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Class 544/301 - Nitrogen attached directly or indirectly to the diazine ring by nonionic bonding


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached directly or indirectly
No. of patents: 238
Last issue date: 04/15/2008


1            
NumberTitleIssue Date
7358239Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...
04/15/2008
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
7119201Triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W, and R1 are as defined in the specification, and to pharmace...
10/10/2006
RE39266Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compo...
09/05/2006
7074925N-substituted derivatives of 5-oxyiminobarbituric acid
N-substituted derivatives of 5-oximinobarbituric add of the general formula where X is sulfur; R1 is selected from the group consisting of saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl; and ...
07/11/2006
7067663Triazolo pyrimidine compounds
Pyrimidine compound (I) useful as a pharmaceutical intermediate, a process for preparing the pyrimidine compound (I), to intermediates used in the process, and use of the pyrimidine compo...
06/27/2006
7060826Compounds capable of activating cholinergic receptors
Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5...
06/13/2006
RE390564-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula...
04/04/2006
6960688Use of compounds for the elevation of pyruvate dehydrogenase activity
The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon ...
11/01/2005
6919332N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmac...
07/19/2005
6900222Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2
05/31/2005
6841671Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutica...
01/11/2005
6833372Non-peptide GnRH agents, Pharmaceutical compositions, and methods for their use
Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonad...
12/21/2004
68005902-Pyrimidinyloxy-n-aryl-benzylamine derivatives,their processes and uses
This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture. The compound has the following structure: wherein, D or E is hydr...
10/05/2004
67945063-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, a...
09/21/2004
6780868Linear cyclic ureas
Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6
08/24/2004
6720421PHENYLURETHANE COMPOUNDS AND METHODS FOR PRODUCING SAME, ASYMMETRIC UREA COMPOUNDS AND METHODS FOR PRODUCING SAME, BARBITURIC ACID DERIVATIVE, AND DIAZO THERMAL RECORDING MATERIAL CONTAINING THE DERIVATIVE
Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds...
04/13/2004
6716845Barbituric acid derivatives
The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compou...
04/06/2004
6713486Antiviral 2,4-pyrimidinedione derivatives and process for the preparation thereof
2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C6-10 aryl or C3-10 heteroaryl group optionally havin...
03/30/2004
6706723Pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and method...
03/16/2004
6680385Catalytic preparation of aryl methyl ketones using a molecular oxygen-containing gas as the oxidant
A method for the preparation of aryl methyl ketones converts a variety of ethyl arenas to the corresponding aryl methyl ketones using a dioxygen-containing gas as the oxidant. The catalyst used for the reaction is a metal complex bearing general formulas ...
01/20/2004
6664393N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
The present invention relates to compounds of the formula I, ##STR1## in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a stron...
12/16/2003
6624171Substituted aza-oxindole derivatives
Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiati...
09/23/2003
6624309Benzoic acid derivatives and related compounds as antiarrhythmic agents
Benzoic acid derivatives of the formula ##STR1## where X is oxygen, sulfur, --NH, --NR1, --N--CN, --N--OR1 or --N--NO2 ; Y is a single bond, --C.dbd.C--, or --NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycl...
09/23/2003
6613773Fungicides
The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: ##STR1## wherein X is CH2 O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an o...
09/02/2003
6600044Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucl...
07/29/2003
6583161Benzenesulfonamides and benzamides as therapeutic agents
The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particul...
06/24/2003
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
6552030Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: ##STR1## wherein Z1, Z2, R1, R2, R3, R4, R5, R6
04/22/2003
6518425Method of manufacture of 1,3-oxathiolane nucleosides
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the process...
02/11/2003
6498164Barbituric acid derivative and preventive and therapeutic agent for bone and cartilage containing the same
A compound of the formula ##STR1## wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases....
12/24/2002
6472396Barbituric 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 mono...
10/29/2002
6444682Base analogues
Nucleotide or base analogues having structure (3) or (4) ##STR1## wherein X.dbd.O or NH or S and each R6 is independently H or alkyl or alkenyl or alkoxy or aryl or a reporter moiety....
09/03/2002
6369273Chemical compounds and their use to elevate pyruvate dehydrogenase activity
The use of a compound of the formula (I): ##STR1## wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A--B is selecte...
04/09/2002
6342504Aromatic heterocyclic derivatives as enzyme inhibitors
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease ...
01/29/2002
6335332Barbituric acid derivatives with antimetastatic and antitumor activity
The invention is directed to barbituric acid derivatives having inhibitory activity for matrix maetalloproteases comprised of formula (I): ##STR1## pharmaceutical compositions thereof, processes for preparing the derivatives, and methods for treating dise...
01/01/2002
6329523Compounds having a plurality of nitrogenous substitutents
Novel compounds having the formula: ##STR1## wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear grou...
12/11/2001
6310069Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically accep...
10/30/2001
62880711-ethylene-2-alkylene-1,4-cyclohexadiene pesticides
Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection....
09/11/2001
6281219Acaricidal and insecticidal substituted pyrimidines and a process for the preparation thereof
The present invention provides compounds of Formula I ##STR1## methods for their preparation and their use as acaricidal and insecticidal agents....
08/28/2001
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