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Class 544/357 - Plural diazine rings


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain at least two of the six-membered
No. of applications: 323
Last issue date: 05/03/2012


1                  
Application No.Application TitleIssue Date
20120108602Carbamoyl Compounds as DGAT1 Inhibitors 190
DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity

    05/03/2012
20120107273NEW PIPERAZINE COMPOUND AND USE THEREOF AS A HCV POLYMERASE INHIBITOR
The present invention relates to a compound represented by the following formula [I]

wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof...

05/03/2012
20120053149THIAZOLE DERIVATIVES AND THEIR USE AS P2Y12 RECEPTOR ANTAGONISTS
The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular disea...
03/01/2012
20120045470IMATINIB IMMUNOASSAY
Novel conjugates and immunogens derived from imatinib and monoclonal antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of imatinib or its pharmacologically active salts in biological fluids....
02/23/2012
20120040992OLIGOOXOPIPERAZINES AND METHODS OF MAKING AND USING THEM
The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed....
02/16/2012
20120040020COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
The present disclosure relates to pyrazine compounds of formula I:

wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein...

02/16/2012
20120040977INHIBITORS OF HCV NS5A
Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C....
02/16/2012
20120040993NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotect...
02/16/2012
20120040968DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND
Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.

As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion prot...

02/16/2012
20120035407COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
The present invention relates to pyrazine 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 various diseases, disorders, and condit...
02/09/2012
20120035408COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
The present invention relates to pyrazine and pyridine 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 various diseases, disorder...
02/09/2012
20120028954Substituted Pyridine, Pyridazine, Pyrazine And Pyrimidine Compounds And Methods For Using The Same
Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure

wherein E, J, T, the ring system denoted by “B”, T...

02/02/2012
201200289792-(PIPERIDIN-1-YL)-4-HETEROCYCLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS
Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

02/02/2012
20120022254SIRTUIN MODULATING COMPOUNDS
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...
01/26/2012
20120022075NOVEL PHENYLPYRROLE DERIVATIVE
The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof:

...

01/26/2012
20120010410(2R)-1-(3-CHLORO-2-PYRAZINYL)-2-METHYLPIPERAZINE AND SALTS THEREOF
The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system.

In one aspect, the invention relates to a process for the preparation of compounds of the general fo...

01/12/2012
20120004221Antibacterial Compositions
Compounds of formula (I) have antibacterial activity:

wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynyl...

01/05/2012
20120004207THERAPEUTIC USES OF DERIVATIVES OF PIPERIDINYL-AND PIPERIDINYL-ALKYL CARBAMATES
Compound corresponding to the general formula (I):

  • in which A=N or CR2; R2═H, F, OH, CN, CF3, C1-6-alkyl, C1-6-...
01/05/2012
20120004241SUCCINATE SALT OF (2R)-METHYL-1-PIPERAZINE
The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system.

In one aspect, the invention relates to a process for the preparation of compounds of the general fo...

01/05/2012
20110319393ANTHELMINTIC AGENTS AND THEIR USE
This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositio...
12/29/2011
20110313151ANELLATED PYRIDINE COMPOUNDS
The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I)

wherein X, Y, A, R1, R2, and R3 are as descri...

12/22/2011
20110306587UNSATURATED NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
Unsaturated nitrogen heterocyclic compounds of formula (I):

as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treat...

12/15/2011
20110306590ARYL- AND HETEROARYL- NITROGEN-HETEROCYCLIC COMPOUNDS AS PDE10 INHIBITORS
Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependen...
12/15/2011
20110306589NITROGEN CONTAINING HETEROARYL COMPOUNDS
The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I)

wherein A1, A2,

R1,...

12/15/2011
20110301143HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR
12/08/2011
20110294819Hepatitis C Virus Inhibitors
The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the...
12/01/2011
20110295006CYCLIC DIPEPTIDES AS FEED ADDITIVES
Feed additives containing essential amino acids which are diketopiperazines of formulas (IV) or (V) or salts thereof are provided:

In formulas (IV) and (V), R1 and R2 may be an amino aci...

12/01/2011
20110294793HYDROXYPHENYL SULFONAMIDES AS ANTIAPOPTOTIC BCL INHIBITORS
The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compou...
12/01/2011
20110294809TROPANE UREA DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS MODULATORS OF THE ACTIVITY OF 11BETAHSD1
The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11β-hydroxysteroid dehydrogenose type 1 (11βHSD1)....
12/01/2011
20110288091SOLUBLE MTOR COMPLEXES AND MODULATORS THEREOF
The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, a...
11/24/2011
20110281861THIAZOPYRIMIDINONES AND USES THEREOF
The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said ...
11/17/2011
20110275803PROCESS FOR SYNTHESIZING OXIDIZED LACTAM COMPOUNDS
The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:

...

11/10/2011
20110269760TUBULIN INHIBITORS
Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also descr...
11/03/2011
201102697377-(Piperazine-1-Ymethyl)-1H-Indole-2-Carboxylic Acid (Phenyl)-Amide Derivatives and Allied Compounds as P38 Map Kinase Inhibitors for the Treatment of Respiratory Diseases
The present invention provides compounds according to general formula (I)

which are proposed for the treatment of respiratory complaints, particularly asthma and COPD....

11/03/2011
20110269756BENZOTHIAZOLONE DERIVATIVES
Compounds of the formula I, in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, an...
11/03/2011
20110263571NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE
Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide deri...
10/27/2011
20110257398Compositions and Methods Including Cell Death Inducers and Procaspase Activation
Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction ...
10/20/2011
20110256064Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-like Proteins
The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compou...
10/20/2011
20110251194ANTINEOPLASTIC DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods o...
10/13/2011
20110251209COMPOUNDS FOR TREATING PARASITIC DISEASE
A compound, particularly an antimalarial compound, according to formula I:

    • or a pharmace...
10/13/2011
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