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Class 544/105 - Bicyclo ring system having the oxazine ring as one of the cyclos (e.g., benzoxazines, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the polycyclo ring system consists of
No. of applications: 727
Last issue date: 05/24/2012


1                      
Application No.Application TitleIssue Date
20120126184SURFACE-MODIFIED PIGMENT COMPOSITIONS
The invention relates to a compound comprising a chromophore of formula (II), wherein m is an integer from 1 to 4, preferably 1 or 2; Q2 is a residue of carbon black or of a chromophore which comprises at least one group of the formula (I) or a cis/trans isom...
05/24/2012
20120129840NOVEL VIRAL REPLICATION INHIBITORS
The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to nov...
05/24/2012
20120129846GAMMA SECRETASE MODULATORS
In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing...
05/24/2012
20120108810Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses
The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications....
05/03/2012
20120107275FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis...
05/03/2012
20120053171Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phen...
03/01/2012
201200531664-Oxadiazol-2-YL-Indazoles as Inhibitors of P13 Kinases
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):

and salts thereof. The compounds of the invention are inhibitors of kinase activity, ...

03/01/2012
20120040957Novel Bicyclic Antibiotics
Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halog...
02/16/2012
20120040951HETEROARYL COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
The present invention provides compounds of formula (I) useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.

...

02/16/2012
20120040942NOVEL BRONCHODILATING DIAZAHETEROARYLS
The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma....
02/16/2012
20120040968DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND
Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.

As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion prot...

02/16/2012
20120040975BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic diso...
02/16/2012
20120034275POWDER FORMULATIONS FOR INHALATION, COMPRISING ENANTIOMERICALLY PURE BETA AGONISTS
The present invention relates to powder formulations for inhalation containing enantiomerically pure compounds of general formula 1

wherein the groups R1, R2, R3 and R4 <...

02/09/2012
20120035158Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions
The present invention relates to substituted xanthines of general formula

wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof...

02/09/2012
20120035168N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES
The invention relates to compound of the formula I

in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments ...

02/09/2012
20120035167INDOLE AND BENZOXAZINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disord...
02/09/2012
20120028969BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF
The present invention provides compounds of formula (I);

or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing th...

02/02/2012
20120028939SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS
The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof,

wherein

    02/02/2012
20120028920DERIVATIVES OF 4-PIPERAZIN-1-YL-4-BENZO[B]THIOPHENE SUITABLE FOR THE TREATMENT OF CNS DISORDERS
A heterocyclic compound or a salt thereof represented by the formula (1):

    • where R2 ...
02/02/2012
201200220584,5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans....
01/26/2012
20120022057BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYGLYCEROL ACYLTRANSFERASE
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a...
01/26/2012
20120015940NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2
01/19/2012
20120015920HETEROBICYCLIC METALLOPROTEASE INHIBITORS
The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inh...
01/19/2012
20120015930SUBSTITUTED IMIDAZOHETEROCYCLE DERIVATIVES
The present invention provides substituted imidazoheterocycles having the general structure of formula I:

wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO...

01/19/2012
20120016117INDAZOLEPROPIONIC ACID AMIDE COMPOUND
Disclosed is a compound which is useful in preventing and treating cardiac arrhythmia such as atrial fibrillation. A compound represented by formula (1) or a pharmaceutically acceptable salt of the same.

In f...

01/19/2012
20120015937Kinase 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 inappropriate k...
01/19/2012
20120010203TRIAZOLOPYRIDAZINES AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS
The invention relates to novel compounds of formula I

where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especia...

01/12/2012
20120009151Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof
Disclosed herein are novel triazines and related compounds, the synthesis thereof, and compositions, including pharmaceutical compositions, comprising the novel triazines and related compounds. Such novel triazines and related compounds function to inhibit or block entr...
01/12/2012
20120004165HETEROCYCLICALLY SUBSTITUTED METHOXYPHENYL DERIVATIVES WITH AN OXO GROUP, PROCESSES FOR PREPARATION THEREOF AND USE THEREOF AS MEDICAMENTS
Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments

The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, an...

01/05/2012
20110319378PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
The present invention provides MDM2 inhibitor compounds of Formula I,

    • wherein the variab...
12/29/2011
20110319392Thiazole Sulfonamide And Oxazole Sulfonamide Kinase Inhibitors
The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents....
12/29/2011
20110319613Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses
The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications....
12/29/2011
20110319403BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a...
12/29/2011
20110312951C-Ring Modified Tricyclic Benzonaphthiridinone Protein Kinase Inhibitors and Use Thereof
Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signa...
12/22/2011
20110312954MINERALOCORTICOID RECEPTOR ANTAGONIST AND METHODS OF USE
The present invention provides a compound of the formula: Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiologica...
12/22/2011
20110311458ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF
The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for their preparation, compositions comprising them, and therapeutic uses thereof....
12/22/2011
20110301141AMINOPYRIMIDINE DERIVATIVES AS LRRK2 INHIBITORS
Compounds of the formula I:

or pharmaceutically acceptable salts thereof,
wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined here...

12/08/2011
20110301145PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Method...
12/08/2011
20110301156Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process For Making Them, and Use Thereof to Treat Pain and Other Conditions
Vanilloid receptor ligand compounds corresponding to formula I:

pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating ...

12/08/2011
20110301149COMPOSITIONS AND METHODS FOR TREATING ALCOHOL USE DISORDERS, PAIN AND OTHER DISEASES
The present invention provides compounds which antagonize epsilon protein kinase C (PKCε). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating v...
12/08/2011
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