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7388002 |
Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
Compounds represented by the formula:
A is (CH 2 ) n R 2 , —CH═CH 2 , CH 2 —CH═CH 2 , O(CH 2 ) n R 2 , CH(OH)CH 3 , CH(OH)CH 2 OH, CH 2 —CH(OH)CH 3 , CH 2 CH(OH)CH 2 OH, or...
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7342021 |
Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I:
wherein R 1 and R 2 are as defined herein.
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7332486 |
Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I:
wherein R 1 and R 2 are as defined herein.
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7319101 |
COMT inhibitors for the treatment of depression and impaired cognition
The present invention relates to compounds of formula I
wherein R 1 is as defined in the specification
and to esters thereof which are hydrolyzable under physiological conditions and to the...
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7317018 |
Anti-inflammatory medicament
The use of adenosine-5′-triphosphate-2′,3′-dialdehyde (oATP) as a medicament useful for the treatment of inflammatory conditions is disclosed.
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7279483 |
Famciclovir monohydrate
Famciclovir monohydrate and its pharmaceutical use.
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7279482 |
Heterocyclic compound based on N6-substituted adenine, methods, of their preparation, their use for preparation of drugs, cosmetic preparations and growth regulators, pharmaceutical preparations, cosmetic preparations and growth regulators containing these compounds
Heterocyclic derivatives based on N 6 -substituted adenine of, e.g.,a formula:
wherein R2 is hydrogen, R6 is R6′-X, X is —NH—, and R6′ is substituted phenyl or substituted benzyl. The...
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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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7270804 |
Use of one or several substances selected from the group of pyrimidines and purines in cosmetic preparations for tanning the skin
Use of one or more substances selected from the group of pyrimidines and purines for the preparation of cosmetic or dermatological preparations for boosting natural skin tanning and/or for...
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7265111 |
Adenosine analogues and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I)
wherein X is selected from the group consisting of
wherein n and p are independently 0, 1, 2, or 3, provided...
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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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7253175 |
Method for treating athlete's foot
A method of treating a patient having a fungal infection comprises administering an effective fungal infection treatment amount of an antiviral agent, such as valacyclovir, to eliminate the...
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7253154 |
Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
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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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7220757 |
Compositions and methods for topical administration of 2-NH-heteroarylimidazoles
Compounds of formula (I):
are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
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7220748 |
Use of 4-(2-Flurophenyl)-6-methyl-2-(1-piperazinyl)thieno(2,3-D)-pyrimidine for treating of urinary incontinence
4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)-Thieno(2,3-D)p
yrimidine or a salt thereof is useful for the treatment of urinary incontinence.
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7217716 |
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain
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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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7214665 |
2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
The invention provides compounds having the following general formula (I):
wherein X, R 1 , R 2 , R 7 and Z are as described here.
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7196093 |
Reversible inhibitors of SAH hydrolase and uses thereof
1. The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used as an...
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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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7183268 |
2-amino-9-[(2-hydroxymethyl) cyclopropylidenemethyl] purine antiviral agents
Compounds which are active against viruses have the following Formulas:
wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR 1 , OR 2 , or...
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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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7138401 |
2-aminopurine analogs having HSP90-inhibiting activity
2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated...
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7129239 |
Purine compounds and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. ...
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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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7053097 |
Inhibitors of glycogen synthase 3 kinase
Compounds of formula 1:
wherein
R 1 is alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl, substituted with 0–3 substituents selected from lower alkyl, halo, hydroxy,...
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RE39112 |
Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine...
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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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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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6887880 |
Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof
The present invention relates to derivatives and analogues of adenine of the formula:
wherein L, A, Y and Z are those defined herein. Compounds of the present invention are useful in...
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6841549 |
Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is,...
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6803371 |
Purine inhibitors of protein kinases, G proteins and polymerases
The present invention relates to 2-N-substituted 6-(4-methoxybenzylamino)-9-isopropylpurines that inhibit, inter alia, protein kinases, G-proteins and polymerases. In addition, the present...
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6794390 |
Purine inhibitors of cyclin dependent kinase 2 & ikappabalpha
A compound having the formula: wherein: R 1 is —X—R 1 ′; in which R 1 ′ is lower alkyl, substituted lower alkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or...
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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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6784174 |
Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease
This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from...
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6784166 |
4′-substituted nucleoside derivatives as inhibitors of HCV RNA replication.
The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols...
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6767906 |
2-amino-6-anilino-purines and their use as medicaments
This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R 1 is α) —S(═O) k —NR 6 R 7 , in which k is 1 or 2, wherein under the proviso...
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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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6703395 |
Cyclin dependent kinase inhibitor
The present invention is based on the method of treating a patient suffering from leukemia comprising administering a therapeutically effective amount of the compound...
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6696454 |
Inhibitors of spermidine synthase for the treatment of osteoarthritis and cartilage rehabilitation
This invention provides a method for the treatment of a subject in need of treatment for osteoarthritis comprising administering to said subject an amount of an inhibitor of spermidine biosynthesis...
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6642231 |
6,9-disubstituted 2-&lsqb trans-(4-aminocyclohexyl)amino&rsqb purines
The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also...
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6641843 |
Pharmaceutical compositions
The present invention relates to pharmaceutical compostions of (1S,4R)-cis-4-[2-amino-6-cyclopropylamino}-9H-purin-9-yl]-2-
cyclopentene-1-methanol (1592U89).
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6630477 |
Therapeutic nucleoside compound
The present invention relates to (1R,4S)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol and its use in medical therapy for the treatment of hepatitis B infection.
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6627633 |
6-substituted biaryl purine derivatives as potent cyclin/CDK inhibitors and antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine inhibitors of cyclin/cdk complexes. The compounds also are potent inhibitors of human cellular proliferation. As such, the...
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6605619 |
Nitroxides as protectors against oxidatives stress
The instant invention is directed to the use of a biologically compatible composition, containing an effective amount of a metal-independent nitroxide compound which is preferably represented by...
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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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6559148 |
Use of P2Y purinoreceptor antagonist for the treatment of ischemia reperfusion
Use of compounds modulating P2 purinoceptors, in particular antagonists such as Basilen Blue E-3G (Reactive Blue 2), for the prevention of the damages due to global cerebral ischemia and...
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6541482 |
Carbocyclic nucleoside agents useful as selective inhibitors of proinflammatory cytokines
The present invention relates to compounds of the formula wherein X is N 3 , NH 2 , NHR, N(R) 2 , CN, SH, SR, or OR 1 ; R is C 1 -C 4 alkyl or (CH 2 ) n —φ; n is an integer 0, 1, 2, 3 or 4;...
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