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Class 548/550 - Nitrogen attached directly or indirectly to the five-membered hetero ring by acyclic nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached to the five-membered
No. of patents: 329
Last issue date: 03/20/2012


1                  
NumberTitleIssue Date
8138354N-substituted pyrrolidonium ionic liquids
This invention relates to compounds useful as ionic liquids that are based on an N-substituted pyrrolidinone and incorporate a pendant ammonium cation that is spaced from the pyrrolidone ring by a variable length linker, which compounds may be represented by the str...
03/20/2012
8119818Functionalized N-substituted pyrrolidonium ionic liquids
This invention relates to compounds useful as ionic liquids that are based on an N-substituted pyrrolidinone and incorporate a pendant ammonium cation that is spaced from the pyrrolidone ring by a variable length linker. ...
02/21/2012
8049019Substituted pyrrolidine-2-one compounds
The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically accept...
11/01/2011
7754898Method of enantioselective nucleophilic addition reaction of enamide to imine and synthesis method of α-amino-γ-keto acid ester
An asymmetric synthesis of amino acid compound that is useful as a starting material or synthetic intermediate for production of medicinal products, agrichemicals, perfumes, functional polymers, etc. There is provided a method of enanthio-selective nucleophilic addi...
07/13/2010
7612215Process for preparing 2-oxo-1-pyrrolidine derivatives by intramolecular allylation
The present invention relates to a new process for preparing 2-oxo-1-pyrrolidine derivatives of general formula (I), comprising the cyclisation of an intermediate of general formula (II) wherein the substituents are as defined in the specification.
11/03/2009
7560572Production and use of derivatized homoserine lactones
The present invention provides analogues of autoinducer molecules that are derivatized to allow their attachment to other molecules and surfaces. Libraries of the autoinducer analogues are also contemplated. Also provided are methods for using the compounds of the i...
07/14/2009
7501528Method for preparing enantiomerically pure 4-pyrrolidino phenylbenzyl ether derivatives
The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are...
03/10/2009
7485731Method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives
The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are...
02/03/2009
7396846Growth hormone secretagogues
This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in thes...
07/08/2008
7338975Lactams as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
03/04/2008
7304088Protease inhibitors
This invention relates to treating an infection with a virus using protease inhibitors. Examples of the protease inhibitors include compounds of formula (I). Each variable is defined in the specification ...
12/04/2007
7291746Process for obtaining an antiepileptic agent
A process for obtaining the pharmaceutical active ingredient, levetiracetam, by means of deaminomethylation of a sufficiently pure enantiomer intermediate (S)-(II), or by means of deaminomethylation of an addition salt thereof with an acid, wherein R1 and...
11/06/2007
7291620N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also direct...
11/06/2007
7279582Retroviral protease inhibiting compounds
A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed. ...
10/09/2007
7244747Imidazole derivatives, processes for preparing them and their uses
The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. ...
07/17/2007
72355814-pyrrolidino-phenyl-benzyl ether derivatives
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoam...
06/26/2007
72178262-oxo-1-pyrrolidine derivatives, process for preparing them and their uses
The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing α-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particula...
05/15/2007
7214803Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence,...
05/08/2007
7199242Processes for the production of amino-protected derivatives of 4-aminomethylene-pyrrolidin-3-one and/or 4-aminomethylene-pyrrolidin-3-alkoxyimino derivatives and/or gemifloxacin or a salt thereof
The invention provides a process for the production of a compound of formula (I): wherein P1 and P2, which may be the same or different, are amino protecting groups, which comprises protection of a compound of formula (II) in solution phase con...
04/03/2007
7196113Lactam tachykinin receptor antagonists
The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these ...
03/27/2007
71798352-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors
The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.
02/20/2007
71511114-pyrrolidino-phenyl-benzyl ether derivatives
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine...
12/19/2006
7132552Process for producing levetiracetam
The invention relates to a method of making optically and chemically pure levetiracetam and to the levetiracetam produced by such process. ...
11/07/2006
7122682Oxopyrrolidine compounds, preparation of said compounds and their use in the manufacturing of levetiracetam and analogues
The present invention relates to an improved process for the preparation of (S)-(−)-α-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof. The invention also relates to compounds of the general formula (6) wherein R1 is methyl or ethyl; and R
10/17/2006
70379354-Pyrrolidino-phenyl-benzyl ether derivatives
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated b...
05/02/2006
7038061Crystalline anhydrous and monohydrate benzoate salts of (2′S,3S)-3-hydroxy-N-(2-[N-methyl-N-4-(N-propylamino-carbonyl)phenyl]amino-2-phenyl)-ethylpyrrolidine
A process for preparing an anhydrous benzoate salt in crystalline form having the formula I: and the corresponding benzoate monohydrate in crystalline form. The benzoate salts and pharmaceutical compositions thereof are...
05/02/2006
7001905Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are us...
02/21/2006
6992103Benzamide derivatives, processes for their preparation, and their pharmaceutical use
The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevat...
01/31/2006
6989384Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical ...
01/24/2006
6977303Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence,...
12/20/2005
69697702-oxo-1-pyrrolidine derivatives, process for preparing them and their uses
The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing α-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particula...
11/29/2005
6965019Mono-and bis-hydrazone pigments
Mono- and Bis-Azo/Hydrazone Pyrrole Pigments and Methods for preparing same. ...
11/15/2005
6962942Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having F...
11/08/2005
69060978-azaprostaglandin analogs as agents for lowering intraocular pressure
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
06/14/2005
6900213Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV ...
05/31/2005
6897323Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence,...
05/24/2005
6897233Peptide deformylase inhibitors
PDF inhibitors and novel methods for their use are provided. ...
05/24/2005
6872745Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutica...
03/29/2005
68587402-oxo-1-pyrrolidine derivatives, process for preparing them and their uses
The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing α-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particula...
02/22/2005
6849639Integrin inhibitors and their methods of use
The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a αvβ3, α
02/01/2005
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