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Class 548/477 - Nitrogen attached indirectly to the ring nitrogen of the five-membered hetero ring by acyclic nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached indirectly to the
No. of patents: 156
Last issue date: 05/17/2011


1        
NumberTitleIssue Date
7943785Process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2- phthalimidomethylcyclopropane
The present invention provides a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-phthalimidomethylcyclopropane, which includes reacting (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-hydroxymethylcyclopropane with an orthoester and a brønsted acid, a...
05/17/2011
7820831Compounds comprising a thiocarbonyl-sulfanyl group which can be used for the radical synthesis of α-perfluoroalkylamine compounds
The invention relates to compounds having the general formula (I), the method of preparation thereof and the use thereof in organic radical synthesis. The invention also relates to compounds having the formula (II), the method of preparation thereof and a method for...
10/26/2010
7405237Isoindoline compounds and methods of their use
Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclos...
07/29/2008
7345062Substituted acylhydroxamic acids and method of reducing TNFαlevels
Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate. ...
03/18/2008
7262222Synergistic mixtures of o-phenylphenol and other nitrogen and aldehyde microbiocides
Ortho phenylphenol or its sodium salt is shown to form synergistic antimicrobial mixtures with nitrogen and aldehyde-containing microbiocides. ...
08/28/2007
7244759Isoindoline compounds and methods of making and using the same
The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel...
07/17/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7081464Topical compositions of cyclic amides as immunotherapeutic agents
Novel amides and imides are inhibitors of tumor necrosis factorα and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. ...
07/25/2006
7056932Heterocyclyl substituted 1-alkoxy acetic acid amides
The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as ...
06/06/2006
6989401Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products
The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable s...
01/24/2006
6939986Process for preparing 1,2-diamino compounds
The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides. ...
09/06/2005
6911464N-alkyl-hydroxamic acid-isoindolyl compounds and their pharmaceutical uses
The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases a...
06/28/2005
6844359Substituted imides
Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2-Phthalimido-3-(3′,4′-dimethoxyphenyl)propane. ...
01/18/2005
6812237N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in ...
11/02/2004
6699899Substituted acylhydroxamic acids and method of reducing TNF଱ levels
Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF଱ and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)p ropanoate....
03/02/2004
6693202Muscarinic receptor antagonists
Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscari...
02/17/2004
6660736Phthalimido derivatives and a process for their preparation
This invention relates to phthalimido derivatives of the formula ##STR1## wherein X is --N.dbd. or --CH.dbd., and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention f...
12/09/2003
6498004Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): Ɗ-(t)m -XY' (a) XY'-(t)m -Ɗ (b) Ɗ-(t)m -XY'-(...
12/24/2002
6436949Heterocyclically substituted benzamides and their use
Heterocyclically substituted benzamides of the formula I ##STR1## are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for con...
08/20/2002
6429221Substituted imides
Novel imides are inhibitors of tumor necrosis factor ଱ and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-Phthalimido-3-(3',4'-dimethoxyphenyl)propane....
08/06/2002
6359061Amide compound libraries
Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds. ...
03/19/2002
6352958Cycloimido-substituted benzofused heterocyclic herbicides
Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: ##STR1## where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-...
03/05/2002
6342508N-hydroxy-2-(Alkyl,Aryl or Heteroaryl sulfanyl, sulfinyl or sulfonyl) 3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
Matrix metalloproteinases (MMps) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase...
01/29/2002
6310057଱-ketoamide multicatalytic protease inhibitors
This invention relates to ଱-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retar...
10/30/2001
6306873Substituted ଲ-thiocarboxylic acids
This invention relates to compounds of general formula (I): ##STR1## in which Ar is a group selected from: ##STR2## A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These c...
10/23/2001
6294573Reverse hydroxamate inhibitors of matrix metalloproteinases
Compounds having the formula ##STR1## are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal....
09/25/2001
6288063Substituted 4-biarylbutyric and 5-biarylpentanoic acid derivatives as matrix metalloprotease inhibitors
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)x A--B--D--E--G whe...
09/11/2001
6277987Sulfonylamino acid and sulfonylamino hydroxamic acid derivatives
Compounds of formula ##STR1## wherein W is --OH or --NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)m moiety by a ring nitrogen, --CONR2 ...
08/21/2001
6265432Flourine-substituted biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A,...
07/24/2001
6239288Biphenyl hydroxy imino butyric acids and their derivatives for treating arthritis
Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) an...
05/29/2001
6235922Processes and intermediates for preparing benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP
Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## wherein: Y1 and Y2 are each independently hydrogen, alkyl, aryl,...
05/22/2001
6172057N-Hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase...
01/09/2001
6172085Cyclic ether compounds as sodium channel modulators
A compound of the formula: ##STR1## wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lowe...
01/09/2001
6169103Fluorine-substituted biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A,...
01/02/2001
6160126Synthetic Intermediates for the preparation of N, N'-Di-substituted isothiourea derivatives and N-cyclic(methyl)-N'-Substituted isothiourea derivatives
Novel Intermediates ##STR1## wherein R is a substituted or unsubstituted hydrocarbon residue or acyl group; X is an electron withdrawing group; Y1 and Y2, which are the same or different, are each independently oxygen or sulfur;...
12/12/2000
6150416Nanomolar, non-peptide inhibitors of cathepsin D
The present invention provides non-peptide cathepsin D binding compounds and methods for using such compounds in the detection, labelling and inhibition of cathepsin D....
11/21/2000
6114372Peptidyl compounds having MMP and TNF inhibitory activity
Compounds of formula (I) having MMP and TNF inhibitory activity. ##STR1##...
09/05/2000
6090840Peptidyl compounds having MMP and TNF inhibitory activity
The subject invention concerns mercaptoalkylacyl compounds of formula (I): ##STR1## The compounds of the subject invention can be used to inhibit matrix metalloproteinases and/or TNF଱- and L-selectin sheddase-mediated diseases including degener...
07/18/2000
6066743Solventless preparation of phthalimides
A method for the solventless synthesis of a phthalimide or phthalimide mixture is provided comprising contacting at least one amine reactant and at least one anhydride reactant in a solventless environment at a first temperature sufficient to allow the re...
05/23/2000
6017889Metalloproteinase inhibitors
Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption. ##STR1##...
01/25/2000
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