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Class 544/120 - 1,4-Diazine ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the nitrogen atoms of the additional
No. of patents: 127
Last issue date: 12/02/2008


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NumberTitleIssue Date
7459554Imidazopyrazine tyrosine kinase inhibitors
Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various dis...
12/02/2008
7442699Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are...
10/28/2008
7317010Thieno-pyrrole compounds as antagonists of gonadotropin releasing hormone
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and ...
01/08/2008
7265108Nitrogen containing heterocyclic compounds and medicines containing the same
Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2
09/04/2007
71798075-substituted-2-arylpyrazines
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-aryl...
02/20/2007
7157249Delta subunit of human GABAA receptor
The present invention relates to the cloning of novel cDNA sequences encoding the α4 and δ receptor subunits of the human GABA A receptor; to stably co-transfected eukaryotic cell lines capable of expressing a human GABAA receptor,...
01/02/2007
7122544Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6
10/17/2006
7064201Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an in...
06/20/2006
70608222-pyrazolin-5-ones
Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inh...
06/13/2006
6995161Substituted arylpyrazines
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases as...
02/07/2006
6943196NF-κB inhibitor comprising phenylmethyl benzoquinone as the active ingredient
An NF-κB inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R...
09/13/2005
6908919Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a varie...
06/21/2005
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
6875764Urea and thiourea compounds useful for treatment of coccidiosis
The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coc...
04/05/2005
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
6835832Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
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...
12/28/2004
6774127Pyrazole and pyrazoline substituted compounds
Novel pyridyl and pyrimidinyl substituted pyrazole and pyrazoline compounds and compositions for use in therapy. ...
08/10/2004
6756377Compounds and their use
The invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as described in the specification, which compounds are ligands to the serotonin 5-HT2c receptor. ...
06/29/2004
6713472Thiazine or pyrazine derivatives
A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4...
03/30/2004
6710048Pyrazine derivatives as modulators of tyrosine kinases
The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical...
03/23/2004
6706021Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, R
03/16/2004
6699856Pyrazinones, compositions containing such compounds and methods of use
Compounds represented by formula I: ##STR1## as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-...
03/02/2004
6664255Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention...
12/16/2003
6610677Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: ##STR1## wherein Z1 is N or C--R9, Z2 is N or CH, and Z3 is N or C--Rx
08/26/2003
6579982Pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula ##STR1## wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compos...
06/17/2003
6559155Pyrimidinone derivatives for the treatment of atherosclerosis
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, ##STR1## in which: R1 is COOH or a salt thereof, COOR10, CONR11R.sup.12, CN or CH...
05/06/2003
6548512Nitrogen containing heteroaromatics as factor Xa inhibitors
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH2, which are useful...
04/15/2003
6476016Cyclic oxyguanidine pyrazinones as protease inhibitors
Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: ##STR1## wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically ...
11/05/2002
6472399Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR9 and Het, R1, R7, R8, R12 -R15, Ra, Rb
10/29/2002
6458952Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of ...
10/01/2002
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
6458790Substituted piperidines as melanocortin receptor agonists
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, ...
10/01/2002
6403583Thrombin or factor Xa inhibitors
This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention o...
06/11/2002
6362183Aromatic sulfonyl alpha-hydroxy hydroxamic acid compounds
An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid comp...
03/26/2002
6204263Pyrazinone protease inhibitors
Pyrazinone compounds are described, including compounds of the Formula I: ##STR1## wherein X is O, NR11 or CH.dbd.N, R3 -R11, Ra, Rb, Rc, W, m, and n are set forth in the specification, as well ...
03/20/2001
6194413Hemoregulatory compounds
The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases....
02/27/2001
6180627Antithrombotic agents
Compounds of formula (I): ##STR1## Are antithrombotic agents, having utility in a variety of therapeutic areas including the prevention and/or treatment of deep vein thrombosis (DVT) after surgery, major medical illness, paralysis, malignancy, prolonged ...
01/30/2001
6159980Pyrazinones and triazinones and their derivatives thereof
Corticotropin releasing factor (CRF) antagonists of Formula (I) ##STR1## and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorders, supranuclear pa...
12/12/2000
6147078Pyrazinone thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein ##STR2##...
11/14/2000
6093717Imidazopyridine thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein Y1 and Y2 are independently selected from the group consisting of hydrogen, C
07/25/2000
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