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Class 514/233.2 - Ring nitrogen shared by two of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which two of the cyclos in the polycyclo
No. of patents: 398
Last issue date: 04/24/2012


1                    
NumberTitleIssue Date
8163741Use of aryl-substituted polycyclic amines as medicaments
The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; whe...
04/24/2012
8148370Polysubstituted derivatives of 2-aryl-6-phenyl-imidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
Compounds of formula (I): wherein R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof...
04/03/2012
8148369Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of c...
04/03/2012
8129374Method of using imidazolothiazole compounds for the treatment of disease
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases. ...
03/06/2012
8106047Triazolophthalazines
The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors. ...
01/31/2012
8088765Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
Compounds of formula (I): wherein R1, R2, R3, R4, Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis th...
01/03/2012
8017604Imidazopyridines
The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, a...
09/13/2011
7943611Imidazo[1,2-A]pyridin-3-yl-acetic acid hydrazides, processes, for their preparation and pharmaceutical uses thereof
The invention provides novel imidazo[1,2-a]pyridin-3-yl-acetic acid hydrazides of formula (I) wherein R1, R2 and R3 have different meanings, and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoi...
05/17/2011
7897600Amino pyrazole compound
The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias. ...
03/01/2011
7893058Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of...
02/22/2011
7868001Cytokine inhibitors
A compound of Formula I: Each variable is defined in the specification. This invention relates to a method of decreasing a level of a cytokine (e.g., TNFα or interlukine such as IL-1β) in a subject with a compound of Form...
01/11/2011
7829556Sirtuin modulating compounds
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, dis...
11/09/2010
7820657Imidazolothiazole compounds for the treatment of disease
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases. ...
10/26/2010
7795255Rigidified compounds for modulating heparanase activity
Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or...
09/14/2010
7781430Benzoxazole carboxamides for treating CINV and IBS-D
Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.
08/24/2010
7763613Substituted N-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid prot...
07/27/2010
7750000Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments
The invention relates to novel inhibitors of kinases, and pharmaceutical compositions comprising them. The inhibitors are substituted imidazo[1,2b]pyridazines. ...
07/06/2010
7713969Compositions and methods for treatment of cancer
The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloq...
05/11/2010
7700593Imidazo- and triazolo-pyridine compounds and methods of use thereof
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wh...
04/20/2010
7687497C10-substituted camptothecin analogs
The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells ...
03/30/2010
7687496C7-substituted camptothecin analogs
The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells i...
03/30/2010
7671050Triazolophthalazines
The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors. ...
03/02/2010
7612067Imidazopyridazine compounds
The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric diso...
11/03/2009
7563788Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I a...
07/21/2009
7501411Triazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment o...
03/10/2009
7498327Indolylalkylamine metabolites as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor. ...
03/03/2009
7419977Imidazoquinoline derivatives as adenosine A3 receptor ligands
This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m...
09/02/2008
7402579Quinobenzoxazine analogs and compositions
The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, ...
07/22/2008
7354918Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected fr...
04/08/2008
7348425Inhibitors of HCV replication
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing ...
03/25/2008
7342012Inhibitors of αβmediated cell adhesion
The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. ...
03/11/2008
7329663Substituted-triazolopyrimidines as anticancer agents
The invention provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pha...
02/12/2008
7323462Morpholine dopamine agonists
Compounds of formula (I), (Ia) and (Ib) useful as a medicament. ...
01/29/2008
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
7279473Pyrazolopyridazine derivatives
Fused pyradazine derivatives which are usefule as CDK inhibitors are described herein. The described invention alos includes methods of making such fused pyradazine derivatives as wells as methods of using the same in the treatment of hyperproliferative diseases.
10/09/2007
7276491Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors. ...
10/02/2007
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
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
7267827Therapeutic compositions for intranasal administration which include KETOROLAC
An analgesic/anti-inflammatory pharmaceutical dosage form which comprises an effective amount of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, optically active forms thereof and pharmaceuti...
09/11/2007
7262199Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
08/28/2007
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