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5656624 |
4-[(heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinones useful as hypolipidemic agents
4-[(Heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: A is optionally...
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5627283 |
Amidinophenylalanine derivatives, a process for the preparation thereof, use thereof and agents containing these as anticoagulants
Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
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5627176 |
Substituted azetidinone compounds useful as hypocholesterolemic agents
Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar 1 is R 3 -substituted aryl; Ar 2 is R 4 -substituted...
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5580976 |
Preparation of β-lactam compounds, and intermediates therefor
A process for preparing a β-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R 1 is hydrogen,...
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5574152 |
4-(1,1-dialkoxycarbonylalkyl) azetidin-2-one derivative and process for producing 4-(1-carboxyalkyl) azetidin-2-one derivative using the same
A process for preferentially producing a 4-(1-carboxyalkyl) azetidin-2-one derivative represented by formula (IIβ): ##STR1## wherein R 3 represents a lower alkyl group and R 4 represents a...
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5571913 |
Process for preparing a lactam
The invention relates to a process for preparing a lactam from an alicyclic ketoxime in the presence of a lactim-O-sulphonic acid and a solvent, the reaction being carried out in the presence of an...
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5563264 |
Preparation of βlactam compounds
A process for preparing a β-lactam compound of the formula (I): ##STR1## which comprises cyclization, in the presence of a catalyst, of an azetidinone derivative of the formula: ##STR2## is...
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5561146 |
Modified guanidino and amidino thrombin inhibitors
Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; and R 1 is cyano, hydroxyl,...
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5550229 |
Alkylation process for preparing azetidinone compound and starting compound therefor
Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R 1 is H or lower alkyl, R 2 and R 3 combine together with the adjacent nitrogen to form heterocyclic...
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5541317 |
Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds
Compounds of formula (I): ##STR1## wherein: R 1 is hydrogen or a hydroxy-protecting group; R 2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R 3 is...
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5532228 |
Side-chain homologous vitamin D derivatives, process for their production, pharmaceutical preparations containing these derivatives and their use as pharmaceutical agents
The invention discloses side-chain homologous vitamin D derivatives of formula I ##STR1## in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , B, and D have the meanings defined in the specification and...
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5532255 |
Adhesion receptor antagonists
Compounds of the formula ##STR1## in which R 1 , X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating...
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5510477 |
Process for the acylation of lactams
High quality acyl lactam imides are prepared by reacting an acyl lactam of the formula ##STR1## where 5 carbon atoms and an acylating acid of the formula R'CO 2 H or by reacting a lactam, an...
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5480987 |
2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of producing them
The invention provides substituted allylazetidinone compounds having the formula: ##STR1## and propargyl azetidinone compounds having the formula: ##STR2## wherein R 1 , R 2 , R 3 , R 30 , X, Y and...
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5457114 |
Amidinophenylalanine derivatives, a process for the preparation thereof, use thereof and agents containing these as anticoagulants
Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
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5424422 |
Beta-lactams and their production
A beta-lactam compound of the formula: ##STR1## wherein R 1 and R 2 are, the same or different, each a hydrogen atom or a lower alkyl group, R 3 o is a lower alkyl group having a...
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5386029 |
Process for the manufacture of 4-acyloxy-3-hydroxyethyl-azetidinones
The invention relates to a novel process for the manufacture of (3R,1'R)-4-acyloxy-3-(1'-hydroxyethyl)-2-azetidinones of formula ##STR1## in which R 1 represents lower alkyl or aryl, by...
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5326863 |
Azetidin-2-one derivatives as serine protease inhibitors
The present invention relates to new 3-guanidinoalkyl-2-azetidinones of the formula ##STR1## wherein: U and W can be the same or different and are selected from the group consisting of hydrogen and...
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5322939 |
Process for preparing azetidin-2-one derivatives
A process for preparing an azetidin-2-one derivative represented by formula (2): ##STR1## wherein R 4 and R 5 , which may be the same or different, each represents a hydrogen atom, an alkyl group...
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5317100 |
Process for the preparation of optically active acyloxyazetidinones
Compounds of the formula ##STR1## in which R 1 is hydrogen or lower alkyl, R 2 is hydrogen or a hydroxyl protective group R 2 ' and R 3 is substituted or unsubstituted phenyl or lower alkyl can...
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5306816 |
Processes for preparing carbapenem derivatives
The invention relates to carbapenem derivatives useful as antimicrobial agents, more particularly to intermediate compounds for the preparations thereof of the formula ##STR1##
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5296595 |
Method of enantioselectively inserting a carbene
A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented...
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5284963 |
Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
The invention provides a novel method for producing compounds of the formula I: ##STR1## wherein X and R are defined in the specifications. The invention also provides a method for making...
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5283355 |
Benzoquinone compounds
Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted...
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5274098 |
Amidinophenylalanine derivatives, process for their preparation, their use and compositions containing them
Amidinophenylalanine derivatives, a process for their preparation, their use and pharmaceutical compositions which contain these compounds are described.
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5252698 |
Metal ion porphyrin-containing poly(azine)
The present invention relates to porphyrin and metal ion-containing monomers and polymers. The monomers ##STR1## wherein R 1 , R 2 , R 3 , and R 4 are independently selected from H, alkyl having 1...
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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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5240919 |
Benzthiazolinonyl-substituted alkylamides
Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.
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5231179 |
Heterocyclic compounds and their production
A compound of the formula: ##STR1## wherein R 1 , R 2 , R 3 and R 4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R 1 and R 2 may be combined...
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5225552 |
4-cyclohexenyl azetidinone derivatives
Compounds of formula ##STR1## in which R 1 represents a hydrogen atom or a hydroxyl protecting group; R 2 represents a hydrogen atom or a trialkylsilyl group, and --X--Y-- represents the epoxide...
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5204461 |
Process for preparing (1'R,3S)-3-(1'-hydroxyethyl)-azetidin-2-one and derivatives thereof
A process for preparing (1'R,3S)-3-(1'-hydroxyethyl)-azetidin-2-one or a derivative thereof represented by formula (I): ##STR1## wherein R 1 represents a hydrogen atom or a hydroxyl-protective...
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5202433 |
Polysaccharide derivatives as separating agents
A polysaccharide derivative prepared by replacing a part or the whole of hydrogen atoms of hydroxyl and/or amino groups of a polysaccharide with one or more atomic groups represented by the...
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5196528 |
4-cyclohexenyl azetidinones and epoxy derivatives thereof
Compounds of formula ##STR1## in which R 1 is hydrogen or a hydroxyl protecting group and --X--Y-- is --CHCH-- or ##STR2## useful as intermediates in the preparation of antibacterially active...
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5191074 |
β-lactam compounds and production process thereof
A process for producing a β-lactam compound of the formula ##STR1## wherein OR 1 is a protected or unprotected hydroxyl group; R 2 is a C 1 to C 7 alkyl or aryl group; from an azetidinone...
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5177201 |
Nitrogen deprotected 4-acyloxyazetidin-2-ones
The 4-acyloxyazetidin-2-ones, which are intermediates in the production of carbapenems and penems, are produced from nitrogen deprotected 4-furanylazetidin-2-ones.
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5149802 |
Process for producing azetidinone derivatives
A process for producing 2-azetidinone derivatives represented by formula ##STR1## wherein R 1 denotes a protecting group of a hydroxyl group, Z denotes a hydrogen atom or a protecting group of...
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5145957 |
Stereoselective synthesis of a chiral cis 3-beta hydrogen (3R) 4-aroyloxy azetidinone
A process is described for the stereocontrolled synthesis of (3R,4R)-3-[(1R)-1-hydroxyethyl]-4-benzoyloxyazetidin-2-ones and their derivatives by cycloaddition involving an imine and a ketone,...
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5142038 |
Process of enantiomeric separation of carbacephem intermediates
Enantiomerically pure β-lactam intermediates of the formula (I) ##STR1## are isolated from a haloalkane solvent through precipitation with methyl-t-butyl ether or methanol. The products thus...
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5138048 |
4-(2-Oxo-cyclohexyl) azetidinones
Compounds of the general formula (I) ##STR1## in which: R 1 represents a hydroxyl protecting group; and R 2 represents a hydrogen or halogen atom, an azido group, a C 1 -3 alkyl group, a group...
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5134231 |
3(1-hydoxyethyl)azetidinone compounds and their production
An amino acid compound of the formula: ##STR1## wherein R is a lower alkyl group, R 1 is a hydrogen atom or a protecting group for carboxyl, R 2 is a hydrogen atom, a protecting group for amino,...
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5112966 |
Beta-lactams
A beta-lactam compound of the formula: ##STR1## wherein R 1 is a hydrogen atom, a lower alkyl group or a 1-hydroxy(lower)alkyl group wherein the hydroxyl group is optionally protected, R 2 is a...
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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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5104984 |
Enantioselective process for producing 1-beta-methyl carbapenem antibiotic intermediates
A process is described for the stereochemically controlled synthesis of intermediates useful in producing 1-betamethylcarbapenem antibiotic intermediates involving reacting a beta lactam with a...
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5089609 |
4-benzoyl azetidinones
Compounds of the formula ##STR1## wherein each R' is independently hydrogen, one, two or three of halogen, lower alkyl or lower alkoxy and R" is methyl, ethyl, allyl or a phenyl, are described....
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5081237 |
3-alkenyl-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds
The invention relates to novel intermediate compounds for preparation of compounds of high antimicrobial activity, said intermediate compounds being of one of the formulas: ##STR1## wherein R 1 is...
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5081238 |
βmethyl azetidinone derivatives and stereoselective process for preparing the same
An azetidinone derivative having the general formula (I): ##STR1## wherein R 1 and R 2 are hydrogen atom or a protective group and R 3 is an alkyl group or hydrogen atom, a process for preparing...
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5075435 |
Beta-lactams and their production via stereospecific hydrogenation
A beta-lactam compound of the formula: ##STR1## wherein R 1 is a hydrogen atom, a lower alkyl group or a 1-hydroxy(lower)alkyl group wherein the hydroxyl group is optionally protected, R 2 is a...
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5075437 |
3,4-disubstituted-2-azetidinone derivatives and processes for preparation using tin enolates
The invention relates to the preparation of 3,4-disubstituted-2-azetidinone compounds of the formula: ##STR1## in which R 1 is hydrogen or amido-protective group, R 2 is hydroxy(lower)alkyl or...
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5075436 |
Chiral 1-β-methyl-carbapenem intermediates
A multistep process is described for selectively obtaining 1-β-methylcarbapenem intermediates in high overall yield. The desired 1-β-methyl chirality is obtained through the hydrogenation of...
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5047526 |
Dehydrogenative silylation process of organic compounds having active hydrogen
A dehydrogenative silylation process of organic compounds having active hydrogen which comprises reacting an organic compound having active hydrogen with t-butyldimethylsilane in the presence of a...
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