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Class 514/280 - Pentacyclo ring system having the 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 polycyclo ring system consists
No. of patents: 229
Last issue date: 09/20/2011


1            
NumberTitleIssue Date
8022080Small molecules with antiprotozoal activity
The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. ...
09/20/2011
7989466Methods to inhibit or augment an inflammatory response
Isolated and purified chemokine peptides, variants, and derivatives thereof, as well as chemokine peptide analogs, are provided. ...
08/02/2011
7915276Berberrubine derivatives having antifungal activities
The present invention relates to a berberrubine derivative having superior antifungal activity, more particularly to a berberrubine derivative having activity against chitin synthase, which participates in the synthesis of chitin and is essential in the growth of fu...
03/29/2011
7691872Methods and compositions for optimizing blood and tissue stability of camptothecin and other albumin-binding therapeutic compounds
The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves method...
04/06/2010
76788085 HT receptor mediated neurogenesis
The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combina...
03/16/2010
7645766Method for treatment of depression and depressive mood disorders
A method for treatment of depression and depressive mood disorders. The patient is administered an amount of a compound that increases the catalytic activity of MAO-A, so as to increase synaptic metabolism of serotonin to 5-HIAL. The effective compound is preferably...
01/12/2010
7531550Pseudobase benzo[c]phenanthridines with improved efficacy, stability, and safety
Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Cert...
05/12/2009
7470703Yohimbine derivatives and use thereof
Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of...
12/30/2008
7387790Pharmaceutical and diagnostic compositions containing nanoparticles useful for treating targeted tissues and cells
Nanoparticles made from a select group of lipids and optionally containing a therapeutically active agent are employed in pharmaceutical compositions for delivery to targeted tissues and/or cells for the treatment or diagnosis of such diseases as cancer. ...
06/17/2008
7371415Method and composition for improving sexual fitness
The invention provides methods and compositions for maintaining a state of wellness in a human by providing a dietary supplement comprising L-arginine, alone or in combination with either ginseng or ginkgo biloba or the combination of all three. The compositi...
05/13/2008
7335771Quinacridone derivatives as labelling reagents for fluorescence detection of biological materials
Disclosed are new quinacridone dye derivatives having characteristic fluorescence lifetimes. Also disclosed are methods for labelling target biological materials employing the quinacridone dyes and use of the labelled materials in biological assays. The quinacridone...
02/26/2008
7323449Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependen...
01/29/2008
7319105Cytotoxic agents
The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treat...
01/15/2008
7312228Cytotoxic indeno and isoindoloisoquinolones
The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions o...
12/25/2007
7276512Benzo[a]pyrano[3,2-h]acridin-7-one compounds
A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, alkyl, trihaloalkyl and NR...
10/02/2007
7268148Compositions and methods for use against acne-induced inflammation and dermal matrix-degrading enzymes
Acne-affected skin has been found to be accompanied by the presence of matrix-degrading enzymes such as MMPs and neutrophil elastase, induction of neutrophils, and a reduction in procollagen biosynthesis. This invention treats scarring and inflammation accompanying ...
09/11/2007
7261889Local anesthetic methods and kits
Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. A...
08/28/2007
7232830Method for treatment of neurodegenerative diseases and effects of aging
A method for treatment of neurodegenerative disease conditions stemming from multiple sclerosis, aging, autoimmune diseases and fibromyalgia. A compound effective to increase neuronal metabolism of histamine to a histamine H2 agonist is administered in an...
06/19/2007
7229649Method and composition for improving sexual fitness
The invention provides methods and compositions for maintaining a state of wellness in a human by providing a dietary supplement comprising L-arginine, alone or in combination with ginseng and ginkgo biloba and/or additional nutritional supplements. The invention pr...
06/12/2007
7220754Mono-ester and asymmetrically substatuted di-ester pro-drugs of dopamide D1 receptor agonists
Mono-ester and asymmetrically substituted diesters of dihydrexidine, dinapsoline and A-86929 and substituted derivatives thereof are described. The novel ester/diester derivatives exhibit improved pharmacokinetic characteristics relative to their unesterified parent...
05/22/2007
7220428Pharmaceutical and diagnostic compositions containing nanoparticles useful for treating targeted tissues and cells
Nanoparticles made from a select group of lipids and optionally containing a therapeutically active agent are employed in pharmaceutical compositions for delivery to targeted tissues and/or cells for the treatment or diagnosis of such diseases as cancer. ...
05/22/2007
7208492Topoisomerase-targeting agents
The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R1–R5, X, and Y have any of the meanin...
04/24/2007
7205312N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydrox...
04/17/2007
7201913Oral formulations for anti-tumor compounds
The present invention relates to a semi-solid filling medium which comprises a camptothecin derivative; a pharmaceutically acceptable carrier matrix which is a polyglycolized glyceride; and an effective thickening-reducing and stabilizing-promoting amount of one or ...
04/10/2007
7199130Substituted 5,6,6a, 11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds as NMDA-antagonists
Substituted 5,6,6a,11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the use thereof in treatment methods and for the production of pharmaceut...
04/03/2007
7192736Nucleic acid molecules encoding cytotoxic conjugates that contain a chemokine receptor targeting agent
Nucleic acid moleucles that encode conjugates containing as a ligand a chemokine receptor targeting agent, such as a chemokine, and a targeted agent, such as a toxin are provided. These conjugates are used to treat inflammatory responses associated with activation, ...
03/20/2007
7173041Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use. ...
02/06/2007
7166702Cytotoxic conjugates comprising a chemokine receptor targeting agent
Conjugates containing as a ligand chemokine receptor targeting agents, such as chemokines, and a targeted agent, such as a toxin are provided. These conjugates are used to treat inflammatory responses associated with activation, proliferation and migration of immune...
01/23/2007
7164021Opiate analogs selective for the δ-opioid receptor
Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the δ-opioid recept...
01/16/2007
7157418Methods and compositions for treating secondary tissue damage and other inflammatory conditions and disorders
Conjugates containing as a ligand a chemokine receptor targeting agents, such as chemokines, and a targeted agent, such as a toxin are provided. These conjugates are used to treat inflammatory responses associated with activation, proliferation and migration of immu...
01/02/2007
7153864Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use. ...
12/26/2006
7151108[3,4-a:3,4-c]carbazole compounds
A compound selected from those of formula (I): wherein: W1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a gr...
12/19/2006
7144891Benzo[b ]pyrano[3,2- h ]acridin-7-one cinnamate compounds
A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, alkoxy, nitro, cyano, alkyl, alkenyl, polyhaloalkyl and —NR
12/05/2006
7135497Treating neural conditions resulting from spinal cord contusions and other causes
β2-agonists, such as clenbuterol and salbutamol can enhance the recovery of locomotive function and/or neuromuscular strength following spinal cord injuries or as a result of degenerative neural conditions such as Mnd. Pharmacological compositions for tr...
11/14/2006
7125873Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabet...
10/24/2006
7115619N, N-disubstituted quino[4,3,2-kl]acridinium salts as therapeutic agents
The present invention pertains to certain N8,N13-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q−) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4;...
10/03/2006
7109380Cyclopentenedione antifungal compounds and methods for their use
Compounds and methods useful in the control, treatment, and prevention of fungal activity, of the following formula: where R1-3 are independently H, alkyl, methyl, acyl, halogen, phenyl, R4 ...
09/19/2006
7105492Camptothecin derivatives having antitumor activity
Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum. ...
09/12/2006
7091212Chiral dinapsoline
The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahy...
08/15/2006
7078411Phospholipid transfer protein (PLTP) and cholestoral metabolism
A method for controlling cholesterol metabolism in a host, a screening assay for agents that can control cholesterol metabolism, and the agents that may be identified are practiced and determined in relation to the expression of PLTP in HepG2 cells and a clone from ...
07/18/2006
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