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Class 514/217.05 - Plural ring hetero atoms in the additional hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter under 217.04 wherein the additional hetero
No. of patents: 304
Last issue date: 04/24/2012


1                
NumberTitleIssue Date
8163734Use of a mast cell activation or degranulation blocking agent in the manufacture of a medicament for the treatment of a patient subjected to thrombolyses
The invention concerns the use of a mast cell activation- or degranulation-blocking agent in the manufacture of a medicament for preventing and treating cerebral complications caused by thrombolytic treatment. The invention also relates to treatment of patients suff...
04/24/2012
7803795Phthalazine derivatives as parp inhibitors
The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanin...
09/28/2010
7745427CGRP receptor antagonists
The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in...
06/29/2010
7709468Imidazo based heterocycles
The present invention is directed to novel imidazopyrazine and imidazopyrimidine compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such...
05/04/2010
7704995Protein kinase modulators and methods of use
This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such com...
04/27/2010
7648978Small molecule modulators of cytokine activity
The present invention provides compounds having formula (I) or (II): and pharmaceutically acceptable derivatives thereof, wherein m, p, R1, R2, R3 and R4 ...
01/19/2010
7642252Angiogenesis inhibition by cephalotaxine alkaloids, derivatives, compositions and uses thereof
The invention relates to compositions and methods useful in treating or preventing angiogenic disease. The invention provides for compositions comprising cephalotaxine alkaloids as antiangiogenic agents for treatment of a host with an angiogenic disease or for proph...
01/05/2010
7514424Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NKËœantagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular fo...
04/07/2009
74949902-(piperidin-4-yl)-4,5-dihydro-2H-pyridazin-3-one derivatives as PDE4 inhibitors
The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors. ...
02/24/2009
74322551H-indol-5-yl-piperazin-1-yl-methanone derivatives
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds...
10/07/2008
7427612Benzoyl-piperazine derivatives
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in ...
09/23/2008
74230301-amino-phthalazine derivatives, the preparation and the therapeutic use thereof
A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments u...
09/09/2008
7414047Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
08/19/2008
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7390799Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed. ...
06/24/2008
7368445Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms
The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds. ...
05/06/2008
7365063Quinazolinone and benzoxazinone derivatives and uses thereof
Compounds of the formula I: and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CRaRb)r—, A is —NR3, m is 2, n is 1, q is 2, R2 is optioi...
04/29/2008
7351708Pyrrolo [2,3-b] pyridine derivatives
The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the tr...
04/01/2008
7348323Pyrrolo [2,3-c] pyridine derivatives
The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the tr...
03/25/2008
7323456Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient
A compound of formula (I) (wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a ...
01/29/2008
7319097Compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
01/15/2008
7309707Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament
The invention relates to a crystalline micronisate of (1α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition...
12/18/2007
7309800Biphenylcarboxylic amide derivatives as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
12/18/2007
73070791,3,5-Triazine derivatives as ligands for human adenosine-A3 receptors
The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingre...
12/11/2007
7304052Substituted homopiperidinyl benzimidazole analogues as fundic relaxants
The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres...
12/04/2007
7304051Quinoxaline compounds
Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases. ...
12/04/2007
7300941Non-imidazole compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
11/27/2007
7279470Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may...
10/09/2007
7253204Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and cond...
08/07/2007
7247623Method of treating dry eye disease with non-drying antihistamines
A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the eyes of the subject a non-drying antihistamine compound, such as epinastine hydrochlori...
07/24/2007
7238688Piperidine compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
07/03/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
72086295′-Carbamoyl-1,1-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, â€...
04/24/2007
7196087Quinazolinone and benzoxazinone derivatives and uses thereof
Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—,...
03/27/2007
7183297Biphenyl-derivatives as p38-kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
02/27/2007
7179803Method of modulating ion channel functional activity
The present invention relates generally to a method of retarding, reducing or otherwise inhibiting viral functional activity and, more particularly, to a method of reducing, retarding or otherwise inhibiting viral functional activity by down-regulating Vpu ion chann...
02/20/2007
7173032Methods and compositions of novel triazine compounds
The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced...
02/06/2007
71666232′-Methyl-5′-(1,3,4-oxadiazol-2-yl)-1,1′-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
01/23/2007
7151118Biphenylcarboxylic amide derivatives as p38-kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
12/19/2006
7151097Bicyclic pyrazolyl and imidazolyl compounds and uses thereof
Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid...
12/19/2006
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