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Class 514/431 - The hetero ring has at least seven members


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the hetero ring has at least seven
No. of patents: 229
Last issue date: 05/29/2012


1            
NumberTitleIssue Date
8188141Isomigrastatin analogs in the treatment of cancer
The present invention provides compounds having formula (I): (I) wherein n, R1-R5, Ra-Rb, Q, Y1 and Y2 are as defined herein; and additionally provides methods for the synthesis thereof, compositions ...
05/29/2012
8067459Lapachone compounds and methods of use thereof
The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment ...
11/29/2011
8030345Tricyclic pyrazole derivatives as cannabinoid receptor modulators
The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing co...
10/04/2011
7994210Method of treating Down Syndrome
The present invention relates to methods of treating of Down syndrome in a person using compounds of the invention. ...
08/09/2011
7964631Fused tricyclic compounds as inhibitors of tumor necrosis factor-α
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R...
06/21/2011
79560851,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof
This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof. ...
06/07/2011
79234681,4-benzothiepin-1,1-dioxide derivatives which are substituted with cyclohexyl groups, method for producing the same, drugs containing said compounds and use thereof
This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with cyclohexyl groups, method for producing the same, drugs containing said compounds and use thereof. ...
04/12/2011
7834052Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha
Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R...
11/16/2010
7799824Quaternary salt CCR2 antagonists
Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or dis...
09/21/2010
7625942Method of treating Down syndrome
A method of, or the use of compounds of the invention for, treating the cognitive impairments associated with Down syndrome, the method or use comprising treating or administering to a person with an effective amount of phenserine and isomers thereof or a pharmaceut...
12/01/2009
7439264Therapeutic compounds
This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also rel...
10/21/2008
7381743Macrocycles for the treatment of cancer
The present invention relates to new macrocycles of the general formula (I) as well as their use for the treatment of cancer diseases ...
06/03/2008
7355069Ortho-substituted benzoic acid derivatives for the treatment of insulin resistance
The present invention provides a compound of formula (I), wherein n is 0, 1 or 2 and R1 represents halo, a C1-4alkyl group which is optionally substituted by one or more fluoro, a C1-4alkoxy group which is optionally substituted by o...
04/08/2008
7354949Therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia
The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein ...
04/08/2008
7332516Geminally di-substituted NSAID derivatives as Aβ42 lowering agents
The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is â€...
02/19/2008
7329654Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their prepar...
02/12/2008
73122031-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
The present invention relates to 1-aza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumo...
12/25/2007
7276532Remedies for vesical hyperactivity
The present invention provides a therapeutic agent for overactive bladder comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, s...
10/02/2007
7262185Benzazepine derivative, process for producing the same, and use
The present invention provides a novel benzazepine derivative represented by formula: wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally subst...
08/28/2007
72623091- or 3-thia-benzonaphthoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof
The present invention relates to benzonaphthoazulene derivatives of tiophene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the i...
08/28/2007
72328151-oxa-3-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the production thereof
The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inh...
06/19/2007
7229982Pharmaceutical formulation
The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The ...
06/12/2007
7226943Benzothiepine ileal bile acid transport inhibitors
The present invention relates to compounds of formula (I) wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the tre...
06/05/2007
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
7179792Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least one other active ingredient and the use of the product
The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I in which the radicals have the meanings defined herein, or a pharmaceutically acceptable salt or physiologically function...
02/20/2007
71665831,3-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
The present invention relates to 1,3-diaza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of ...
01/23/2007
7122173Agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia
The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a phar...
10/17/2006
7112683Cyclic sulfone containing retroviral protease inhibitors
The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease. ...
09/26/2006
7109233Protease inhibitors
This invention relates in general to certain substituted substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamides of formula I as defined herein which are protease inhibitors. ...
09/19/2006
7109234Benzoxathiepine derivatives and their use as medicines
The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, al...
09/19/2006
7102013Methods of making amidino compounds useful as nitric oxide synthase inhibitors
Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33:
09/05/2006
7067510Dihydro-dibenzo[b,e]oxepine based selective estrogren receptor modulators, 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...
06/27/2006
7053109Aminediols for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
05/30/2006
7019023Benzothiepine 1, 1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
Substituted benzothiepine 1,1-dioxide derivatives of formula I: in which R1, R2, R3, R4, R5 and Z have the meanings indicated, and their physiologically tolerable s...
03/28/2006
70054502-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives useful as nitric oxide synthase inhibitors
The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors. ...
02/28/2006
69561312-amino-3, 4 heptenoic compounds useful as nitric oxide synthase inhibitors
The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 is selected from the group consisting of H and methyl; and R...
10/18/2005
6951860Calcium channel blockers
The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel ...
10/04/2005
69518892-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors
The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors. ...
10/04/2005
6943189Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG CO-A reductase inhibitors
Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as th...
09/13/2005
6908934Therapeutic compounds for treating dyslipidemic conditions
Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia
06/21/2005
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