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Class 544/137 - The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atoms


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring contains
No. of patents: 294
Last issue date: 05/29/2012


1                
NumberTitleIssue Date
8188270Polymorphous form of 5-chloro-N-({(5S)-2-oxo-3[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide
The present invention relates to a novel polymorphic form and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene-carboxamide, processes for their preparation, medicaments comprising these forms, ...
05/29/2012
8106192Method for producing 5-chloro--({(5)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
The invention relates to a method for producing 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3-amino-propane-1,2-diol and 4-(4-aminophenyl)-3-m...
01/31/2012
7989618Linezolid crystalline hydrate form and linezolid salts
Linezolid salts, useful as such and as intermediates in a process for the preparation of novel and known crystalline linezolid forms, in particular known as Form III. ...
08/02/2011
7741480Process for the preparation of linezolid and related compounds
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-4-morpholinyl aniline ...
06/22/2010
7732597Crystalline form of linezolid
The present invention relates to a novel crystalline form of linezolid, to processes for its preparation and to a pharmaceutical composition containing it. ...
06/08/2010
7718799Crystalline form of linezolid
The present invention relates to a novel crystalline form of linezolid, to processes for its preparation and to a pharmaceutical composition containing it. ...
05/18/2010
7718800Crystalline form of linezolid
The present invention relates to a novel crystalline form of linezolid, to processes for its preparation and to a pharmaceutical composition containing it. ...
05/18/2010
7714128Crystalline form of linezolid
The present invention relates to a novel crystalline form of linezolid, to processes for its preparation and to a pharmaceutical composition containing it. ...
05/11/2010
7524954Process for the preparation of linezolid and related compounds
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-4-morpholinyl aniline ...
04/28/2009
7485722Spiro-oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators
Compounds in accord with Formula I: wherein R1, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation...
02/03/2009
7429588Crystalline isoxazole derivative and medical preparation thereof
Crystalline 3-[(1S)-1-(2-fluorobiphenyl-4-yl)ethyl]-5-{[amino(morpholin-4-yl)methylene]amino}-isoxazole that exhibits the following angle of diffraction (2θ) and relative intensity in a powder X-ray diffraction pattern, is very easy to handle and stable in a proces...
09/30/2008
74255613-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The ar...
09/16/2008
7371755Antiviral agents
This invention relates to a compound capable of binding to a picornavirus capsid comprising two or more capsid binding moieties. ...
05/13/2008
7354919Isoxazole compositions useful as inhibitors of ERK
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo...
04/08/2008
7351824Process for the preparation of linezolid and related compounds
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-...
04/01/2008
7351823Preparation process
The present invention relates to a process for preparing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide starting from 2-[(2S)-2-oxiranylmethyl]-1H-isoindole-1,3(2H)-dione, 4-(4-aminophenyl)-3-morpholinone...
04/01/2008
7348427Antipathogenic benzamide compounds
Antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein. ...
03/25/2008
7335653Bis-aryl sulfonamides
Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls i...
02/26/2008
7314872Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides m...
01/01/2008
7307163Process for the preparation of linezolid and related compounds
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-4-morpholinyl aniline with R-epichl...
12/11/2007
7304050Antibacterial agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I a...
12/04/2007
7282501Modulators of peroxisome proliferator activated receptors (PPAR)
The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hyperte...
10/16/2007
7265103Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o...
09/04/2007
7238689Isoxazoline derivative and herbicide comprising the same as active ingredient
An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; R
07/03/2007
7229987Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obes...
06/12/2007
7226991Phenylalanine derivatives
Disclosed herein are phenylalanine derivative compounds of the following formula W—Y—(AA)n—Z wherein Y is a phenylalanyl radical, AA is an amino acid, n is an integer of 1 to 15, and substituent variables W and Z are as described...
06/05/2007
71897121,3-Oxazole compounds for the treatment of cancer
Oxazole derivatives, which are useful as VEGFR2, CDK2, and CDK4 inhibitors are described herein. The described invention also includes methods of making such oxazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
03/13/2007
7186844Method for producing cyclic carbamate ester
A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two hydrogen atoms on a nitrogen atom, and carbon dioxide. ...
03/06/2007
7183276Azole compounds
The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocycl...
02/27/2007
7173129Sulfonamide-substituted chalcone derivatives and their use to treat diseases
The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the ...
02/06/2007
7153880Substituted diphenyl heterocycles useful for treating HCV infection
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
12/26/2006
7144903CCR4 antagonists
Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds ...
12/05/2006
7141570N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formula I described herein. ...
11/28/2006
7141588N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formulae I, II, and III described herein. ...
11/28/2006
7129259Halogenated biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having at least one halogenated hydrocarbon moiety, a biaryl moiet...
10/31/2006
7128928Ophthalmic formulation with novel gum composition
There is provided a pharmaceutical composition suitable for topical administration to an eye, the composition comprising (a) a pharmacologically effective concentration of an active agent and (b) a combination of at least two ophthalmically compatible polymers compr...
10/31/2006
7125865Therapeutic compounds for treating dyslipidemic conditions
The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
10/24/2006
7115642Substituted diphenyl isoxazoles, pyrazoles and oxadiazoles useful for treating HCV infection
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
10/03/2006
7112670Crystal form
The present invention involves a novel crystal form of 17β-hydroxy-7α-(5′-methyl-2′-furyl)-pregna-4,9(11)-dien-3-one-21-carboxylic acid, γ-lactone, having the formula which is an intermediate useful in pre...
09/26/2006
7102000Heterocyclic amide derivatives for the treatment of diabetes and other diseases
The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Ar5 form a ring containing at least one amide residue, and W, X, Y and Z t...
09/05/2006
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