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Class 544/270 - Plural ring nitrogens in the additional hetero ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring contains at
No. of patents: 74
Last issue date: 09/16/2008


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NumberTitleIssue Date
7425560Thioxanthine derivatives as myeloperoxidase inhibitors
There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for t...
09/16/2008
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
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
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
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
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
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
72054038-Heteroaryl xanthine adenosine Areceptor antagonists
The present invention relates generally to compounds of the formula (I): wherein: X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected f...
04/17/2007
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
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
7037916Pyrimidine derivatives as IL-8 receptor antagonists
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q...
05/02/2006
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
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
6774130Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same
Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intrace...
08/10/2004
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
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
6221874Method of treating bone loss by stimulation of calcitonin
Compounds of the formula ##STR1## R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon ...
04/24/2001
6175008Processes 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 R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO2...
01/16/2001
61660231,5- and 3-O-substituted 1H-indazoles having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments
The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##...
12/26/2000
6124288Xanthines 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 consisting of C1-6 alkyl (optionally substi...
09/26/2000
6103730Amine 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 compounds, j is an integer from one to three; the core moiet...
08/15/2000
6090816Aryl thioxanthines
Disclosed are compounds having the formulae: ##STR1## wherein: Q3,Q6a,Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-6 alkynylene, and R3, ...
07/18/2000
6075029Xanthine 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 compounds generally are useful in affecting drug metabolism ...
06/13/2000
6066641Aryl thioxanthines
The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q3 R3 and Q8 R8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with reg...
05/23/2000
6043228O6 -substituted guanine derivatives, a process for their preparation and their use in treating tumor cells
O6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR', wherein X is O or S, R" and R"' are alkyl, or substituted derivatives thereof, R' is H, or alkyl or hydroxyalkyl R ...
03/28/2000
5994361Substituted purinyl derivatives with immunomodulating activity
The present invention comprises a compound of formula I: ##STR1## R1 of Formula I is substituted amino represented by formula NR5 R6 wherein R5 and R6 are independently selected from the group co...
11/30/1999
5919789Xanthines and their therapeutic use
Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase....
07/06/1999
5821366Xanthines and their therapeutic use
1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition....
10/13/1998
5807854Pyrimidone 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 compounds and processes for their preparation are also prov...
09/15/1998
5756735Xanthine derivatives
The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R1
05/26/1998
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