Class 540/601 - The additional hetero ring is 1,3-diazine (including hydrogenated)

Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring has the following
No. of patents: 137
Last issue date: 07/29/2008

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Number	Title	Issue Date
7405209	Protease inhibitors The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...	07/29/2008
7390815	Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R...	06/24/2008
7351700	Aminomethylpyrimidines as allosteric enhancers of the GABA receptors The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached for...	04/01/2008
7223750	Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl,...	05/29/2007
7186827	Dipeptide synthesis Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section: ...	03/06/2007
7166597	Fused pyrazole derivatives being protein kinase inhibitors Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, R2, and R4 are various substituent groups, are protein kinase inhibitors	01/23/2007
7115597	Tyrosine kinase inhibitors The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...	10/03/2006
7071184	Protease inhibitors The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int...	07/04/2006
6921821	Antagonists of melanin concentrating hormone receptor This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R	07/26/2005
6916804	Pyrimidine A2b selective antagonist compounds, their synthesis and use The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R	07/12/2005
6887864	Azepane derivatives This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ...	05/03/2005
6844347	Substituted 4-amino-2aryl-pyrimidines, their production and use and pharmaceutical preparations containing same The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the trea...	01/18/2005
6743798	Substituted pyrazole derivatives condensed with six-membered heterocyclic rings The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation an...	06/01/2004
6730668	6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula:	05/04/2004
6680314	Azacyclooctane and heptane derivatives, their preparation and use in therapy Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ...	01/20/2004
6660731	Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula IV: ##STR1## wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are inde...	12/09/2003
6630475	Adenosine A2a receptor antagonists Compounds having the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or --C(O)CH2 --; Y is --N(R2)CH2 CH...	10/07/2003
6610677	Pyrazole 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
6602872	Substituted pyridazines having cytokine inhibitory activity There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis....	08/05/2003
6559155	Pyrimidinone 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
6476016	Cyclic 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
6420395	Azacyclooctane and heptane derivatives, their preparation and use in therapy The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl ...	07/16/2002
6410482	(Het) arylsulfonylureas having an amino function, their presentation and their use as herbicides and plant growth regulators (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof ##STR1## in which A is a (hetero)aromatic or heterocyclic bridge linked to the group...	06/25/2002
6384035	Heterocycles useful in the treatment of benign prostatic hyperplasia This invention relates a to a series of heterocyclic substituted piperazines of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to ...	05/07/2002
6380387	4-Pyrimidinyl-n-acyl-l phenylalanines Compounds of Formula I are disclosed, ##STR1## having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells ...	04/30/2002
6331506	Disubstituted methylidene hydrazinophenyl sulfonylureas, process for their production and their use as herbicides and plant growth regulators Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof ##STR1## in which R1 to R6, W, X, Y, Z are ...	12/18/2001
6294542	Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by bindi...	09/25/2001
6291450	Carboxylic acid substituted heterocycles, derivatives thereof and methods of use Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm...	09/18/2001
6268311	1-Amino-3-benzyluracils 1-Amino-3-benzyluracils I ##STR1## (X=oxygen, sulfur; R1 =C1 -C4 -haloalkyl; R2 =H, halogen; R3, R7 =H, CN, SCN, halogen, C1 -C4 -haloalkyl, C1 -C4 -h...	07/31/2001
6218538	2-aryl dihydropyrimidine compounds There are provided novel compounds of formula (I) ##STR1## including their 3,4-dihydropyrimidine tautomer form, wherein R1, R2, R3, R4, R5, X and n are as defined in the specification, and optical iso...	04/17/2001
6015813	Heterocyclic compounds and their preparation and use The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R1, R2, R3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutic...	01/18/2000
6013606	Substituted cinnamic oxime and hydroxamide derivatives Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R1= halogen, NO2, CN, CF3 ; R2 =H, halogen; R3= H, halogen, C1 -C6 -alkyl, C1...	01/11/2000
5922645	Alkylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof ##STR1## in which R1 to R6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties. They can be prepared by processes analogous to known processes...	07/13/1999
5922646	Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Acylated aminophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators. Compounds of the formula (I) and salts thereof ##STR1## in which W1, W2, R, n, R1, R2	07/13/1999
5914351	Anti-viral aromatic hydrazones Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R1 is hydrogen, halogen, alkyl or alkoxy; R2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; a...	06/22/1999
5869476	Pyrimidinone derivatives The invention relates to pyrimidinone derivatives and the pharmaceutically acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, and thus useful in treating cardiovascular diseases caused by angiotensin II....	02/09/1999
5866583	Substituted 2,4-diaminopyrimidines Compounds of formula I ##STR1## wherein R1 is lower-alkoxy, R2 is bromine, lower-alkoxy or hydroxy, R3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R4	02/02/1999
5854179	Sulfur-substituted phenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Sulfur-substituted phenylsulfonylureas; processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof ##STR1## in which R*, R1, R2, R3, X, Y, Z, W, n...	12/29/1998
5854234	Amidino dervatives useful as nitric oxide synthase inhibitors The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors....	12/29/1998
5846965	3-aza and 3-oxa piperidone tachykinin antagonists Compounds of the formula: ##STR1## wherein: X is O, NH or NR1 ; R1 is C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C4)alkyl, aryl ...	12/08/1998

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Class 540/601 - The additional hetero ring is 1,3-diazine (including hydrogenated)