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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 546/275.4 - 1,2-diazoles (including hydrogenated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring has nitrogens
No. of patents: 543
Last issue date: 05/22/2012


1                      
NumberTitleIssue Date
8183381N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. ...
05/22/2012
8119811Method for producing amide compound
Disclosed is a method for producing an amide compound represented by the formula (3) below and having an excellent control activity against a harmful arthropod, which is characterized in that an aniline compound represented by the formula (1) below and an aldehyde c...
02/21/2012
8115006Process for producing anthranilamide compound
To provide a process for producing a specific anthranilamide compound or its salt. To provide a process for producing an anthranilamide compound represented by the formula (I) or its salt: wherein each of R1a
02/14/2012
8101773Hydroxy methyl phenyl pyrazolyl urea compounds useful in the treatment of cancer
The compound 4-{4-[({3-tert-Butyl-1-[3-(hydroxymethyl)phenyl]-1H-pyrazol-5-yl}carbamoyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide and alternative forms thereof (e.g., salts, solvates, hydrates, prodrugs, polymorphs and metabolites); pharmaceutical compo...
01/24/2012
8071782Synthesis of 1,3,4-trisubstituted and 1,3,4,5-tetrasubstituted pyrazoles
This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins. ...
12/06/2011
7951953Conversion of 2-pyrazolines to pyrazoles using bromine
This invention relates to a method for preparing a compound of Formula 1 wherein L, R1, R2 and X are as defined in the disclosure, comprising contacting a 2 pyrazoline of Formula 2 with bromine at a temperature of at least about 80° C. (Formul...
05/31/2011
7919627Processes for the preparation of hydroxylamines
The present invention relates generally to novel methods for the synthesis of O-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acce...
04/05/2011
7855297Amide derivatives and medicinal use thereof
The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an opt...
12/21/2010
7834186Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates
A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(...
11/16/2010
7812170Insecticides
Compounds of the formula (I) in which Z, is an oxygen atom; or a sulfur atom; Z2 is an oxygen atom; or a sulfur atom; R, is an aryl or heteroaryl group, which is unsubstituted or substituted; R2 is hydrogen; or an organic substituent; R3
10/12/2010
7538225Processes for the preparation of o-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine
The present invention relates generally to novel methods for the synthesis of O-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acce...
05/26/2009
7442799Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates
A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II)wher...
10/28/2008
7442702Prostaglandin agonists
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 the treatmen...
10/28/2008
7414060Pyridine-2-carboxyamide derivatives
The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods...
08/19/2008
7414055Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven...
08/19/2008
7407972Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7396929Synthesis of 3-amino-4-substituted pyrazole derivatives
This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility. ...
07/08/2008
7396935Aryl-substituted pyrazole-amide compounds useful as kinase inhibitors
The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted pyridyl, ring; R2
07/08/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
73880184-Piridinylmethylsulphonamide derivatives as fungicidal plant protein agents
Sulfonamides of the formula I where the substituents are as follows: R1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R2, R3, R4, R5 are...
06/17/2008
7375232Ortho-heterocyclic substituted aryl amides for controlling invertebrate pests
Compounds of Formula I, their N-oxides and salts are disclosed wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring member...
05/20/2008
7354938Pyrazole compounds and uses related thereto
Substituted pyrazoles are provided that are useful for the treatment of, for example, diabetes, obesity and metabolic syndrome. ...
04/08/2008
7348342Heterocyclic compounds process for their preparation and pharmaceutical compositions containing them and their use in medicine
We describe substituted benzenesulfoximine compounds having anti-inflammatory activity, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of inflammatory diseases. ...
03/25/2008
7329670Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre...
02/12/2008
7312350Process for preparing arylalkynes
The invention relates to a process for preparing arylvinyl halides and sulphonates and arylalkynes by reacting haloaromatics or aryl sulphonates with vinyl halides or sulphonates in the presence of a palladium catalyst and a base and, if appropriate, subsequent elim...
12/25/2007
7309710Crystals
Obtaining the crystal of 4,6-dimethyl-4′-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]nicotinanilide having excellent activity of inhibiting Ca2+ release-activated Ca2+ channel and suppressing IL-2 production to find that the compound includes t...
12/18/2007
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
7288541Propylcarbamate derivatives as inhibitors of serine and cysteine proteases
The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors. The described invention also includes methods of making such ketone derivatives as well as methods of using the same in the treatment of disorders, including ...
10/30/2007
7285554Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta...
10/23/2007
72824694-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines
A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of the formula (I) and of their use as herbicides. In this formula (I), R1, R2, R3 and R
10/16/2007
7279476Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are...
10/09/2007
7279470Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may...
10/09/2007
7253170Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...
08/07/2007
7253187Heterocyclic inhibitors of ERK2 and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1...
08/07/2007
7247635Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta...
07/24/2007
7241758Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease...
07/10/2007
7238721Pyrazole compounds for treatment of neurodegenerative disorders
The invention provides compounds of Formula I: wherein R1, R2, R3, R4, R6, R7, R8, and A are as defined. Compounds of formula I have ac...
07/03/2007
7232836Arthropodicidal anthranilamides
This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b
06/19/2007
RE396811-(4-sulfamyaryl)-3-substituted-5-aryl-2-pyrazolines and inhibitors of cyclooxygenase-2
Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C1-C6 alkyl, and a group of formula II: ...
06/05/2007
7227025Substituted dihydro 3-halo-1H-pyrazole-T-carboxylates, their preparation and use
This invention relates to a compound of Formula I, a method for its preparation and its use in the preparation of a compound of Formula II wherein R1, R2, R3, X and n are as defin...
06/05/2007
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