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Class 544/279 - Three ring nitrogens in the bicyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system contains three
No. of patents: 448
Last issue date: 03/27/2012


1                      
NumberTitleIssue Date
8143394Pyrido(3,2-d)pyrimidines useful for treating viral infections
2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a ...
03/27/2012
8071766HSP90 inhibitors
The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture compris...
12/06/2011
8039618Method for producing bicyclic guanidines by use of a cyclic urea
The present invention is directed to a method for producing bicyclic guanidines comprising heating a cyclic urea to a temperature >200° C. to form the bicyclic guanidines. ...
10/18/2011
7915264Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
03/29/2011
7915411Anti-viral compounds
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or t...
03/29/2011
7893259Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of ena...
02/22/2011
7842806Pyridopyrimidone derivatives, preparation thereof, therapeutic use thereof
The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt wit...
11/30/2010
7820816Process for the synthesis of CMHTP and intermediates thereof
The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hy...
10/26/2010
7816526Condensed heterocyclic sulfonyl urea compound, a herbicide containing the same, and a method for weed control using the same
The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an opt...
10/19/2010
7781583Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d] pryimidin-7-ones
The present invention provides methods of preparing substituted 2-(pyridin-2-ylamino)-pirido[2,3-d]pyrimidin-7-ones (formula 1), useful in treating cell proliferative disorders, or a pharmaceutically acceptable salt thereof...
08/24/2010
7777033Monomer with anti-microbial character, polymer using the same, and manufacturing method thereof
The present invention relates to a monomer with anti-microbial characteristics, a polymeric compound with anti-microbial characteristics using the same, and manufacturing methods thereof, and more particularly, to an antimicrobial monomer comprising a saturated or u...
08/17/2010
7601836Pyrido[2,3-D]pyrimidine inhibitors of phosphodiesterase (PDE) 7
Pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors are provided which are useful in treating T-cell mediated diseases, said inhibitors include: (i) 2-[[4-[[[4-(Aminosulfonyl)phenyl]methyl]amino]pyrido[2,3-d]pyrimidin-2-yl]amino]-4-methyl-5-t...
10/13/2009
75505896-(2-alkyl-phenyl)-pyrido[2,3-D]pyrimidines useful as protein kinase inhibitors
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as wel...
06/23/2009
7442710Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R...
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
7423042Compounds
This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and p...
09/09/2008
7407962Heteroaryl compounds useful as inhibitors or protein kinases
The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmac...
08/05/2008
7407963Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable p...
08/05/2008
7393853Use of substituted 8-Perfluoroalkyl-6,7,8,9-tetrahydropyrimido[1,2-] pyrimidin-4-one derivatives as therapeutic agents
The invention relates to use of a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein for treating a variety of disease states...
07/01/2008
7388005Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ...
06/17/2008
73880193-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV en...
06/17/2008
7378423Pyrimidine compound and medical use thereof
The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeuti...
05/27/2008
7375102Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use
Compounds are provided having the formula: wherein variables A1, A2, A3, A4, R1, R2, R3, R4, Q and L are as described herein. The subje...
05/20/2008
7371750Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d...
05/13/2008
7361662Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same
A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a phar...
04/22/2008
7348331Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in trea...
03/25/2008
7345171Isethionate salt of a selective CKD4 inhibitor
Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor use...
03/18/2008
7345045Pyrido-pyrimidine compounds as medicaments
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a nonin...
03/18/2008
7345040Reverse-turn mimetics and compositions and methods relating thereto
Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3
03/18/2008
7332498Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts there...
02/19/2008
7329664Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with ...
02/12/2008
73234722,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof. ...
01/29/2008
73209876-Alkoxy-pyrido-pyrimidines
The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(═O), Z is N or C...
01/22/2008
7314873(Halo-benzo carbonyl)heterobi cyclic p38 linase inhibiting agents
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty ar...
01/01/2008
73148812,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
01/01/2008
7312330Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of condi...
12/25/2007
7303750Methods to improve immunogenicity of antigens and specificity of antibodies
A method of improving specific immune response to small immunogens, haptens, has been developed by changing the linkage between the hapten and carrier being used for immunization. High affinity antibodies to cotinine have been produced using this method. Antibodies ...
12/04/2007
7279484Heterocyclic compounds
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent...
10/09/2007
7271181Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
09/18/2007
7265123Heterocyclic compounds
Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein...
09/04/2007
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