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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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7358235 |
Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these...
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7342006 |
Substituted 8-heteroaryl xanthines
Selective antagonists of A 2B adenosine receptors like those of formula I are provide.
The compounds and compositions are useful as pharmaceutical agents.
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7335655 |
8-heteroaryl xanthine adenosine A2B receptor antagonists
The present invention relates generally to compounds of formula (I):
wherein
X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen,...
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7317017 |
A2B adenosine receptor antagonists
Disclosed are novel A 2B adenosine receptor antagonists having the structure of Formula I or Formula II
The compounds are particularly useful for treating asthma, inflammatory gastrointestinal...
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7271179 |
Inhibitors of JAK protein kinase
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7265129 |
Anti-infective biaryl compounds
Compounds represented by the formula (I), where R1, R2, R3, R4, R5, and Q are as defined herein, exhibit activity against infectious pathogens
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7262176 |
Adenosine A3 receptor agonists
Disclosed are novel compounds that are A 3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.
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7259159 |
Guanidino derivatives as inhibitors of cell adhesion
The present invention relates to acylguanidino derivatives of formula (I), in which R 1 , R 2 , R 3 , A, B, X, Y and n have the meanings indicated in claim 1 , their physiologically tolerable...
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7253176 |
Immunosuppressive effects of 8-substituted xanthine derivatives
The invention relates to a novel use of 8-substituted xanthine derivatives for the manufacture of a medicament for the treatment of auto-immuno disorders.
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7235538 |
Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I
wherein each n is one or two independently and R 1 , R 2 , R 3 , R...
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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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7148229 |
Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I:
or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl,...
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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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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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7074798 |
Xanthine derivative and DPPIV inhibitor
The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula:
wherein, m is 0 or 1;
n is 0; R 31 , R 32 , R 33 ,...
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7071199 |
Kinase inhibitors as therapeutic agents
The present application is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors.
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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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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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7037916 |
Pyrimidine derivatives as IL-8 receptor antagonists
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I...
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7022710 |
A1 adenosine receptor antagonists
Disclosed are novel methods of antagonizing the A 1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the...
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7001910 |
Thiazolidinedione derivatives as antidiabetic agents
The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for...
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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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6949559 |
Nitrogen substituted biaryl 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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6936618 |
Cystic fibrosis medicaments
The use of a type V cyclic nucleotide phosphodiesterase inhibitor for the preparation of a medicament for the treatment of cystic fibrosis.
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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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6916811 |
Adenosine A2a receptor antagonists
Disclosed herein are compounds having the structural formula A
including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the...
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6894056 |
Method for diagnosing and alleviating the symptoms of chronic fatigue syndrome
A method for alleviating chronic fatigue syndrome with the administration of antiviral agents. Based on clinical tests, chronic fatigue syndrome is a persistent herpes virus infection including...
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6894054 |
Heterocyclic inhibitors of glycine transporter 2
Compounds, compositions, and methods for inhibiting the glycine transporter 2 and for inhibiting glycine transporter mediated neuronal activity. These compounds are particularly useful for...
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6894045 |
Tetrahydropurinones and derivatives thereof as corticotropin releasing factor receptor ligands
Compounds provided herein are novel substituted tetrahydropurinones of Formula (I):
wherein R 3 is aryl substituted with 0-5 X Ar or heteroaryl substituted with 0-4 X hAr . Such compounds...
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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6894021 |
Method for identifying and using A2B adenosine receptor antagonists to mediate mammalian cell proliferation
This invention concerns methods for identifying A 2B adenosine receptor agonists and antagonists as well as methods for using A 2B adenosine receptor antagonists to treat cell proliferation...
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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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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6844320 |
Treatment of preeclampsia, toxemia and preterm labor with combination of progestational agent and a nitric oxide synthase substrate and/or donor
Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both,...
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6815446 |
Selective antagonists of A2B adenosine receptors
A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The...
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6812232 |
Heterocycle 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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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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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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6774129 |
Benzothieno&lsqb 3,2-c&rsqb pyridines as α2 antagonists
The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R 1 is...
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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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6747016 |
Substituted purine derivatives as inhibitors of cell adhesion
The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R 1 , R 2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their...
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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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6743800 |
Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them
The present invention relates to compounds of formula (1), in which H, G, Z, X, Y, r, s and t have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs....
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R 1 , R 2 , R 3 and A are each as defined, and to processes for their preparation and...
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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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6710051 |
Screening method
The invention relates to a method for identification of substances which are applicable for treatment or prevention of an insufficient longitudinal growth of the eye (hypermetropia) or for...
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6693105 |
Hydroxyl-containing compounds
Disclosed are therapeutic compounds having the formula: (R) j —(CORE MOIETY), including resolved enantiomers, diastereomers, hydrates, salts, solvates or mixtures thereof where j is an integer...
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