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Class 544/295 - Plural diazine rings


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain at least two of the six-membered
No. of patents: 1105
Last issue date: 04/26/2011


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NumberTitleIssue Date
6197750C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients su...
03/06/2001
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
6174901Substituted pyridine and pyridazine compounds and methods of use
Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-଱, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The inventio...
01/16/2001
6172066Dihydropyrimidines and uses thereof
This invention is directed to dihydropyrimidine compounds which are selective antagonists for human 򳄚 receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthes...
01/09/2001
61722274,5-diaminopyrimidine derivatives and a method for the preparation thereof
Novel 4,5-diamino pyrimidine derivatives are described by the following general formula I: ##STR1## in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a...
01/09/2001
6169086Pyrazole derivatives
The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): ##STR1## wherein G represents a nitrogen containing saturated heterocyclic structure ...
01/02/2001
6166027Heterocyclylmethyl-substituted pyrazole derivatives and their use for treating cardiovascular diseases
The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases....
12/26/2000
6166020Aryl and heteroaryl alkoxynaphthalene derivatives
Compounds of the formula ##STR1## wherein R1, R2, R4, R23, R24, R25 and R26 are defined as in the specification. These compounds are useful psychotherapeutics and are potent sero...
12/26/2000
6162809Pyridylthio compounds for controlling helicobacter bacteria
Pyridinylthiomethyl- and pyrimidinylthiomethyl-pyridines and their pharmacologically-acceptable compositions are useful for controlling Helicobacter bacteria and for treating those afflicted with diseases based on Helicobacter bacteria....
12/19/2000
6159995Substituted diaminocarboxylic acids
Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved....
12/12/2000
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
61536132,3-diketopiperazine derivatives or their salts
The present invention relates to a 2,3-diketopiperazine derivative or a salt thereof, which has inhibitory effect on platelet aggregation because of glycoprotein IIb/IIIa receptor antagonism and hence is useful as a prophylactic and therapeutic agent for ...
11/28/2000
6150356Potassium channel inhibitors and method
Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds...
11/21/2000
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
6143892Process for making 5-substituted pyrazoles
This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors....
11/07/2000
6143750Alpha 1a adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds ...
11/07/2000
6143744Sulfamide-metalloprotease inhibitors
This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds....
11/07/2000
6136971Preparation of sulfonamides
The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M1...
10/24/2000
61332681,4-disubstituted piperazines
The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R1, R2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their ...
10/17/2000
6130215Piperazinylalkylthiopyrimidine derivatives, pharmaceutical compositions containing the same and a process for the preparation of the novel compounds
The invention refers to novel piperazinylalkylthiopyrimidine derivatives of formula (I) being suitable for the treatment of diseases due to pathological alterations of the central nervous system, pharmaceutical compositions containing the above derivative...
10/10/2000
6127357N-((phenyl, benzodioxinyl or N-heteroarylpiperazinyl)alkyl)-N-(N-heteroaryl)substituted carboxamides
Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT1A binding agents, particularly 5-HT1A antagonists and may be used, for example, as anxiolytics. In the formula A is ...
10/03/2000
6124306Thioalkyl alpha substituted pyrimidine compounds
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R4 is selected from the group consisting of --H or --NR15 R16...
09/26/2000
6124294Triazole compounds and the use thereof
The present invention relates to triazole compounds of the following formula: where R1, R2, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 re...
09/26/2000
61143422-(O-[pyrimidin-4-yl]methylenoxy)phenylacetic acid derivatives and their use for controlling harmful fungi and animal pests
2-(O-[pyrimidin-4-yl]methylenoxy)phenylacetic acid derivatives of the general formula I and the salts and N-oxides thereof where the radicals R1 to R4 and Q have the following meanings: R1 is hydrogen or alkyl; R2 is...
09/05/2000
6114334Piperazine derivatives as therapeutic agents
Substituted piperazine compounds of formula I ##STR1## in which HET is a substituted pyrazole, imidazole or 1,2,4-triazole have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schi...
09/05/2000
61143332-Pyrimidineamine derivatives and processes for their preparation
Compounds of general formula (1) ##STR1## are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group --X1 --R2a where X1 is a direct bond or a linker atom ...
09/05/2000
6110924Barbituric acid derivatives, processes for their production and pharmaceutical agents containing these compounds
Compounds of formula I, useful as matrix metalloprotease inhibitors, ##STR1## wherein X, Y and Z are each oxygen; R1 is selected from the group consisting of (a) n-octyl, (b) n-decyl, (c) biphenyl and (d) (4-phenoxy)phenyl, wherein the terminal...
08/29/2000
6103719Neurokinin antagonists, processes for preparing them and pharmaceutical compositions containing these compounds
The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R3 or CH--R4, Y=CH2 or (CH2)2, Z=O or H2 ; and R1
08/15/2000
6100265Thiopyran derivatives
A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## ...
08/08/2000
6096753Substituted pyrimidinone and pyridone compounds and methods of use
Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-଱, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention enco...
08/01/2000
6093718Substituted pyrimidine derivatives and their pharmaceutical use
This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives ...
07/25/2000
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
6093716Substituted 2-pyrimidineamines and processes for their preparation
Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R1 is a hydrogen atom or a straight or branched chain alkyl group; R2 is a hydrogen or halogen atom or a gro...
07/25/2000
60908091-(4-arylpiperazin-1-yl)-ω-[n-(଱.. omega.-dicarboximido)]-alkanes useful as uro-selective ଱1 -adrenoceptor blockers
Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective 򳄚 adrenergic activi...
07/18/2000
60839501-(4-arylpiperazin-1-yl)-ω-[n-(଱,ω-dicarboximido)]-alka nes useful as uro-selective 댑-adrenoceptor blockers
Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective 򳄚 adrenergic activi...
07/04/2000
6080738Heterocyclic amide compounds and medicinal uses thereof
A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and a pharmaceutical use thereof. The heterocyclic ami...
06/27/2000
6069251Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4- substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4
05/30/2000
6066637Indolyl derivatives as serotonergic agents
The present invention provides compounds represented by the general formula (1) wherein R1 is selected from H, OH, OR2 or halogen (F, Cl, Br, I); R2 is lower alkyl (C1 to C6); n is selected from 0, 1 or 2; X is...
05/23/2000
6057304Quinoxaline-phosphonic acid derivatives
The disclosure relates to quinoxaline derivatives of Formula I ##STR1## wherein R1, R4, R5, R6, R7 and R8 are as defined in the disclosure, as well as their production and use in medic...
05/02/2000
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