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Class 544/324 - Additional hetero ring which is unsaturated


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds having, in addition to the six-membered hetero
No. of patents: 425
Last issue date: 04/19/2011


1                      
NumberTitleIssue Date
7928230Method for modulating GPR119 G protein-coupled receptor and selected compounds
A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therape...
04/19/2011
7442705HIV replication inhibiting pyrimidines and triazines
This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharm...
10/28/2008
74358142,4-Pyrimidinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...
10/14/2008
7427681Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, whe...
09/23/2008
7419984Pyrimidines and uses thereof
The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells. ...
09/02/2008
7414046Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...
08/19/2008
7405221Substituted pyrimidines
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are...
07/29/2008
RE40245Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...
04/15/2008
7351712Pyrimidine 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...
04/01/2008
7345048Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors
The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, an...
03/18/2008
7338959Diamino-pyrimidines and their use as angiogenesis inhibitors
Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative di...
03/04/2008
7335672Vanilloid receptor ligands and their use in treatments
Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inf...
02/26/2008
73324842,4-pyrimidinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...
02/19/2008
7288547CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or If as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases. ...
10/30/2007
7282504Kinase inhibitors
The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention...
10/16/2007
7262200Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK...
08/28/2007
7262203Pyrimidineamines as angiogenesis modulators
Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. ...
08/28/2007
7253174N-heterocyclic inhibitors of TNF-α expression
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharm...
08/07/2007
7241769Pyrimidines as PLK inhibitors
The present invention comprises compounds of general formula (1) wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in clai...
07/10/2007
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
7230104Fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines
Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered h...
06/12/2007
7220736Pyrimidine compounds
A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—,...
05/22/2007
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
7205310Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. Such compounds are useful in the treatment of inflammatory diseases in a mammal...
04/17/2007
7205307Pyrimidines as novel openers of potassium ion channels
The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods. ...
04/17/2007
7179604Methods of use of DNA encoding a human histamine receptor of the H3 subtype
DNAs encoding the human histamine H3 receptor have been cloned and characterized. The recombinant protein is capable of forming biologically active histamine H3 receptor protein. The cDNA's have been expressed in recombinant host cells which produce active recombina...
02/20/2007
7179816Chemical derivatives and their application as antitelomerase agents
The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which inhibits telomerase. It also relates to novel chemical compounds as well as their therapeutic application in humans. ...
02/20/2007
7173028Pyrimidine derivatives
The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characteri...
02/06/2007
7166599Trisubstituted pyrimidines
The present invention relates to trisubstituted pyrimidines of formula wherein Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses in which β-amy...
01/23/2007
71574554-Aminopyrimidine-5-one derivatives
Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are ...
01/02/2007
7153964Pyrimidine compounds
Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2
12/26/2006
71538605-Phenylpyrimidines, methods and intermediate products for the production thereof and use of the same for controlling pathogenic fungi
The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains betwee...
12/26/2006
7151106Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use
The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumor therapy.
12/19/2006
7148219Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th...
12/12/2006
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
7135477Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the ...
11/14/2006
7122552Inhibitors of JAK and CDK2 protein kinases
The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of JAK and CDK2 mammalian protein ...
10/17/2006
7122670Selective synthesis of CF3-substituted pyrimidines
The present invention relates to a method of making a compound of the formula wherein X1, X2 and R3—R4 are as defined herein. The method includes reacting a compound ...
10/17/2006
7115617Amino-substituted pyrimidinyl derivatives and methods of use
The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer. ...
10/03/2006
7109204Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
09/19/2006
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