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Class 514/263.1 - Purine (including hydrogenated)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system is the
No. of patents: 77
Last issue date: 03/20/2012


1    
NumberTitleIssue Date
8138195Inhibitors of human phosphatidylinositol 3-kinase delta
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ ac...
03/20/2012
7968555Intermediates in the preparation of entecavir via carbon-silicon oxidation
Processes for preparing entecavir and novel intermediates thereof using carbon-silicon oxidation. ...
06/28/2011
7879863Aniline derivatives
The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined...
02/01/2011
7696211Methods and pharmaceutical compositions for treating sepsis
Methods and compositions for treating and preventing sepsis are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist in combination with an antibiotic agent. The inventio...
04/13/2010
7569573Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase
A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS a...
08/04/2009
7439240Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity
The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases ...
10/21/2008
7432272Antiviral analogs
The application relates to 4′-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such compounds, to meth...
10/07/2008
73938552,2-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 6-aminopurine (adenine), 6-hydroxypurine (...
07/01/2008
73717372-substituted-6-trifluoromethyl purine derivatives with adenosine-Aantagonistic activity
The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful fo...
05/13/2008
73616618-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alken...
04/22/2008
7335654Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/26/2008
7300923Partial and full agonists of A1 adenosine receptors
Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infa...
11/27/2007
7285558Pyrazolo[3,4-d]pyrimidines inhibiting infections
Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection. ...
10/23/2007
7271157Aadenosine receptor agonists
Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally subst...
09/18/2007
7253175Method for treating athlete's foot
A method of treating a patient having a fungal infection comprises administering an effective fungal infection treatment amount of an antiviral agent, such as valacyclovir, to eliminate the symptoms of the fungal infection. ...
08/07/2007
7253154Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which m...
08/07/2007
7230000Methods and compositions utilizing quinazolinones
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...
06/12/2007
7211667Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of m...
05/01/2007
7148226Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The ...
12/12/2006
7005425Method for treating arrhythmias
Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a ...
02/28/2006
6946449Partial and full agonists of A1 adenosine receptors
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction. ...
09/20/2005
6936618Cystic fibrosis medicaments
The use of a type V cyclic nucleotide phosphodiesterase inhibitor for the preparation of a medicament for the treatment of cystic fibrosis. ...
08/30/2005
6894021Method for identifying and using A2B adenosine receptor antagonists to mediate mammalian cell proliferation
This invention concerns methods for identifying A2B adenosine receptor agonists and antagonists as well as methods for using A2B adenosine receptor antagonists to treat cell proliferation orders mediated by the A2B adenosine receptor...
05/17/2005
6841549Condensed imidazole compounds and a therapeutic agent for diabetes mellitus
The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an ...
01/11/2005
6821978Xanthine phosphodiesterase V inhibitors
A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
11/23/2004
6740654Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —Sâ€...
05/25/2004
6734186Compounds for the treatment of female sexual dysfunction
A method of treating a female suffering from FSD, in particular FSAD, is described. The method comprises delivering to the female an agent that is capable of potentiating cAMP in the sexual genitalia; wherein the agent is in an amount to cause potentiation of cAMP i...
05/11/2004
6710051Screening method
The invention relates to a method for identification of substances which are applicable for treatment or prevention of an insufficient longitudinal growth of the eye (hypermetropia) or for treatment or prevention of an excessive longitudinal growth of the eye (myopi...
03/23/2004
6680302Methods of optimizing drug therapeutic efficacy for treatment of immune-mediated gastrointestinal disorders
The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the inventio...
01/20/2004
6653309Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for inhibit...
11/25/2003
6653301Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IIa: ##STR1## wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R
11/25/2003
6599907Cystic fibrosis medicaments
A method of treating cystic fibrosis in a patient comprising: administering to said patient an effective amount of a type V cyclic nucleotide phosphodisterase inhibitor, wherein said inhibitor is a compound of formula (I): ##STR1## wherein A is a five- or six...
07/29/2003
6599926Heteroaryl-phenyl substituted factor Xa inhibitors
The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa....
07/29/2003
65766283-aryl-succinamido-hydroxamic acids, methods for producing said acids and medicaments containing the same
The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) ##STR1## and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharma...
06/10/2003
6545001Antiviral nucleoside analogues
The invention relates to cis-nucleosides of formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein X, R3, R4 and are as defined herein. The nucleosides can be in racemic form or in the form of their (+) or (-) e...
04/08/2003
6537974Method of treating arrhythmias
A method for treating arrhythmia in mammals is provided comprising administering a low dose of an adenosine receptor agonist of the Formula I: ##STR1## wherein R1 is an optionally substituted heterocyclic group, preferably monocyclic....
03/25/2003
6534512Dideoxycarbocyclic nucleosides
A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is HI OR' or N(R)2, wherein R' is H, (C1 -C4)alkyl, aryl, CHO, (C1 -C16)alkanoyl or O....
03/18/2003
6518277Inhibitors of human phosphatidylinositol 3-kinase delta
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the method...
02/11/2003
6492332Irrigation solution and methods for inhibition of tumor cell adhesion, pain and inflammation
This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell anti-adhesion agent and a plurality of additional agents to an...
12/10/2002
6492393Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammat...
12/10/2002
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