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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 548/494 - Having -C(=X)-, wherein X is chalcogen, attached indirectly to ring carbon of the five-membered hetero ring by an acyclic carbon or acyclic carbon chain (e.g., indole-3-acetic acid, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a group, in which X is chalcogen (i.e.,
No. of patents: 236
Last issue date: 04/24/2012


1            
NumberTitleIssue Date
8163936Treatment of CRTH2-mediated diseases and conditions
The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2. ...
04/24/2012
8143426IAP inhibitors
Smac mimetics that inhibit IAPs. ...
03/27/2012
8022230Dimeric IAP inhibitors
Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid...
09/20/2011
7939674Process for producing an aromatic unsaturated compound
The present invention provides a process for producing an aromatic unsaturated compound of the formula (4) wherein Ar represents an optionally substituted aromatic group or an optionally substituted heteroaromatic group, an...
05/10/2011
7868187Processes of producing glutamic acid compounds and production intermediates therefore and novel intermediate for the processes
The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products. ...
01/11/2011
7816541Process for producing an optically active compound
The present invention provides a process for selectively producing an enantiomer at position 4 of an optically active compound in the cross aldol reaction of pyruvic acid and indole-3-pyruvic acid. The process comprises the step of reacting pyruvic acid with indole-...
10/19/2010
7795451Polymorphic forms of fluvastatin sodium and process for preparing the same
Disclosed herein are novel polymorphic forms of Fluvastatin sodium, wherein said polymorphic forms are designated as JF, JF1, JF2, JF3 and are characterized by their powder X-ray diffraction patterns, Infrared absorption s...
09/14/2010
7687642Fluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them
Provided are crystalline forms of fluvastatin sodium and processes for their preparation. ...
03/30/2010
7432380Crystalline form of Fluvastatin sodium
A novel crystalline form of Fluvastatin sodium hydrate is described, referred to hereinafter as polymorphic Form G. Furthermore, processes for the preparation of this crystalline form and pharmaceutical compositions comprising this crystalline form are reported....
10/07/2008
7414140Fluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them
Provided are polymorphic forms of fluvastatin sodium and processes for their preparation. ...
08/19/2008
7368468Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them
Provided are polymorphic forms of fluvastatin sodium and processes for their preparation. ...
05/06/2008
7368581Process for the preparation of fluvastatin sodium crystal from XIV
Provided is a process for preparing a polymorphic form of fluvastatin sodium, particularly Form XIV. ...
05/06/2008
7368471Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, ...
05/06/2008
73650612-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia...
04/29/2008
7365091Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful fo...
04/29/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7351726Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
04/01/2008
7348351Substituted 3-alkyl and 3-arylalkyl -indol-1yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure ...
03/25/2008
7348354Cyclohexylurea compounds
Cyclohexylurea compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and the use of such compounds as pharmaceutically active agents with nociceptin/ORL1 receptor sys...
03/25/2008
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
7332521Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them. ...
02/19/2008
7317035Tetracyclic arylcarbonyl indoles having serotonin receptor affinity useful as therapeutic agents, process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel tetracyclic arylcarbonyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel int...
01/08/2008
7297800Process of producing glutamate derivatives
The present invention relates to a process for producing efficiently glutamic acid derivatives (including salts thereof) such as monatin by converting a substituted α-keto acid of formula (1) into a glutamic acid derivative of formula (2) in the presence of an enzy...
11/20/2007
7288553Indole derivatives as selective androgen receptor modulator (SARMS)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ...
10/30/2007
7268159Substituted indoles
The present invention relates generally to substituted indoles and methods of using them. ...
09/11/2007
7265148Substituted pyrrole-indoles
The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them. ...
09/04/2007
7259182Aryl, aryloxy, and aklyloxy substituted 1-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor ...
08/21/2007
7241800Anhydrous amorphous form of fluvastatin sodium
The present invention relates to novel anhydrous amorphous forms of bis[(E)[4-(4-fluorophenyl)isopropyl[methyl(methylsulfonyl)amino]pyrimidinyl](3R,5S)-3,5-dihydroxyhept enoic acid]calcium salt (rosuvastatin calcium), (±)7-(3-(4-fluorophenyl)-1-(1-methylethyl)-1H-i...
07/10/2007
7208491N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as c...
04/24/2007
7202268Derivatives of indole-3-carboxamide, preparation method thereof and application of same in therapeutics
The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3–C10 alkyl, a C5–C10 carbocyclic radi...
04/10/2007
7202266PPAR active compounds
Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile. ...
04/10/2007
7186749Pyrrolo-naphthyl acids and methods for using them
The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders. ...
03/06/2007
7163954Substituted naphthyl benzothiophene acids
The present invention relates generally to substituted naphthyl benzothiophene acids and methods of using them. ...
01/16/2007
7141592Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
11/28/2006
7129238Mandelic acid derivatives
The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acc...
10/31/2006
7101903Substituted dihydropyrano indole-3,4-dione derivatives as inhibitiors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, pheny...
09/05/2006
7078425Preparation of phosphatase inhibitors
Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R1, R2, R3, and R4 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitor...
07/18/2006
7078429Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful a...
07/18/2006
7074817Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridi...
07/11/2006
7075582Methods for identifying and using MarR family polypeptide binding compounds
Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides. ...
07/11/2006
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