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Class 546/283.7 - Plural ring oxygens in the additional hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional hetero ring contains at
No. of patents: 305
Last issue date: 02/28/2012


1                
NumberTitleIssue Date
8124781Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1). ...
02/28/2012
7678919Method for producing pentacyclic taxans
Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group...
03/16/2010
7410980Crystals of taxane derivative and process for their production
A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at dif...
08/12/2008
7297797Pyrrolines
The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R
11/20/2007
7205305Inhibitors 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...
04/17/2007
7157454Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal pr...
01/02/2007
7119208Anti-sickling agents
Compounds for the treatment of sickle-cell disease, and methods for their use are provided. The compounds have a dual mode of action. First, binding of the compounds to hemoglobin increases the oxygen affinity of both normal and sickle hemoglobin. Secondly, binding ...
10/10/2006
7026476Intermediate 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
6900231Aminopyridyl-substituted phenyl acetamides as protease inhibitors
Phenyl acetamide compounds are described, including compounds of or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the s...
05/31/2005
6867230Hygromycin A derivatives
This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10
03/15/2005
6689798Benzofuran derivatives
The present invention provides novel benzofuran derivatives represented by the following formula (I) or salts thereof: ##STR1## wherein Py is a 2-, 3-, or 4-pyridyl group and R is a substituted or unsubstituted phenyl group or a substituted or unsubstitut...
02/10/2004
6677330Fluorides of 4-substituted piperidine derivatives
The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof ...
01/13/2004
6649633Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the form...
11/18/2003
6646123Pentacyclic Compound
The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R1 : a phenyl group, R2 : an alkyl group, an alkenyl group, an alkynyl group, a...
11/11/2003
6608060Inhibitors 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...
08/19/2003
6545151Pentacyclic compound
The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). ##STR1## [In the formula (I), R1 : a phenyl group, R2 : an alkyl group, an alkenyl group, an alkynyl group, a...
04/08/2003
6511995Pyridine derivative and pharmaceutical containing the same
A pyridine derivative represented by formula (1) wherein all the variables have been defined in the specification. The compounds are used for inhibiting collagen production and are useful for preventing or treating fibrosis. ##STR1##...
01/28/2003
6498172Prostaglandin agonists and their use to treat bone disorders
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for t...
12/24/2002
6441173Process for preparing indane carboxylate and cyclopentano [6] pyridine derivatives
This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedi oxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the eth...
08/27/2002
6417161Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1## wherein X is O or NR19 and A1, A2, R7 -R10, R18, Ra,...
07/09/2002
6413979Substituted 5-(2,2-difluoro-1,3-benzodioxol-5-yl) cyclopentenopyridine derivative
The present invention relates to a cyclopentenopyridine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is a phenyl group or the like. R1 is a mono- or di-C1 -C6 alky...
07/02/2002
6376538Cell adhesion inhibitors
The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of us...
04/23/2002
63690832-methoxyimino-2 (pyrinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of ...
04/09/2002
6353110Asymmetric conjugate addition reaction
This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction....
03/05/2002
63424972"-deoxy hygromycin derivatives
This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotoz...
01/29/2002
6340704Cell differentiation inducing amide derivatives, their production and use
The present invention provides a compound represented by the formula: ##STR1## wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which m...
01/22/2002
6262084Compounds that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of 댔ଲ.sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions the...
07/17/2001
6262083Genipin derivative having liver protection activity
The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects....
07/17/2001
6232319Substituted tetrahydropyridin derivatives, method of preparation and pharmaceutical compositions containing them
The invention relates to compounds of general formula (I): ##STR1## in which R, R1, R2, X and Y are as defined in the description, their geometrical and/or optical isomers, and their addition salts with a pharmaceutically-acceptable ...
05/15/2001
6211363Pentacyclic compound
The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). ##STR1## [In the formula (I), R1 : a phenyl group, R2 : an alkyl group, an alkenyl group, an alkynyl group, a...
04/03/2001
62112022-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides with substituted ketal derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with substituted ketal substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at l...
04/03/2001
6194448N, N-disubstituted amides that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of 댔ଲ.sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions com...
02/27/2001
6172235Asymmetric conjugate addition reaction
This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction....
01/09/2001
6133442Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Compounds of formula I ##STR1## wherein R1 signifies phenyl, substituted phenyl or heterocyclyl; R2 signifies phenyl or substituted phenyl; R3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, su...
10/17/2000
6130335N-([1,2,4]triazoloazinyl) benzenesulfonamide and pyridinesulfonamide compounds and their use as herbicides
N-(Triazoloazinyl)arylsulfonamide compounds, such as 2,6-dimethoxy-N-(8-chloro-5-methoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)be nzenesulfonamide, 2-methoxy-4-(trifluoromethyl)-N-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimi din-2-yl)pyridine-3-sulfonamide...
10/10/2000
6121451Intermediates and process for the manufacture of camptothecin derivatives (CPT-11) and related compounds
This invention relates to intermediates and processes for the synthesis of camtothecin derivatives, such as irinotecan. Related procedures and compounds are disclosed, such as a method of making mappicine....
09/19/2000
6075140Pentacyclic compound
The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R1 : a phenyl group, R2 : an alkyl group, an alkenyl group, an alkynyl gro...
06/13/2000
6060487Indanol compounds
A compound of formula (I): ##STR1## wherein R1, R2, R3, R4, X--Y, A, Z and Z' are as defined in the description, in the form of the cis or trans isomers each in racemic or optically active form, and acid ad...
05/09/2000
6037356Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR9 and Het, R1, R7, R8, R12 -R15, Ra, Rb...
03/14/2000
6028033N-aminopyridone derivatives and their use as herbicides
There are described N-aminopyridone derivatives of the formula I: ##STR1## where the substituents R1 to R12 have the meanings given in claim 1, a process for their preparation, and their use for controlling undesirable vegetatio...
02/22/2000
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