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7589216 |
Process for preparing N-hydroxyformamido-propyl pyrrolidin compounds and intermediates
The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase...
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7514571 |
Bicyclo derivative
A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor:
One example is...
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7488725 |
Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase IV and methods
Compounds are provided having the formula:
wherein R 1 , R 2 , R 2′ , R 3 , R 3′ , R 4 , R 4′ , R 5 , X, Y and Z are as defined herein.
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7462641 |
(2S,4S)-4-fluoro-1-[4-fluoro-beta-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-β-(4-fluorophenyl)-L-phenylala
nyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.
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7375238 |
Process for the preparation of N-substituted 2-cyanopyrrolidines
The present invention relates to a process for the preparation of a N-(N′-substituted glycyl)- 2 -cyanopyrrolidine comprising at least
(a) reacting, in the presence of dimethylformamide, a...
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7361663 |
N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing...
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7329762 |
Prodrugs of mitotic kinesin inhibitors
The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP...
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7309714 |
Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or...
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7304166 |
Benzenesulfonate salt of 4-fluoro-2-cyanopyrrolidine derivatives
A benzenesulfonate salt of (2S,4S)-2-cyano-4-fluoro-1-[(2-hydroxy-1,1-dimethyl)ethylami
no]acetylpyrrolidine that has an excellent DPPIV inhibition activity as well as physical properties (e.g.,...
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7241902 |
Allylmercaptocaptopril compounds and uses thereof
Compounds which are the reaction product of allicin and ACE-inhibiting compounds are useful in treating hypertension, elevated triglycerides, and elevated insulin.
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7238683 |
Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or...
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7199150 |
Amino alcohol compounds
Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and...
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7196201 |
Pyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their...
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7183290 |
Fluoropyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl...
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7179918 |
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
Compounds of the formula:
where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as...
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7169806 |
Antidiabetic agents
Compounds which are 1-(2′-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A...
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7157454 |
Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula:
These compounds show affinity for the bradykinin receptors with selectivity towards the B 1 receptors; they may be used for the preparation of...
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7132539 |
Melanocortin receptor ligands
The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R 1 alkyl units selected from the group consisting of C 1 –C 12 linear or...
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7132443 |
Fluoropyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their...
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7087759 |
Melanocortin receptor ligands
Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula:
wherein A is a conformationally restricted ring system selected from the group consisting of:
a)...
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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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7041831 |
Diastereoselective synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors
Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I):
The method comprises the step of reacting an aldehyde compound R 10 CHO with an...
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7026316 |
Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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RE38947 |
Method of enantioselectively catalyzing a reaction
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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6943269 |
Contrast media for angiography
The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or...
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6867310 |
Arylation and vinylation of activated carbons
The present invention provides transition-metal-catalyst-based methods for the arylation and vinylation of activated methyl, methylene, and methine carbons with aryl halides, vinyl halides, and the...
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6812350 |
Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that...
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6723856 |
Process for the preparation of 2-acetyl-1-pyrroline, the basmati rice flavorant
The present invention provides a process for preparing of 2-acetyl-1-pyrroline, the principle aroma component of basmati and other varieties of scented rice, and also of processed cereal and grain...
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6716843 |
Alpha-amino acid sulphonyl compounds
Compound of formula (I): wherein: represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R 1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or...
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6710040 |
Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such...
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6706742 |
Alpha-amino-acid compounds
Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single...
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6699990 |
3-(2,5-diaminophenyl)-acrylamide derivatives and coloring agents containing said compounds
The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing...
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6645995 |
Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or...
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6642391 |
Amycomycin, a process for its production and its use as a pharmaceutical
A compound named Amycomycin of the formula: is described, as well as its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms. The compound is...
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6630504 |
Phenoxyphenylheterocyclyl derivatives as SSRIs
The invention provides compounds of general formula (I) wherein R 1 is H or C 1 -C 6 alkyl; R 2 and R 3 , together with the interconnecting atoms form a 4 to 8-membered saturated ring containing...
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6627769 |
RGD-analog non-peptidic molecules having anti-adhesive, anti-migration and anti-proliferative effects
Novel molecules without intramolecular peptidic bonds, able to mimic the RGD peptide, containing ARG-GLY-ASP motif “arginine-glycine-aspartic acid” (that is a potent inhibitor, in vivo and in...
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6610729 |
Hydroxamic acid derivatives and medicinal utilization thereof
The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a...
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6593312 |
Cyclic α-amino-&ggr -hydroxyamide compounds
A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R 1 and R 4 , which may be identical or different, each...
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6531511 |
2-adamantanemethanamine compounds for treating abnormalities in glutamatergic transmission
The use of a compound of formula (1), as disclosed in the specification, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are independently selected from hydrogen, alkyl and aryl, or pharmaceutically...
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6521760 |
Process for the preparation of zofenopril calcium salt
A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: a) reaction of S(−)-3-benzoylthio-2-methylpropanoic acid chloride with...
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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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6433185 |
N-(arylsulphonyl) amino acid derivatives, process for their preparation and pharmaceutical compositions containing them
The invention relates to compounds of formula in which R 1 to R 9 , R 16 and R 17 are as defined in claim 1. These compounds are pharmacologically active.
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6432969 |
N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
The present invention relates to certain N-(substituted glycyl)-2-cyanopyrrolidines of formula I wherein Y is as defined herein, in free form or in acid addition salt form. Compounds of formula...
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6399628 |
N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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6395737 |
Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings...
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6388122 |
Tryptase inhibitor and novel guanidino derivatives
A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the...
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6380254 |
Method and composition for treating and preventing pathogenic effects caused by intracellular calcium overload
The present invention provides a method and composition for treating or preventing pathogenic effects in a mammal caused by intracellular calcium overload, comprising administering to a mammal a...
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6362174 |
Reduced dipeptide analogues as calcium channel antagonitsts
The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke,...
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6331537 |
Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and...
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6313120 |
N-(arylsulfonyl) amino acid derivatives, process for their preparation and pharmaceutical compositions containing them
The invention relates to compounds of formula ##STR1## in which R 1 to R 9 , R 16 and R 17 are as defined in Claim 1. These compounds are pharmacologically active.
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