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8048874 |
Beta-lactamyl phenylalanine, cysteine, and serine vasopressin antagonists
Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described...
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7550453 |
2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof
The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
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7501404 |
Substituted azetidinones
Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor X...
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7268125 |
β-lactamyl vasopressin V1a 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...
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7179907 |
Antibiotic 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...
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7067532 |
Substituted 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...
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6900312 |
Thiazole-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 ...
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6602864 |
Sulfonic 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...
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6579989 |
Sulphostin analogue and process for producing sulphostin and its analogue
A sulphostin analogue represented by the general formula, 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,...
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6562962 |
Preparation of substituted isoserine esters using metal alkoxides and β-lactams
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a β-lactam.
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6509463 |
Isocyanoalkylcarbonic 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 wherein A is a group of the formula and Z is an O or S atom, to the further processing thereof to form novel...
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6127543 |
Antimalarial 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...
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6031094 |
Beta-lactam substrates and uses thereof
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6011151 |
Process for preparing β-lactam halide compound
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5708169 |
5-amidomethyl α,β-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents
The present invention provides for new 5-amidomethyl, α,β-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, f...
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5539103 |
β-lactams as taxol intermediates N-acylated
β-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters.
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5482920 |
Triazinyl 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...
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5334328 |
Chiral 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 and...
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5250676 |
Process 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...
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5194604 |
Process 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...
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5137884 |
N-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...
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5106475 |
Process for preparing 4-substituted azetidinones
A process for preparing 3-4-cis-β,β-(4)-substituted and 3-4-trans,β,α-(4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones.
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5106977 |
Intermediates 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.
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5037983 |
6,7-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##
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5015737 |
Therapeutically 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 -C8) alkynyl, (C3...
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5006650 |
Novel 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, (d) (C2...
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5001235 |
Antibiotic 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 wherein R6 and R7 are the same or...
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4992545 |
Process for preparing 4-substituted azetidinones
A process for preparing 3-4-cis-β,β-(4)-substituted and 3-4-trans,β,α- (4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones.
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4983732 |
Method of deprotection of 3-amino azetidinones
A method for preparing 2-amino-β-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-β-lactam is further acylated with a d...
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4980465 |
Process 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...
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4975538 |
Antibiotic 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...
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4959470 |
2-oxo-[[(substituted sulfonyl)-amino]carbonyl]-azetidines
Componds having the formula ##STR1## and pharmaceutically acceptable salts thereof, exhibit antibacterial activity wherein R is ##STR2##
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4923983 |
Method of resolving cis 3-amino-4-[2-(2-furyl)eth-1-yl]-1-methoxycarbonylmethyl-azetidin-2-one
Cis αα/ββ-3-amino-[2-(2-furyl)eth-1-yl]-1-methoxycarbony lmethyl-azetidin-2-one is resolved via optically active tartaric acid.
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4912214 |
Isothiazolyl beta-lactam antibacterial agents
Compounds of the formula ##STR1## wherein A is ##STR2## in which R1 is acyl, R2 is hydrogen, lower alkyl, lower alkoxy-carbonyl or aminocarbonyl, R3 is hydrogen or lower alkyl, R4 and R4, are each...
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4904775 |
Heteroaroylhydrazide derivatives of monocyclic beta-lactam antibiotics
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activity, and intermediates to compounds of formula I having the formula
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4889930 |
Process for making 2-oxo-1-((substituted sulfonyl)amino)carbonzyl)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...
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4871841 |
2-Oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines
Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1## wherein R4 is ##STR2## wherein A1 is...
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4834846 |
Process for deblocking N-substituted β-lactams
This invention relates to a process for preparing β-lactams by electrochemically deblocking N-substituting β-lactams using anodic oxidation.
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4831130 |
β-lactam antibacterial agents
Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R1, is acyl, R2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R3 is hydrogen or lower alkyl...
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4820815 |
Azetidinone N-phosphonomethyl esters
The invention provides azetidinones of the formula ##STR1## where R4 is hydrogen, amino or protected amino; R0 is H when R4 is amino or protected amino, or C1 -C4 alkyl when R4 is H; R1 is H, CH3,...
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4808579 |
Novel monocycle β-lactam antibacterials
The disclosure describes (S)-3-[2-(2-amino-4-thiazolyl)]-(Z)-2-methoxyiminoacetylamin
o-2-oxo-1-azet idinyliminoacetic acid and...
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4801705 |
2-oxo-1-(((substituted sulfonyl)amino)-carbonyl)azetidines
Antibacterial activity is exhibited by β-lactams having a 3-acylamino substituent and having in the 1-position an activating group of the formula ##STR1## wherein R is
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4777252 |
2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines
Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula ##STR1## wherein R is ##STR2## and R4 is ##STR3##
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4751299 |
Optically active β-lactams and method of their production
Optically active β-lactams of the general formula ##STR1## wherein R1 is an amino or protected amino group, R2 is an organic residue bonding through a carbon atom thereof and R3 is the residue ...
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4723002 |
1-(substituted phosphorous)-azetidinone antibacterials
Antibacterial activity is exhibited by 2-azetidinones having an acylamino substituent in the 3-position and having an activating group in the 1-position of the formula ##STR1##
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4719207 |
CNS active substituted azetidinone compounds
Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R1 and R2 represents a substituted lower alkyl group, an azido group, an amino group, a lower...
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4704385 |
3-formamido azetidinone antibacterial agents, their preparation and use
A monocyclic β-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO3 H; --PO(OH)Y wherein Y is ...
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4683303 |
Reduction process for the preparation of 4-unsubstituted azetidin-2-ones
Novel process for the preparation of azetidin-2-ones of the formula ##STR1## wherein R1 and R2 independently from each other are hydrogen, or an organic group linked to the ring carbon via a carbon...
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4680391 |
Substituted azetidinones as anti-inflammatory and antidegenerative agents
New substituted azetidinones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
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4678782 |
3S-formamido azetidinone antibacterial agents, their preparation and use
A monocyclic β-lactam antibiotic having a formamido substitutent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO3 H; --PO(OH)Y wherein Y is ...
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