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Class 548/313.1 - Additional diverse hetero ring attached directly or indirectly to a diazole ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds containing an additional hetero ring other than
No. of patents: 112
Last issue date: 02/15/2011


1      
NumberTitleIssue Date
7888516TGF-β gene expression inhibitor
A TGF-β gene expression inhibitor containing a pyrrole-immidazole polyamide comprising an N-methylpyrrole unit (hereinafter also referred to as Py), an N-methylimidazole unit (hereinafter also referred to as Im) and a γ-aminobutyric acid unit which can be folded i...
02/15/2011
7399778Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted ph...
07/15/2008
7199145Derivatives of hydantoins, thiohydantoins, pyrimidinediones and thioxopyrimidinones, their preparation processes and their use as medicaments
Compounds of the formula in racemic or enantiomeric forms wherein the substituents are as defined in the application. Useful for treating acromegalia, hypophyseal adenomas or endocrinic gastroenteropancre...
04/03/2007
7141680Aromatic compounds possessing antifungal or antibacterial activity
The present invention provides novel compounds possessing antibacterial, and/or antifungal activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided. ...
11/28/2006
7132543Para-phenylenediamine derivatives containing a disubstituted pyrrolidinyl group bearing a cationic radical, and use of the same for dyeing keratin fibers
The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenyl...
11/07/2006
7078528Biimidazole diamide anion binding agents
Biimidazole diamide compounds that are useful for binding anions such as sulfate are described, along with the use thereof for purposes such as extracting anions from a waste stream and/or detecting anions. ...
07/18/2006
6906199Process for preparing distamycin derivatives
It is described a process for preparing, in high yields and purity and without the need of carrying out several steps and/or isolating many intermediates which could lead to undesired by-products, a distamycin derivative of formula
06/14/2005
6903221Method for producing β-ketoenol esters
The invention relates to a method for producing β-ketoenol esters of the general formula (Ia) or (Ib), wherein Ar, Ra and Rb are defined as in claim 1. The inventive method is characterized by reacting an arylhalogenide of the general f...
06/07/2005
6753316Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1
06/22/2004
6683189Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise ...
01/27/2004
6673940Compositions and methods relating to cyclic compounds that undergo nucleotide base pair-specific interactions with double-stranded nucleic acids
The design, synthesis, and use of cyclic compounds, including cyclic polyamides, is described. Such compounds comprise at least two polymer portions, one of which comprises at least three molecular units, and the other comprises at least four molecular un...
01/06/2004
6555692Preparation and use of bifunctional molecules having DNA sequence binding specificity
Novel small molecule polyamides that specifically bind with subnanomolar affinity to a predetermined sequence with potential use in molecular biology and human medicine are described. The designed compounds which target the minor groove of B-form double h...
04/29/2003
6472537Polyamides for binding in the minor groove of double stranded DNA
The invention encompasses improved polyamides for binding to specific nucleotide sequences in the minor groove of double stranded DNA. The 3-hydroxy-N-methylpyrrole/N-methylpyrrole carboxamide pair specifically recognizes the T.multidot.A base pair, while...
10/29/2002
6159995Substituted diaminocarboxylic acids
Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved....
12/12/2000
6090947Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise ...
07/18/2000
5719240Compounds containing cyclic amidine and uretdione groups, a process for their preparation and the use thereof
A compound containing cyclic amidine groups and uretdione groups, having the formula: ##STR1## wherein X is O or NR2, R is the hydrocarbon radical of isophorone diisocyanate: ##STR2## R1 is a substituted (cyclo)alkylen...
02/17/1998
5698563Bis-›hydrazones!
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the format...
12/16/1997
5668165Small molecule inhibition of RNA/ligand binding
Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule that binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are compounds exemp...
09/16/1997
5470834Sulfoximine and suldodiimine matrix metalloproteinase inhibitors
Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of the formula, ##STR1## wherein: R1 is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino lower-alkyl, carbamoyl lower-alkyl, lower-alkyl ...
11/28/1995
5401851Angiotensin II antagonists
This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals....
03/28/1995
5352831Oligomeric cyanoguanidines
Oligomeric cyanoguanidines of formula I ##STR1## wherein, for example, R1 and R2 are each phenyl, R is 1,4-phenylene and n is an integer from 1 to 20, are suitable latent hardeners for epoxy resins. They are readily soluble in s...
10/04/1994
5340828Inhibitors of farnesyl protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
08/23/1994
5326773Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent...
07/05/1994
5290670Silver halide photographic elements
An infrared sensitive silver halide photographic element which contains an infrared-absorbing dye represented by the following formula ##STR1## wherein: R1 and R2 each independently represents a sulfoalkyl or a sulfatoalkyl grou...
03/01/1994
5258357Carboxamides, their preparation and their use as herbicides
Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur; R1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl; R2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl ...
11/02/1993
5242939Anilide derivatives with angiotensin II antagonist properties
This invention relates to anilide derivatives of Formula I ##STR1## which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods o...
09/07/1993
5235057Aminodiol derivatives
The invention relates to compounds of the formula ##STR1## in which R1 and R2 are identical or different and are hydrogen or aralkyl, R3 is alkyl, cycloalkyl or cycloalkylalkyl, R4 and R5 are ide...
08/10/1993
5233029Elaiophylin derivatives and a process for the preparation thereof
The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have antibacterial and antiviral activity....
08/03/1993
5212316Ethers and thioethers having therapeutical activity, their preparation and pharmaceutical compositions containing them
Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH2 OCH2)n being n=or 2, a a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxola...
05/18/1993
5212291Anthracycline derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions ...
05/18/1993
5187290Acylaminoalkanoyl urethanes or thiourethanes
Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful a...
02/16/1993
5183810Imidazole angiotensin II antagonists incorporating a substituted benzyl element
Substituted imidazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists. ##STR1##...
02/02/1993
51380643-Pyrrolidinylthio-1-azabicyclo-[3.2.0]hept-2-ene-2-carboxylic acid compounds
Novel 3-pyrrolidinylthio-1-azabiycyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof have antimicrobial activity and are useful as medicaments in the treatment of infectious diseases caused by pathogenic microo...
08/11/1992
5116835Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof
Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof. The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one anothe...
05/26/1992
5116827Quinolinecarboxylic acid derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions ...
05/26/1992
51149612,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3, 4 ...
05/19/1992
5084465Antifungal carbinols
Antifungal carbinols, particularly ଱-styryl carbinols, and the corresponding epoxy carbinols are provided. These carbinol compounds have the formula: ##STR1## or a pharmaceutically or agriculturally suitable salt thereof wherein E is a bon...
01/28/1992
5077283Solubilized imidazole pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, quanidine, isourea, isothiourea and biguanide functions ...
12/31/1991
5075301Furan derivatives useful for the treatment of gastro-intestinal disorders
A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with gastrointestinal dyskinesia....
12/24/1991
5032590Substituted hydroxylamines
Substituted hydroxylamines of the formula ##STR1## in which R1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis....
07/16/1991
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