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Class 548/491 - Chalcogen or nitrogen attached indirectly to 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 chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 433
Last issue date: 02/14/2012


1                      
NumberTitleIssue Date
8115013Process for the preparation of amorphous fluvastatin sodium
The present invention relates to a novel process for the preparation of the HMG-CoA reductase inhibitor, fluvastatin, more specifically to a process for the preparation of amorphous form of fluvastatin sodium. ...
02/14/2012
8115014Ethynylindole compounds
As a compound having a potent oral activity and a long-lasting cysLT1/cysLT2 receptor antagonistic activity, the compound of the formula (I): which exhibits potent antagonistic activity against the cys...
02/14/2012
7960568Heterocyclyl-substituted sulfonamides for the treatment of cognitive or food ingestion related disorders
The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders. ...
06/14/2011
7834193Indoline compound and process for producing the same
The present invention provides an industrial method production of silodosin, which is useful for a therapeutic agent for dysuria associated with benign prostatic hyperplasia. The production of silodosine is characterized by mixing 3-{7-cyano-5-[(2R)-2-({2-[2-(2,2,2-...
11/16/2010
7795450Antagonist of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of m...
09/14/2010
7754896Indol-alanine derivatives as selective S1P4-agonists
The present invention relates to agonists of the S1P4 receptor, which are selective for the S1P4 receptor over one or more of the S1P1, S1P2, S1P3 or S1P5 receptors of at least 10 fold, in particular new indol-alanine derivatives of structure I, process for their pr...
07/13/2010
7582771Process for the synthesis of cPLA inhibitors
A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN,...
09/01/2009
7429612Indoline compound and medicinal use thereof
The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition contai...
09/30/2008
7414070Indol-7-YL sulfonamide derivatives, their preparation and their use in pharmaceutical compositions
The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, p...
08/19/2008
7384970Inhibitors 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...
06/10/2008
7384973Materials and methods for treating hypercholesterolemia
The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can ...
06/10/2008
7375118Phenyl-indole compounds for modulating IgE and Inhibiting cellular proliferation
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellu...
05/20/2008
7358364Substituted carboxylic acids
The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds inclu...
04/15/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
7332521Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them. ...
02/19/2008
7294648Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof
Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X
11/13/2007
7291644Indole derivatives
Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonize...
11/06/2007
7288564Indole derivatives
Compounds of formula (I) or salts or solvates thereof or physiologically functional derivatives thereof are potent binders at the EP4 receptor and are of use in the treatment or prevention of conditions such as a...
10/30/2007
7276612Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase...
10/02/2007
7268159Substituted indoles
The present invention relates generally to substituted indoles and methods of using them. ...
09/11/2007
7259182Aryl, aryloxy, and aklyloxy substituted 1-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor ...
08/21/2007
7253156Carbonate and carbamate modified forms of glucocorticoids in combination with Badrenergic agonists
Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula and in combination with related steroid carbonates and carbamates are disclosed. The composi...
08/07/2007
7244743Non-peptidic BRS-3 agonists
Selectively BRS-3-agonistic compounds of formula I wherein A1, A2, A3, R1, R2, R3, Ar1, Ar2, Ar3, m and n have th...
07/17/2007
7241801Viral polymerase inhibitors
A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enant...
07/10/2007
7229986Melanin-concentrating hormone antagonist
A melanin-concentrating hormone antagonist comprising a compound of the formula: wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms...
06/12/2007
7230118Process for the preparation of ropinirole
A new process for the preparation of Ropinirole (1) and pharmaceutically acceptable hydrochloride salt thereof comprising reacting the compound (V) with nitromethane to obtain the compound of formula (II), which is reduced to compound (III) and alkylated to obtain c...
06/12/2007
7220553Use of Russell's viper venom-induced plasma factor Xa activity to monitor the activity of factor Xa inhibitors
The invention relates to a method of monitoring the effect of a direct of indirect Factor Xa inhibitors comprising the steps of collecting a plasma sample from a patient, adding a solution of Russell's viper venom to the plasma sample and measuring the clotting time...
05/22/2007
7199265Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones
This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor β, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of m...
04/03/2007
7199258Process for preparing nitrooxyderivatives of naproxen
The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of naproxen or bromonaproxen and R1–R12 are hydrogen or alkyl groups, m, n, o, q, r and s are ea...
04/03/2007
7186753Pharmaceutical compounds
Compounds or their salts of general formula (I): A—B—N(O)s wherein: s is an integer equal to 1 or 2; A=R—T1—, wherein R is the drug radical and T1=(CO)t or (X)t′, wherein X=O, S, NR1c, R
03/06/2007
7179921Indoline and tetrahydro-quinolines as prodrugs for tumour treatment
Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X...
02/20/2007
7176200Derivatives of sulphonamides, their preparation and use as medicaments
The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the ph...
02/13/2007
7169936Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments
The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, e...
01/30/2007
7166637Hydroxyindoles, their use as inhibitors of phosphodiesterase 4, and processes for preparing them
The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active c...
01/23/2007
7157585Serine protease inhibitors
Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents. ...
01/02/2007
7148240Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular...
12/12/2006
7141600Small molecule inhibition of a PDZ-domain interaction
Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein an...
11/28/2006
7138424Indole derivatives, method for preparing same and pharmaceutical compositions containing same
The present invention provides compounds of formula: and also provides their preparation and the pharmaceutical compositions comprising them. These compounds are ligands of CB2 cannabinoid receptors.
11/21/2006
7138527Indole derivatives useful for the treatment of diseases
The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous...
11/21/2006
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