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Class 546/113 - Plural ring hetero atoms in the bicyclo ring system


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system includes at least
No. of patents: 524
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188281Azaindoles useful as inhibitors of JAK and other protein kinases
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. ...
05/29/2012
8163917Azaindoles useful as inhibitors of Janus kinases
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatm...
04/24/2012
8148529Pyrrolo[3,2-C] pyridine derivatives and processes for the preparation thereof
The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable s...
04/03/2012
8067599Imidazo [4,5-B] pyridine and pyrrolo [2,3-B] pyridine protein kinase inhibitors
Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments cont...
11/29/2011
7977484Crystalline form of cyano-1-cyclopropy1-7-1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid
The present invention relates to the trihydrate of pradofloxacin, to a process for its preparation and to antibacterial compositions comprising them. ...
07/12/2011
7968718Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and proce...
06/28/2011
7964728Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reup...
06/21/2011
7932389Octahydropyrrolo[2,3C]pyridine derivatives and pharmaceutical use thereof
The present invention is related to octahydropyrrolo[2,3,c]pyridine derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, can...
04/26/2011
7906648Pyrrolo-pyridine kinase modulators
The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. ...
03/15/2011
7897771Fused heterocyclic compounds
Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. ...
03/01/2011
7888508Pyrrolo[2,3-B]pyridine derivatives active as kinase inhibitors
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...
02/15/2011
7880004Met kinase inhibitors
The invention is directed to compounds that are useful for the treatment of cancer having the following Formula: ...
02/01/2011
7812166Kinase inhibitors
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using th...
10/12/2010
7803944Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; — repr...
09/28/2010
7767816Azaindoles useful as inhibitors of janus kinases
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatm...
08/03/2010
7728140Pyrrolo[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...
06/01/2010
7709644Process for the enantiomeric enrichment of cis-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane
The present invention relates to a process for the enantiomeric enrichment of cis-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane with the aid of continuous countercurrent chromatography, which is also described as SMB chromatography (SMB=simulated moving bed)....
05/04/2010
7709645Pyrrolo-pyridine kinase modulators
The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. ...
05/04/2010
7692015Economical process for preparing (S, S)-2, 8-diazabicyclo[4.3.0]nonane and its enantiomer
The present invention relates to a novel and economical process for preparing (S,S)-2,8-diazabicyclo[4.3.0]nonane, a valuable intermediate used for constructing quinolone and naphthyridine derivatives having antibacterial effectiveness, e.g. moxifloxacin and its ena...
04/06/2010
7678909Dipeptidyl peptidase inhibitors
Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims. ...
03/16/2010
7626027Substituted 1H-pyrrolo[2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase Iε
The present invention discloses and claims compounds of formula (I) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective as inhibitors of human casein ...
12/01/2009
7622583Heteroaryl sulfonamides and CCR2
Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in...
11/24/2009
7605266Azaindole inhibitors of Aurora kinases
The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a...
10/20/2009
7601839Pyrrolo-pyridine kinase modulators
The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity. ...
10/13/2009
7598383Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the spe...
10/06/2009
7589206Pyrrolopyridine derivatives
The present invention relates to novel pyrrolopyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in a...
09/15/2009
7579470Fused heterocyclic compounds
Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. ...
08/25/2009
7579469Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or s...
08/25/2009
7566784Bicyclic heterocycles as kinase inhibitors
The compounds of the instant invention can be used as anticancer agents. More specifically, the invention comprises a compound having Formula I or II, ...
07/28/2009
7553966Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug,...
06/30/2009
75414647-azaindoles, pharmaceutical compositions and their therapeutic applications
The present invention relates generally to compounds and compositions for the treatment of metabolic diseases and specifically, the present invention relates to compounds that therapeutically modulation and control lipid and/or carbohydrate metabolism and are thus s...
06/02/2009
7521557Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
Compounds are provided having the formula (I) wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases. ...
04/21/2009
7507826Azaindoles useful as inhibitors of JAK and other protein kinases
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. ...
03/24/2009
7504509Compounds 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...
03/17/2009
7488826Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors and methods for treating or ameliorating a kinase or dual-kinase mediated disorder. ...
02/10/2009
7456286Bicyclic heteroaromatic compounds as kinase inhibitors
A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 5-oxo-4,5-dihydro-1H-pyrrolo[3,2-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of ...
11/25/2008
7446199Compositions useful as inhibitors of protein kinases
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
11/04/2008
7439246Fused heterocyclic kinase inhibitors
In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful...
10/21/2008
7432375JNK inhibitors
The present invention provides novel compounds of formula (I) and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegener...
10/07/2008
7427682Indole derivatives as selective androgen receptor modulators (SARMS)
The present invention is directed to novel insole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ...
09/23/2008
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