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...that in 1800 ether was first used by partyers as a fun diversion? Sniffing the gas led to hilarious and raucous laughter as people watched each other become more and more intoxicated and silly. Several doctors independently realized the value ether would have to anesthetize surgery patients. Of those who claimed rights to the "discovery," none had a happy ending. One had a seizure and died defending his rights. Another spent his life in an asylum because he had been denied acclaim. A third became addicted to chloroform and, in a New York City jail, he soaked a cloth in the drug, severed an artery and bled to death.

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Class 514/313 - Nitrogen, other than as nitro or nitroso, attached directly to the six membered hetero ring by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein nitrogen, except as a member of the
No. of patents: 638
Last issue date: 05/08/2012


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NumberTitleIssue Date
59624687-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1- cyclopropyl-6-fluoro-4-oxo-1, 4-dihydro-1, 8-naphthyridine-3-carboxylic acid and the process for the preparation thereof
The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1,4-dihydro-1,8...
10/05/1999
5958947DNA-affinic hypoxia selective cytotoxins
Hypoxia selective cytotoxins having the structural formula ##STR1## wherein D, E, F and G, independently, are carbon or nitrogen, with the proviso that three or more of D, E, F and G are carbon; R1 and R2, independently, are sel...
09/28/1999
5955473Fungicidal quinolines
Quinolines of the formula I ##STR1## where the substituents are as defined herein, the corresponding N-oxides and acid addition salts, a process for their preparation, fungicidal compositions, and their use for controlling harmful fungi....
09/21/1999
5952354Tris carbamic acid esters: inhibitors of cholesterol absorption
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholester...
09/14/1999
5948791Quinoline derivatives for treating malaria
The invention relates to novel quinoline derivatives and their therapeutic use against malaria....
09/07/1999
5935973Heterocyclcarboxamide derivatives and their use as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R1 is an optional substituent; U is an alkylene chain optionally substituted by one or more...
08/10/1999
5932195Arylaminomethylenecamphor derivatives
Arylaminomethylenecamphor derivatives of the formula (1) ##STR1## where the C.dbd.C double bond is in the Z or E configuration, and the variables have the following meanings: R1 H, CH3, R2 H, C1 -C6 -...
08/03/1999
5925660Phosphatase inhibitors and methods of use thereof
The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B...
07/20/1999
5922733Pyridil carboxamides as 5HT2B/2C receptor antagonists
Novel heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders are disclosed....
07/13/1999
59169007-(2-imidazolinylamino)quinoline compounds useful as alpha-2 adrenoceptor agonists
This invention involves involves the use of compounds having the following structure: ##STR1## wherein: (a) R is unsubstituted C1 -C3 alkanyl or alkenyl; and (b) R' is selected from hydrogen; unsubstituted C1 -C3
06/29/1999
5908842Substituted 2-acylamino-pyridines as inhibitors of nitric oxide synthase
Substituted 2-acylaminopyridine compounds and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders....
06/01/1999
5889021Active Compounds
The present invention relates to novel quinoline derivatives of the formula ##STR1## which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory dis...
03/30/1999
5885967Antithrombotic agents
This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors....
03/23/1999
5880135Substituted 4-phenylaminothiazoles, their process of preparation and the pharmaceutical compositions containing them
A compound, as well as its stereoisomers and addition salts, possssing antagonist activity with respect to corticotropin releasing hormone (CRF) has the formula: ##STR1## in which R1, and R21 which are identical or different, ar...
03/09/1999
5866562Ring-bridged bis-quinolines
The present invention relates to ring-bridged bis-quinolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides a process for the preparation of compounds of the ...
02/02/1999
5866579Imidazole and imidazoline derivatives and uses thereof
This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human 댒 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease...
02/02/1999
5859025Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process for their preparation, and their use
Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process or their preparation, and their use Heterocyclic fluoroalkyl derivatives and fluoroalkoxy derivatives of the formula (I) having bradykinin-antagonistic action ##STR1## ...
01/12/1999
5856309Amidinopyrroline derivatives, processes for their production and pharmaceutical agents containing these compounds
Compound of formula (I) are disclosed ##STR1## as well as optically active isomers or pharmacologically acceptable salts thereof. The compounds are useful active ingredients in pharmaceutical compositions, and methods of treating osteoporosis, inflam...
01/05/1999
5856338Sulfonamide-substituted compounds, processes for their preparation, their use as a medicament or diagnostic, and pharmaceutical preparation comprising them
Compounds of formula I ##STR1## having the meanings indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias; for the tre...
01/05/1999
5856322Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in t...
01/05/1999
5837714Solid pharmaceutical dispersions
This invention provides solid pharmaceutical dispersions comprising a poorly soluble drug substance, as SR48692 or naproxen, xylitol and Transcutol, and a method of preparing such dispersions comprising the steps of dissolving the poorly soluble drug subs...
11/17/1998
5834485Quinoline sulfonamides and their therapeutic use
The subject invention pertains to quinolinesulfonamides. The subject compounds can be used to treat disease states, such as those that are associated with proteins that mediate cellular activity, for example, by inhibiting phosphodiesterase IV (PDE IV) or...
11/10/1998
5827865Heterocyclic compounds as pharmaceutical
Compounds of Formula (I) A1 --X--(CH2)n --O--A2 --A3 --Y.R2(I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wh...
10/27/1998
5798365Substituted quinoline derivatives, a process for their preparation, and their use
Compounds of the formula I, ##STR1## and also their tautomeric forms of the formula Ia, ##STR2## in which the substituents R1 to R6 and X have said meanings, exhibit antiviral activity....
08/25/1998
5795889Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from ...
08/18/1998
5786365Use of nonpeptide bradykinin antagonists for the treatment and prevention of chronic fibrogenetic liver disorders, acute liver disorders and the complications associated therewith
The invention relates to the use of nonpeptide bradykinin antagonists for the production of pharmaceuticals for the treatment of chronic fibrogenetic liver disorders (hepatic cirrhosis and hepatic fibrosis), acute liver disorders and for the prevention of...
07/28/1998
5783576Benzoyl guanidine derivatives, the preparation thereof and their use in pharmaceutical compositions
New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions....
07/21/1998
5776947Use of quinoline-3-carboxamide compounds for inhibiting the production of tumor necrosis factor (TNF) and/or for the treatment of septic shock
The use of a quinoline-3-carboxamide compound comprising structure (I), optionally with substituents for the hydrogen atoms shown (H1-9), and a salt of compound (I) where (a) ---- represents that there are two conjugated double bonds between th...
07/07/1998
5767129Substituted quinolines and isoquinolines as calcium channel blockers, their preparation and the use thereof
The present invention relates to novel substituted quinolines and isoquinolines and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compo...
06/16/1998
5756532Aminomethyl-2 3 8 9-tetrahydro-7H-1 4-dioxino›2 3-E!-indol-8-ones and derivatives
The compounds of formula I: ##STR1## wherein R1 and R2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defin...
05/26/1998
5747532Combinational therapeutic methods employing nitric oxide scavengers and compositions useful therefor
In accordance with the present invention, there are provided combinational therapeutic methods for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of nitric oxide synthase, as well...
05/05/1998
57391486-(2-Imidazolinylamino) quinoline compounds useful as alpha-2 adrenoceptor agonists
The subject invention relates to compounds having the structure: ##STR1## wherein: (a) R is unsubstituted C1 -C3 alkanyl or alkenyl; (b) R' is selected from unsubstituted C1 14 C3 alkanyl or alkenyl; unsubstitut...
04/14/1998
5736557N,N-bis (quinolin-4-yl)-diamine derivatives, their preparation and their use as antimalarials
Disclosed are N,N'-bis(quinolin-4-yl)diamine derivatives of general formula I wherein R1 signifies halogen or trifluoromethyl, R2 signifies hydrogen or halogen, A signifies cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohe...
04/07/1998
5733931Cyclohexanediurea derivative and process for its production
The present invention provides a cyclohexanediurea derivative, inclusive of its salt, represented by the following formula (I): ##STR1## wherein R1 and R2 are the same or different and they each represent a straight-chain or bra...
03/31/1998
5719144Fibrinogen receptor antagonists
Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH2)p, where p is 1 or 2; and Z is --CR1 .dbd.CR2 --; which are useful for inhibiting platelet aggregation for example ##STR...
02/17/1998
5716967Isoxazoline compounds as antiinflammatory agents
This invention relates to isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDEIV). The isoxazoline compounds are useful in inhibiting PDEIV and in the treatment of AIDS, asthma, arthritis, bronchitis...
02/10/1998
57169667-(2-imidazolinylamino)quinoline compounds useful as alpha-2 adrenoceptor agonists
The subject invention involves methods of treating nasal congestion comprising administration, to a human or lower animal in need of such treatment of a safe and effective amount of a compound having the following structure: ##STR1## wherein: (a...
02/10/1998
5712289Quinoline-5,8-diones and methods of using them
The invention provides quinoline-5,8-diones having the following formula: ##STR1## wherein X, Z and R1 through R3 are defined in the specification, and salts of these quinolinediones. The invention also provides a method of maki...
01/27/1998
5700821Phosphatase inhibitors and methods of use thereof
The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B...
12/23/1997
5698581Substituted N-heteroaroylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing them
The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly sui...
12/16/1997
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