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Class 544/247 - Three or more ring hetero atoms in the tetracyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the tetracyclo ring system includes at
No. of patents: 140
Last issue date: 02/15/2011


1        
NumberTitleIssue Date
78885056,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one carboxylic acids, their esters, and methods of synthesis thereof
The present invention relates to a 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one carboxylic acid and its esters of the general structural formula (I), and provides a method for their synthesis (I) where R and each R′ are selected independently from the list compri...
02/15/2011
7838674Tetracyclic lactame derivatives
The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending...
11/23/2010
7834180Methods of preparing quinolone analogs
Compounds having formula 1: are produced by contacting a compound having formula (6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base,
11/16/2010
7816524Methods of preparing quinolone analogs
Compounds having formula 1 are produced by contacting a compound having formula(6A) with a compound having formula (7), or tautomers thereof, in the presence of a non-nucleophilic base,
10/19/2010
7763725Pyrimido-benzimidazole derivatives and the use thereof in the form of agonists and antagonists of melanocortin receptors
The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and d...
07/27/2010
7294738Phosphorous containing steroid mimics
The present invention discloses novel steroid mimics wherein a tri- or tetravalent phosphorous atom is isosterically substituted at any one of the seventeen positions occupied by the carbon atom in the steroidal skeleton, and wherein each adjacent position to the ph...
11/13/2007
7256196Purine cytokine inhibitors
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions c...
08/14/2007
7253292Synthesis of cyclopentadiene derivatives
A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.
08/07/2007
7253177Synthesis and antimalarial activity of pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives
The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and
08/07/2007
7195879Method for identifying modulators of NAion channels
The present invention provides methods to manipulate differentiation of a neuroblastoma cell line (IMR-32) such that predominant Nav expression is either Nav1.3 in IMR-32 cells exposed to retinoic acid or Nav1.7 in cells grown under ...
03/27/2007
7176310Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents
This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions ...
02/13/2007
6969719Polycyclic guanine phosphodiesterase V inhibitors
A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological disorders: A representativ...
11/29/2005
6960585Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders, wherein X, Y1, Y2, and R
11/01/2005
6951942Glucocorticoid-selective anti-inflammatory agents
Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also di...
10/04/2005
6921761Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, R1
07/26/2005
6894055Thieno-2′,3′ -5,6pyrimido[3,4-A]-1,2,4-triazole derivatives as modulators of phoshoinositide 3-kinase
Compounds of formula 1 are effective modulators of PI3 kinase: wherein X is CR9R10, O, NR11 (where R9 and R10 are each independently H, lo...
05/17/2005
6872743sPLA2 inhibitors
A novel class of tetracyclic compounds represented by the formula I wherein R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, and n are as defined is disclosed together with the use of such compounds for inhibiting sPLA2 medi...
03/29/2005
6750214Quinoline and quinazoline compounds useful in therapy
The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optional...
06/15/2004
6747039Aza-benzothiopyranoindazoles with antitumor activity
The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds ...
06/08/2004
6673798PDGF receptor kinase inhibitory compounds, their preparation, purification and pharmaceutical compositions including same
A purified tyrphostin of a general formula: ##STR1## wherein, for Compound I, R6 is either at position 6 or at position 7, or, for Compound II, R6 is either at position 6 or at position 8....
01/06/2004
6667405Methine compound and silver halide photographic material containing the same
Disclosed is a compound represented by the following formula (I): ##STR1## wherein Z1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing heterocyclic ring; Z2 represents an atomic group necessary to f...
12/23/2003
6605610Aryl fused azapolycyclic compounds
Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such co...
08/12/2003
6562968Method of purifying tetrodotoxin
The present invention relates to a new process of purifying tetrodotoxin using high performance liquid chromatograph technology....
05/13/2003
6552191Method of extracting tetrodotoxin
The present invention relates to a new process of extracting tetrodotoxin from the tissues of an organism. The invention provides increased yield of tetrodotoxin from animal tissues. In the invention, a lixiviated solution is obtained by soaking the tissu...
04/22/2003
6478966System for extracting tetrodotoxin
The invention relates to a system for extracting toxins from biological tissues. The system comprises a lixiviator, an ion-exchange column, a diatomaceous silica-active carbon column, and a vacuum concentrator. Twenty to one hundred kilograms of raw mater...
11/12/2002
6444808Methods of making cross-bridged macropolycycles
Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle....
09/03/2002
6429311Compositions containing N-amino- and N-hydroxy-quinazolinones and methods for preparing libraries thereof
The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis...
08/06/2002
6380193Fused tricyclic compounds, methods and compositions for inhibiting PARP activity
A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof....
04/30/2002
6358954PDGF receptor kinase inhibitory compounds, their preparation, purification and pharmaceutical compositions including same
An isometric enriched tyrphostin of a general formula: ##STR1## wherein, for Compound I, the tyrphostin is enriched either for R6 at position 6 or for R6 at position 7, or, for Compound II, the tyrphostin is enriched either for R
03/19/2002
6355803Near infrared chemiluminescent acridinium compounds and uses thereof
This application relates to long-wavelength acridinium compounds having electron-donating groups, which may either be: (a) Part of an extended conjugation system attached by appropriate functional groups to the acridinium nucleus, with coplanarity of the ...
03/12/2002
6337331Triazolo-pyrimidine as ligands for GABA receptors
Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-଱]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions....
01/08/2002
6288094Polycyclic thiazol-2-ylidene amines, processes for their preparation and their use as medicaments
The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, ##STR1## in which the radicals have the stated...
09/11/2001
6281355Nitrogen-containing tetracyclic compounds
A nitrogen-containing tetracyclic compound represented by the formula: ##STR1## wherein Y1 --Y2 --Y3 is N--C.dbd.N or a group represented by the formula: C.dbd.C--NR3 (wherein R3 is a hydrogen atom, a ...
08/28/2001
6225464Methods of making cross-bridged macropolycycles
Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle....
05/01/2001
6218400Treatment method using a cGMP-Specific PDE inhibitor
A compound of formula ##STR1## and salts and solvates thereof, wherein R0, R1, and R2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has u...
04/17/2001
6184377Compositions containing N-amino- and N-hydroxy-quinazolinones and methods for preparing libraries thereof
The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis...
02/06/2001
6159996Polycyclic thiazolidin-2-ylidene amines, process for their preparation, and their use as pharmaceuticals
Polycyclic thiazolidin-2-ylidene amines and their physiologically tolerable salts and physiologically functional derivatives of the formula I ##STR1## in which the radicals have the meanings indicated, and their physiologically tolerable salts and a ...
12/12/2000
6107304Thieno[2,3-b]pyrazolo[3,4-d]pyridine-3-ones to enhance erythropoiesis
Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also invented are intermediates and processess used in preparing ...
08/22/2000
6057329Fused polycyclic 2-aminopyrimidine derivatives
Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group; X is a carbon or nitrogen atom; Y is a carbon or nitrogen atom; Z is a linker group; A together with X and Y forms an optiona...
05/02/2000
6022497Photochromic six-membered heterocyclic-fused naphthopyrans
Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted six-membered heterocyclic group fused to one side of the naphtho portion of the nap...
02/08/2000
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