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Class 544/59 - Thiomorpholines (i.e., fully hydrogenated 1,4-thiazines)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the six-membered hetero ring contains
No. of patents: 327
Last issue date: 12/06/2011


1                  
NumberTitleIssue Date
8071762Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2
12/06/2011
7714126Diacylglycerol acyltransferase inhibitors
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
05/11/2010
7435851Puleganic 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
7393852Piperazine 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
7332511Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular an...
02/19/2008
7285686Process for the preparation of 1,3-substituted indenes
An improved process for the preparation of 1,3 substituted indenes which are useful intermediates in the synthesis of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders. ...
10/23/2007
7285565Benzamides 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
7273863Benzophenones as inhibitors of reverse transcriptase
The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections. ...
09/25/2007
7256275Methods, kits and compositions pertaining to combination oligomers and libraries for their preparation
This invention pertains to the field of combination oligomers, including the block synthesis of combination oligomers in the absence of a template, as well as related methods, kits, libraries and other compositions. ...
08/14/2007
7256152Composition of catalyst and solvent and catalysis processes using this composition
A composition defined: either as comprising at least one Broensted acid, designated HB, dissolved in a liquid medium with an ionic nature of general formula Q+A−, in which Q+ represents an organic cation and A− represents an an...
08/14/2007
7229803Reaction of (di)amines in the presence of a lysine oxidase and of a reducing agent
The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing c...
06/12/2007
721471420-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a...
05/08/2007
7153858Arylpiperazinyl compounds
The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT rec...
12/26/2006
7141560Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of th...
11/28/2006
7129228Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
10/31/2006
7112582Bicyclic 6-alkylidene-penems as β-lactamase inhibitors
The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B den...
09/26/2006
7112679Convergent synthesis of α-aryl-β-ketonitriles
The present invention relates to processes for the production of α-aryl-β-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists....
09/26/2006
7105507Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R
09/12/2006
7060856Polymorphic form of N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide
This invention provides a novel polymorphic form of N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, as well a pharmaceutical compositions and therapeutic methods utilizing the polymorphic form. ...
06/13/2006
7053071Induction of apoptosis in cancer cells
The present invention provides compounds that are inducers or inhibitors of apoptosis or 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...
05/30/2006
7053085EP receptor agonist, compositions and methods thereof
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a ...
05/30/2006
7053212Acyclic amide and sulfonamide ligands for the estrogen receptor
The present invention provides estrogen receptor (ER) ligands of structural formula (I) the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the...
05/30/2006
7045517Triazine compounds
This invention relates to triazine compounds of formula (I): R1 is , aryl, or heteroaryl; each of R2, R4, and R5, independently,...
05/16/2006
7026510Quaternary ammonium salts of omega-aminoalkylamides of r-2-aryl-propionic acids and pharmaceutical compositions containing them
(R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparati...
04/11/2006
7015217Cyclic sulfone derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel cyclic sulfone derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α c...
03/21/2006
7001905Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are us...
02/21/2006
6995183Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n+m less then or equal to 2;
02/07/2006
6992081Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases. ...
01/31/2006
6984639Heterocyclic ketone and thioester compounds and uses
This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neu...
01/10/2006
6972287Method of inhibiting amyloid protein aggregation and imaging amyloid deposits
The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well...
12/06/2005
6958332Pyrimidine compounds
This invention features pyrimidine compounds of formula (I): each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alky...
10/25/2005
6943196NF-κB inhibitor comprising phenylmethyl benzoquinone as the active ingredient
An NF-κB inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R...
09/13/2005
6940092Electrically conducting organic compound and electronic device
An electrically conducting organic compound comprising a condensed polycyclic aromatic compound containing from 8 to 14 condensed rings and being solubilized in a solvent by the introduction of a functional group into any condensed ring of the compound. The electric...
09/06/2005
6916800Combination therapy including a matrix metalloproteinase inhibitor and an antineoplastic agent
The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent. ...
07/12/2005
6903092Naphthamide neurokinin antagonists for use as medicaments
Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compoun...
06/07/2005
6900350Method for the production of ω-aminoalkylsulphonic acids
The invention relates to a method for the production of ω-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have t...
05/31/2005
6900313Chiral ionic liquids
The invention relates to chiral ionic liquids of the general formula [A]n+[Y]n−, whereby n=1 or 2, the anion [Y]n− is the anion of an organic or inorganic proton acid and the cation [A]+ ...
05/31/2005
6897210Quinazoline derivatives and pharmaceutical compositions containing them
The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR
05/24/2005
6858598Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
A method of using an MMP inhibitor and optionally radiation therapy, and one or more antineoplastic agents of the topoisomerase class selected from the group consisting of irinotecan and topotecan, as a combination therapy for the treatment of neoplasia is disclosed...
02/22/2005
6844366Sulfonamide hydroxamates
This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds. ...
01/18/2005
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