## wherein R 1 and R 4 represent each hydrogen, halogeno, hydroxy, mercapto, or amino; R 2 represents...
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5922694 |
Optically-active isomers of dideoxycarbocyclic nucleosides
A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R) 2 , where n R' is H, (C 1 -C 4 )alkyl, aryl, CHO, (C 1 -C 16...
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5916894 |
Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
The present invention provides 8-substituted O 6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such...
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5912252 |
Purine and guanine derivatives as PNP inhibitors
The subject invention concerns compounds of formula (I): wherein n=1 or 2; R 1 is H, NH 2 or halogen; R 2 is H or NH 2 ; R 3 represents the group CR 6 R 7 R 8 where R 6 , R 7 ...
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5891881 |
Aminoheterocycle-substituted glycerols
Aminoheterocycle-substituted glycerols of Formula I are disclosed: ##STR1## wherein one of A, B or C is --X--R, wherein X is --O-- or --S--, and R is a substituted or unsubstituted C 12 -24 alkyl...
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5863921 |
Purine and guanine derivatives
Compounds of formula (I) ##STR1## wherein n=1 or 2; R 1 is H, NH 2 or halogen; R 2 is H or NH 2 ; R 3 represents the group ##STR2## where m=0 or 1; R 4 and R 5 are the same or...
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5840728 |
Conformationally locked nucleoside analogs as antiherpetic agents
A method for treatment of herpes virus infection by administering an effective virus-inhibiting amount of a cyclopropanated carbocyclic 2'-deoxynucleoside to an individual in need thereof. The...
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5786359 |
N.sup.9 alkyl or aralkyl derivatives of 7, 8-disubstituted guanines
Immunostimulating 7,8-disubstituted guanine derivatives that also contain a 9-alkyl, 9-alkoxy or 9-aralkyl substituent are disclosed whose structures are represented by Formula I ##STR1## wherein X...
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5753635 |
Purine derivatives and their use as anti-coagulants
This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z 1 is --O--, --N(R 10 )-- or --CH 2 O--; Z 2 is --O--, --N(R 10 )-- or --OCH 2 --; R 1 and R...
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5736549 |
Hypoxanthine and guanine compounds
Compounds of formula I ##STR1## where n=0-2; R 1 is H, NH 2 or a halogen; R 2 is H or NH 2 ; R 3 is any of the four groups ##STR2## where m=0 or 1; and X is O, NR 5 , or S(O) 0 -2...
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5691307 |
O.sup.6 -substituted guanine compositions and methods for depleting O.sup.6
Novel O 6 -substituted guanine compounds and pharmaceutical compositions thereof are useful for effectively reducing O 6 -alkylguanine-DNA alkyltransferase (AGT). The novel compounds are useful...
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5656617 |
Derivatives of purine, process for their preparation and a pharmaceutical preparation
Antivirally active compounds of formula (I), wherein R 1 is hydrogen, hydroxy, mercapto or amino; R 2 is hydrogen, hydroxy, fluoro, chloro or amino; R 3 and R 4 are independently selected from...
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5631259 |
Cycloalkltriols containing cyclic substituents, processes and intermediate products for their preparation and their use as antiviral and antiparasitic agents
Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituents Compounds of the formulae I and II ##STR1## in which the...
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5567703 |
Method for treating HIV infections with dideoxycarbocyclic nucleosides
A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R) 2 , wherein R' is H, (C 1 -C 4 )alkyl, aryl, CHO, (C 1 -C 16...
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5500428 |
Furyl-substituted purines and adenosine antagonists
Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl; A is --NCQ--O--, NCQ--NR 8 --, --NCQ--CHN--or...
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5369098 |
Hydroxymethyl cyclobutyl purines
Antiviral activity is exhibited by compounds having the formula ##STR1## and their pharmaceutically acceptable salts. R 1 is ##STR2## R 2 is hydrogen, --PO 3 H 2 , ##STR3## wherein R 3 is...
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