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Class 514/255.01 - Nitrogen or -C(=X)-, wherein X is chalcogen, bonded directly to the piperazine ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein nitrogen or a -C(=X)- group,
No. of applications: 391
Last issue date: 05/03/2012


1                    
Application No.Application TitleIssue Date
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
20120108603AMINOCARBONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE
This invention comprises the novel compounds of formula (I)

wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and

05/03/2012

20120107276Anti-Arenaviral Compounds
Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associ...
05/03/2012
20120108592PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses....
05/03/2012
20120052019CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described....
03/01/2012
20120046292DIACYLETHYLENEDIAMINE COMPOUND
[Problem]

A compound which is useful as an anti-obesity agent is provided.

[Means for Solution]

The present inventors have investigated a compound having a DGAT1 inhibitory action,...

02/23/2012
20120046293RENIN INHIBITORS
The present invention relates to renin inhibitor compounds having the structure

and their use in treating cardiovascular events and renal insufficiency....

02/23/2012
20120040986OMEGA CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS RAF KINASE INHIBITORS
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy....
02/16/2012
20120022080Plasminogen Activator Inhibitor-1 Inhibitor
The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory...
01/26/2012
20120015928Amido Compounds And Their Use As Pharmaceuticals
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases ass...
01/19/2012
20120015960CHEMICAL INHIBITOR OF P53-SNAIL BINDING AND PHARMACEUTICAL COMPOSITION FOR TREATING CANCER DISEASE CONTAINING SAME AS ITS ACTIVE INGREDIENT
Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or pre...
01/19/2012
20120004213NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds....
01/05/2012
20110318329METHOD OF TREATMENT OR PROPHYLAXIS
The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2
12/29/2011
20110312965RETINOID DERIVATIVES ENDOWED WITH CYTOTOXIC AND/OR ANTIANGIOGENIC PROPERTIES
The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chr...
12/22/2011
20110294814COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS
Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed...
12/01/2011
20110294775NOVEL COMPOUNDS
Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary:

...

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
20110288068AZA SPIRO ALKANE DERIVATIVES AS INHIBITORS OF METALLOPROTEASES
The present invention provides a compound of Formula I or Formula II:

enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are pro...

11/24/2011
20110281891N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF
The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory dise...
11/17/2011
20110281886Pharmaceutical Compositions with Attenuated Release of Phenolic Opioids
Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) tha...
11/17/2011
20110275650METHODS AND COMPOSITIONS RELATED TO TARGETING MONOACYLGLYCEROL LIPASE
This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat cond...
11/10/2011
201102697361,1'-Diadamantyl carboxylic acids, medicaments containing such compounds and their use
The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suit...
11/03/2011
20110269761ARYLSULPHONYLGLYCINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS MEDICAMENTS
The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the...
11/03/2011
20110269776TREATMENT OF OXIDATIVE STRESS DISORDERS INCLUDING CONTRAST NEPHROPATHY, RADIATION DAMAGE AND DISRUPTIONS IN THE FUNCTION OF RED CELLS
Methods of treating or suppressing oxidative stress diseases and symptoms related to oxidative stress affecting normal electron flow in the cells or caused by reactive oxygen species with redox-active therapeutics. Use of redox-active therapeutics for the reduction, sup...
11/03/2011
20110263604Oxidase inhibitors and their use
The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases....
10/27/2011
20110250135Piperazine Derivatives for Binding and Imaging Amyloid Plaques and Their Use
The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient....
10/13/2011
20110245179Composition for Prevention or Treatment of Heart Failure
Provided are a composition for preventing or treating heart failure and a method for screening an agent for treating heart failure. The present disclosure demonstrates for the first time that administration of PKCζ inhibitor provides inotropic effect by increasing myoc...
10/06/2011
20110218200METHODS OF TREATING AMYLOID DISEASE USING ANALOGS OF 1-(4-NITROPHENYL) PIPERAZINE
The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with....
09/08/2011
20110212080UREA DERIVATIVES AS ANTIBACTERIAL AGENTS
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.

...

09/01/2011
20110212974METHOD FOR IDENTIFYING COMPOUNDS USEFUL FOR TREATING AND/OR PREVENTING DISEASE-ASSOCIATED BONE LOSS
The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inacti...
09/01/2011
20110212971DIKETO FUSED AZOLOPIPERIDINES AND AZOLOPIPERAZINES AS ANTI-HIV AGENTS
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 that possess unique antiviral activity are provided. These compounds are u...
09/01/2011
20110207730ION CHANNEL MODULATING COMPOUNDS AND USES THEREOF
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment o...
08/25/2011
20110207741Activation of the Renin-Angiotensin System (RAS) and Sudden Cardiac Death
Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of...
08/25/2011
20110201622Solid Forms Comprising A Cyclopropyl Amide Derivative
This disclosure relates to at least one solid form of 4-{(1S, 2S)-2-[((R)-4-cyclobutyl-2-methylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide. This disclosure also relates to at least one pharmaceutical composition comprising at least one solid form described herein, m...
08/18/2011
20110201623Crystalline Form Of A Cyclopropyl Benzamide Derivative
The present invention relates to a crystalline form of compound (I), 4-{(1S,2S)-2-[(4-cyclobutylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide,

pharmaceutical formulations containing said compound and...

08/18/2011
20110201624Pharmaceutical Composition for Prevention and Treatment of Diabetes or Obesity Comprising a Compound that Inhibits Activity of Dipeptidyl Peptidase-IV, and other Antidiabetic or Antiobesity Agents as Active Ingredients
The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes or obesity comprising as active ingredients a compound which inhibits the activity of dipeptidyl peptidase-IV (DPP-IV), a pharmaceutically acceptable salt thereof,...
08/18/2011
20110195977ACRYLAMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION
Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfu...
08/11/2011
20110195963NOVEL CARBAMOYLOXY ARYLALKANOYL ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND
There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceuti...
08/11/2011
20110178096OCTAHYDROPENTALENE COMPOUNDS AS CHEMOKINE RECEPTOR ANTAGONISTS
The present invention is directed to novel compounds of Formula (I)

pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers ther...

07/21/2011
20110178077Anti-infective compounds
The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis....
07/21/2011
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