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Class 544/147 - Additional oxygen containing hetero ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds having, in addition to the morpholine ring, a
No. of patents: 110
Last issue date: 09/30/2008


1      
NumberTitleIssue Date
7429660ATM inhibitors
A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an op...
09/30/2008
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
7390898Cytotoxic agents containing novel potent taxanes and their therapeutic use
Included within the scope of the present invention are potent taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell pop...
06/24/2008
7297714Inhibitors 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...
11/20/2007
7276499Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking gro...
10/02/2007
7271264Pentacyclic oxepines and derivatives thereof, compositions and methods
The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6
09/18/2007
7232818Compounds 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...
06/19/2007
7217819Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking gro...
05/15/2007
7049313ATM inhibitors
The application concerns a compound of formula I: wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3
05/23/2006
7008940Dihydrobenzofuran derivatives, process for the preparing thereof and agents
A compound represented by the formula (I): or a salt thereof exhibits excellent inhibitory activity of lipid peroxidation and is useful as an agent for inhibiting lipoperoxide production, wherei...
03/07/2006
7008942Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking gro...
03/07/2006
6924285Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereois...
08/02/2005
6849658Biaromatic compounds and pharmaceutical and cosmetic compositions comprising them
The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8
02/01/2005
6849733Neuropeptide-Y ligands
There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of...
02/01/2005
6730671Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
05/04/2004
6723718Substituted α, β-anellated butyrolactones
The present invention relates to novel substituted α,β-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebra...
04/20/2004
6706708Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking gro...
03/16/2004
6683093Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrec...
01/27/2004
6677483Process for the production of monoamides of DTPA
A new process for the preparation of diethylenetriaminepentaacetic-monoamides in which amines can be reacted with sensitive groups, a higher mono/diamide selectivity is achieved, a higher yield of monoamide is achieved and has a simple reaction scheme and...
01/13/2004
6638967Thiophene of furan pyrrolidine compounds
Compounds of Formula I ##STR1## Wherein Z2 is an Oxygen or a Sulfur, Z1 is --CH.dbd.CH-- and Y is a bond, W1 and W2 are hydrogens and X1 and X2 are various heterocyclic rings are disclosed....
10/28/2003
6638930Morpholine and thiomorpholine tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiov...
10/28/2003
6608057Compounds useful as reversible inhibitors of cathepsin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds ##STR1##...
08/19/2003
6525086Compounds, their preparation and use
The present invention relates to compounds of formula (I) ##STR1## wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the speci...
02/25/2003
6486332Fluorescent pigments
Compounds of formula A(B)x, (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which ...
11/26/2002
6436931Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a ...
08/20/2002
6372738Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a ...
04/16/2002
6340701Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a ...
01/22/2002
6271401Fluorescent anthraquinoid pigments
Compounds of formula A(B)x, (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which...
08/07/2001
6242484Hypoestoxides, derivatives and agonists thereof for use of antiparasitic agents
Novel enhanced usage of hypoestoxides derivatives and agonists theeof as active agents against nucleated infectious entities including known parasites and the like microbiological insultors of living tissue, systems and organisms, known modes of administr...
06/05/2001
6166006Anilide derivative, production and use thereof
This invention is to provide a compound of the formula: ##STR1## wherein R1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-mem...
12/26/2000
6060468N-substituted azaheterocyclic compounds
The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R1, R1a, R2, R2a, p, r and s are as defined in the detailed part of the presen...
05/09/2000
6034239Tricyclic compounds, their production and use
A compound of the formula: ##STR1## wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydroc...
03/07/2000
5914351Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R1 is hydrogen, halogen, alkyl or alkoxy; R2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; a...
06/22/1999
5891368Fluoranthenopyrans
Described are novel photochromic 8-substituted fluoranthenopyran compounds having certain substituents at the 5 position of the pyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric org...
04/06/1999
5866577Aromatic amidine derivatives and salts thereof
An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from ...
02/02/1999
5847169Process for preparing oxiranemethanamine derivatives
A process for preparing oxiranemethane derivatives which are useful as intermediates for preparing aspartyl protease inhibitors comprising the steps of activating an aminodiol, acylating the aminodiol and reacting the acylated aminodiol with a base to for...
12/08/1998
5821263Sulfenamide taxane derivatives
This invention provides a novel series of taxane derivatives which are characterized by the C3' nitrogen bearing one or two sulfur substituents. The new derivatives are antitumor agents useful in the treatment of such cancers as ovarian, breast, lung, gas...
10/13/1998
5801193Compositions and methods for immunosuppressing
Methods and compounds for inducing immunosuppression in animals which need immunosuppressive treatment involving administration to animals of a therapeutically effective amount of a compound of the following formula ##STR1## where R is H, PO3
09/01/1998
5780653Nitrophenyl, 10-deacetylated substituted taxol derivatives as dual functional cytotoxic/radiosensitizers
In accordance with the present invention, there are provided derivatives of chemotherapeutic agents (e.g., paclitaxel), which serve as bifunctional agents. Invention derivatives retain the antitumor activity of the parent compound, and, coupled with the e...
07/14/1998
5763631Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R1 is a cycloalkyl, or arly-substituted lower alkyl group; K and J are independently a group having the formula of ...
06/09/1998
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