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Class 544/257 - Pteridines (including hydrogenated)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 116
Last issue date: 01/17/2012


1      
NumberTitleIssue Date
RE43115Process for the manufacture of fused piperazin-2-one derivatives
Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claim...
01/17/2012
8039617Method for producing alpha form crystals of sapropterin hydrochloride
A method for selectively producing stable alpha form crystals of sapropterin hydrochloride is provided. In this method, the alpha form crystal of sapropterin hydrochloride is produced by dissolving sapropterin hydrochloride with hydrochloric acid at a concentration ...
10/18/2011
7875716Inhibitors of folic acid-dependent enzymes
The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: wherein: Z=O or S; n=1-3; R3=—CO
01/25/2011
7750152Intermediate compounds for making dihydropteridinones useful as pharmaceutical compositions and processes of making the same
Disclosed are dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the pharmaceutical compositions, isomers, intermediates ...
07/06/2010
7626019Intermediate compounds for the manufacture of fused piperazin-2-one derivatives
Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claim...
12/01/2009
7439358Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pt...
10/21/2008
7429581Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is...
09/30/2008
7414053Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f...
08/19/2008
7332491Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specificat...
02/19/2008
7238807Process for the manufacture of fused piperazin-2-one derivatives
Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given i...
07/03/2007
7235370Site-specific aminoglycoside derivatives for use in immunodiagnostic assays
A method of making a derivatized aminoglycoside includes reacting an aminoglycoside with at least 2 equivalents of a divalent metal ion in an aprotic solvent to complex two neighboring amino group and hydroxyl group pairs; reacting the non-complexed amino groups wit...
06/26/2007
7192729Methods for assaying homocysteine
The present invention relates to compositions and methods for assaying homocysteine (Hcy) and thus related moieties, e.g., S-adenosylhomocysteine (SAH) or adenosine. More particularly, assay methods that employ, mutant SAH hydrolase having binding affinity for Hcy, ...
03/20/2007
7169778Pteridinones as kinase inhibitors
Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R
01/30/2007
7148224Pyrazinone derivatives
The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc...
12/12/2006
RE39198Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgesics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compoun...
07/18/2006
7074929Certain alkylene diamine-substituted heterocycles
This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula II, IV, V, VII–IX and X...
07/11/2006
7067658Pyridino and pyrimidino pyrazinones
The present invention provides compounds of Formula I: wherein the variables A, B, Ar, R1, R2, and R3 are as defined herein. The compounds of Formula (I) can function as corticotr...
06/27/2006
6989446Process for the preparation of 3-aryl-benzofuranones
Process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V wherein ...
01/24/2006
6946465Immunosuppressive effects of pteridine derivatives
Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, b...
09/20/2005
6914062Pyrazinone derivatives
The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V i...
07/05/2005
6894173Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same
Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic co...
05/17/2005
6894041Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula:
05/17/2005
6869945Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula:
03/22/2005
6861422Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, proces...
03/01/2005
6806272Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to new dihydropteridinones of the formula (I) wherein the groups X, R1, R2, R3, R4, R5 and R7 have the meanings given in t...
10/19/2004
6762188Pharmaceutically active benzoquinazoline compounds
Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the sa...
07/13/2004
6743817Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists...
06/01/2004
6740654Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —Sâ€...
05/25/2004
6696443Piperidine/piperazine-type inhibitors of p38 kinase
Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-଱ kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-଱ kinase activity....
02/24/2004
6664043Acridinium ester labels having hydrophilic modifiers
The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays f...
12/16/2003
6617330Pyrimidin-4-enamine as fungicide
Novel pyrimidine derivatives of formula I ##STR1## as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms ...
09/09/2003
6613772Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I ##STR1## in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular di...
09/02/2003
6593332Pharmaceutically active compounds
There is provided compounds of formula IA and of formula IB, ##STR1## wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical...
07/15/2003
6586439Pharmaceutically active compounds
There is provided compounds of formula IA and of formula IB, ##STR1## wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical...
07/01/2003
6525086Compounds, their preparation and use
The present invention relates to compounds of formula (I) ##STR1## wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the speci...
02/25/2003
6514988Condensed-ring thiophene derivatives, their production and use
A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or...
02/04/2003
6506762Certain alkylene diamine-substituted heterocycles
The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of N...
01/14/2003
6482859Microbicidal N-sulfonylglycin alkynyloxyphenethyl amide derivatives
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1 -C12 alkyl that is unsu...
11/19/2002
6458950Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,...
10/01/2002
64237184,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reve...
07/23/2002
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