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Class 514/231.5 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the morpholine ring is attached
No. of patents: 575
Last issue date: 05/08/2012


1                      
NumberTitleIssue Date
8173647PI 3-kinase inhibitors and methods of their use
Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptabl...
05/08/2012
8158622Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, ...
04/17/2012
8138182Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient
The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of...
03/20/2012
8114870Method of treating disease states using substituted pyrazole compounds
Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein k...
02/14/2012
81060452-morpholino-4-pyrimidone compound
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R′ rep...
01/31/2012
8080545Compounds for enzyme inhibition
One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compo...
12/20/2011
8039468Method of inhibition of respiratory depression using positive allosteric AMPA receptor modulators
The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the...
10/18/2011
7998957Oxabicycloheptanes and oxabicylcoheptenes, their preparation and use
This invention provides compounds having the structure which may be used for the treatment of tumors. ...
08/16/2011
7981887Therapeutic compounds
Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed, for treating ...
07/19/2011
7968542Thiophene compounds and thrombopoietin receptor activators
A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
06/28/2011
7968543Methods of administering -(5--butyl-isoxazol-3-yl)-′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea to treat proliferative disease
Provided herein are methods of administering N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt or solvate thereof, to human patients. Specifically, dosing, dosin...
06/28/2011
7964595Thiophenyl prostaglandin derivatives for treating glaucoma and ocular hypertension
Disclosed herein is a compound according to one of the formulas wherein R is Additionally, pharmaceutically acceptable salt thereof, and methods of treating disease, medicaments, ...
06/21/2011
7960378Therapeutic compounds
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, R1, R2, Z, and G are as described. Methods, compositions...
06/14/2011
7956051Therapeutic amides and related compounds
Disclosed herein are compounds useful in treating glaucoma, inflammatory bowel disease, the stimulation of hair growth, and the stimulation of the conversion of vellus hair to terminal hair. The compounds themselves are herein. ...
06/07/2011
7935696Heterocyclic amide compounds useful as kinase inhibitors
A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions asso...
05/03/2011
7863270IL-12 modulatory compounds
The invention relates to cyclic hydrazone compounds and compositions including the cyclic hydrazone compounds according to formula (I): The compounds (and compositions) are useful, inter alia, in modulating IL-12 production...
01/04/2011
7838520Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and cond...
11/23/2010
7807670Inhibitors of papilloma virus
A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as in...
10/05/2010
7803798Therapeutic compounds
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, D, and Y are as described. Methods, compositions, and medicaments related thereto are also disc...
09/28/2010
7803797Substituted arylcyclopentenes as therapeutic agents
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disc...
09/28/2010
7767669Small molecule PI 3-kinase inhibitors and methods of their use
Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable ca...
08/03/2010
7763611Aroylsemicarbazide derivatives against thromboembolic diseases
Novel compounds of the formula (I) in which Het, R1, R2 and R3 have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic dise...
07/27/2010
7763612Therapeutic amine-arylsulfonamide conjugate compounds
Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R′ is [D-W-], hydroxyl, or alkoxyl; R″ is independently [D-W′-], hydrog...
07/27/2010
7737140Therapeutic compounds
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicamen...
06/15/2010
7713968Substituted arylcyclopentenes as therapeutic agents
Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed. ...
05/11/2010
7691852Compounds for enzyme inhibition
One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compo...
04/06/2010
7666867Heteroindanes: a new class of potent cannabimimetic ligands
One aspect of the invention is concerned with cannabimimetic heteroindane analogs having affinities and/or selectivities for a cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and m...
02/23/2010
7622464Morpholinyl-urea derivatives for use in the treatment of inflammatory diseases
Compounds of formula (I): wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents —(CRnaRnb)n—; ...
11/24/2009
7615552Fused heterocyclic compounds
This invention provides fused heterocyclic compounds, pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12 related disease and disorders. ...
11/10/2009
7612064Sulfopyrroles
The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds...
11/03/2009
7612065Inhibitors of c-JUN N-terminal kinases (JNK)
The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
11/03/2009
7608618Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula wherein: Y′ is O or S, W′ is optionally substituted, Z′ is selected from the group consisting of
10/27/2009
7598242Compounds 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 MMPs, TNF-α or combinati...
10/06/2009
7579346Carboxamides
Novel compounds of the formula (I), in which D, W, X, Y, T, m and R1 have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the...
08/25/2009
7579347Vanilloid 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 and non-vascu...
08/25/2009
7563787Substituted pyrazole compounds
Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein k...
07/21/2009
7563786Substituted thiophenecarboxamides, their preparation and their use as medicaments
The present invention relates to novel substituted thiophene-2-carboxamides of the general formula in which A, Ar and R1 to R5 are as defined in claim 1, their tautomers, their enantiomers, thei...
07/21/2009
7534791Benzo[b]furane and benzo[b]thiophene derivatives
The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use. ...
05/19/2009
7501409Preparations for oral administration
The present invention provides a preparation for oral administration containing a medicinal substance having cGMP-specific phosphodiesterase inhibitory activity and showing decrease of solubility in the neutral and alkaline regions, wherein an acidic substance is co...
03/10/2009
7470685Pyrimidine compounds
This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl op...
12/30/2008
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