Class 544/152 - The additional hetero ring is five-membered

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is five-membered.
No. of patents: 135
Last issue date: 05/20/2008

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Number	Title	Issue Date
7375105	Pyridine substituted furan derivatives as Raf kinase inhibitors Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R	05/20/2008
7189714	N-type calcium channel antagonists for the treatment of pain Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and...	03/13/2007
7101878	Non-peptide GNRH agents, methods and intermediates for their preparation Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorde...	09/05/2006
7026476	Intermediate arylamine compounds Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes...	04/11/2006
6759409	Inhibitors of papilloma virus A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as ...	07/06/2004
6730671	Compounds useful as reversible inhibitors of cathespin S Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.	05/04/2004
6686390	Compounds having antiinflamatory activity: process for their preparation and pharmaceutical compositions containing them The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their p...	02/03/2004
6638967	Thiophene of furan pyrrolidine compounds Compounds of Formula I ##STR1## Wherein Z2 is an Oxygen or a Sulfur, Z1 is --CH.dbd.CH-- and Y is a bond, W1 and W2 are hydrogens and X1 and X2 are various heterocyclic rings are disclosed....	10/28/2003
6608057	Compounds useful as reversible inhibitors of cathepsin S Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds ##STR1##...	08/19/2003
6444615	Herbicidal imidazolidinetrione and thioxo-imidazolidinediones This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In...	09/03/2002
6362183	Aromatic sulfonyl alpha-hydroxy hydroxamic acid compounds An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid comp...	03/26/2002
6258841	Tubulin binding compounds (COBRA) Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds a...	07/10/2001
6117870	Cyclic amide derivatives A cyclic amide derivative of formula (I): ##STR1## wherein R1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl...	09/12/2000
6051571	Methods for treating medical dysfunctions and diseases using furan nitrone compounds Disclosed are methods for treating a patient with an acute central nervous system or cardiovascular disorder or a neurodegenerative, autoimmune or inflammatory disease using a pharmaceutical composition containing a pharmaceutically acceptable carrier and...	04/18/2000
6040444	Process for preparing furan nitrone compounds Disclosed are processes for preparing furan nitrone compounds using a furan carbonyl compound and a hydroxylamine compound....	03/21/2000
6022870	Fungicidal cyclic amides Cyclic amides of Formula I which are useful as fungicides: ##STR1## wherein A is N; G is N and the floating double bond is attached to A; W is O or S; X is OR1, S(O)m R1 or halogen; R1, R2, R	02/08/2000
6017947	Heterocyclic carbodithioperoxyimidic compounds useful for the inhibition of the replication of HIV R6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro; R10 is phenylthio, dialkylamino, alkylthio, alkoxycarbonyl, N-morpholinyl, or N-piperidinyl; R11 is hydrogen or alkyl; Q is alkoxy, alkenyloxy, alkynyloxy, alkylthio, alke...	01/25/2000
5994396	Furansulfonic acid derivatives and pharmaceutical compositions containing the same Disclosed are furansulfonic acid derivatives and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals....	11/30/1999
5942507	Furan nitrone compounds Disclosed are furan nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compounds are useful as analytical reagents for detecting free radicals and as therapeutics for treating a wide variety of medical dysfunctions ...	08/24/1999
5922706	Morpholine and thiomorpholine tachykinin receptor antagonists Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of ca...	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
5891368	Fluoranthenopyrans Described are novel photochromic 8-substituted fluoranthenopyran compounds having certain substituents at the 5 position of the pyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric org...	04/06/1999
5891876	Heteroatom substituted benzoyl derivatives that enhance synaptic responses mediated by AMPA receptors Compounds useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof, and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to ...	04/06/1999
5744607	Basic derivatives of glutamic acid and aspartic acid as gastrin or cholecystokinin antagonists The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or...	04/28/1998
5723607	Compounds useful as antiproliferative agents and GARFT inhibitors The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH2, O, NH or Se, and when n is 0, A i...	03/03/1998
5714484	଱-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a ...	02/03/1998
5708169	5-amidomethyl ଱,ଲ-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents The present invention provides for new 5-amidomethyl, ଱,ଲ-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substi...	01/13/1998
5691374	Diaryl-5-oxygenated-2-(5H) -furanones as COX-2 inhibitors The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of ...	11/25/1997
5674811	Cyanoketone derivative and herbicide containing it as an active component A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth a...	10/07/1997
5648486	Compounds and methods for the treatment of inflammatory and immune disorders 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respira...	07/15/1997
5599820	Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## ...	02/04/1997
5567721	Di(aromatic) compounds and their use in human and veterinary medicine and in cosmetics Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R1, R2	10/22/1996
5472956	Phosphoramidates useful as antitumor agents Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R1 and R2 are each (C2 -C6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R3 and R4 ...	12/05/1995
5462939	Peptidic ketones as interleukin-1ଲ-converting enzyme inhibitors Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R1 is (CR5 R6)n, (CR5 R6)n -aryl, (CR5 R6)	10/31/1995
5459131	Renin inhibitors Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO2, P is 1 or 2 and X is --O-- or --S--; and analogs thereof which inhibit the substrate-c...	10/17/1995
5434151	Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respira...	07/18/1995
5358938	Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respirato...	10/25/1994
5314889	Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them A 2-Acylaminothiazole of formula: ##STR1## in which R1 is H, an alkyl or a substituted alkyl; RIV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; RV is...	05/24/1994
5240924	N-acylamino acid derivatives and their use An N-acylamino acid derivative of the formula: ##STR1## wherein the substituents are herein defined, or a salt thereof, which is useful as hypotensive drugs....	08/31/1993
5227400	Furyl and thienyl substituted taxanes and pharmaceutical compositions containing them A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT1, T1 is hydrogen, hydroxyl protecting group, or --COT2, T2 is H, C1 -C6 alkyl, C1 -C6 ...	07/13/1993

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Class 544/152 - The additional hetero ring is five-membered