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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...
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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...
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7550468 |
Theophylline and 3-isobutyl-1 methylxanthine based N-7 substituted derivatives displaying inhibitory activities on PDE-5 phospodiesterase
A variety of N-substituted derivatives are based upon the base chemicals of
that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic...
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7495005 |
Xanthine derivatives, their preparation and their use in pharmaceutical compositions
Compounds of formula (I)
wherein R 1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R 2 to R 4 are defined as in the claims, or the prodrugs or salts thereof,...
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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...
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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...
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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...
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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...
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7148229 |
Sulfonamide 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,...
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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.
...
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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...
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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,...
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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...
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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 ,...
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7053096 |
Compounds 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...
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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...
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7002012 |
Substituted (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...
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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...
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6780865 |
Compounds 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...
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6734187 |
Purine derivatives and medicaments comprising the same as active ingredient
Purine derivatives represented by the following formula and salts thereof: wherein R 1 represents a C 1 -C 4 alkyl group or difluoromethyl group; R 2 represents tetrahydrofuranyl group, a C 1...
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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...
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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...
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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,...
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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...
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6545002 |
Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors
The present invention provides compounds having the formula I: X is (C 1 -C 8 )alkylene, (C 2 -C 8 )alkenylene, (C 2 -C 8 )alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene...
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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...
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6465650 |
Substituted 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 wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH 2 , O,...
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6437124 |
Substituted (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) or a solvate thereof wherein: X is —O— or —NH—; Q is (—CH 2 —) p , (—CH═CH—) p , (—C≡C—) p where p is an integer...
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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...
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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...
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6258809 |
6-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...
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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...
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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...
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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...
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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,...
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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)...
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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...
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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...
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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...
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6100271 |
Therapeutic compounds containing xanthinyl
Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula: CORE MOIETY --(R) j wherein j is an integer from one to three. The core moiety is...
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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...
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6075029 |
Xanthine modulators of metabolism of cellular P-450
A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These...
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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...
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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...
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5968940 |
Retinoids and methods of use of same
New purine retinoid compounds according to the formula: ##STR1## wherein R is a purine derivative, and pharmaceutical compositions thereof, are provided which exhibit cancer-inhibiting activity.
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5922868 |
Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation
Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation. The invention relates to the use of xanthine derivatives of the formula I ##STR1## in...
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5919789 |
Xanthines and their therapeutic use
Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.
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5861405 |
S-substituted 1,3,7-trialkyl-xanthine derivatives
The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A 2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the...
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5861403 |
Purinylalkyl benzamide derivatives
The present invention relates to compounds of the formula ##STR1## wherein HET is ##STR2## m is an integer from 1 to 4; R 1 and R 2 are independently selected from the group consisting of linear...
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5807854 |
Pyrimidone derivatives with antifungal activity
Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these...
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