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Class 548/543 - Chalcogen bonded directly to a ring carbon of the five-membered hetero ring which is adjacent to the ring nitrogen (e.g., 2-pyrrolidones, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of applications: 99
Last issue date: 05/24/2012


1      
Application No.Application TitleIssue Date
20120129833CYCLIC KETOENOLS FOR THERAPY
The invention relates to 5′-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders o...
05/24/2012
20120083500OXAZOLONE AND PYRROLIDINONE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X 2/3 ANTAGONISTS
Compounds of the formula I:

or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defi...

04/05/2012
20120041212PROCESS FOR THE PREPARATION OF PREGABALIN
The present invention provides a new enantioselective method of preparing (S)-3-(aminomethyl)-5-methylhexanoic acid, commonly known as pregabalin. The invention also provides new chiral intermediates useful in the production of pregabalin....
02/16/2012
20110290418HYDROGEN PEROXIDE COMPLEXES AND THEIR USE IN THE CURE SYSTEM OF ANAEROBIC ADHESIVES
Provided is a complex of hydrogen peroxide and at least one compound represented by Formula I:

wherein X is:

—C(R3)3, —C...

12/01/2011
20110245223HETEROCYCLIC COMPOUNDS
The present invention provides a compound represented by the following formula [1′] or a salt thereof:

wherein ring A, R2, R3, R4 and X are as defined in the description, an...

10/06/2011
20110245444TRANSFORMATION OF BIOMASS
A method for processing biomass comprising heating an aqueous slurry comprising biomass, water and a phosphate catalyst in a pressure vessel at a temperature of about 150° C. to about 500° C. to produce a mixture comprising a dispersion of an organic phase and an aque...
10/06/2011
20110218214Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insul...
09/08/2011
20110213146Transition Metal-Catalyzed C-H Amination Using Unactivated Amines
One aspect of the invention relates to a method of animation or amidation, comprising the step of combining a substrate, comprising a reactive C—H bond, and an amine or amide, comprising a reactive N—H bond, in the presence of an oxidizing agent and a metal-containi...
09/01/2011
20110098302CYCLIC DIARYL ETHER COMPOUNDS AS ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of P...
04/28/2011
20110021779PROCESS FOR THE PREPARATION OF 6-SUBSTITUTED-1-(2H)-ISOQUINOLINONES
The present invention relates to a process for making 6-substituted-1-(2H)-isoquinolinone derivatives of formula (I)

wherein R1 and n are as described in the specification. The present invention further relat...

01/27/2011
20100311794CYCLOALKYLCARBAMATE BENZAMIDE ANILINE HDAC INHIBITOR COMPOUNDS
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

...

12/09/2010
20100286204COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE
There is provided a compound having Formula I

wherein

  • each of R1, R2, R3, R4, R5, ...
11/11/2010
20100234365COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1)....
09/16/2010
20100222581NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
There is provided a series of substituted isophthalates of formula (I)

or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as de...

09/02/2010
20100222326New Heterocyclic Derivatives Useful For The Treatment of CNS Disorders
The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals....
09/02/2010
20100184764CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as we...
07/22/2010
20100168189THERAPEUTIC SUBSTITUTED LACTAMS
Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein....
07/01/2010
20100113460Organic Compounds
Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them....
05/06/2010
20100113801Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof,

wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the pre...

05/06/2010
20100087506CYCLIC AMINE COMPOUND
Provision of a compound having a superior androgen receptor regulating action.

A compound represented by the formula (I)

wherein R1 is a hydrogen atom, a halogen atom,...

04/08/2010
20100069630NAPHTHALENYLOXYPROPENYL DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST HISTONE DEACETYLASE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation....
03/18/2010
20100035948Furanone compounds and lactam analogues thereof
The present invention provides a compound of formula I and a compound of formula II, methods of use and formulations thereof.

...

02/11/2010
20090326240Iron-Copper Co-Catalyzed Process for Carbon-Carbon or Carbon-Heteroatom Bonding
The present invention relates to a process for creating a Carbon-Carbon bond (C—C) or a Carbon-Heteroatom bond (C—HE) by reacting a compound carrying a leaving group with a nucleophilic compound carrying a carbon atom or a heteroatom (HE) that can substitute for the...
12/31/2009
200903187082-Oxo-1-Pyrrolidine Derivatives, Processes For Preparing Them And Their Uses
The present invention relates to optically enriched or substantially optically pure 4-substituted-pyrrolidin-2-ones of formula (III), and their uses for the synthesis of 2-oxo-pyrrolidin-1-yl derivatives.

...

12/24/2009
20090264650Prophylactic/Therapeutic Agent for Diabetes
The present invention relates to a 11β-hydroxysteroid dehydrogenase 1 inhibitor comprising a compound represented by the formula (1):

wherein each symbol is as defined in the description,
or a salt the...

10/22/2009
20090239911CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as we...
09/24/2009
20090215736CASPASE INHIBITORS AND USES THEREOF
This invention provides caspase inhibitors of formula I:

wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; 08/27/2009

20090176799PHOSPHODIESTERASE 4 INHIBITORS
Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the...
07/09/2009
20090099182INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I:

having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharma...

04/16/2009
20090088579Production Method of N-Vinyl-2-Pyrrolidone
High-purity NVP can be produced by comprising at least two crystallization processes and supplying the mother liquor from the first crystallization process to the second crystallization process.

Further, high-purity NVP can be obtained cont...

04/02/2009
20090012144Optically active 2,5-bisaryl-delta¹ -pyrrolines and their use as pest control agents
Novel optically active Δ1-pyrrolines of the formula (I)

in which

  • R1, R2, R3, R4, ...
01/08/2009
20080312432Stabilizers for Use in Nvp Synthesis
A process for preparing N-alkenyl compounds by reacting the corresponding NH compounds with alkynes in the liquid phase in the presence of a catalyst, wherein the reaction is carried out in the presence of at least one stabilizer, and the use of stabilizers for increasi...
12/18/2008
20080287522BENZYLATED PDE4 INHIBITORS
The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for ...
11/20/2008
20080287516Phenyl-Substituted Pyrrolidones
The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, method...
11/20/2008
20080275043Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as we...
11/06/2008
20080255136PYRROLIDONES WITH ANTI-HIV ACTIVITY
The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a ce...
10/16/2008
20080214836Process for the synthesis of lauryllactam (L12) by gas phase catalytic rearrangement of cyclododecanone oxime
The present invention relates to a process for the preparation of lauryllactam in which a Beckmann rearrangement of cyclododecanone oxime is carried out. Said process is carried out in the gas phase at a temperature of between 180 and 450° C. in the presence of a micro...
09/04/2008
20080214621Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmace...
09/04/2008
20080207686Peptide Deformylase (Pdf) Inhibitors 4
The present invention relates to compounds of formula (I).

These compounds are a novel type of peptide deformylase (PDF) inhibitors, and are therefore of great interest especially as new antibiotics....

08/28/2008
20080188520Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them
The invention relates to compounds of formula I

in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredient...

08/07/2008
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