Class 514/234.2 - Three or more ring hetero atoms in the bicyclo ring system

Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the bicyclo ring system contains
No. of patents: 454
Last issue date: 05/08/2012

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Number	Title	Issue Date
8173650	Bicyclic pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2	05/08/2012
8168633	Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating diseases and disorders arising from abnormal cell growth, function or behavior associated with...	05/01/2012
8158625	Bicyclic indole-pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 i...	04/17/2012
8158626	Thiazolopyrimidine PI3K inhibitor compounds and methods of use Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediate...	04/17/2012
8158624	Purine PI3K inhibitor compounds and methods of use Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating d...	04/17/2012
8153628	Pyrazolyl substituted xanthines The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected f...	04/10/2012
8148371	Adenine compound and use thereof A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ri...	04/03/2012
8143249	Prodrugs of Aadenosine receptor antagonists Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted...	03/27/2012
8114871	3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention...	02/14/2012
8097621	Pyrazolo[4,3-d]pyrimidines as phosphodiesterase inhibitors This invention relates to compounds of formula (I) ...	01/17/2012
8097622	Morpholinopurine derivatives There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various ...	01/17/2012
8097620	Diazaquinolones that inhibit prolyl hydroxylase activity Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein. ...	01/17/2012
8080546	Pyrazolo-pyridinone derivatives and methods of use The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I...	12/20/2011
8080547	Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention furth...	12/20/2011
8071593	2-oxo-3-benzylbenzoxazol-2-one derivatives and related compounds as Met kinase inhibitors for the treatment of tumours Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]...	12/06/2011
8067413	9-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7 ) modulators The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as...	11/29/2011
8053434	Kinase inhibitors and their uses The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropria...	11/08/2011
8048879	Substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compounds and use thereof for producing medicaments The present invention relates to substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compound corresponding to formula I, methods for producing them, to medicaments containing these compounds, the use of these compounds for producing medicaments and related trea...	11/01/2011
8026236	6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for t...	09/27/2011
8017605	P38 kinase inhibiting agents Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid ...	09/13/2011
8012964	9-substituted 8-oxoadenine compound The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1):	09/06/2011
7968544	Modulators of toll-like receptor 7 The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administrati...	06/28/2011
7951803	8-heteroarylpurine MNK2 inhibitors for treating metabolic disorders Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroa...	05/31/2011
7947679	Fungicides The naphthyridine derivatives of formula (I) a and method of combating or controlling phytopathogenic fungi which comprises applying the compounds of formula (I) to a plant, to a seed of a plant and to the locus of the plant. ...	05/24/2011
7939527	Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatmen...	05/10/2011
7932251	6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for t...	04/26/2011
7932250	Thienopyrazole derivative having PDE7 inhibitory activity To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The c...	04/26/2011
7893060	Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is...	02/22/2011
7893059	Thiazolopyrimidine PI3K inhibitor compounds and methods of use Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediate...	02/22/2011
7884100	Substituted 8-[6-amino-3-pyridyl]xanthines The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptor...	02/08/2011
7879850	Organic compounds The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans. ...	02/01/2011
7875608	Substituted 8-[6-amino-3pyridyl]xanthines The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptor...	01/25/2011
7868002	Deazapurines and uses thereof As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I),	01/11/2011
7855202	Imidazopyridine derivatives as Aadenosine receptor antagonists The present disclosure relates to imidazopyridine derivatives of formula (I): The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to ameliora...	12/21/2010
7846928	Substituted pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined...	12/07/2010
7846927	N,N′-diphenylurea derivatives suitable as kinase inhibitors Compounds of the formula (I), in which R1, R3 and X have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.	12/07/2010
7829558	Fused ring heterocycle kinase modulators The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity. ...	11/09/2010
7825114	Substituted aminopyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same The invention relates to substituted aminopyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as de...	11/02/2010
7799781	5,6,7,8-tetrahydropteridine derivatives as HSP90 inhibitors The present invention relates to compounds that inhibit HSP90 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in t...	09/21/2010
7795257	Organic compounds The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the co...	09/14/2010

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Class 514/234.2 - Three or more ring hetero atoms in the bicyclo ring system