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7259263 |
Method of synthesis of azole-containing amino acids
The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I):
The invention is also relates to compounds of formula (I) and to intermediate compounds in the...
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7045532 |
ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include...
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6949658 |
Process for producing optically active α-amino acid and optically active α-amino acid amide
The present invention provides a process for efficiently producing an optically active α-amino acid and an optically active α-amino acid amide. After contacting with cells or processed cells...
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6878829 |
Method for producing β-alaninamides
β-alaninamides of the general formula
Wherein R 1 is hydrogen or C 1-6 alkyl which is unsubstituted or substituted with hyroxy, amino, carboxy, carbamoyl, methylmercapto, guanidino,...
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6730693 |
Double salts of fumaric acid with a carnitine and an amino acid and food supplements, dietary supplements and drugs containing same
Double fumarates of L-carnitine or isovaleryl L-carnitine and an amino acid having formula (I) are disclosed which are useful as active ingredients of food supplements, dietary supplements or...
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6673942 |
Resolution of DL-racemic mixtures
The present invention relates to a process for the resolution of DL-racemic mixtures of compounds which crystalize in the form of a conglumerate. Both, the D and L-enantiomers are obtained...
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6632830 |
ACE-2 inhibiting compounds and methods of use thereof
ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing...
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6350907 |
Matrix metalloprotease inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix...
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6316656 |
Process for making optically active alpha-amino ketones and selected novel optically active alpha-amino ketones
The invention includes selected novel optically active α-ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as...
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RE37303 |
Imidazole compounds and their therapeutic applications
A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having antagonist properties to histamine H 3 ...
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6265382 |
Dipeptide inhibitors of protein farnesyltransferase
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6194184 |
Compounds labeled with cyanate or thiocyanate metal complexes for detection by infrared spectroscopy
A labeled compound detectable by IR spectroscopy contains at least one histidine residue bound to a cyanate or thiocyanate metal complex that has an IR absorption band within the spectral region of...
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6180116 |
Histidine derivatives, preparation process and uses
Histidine derivatives and processes of preparing the histidine derivatives. The histidine derivatives can be used to combat free radicals. The histidine derivatives may be used in cosmetic and/or...
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5981564 |
Water-soluble derivatives of paclitaxel, method for producing same and uses thereof
The invention relates to new paclitaxel derivatives showing an increased solubility in water. More particularly, the invention relates to glutarylpaclitaxel, glutarylpaclitaxel 6-aminohexanol...
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5981761 |
Crosslinked polyaspartate salts a process for their production
A first embodiment comprises reacting PSI with polyhydrazide selected from the group consisting of dihydrazides and trihydrazides and mixtures thereof, subsequently hydrolyzing the crosslinked PSI...
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5962722 |
α-hydrazino acid derivatives and method for making same
An α-hydrazino acid derivative of general formula (I) is described, wherein R 1 , R 2 , R 3 are hydrogen or a carbon radical, such that when R 2 and R 3 are different, C* is an asymmetric...
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5916915 |
Water-in-stable L-ascorbic acid derivative and a method for preparation thereof, and a skin-whitening cosmetic composition containing the same
Disclosed herein are a L-ascorbic acid derivative having an improved water-in-stability, represented by a following general formula (I): ##STR1## and a method for preparation thereof, and to a...
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5811446 |
Prophylactic and therapeutic methods for ocular degenerative diseases and inflammations and histidine compositions therefor
The present invention relates to methods for protecting the eye from degenerative eye conditions by administering prophylactic histidine compositions. The invention also relates to methods for...
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5770739 |
Non-aqueous hydrogen peroxide complex
An apparatus and process for hydrogen peroxide vapor sterilization of medical instruments and similar devices make use of hydrogen peroxide vapor released from a substantially non-aqueous organic...
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5763657 |
Phosphoric acid-amino acid-polyvalent metal composite salt and ruminant feed additive composition
The present specification discloses a ruminant feed additive composition which contains as an active ingredient a phosphoric acid-amino acid-polyvalent metal composite salt (final composite salt)...
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5741807 |
Histidine compositions and methods for treating or preventing infectious and non-infectious diarrheas
A method of preventing or reducing fluid and electrolyte losses in mammalian subjects under the effect of a stimulus that directly or indirectly causes such losses, by administering a...
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5741794 |
Heterocyclic sulfonamide derivatives as antagonists of PAF and angiotensin II
Compounds of formula (I), wherein: A represents: a) a --VR 6 group wherein v is --C(O), --C(O)O--, --CH 2 O--, --CH 2 OC(O)--, --C(S)--, --CH 2 OC(O)NH--, --C(S)O--, --CH 2 ...
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5708171 |
Imidazole derivatives for pharmaceutical use
A compound selected from the group consisting of a compound of the formula ##STR1## having antagonist properties to histamine H 3 -receptors.
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5688946 |
Amino acid derivatives having renin inhibiting activity
The compounds of the formula ##STR1## in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as...
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5679852 |
Process for the production of DTPA-monoamides of the central carboxylic acid and their use as pharmaceutical agents
A process for the production of of general formula I diethylenetriaminepentacarboxylic acid monoamide derivatives ##STR1## in which E 1 , E 2 and Z have varying meanings.
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5659065 |
Alpha-aminoalkanoic acids and reduction products
Compounds of formula I ##STR1## wherein R 1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or...
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5631031 |
Water-insoluble amino acid salt
Disclosed are water-insoluble, calcium or magnesium salts of alpha amino acids and a process for their preparation. The process comprises the steps of reacting an alpha-amino-protected alkyl ester...
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5585498 |
Imidazole derivatives useful as synthetic intermediates
Compounds of formula (I) ##STR1## wherein R 1 represents either a hydrogen atom, or a (C 1 -C 4 )alkyl group, X represents either a sulphur atom, an oxygen atom or a methylene group, Z 1 ...
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5536815 |
Cyclopropyl based O- and N- and S-protecting groups
The present invention is directed to the use of a cyclopropylmethyl derivative as a protecting group for compounds containing an amino group, carboxy group, amido group, mercapto group or hydroxy...
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5514781 |
Use of azoles as virucidal agents in solutions of biologically active proteins
Soluble azoles in aqueous solutions can be used as virucidal agents for biologically active protein preparations.
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5506362 |
Process for the preparation of an α-amino acid amide
An α-amino acid amide is prepared by reaction of an N α -aryloxycarbonylamino acid with a compound containing a free amino group. This process makes it possible readily to prepare peptides, by...
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5496955 |
Preparation of D-histidine and derivatives thereof from L-histidine
D-histidine and its derivatives are manufactured from L-histidine, by mixing L-histidine and tartaric acid with an aldehyde in acetic acid medium and thereafter precipitating D-histidine tartrate...
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5399707 |
Selective precipitation of α-aryl carboxylic acid salts
A process is provided whereby S(+)-ibuprofen or R(-)-ibuprofen L-lysinate salt is produced by selective precipitation from a mixture containing enantiomers of ibuprofen and L-lysine. The quantity...
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5371234 |
Ion specific chelating agents derived from β-hydroxyhistidine, 4-(1-hydroxy-1-alkyl)imidazole and derivatives thereof
β-hydroxyhistidine, 4-(1-hydroxy-1-alkyl)imidazole or derivatives thereof can be used as a bidentate ligand in the chelation of iron(III), Al(III), Cr(III), Ga(III) and the actinides(IV), such as...
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5359128 |
Malic acid derivatives and compositions for the treatment of psoriasis
The invention comprises compositions and methods for the treatment of psoriasis. The compositions comprise compounds of the formula: ##STR1##
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5332834 |
Racemization of an enantomerically enriched α-aryl carboxylic acid
There is disclosed and claimed a process whereby S(+)-ibuprofen L-lysinate salt is produced by selective precipitation from a mixture containing enantiomers of ibuprofen and L-lysine. The quantity...
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5276147 |
Compounds and complexes useful in medical imaging
The subject of the present invention is compounds which correspond to the following general formula: ##STR1## in which R 1 and R 3 independently of one another represent H, an alkyl, alkenyl,...
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5179117 |
Antihypercholesterolemic 2-substituted imidazoles
The compounds of the described invention are potent ACAT inhibitors and are useful in pharmaceutical compositions for the treatment of atherosclerosis and have the formulas: ##STR1## when Q is a...
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5153358 |
Process for the preparation of alpha-alkylated alpha-amino acids and alpha-halogenated alpha-amino acids
A novel process for the preparation of α-alkylated α-amino acids and α-halogenated α-amino acids is disclosed. These α-alkylated α-amino acids and α-halogenated α-amino acids are useful as...
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5149692 |
Bisalkoxyphosphinyl compounds as renin inhibitors
The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by...
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5110799 |
Antiherpetic agents
A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide...
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5110797 |
Peptide compound and a pharmaceutically acceptable salt thereof
Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp,...
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5072041 |
Optically active N-hydroxy-alpha-amino acids, amides and their derivatives
The invention relates to new pure D- or L-N-hydroxy-alpha-amino acids and the derivatives thereof, including optically active N-hydroxy-phenylglycine amide, which has antibiotic and antitumor...
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5063208 |
Peptidyl aminodiol renin inhibitors
A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.
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5055588 |
Process for preparing N-substituted amino acid esters
A process for preparing N-substituted amino acid esters having the formula (I): ##STR1## wherein R 1 and R 4 , the same or different, are an alkyl, aralkyl, cycloalkyl or aryl group; and R 2 and...
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5041644 |
Peptide derivatives of β-chloro-L(Z)-dehydro-glutamic acid
New peptide derivatives β-chloro-L-(Z)-dehydroglutamic acid are described which display antibacterial activity.
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5039664 |
Renin inhibitors containing phenylalanyl-histidine replacements
Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving...
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5034539 |
Histamine derivative, process for preparing it and its therapeutic use
The present invention relates to α,β-dimethylhistamine, of the rmula: ##STR1## in racemic form, or an optical isomer form or mixture of diastereoisomers and its acid addition salts. It may be...
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5026909 |
Method for preparing biologically active organic compound labelled with hydrogen isotope
A method according to the invention comprises mixing the starting biologically active organic compound, an inorganic vehicle and a catalyst in the form of a platinum-group metal, followed by...
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5025027 |
Cyclic carbamate analogues of (+)-pilocarpine
Pilocarpine analogues are provided having the structure ##STR1## where one of R 1 or R 2 is an alkyl, such as methyl, ethyl, propyl, butyl, and so forth, and the corresponding secondary alkyl...
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