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Document Title |
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7528264 |
Hydride reduction process for preparing quinolone intermediates
Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.
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7410995 |
N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked...
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7390910 |
Compounds for treating tumors
The invention provides compounds of formula (I):
wherein E, A, B′, R 6 , R 7 , R 8 , and R 9 are defined in the specification which compounds exhibit anticancer activity and are useful for...
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7378440 |
Substituted benzoylureido-o-benzoylamides, process for their preparation and their use
The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of...
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7338976 |
Heterocyclic esters or amides for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic...
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7323489 |
Proline ester and preparation containing the same for percutaneous administration
A proline ester represented by the following formula (I):
wherein R 1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group...
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7279584 |
Method for production of cis-4-fluoro-L-proline derivatives
The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale...
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7265150 |
Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders
This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment...
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7250409 |
Ningalin B analogs employable for reversing multidrug resistance
Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell...
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7250520 |
Processes for preparing pyrroles
The present invention relates to an improved synthesis of pyrrole capping group precursors.
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7189754 |
Pyrrolidine ester derivatives with oxytocin modulating activity
The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present...
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7022677 |
Amide derivatives as growth hormone secretagogues
Disclosed are the novel compounds as growth hormone secretagogues represented by structural Formula (I), wherein R 1 is, substituted or unsubstituted alkyl, substituted or unsubstituted...
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6972331 |
Carboxy pyrrole, process of preparing and use as precursor
4-Oxo-4,5-dihydro-3H-pyrrolo[3,2-d] pyrimidine-7-carboxylic acid methyl ester and process for preparing are provided. The process for producing the...
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6933269 |
Polyaspartate derivatives for use in detergent compositions
Polyaspartate derivatives, especially hydrophobically modified and/or hydrophilically modified polyaspartate derivatives, most especially polyaspartate derivatives that are both hydrophilically and...
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6740760 |
D-proline derivatives
New compounds have the formula: wherein R, R 1 , X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases...
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6713502 |
Anti-infectives
Novel anti-infective and methods of using them are provided.
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6713628 |
Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid
There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and...
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6713503 |
Treatment of breast cancer
Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which...
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6627760 |
Amorphous compound
The present invention relates to a novel form of (S)-1-[N 2 -(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to...
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6541635 |
Method for producing angiotensin converting enzyme inhibitor
The present invention discloses a method for producing angiotensin converting enzyme inhibitor of the following formula (I) and pharmaceutically acceptable salts thereof, in which a compound of the...
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6534657 |
Chiral ferrocene phosphines and their use in asymmetric catalytic reactions
Ferrocene anchored chiral ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes according to the present invention are useful as...
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6515179 |
Process for the removal of nitrobenzenesulfonyl
A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a...
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6500959 |
Pyrrolidine derivatives and processes for preparing same
This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated...
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6462072 |
Cyclic ester or amide derivatives
This invention relates to low molecular weight, small molecule cyclic esters and amides having an affinity for FKBP-type immunophilins, pharmaceutical compositions comprising the same, and methods...
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6455705 |
1-&lsqb N2-((S)-ethoxycarbonyl)-3-phenylproply)-N6-trifluoroacetyl&rsqb -L-ysyl-L-proline (lisinopril (TFA) ethyl ester, LPE)
A method of isolating 1-[N 2 -((S)-ethoxycarbonyl)-3-phenylpropyl)-N 6 -trifluoroacetyl]-L-lysyl-L-proline (lisinopril (TFA) ethyl ester, LPE). The solvent or solvent mixture used for the...
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6448286 |
Imino pyrrolidine derivatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
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6350882 |
Synthesis of substituted prolines
The instant invention is directed to a process for synthesizing substituted prolines, in particular, optically pure substituted prolines, which comprises the steps of: a) adding an unsubstituted...
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6329418 |
Substituted pyrrolidine hydroxamate metalloprotease inhibitors
The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the...
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6313159 |
Metabotropic glutamate receptor ligand derivatives as naaladase inhibitors
The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit...
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6271393 |
Process for producing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline
The process for producing N 2 -(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline in a simple, efficient and industrially advantageous manner, including the following steps: 1) subjecting N 2 ...
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6258959 |
Process for the preparation of 2,4-dimethyl-3,5-bisalkoxycarbonylpyrrole
A process for the preparation of 2,4-dimethyl-3,5-bisalkoxycarbonylpyrrole is described, in which an acetoacetic alkyl ester is nitrosated to give the 2-nitrosoacetoacetic alkyl ester, the nitroso...
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6242476 |
Leukotriene A4 hydrolase inhibitors
The present invention relates to leukotriene A 4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients, ##STR1## wherein R 1 represents...
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6239146 |
Neurotrophic difluoroamide agents
The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel α,α-difluoroacetamido compounds that are neurotrophic...
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6232467 |
Method for the synthesis of amines and amino acids with organoboron derivatives
Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
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6218551 |
Combinatorial hydroxy-amino acid amide libraries
Combination chemical libraries of Formula I ##STR1## and methods for preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with...
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6218417 |
Ace-inhibitor nitric salts
Compounds having platelet anti-aggregating activity and antihypertension activity having reduced branchial side effects.
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6204393 |
Method for crystallizing maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline
A process for simply and easily crystallizing a maleate salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (enalapril) having a high quality out of an aqueous liquid, which comprises...
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6187932 |
Simple process for producing high quality captopril
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6150527 |
Synthetic multimerizing agents
New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic...
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6084066 |
Polypetides that include conformation-constraining groups which flank a protein-protein interaction site
Homologs and analogs of naturally-occurring stem cell factor polypeptides contain one or more interaction sites of the natural counterpart. The interaction sites are flanked by...
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6063931 |
Process for synthesizing carbapenem side chain intermediates
A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid...
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6039939 |
N-acyl-hydroxyamino acid esters and their use
N-Acyl-hydroxyamino acid alkyl esters help to strengthen the natural barrier function of the skin against environmental influences and external irritation. They improve the suppleness and the...
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6031112 |
Process for the production of alkoxycarbonyl-dipeptides intermediates in the synthesis of the lisinopril
Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group,...
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6025500 |
Stereoselective process for enalapril
The invention relates to an improved stereoselective heterogenous catalytic reductive amination between ethyl 2-oxo-4-phenylbutyrate and alanylproline using hydrogen, a catalyst and one or more...
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5990131 |
Heterocyclic thioesters and ketones
This invention relates to neurotrophic low molecular weight, small molecule heterocyclic thioesters and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the...
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5977380 |
Process for preparing N-[1- (S)-ethoxycarbonyl-3- phenylpropyl]-L-alanine derivatives
A process for synthesizing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine derivatives of the following formula (I): ##STR1## in which the definition of R has the same meaning as given in the...
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5962696 |
Process for the preparation of 1-(N 2-(S)-ethoxycarbonyl)--3 phenylpropyl-N6-trifluoracetyl))-L-lysyl-L-prolin (Lisinopril(Tfa) ethylester, LPE))
There is provided a process for the work-up of this material having the formula ##STR1## because of its poor crystallizability has heretofore been available only with large yield losses. The yield...
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5917055 |
Process for producing N-(D-α-methyl-β-mercaptopropionyl)-L-proline and its intermediate
A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and...
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5907044 |
Method of isolating 1- N.sup.2 -((S)-ethoxycarbonyl)-3-phenylpropyl)-N.sup.6 -trifluoroacetyl!-L-lysyl-L-proline (lisinopril (TFA) ethyl ester, LPE)
A method of isolating 1- N 2 -((S)-ethoxycarbonyl)-3-phenylpropyl)-N 6 -trifluoroacetyl!-L-lysyl-L-proline (lisinopril (TFA) ethyl ester, LPE). The solvent or solvent mixture used for the...
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5898076 |
Process for preparing 1-pyruvyl-L-proline
Process for preparing N-pyruvyl-L-proline by reaction of L-proline with methyl pyruvate dimethyl ketal in the presence of an alkali metal alkoxide, subsequent acid hydrolysis and extraction of...
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