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Class 544/295 - 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: 769
Last issue date: 05/24/2012


1                      
Application No.Application TitleIssue Date
20120129840NOVEL VIRAL REPLICATION INHIBITORS
The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to nov...
05/24/2012
20120129867INHIBITORS OF PROTEIN KINASES
The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds...
05/24/2012
20120129870PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds...
05/24/2012
20120108572NOVEL BENZAMIDES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
Heteroaryloxy-substituted benzoic acid amides of general formula I

wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the st...

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

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
20120083474HETEROCYCLIC AMIDES AS MODULATORS OF TRPA1
Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowe...
04/05/2012
20120083440METHODS AND COMPOUNDS FOR THE TARGETED DELIVERY OF AGENTS TO BONE FOR INTERACTION THEREWITH
Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting...
04/05/2012
20120071487PIPERAZINE, PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof....
03/22/2012
20120071491Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates
The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, n...
03/22/2012
20120071492Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates
The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, n...
03/22/2012
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
20120071472RIMINOPHENAZINES WITH 2-(HETEROARYL)AMINO SUBSTITUENTS AND THEIR ANTI-MICROBIAL ACTIVITY
The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, ei...
03/22/2012
20120053164CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD
The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single...
03/01/2012
20120053180CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS
This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human h...
03/01/2012
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
20120046277BENZOFURAN DERIVATIVES
The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R
02/23/2012
20120046295COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
The present invention relates to pyrrolopyrazines 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 of various diseases, disorders,...
02/23/2012
20120046463Process for the Preparation of Imatinib Base
Provided is an environmentally-friendly process for preparing imatinib base in high yield, without the use of an organic solvent....
02/23/2012
20120040967Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine Compounds and Their Use
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine co...
02/16/2012
201200409913-AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS
Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.

...

02/16/2012
20120040997VINYL-ARYL DERIVATIVES FOR INFLAMMATION AND IMMUNE-RELATED USES
The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders....
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
20120027842TOPICAL FORMULATIONS OF FLAP INHIBITORS FOR ADMINISTRATION TO AN EYE
Described herein are topical formulations for administration to an eye, wherein the formulation is administered to treat ophthalmic diseases, disorders, or conditions. A topical formulation for administration to an eye disclosed herein comprises a therapeutically-effect...
02/02/2012
20120028983NOVEL COMPOUND HAVING 3-HETEROARYLPYRIMIDIN-4-(3H)-ONE STRUCTURE AND PHARMACEUTICAL PREPARATION CONTAINING SAME
Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circu...
02/02/2012
20120028907METHODS FOR IDENTIFICATION OF TUMOR PHENOTYPE AND TREATMENT
The disclosure relates to methods for identifying a tumor as an E2F-responsive gene over-expressing (ERGO) tumor, methods of determining the likelihood that an ERGO tumor patient will survive to a future date, methods of treating an ERGO tumor in a patient, and methods ...
02/02/2012
201200289585-ALKYNYL-PYRIMIDINES
The present invention encompasses compounds of general formula (1)

wherein

R1 to R4 R3 are defined as in claim 1, which are suitable for the trea...

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
201200289525-ALKYNYL-PYRIMIDINES
The present invention encompasses compounds of general formula (1)

    • wherein
    • ...
02/02/2012
20120028923COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically...
02/02/2012
201200289896-(3-AZA-BICYCLO[3.1.0]HEX-3-YL)-2-PHENYL-PYRIMIDINES
The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascul...
02/02/2012
20120028924CHEMICAL COMPOUNDS
The present invention relates to compounds of Formula (I) and/or Formula (Ia):

and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK k...

02/02/2012
20120022077NOVEL CYANOPYRIMIDINE DERIVATIVE
The present invention relates to a novel cyanopyrimidine compound and a pharmaceutical composition which have a safe and potent adenosine A2a receptor agonistic activity....
01/26/2012
20120015956DEUTERIUM-ENRICHED DASATINIB
The present application describes deuterium-enriched dasatinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same....
01/19/2012
20120015027F, G, H, I and K Crystal Forms of Imatinib Mesylate
The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, cert...
01/19/2012
20120010182Chemical Compounds
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

More particularly the invention relates to new sulf...

01/12/2012
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
20110319420PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the...
12/29/2011
20110319379Substituted Indazole Amides And Their Use As Glucokinase Activators
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. C...
12/29/2011
20110319392Thiazole Sulfonamide And Oxazole Sulfonamide Kinase Inhibitors
The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents....
12/29/2011
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