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Class 514/231.2 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the six-membered hetero ring has
No. of patents: 413
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188077Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. ...
05/29/2012
8053432Cyclic hydroxylamine as psychoactive compounds
A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected ...
11/08/2011
8034810Arylsulfonamido-substituted hydroxamic acid derivatives
α-Amino hydroxamic acid derivative of the formula I, in which R is C2-C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5
10/11/2011
7973037Cathepsin cysteine protease inhibitors
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s...
07/05/2011
7902188Morpholine dopamine agonists
The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and...
03/08/2011
7897598Inhibitors of the anandamide transporter
Analogs that inhibit the transport of anandamide across cell membranes. The inhibitors are amide and ester analogs of anandamide having a tail portion X that is a fatty acid chain remnant, a central portion Y that is an amide or ester radical and a head portion Z th...
03/01/2011
7897599Cytokine inhibitors
The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such ag...
03/01/2011
7858618Compounds
The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the dias...
12/28/2010
7842690Cyclic hydroxylamine as psychoactive compounds
A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected ...
11/30/2010
7842689Cyclic hydroxylamine as psychoactive compounds
A compound of formula (II): in which— R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R re...
11/30/2010
7820656Pharmaceutical composition comprising N-aryl N′ morpholino/piperidino thiocarbamide derivatives for treating type II diabetes
Disclosed is a medicament comprising N-aryl N′ morpholino/piperidino thiocarbamide derivatives represented by the following formula 1 for preventing and treating diabetes, diabetic complications, insulin resistance and insulin resistance syndrome, and can be used ...
10/26/2010
78120174-substituted indole and indoline compounds
The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to phar...
10/12/2010
7807669Biaromatic compounds which activate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardio...
10/05/2010
7749999Alpha-ketoamides and derivatives thereof
The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such ag...
07/06/2010
7737139Sulfonic acids, their derivatives and pharmaceutical compositions containing them
Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane...
06/15/2010
7732443Therapeutic substituted cyclopentanes
Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness. ...
06/08/2010
7723328Methods of facilitating cell survival using neurotrophin mimetics
Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural a...
05/25/2010
7723327Carotenoid ester analogs or derivatives for the inhibition and amelioration of liver disease
A method of treating liver disease in a subject may include administering to the subject an effective amount of a pharmaceutically acceptable formulation. The pharmaceutically acceptable formulation may include a synthetic analog or derivative of a carotenoid. The s...
05/25/2010
7713967Therapeutic substituted hydantoins, and related compounds
Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed,...
05/11/2010
7671049Pyrrole based inhibitors of glycogen synthase kinase 3
New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed al...
03/02/2010
7666865Calcium channel blockers
Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organi...
02/23/2010
7666866Antithrombotic diamides
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation a...
02/23/2010
7550461Benzofuran and benzothiophene compounds useful in treating cytokine mediated diseases
Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes ...
06/23/2009
7534790Ion channel modulating compounds and uses thereof
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatme...
05/19/2009
7514431Piperidinyl cyclopentyl aryl benzylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In par...
04/07/2009
7452878Biaromatic compounds which activate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardio...
11/18/2008
74427162-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to t...
10/28/2008
7425555Heteroaryl substituted biphenyl derivatives as p38 kinase inhibitors
Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38. ...
09/16/2008
7417042Compounds for enzyme inhibition
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited b...
08/26/2008
7414067Ophthalmic compositions for treating ocular hypertension
This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such co...
08/19/2008
74140543-(arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ...
08/19/2008
7407985Compounds that abrogate DNA damage induced cell cycle G2 checkpoint and/or augment anti-cancer activity of DNA-damaging treatments
The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to...
08/05/2008
7390803Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28...
06/24/2008
7388007Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6
06/17/2008
7378446Compound having anti-HCV activity and process for producing the same
The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV,...
05/27/2008
7371749Benzothiazole derivatives
The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with t...
05/13/2008
73717461,2,4-Thiadiazole compounds and pests controlling composition containing the same
The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene o...
05/13/2008
7365066Pyrazolopyridine derivatives as pharmaceutical agents
Novel pyrazolopyridine derivative compounds are disclosed and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors useful in the treatment of cancer and other disease states influenced by TGF beta. ...
04/29/2008
7365095Chromane and chromene derivatives and uses thereof
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subc...
04/29/2008
7358247Mycophenolate mofetil impurity
Provided is an impurity of mycophenolate mofetil, processes for its preparation and its use as a reference. ...
04/15/2008
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