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Class 514/254.02 - The additional five-membered hetero ring also has chalcogen as a ring member


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein nitrogen and chalcogen (i.e. oxygen,
No. of applications: 407
Last issue date: 05/24/2012


1                      
Application No.Application TitleIssue Date
20120129811TRICYCLIC INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented ...
05/24/2012
20120129842BISTHIAZOLE INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

05/24/2012

20120129872FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

05/24/2012

20120128625COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells....
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
20120129847COMPOSITIONS AND METHODS FOR TREATING OCULAR EDEMA, NEOVASCULARIZATION AND RELATED DISEASES
Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (we...
05/24/2012
20120108591ALKYLSULFINYL-SUBSTITUTED THIAZOLIDE COMPOUNDS
A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses....
05/03/2012
20120108565PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS
The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaer...
05/03/2012
20120108571SUBSTITUTED PHENOXY N-ALKYLATED THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS
The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ...

05/03/2012
20120083490CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF
The present invention features compounds of formula I

or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. T...

04/05/2012
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
20120046286Novel Compounds
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, ...

02/23/2012
20120028920DERIVATIVES OF 4-PIPERAZIN-1-YL-4-BENZO[B]THIOPHENE SUITABLE FOR THE TREATMENT OF CNS DISORDERS
A heterocyclic compound or a salt thereof represented by the formula (1):

    • where R2 ...
02/02/2012
201200289903 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE
A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, ...
02/02/2012
20120022078ARYL INDOLE DERIVATIVES
A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alky...
01/26/2012
20120022052SMALL MOLECULE INHIBITORS OF KYNURENINE-3-MONOOXYGENASE
The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.

...

01/26/2012
201200159581-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES
The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C...
01/19/2012
20120015959HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS
Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours....
01/19/2012
20120015957PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) 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 ...
01/19/2012
20120015954THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
A compound of formula:

wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptab...

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
20120004216MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating A...
01/05/2012
20110319423NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME
The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound...
12/29/2011
20110312969COMPOUNDS FOR TREATING CANCER
Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dy...
12/22/2011
20110306620Heteroarylpiperidine And-Piperazine Derivatives
Heteroarylpiperidine and -piperazine derivatives of the formula (I),

in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phyto...

12/15/2011
20110301158ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS
This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial....
12/08/2011
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
20110301176IMIDAZOTHIAZOLE DERIVATIVES HAVING PROLINE RING STRUCTURE
There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhib...
12/08/2011
20110301149COMPOSITIONS AND METHODS FOR TREATING ALCOHOL USE DISORDERS, PAIN AND OTHER DISEASES
The present invention provides compounds which antagonize epsilon protein kinase C (PKCε). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating v...
12/08/2011
20110294813OXAZOLIDINONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.

A compound represented by the formula:

its pharmaceutically acceptable salt, or ...

12/01/2011
20110294822Substituted Phenylpiperazinyl Aralkylalcohol Derivatives, Pharmaceutical Compositions Containing Such Derivatives and Uses Thereof
The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate,

wherein C1 and C2 represent chiral ...

12/01/2011
20110294780SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-a MODULATORS
The present invention relates to compounds of Formula (I),

methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ...

12/01/2011
20110288083METHOD OF TREATING CANCER BY INHIBITION OF PROTEIN KINASE-LIKE ENDOPLASMIC RETICULUM PROTEIN KINASE
The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are select...
11/24/2011
20110288088SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be use...
11/24/2011
20110275609BICYCLIC PYRAZOLO-HETEROCYCLES
The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I

The structures of rings A and B and substituents Ra, Rb and Rc are d...

11/10/2011
20110275636DESAZADESFERROTHIOCIN AND DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS
Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals...
11/10/2011
20110269750ROFLUMILAST FOR THE TREATMENT OF DIABETES MELLITUS
The application relates to specific combinations of Roflumilast and/or Roflumilast N-Oxide and a PPAR-agonist, as well as their use in the treatment of diabetes mellitus type 2....
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
20110269817COMPOSITIONS AND METHODS RELATED TO SIRT1 FUNCTION
The invention relates to modulation of circadian rhythm and underlying biological processes....
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
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