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Class 514/300 - Plural hetero atoms in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system includes
No. of applications: 1499
Last issue date: 05/24/2012


1                      
Application No.Application TitleIssue Date
20120129872FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

05/24/2012

20120129884PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY
The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3...
05/24/2012
20120129856COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION
The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, ...
05/24/2012
20120108595PLATELET-ACTIVATING FACTOR RECEPTOR ANTAGONISTS
Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorder...
05/03/2012
20120108581FUSED PIPERIDINE COMPOUND AND PHARMACEUTICAL CONTAINING SAME
The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1):

05/03/2012
20120108576THIAZOLE COMPOUNDS AND METHODS OF USE
The present invention provides compounds, salts and hydrates of Formula I,

wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds ...

05/03/2012
20120108557FLUOROQUINOLONE DERIVATIVES FOR OPHTHALMIC APPLICATIONS
The present invention relates to fluoroquinolone derivatives having enhanced ocular penetration characteristics and/or antimicrobial activity, and to compositions comprising such derivatives. The derivatives and compositions are particularly well suited for treating oph...
05/03/2012
20120082729QUICK DISSOLVE COMPOSITIONS AND TABLETS BASED THEREON
The invention provides a composition useful for making oral dosage forms capable of dissolving in the mouth in less than 40 seconds without the need for a conventional super disintegrant and having a friability of less than 1%; wherein the composition includes liquiflas...
04/05/2012
20120071474INHIBITORS OF PI3 KINASE
The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof;

03/22/2012
20120070467Ophthalmic Drug Delivery
The present invention includes and provides a method of delivering a medicament to an eye of a subject in need thereof a solution, the method comprising: (a) providing droplets containing the medicament with a specified average size and average initial ejecting velocity...
03/22/2012
20120070413METHOD OF TREATING CANCER WITH SUBSTITUTED AMIDE DERIVATIVES
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...
03/22/2012
20120071460PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS
The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description....
03/22/2012
20120053175MLK INHIBITORS AND METHODS OF USE
Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therap...
03/01/2012
20120053177COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases....
03/01/2012
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
20120053132COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450
Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the...
03/01/2012
201200531783-(1,2,3-Triazol-4-yl) pyrrolo [2,3-b] pyridine derivatives
Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim (1), are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours....
03/01/2012
20120053202POLYSUBSTITUTED 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 ...

03/01/2012
20120053201SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
This invention provides compounds of formula (I):

    • wherein R1a, R1b...
03/01/2012
20120045412CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

...

02/23/2012
20120045433COMBINATION THERAPY
The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an topoisomerase inhibitor for treating a patien...
02/23/2012
20120045434COMBINATION THERAPY
The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for treating a patient suffer...
02/23/2012
20120041002SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINES AS METABOTROPIC GLUTAMATE ANTAGONISTS
The present invention relates to compounds of formula (I)

wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to...

02/16/2012
20120040994THERAPEUTIC AGENT FOR GLAUCOMA COMPRISING Rho KINASE INHIBITOR AND PROSTAGLANDIN
A therapeutic composition for treating glaucoma or for reducing intraocular pressure containing a combination of pharmaceutically effective amounts of drugs including (i) a Rho kinase inhibitor selected from the group consisting of (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-...
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
20120040936CYCLIC COMPOUND HAVING SUBSTITUTED PHENYL GROUP
Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:

...

02/16/2012
20120040950ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, con...
02/16/2012
20120041000IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer....
02/16/2012
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
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
20120035171BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer....
02/09/2012
20120035152BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, q, A, B, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comp...
02/09/2012
20120035153BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, A, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comprising...
02/09/2012
20120035409BI- AND TRICYCLIC INDAZOLE-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND USES THEREOF
This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-M...
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
20120034300STABILIZED ZOLPIDEM PHARMACEUTICAL COMPOSITIONS
Methods of inducing antinociception in a human are described. The method includes the step of administering an effective dose of a polypeptide comprising L-neo-tryptophan to the human extracranially. The polypeptide containing L-neo-tryptophan could be, but is not limit...
02/09/2012
20120035149Prokineticin Receptor Antagonists And Uses Thereof
Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes....
02/09/2012
20120028940FUNCTIONALLY SELECTIVE AZANITRILE ALPHA-2C ADRENORECEPTOR AGONISTS
In its many embodiments, the present invention provides a novel class of azanitrile compounds as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing...
02/02/2012
20120028956BICYCLIC MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME
In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glu...
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
1                      
 
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