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7608603 |
Substituted pyrazolo[3,4-D]pyrimidines as p38 MAP kinase inhibitors
Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih:
wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CR g , and W, D, E, R 4 , R 5 , R 6 and R g are as defined...
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7605147 |
Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1):
in which represents single bond or double bond, R 1 , R 2 , R 3 , R 7 ...
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7579354 |
Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A 1 receptor. Adenosine A 1 antagonists can be useful...
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7579332 |
Nucleobase phosphonate analogs for antiviral treatment
The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the...
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7579325 |
Drugs containing reduced of vitamin B2
The present invention provides medicines for preventing or treating infectious diseases, sepsis and/or septic shock, which exhibit excellent immunostimulating effects. More specifically, the...
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7566721 |
Substituted thienol[2,3-d]pyrimidines as kinase inhibitors
Compounds of the formula
and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or...
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7563781 |
Triazolopyrimidine derivatives
The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
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7553825 |
Anti-proliferative compounds, compositions, and methods of use thereof
Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV,
wherein:
Y 1A and Y 1B are independently Y 1 ; R X1 and R X2 ...
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7544672 |
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of...
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7528121 |
Phosphonooxy quinazoline derivatives and their pharmaceutical use
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their...
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7514442 |
Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7511037 |
N-[[4-fluoro-2-(5-methy-1H-1,2,4-triazol-1-yl)phenyl]methyl]-4-,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor
The invention encompasses a series of bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful...
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7504398 |
Substituted-4-(pyrrolo pyrimidin-6-yl)benzenesulphonamide derivatives
This invention is directed to selective antagonists of A 2A and/or A 2B adenosine receptors having the general formula (I); to processes for their preparation; to pharmaceutical compositions...
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7494984 |
Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the...
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7479277 |
Method for reducing intraocular pressure using integrin-linked kinase inhibitor
Methods for treating increased intraocular pressure by administering agents that interfere with activities of integrin-linked kinase. By interfering with the ability of integrin-linked kinase to...
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7476661 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract...
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7470695 |
N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7459444 |
Inhibitors of chymase
The present invention is directed to a compound of formula (I),
methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory...
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7439249 |
Inhibitors of phosphatases
The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.
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7435739 |
Substituted pyrrolopyrimidines useful in the treatment of cancer
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R 1 , R 2 , R 3 and R 4 are as defined herein. The...
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7429596 |
1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention...
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7429574 |
4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use
Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.
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7419969 |
HIV integrase inhibitors: cyclic pyrimidinone compounds
The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating...
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7417036 |
Crystal form of adefovir dipivoxil and its preparation
A new crystal form of adefovir dipivoxil {9-[2-[bis(pivaloyloxy)-methoxy]-phosphinyl]-methoxyl]-ethyl
]-adenime} and its composition is disclosed, as is a method to prepare the crystal comprising...
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7390791 |
Prodrugs of phosphonate nucleotide analogues
A novel method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a)
having substituent groups as...
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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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7368437 |
Bicyclic heterocycles, processes for their preparation and their use as herbicides and pharmaceutical agents
Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or...
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7358250 |
Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity
Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general...
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7323449 |
Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent...
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7312204 |
Insecticides
The present invention relates to insecticidal mixtures of chloronicotinyl insecticides of the formula (I)
in which
R 1 represents C 1 -C 5 -alkyl, R 2 represents hydrogen or C 1 -C 5 -alkyl...
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7300924 |
Anti-infective phosphonate analogs
The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as...
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7285543 |
Purine inhibitors of fructose-1,6-bisphosphatase
Novel purine compounds of Formula 1, pharmaceutically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitors
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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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7238679 |
Heterocycles and uses thereof
Compounds of the following formula are disclosed:
wherein R B is a substituted or unsubstituted aryl or heteroaryl moiety; at least one of R U and R L is a phosphorus-containing moiety, J,...
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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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7229976 |
Modulation of forkhead box O1A expression
Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides,...
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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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7214668 |
Phosphonic acid based prodrugs of PMEA and its analogues
Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described:
wherein: M and V are cis to one another and MPO 3 H 2 is a phosphonic acid selected...
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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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7157448 |
Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
The present invention relates to a nucleoside phosphonate derivative represented by formula (1):
pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is...
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7151100 |
Indole compounds useful for the treatment of cancer
The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
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7148210 |
Method of treating bone metastasis
The invention provides a drug combination for the treatment of diseases associated with bone metastasis. The combination provides adenosine or a derivative thereof, a bisphosphonate, and a...
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7129261 |
Cytotoxic agents
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming...
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7129227 |
Lipid analogs for treating viral infections
A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpesviruses, is disclosed. The method comprises administering to a subject in need of such treatment an...
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7115590 |
Phosphoramidate, and mono-, di-, and tri-phosphate esters of (1R, cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol as antiviral agents
The present invention relates to phosphoramidate, and phosphate esters of (1R,cis)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1nethanol,
processes for their preparation, and their use in treating...
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7115589 |
Purine derivatives
This invention relates to compounds of the general formula:
in which R A , R B , R C and R D are as defined herein, and to their preparation and use. In these compounds, R B is an aliphatic,...
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7109165 |
Conjugates and compositions for cellular delivery
This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids...
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RE39264 |
Pharmaceutical combination
The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically...
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7098216 |
Thiazolopyrimidines useful as TNFα inhibitors
The invention provides derivatives of thiazolo[4,5-d1]pyrimidine and their use as inhibitors of proinflammatory cytokines.
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7098196 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract...
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