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Class 546/84 - One of the cyclos is five-membered


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein one of the cyclos of the tricyclo ring
No. of patents: 275
Last issue date: 06/05/2012


1              
NumberTitleIssue Date
8193357Androgen receptor modulator compounds
Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositio...
06/05/2012
8013159Quinoline derivatives as EP4 antagonists
The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the...
09/06/2011
7732607Heteroaryl-substituted diazatricycloalkanes and methods of use thereof
The present invention relates to amide and urea derivatives of heteroaryl-substituted diazatricycloalkanes, pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the ...
06/08/2010
7592454Substituted hexahydro-pyridoindole derivatives as serotonin receptor agonists and antagonists
The present application provides novel compounds according to Formula (I): including all stereoisomers, solvates, prodrug esters and pharmaceutically acceptable salt forms thereof, wherein R1, R4a, R
09/22/2009
7439253Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in p...
10/21/2008
7407963Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable p...
08/05/2008
7390818Pyridoindolone derivatives substituted in the 3-position by a phenyl, their preparation and their application in therapeutics
The present invention relates to pyridoindolone derivatives substituted in the 3-position by a phenyl of general formula (I): to processes for preparing the same and to their use in therapeutics. ...
06/24/2008
7390819Imidazo[4,5-b]quinoline-derivatives and their use as no-synthase inhibitors
The compounds of formula I in which R1, R2, R3 and A have the meanings as given in the description are novel effective INOS inhibitors. ...
06/24/2008
7323473Condensed indoline derivatives and their use as 5-HT, in particular 5-HT, receptor ligands
A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independe...
01/29/2008
7323567RSV polymerase inhibitors
Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicamen...
01/29/2008
7317020Isolation and structure of Cribrostatin 6
Cribrostatin 6, a dark blue cancer cell growth inhibiting constituent of the Republic of Maldives marine sponge Cribrochalina sp. has been isolated, and its structure (shown below) elucidated, based on a combination of RMS, high field (500 MHz, HMBC, and GOESY exper...
01/08/2008
73097894-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, ...
12/18/2007
7288549Heterocyclic compounds, method for preparing same and use thereof as medicines, in particular as antibacterial agents
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their u...
10/30/2007
7288653Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders
This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH. ...
10/30/2007
7253180Pre-organized tricyclic integrase inhibitor compounds
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or...
08/07/2007
7238699Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) usefu...
07/03/2007
7211669Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) usefu...
05/01/2007
7176213Imidazoquinoline derivatives and their use as adenosine A3 ligands
The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds...
02/13/2007
7166613Condensed indoline derivatives and their use as 5HT, in particular 5HT, receptor ligands
A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independe...
01/23/2007
7153967Preparation of 1H-imidazo [4,5-C] quinolin-4-amines via 1H-imidazo [4,5-C] quinolin-4-phthalimide intermediates
The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imida...
12/26/2006
7129261Cytotoxic agents
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as ot...
10/31/2006
7115621Chemical compounds
Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders ...
10/03/2006
7109351Fused pyrrolecarboxamides; GABA brain receptor ligands
Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors ...
09/19/2006
7105663Derivatives of pyrimido[6,1-a]isoquinolin-4-one
Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3...
09/12/2006
7091214Aryl substituted Imidazoquinolines
Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases ...
08/15/2006
7087607Salts of bicyclic, N-acylated imidazo-3-amines and imidazo-5-amines
Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceut...
08/08/2006
7087600Peptidyl prodrugs and linkers and stabilizers useful therefor
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as ot...
08/08/2006
7074927Heterocyclic amines having central nervous system activity
Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof where...
07/11/2006
7071180Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2...
07/04/2006
7037919Tetrahydroquinoline derivatives
Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.
05/02/2006
7026484Tricyclic androgen receptor modulator compounds and methods
This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds. ...
04/11/2006
6992192Carboline derivatives as PDE5 inhibitors
Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents. ...
01/31/2006
6989389Aryl ether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines...
01/24/2006
6984646Imidazopyridinones as p38 map kinase inhibitors
The invention relates to imidazopyridinones of the formula wherein the groups R1, R2, R3, and R4 are as defined in claim 1, to the process for their preparation, to pharmaceu...
01/10/2006
6977298Tricyclic inhibitors of poly(ADP-ribose) polymerases
Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. ...
12/20/2005
6974824Kappa opioid receptor ligands
Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kapp...
12/13/2005
6964958Method of simultaneously treating sensory auditory gating deficit and associated psychosis in schizophrenia and bipolar disorder patients with mania
Schizophrenia and bipolar disorders with mania may be treated by imidazenil or other benzodiazepine-3-carboxamide derviatives. ...
11/15/2005
6953804Aryl ether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines...
10/11/2005
6953791Dipeptide derivatives
This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which inc...
10/11/2005
6949549Imidazolophthalazine derivatives as ligands for GABAA receptors
A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I which are partial or full inverse agonists of an α5 receptor subunit while being relatively free of...
09/27/2005
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