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Class 544/118 - Four or more ring nitrogens in the bicyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system cont
No. of patents: 219
Last issue date: 12/13/2011


1            
NumberTitleIssue Date
8076476Synthesis of morpholino oligomers using doubly protected guanine morpholino subunits
Morpholino compounds are provided having the structure: where R1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R2...
12/13/2011
7759485Process for the manufacture of dihydropteridinones
Disclosed are processes for preparing dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and in the specification. ...
07/20/2010
7700768Compounds
Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
04/20/2010
7479558Process for preparing pyrido[2,3-]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-]pyrimidin-2(1)-one derivatives
The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 o...
01/20/2009
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
7435731Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same
Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R1, R2, R3, R4 and R5 are those defined herein, and compositions comprising the same. The present invent...
10/14/2008
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
7423038Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d...
09/09/2008
7414053Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f...
08/19/2008
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
7371753Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and sp...
05/13/2008
7371750Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d...
05/13/2008
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
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
7332486Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/19/2008
7332491Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specificat...
02/19/2008
73148712-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors, for treatment of hypertension
The application claims a method for treating hypertension by administering an effective amount of a compound of the formula (I) wherein the variable groups are as defined in the specification and claims. These 2-...
01/01/2008
7273864Compositions and methods for inducing osteogenesis
The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: wherein R4 ...
09/25/2007
7268133Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...
09/11/2007
7268136Compositions useful as inhibitors of protein kinases
The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of PIM-...
09/11/2007
72681281,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action
Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively in...
09/11/2007
7265111Adenosine analogues and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are indepe...
09/04/2007
7262192Substituted pyrazolo[4,3-d]pyrimidines and their use as PDE-5 inhibitors
The present invention comprises a class of 5,7-diaminopyrazolo[4,3-d]pyrimidine compounds. These compounds are useful as phosphodiesterase type 5 inhibitors. The present invention further comprises compositions containing the compounds use of the compounds and compo...
08/28/2007
7256196Purine cytokine inhibitors
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions c...
08/14/2007
72355511,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
06/26/2007
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
7217711Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R1 to R3 and n are defined as in claims 1 to 8, the tautomers, enantiomer...
05/15/2007
7217710Substituted pyrazolopyrimidines
Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases. ...
05/15/2007
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
7211381β2 andrenergic polymorphism detection
Nucleic acid sequences are provided that are useful as amplification primers and hybridization probes for amplifying and detecting target sequence from the β2 adrenergic receptor gene. The primers and probes can be employed in amplification based methods for detect...
05/01/2007
7208628Compositions and methods for the treatment of hepatitis C virus infection
This invention relates to methods and compositions directed towards the diagnosis and treatment of Hepatitis C virus infection and the screening of potential therapeutic compounds using novel small molecules based on imidazole-4,5-dicarboxylic acids scaffolds. ...
04/24/2007
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
71798092-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions
The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 t...
02/20/2007
7176311Process for preparing pharmaceutically active compounds
A process for the preparation of Compounds of the formula (1): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymo...
02/13/2007
7157448Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
The present invention relates to a nucleoside phosphonate derivative represented by formula (1): pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is useful as an antivi...
01/02/2007
7129239Purine compounds and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. ...
10/31/2006
7122665Heterocyclic compounds
This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb
10/17/2006
71225402-Phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizi...
10/17/2006
7094765Antisense restenosis composition and method
The present invention provides an improved method for reducing the risk or severity of restenosis following cardiac angioplasty. The method includes administering to a target vessel region, a morpholino antisense compound having uncharged phosphorus-containing backb...
08/22/2006
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