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Class 544/124 - Six-membered ring consisting of one nitrogen and five carbons (e.g., pyridine, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional hetero ring is a six-membered
No. of patents: 542
Last issue date: 02/21/2012


1                      
NumberTitleIssue Date
8119797Production method
The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereo...
02/21/2012
8101750Process for the manufacturing of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-indole-5-carbonitrile 701
The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5-(morpholin-4-y...
01/24/2012
7714127Process for making heteroaryl amine intermediate compounds
Disclosed are processes to produce a compound of the formula (I): ...
05/11/2010
7659394Substituted morpholine compounds for the treatment of central nervous system disorders
This invention relates to compounds of the formulae I wherein R1-R8, A, X, and Z are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of centr...
02/09/2010
74322895-Acylamino-1,1′-biphenyl-4-carboxamide derivatives and their use as P38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
10/07/2008
7420055Aryl sulfonamides
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful...
09/02/2008
7414055Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
08/19/2008
7414046Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...
08/19/2008
7410976Spirochromanone derivatives
The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders. ...
08/12/2008
7396842Five-membered cyclic compounds
A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or ...
07/08/2008
7365067Indanol derivative
The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally s...
04/29/2008
7365068Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds o...
04/29/2008
7361682Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ...
04/22/2008
RE40245Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...
04/15/2008
7351713Spirohydantoin compounds and methods for the modulation of chemokine receptor activity
Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modul...
04/01/2008
7342013Benzamides and related inhibitors of factor Xa
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and c...
03/11/2008
7338951Pyridine compounds
This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders. ...
03/04/2008
7338950Amide compounds as ion channel ligands and uses thereof
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals ...
03/04/2008
7332602Pyridyl substituted heterocycles useful for treating or preventing HCV infection
The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles ...
02/19/2008
7329656Arylthiobenzylpiperidine derivatives
This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically accepta...
02/12/2008
7323462Morpholine dopamine agonists
Compounds of formula (I), (Ia) and (Ib) useful as a medicament. ...
01/29/2008
7317007Benzothiazole derivatives with activity as adenosine receptor ligands
The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor. ...
01/08/2008
7314874Benzamides and related inhibitors of factor Xa
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and c...
01/01/2008
7314872Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides m...
01/01/2008
7312326Fluorescent labeled nucleotide derivatives
Fluorescent labeled reporter compounds having a modified cyanine dye that is coupled to a nucleotide derivative through a linker are disclosed. The compounds are useful for nucleic acid sequence analysis. The fluorescent labeled reporter compounds are ring-locked cy...
12/25/2007
7301029Bipyridine Derivatives
The invention provides a bipyridine derivative useful as an intermediate for pharmaceutical products, agricultural chemicals, electrophotographic photosensitive materials, dyes and the like, which is a bipyridine derivative represented by the general formula (I) and...
11/27/2007
7288548Spiro compounds and methods for the modulation of chemokine receptor activity
Compounds of formula I wherein X, Y, Z, W, R1 and R2 as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine re...
10/30/2007
7288658Process for preparation of pyridine derivatives
The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound o...
10/30/2007
7282500Imidazole-2-carboxamide derivatives as Raf kinase inhibitors
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, use as Raf Kinase Inhibitors and treatment methods for neurotrau...
10/16/2007
7279491Phenylpiperidines and phenylpyrrolidines
Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
10/09/2007
7279470Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may...
10/09/2007
7265112Small molecule modulators of hepatocyte growth factor (scatter factor) activity
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2 and B are as described generally and in classes and subclasse...
09/04/2007
7252815Pathological tissue detection and treatment employing targeted benzoindole optical agents
Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and pho...
08/07/2007
7253192Phenyl derivatives comprising an acetylene group
This invention is concerned with compounds of the formula I: wherein one of R5, R6 and R7 is and X1, X2
08/07/2007
7241758Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease...
07/10/2007
7230098Aminoheteroaryl compounds as protein kinase inhibitors
Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET ...
06/12/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
721471420-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a...
05/08/2007
7201892Pathological tissue detection and treatment employing targeted optical agents
Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and pho...
04/10/2007
7198778Tumor-targeted optical contrast agents
Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologs. The compounds may be conjugated to bioactive peptides, carbohydrates, hormo...
04/03/2007
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