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7384928 |
Broad spectrum cephem compounds
A compound of the formula:
(wherein,
T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower...
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7115624 |
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ,...
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6599892 |
7-alkylidene cephalosporanic acid derivatives and methods of using the same
Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of β-lactamase enzymes.
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6583133 |
Propenyl cephalosporin derivatives and process for the manufacture thereof
Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and...
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6440957 |
Cephalosporines having cyclic aminoguanidine substituents as antibiotics
A compound useful as an anti-bacterial agent, having the formula wherein R 2 together with the nitrogen atom to which it is attached forms a cyclic aminoguanidine group or derivative thereof as...
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6294527 |
Cephem compounds
An antibacterial compound ##STR1## wherein ##STR2## represents benzene ring, pyridine ring, pyrazine ring or 5-membered aromatic neterocycle (having one oxygen or sulfur atom as...
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6262044 |
Modulators of protein tyrosine phosphatases (PTPASES)
The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein...
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6242437 |
Cephem derivatives
A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative...
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6180621 |
Method and treatment using 1-methylcarbapenem derivatives as an anti-helicobacter pylori agent
A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula...
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5994340 |
Azetidinone derivatives as β-lactamase inhibitors
New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These...
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5945414 |
Process for the preparation of new intermediates useful in the synthesis of cephalosporins
Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II): R--SH ...
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5883089 |
Cephem derivatives
Compounds, represented by the following formula (I), having a β-(substituted or unsubstituted imidazo 5,1-b!thiazolyl)vinyl group at the 3-position of the cephem ring and a salt and an ester...
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5728691 |
Quinolonylcarboxamidocephalosporin derivatives and pharmaceutical compositions containing them
Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as...
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5710146 |
Cephem derivatives and processes for their manufacture
Cephem derivatives of the general formula ##STR1## in which the R 2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against...
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5698547 |
Cephalosporin antibiotics
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide...
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5607927 |
Cephalosporin derivative
An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that...
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5593984 |
Cephalosporin derivatives
The present invention relates to novel cephalosporin derivatives or pharmaceutically acceptable non-toxic salts thereof useful as antibiotics and to processes for the preparation thereof. ##STR1##...
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5571804 |
Cephalosporin antibiotics
Cephalosporin compounds of formula (I): ##STR1## wherein: R 1 is a hydrogen or an amino protecting group; R 2 and R 3 are, independently, a hydrogen or a hydroxy protecting group, or form...
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5446037 |
2-[(substituted) methylene]cephalosporin sulfones as antiinflammatory, antidegenerative and antithrombin agents
This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as...
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5373000 |
7Beta-(thiadiazolyl)-2-iminoacetamido-3cephem compounds
A cephalosporin derivative represented by the formula: ##STR1## wherein R 1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R 2 and R 3 ...
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5312813 |
Biofilm reduction method
A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in...
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5192770 |
Serotonergic alpha-oxoacetamides
α-Oxoacetamides of the formula R 1 C(O)C(O)NR 2 R 3 in which R 1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl,...
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RE33948 |
β-lactam antibiotics
Antibacterially active and animal growth-promoting novel β-lactam compounds of the formula ##STR1## in which R 1 represents the radical ##STR2## Y representing N or CR 9 , or Y--R 7 representing...
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4826834 |
Cephem compounds
A compound having the general formula ##STR1## wherein, R 0 is a hydrogen atom, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; Z is S, S➝O,O or CH 2 ; R 4...
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4788185 |
Cephalosporin compounds
A compound of the formula; ##STR1## wherein R 0 stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or esterified carboxyl group, Z stands for S, S➝O, O or CH 2 , R 4 ...
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4734407 |
Alpha-aminoacyl-penicillins and cephalosporins
Antibacterially active and animal growth-regulating novel β-lactam compounds of the formula ##STR1## in which R 1 represents an optionally substituted radical of the formula ##STR2## Z represents...
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4692441 |
Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
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4690921 |
Cephalosporin compounds and salts thereof
Novel cephalosporin compounds of the formula ##STR1## wherein the wavy line means syn-form and anti-form bonds, R 1 represents a cyanomethyl group, a thiocarbamoylmethyl group or an...
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4504478 |
Cephalosporin-1-oxide derivatives
An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X 1 is sulphinyl; R 1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art;...
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4468394 |
Cephalosporin compounds
A compound represented by the formula: ##STR1## wherein R 1 is hydrogen or methoxy; R 2 is hydrogen or hydroxy; R is ##STR2## wherein R 3 and R 4 are hydroxy or acyloxy, Y is oxygen, sulfur or...
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4425337 |
Adjuvants for rectal delivery of drug
A method and drug form enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps of...
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4415562 |
3-Thiovinylcephalosporins and pharmaceutical compositions
New cephalosporins of the general formula: ##STR1## in which R is alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic rings, R' is a hydrogen atom or a radical of the general formula:...
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4410522 |
Cephalosporins
Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable...
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4406896 |
Adjuvants for rectal delivery of drug substances
A method and drug form for enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps...
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4388314 |
Heteromonocyclic and heterobicyclic derivatives of unsaturated 7-acylamido-3-cephem-4-carboxylic acid
Heteromonocyclic and heterobicyclic derivatives of unsaturated 7-ayclamide-3-cephem-4-carboxylic acid are disclosed, and process for preparing same. These compounds are suitable for treating...
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4376767 |
Pyridylmethyl esters of selected bio-affecting carboxylic acids
Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R 1 and R 2 , which can be...
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4364943 |
Syn-isomer of 7-[2-alkoxyimino-2-(2-amino-alkanoylamino-or haloalkanoylamino-thiazol-4-yl) acetamids]-3-[hexanoyl-, or phenylalkanoyl-oxymethyl or benzothiazolylthiomethyl]-3-cephem-4-carboxylic acid
Syn-isomers of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have anti-bacterial activities and the processes for the preparation...
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4358447 |
7-N-Heterocyclyl cephalosporins
Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing...
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4352801 |
Cephem derivatives and antibacterial agents comprising said compounds
Cephem derivatives represented by the formula: ##STR1## wherein R 1 represents a hydrogen atom or a hydroxyl group, R 2 represents a lower alkyl group or a chloro-substituted lower alkyl group,...
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4352800 |
Adjuvant for promoting absorption of therapeutically active substances through the digestive tract
The enamine derivatives having following formula ##STR1## promote absorption of therapeutically active substances through the digestive tract into the blood stream and are able to effectively...
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4331666 |
3-[(8-Carboxy-6-tetraz olo[1,5-b]pyridazinyl)-thiomethyl]-7-[2-(2-amino-4-thiazolyl)-2-methoxyim ino-acetamido]-3-cephem-4-carboxylic acid
Heterocyclyl derivatives of oxy-imino-substituted cephalosporins are disclosed, such, for instance the compound 3-[(8-amino-6-tetrazolo[1,5-b]pyridazinyl)-thiomethyl]-7-[2-
(2-amino-4-thi...
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4307090 |
Novel oximes
Novel oximes of the syn isomers of 7-(2-amino-4-thiazolyl)-acetamido-cephalosporanic acid of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, chlorine, methoxy,...
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4288435 |
3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutical antibacterial compositions containing them
The present invention relates to new 3,7 disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to new...
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4275062 |
Aminothiazolyl ureido sulfoxide cephalosporins
Cephalosporins of the formula ##STR1## R represents hydrogen, sodium, potassium, or certain ester groups, R 1 is in the α-configuration and is hydrogen or methoxy, X represents hydrogen ##STR2##...
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4201781 |
Substituted 7[s-oxopyrido[2,3-d]pyrimidine carboxamido acetamido]cephalosporins
Cephalosporin compounds of the formula ##STR1## wherein R is 1-carboxymethyl-1,2,3,4-tetrazol-5-yl or 5-carboxymethyl-1,3,4-thiadiazol-2-yl, and non-toxic pharmaceutically acceptable salts thereof,...
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4200575 |
7[(2-Thiazolyl)-2-(oxoimino)acetamido]cephalosporin derivatives
Novel [2-(syn)-carbamoyloximinoacetamido]cephalosporins of the formula: ##STR1## [wherein, Y 1 is hydrogen, hydroxyl, carbamoyloxy, acyloxy, quaternary ammonium or nitrogen-containing heterocyclic...
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4168309 |
Cephalosporins having a 7-(carboxy substituted α-etherified oximinoarylacetamido) group
Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R a and R b which may be the same or different, are each selected from hydrogen, C 1 -4 alkyl,...
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4165373 |
7-(α-Acylamino-α-phenyl or thienylacetamido) cephalosporin derivatives
A compound of the formula (I): ##STR1## wherein A is a monocyclic or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted...
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4156724 |
N-acylamino-alpha-arylacetamido cephalosporins and antibacterial compositions and methods containing them
A cephalosporin derivative of the formula (I), ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be...
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4147693 |
βLactam antibiotics and process for their use
6-[α-(Imidazolidin-2-on-1-ylcarbonylamino)-substutited acetamido]penicillanic acids, and the correspondingly 7-substituted ceph-3-em-4-carboxylic acids, characterized by the presence of a...
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