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7361662 |
Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same
A compound of formula (I):
wherein:
R 1 , R 2 , R 3 , R 4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a pharmaceutically...
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7348331 |
Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
Compounds of the Formula:
where X 1 , Ar 1 , R 1 , and R 2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in treating...
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7329664 |
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and...
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7323472 |
2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof.
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7279484 |
Heterocyclic compounds
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I)
wherein R is an alkyl group optionally...
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7235551 |
1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
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7232824 |
Quinazoline derivatives as medicaments
Quinazoline derivatives have the formula:
or the pharmaceutically acceptable salts thereof; wherein each of Z 5 , Z 6 , Z 7 and Z 8 is N or CH and wherein one or two Z 5 , Z 6 , Z 7 and...
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7208489 |
2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
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7202249 |
Antagonists of chemokine receptors
Compounds are provided which are antagonists of chemokine receptor activity. The compounds thereof have the structure
including enantiomers, diastereomers, tautomers, pharmaceutically...
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7189732 |
Pyrido[2,3-d]pyrimidine dichloro-phenyl derivatives
The invention describes compounds of the general formula I
a process for their manufacture, compositions containing them and their manufacture as well as the use of these compounds as...
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7189731 |
Substituted 7-azaquinazoline compounds useful as p38 kinase inhibitors
Compounds having the formula (I) or (II),
are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R 6 is hydrogen or lower alkyl; R 7 is...
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7163941 |
Pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents
The invention describes compounds of the general formula I
a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as...
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7157466 |
Quinazoline ditosylate salt compounds
Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.
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7141576 |
Cancer treatment method
A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as pharmaceutical combinations and compositions...
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RE39266 |
Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their...
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7074799 |
Substituted quinazolin-4-ylamine analogues
Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the...
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7053070 |
Pyrido[2,3-d]pyrimidine-2,7-diamine kinase inhibitors
Disclosed are compounds of the formula
wherein R 2 , R 5 , R 6 , R 7 , and R 8 are as defined herein. These compounds and their pharmaceutical compositions are useful for treating cell...
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7022711 |
2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones
This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis,...
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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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7008948 |
Fused pyrimidyl pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV:
wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or...
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6927220 |
Bicyclic-substituted 4-amino-pyridopyrimidine derivatives
The invention relates to 6- or 7-bicyclic-substituted 4-amino-subsituted pyridopyrimidines and to pharmaceutically acceptable salts, prodrugs and hydrates thereof. The invention also relates to...
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6903096 |
Quinazoline derivatives as medicaments
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula
or the pharmaceutically acceptable salts thereof
wherein R 3 is a...
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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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6861423 |
Methods of treating p38 kinase-mediated disorders with pyrido[2,3-d]pyrimidin-7-one compounds
Disorders mediated by p38 kinase inhibitors are treated with compounds of the formula:
or salts thereof, wherein: R 1 is hydrogen or alkyl; R 2 is substituted cycloalkyl,...
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6784174 |
Pyridine and pyrimidine derivatives and their use as inhibitors of cytokine mediated disease
This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from...
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6730682 |
Heterocycle carboxamides as antiviral agents
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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6602863 |
Irreversible inhibitors of tyrosine kinases
The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and...
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6545001 |
Antiviral nucleoside analogues
The invention relates to cis-nucleosides of formula (I): and pharmaceutically acceptable salts thereof, wherein X, R 3 , R 4 and are as defined herein. The nucleosides can be in racemic form or...
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6506749 |
7-oxo-pyridopyrimidines (I)
The present invention provides compounds of the formula: wherein R 2 is substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted...
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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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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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6245770 |
Fungicidal pyrimidinones
Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## wherein W is O, S(O) n or NR 5 ; n is 0, 1 or 2; Q is...
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6114339 |
Derivatives of pyrido [2,3-D] and [3,2-D] pyrimidine method of using these derivatives
The invention also discloses compounds and pharmaceutically acceptable salts having the generic formula (2) ##STR1## wherein X and Y may be the same or different and are selected from the group...
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6066639 |
5,6,7,8-tetrahydropyrido[2,3-D]pyrimidines
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6030969 |
5,6,7-trisubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
A compound having the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined, a method for inhibiting adenosine kinase by administering a compound thereof, a pharmaceutical...
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5952342 |
6-aryl naphthyridines for inhibiting protein tyrosine kinase mediated cellular proliferation
6-Aryl naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating...
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5945422 |
N-oxides of amino containing pyrido 2,3-D! pyrimidines
N-oxides of amino containing 6-aryl pyrido 2,3-d!-pyrimidine 7-imines, 7-ones, and 7-thiones have the formula ##STR1## where A and B are linkers, Ar is aryl, R 2 is aklyl, X is O, S, or NH, or...
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5900428 |
Pharmacological use of AII-receptor antagonists
A method for the prophylaxis and treatment of MOF using certain angiotensin II type 1 receptor antagonists and a pharmaceutical preparation comprising these compounds.
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5889025 |
Antidiabetic compounds having hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
Novel antidiabetic compounds, their tautomeric forms, their derivatives, their steroisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates...
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5786358 |
Pyridopyrimidines as nonclassical antifolates
2-Amino-4-hydroxy-4,5,6,7-tetrahydropyrido 2,3-d!pyrimidine derivatives of aromatic amides, such as a benzamide or thienylcarboxamide in which the amino portion of the amide is other than...
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5733914 |
Pyrido 2, 3-d!pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
6-Aryl pyrido 2,3-d!pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are...
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5733913 |
6-Aryl pyrido 2,3-d! pyrimidines and naphthyridines for inhibiting protein tyrosine kinase mediated cellular proliferation
6-Aryl pyrido 2,3-d!pyrimidines and naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially...
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5710157 |
2,4-diamino-5,6-disubstituted-and 5,6,7-trisubstituted-5-deazapteridines as insecticides
An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 5-deazapteridine compound of the formula: ##STR1## wherein R...
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5688800 |
Condensed pyrimidine derivative
A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R 1 ...
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5639753 |
Insecticidal pteridines and 8-deazapteridines
This invention relates to pteridine and 8-deazapteridine compounds and compositions containing the same which are useful for controlling insects in agricultural crops. These pteridines may be...
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5620981 |
Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are...
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5536724 |
Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins
Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins and their 5 and 10 alkyl analogs. A method for the treatment and prevention of inflammatory disease, such as...
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5521190 |
Insecticidal pterdines and 8-deazapteridines
This invention relates to pteridine and 8-deazapteridine compounds and compositions containing the same which are useful for controlling insects in agricultural crops. These pteridines may be...
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5405848 |
Substituted thiazolylaminotetrahydropyridopyrimidines derivatives useful as platelet aggregation inhibitors
This invention relates to substituted thiazolylaminotetrahydropyridopyrimidines derivatives of the following general formula, the substituent groups of which are as defined in the specification...
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5385906 |
Antibacterial quinolone compounds
A quinolone compound of Formula (I) ##STR1## as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial...
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