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Class 514/263.22 - The additional hetero ring is six-membered consisting of one nitrogen and five carbons


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring is
No. of patents: 204
Last issue date: 01/31/2012


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NumberTitleIssue Date
81060608-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals
The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof. ...
01/31/2012
80674266-amino-purin-8-one compounds
Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and s...
11/29/2011
7985754Selective antagonists of Aadenosine receptors
The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A...
07/26/2011
7884110Fused heteroaryl pyridyl and phenyl benzenesuflonamides as CCR2 modulators for the treatment of inflammation
Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the ...
02/08/2011
7838529Xanthine derivates, their preparation and their use in pharmaceutical compositions
Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted by R10 and R11 and R2 to R4 and R
11/23/2010
7696212Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, whic...
04/13/2010
76120792,6,9-substituted purine derivatives and their use in the treatment of proliferative disorders
The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein ...
11/03/2009
7582642Purine derivatives
The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H;
09/01/2009
7569574Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts ther...
08/04/2009
7544689Purine derivatives
The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H;
06/09/2009
7514444Inhibitors of bruton's tyrosine kinase
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include th...
04/07/2009
7495005Xanthine derivatives, their preparation and their use in pharmaceutical compositions
Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, par...
02/24/2009
7470696Tyrosine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. ...
12/30/2008
7452894Purine derivatives as purinergic receptor antagonists
Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2
11/18/2008
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
7429595Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents
The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4 -diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)2—, and ...
09/30/2008
7423041A1 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 described. ...
09/09/2008
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
7388002Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
Compounds represented by the formula: A is (CH2)nR2, —CH═CH2, CH2—CH═CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)...
06/17/2008
7368438Non-nucleotide compositions and method for inhibiting platelet aggregation
This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharm...
05/06/2008
7365083Amide derivatives as NMDA receptor antagonists
Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4
04/29/2008
7361670Amide derivatives as NMDA receptor antagonists
Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3
04/22/2008
7358235Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition...
04/15/2008
73483301-azabicyclo [2,2,2] octan-3-one derivatives
The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activ...
03/25/2008
7342006Substituted 8-heteroaryl xanthines
Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents. ...
03/11/2008
73356558-heteroaryl xanthine adenosine Areceptor antagonists
The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, ox...
02/26/2008
7335648Non-nucleotide composition and method for inhibiting platelet aggregation
This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a compounds usefu...
02/26/2008
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
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
7279488Imidazopyridine-derivatives as inducible no-synthase inhibitors
The compounds of Formula (I) in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors. ...
10/09/2007
7268141Xanthine 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:
09/11/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
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
7223738Inhibitors of Akt activity
The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
05/29/2007
7217702Selective antagonists of A2A adenosine receptors
Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and o...
05/15/2007
7208502Methods of treating conditions associated with an Edg-3 receptor
In one aspect, the present invention provides a method of modulating an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with a modulator of the Edg-3 receptor sufficient to modulate the Edg-3 receptor mediated...
04/24/2007
7202252Aadenosine 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 described. ...
04/10/2007
7192952Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that a...
03/20/2007
7189730Aadenosine receptor antagonists
Disclosed are novel A2A adenosine receptor antagonists of the formula: wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl;
03/13/2007
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