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Class 514/235.8 - Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the additional hetero ring contains
No. of patents: 941
Last issue date: 05/22/2012


1                      
NumberTitleIssue Date
8183239Substituted piperazines and piperidines as modulators of the neuropeptide Y2 receptor
The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurologica...
05/22/2012
8183240Heteroaryls and uses thereof
This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specif...
05/22/2012
8178530Imidazolopyrazine 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 a vari...
05/15/2012
8178529Imidazole substituted pyrimidines
Imidazole substituted pyrimidines and pharmaceutically acceptable salts thereof; pharmaceutical formulations containing such pyrimidines; the use of such compounds in therapy; the use of such compounds for the treatment of conditions associated with glycogen synthas...
05/15/2012
8178531Antiviral agents
The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention o...
05/15/2012
8163745HIV inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines
This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds. ...
04/24/2012
8163746Azolecarboxamide derivative
Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinar...
04/24/2012
8153630Kinase inhibitors
Disclosed are protein kinase inhibitors of Formula Ia and Ib, compositions comprising such inhibitors, and methods of use, thereof. More particularly, these compounds and compositions are inhibitors of Aurora-A (Aurora-2) and Aurora-B (Aurora-1) protein kinase. Also...
04/10/2012
8138183Morpholino pyrimidine derivatives used in diseases linked to mTOR kinase and/or PI3K
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in d...
03/20/2012
81293776-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a h...
03/06/2012
8114872Triazolyl aminopyrimidine compounds
The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer. ...
02/14/2012
8093246O-linked pyrimidin-4-amine-based compounds, compositions comprising them, and methods of their use to treat cancer
O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described. Particular compounds of the invention are of formula I: ...
01/10/2012
8093244Heteroaryl urea derivatives useful for inhibiting CHK1
Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases ...
01/10/2012
80932454-amino-1H-pyrimidin-2-one based compounds, compositions comprising them and methods of their use
4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed. Particular compounds are of formula I:
01/10/2012
8088769Cyanopyrimidinones
The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory. ...
01/03/2012
8048881Pyrimidine derivatives and their use as P2Y12 receptor antagonists
The invention relates to 4-aminocarbonyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cer...
11/01/2011
80176085-Phenylthiazole derivatives and their use as p13 kinase inhibitors
Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediate...
09/13/2011
8003643Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the comp...
08/23/2011
7973039Sulfonyl amino cyclic derivatives and use thereof
The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fi...
07/05/2011
7964597Piperazinyl-sulfonamide derivatives useful in the treatment of GPR38 receptor mediated diseases
Disclosed are motilin agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. ...
06/21/2011
7956053Inhibitors of tyrosine kinases
The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, p...
06/07/2011
7935698Heteroaryl-hydrazone compounds
This invention relates to compounds having a formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, hydrate, prodrug or polymorph thereof wherein X is —C(Rg)═N-A. The invention also relates t...
05/03/2011
7919492Compounds
Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R
04/05/2011
7915256Triazolopyrazine 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 of ...
03/29/2011
7910585Pyrimidine derivatives
Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. ...
03/22/2011
7906511Cyclic compound having pyrimidinylalkylthio group
The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a salt thereo...
03/15/2011
7902192Inhibitors of P38 and methods of using the same
In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity. ...
03/08/2011
7893064Hydrazone derivatives as kinase inhibitors
The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof as inhibitors of ATP-protein kinase interactions, wherein substituents on each side of the iminomethyl...
02/22/2011
78930632,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
The invention concerns pyrimidine derivatives of Formula (I) wherein each of Qa, G1, G2, q, R3, r, R4, X1 and Qb have any of the meanings defined in the description; processes for their pre...
02/22/2011
78798534,6-disubstituted pyrimidines and their use as protein kinase inhibitors
The invention relates to novel pyrimidine derivatives of Formula (1) which are efficacious inhibitors of protein kinases, in particular of one or more isoforms of the protein kinase B/Akt. ...
02/01/2011
7875610Pyrimidinyl-piperazines useful as D/Dreceptor ligands
The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or s...
01/25/2011
78720052-substituted heteroaryl compounds
This invention relates to compounds of formula (I): or pharmaceutically acceptable salts, solvate, clathrates hydrates or polymorphs thereof, their compositions and methods of use and methods of making thereof. The compound...
01/18/2011
7855205Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhi...
12/21/2010
7851471Compounds I
The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mime...
12/14/2010
7842693Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
11/30/2010
7838524Substituted pyrazolyl urea derivatives useful in the treatment of cancer
The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I). ...
11/23/2010
7838525Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or trea...
11/23/2010
7834011Heterocyclylalkyl derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein R1, T, X, Y, A, n, m and p have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions cont...
11/16/2010
78295601,4-disubstituted naphthalenes as inhibitors of P38 MAP kinase
1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases. ...
11/09/2010
7825116N2, N4-bis-aryl-5-fluoro-2,4-pyrimidinediamines
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...
11/02/2010
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