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7615634 |
4-aminopyrimidine-5-one derivatives
Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent...
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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula
wherein: Y′ is O or S, W′ is
optionally substituted,
Z′ is selected from the group consisting of
wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
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7582644 |
Pyrimidyl sulphone amide derivatives as chemokine receptor modulators
A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease,...
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7569575 |
Synthesis of locked nucleic acid derivatives
The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and...
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7547782 |
Met kinase inhibitors
The present invention is directed to compounds having the formula I or II:
including salts thereof, and methods for using them for the treatment of cancer.
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7544692 |
Polymorphic and other crystalline forms of cis-FTC
Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray...
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7534885 |
Process and intermediates for preparing emtricitabine
A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The...
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7531536 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IIIa:
wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl,...
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7528142 |
Aminopyrimidines useful as kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of...
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7501514 |
Enantiomeric resolution of 2-substituted 4-substituted 1,3-oxathiolanes nucleosides
Single enantionmers of compounds of formula (B), in either the cis or trans configuration,
wherein R 1 and R 2 are as defined herein, can be separated from enantiomeric mixtures thereof by...
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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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7479495 |
N-heterocyclic inhibitors of TNF-α expression
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I:
Methods of...
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7470685 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
in which one of R a and R b is H or alkyl, and the other is aryl or heteroaryl optionally substituted with R d and R...
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7468436 |
Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers
A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of...
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7465735 |
5-Phenypyrimidines their preparation compositions comprising them and their use
5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 ...
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7465725 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c , or OR c ;...
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7449471 |
5-phenylpyrimidines, their preparation, compositions comprising them and their use
5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl,...
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7402588 |
Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of...
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7314934 |
4-amino substituted-6-aryl/heteroaryl substituted-2-methylsulfanyl-pyrimidine-5-carbaldehyde intermediates
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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7312180 |
Substituted 4-(4-trifluoromethylpyrazolyl)pyrimidines
A description is given of 4-(4-trifluoromethylpyrazolyl)pyrimidines of the formula (I) and of their use as herbicides.
In this general formula (I), R 1 , R 2 , R 3 and R 4 are various radicals...
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7294627 |
Chemical compounds
Compounds of formula (I)
in which R 1 , R 2 , R 3 and R 4 , have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
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7285533 |
Apo-2 ligand
A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2...
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7247633 |
Pyrimidine compounds and their use
A compound of the general formula (I):
wherein R 1 , R 2 , X, Y and Z are as described in the specification.
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7235571 |
Heterocyclic amide and imine derivatives, processes for their preparation, compositions comprising them and their use as pesticides
What is described are compounds of the formulae (I) and (II)
where the symbols and indices have the meanings given in the description.
These compounds are suitable for controlling animal pests.
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7230104 |
Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines
Pyrimidines of formula I
in which
R 1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered...
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7230100 |
Stereoselective method for the preparation of nucleosides
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A):
wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof...
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7220736 |
Pyrimidine compounds
A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,
wherein X is ═CH— or ═N—, Y is —NH—, —NR 4 —, —S—, —O—, —CH═N—,...
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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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7151092 |
Cytarabine monophosphate prodrugs
Compounds of Formula I, their preparation and uses are described:
wherein:
M and V are cis to one another and MH is cytarabine; the 5′ oxygen of said cytarabine is attached to the...
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7138404 |
4-aminopyrimidine derivatives
This invention is 4-aminopyrimidine derivatives of the formula
wherein R 1 , R 2 , R 3 and R 4 are as defined in the specification or a pharmaceutically acceptable salt thereof. The invention...
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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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7122552 |
Inhibitors of JAK and CDK2 protein kinases
The present invention provides a compound of formula I:
or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of JAK and CDK2...
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7119202 |
Substituted-1,3-oxathiolanes and substituted-1,3-dioxolanes with antiviral properties
Disclosed are compounds of the formula
wherein R 1 is hydrogen or an acyl group having 1 to 16 carbon atoms;
R 2 is a purine or pyrimidine base or an analogue or derivative thereof; Z...
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7115740 |
Pyrimido compounds having antiproliferative activity
Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful...
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7109334 |
Stereoselective methods for the preparation of nucleosides
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A):
wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof...
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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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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7098197 |
Phosphonate compounds
The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and...
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7094772 |
Phosphonate compounds
The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and...
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7091343 |
Compositions useful as inhibitors of protein kinases
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7087616 |
Pyrazolyl pyrimidines
This invention relates to novel pyrazolylpyrimidines of the formula
in which R 1 , R 2 , X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing...
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7067664 |
Corticotropin releasing factor antagonists
Corticotropin-releasing factor (CRF) antagonists having the formulae
wherein the dashed lines, A, B, Y, Z, G, R 3 , R 4 , R 5 , R 6 , R 16 and R 17 are as defined in the application, and...
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7053213 |
Therapeutic heterocycles
Pharmaceutical compositions containing novel therapeutic heterocycles for use in diseases in which an NK2 receptor is implicated, processes for preparing and methods for using the same.
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7026336 |
Compounds
Compounds of formula (I) wherein X is O, CH 2 , S or NH, or the moiety X—R 1 is hydrogen; V is CH or N; Y is NR 10 R 11 , NR 10 C(Z)NR 10 R 11 , NR 10 COOR 11 or NR 10 SO 2 R 11 ; Ar is phenyl...
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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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7019002 |
Pyridopyrimidinones derivatives as telomerase inhibitors
The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formula
where R1, R2 are as defined herein. The invention also provides methods for preparing the compounds...
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7009050 |
5-Substituted pyrimidine derivatives of conformationally locked nucleoside analogues
The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer...
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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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6960662 |
Process for preparing 2-(4-pyridyl)amino-6-dialkyloxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
The present invention relates to a process for preparing 2-(pyridin-4-ylamino-pyrido [2,3-d]pyrimidine of Formula II
by reacting a 4-aminopyridine of the formula
with a...
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