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Class 548/113 - Polycyclo ring system having the five-membered hetero ring as one of the cyclos


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the five-membered hetero ring is one of
No. of patents: 201
Last issue date: 08/09/2011


1            
NumberTitleIssue Date
7994335Electronically tuned ligands for asymmetric hydrogenation
Disclosed is a new class of chiral bidentate ligands capable of performing asymmetric hydrogenation. Also disclosed are processes of performing asymmetric hydrogenation the chiral bidentate ligands. ...
08/09/2011
7897781Cold menthol receptor-1 antagonists
The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated d...
03/01/2011
7893271Benzimidazole carbamates and (thio) carbamates, and the synthesis and use thereof
This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is ...
02/22/2011
7759491Method for producing indazol-3-ylmethyl phosphonium salt
The present invention provides a method for producing an indazol-3-ylmethyl phosphonium salt represented by Formula (IV): [wherein X represents halogen, OSO2Ra (wherein Ra represents substit...
07/20/2010
7709652Dual function UV-absorbers for ophthalmic lens materials
Disclosed are UV absorbers that contain a labile functional group capable of initiating free radical polymerization. ...
05/04/2010
7439385Process for the preparation of biphosphonic derivatives
The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halop...
10/21/2008
7410956Caspase inhibitor prodrugs
The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. ...
08/12/2008
7312219Heteroaromatic inhibitors of fructose 1,6-bisphosphatase
Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose. ...
12/25/2007
7235537N3 alkylated benzimidazole derivatives as MEK inhibitors
Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as ...
06/26/2007
7208606Hydroformylation process for the conversion of an ethylenically unsaturated compound to an alcohol
The invention pertains to a hydroformylation process for the conversion of an ethylenically unsaturated compound to an alcohol comprising a first step of reacting at an elevated temperature in a reactor the ethylenically unsaturated compound, carbon monoxide, hydrog...
04/24/2007
7205412Antibiotic additive and ink composition comprising the same
An antibiotic additive and an ink composition including the antibiotic additive include a compound produced by binding of an antibiotic substance having the following formula (I) to a predetermined additive via a chemical reaction. The ink composition includes a col...
04/17/2007
7192968Ethylenediamine derivatives
The invention relates a compound represented by the formula (1): Q1-Q2-C(═O)—N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 represent H...
03/20/2007
7183276Azole compounds
The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocycl...
02/27/2007
7160915N-methyl-substituted benzamidazoles
The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I): as defined in the specification; pharmaceutical compositions and methods of use thereof. ...
01/09/2007
7060290Phosphocholine linked prodrug derivatives
Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substitute...
06/13/2006
7030103Sulfonamidomethyl phosphonate inhibitors of β-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and...
04/18/2006
6960572Indolinones and uses thereof
This invention relates to compounds of the general formula: in which RA, RB, RC, RD, RE, p, q and X are as defined herein, and to their pr...
11/01/2005
6921756Inhibitors of β-lactamase
The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and...
07/26/2005
6884791Inhibitors of β-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and...
04/26/2005
6777433Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing...
08/17/2004
6706698α-Substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and ver...
03/16/2004
6645950Benzimidazole vascular damaging agents
Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment...
11/11/2003
6613945Resolution method for a racemic mixture of aldehydes
The invention concerns a resolution method for a racemic mixture of aldehyde of formula (I). ##STR1## The aldehydes of formula I are useful in their enantiomeric form or their racemic form for preparing transition metal complexes useful as catalysts ...
09/02/2003
6576760Processes for synthesis of cyclic and linear polyamine chelators containing N-monosubstituted coordinating arms
Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining t...
06/10/2003
6555528Derivatized biotin compounds and methods of use
An efficient synthesis for the selective and efficient 1'-N derivatization of biotin is reported. The derivatized biotin acts as a stable analog of the carboxyphosphate intermediate in naturally-occurring biotin-mediated CO2 transfer. The synth...
04/29/2003
6506738Benzimidazolone antiviral agents
The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection....
01/14/2003
6500811Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use
Compounds of the 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 enzymes is involved....
12/31/2002
6498151Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors
The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated d...
12/24/2002
6489476Heteroaromatic compounds containing a phosphonate group that are inhibitors of fructose-1,6-bisphosphatase
FBPase inhibitors of the formula I and X ##STR1## are useful in the treatment of diabetes and other conditions associated with elevated blood glucose or excess glycogen storage....
12/03/2002
6486142Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases,...
11/26/2002
6485941Inhibition of the carboxyltransferase component of acetyl-CoA carboxylase, and the use of such inhibition in anti-cancer and anti-lipogenic therapies
A method is disclosed for inhibiting carboxyltransferase with bisubstrate analogs. One such analog has been shown to inhibit the carboxyltransferase component of E. coli acetyl-CoA carboxylase. It is also expected to inhibit mammalian acetyl-CoA carboxyla...
11/26/2002
6472406Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ଲ-lactamase inhibitors, which are structurally unrelated to the nat...
10/29/2002
6399782Benzimidazole inhibitors of fructose 1,6-bisphosphatase
Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described ##STR1##...
06/04/2002
63920562H-benzotriazole UV absorders substituted with 1,1-diphenylalkyl groups and compositions stabilized therewith
2H-Benzotriazole UV absorbers substituted at the 3-position or at the 5-position of the phenyl ring by a 1,1-diphenylalkyl moiety, particularly a 1,1-diphenylethyl group, are particularly photostable in automotive coatings, and are of low color and exhibi...
05/21/2002
6339160Metalloproteinase inhibitors, their therapeutic use and process for the production of the starting compound in the synthesis thereof
Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation wit...
01/15/2002
6307090Acylated oligopeptide derivatives having cell signal inhibiting activity
The invention relates to an acylated peptide, namely a compound of formula (I), ##STR1## wherein n is 0 to 15, X is oxalyl PTI is the bivalent radical of tyrosine or (preferably) the bivalent radical of phosphotyrosine or a phosphotyrosine mimetic, AA sta...
10/23/2001
6270695Compounds, compositions, and methods for generating chemiluminescence with phosphatase enzymes
Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing he...
08/07/2001
62520841H-indole-3-acetamide sPLA2 inhibitors
A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock....
06/26/2001
6242471Condensed 4,5,6,7-tetrahydrobenzo[C]thiophenes as enhancer for cell differentiation induction factor action
A compound represented by the formula: ##STR1## wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optio...
06/05/2001
6242610Derivatized biotin compounds and methods of use
An efficient synthesis for the selective and efficient 1'-N derivatization of biotin is reported. The derivatized biotin acts as a stable analog of the carboxyphosphate intermediate in naturally-occurring biotin-mediated CO2 transfer. The synth...
06/05/2001
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