Class 514/227.5 - 1,4-Thiazines

Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the hetero ring has the following
No. of patents: 418
Last issue date: 05/08/2012

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Number	Title	Issue Date
8173643	N-substituted thiomorpholine derivatives as the inhibitors of dipeptidyl peptidase IV and the pharmaceutical uses thereof The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method f...	05/08/2012
8088763	Cyclohexyl-1, 4-diamine compounds Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including the...	01/03/2012
RE42700	Induction of apoptosis in cancer cells The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of...	09/13/2011
8012962	Substituted thiomorpholine derivatives The present invention relates to thiomorpholine derivatives of formula I or pharmaceutically acceptable salts thereof and their use in treating seizure disorders, anxiety disorders, bipolar disorders, neuropathic pain disorders and migraine pain disorders.	09/06/2011
7964592	2,4-di (phenylamino) pyrimidines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders Novel pyrimidine derivatives of formula I to process for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. ...	06/21/2011
7767666	Butyl and butynyl benzyl amine compounds Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases. ...	08/03/2010
7696198	Phosphodiesterase 4 inhibitors Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of...	04/13/2010
7683054	Galenic formulations of organic compounds The present invention relates to a solid oral dosage form comprising a therapeutically effective amount of aliskiren or a pharmaceutically acceptable salt thereof, and wherein the active ingredient is present in an amount of more than 46% by weight based on the tota...	03/23/2010
7683055	Lanthionine-related compounds for the treatment of inflammatory diseases The present invention provides compositions comprising lanthionine ketimine derivatives and thiomorpholine dicarboxylic acid derivatives, as well as processes for the preparation of such compounds. The invention also concerns the use of lanthionine, lanthionine keti...	03/23/2010
7648984	Antibacterial agents Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein. ...	01/19/2010
7572790	Biphenyl carboxylic amide p38 kinase inhibitors Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...	08/11/2009
7517877	5-substituted-alkylaminopyrazole derivatives as pesticides The invention relates to the use for the control of parasites in animals, of a compound which is a 5-substituted-alkylaminopyrazole derivative of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to novel 5-substituted-alk...	04/14/2009
7514428	Pesticidal 1-aryl-3-amidoxime-pyrazole derivatives 1-Arylpyrazole-3-substituted-amidoxime derivatives of formula (Ia) or (Ib): or salts thereof, wherein the various symbols are as defined in the description, and pesticidal compositions thereof, processes for their preparati...	04/07/2009
7511036	Dihydrothiazine prodrugs of thiazolium agents Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or α-hydroxyethyl; R...	03/31/2009
7501408	Inhibitors of cathepsin S The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides m...	03/10/2009
7482340	Pyridine derivatives useful for inhibiting sodium/calcium exchange system Therapeutically active compounds of formula (I) or (II): wherein the variables in formulas (I) and (II) are defined in the description, and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhi...	01/27/2009
7446104	Phenylalkynes Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...	11/04/2008
7435851	Puleganic amides The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods. ...	10/14/2008
7435732	Crystalline polymorphs of (3S)-N-hydroxy-4-({4-[-(4-hydroxy-2-butynyl)oxy]phenyl}sulfonyl)-2,2-dimethyl-3-thiomorpholine carboxamide This invention relates to crystalline polymorphs of (3S)-N-hydroxy4-({4-[(4-hydroxy-2-butynyl)oxy]phenyl}sulfonyl)-2,2-dimethyl-3-thiomorpholine carboxamide, and preparation and uses thereof. ...	10/14/2008
7429581	Pyrazole-derivatives as factor Xa inhibitors The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is...	09/30/2008
7393852	Piperazine derivatives and methods of use Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for...	07/01/2008
7381719	Diaryl ethers as opioid receptor antagonist A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o...	06/03/2008
7378421	Chromenone derivatives Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for...	05/27/2008
7358376	Substituted Thiophene compounds The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical c...	04/15/2008
7354934	Chemokine 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
7351703	Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compound...	04/01/2008
7348440	Mitotic kinesin inhibitors The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comp...	03/25/2008
7348341	Chemical compounds The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity. ...	03/25/2008
7342028	Medical use for tachykinin antagonists The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharm...	03/11/2008
7335753	Bifunctional heterocyclic compounds and methods of making and using same The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using...	02/26/2008
7329670	Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre...	02/12/2008
7329655	Nitrogenous heterocyclic compounds The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to ...	02/12/2008
7323563	Hydroxamic acid derivatives as antibacterials A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily accepta...	01/29/2008
7314938	Modulators of cellular adhesion The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1	01/01/2008
7314939	Compositions and methods for inhibiting TGF-β The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R...	01/01/2008
7304057	Substituted 6-membered N-heterocyclic compounds and method for their use as neurological regulator This invention relates to substituted 6-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R1, R2, X, Y, and Z are as defined in the description; their preparation me...	12/04/2007
7294637	Method of treating addiction or dependence using a ligand for a monamine receptor or transporter One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substitute...	11/13/2007
7288526	Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...	10/30/2007
7285565	Benzamides and related inhibitors of factor Xa Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. ...	10/23/2007
7282496	Allenic aryl sulfonamide hydroxamic acids as matrix metalloproteinase and TACE inhibitors Compounds of the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease, degenera...	10/16/2007

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Class 514/227.5 - 1,4-Thiazines