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Class 540/363 - Nitrogen bonded directly at the 3-position of the hetero ring


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen is bonded directly at the 3-position
No. of patents: 97
Last issue date: 09/11/2007


1      
NumberTitleIssue Date
7268125β-lactamyl vasopressin V antagonists
Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor
09/11/2007
7179907Antibiotic compounds
The present invention provides methods for identifying (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity. The method involves the selection of RNA biocatalysts that promote the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid deriv...
02/20/2007
7144696Use of azetidinone compounds
The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or cholesteryl esters in biological systems is presented. These compounds can...
12/05/2006
7119083β-Lactamyl vasopressin VAntagonists
Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor. ...
10/10/2006
7067509Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure:
06/27/2006
7067532Substituted quinolines as antitumor agents
The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) a...
06/27/2006
6900312Thiazole-substituted β-lactams
The present discovery consists in new thiazole-substituted β-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen...
05/31/2005
6602864Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit...
08/05/2003
6579989Sulphostin analogue and process for producing sulphostin and its analogue
A sulphostin analogue represented by the general formula, ##STR1## wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable sa...
06/17/2003
6562962Preparation of substituted isoserine esters using metal alkoxides and ଲ-lactams
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a ଲ-lactam....
05/13/2003
6509463Isocyanoalkylcarbonic acid derivatives, the reaction thereof in isocyanide multicomponent reactions to form sec-amido-alkylcarbonic acid derivatives, and those sec-amidoalkyl-carbonic acid derivatives
The present invention relates to compounds of the general formula I ##STR1## wherein A is a group of the formula ##STR2## and Z is an O or S atom, to the further processing thereof to form novel sec-amidoalkylcarbonic acid derivatives and to those se...
01/21/2003
6281227Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit...
08/28/2001
6127543Antimalarial organometallic iron complexes
Organometallic iron complexes containing one or more basic structural components characterizing a molecule with antimalarial properties such as quinine, chloroquinine or mepacrine, as well as one or more iron atoms are described. The complexes of the inve...
10/03/2000
6031094Beta-lactam substrates and uses thereof
02/29/2000
6011151Process for preparing ଲ-lactam halide compound
A process for preparing a ଲ-lactam halide compound represented by the formula (2) characterized by halogenating the allenyl group of an allenyl ଲ-lactam compound represented by the formula (1) with a cupric halide and a metal halide to obtain ...
01/04/2000
5728827Process for the synthesis of azetidinones
This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the rin...
03/17/1998
57081695-amidomethyl ଱,ଲ-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents
The present invention provides for new 5-amidomethyl, ଱,ଲ-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substi...
01/13/1998
5561227Process for the stereospecific synthesis of azetidinones
This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R2 --D--CH2 CO...
10/01/1996
5539103ଲ-lactams as taxol intermediates N-acylated
ଲ-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters....
07/23/1996
5482920Triazinyl compounds with herbicidal activity
Pyrimidinyloxy- and triazinyloxy- and pyrimidinylthio- and triazinylthio-butyric acid derivatives of formula I ##STR1## wherein Q is ##STR2## A is hydroxy or a group ##STR3## and the other substituents are as described in patent claim ...
01/09/1996
5334328Chiral azetidinone derivatives, and their use as dopes in liquid-crystal mixtures
Azetidinones of the formula I ##STR1## in which, for example, R1 is an alkyl or alkenyl radical, R2 and R3 are hydrogen or an alkyl or alkenyl radical, Z is hydrogen or (pseudo)halogen, A1, A2 an...
08/02/1994
5250676Process for the preparation of 3-substituted-2-azetidinones
Provided is a process for diastereoselectively preparing compounds of the formula ##STR1## which includes the step of subjecting a compound of the formula ##STR2## to a salt whose anion is a nucleophilic base whose conjugate acid has a pKa ...
10/05/1993
5239069Amino protecting group
The invention provides compounds of the formula ##STR1## wherein R* is a group of the formula ##STR2## wherein R and R0 are individually C1 -C6 alkyl groups or together form a ring consisting of the nitrogen atom...
08/24/1993
5229381Substituted azetidinones as anti-inflammatory and antidegenerative agents
New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1##...
07/20/1993
5194604Process and intermediates for beta-lactams having aminothiazole(iminooxyacetic acid)acetic acid sidechains
Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as def...
03/16/1993
5169945Amino protecting group
The present invention provides a process for protecting an amino group in a compound exposed to nucleophilic reaction conditions in which the imido group used for protection is reacted with a secondary amine to form an acyl group which protects the amino ...
12/08/1992
5137884N-tetrazolyl beta-lactams
N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; and Z is ##STR2## and W is ...
08/11/1992
5106475Process for preparing 4-substituted azetidinones
A process for preparing 3-4-cis-ଲ,ଲ-(4)-substituted and 3-4-trans,ଲ,଱-(4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones....
04/21/1992
5106977Intermediates for a process for making 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines
Novel intermediates for preparing 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines are disclosed. These intermediates have the formula ##STR1## wherein Prot is as defined herein....
04/21/1992
50379836,7-dihydroxyquinoxalines as intermediates to beta-lactam antibiotics
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activiy, and intermediates to compounds of formula I having the formula ##STR2##...
08/06/1991
5028711Novel benzopyran derivatives, processes for their preparation and their use and preparations containing the compounds
Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds....
07/02/1991
5015737Therapeutically useful beta-lactams
This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R1 and R2 are the same or different and are hydrogen (C1 -C12) alkyl, (C2 -C8) alkenyl, (C2 ...
05/14/1991
5006650Novel N-1 substituted beta-lactams as antibiotics
This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R10 and R15 are the same or different and are (a) hydrogen, (b) (C1 -C12) alkyl, (c) (C2 -C8) alkenyl, ...
04/09/1991
5001235Antibiotic beta-lactams containing a pyridone carboxylic acid or acid derivative
This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R80 is --CO2 R5 or --CONR6 R7 ; wherein R5 is hydrogen or (C1 -C4) alkyl; and whe...
03/19/1991
4992545Process for preparing 4-substituted azetidinones
A process for preparing 3-4-cis-ଲ,ଲ-(4)-substituted and 3-4-trans,ଲ,଱- (4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones....
02/12/1991
4983732Method of deprotection of 3-amino azetidinones
A method for preparing 2-amino-ଲ-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-ଲ-lactam is further acylated with a different acyl group and is subsequently treated ...
01/08/1991
4980465Process for making 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl)] azetidines and intermediates used therein
An improved process for making compounds having the formula ##STR1## includes subjecting an intermediate of the formula ##STR2## to hydrogenolysis in the presence of a ketonic solvent so as to simultaneously remove both Z-protecting groups from ...
12/25/1990
4975538Antibiotic sulfonylaminocarbonyl activated beta-lactams
This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula ##STR1## wherein R401 and R402 are the same or different and are (a) ...
12/04/1990
49594702-oxo-[[(substituted sulfonyl)-amino]carbonyl]-azetidines
Componds having the formula ##STR1## and pharmaceutically acceptable salts thereof, exhibit antibacterial activity wherein R is ##STR2##...
09/25/1990
4923983Method of resolving cis 3-amino-4-[2-(2-furyl)eth-1-yl]-1-methoxycarbonylmethyl-azetidin-2-one
Cis ଱଱/ଲଲ-3-amino-[2-(2-furyl)eth-1-yl]-1-methoxycarbony lmethyl-azetidin-2-one is resolved via optically active tartaric acid....
05/08/1990
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