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7569575 Synthesis of locked nucleic acid derivatives  
The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and...
7569574 Purine derivatives, the preparation thereof and their use as pharmaceutical compositions  
The invention relates to new purine derivatives of general formula wherein R 1 to R 4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and...
7560450 Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions  
The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable...
7550455 8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition  
The present invention relates to substituted xanthines of the general formula in which R 1 to R 3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their...
7501426 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions  
Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1 , the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable...
7495004 Purine derivatives as liver X receptor agonists  
The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds of formula (I) for...
7495003 8-(3-amino-piperidin-1-yl)-7-(but-2-ynyl)-xanthines, the preparation thereof and their use as pharmaceutical compositions  
The application relates to new substituted xanthines of general formula wherein R 1 and R 2 are defined as in claims 1 to 11 , the tautomers, the enantiomers, the diastereomers, the...
7495002 3-methyl-7-butinyl-xanthines, the preparation thereof and their use as pharmaceutical compositions  
The present invention relates to new substituted xanthines of general formula wherein R 1 , R 2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the...
7482337 Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions  
Disclosed are substituted xanthines of general formula wherein R 1 to R 4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts...
7423041 A1 adenosine receptor antagonists  
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also...
7317017 A2B adenosine receptor antagonists  
Disclosed are novel A 2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal...
7312223 Metabolite 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...
7307166 Oxpurine 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...
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...
7192962 Xanthine phosphodiesterase V inhibitor polymorphs  
Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4 -methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit...
7135475 Amide substituted xanthine derivatives  
The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are as defined in the specification. ...
7125993 A2B adenosine receptor antagonists  
Disclosed are processes for the synthesis of novel compounds that are A 2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the...
7105665 A2B adenosine receptor antagonists  
Disclosed are methods for making novel A 2B adenosine receptor antagonists having the structure of formula I or Formula II: The compounds are particularly useful for treating asthma,...
7074923 Process 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...
7074798 Xanthine 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; R 31 , R 32 , R 33 ,...
7005430 Fused purine derivatives  
A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R 1 N—C═O or N═C—W, R 2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl...
6998484 Synthesis 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...
6815446 Selective antagonists of A2B adenosine receptors  
A compound of the following formula: wherein R is an aliphatic or cycloaliphatic amine group or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof. The...
6723727 Substituted 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, W a , G and G a have the meanings given in the patent claims, and their physiologically tolerable salts and...
6653312 Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same  
Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.
6649600 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 usefull...
6608069 Phenyl xanthine derivatives  
The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl,...
6605600 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...
6600044 Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers  
A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof,...
6583283 Polymorphic forms of cipamfylline  
This invention relates to novel crystalline polymorphic forms, Form I, II and IV of Cipamfylline, methods of preparation, and use thereof in the treatment of PDE4 and TNF mediated diseases....
6495687 A1 adenosine receptor antagonists  
A compound useful as an A 1 adenosine receptor antagonist has the formula: wherein R 1 is selected from the group consisting of C 1 -C 8 alkyl; R 2 is of the formula: R 3 is of the...
6413975 Purine derivatives having phosphodiesterase iv inhibition activity  
Disclosed are compounds of the formula: wherein R 3 , R 6a , R 6b and R 8 are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need...
6333331 Substituted O6-benzylguanines  
The present invention provides AGT inactivating compounds such as substituted O 6 -benzylguanines of the formula ##STR1## 7- or 9-substituted 8-aza-O 6 -benzylguanines, 7,8-disubstituted O 6 ...
6316457 Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses  
Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NO n -PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such...
6294541 Purine derivatives having phosphodiesterase IV inhibition activity  
A compound of the formula: ##STR1## wherein R 3 represent a C 1 -8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO 2 H, NOH, NOCONH 2 , or...
6252075 Process 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...
6248746 3-(arylalkyl) xanthines  
With the above and other objects in view, the present invention comprises compounds having the general formula (I): ##STR1## wherein: R 1 is a C 2 -8 alkyl, C 2 -8 alkenyl, C 2 -8 alkynyl, C 3...
6245910 Process for producing purine derivatives  
Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of...
6221874 Method of treating bone loss by stimulation of calcitonin  
Compounds of the formula ##STR1## R 1 and R 2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R 3 is hydrogen, alkyl of 1 to 6 carbon atoms,...
6187780 Assymetrically substituted xanthine derivatives having adenosine A1 antagonistic activity  
Asymmetrically substituted xanthine derivatives having adenosine A 1 antagonistic activity. These are useful as pharmaceuticals. Exemplary are: (a)...
6180791 Synthesis of 8-substituted xanthines  
A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or other disorders which method comprises the administration of an effective,...
6175008 Processes for preparing substituted 1,3-oxathiolanes with antiviral properties  
Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R 2 is a purine or pyrimidine base or an analogue or...
6124288 Xanthines and their therapeutic use  
The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group...
6103730 Amine substituted compounds  
Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula: CORE MOIETY--(R) j In these...
6090816 Aryl thioxanthines  
Disclosed are compounds having the formulae: ##STR1## wherein: Q 3 ,Q 6a ,Q 6b and Q 8 are independently a bond, C 1 -8 alkylene, C 2 -8 alkenylene and C 2 -6 alkynylene, and R 3 , R 6a , R 6b...
6069250 Method and compositions for the synthesis of dioxolane nucleosides with β-configuration  
The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to...
6020337 Electronegative-substituted long chain xanthine compounds  
Therapeutic compounds, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, having a formula: ##STR1## wherein R 0 is selected from the group...
5994361 Substituted purinyl derivatives with immunomodulating activity  
The present invention comprises a compound of formula I: ##STR1## R 1 of Formula I is substituted amino represented by formula NR 5 R 6 wherein R 5 and R 6 are independently selected from the...
5981535 Substituted xanthines and their use in the treatment of cerebrovascular disorders and other diseases  
A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or allergic disorders, proliferative skin disorders, and bronchodilation which method...
5965555 Xanthine compounds having terminally animated alkynol side chains  
Compounds of the formula I, ##STR1## in which one of the radicals R 1 and R 3 is an alkynol residue of the formula Ia or Ib ##STR2## are suitable for producing pharmaceuticals having a...
Matches 1 - 50 out of 151 1 2 3 4 >