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7390805 |
4-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I
wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof,...
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7381729 |
4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo [2,3D] pyrimidine hydrogen mesylate, its polymorphic forms, and methods for making same
The present invention relates to the novel compound 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo[2,3d]
pyrimidine hydrogen mesylate, the polymorphic α and β forms thereof, and a method...
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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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7326699 |
4-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives
The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the...
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7323469 |
7H-pyrrolo[2,3-d]pyrimidine derivatives
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I
wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof,...
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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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7319102 |
Pyrrolo[2,3-d]pyrimidine cytokine inhibitors
The present invention relates to 2,6,7-substituted pyrrolo[2,3-d]pyrimidines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or...
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7307082 |
Heterocyclic derivatives as CRF antagonists
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I wherein X 1 is (CH 2 ) n or CO, n is 0 to 2 and R 1 , R 2 , R 3 and R 4 ...
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7279474 |
Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF)
The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the...
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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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7259154 |
Pyrrolopyrimidines
Compounds of the formula
and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or...
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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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7253166 |
6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
The invention provides a novel class of compounds and compositions of Formula I:
in which R 1 , R 2 and R 3 are defined herein, that are useful in the treatment or prevention of diseases...
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7250420 |
Method of treatment of transplant rejection
A method of treating or preventing chronic organ transplant rejection comprising administering a compound of the formula
wherein R 1 , R 2 and R 3 are as defined above.
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7217710 |
Substituted pyrazolopyrimidines
Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.
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7160890 |
Compounds specific to adenosine A3 receptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A 3 receptor and the use of these compounds to treat a disease associated with A 3 adenosine receptor in a subject,...
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7138402 |
Pyrrolopyrimidines and related analogs as HSP90-inhibitors
The present invention provides compounds represented by Formula I. R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 , R 1 is halogen, or lower alkyl; R...
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7125880 |
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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7101869 |
2,4-diaminopyrimidine compounds useful as immunosuppressants
Novel compounds according to the formula
and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is...
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7074792 |
1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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7053065 |
Vitamin B12 and pemetrexed disodium combination therapies
A method of administering an antifolate to a mammal in need thereof, comprising administering an effective amount of said antifolate in combination with a methylmalonic acid lowering agent.
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6987113 |
Tyrosine kinase inhibitors
The present invention relates to novel 3-hetero-arylideneazaindolin-2-one compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein...
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6962911 |
Pyrrolopyrimidinone derivatives, process of preparation and use
The invention relates to a series of pyrrolopyrimidinone derivatives of the formula ( 1 ):
wherein R 1 is H; C 1 -C 3 alkyl optionally substituted with one or more fluoro atoms; or C 3...
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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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6878716 |
Compounds specific to adenosine A1 receptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A 1 receptor and the use of these compounds to treat a disease associated with A 1 adenosine receptor in a subject,...
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6867208 |
Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
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6867201 |
Heteroaromatic bicyclic derivatives useful as anticancer agents
The invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R 1 , R 3 and R 4 are as defined herein. The invention also...
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6825184 |
1,4-Disubstituted benzo-fused urea compounds
Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein G, X, A and Q...
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6800633 |
Pyrrolo&lsqb 2,3d&rsqb pyrimidine compositions and their use
This invention pertains to compounds having the structure: wherein R 1 and R 2 are each independently a hydrogen atom, substituted alkyl, or a substituted or unsubstituted aryl, or alkylaryl...
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6770652 |
Multiple acting anti-angiogenic and cytotoxic compounds and methods for using the same
This invention discloses pyrrolo pyrimidine compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, of the following formula (3): These compounds are useful in...
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6765008 |
Pyrrolopyrimidines as CRF antagonists
The compounds of the formula wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein, are useful in the treatment of stress-related and other diseases. These compounds have...
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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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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6734185 |
Pyrrolo&lsqb 3,4-d&rsqb pyrimidines as corticotropin releasing factor (CRF) antagonists
Corticotropin releasing factor (CRF) antagonists of Formula (II) and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of...
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6727257 |
5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human α 1C receptors. This invention is also related to...
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6713474 |
Pyrrolopyrimidines as therapeutic agents
Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the...
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6680324 |
Compounds specific to adenosine A1 receptors and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A 1 receptor and the use of these compounds to treat a disease associated with A 1 adenosine receptors in a subject.
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6630476 |
Pyrrolo &lsqb 3,4-d&rsqb pyrimidines as corticotropin releasing factor (CRF) antagonists
Corticotropin releasing factor (CRF) antagonists of Formula (I) or (II) and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of...
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6617330 |
Pyrimidin-4-enamine as fungicide
Novel pyrimidine derivatives of formula I as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants...
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6541481 |
Substituted bicyclic derivatives useful as anticancer agents
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R 1 , R 3 and R 4 are as defined herein. The invention also...
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6489333 |
Integrin antagonists
This invention relates to novel heterocycles which are useful as antagonists of the α v β 3 integrin, the α 2b β 3 integrin, and related cell surface adhesive protein receptors, to...
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6465507 |
3-(pyrolyllactone)-2-indolinone compounds as kinase inhibitors
The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to...
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6458799 |
Deazaguanine analog, preparation thereof and use thereof
1-C-(9-deazaaden-9-yl)-1,4-imino-D-5′-deoxy-5′-methylthi
oribitol) and pharmaceutically acceptable salts thereof are useful for inhibiting MTAP and treating cancer. A method for preparing the...
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6436932 |
Aminoalkyl substituted pyrrolo&lsqb 3,2-e&rsqb pyridine and pyrrolo&lsqb 2,3-b&rsqb pyrimidine derivatives: modulators of CRF1 receptors
Disclosed are compounds of the formula: wherein Ar, Q 1 , Q 2 , R 1 , W and X are substituents as defined herein, which compounds are water-soluble CRF 1 receptor antagonists, and are therefore...
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6413971 |
Fused bicyclic pyrimidine derivatives
The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and Z are as defined herein. The invention also relates to pharmaceutical...
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6395733 |
Heterocyclic ring-fused pyrimidine derivatives
The present invention relates to heterocyclic ring-fused pyrimidine derivatives of formula (I) or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, wherein Z and Y are as...
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6384041 |
Bicyclic sPLA2 inhibitors
The compounds are of the class of pyrrolo[2,3-d]pyrimidines useful for inhibiting sPLA 2 mediated release of fatty acids for treatment of diseases such as septic shock.
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6342501 |
Pyrrolo&lsqb 2,3-d&rsqb pyrimidines as antiviral agents
This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and...
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6310063 |
Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors
Disclosed are compounds of the formula: ##STR1## wherein Ar, Q 1 , Q 2 , R 1 , W and X are substituents as defined herein, which compounds are water-soluble CRF 1 receptor antagonists, and are...
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6306863 |
Pyrrolo[3,4-d]pyrimidinone derivatives and their use as medicaments
Compounds of the formula ##STR1## W, Q, R 1 , R 2 and R 10 are as defined in the specification. A process for their preparation and pharmaceutical compositions and methods of treatment involving...
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