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Class 514/257 - Polycyclo ring system having 1,3-diazine as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the 1,3 - diazine is a part of a
No. of patents: 210
Last issue date: 02/28/2012


1            
NumberTitleIssue Date
8124608Stable pharmaceutical composition of freeze-dried tetrodotoxin powder
This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin, including disaccharide(s) or polyglucose(s) or analogues thereof and solvent(...
02/28/2012
8093254Aspartyl protease inhibitors
Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3...
01/10/2012
8012987Indolo[2,1-b] quinazole-6,12-dione antimalarial compounds and methods of treating malaria therewith
Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo [2,1-b]quinazoline-6,12-dione compounds of Formula I. wherein A, B, C, D, B, F, G and H are indepe...
09/06/2011
7956060Pyrimidine derivative compound
The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): [wherein —X—Y—Z— represents —O—CR3═N— (...
06/07/2011
7910593Water-soluble prodrugs
An objective of the present invention is to provide water-soluble prodrugs that can be administered parenterally, and which show excellent water solubility and small interspecies or individual differences and are rapidly converted to the active form by chemical conv...
03/22/2011
7855214Fused cyclic systems useful as inhibitors of TEC family protein kinases
The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2,...
12/21/2010
7642265Benzimidazoles and analogs thereof as antivirals
Provided are compounds of the formula: wherein RN1 is a substituent of formula G1—NX1X2, wherein G1 is an optionally further substituted alky...
01/05/2010
7511048Pyrimidothienoindazoles
The invention relates to novel pyrimidothienoindazoles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative d...
03/31/2009
7476676Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3β
This invention relates to the use of inhibitors of glycogen synthase kinase-3β to increase bone formation. ...
01/13/2009
7439249Inhibitors of phosphatases
The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases. ...
10/21/2008
7427616Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms selected from O, N and S, and wherein the 5-membered ring containing G ...
09/23/2008
RE40332Fungicidal trifluoromethylalkylamino-triazolopyrimidines
The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with ca...
05/20/2008
7364866G protein coupled receptors, nucleic acids, and methods related to the same
The present invention provides Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells, and methods for its production. The invention al...
04/29/2008
7354724Drosophila G protein coupled receptors, nucleic acids, and methods related to the same
The present invention provides a Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells and methods for its production. The invention a...
04/08/2008
7312225Macrocyclic pyrimidines, their production and use as pharmaceutical agents
Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent ...
12/25/2007
7304037Cytostatic conjugates with integrin ligands
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especial...
12/04/2007
7273871Phenyl-5,6,6A,7,8,9-hexahydro-4H-1,4,9-triaza-phenalene derivatives as CRF antagonists
The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof: ...
09/25/2007
7268141Xanthine phosphodiesterase V inhibitors
A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
09/11/2007
7259167Antimalarial and antiproliferative pharmacophore models, novel tryptanthrin compounds having increased solubility, and methods of making and using thereof
Disclosed herein is a pharmacophore model for antimalarial activity and methods of making and using thereof. The pharmacophore comprises two hydrogen bond acceptor (lipid) functions and two hydrophobic (aromatic) functions. The pharmacophore model was made using a t...
08/21/2007
7244746Imidazolyl 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...
07/17/2007
7235562Pyrimidine derivatives for the treatment of abnormal cell growth
The present invention relates to a compound of the formula 1 wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatmen...
06/26/2007
7220824Integrin-mediated drug targeting
The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units. The preferred linking units guarantee serum stability of the conjugate of cytost...
05/22/2007
7217717Phenalene derivatives
Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative...
05/15/2007
7208499Pyrimidine derivatives for the treatment of abnormal cell growth
The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals...
04/24/2007
7202236Modified release pharmaceutical formulation
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy;...
04/10/2007
7196111Pyrazolo[1,5a]pyrimidine compounds as antiviral agents
The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and...
03/27/2007
7160890Compounds specific to adenosine Areceptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeuti...
01/09/2007
7145008Pyrimidine derivatives for the treatment of abnormal cell growth
The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof, wherein R1–R4 and Ar are ...
12/05/2006
7144887Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an a...
12/05/2006
7115710Diagnosis and treatment of PTP related disorders
The present invention relates to PTP05 polypeptides and PTP10 polypeptides, nucleic acids encoding such polypeptides, cells, tissues and animals containing such nucleic acids, antibodies to such polypeptides, assays utilizing such polypeptides, and methods relating ...
10/03/2006
7109337Pyrimidine derivatives for the treatment of abnormal cell growth
The present invention relates to a compound of the formula 1 wherein R1–R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, suc...
09/19/2006
7109195Hexacyclic compounds and their therapeutic use
The present invention relates to hexacyclic compound of the formula [1], wherein Z, R3 and R4 are as identified therein, and pharmaceutically acceptable salts thereof. These compounds are us...
09/19/2006
7074797Pyrazolopyrimidines as CRF receptor antagonists
This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is NR4R5 or OR5
07/11/2006
70675197,8,9,10-tetrahydro-6-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2-pyrrolo[2,1-]-quinazolinone derivatives
The invention relates to novel 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns re...
06/27/2006
7064204Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use
New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications. ...
06/20/2006
7005425Method for treating arrhythmias
Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a ...
02/28/2006
6995163Tricyclic fused heterocyclic compound, process for preparing it and medicament comprising it
The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof,...
02/07/2006
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
6967203Use of pyridoindolone derivatives for preparing anticancer medicines
The invention relates to a novel use of compounds of formula: for the preparation of medicinal products that are useful as anticancer agents. ...
11/22/2005
6964960Indoloquinazolinones
The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP. ...
11/15/2005
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