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Class 544/271 - Having -C(=X)-, wherein X is chalcogen attached directly or indirectly to the purine ring system by nonionic bonding or halogen bonded directly at 8-position (e.g., theophylline acetate, 8-chlorotheophylline, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein either a group, in which X is chalcogen
No. of patents: 145
Last issue date: 03/08/2011


1        
NumberTitleIssue Date
7902360Aadenosine receptor antagonists
wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene. The present in...
03/08/2011
74079558-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs t...
08/05/2008
7317017Aadenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract dis...
01/08/2008
7312223Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. ...
12/25/2007
7307166Oxpurine nucleosides and their congeners, and acyl, derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoiet...
12/11/2007
7304070Aadenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract di...
12/04/2007
7247639A1 adenosine receptor antagonists
The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceut...
07/24/2007
7235538Heterocyclic 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 R1, R2, R3
06/26/2007
7148229Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl sub...
12/12/2006
7135475Amide substituted xanthine derivatives
The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specificat...
11/14/2006
7125993Aadenosine receptor antagonists
Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):
10/24/2006
7105665Aadenosine receptor antagonists
Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastro...
09/12/2006
7074923Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof
A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to sy...
07/11/2006
7074798Xanthine derivative and DPPIV inhibitor
The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula: wherein, m is 0 or 1; n is 0; R3...
07/11/2006
7053096Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. ...
05/30/2006
7005430Fused purine derivatives
A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a sub...
02/28/2006
7002012Substituted (1,3-bis(cyclohexylmethyl)-1,2,3,6-tetrahydro-2,6-dioxo-9h-purin-8-YI)phenyl derivatives, their preparation and their use in the treatment of inflammatory conditions and immune disorders
A method for the prophylaxis of an inflammatory condition or immune disorder associated with infiltration of leukocytes into inflamed tissue in a subject in need thereof, which method comprises administering to the subject a therapeutically effective amount of a com...
02/21/2006
6998484Synthesis of purine locked nucleic acid analogues
The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic ...
02/14/2006
6977300A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorder...
12/20/2005
6943167Helix mimetics and composition and methods related thereto
Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, where...
09/13/2005
6869974Pharmaceutical compounds
Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1
03/22/2005
6825349A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists compounds having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal trac...
11/30/2004
6780865Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. The disclosed compounds have a structure of formula I: ...
08/24/2004
6734187Purine derivatives and medicaments comprising the same as active ingredient
Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl gr...
05/11/2004
6723727Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them
The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their p...
04/20/2004
6649600Adenosine 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 A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of n...
11/18/2003
6608069Phenyl xanthine derivatives
The present invention relates to novel compounds of formula (I): ##STR1## wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally co...
08/19/2003
6605600Adenosine 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 A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of nu...
08/12/2003
6545002Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors
The present invention provides compounds having the formula I: ##STR1## X is (C1 -C8)alkylene, (C2 -C8)alkenylene, (C2 -C8)alkynylene, wherein one of the carbon atoms in the alkylene, alken...
04/08/2003
6518425Method of manufacture of 1,3-oxathiolane nucleosides
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the process...
02/11/2003
6495687A1 adenosine receptor antagonists
A compound useful as an A1 adenosine receptor antagonist has the formula: ##STR1## wherein R1 is selected from the group consisting of C1 -C8 alkyl; R2 is of the formula: ##STR2## R3 i...
12/17/2002
6489332A1 adenosine receptor antagonists
A compound useful as an A1 adenosine receptor antagonist has the formula: ##STR1## wherein R1 is selected from the group consisting of C1 -C8 alkyl; R2 is of the formula: ##STR2## wherein is an integ...
12/03/2002
6465650Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof ##STR1## wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B' is a base customary in nucleot...
10/15/2002
6455534Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
Described are compounds and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: ##STR1## where: one of A or E is nitrogen, with rema...
09/24/2002
6437124Substituted (1,3-bis(cyclohexylmethyl)-1,2,3,6-tetrahydro-2,6-dioxo-9h-purin-8-yl) phenyl derivatives, their preparation and their use in the treatment of inflammatory conditions and immune disorders
The present invention provides a compound of formula (I) ##STR1## or a solvate thereof wherein: X is --O-- or --NH--; Q is (--CH2 --)p, (--CH.dbd.CH--)p, (--C.ident.C--)p where p is an integer of from 0 to 4; R1...
08/20/2002
6413975Purine derivatives having phosphodiesterase iv inhibition activity
Disclosed are compounds of the formula: ##STR1## wherein R3, R6a, R6b and R8 are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need thereof....
07/02/2002
6355646Substituted (1,3-bis(cyclohexylmethyl)-1,2,3,6-tetrahydro-2,6-dioxo-9H-purin-8-yl)phen yl derivatives, their preparation and their use in treatment of inflammatory conditions and immune disorders
The present invention provides a compound of formula (I) ##STR1## or a solvate thereof wherein: X is --O-- or --NH--; Q is (--CH2 --)p, (--CH.dbd.CH--)p, (--C.ident.C--)p where p is an integer of from 0 to 4; R1...
03/12/2002
6297377Benzocycle-substituted triazine and pyrimidine ultraviolet light absorbers
This invention relates generally to benzocycle-substituted pyrimidines and triazines and the use thereof to protect against degradation by environmental forces, inclusive of ultraviolet light, actinic radiation, oxidation, moisture, atmospheric pollutants...
10/02/2001
62588096-aryloxy and arylthiopurines
Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ...
07/10/2001
6252075Process for producing purine derivatives
A process for preparing 7-benzylpurine derivatives is provided. An acetylpurine nucleoside is reacted with a benzyl halide to benzylate the 7-position of the purine base, and an acid is then added to the reaction mixture to hydrolyze the glycoside bond. T...
06/26/2001
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