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7595401 |
Therapeutic compounds and their use in cancer
The invention relates to compounds of Formula I
and their therapeutic uses, wherein substituent A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carboxylic...
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7582758 |
Lewis acid mediated synthesis of cyclic esters
Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated...
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7569574 |
Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
The invention relates to new purine derivatives of general formula
wherein R 1 to R 4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and...
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7541460 |
Process for preparing the antiviral agent [1S-(1alpha, 3alpha, 4beta)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-3-methylenecyclopentyl]-6H-purin-6-one
Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in...
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7524847 |
Fused 1,3-dihydro-imidazole ring compounds
The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts...
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7495006 |
2′ and 3′-substituted cyclobutyl nucleoside analogs for the treatment of viral infections and abnormal cellular proliferation
Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and...
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7476670 |
Purine derivatives, method for preparing, pharmaceutical compositions and novel use
The invention relates to novel products of formula (I):
in which:
Y represents N, O, S, CHR3 or ═CR3 the dashed line representing a single or double bond, R and R1 represent in particular H,...
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7452886 |
Pyrrolo pyrimidines as agents for the inhibition of cystein proteases
The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use...
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7439359 |
Small molecule compositions for binding to hsp90
Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed...
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7432274 |
Acyclic nucleoside derivatives
Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula:
where one of R 1 and R 2 is an amino acid acyl group and the...
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7393855 |
2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents
Compounds which are active against viruses have the following formulas:
wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include...
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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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7355043 |
Preparation of purines
A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C 1-6 alkoxy or pheny C 1-6 alkoxy; and R a and R b are hydrogen, or acyl or phosphate...
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7345170 |
Crystal and solvate of 2-amino-6-benzyloxypurine and production methods thereof
The present invention can provide a solvate, a cubic crystal and a columnar crystal of 2-amino-6-benzyloxypurine by crystallization from (1) a solvent containing at least one kind of solvent...
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7307166 |
Oxpurine 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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7303773 |
Process for enriching extracts of natural theanine
A process for enhancing theanine extraction from plant material through a series of extraction, adsorption and filtration steps. More specifically, disclosed is a process for isolating theanine...
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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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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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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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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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7241890 |
Purine analogs having HSP90-inhibiting activity
Novel purine compounds of Formula I.
and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O) 2 ; and O is selected from alkyl, cycloalkyl,...
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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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7199127 |
Purine nucleosides
Disclosed are purine nucleoside compounds that are selective to A 3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the...
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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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7189849 |
Synthesis of acyclic nucleoside derivatives
Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid...
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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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7179896 |
Method of making PNA oligomers
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA...
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7176312 |
Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic...
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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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7122669 |
Purine derivatives, preparation method and pharmaceutical compositions containing same
Derivatives of purine having anti-proliferative properties and in particular, derivatives of purine endowed with an inhibitory effect vis-a-vis cycline-dependent kinase proteins i.e. abbreviated to...
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7105666 |
Synthesis of purine derivatives
The present invention provides a method for producing 2-, 6-, 8- and 9-substituted purine compounds from 4,6-dihalo-5-nitro-2-alkyl-pyrimidine compounds in solution or by solid phase techniques....
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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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7078524 |
Process for the synthesis of ganciclovir
The present invention relates to an industrial useful process for the synthesis of antiviral compound, ganciclovir which comprises dissolving a mixture containing N-7 and N-9 isomers of structural...
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7074929 |
Certain alkylene diamine-substituted heterocycles
This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the...
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7034152 |
Process for preparing the antiviral agent [1S-(1alpha,3 alpha,4beta )]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one
Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in...
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7022851 |
PNA monomer and precursor
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA...
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RE39056 |
4-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I)
and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type...
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7005430 |
Fused purine derivatives
A condensed purine derivative represented by Formula (I):
wherein X—Y-Z represents R 1 N—C═O or N═C—W, R 2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl...
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6998484 |
Synthesis of purine locked nucleic acid analogues
The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N...
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6992188 |
Substituted heterocyclic derivatives
Corticotropin-releasing factor (CRF) antagonists having the formula
wherein the dashed lines, A, B, D E, F, Z, G, R 3 , and R 5 having the definitions set forth in the specification...
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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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6949644 |
Methods for the synthesis of substituted purines
The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments,...
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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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6939965 |
Process of manufacture of 1,3-oxathiolane nucleosides using titanium trichloride mono-isopropoxide
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl) 3...
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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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6919332 |
N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula
wherein X, A, Y, B, G, and R 1 are as defined in the...
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