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Class 514/272 - Nitrogen bonded directly to the 1,3-diazine at 2-position


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a nitrogen is bonded directly to
No. of patents: 543
Last issue date: 05/22/2012


1                      
NumberTitleIssue Date
8183252Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2
05/22/2012
8158640Tetrahydroquinoline derivatives and a process for preparing the same
A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is op...
04/17/2012
8153644Diacylglycerol acyltransferase inhibitors
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
04/10/2012
8097631Fungicidal composition comprising cyprodinil
A fungicidal composition in the form of a liquid concentrate, which, in addition to at least one formulation adjuvant, comprises cyprodinil and an unsaturated C18-fatty acid selected from oleic acid, linoleic acid and linolenic acid. ...
01/17/2012
8063057Multicyclic amino acid derivatives and methods of their use
Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders: ...
11/22/2011
7998969Non-nucleoside reverse transcriptase inhibitors
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a
08/16/2011
7935711HIV inhibiting 2-(4-cyanophenylamino) pyrimidine oxide derivatives
HIV replication inhibitors of formula (I) a pharmaceutically acceptable addition salt; or a stereochemically isomeric form thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl. Pharmaceutical composition...
05/03/2011
7935710Microbicidal pyrimidine or triazine for preventing sexual HIV transmission
The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the...
05/03/2011
RE42015N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections
The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the admi...
12/28/2010
7790736Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein. ...
09/07/2010
7776872Diaminopyrimidines as P2Xand P2Xmodulators
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds...
08/17/2010
7767688Combination of pyrimidylaminobenzamide compounds and imatinib for treating gastrointestinal stromal tumours
The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) imatinib. and a method for treating or preventing a proliferative disease, especially GIST, us...
08/03/2010
769621717-acetamido-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uteru...
04/13/2010
7652021Compounds useful for DPP-IV enzyme inhibition
The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of ...
01/26/2010
7592348Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2
09/22/2009
7585870HIV 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...
09/08/2009
7560466Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...
07/14/2009
7531548HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH...
05/12/2009
7514445Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors)
This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1
04/07/2009
7504410Chk-, Pdk- and Akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases. ...
03/17/2009
7470700Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein. ...
12/30/2008
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
7429594Substituted heterocyclic compounds and methods of use
The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 ato...
09/30/2008
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
7423148Small molecule PI 3-kinase inhibitors and methods of their use
Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable ca...
09/09/2008
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
7384924Modified 2′ and 3′-nucleoside prodrugs for treating infections
2′ and/or 3′ prodrugs of 1′, 2′, 3′ or 4′-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and o...
06/10/2008
73784132-amino-3-(alkyl)-pyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; ...
05/27/2008
RE40332Fungicidal trifluoromethylalkylamino-triazolopyrimidines
The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with ca...
05/20/2008
7371758Antimalarial pyrimidine derivatives and methods of making and using them
Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstitu...
05/13/2008
7371871Inhibitors of glutaminyl cyclase
The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's di...
05/13/2008
7368421Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DP IV or DP IV-like enzymes, such as imm...
05/06/2008
7368576Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more pre...
05/06/2008
7365050Methods for modulating a drug-related effect or behavior
The present invention provides a method of reducing or preventing a drug-related effect or behavior in a subject by inhibiting N-type calcium channels. In addition, the invention provides a variety of prescreening and screening methods aimed at identifying agents th...
04/29/2008
7361653Pest control agent composition and method of using the same
The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivative...
04/22/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
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
7345050Pyrimidine compounds
The present invention relates to new compounds of the formula (I) a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, as well as intermediates used in the p...
03/18/2008
7338976Heterocyclic esters or amides for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides. ...
03/04/2008
7338958Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, ...
03/04/2008
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