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Class 514/227.8 - Additional hetero ring attached directly or indirectly to the 1,4-thiazine by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the 1, 4-thiazines is attached directly
No. of patents: 681
Last issue date: 03/27/2012


1                      
NumberTitleIssue Date
81432461-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives
The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkylo...
03/27/2012
8133886Heterobicyclic carboxamides as inhibitors for kinases
The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical ...
03/13/2012
8058268Neuroprotective agents for the prevention and treatment of neurodegenerative diseases
Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: wherein α and R1-R8 are described herein, or a compound hav...
11/15/2011
7960376Benzo-fused heterocycles
The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof.
06/14/2011
7910582Cyclopropyl amines as modulators of the histamine Hreceptor
Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases. ...
03/22/2011
7910581Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl] methyl}-4-methylpiperazine, synthesis process and uses thereof
The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low t...
03/22/2011
7897597Aryloxy and arylalkyleneoxy substituted imidazoquinolines
Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokin...
03/01/2011
7888351Organic compounds
The present invention relates to compounds of the formula; and their use in therapy. ...
02/15/2011
7884098Anthranilamide inhibitors of aurora kinase
The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1′ R2, R
02/08/2011
7875606Izoxazoline derivative and herbicide
The present invention aims at providing an isoxazoline derivative and a pharmaceutically acceptable salt thereof, both having an excellent herbicidal effect and an excellent selectivity between crop and weed. The isoxazoline derivative of the present inventio...
01/25/2011
7820654Pyrimidine compounds, process for their preparation and compositions containing them
The present invention is directed to a compounds, methods and compositions for making the compounds and methods of treating a variety of diseases and disease states including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease s...
10/26/2010
7816349Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Form...
10/19/2010
7786110Thiazole and oxazole-substituted arylamides as P2Xand P2Xantagonists
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R...
08/31/2010
7763608Factor Xa inhibitors
The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical...
07/27/2010
7713963Acylated indanyl amines and their use as pharmaceuticals
The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1
05/11/2010
7709473Substituted 2H-[1,2,4]triazolo[4,3-a]pyrazines as GSK-3 inhibitors
The invention relates to compounds of formula (I) prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein Ra, Rb, R1 and R2 are as defined herein; pharmaceutical compositions ther...
05/04/2010
7696199Sigma receptor inhibitors
The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a di...
04/13/2010
7662813Triazole compounds that modulate HSP90 activity
The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treati...
02/16/2010
7655649Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the comp...
02/02/2010
7645753Benzothiazole, thiazolopyridine, benzooxazole and oxazolopyridine derivatives
This invention is concerned with compounds of the formula wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts there...
01/12/2010
7615550Substituted piperazines,(1,4) diazepines, and 2,5-diazabicyclo (2.2.1)iieptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease...
11/10/2009
7608617Naphthaline derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the ...
10/27/2009
7589088Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
Compounds are provided having the formula (I) wherein R, B, X and Y are as defined herein. ...
09/15/2009
7524842Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by ...
04/28/2009
7491718Sulfonamides having antiangiogenic and anticancer activity
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer....
02/17/2009
7470681Pyrimidine compounds
This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H;...
12/30/2008
7465725Pyrimidine compounds
This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, ...
12/16/2008
7449457Substituted heterocyclic carboxamides with antithrombotic activity
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefo...
11/11/2008
7432254Method for treating glaucoma IC
Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation im...
10/07/2008
7427612Benzoyl-piperazine derivatives
A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in ...
09/23/2008
7414047Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
08/19/2008
7384939Process for preparation of pyridine derivatives of NK-1 receptor antagonist
The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein. ...
06/10/2008
7368461Compounds and method for the treatment of overactive bladder
NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed: wherein in said compounds D, A, R1, R3 and ...
05/06/2008
7354932Chemokine receptor binding heterocyclic compounds with enhanced efficacy
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and opt...
04/08/2008
7354929Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...
04/08/2008
7351721Amino acid derivatives and pharmaceutical composition comprising, as active ingredients, them
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-...
04/01/2008
7351724Oxadiazole ketone inhibitors of fatty acid amide hydrolase
Certain oxadiazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the ...
04/01/2008
73421153-substituted-6-aryl pyridines
3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred...
03/11/2008
7335658Pyridazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): ...
02/26/2008
7329658Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. ...
02/12/2008
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