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Class 540/552 - Bicyclo ring system which contains the hetero ring as one of the cyclos


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the polycyclo ring system consists of
No. of applications: 119
Last issue date: 05/09/2013


1      
Application No.Application TitleIssue Date
20130116213NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY
The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated ...
05/09/2013
20130116237[6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS
Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Th...
05/09/2013
20130090328COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE
The invention relates to the compounds of formula (I):

and pharmaceutically acceptable salts thereof, wherein R1, R2 and X are as defined in the description and claims, which are useful ...

04/11/2013
20130079511BICYCLIC METHYLENE AZIRIDINES AND REACTIONS THEREOF
The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use...
03/28/2013
20130079333OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS
The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula

    • 03/28/2013
20130053343COMPOUNDS AND METHODS FOR INHIBITING SEROTONIN SYNTHESIS
Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.

02/28/2013

20130035326BIARYL COMPOUNDS AND METHODS OF USE THEREOF
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

...

02/07/2013
20130029938Chemical Compounds
Compounds of Formula I and methods for treating metabolic disorders are disclosed.

...

01/31/2013
20130017273COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders,...
01/17/2013
20130012492FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:
01/10/2013
20130012494CYCLOPROPYL-FUSED-1,3-THIAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS
The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I

having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as the...

01/10/2013
20130005706FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:
01/03/2013
20120316135Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I:

wherein the variables are as defined herein....

12/13/2012
20120316153BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
The present invention relates to benzazepine derivatives of the formula (I)

or a physiologically tolerated salt thereof.

The present invention also relates to pharmaceutical comp...

12/13/2012
20120258953Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides met...
10/11/2012
20120252780BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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, disease...
10/04/2012
201202258581,4 THIAZEPINES/SULFONES AS BACE1 AND/OR BACE2 INHIBITORS
The present invention relates to 1,4 Thiazepines/Sulfones of formula I

having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeuti...

09/06/2012
20120220568Histamine-3 Receptor Antagonists
This invention is directed to a compound of formula I,

wherein R1, R2, R4, R5, R6, R7, R8 and n are as defined herein, or a pharmac...

08/30/2012
20120202790[6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS
Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Th...
08/09/2012
20120196848THIENOOXAZEPINE DERIVATIVE
Provision of a compound having a serotonin 5-HT2C receptor activating action.

A compound represented by the formula (I):

wherein each symbol is as described in the des...

08/02/2012
201201845271,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“...
07/19/2012
20120184732NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND SALT THEREOF, AND A FUNGICIDE FOR AGRICULTURAL AND HORTICULTURAL USE
The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.

<...
07/19/2012
201201845287-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“...
07/19/2012
20120165519Fused Bicyclic Derivatives of 2,4-Diaminopyrimidine as ALK and c-MET Inhibitors
The present invention provides a compound of formula I or II

or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1

06/28/2012
20120165312FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula

wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having s...

06/28/2012
20120157440NOVEL FUSED PYRIDINE COMPOUNDS AS CASEIN KINASE INHIBITORS
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I:

and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4

06/21/2012
20120149573HERBICIDAL BUS-NITROGEN-CONTAINING OXO AND SULFONO HETEROCYCLES
Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof,

06/14/2012
20120135979PYRAZINOOXAZEPINE DERIVATIVES
Provided is a compound having a serotonin 5-HT2C receptor activating action, useful for lower urinary tract conditions, obesity and cancer. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a sal...
05/31/2012
20120135981NOVEL SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I)

wherein R1, R2, A1, A2, A3, A4, X,...

05/31/2012
20120135980GAMMA SECRETASE MODULATORS
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and metho...
05/31/2012
20120122843Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases
The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Aβ...
05/17/2012
20120114588IBAT INHIBITORS FOR TREATMENT OF METABOLIC DISORDERS AND RELATED CONDITIONS
The present invention regards specific IBAT inhibitors with improved effect in prophylaxis and treatment of metabolic syndrome, obesity, disorders of fatty acid metabolism, glucose utilization disorders, disorders in which insulin resistance is involved, diabetes mellit...
05/10/2012
20120101085Compounds And Methods For Modulating Activity Of Calcium Release Channels
The present teachings provide compounds of Formulae I and II: and pharmaceutically acceptable salts, hydrates, complexes, esters, and prodrugs thereof, wherein R1, R1′, R2, R2′, R3, R3′, and X are a...
04/26/2012
20120071462Dihydrobenzoxathiazepine compounds, a process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I):

wherein

  • R1 represents a hydrogen atom or a heterocyclic, cyano, alkoxycarbonyl, alkylsulphonylaminoa...
03/22/2012
20120015930SUBSTITUTED IMIDAZOHETEROCYCLE DERIVATIVES
The present invention provides substituted imidazoheterocycles having the general structure of formula I:

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

01/19/2012
20120010193CGRP RECEPTOR ANTAGONISTS
Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the...
01/12/2012
201103129372,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS
This invention relates to compounds of the formula

wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BAC...

12/22/2011
201103065941,4-BENZOTHIAZEPINE-1-OXIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION UTILIZING THE SAME
Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial re...
12/15/2011
20110294784GAMMA SECRETASE MODULATORS
This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and metho...
12/01/2011
20110288291PYRAZINOOXAZEPINE DERIVATIVES
Provided is a compound having a serotonin 5-HT2C receptor activating action.

A compound represented by the formula (I0):

wherein each symbol is as defined i...

11/24/2011
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