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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 patents: 1364
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188113Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, k...
05/29/2012
8188114Pyrrolo[2,3-C]pyridine derivatives and processes for the preparation thereof
The present invention provides novel pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable s...
05/29/2012
8178554Heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-bacterial agents
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medica...
05/15/2012
8178553Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by ...
05/15/2012
81785527-Azaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase
The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in med...
05/15/2012
8168651Protein kinase modulators
The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim ki...
05/01/2012
8168652Inhibitors of AKT activity
The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compo...
05/01/2012
8163769Antibacterial compounds
Antibacterials having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods of prophyl...
04/24/2012
8158647Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators
Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein...
04/17/2012
8153652Fab I inhibitors
Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections. ...
04/10/2012
8148393Zolpidem tablets
A zolpidem tablet having modified release is designed as a tablet-in-tablet dosage form. ...
04/03/2012
8148395Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances. ...
04/03/2012
8148394Azaindoles having serotonin receptor affinity
Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also ...
04/03/2012
8143271Compounds 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. ...
03/27/2012
8138202Stable SNS-595 compositions and methods of preparation
Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles. ...
03/20/2012
8138201Treatment of progressive neurodegenerative disease with ibudilast
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine). ...
03/20/2012
8129403Chemical compounds
This invention relates to novel compounds having the formula (I); and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. ...
03/06/2012
8129404Compounds and uses thereof
N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, c...
03/06/2012
8124615Diketo substituted pyrrolo[2,3-C]pyridines
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives of Formula I: that possess ...
02/28/2012
8119657Enantiomeric compositions of 2-amino-1-(2-isopropylpyrazolo[1,5-α]pyridin-3-yl)propan-1-one and related methods
Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one, (S)-AV1013, is a candidate therapeutic for treating neuropathic pain, addiction behavior and drug withdrawal symptoms. Also described are methods for preparing and using (S)-AV...
02/21/2012
8114889Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds ...
02/14/2012
8114890Anti-constipation composition
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Fo...
02/14/2012
8110585Bicyclic compound and pharmaceutical use thereof
The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substit...
02/07/2012
8106068Compositions and methods for modulating c-kit and PDGFR receptors
The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such c...
01/31/2012
8106069Pyrrolo[2,3-b]pyridine derivatives active as kinase inhibitors and pharmaceutical compositions comprising them
Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or ass...
01/31/2012
8080561Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, ...
12/20/2011
8076354Bicyclic 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 compri...
12/13/2011
8071613Anti-constipation composition
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by ...
12/06/2011
8071614Bicyclic 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 ...
12/06/2011
8067433Methods, compositions, and kits for the treatment of ophthalmic disorders
The invention features methods, kits, and compositions for the treatment of ophthalmic disorders. The compositions include a corticosteroid in combination with a non-steroidal immunophilin-dependent immunosuppressant. ...
11/29/2011
8067434Compounds and methods for development of Ret modulators
Compounds active on Ret are described, as well as methods of using such compounds. Also described are crystal structures of Ret surrogates that were determined using X-ray crystallography. The use of such Ret surrogate crystals and structural information can, for ex...
11/29/2011
8067435Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs
The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2;
11/29/2011
8048892Azaquinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof
are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein. ...
11/01/2011
8044066Derivatives of pyrrolopyridine-2-carboxamides, preparation thereof and therapeutic application thereof
The invention relates to compounds of formula (I): Wherein n, the pyrrolopyridine core, X, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application. ...
10/25/2011
8030327Fused imidazole derivative
The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected fro...
10/04/2011
8022083Antiviral phosphonate analogs
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing su...
09/20/2011
8012992Aza-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R
09/06/2011
8008321Imidazo[1,5-a] pyridine derivatives, method for preparing same and pharmaceutical compositions containing same
The invention concerns compounds of formula I, a method for preparing said compounds, pharmaceutical compositions containing same and the therapeutic uses thereof. ...
08/30/2011
80083203-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors
The present invention relates to a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6...
08/30/2011
7998974Fused heterocyclic compounds and their use 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, dis...
08/16/2011
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