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Class 546/268.4 - The additional hetero ring is five-membered having two or more ring hetero atoms of which at least one is nitrogen


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is five-membered
No. of patents: 403
Last issue date: 12/27/2011


1                      
NumberTitleIssue Date
8084613Tetrazoyloxime derivative and plant disease control agent
The present invention provides a tetrazoyloxime derivative or salt thereof, represented by the following formula (1): [wherein, R1 represents an optionally substituted C1-C6 alkyl group etc., q represents an inte...
12/27/2011
7902369Diaryl-substituted five-membered heterocycle derivative
The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2
03/08/2011
7696352Factor Xa inhibitors
The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, p...
04/13/2010
74427162-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to t...
10/28/2008
74392607-(1,3-thiazol-2-YL)thio-coumarin derivatives and their use as leukotriene biosynthesis inhibitors
The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
10/21/2008
7429605Phenylpyridine derivatives
The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical comp...
09/30/2008
7425570Pyridoxine and pyridoxal analogues: new uses
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these anal...
09/16/2008
7414055Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
08/19/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7375122Compounds useful as pesticides
Compounds useful to control pests are provided. ...
05/20/2008
7361672Heteroarylacetamide inhibitors of factor Xa
The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb)  (I) wherein Ra to Re are as def...
04/22/2008
7361654Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea...
04/22/2008
7323570Farnesyltransferase inhibitors
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase ...
01/29/2008
7309800Biphenylcarboxylic amide derivatives as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
12/18/2007
7273936Oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of tran...
09/25/2007
7268229Compounds to co-localize luminophores with luminescent proteins
A method of measuring the enzymatic activity of a luciferase includes contacting a luminogenic protein, such as a luciferase, with a protected luminophore to form a composition; and detecting light produced from the composition. The protected luminophore provides in...
09/11/2007
7253190Heteroaryl substituted tetrazole modulators of metabotrophic glutamate receptor-5
Tetrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia...
08/07/2007
7250518Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes
Compounds of the formula: useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils. ...
07/31/2007
7238714Aryl or heteroaryl amide compounds
This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 indepe...
07/03/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7211595Farnesyltransferase inhibitors
Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a p...
05/01/2007
7208169Biphenyl carboxamides
The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality...
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
7205318Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Com...
04/17/2007
7205320Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 ...
04/17/2007
7179822Hetero biaryl derivatives as matrix metalloproteinase inhibitors
This invention provides compounds defined by Formula I and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable...
02/20/2007
7169798Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described be...
01/30/2007
7157580Aminopyrimidine and aminopyridine anti-inflammation agents
Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein ...
01/02/2007
7153871Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs
PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3
12/26/2006
7151118Biphenylcarboxylic amide derivatives as p38-kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
12/19/2006
7125887Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokin...
10/24/2006
7112599Oxazole compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula wherein R3, R5, R6, R7, and Z, and other variables enumerated under one or more of R3, R5
09/26/2006
7105548Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5
Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatri...
09/12/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7078419Cytokine inhibitors
Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit pro...
07/18/2006
7071175Pyridine mercapto carboxylic acids as carboxypeptidase U inhibitors
The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prev...
07/04/2006
RE39113Utilization of derivatives of tetrahydropyridines(or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain
Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R1, R2 and R3, which are similar or different, represent each of them hydrogen, halogen, alkyl C1-C4, trifluorometh...
05/30/2006
7038057Substituted 1-dihydropyrazoles, their preparation and use
This invention provides compounds of Formula (I), methods for their preparation and use for preparing compounds of Formula (II) wherein R1, R2, R3, R5, R6, X and n are as defined in the disclosure. This inventio...
05/02/2006
7026324Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C1...
04/11/2006
7026321Substituted heterocyclic compounds
Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ...
04/11/2006
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