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Class 514/217.07 - Polycyclo ring system having the additional six-membered hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional six-membered hetero
No. of patents: 234
Last issue date: 05/22/2012


1            
NumberTitleIssue Date
8183236Compounds with HIV-1 integrase inhibitory activity and use thereof as anti-HIV/AIDS therapeutics
Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the tre...
05/22/2012
8138173Pyrazolo[3,4-C]quinolines, pyrazolo[3,4-C]naphthyridines, analogs thereof, and methods
Pyrazolo[3,4-c]quinolines, pyrazolo[4,5-c]naphthyridines, and analogs thereof, eg., 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinolines, and, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these...
03/20/2012
74494552-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in contraception and in treating melanoma, osteoporosis, acne, dysfunctional ...
11/11/2008
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7345038Pyridyloxymethyl and benzisoxazole azabicyclic derivatives
An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound of formula I, pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as schizophrenia and...
03/18/2008
7319097Compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
01/15/2008
7304052Substituted homopiperidinyl benzimidazole analogues as fundic relaxants
The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres...
12/04/2007
7304051Quinoxaline compounds
Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases. ...
12/04/2007
7285547Amidinophenylalanine derivatives as thrombin inhibitors
The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. T...
10/23/2007
72476242-Phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating colon cancer. ...
07/24/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7230000Methods and compositions utilizing quinazolinones
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...
06/12/2007
7205309Quinazoline derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The...
04/17/2007
7186710Phthalazinones
The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors. ...
03/06/2007
7135466Quinoline and quinazoline derivatives and drugs containing the same
There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy. The compounds are those represented by formula (I) or pharm...
11/14/2006
71324172-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating uterine leiomyoma. ...
11/07/2006
7119084Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to ...
10/10/2006
7112607Allosteric adenosine receptor modulators
The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including p...
09/26/2006
7071184Protease inhibitors
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int...
07/04/2006
7041675Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors. ...
05/09/2006
70416632-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating vaginal and skin atrophy. ...
05/09/2006
7012073Quinoline derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1,...
03/14/2006
6992080Imidazopyridines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of pr...
01/31/2006
6964957Fused pyrazole compounds, pharmaceutical compositions, and methods for modulating or inhibiting ERAB or HADH2 activity
Pyrazole compounds represented by the formula: are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in treating ERAB, HADH2 or amylo...
11/15/2005
6962926Antagonist of MCP-1 function, and compositions and methods of use thereof
Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of ...
11/08/2005
69518522-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in the treatment or inhibition of osteoarthritis. ...
10/04/2005
69366226-phenylbenzonaphthyridines
Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors. ...
08/30/2005
69242812-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating male pattern baldness. ...
08/02/2005
6887864Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ...
05/03/2005
6855724Tropane derivatives useful in therapy
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially...
02/15/2005
68357292-phenyl-1-[4(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in lowering cholesterol levels. ...
12/28/2004
6812234Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10
11/02/2004
67875382-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in providing hormone replacement therapy. ...
09/07/2004
6699492Quinolone carboxylic acid compositions and related methods of treatment
The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid com...
03/02/2004
6680314Azacyclooctane and heptane derivatives, their preparation and use in therapy
Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ...
01/20/2004
6656944Fungicidal mixtures
The invention relates to fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of (a) at least one azolopyrimidine of formula I ##STR1## in which R1 through R2
12/02/2003
6613781Heterocyclylaklylindole or -azaindole compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ##STR1##...
09/02/2003
6602867Triazole compounds with dopamine-D3-receptor affinity
Triazole compounds of the following formula ##STR1## where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 rece...
08/05/2003
6602864Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit...
08/05/2003
6596715Protease inhibitors
This invention relates to the compound of Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition...
07/22/2003
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