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Class 544/121 - Piperazine ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional six-membered hetero ring
No. of applications: 271
Last issue date: 05/03/2012


1              
Application No.Application TitleIssue Date
20120108588NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES
The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I):

wherein X, R1, R2, R3, R4, R5, R6, R7

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
20120083488TETRACYCLIC COMPOUND
A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or c...
04/05/2012
20120082702NICOTINAMIDE COMPOUNDS USEFUL AS KINASE MODULATORS
Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, ...
04/05/2012
20120071652Novel Piperazines, Pharmaceutical Compositions and Methods of Use Thereof
Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells...
03/22/2012
20120071653Human Adam-10 Inhibitors
The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises p...
03/22/2012
201200531664-Oxadiazol-2-YL-Indazoles as Inhibitors of P13 Kinases
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):

and salts thereof. The compounds of the invention are inhibitors of kinase activity, ...

03/01/2012
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
201200409339-(PIPERAZINYLALKYL) CARBAZOLES AS BAX-MODULATORS
piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy,...
02/16/2012
201200409598-METHOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B:

Such compounds possess useful antimicrobial activity. The variables R...

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
20120029191NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES
The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor....
02/02/2012
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
20120010201NOVEL ANELLATED 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...

01/12/2012
20120004197PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT
Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer co...
01/05/2012
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
20110319413PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE
This invention relates to a piperazine compound represented by Formula (I),

  • wherein
    • R
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
20110312939NEW CHEMICAL COMPOUNDS
The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases cha...
12/22/2011
20110294811ABT-263 CRYSTALLINE FORMS
ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer....
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
20110281851BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
The invention provides compounds of formula I:

wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compou...

11/17/2011
201102818385-ALKYNYL-PYRIMIDINES
The present invention encompasses compounds of general Formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof fo...
11/17/2011
20110275804PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF
The invention relates to a new process for the preparation of compounds of general formula (I) wherein
  • R1 and R2 represent independently hydrogen or
    11/10/2011
    201102756332,4-DIAMINOPYRIMIDINE DERIVATES AS PTK2- INHIBITORS FOR THE TREATMENT OF ABNORMAL CELL GROWTH
    The present invention encompasses compounds of general formula (1) wherein R1-R3 and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for p...
    11/10/2011
    20110275803PROCESS FOR SYNTHESIZING OXIDIZED LACTAM COMPOUNDS
    The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:

    ...

    11/10/2011
    20110269959PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES
    The invention relates to a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of general formula (I) by reacting the compound of formula (III) with a carbamoylchloride of general formula (II...
    11/03/2011
    20110269746CYCLIC COMPOUND HAVING HETERO ATOM
    Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:

      • 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
    20110263592IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Imidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insom...
    10/27/2011
    20110263557COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
    The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119; such as, but not limited to, diabetes, obesity and associated me...
    10/27/2011
    20110257100Inhibitors of Protein Tyrosine Kinase Activity
    This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for examp...
    10/20/2011
    201102511742,4-DIAMINO-PYRIMIDINES AS AURORA INHIBITORS
    The present invention encompasses compounds of general formula (1)

    wherein

      • 10/13/2011
    20110237585SUBSTITUTED PROPENYL PIPERAZINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE
    This invention comprises the novel compounds of formula (I)

    wherein R1, R2, R3, R4 and X have defined meanings, having histone deacetylase inhibiting enzymatic acti...

    09/29/2011
    20110230476PI3 KINASE INHIBITORS AND USES THEREOF
    The present invention provides compounds, compositions thereof, and methods of using the same....
    09/22/2011
    20110230471BENZONAPHTYRIDINE COMPOUNDS AS INHIBITORS OF AUTOTAXIN
    Compounds of the formula (I), in which R1, R2, R3, R4, R5, D, Z, X, Y, m and p have the meanings indicated in Claim 1, can and be employed for the treatment of tumours....
    09/22/2011
    20110224211Anti-Viral Compounds, Compositions, And Methods Of Use
    Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses....
    09/15/2011
    20110218182CHEMICAL COMPOUNDS 251
    The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invent...
    09/08/2011
    20110218184QUINOLONE ANALOGS AND METHODS RELATED THERETO
    The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of ma...
    09/08/2011
    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
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