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7112572 |
Multivalent metal salts of boronic acids
Salts of a pharmaceutically acceptable divalent metal and an organoboronic acid drug. Examples of such metals are calcium, magnesium and zinc. The organoboronic acid drug may be a boropeptide...
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7112571 |
Peptide Y-2
Peptide which is obtained by treating fish meat such as sardine with an alkaline protease is adsorbed with a peptide-adsorbing resin (such as ODS resin) and eluted with 10 aqueous ethanol to obtain...
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7105483 |
Phosphinic pseudopeptide derivatives for the selective inhibition of the C-terminal active site of angiotensin I converting enzyme (ACE)
The invention relates to the use of phosphinic pseudopeptide derivatives for production of a medicament for selectively inhibiting the active C-terminal site of angiotensin I converting enzyme....
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7105488 |
G protein-coupled receptor antagonists
G-protein coupled receptors (GPCR) generally contain seven transmembrane helices. The present invention provides synthetic peptides derived from these transmembrane helices. The peptides inhibit...
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7101855 |
Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by...
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7094769 |
2-aminocarbonyl-9H-purine derivatives
The present invention relates to compounds of the formula:
and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the...
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7091186 |
p-Amidobenzylethers in drug delivery agents
Compounds of the formulae
L A n -Z-X—W w D and B Z-X—W w D
wherein: D is...
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7091185 |
Periodic antimicrobial peptides
One embodiment of the invention comprises a method of producing periodic peptides, which can have antimicrobial uses, and further comprises the peptides themselves. A preferred method comprises the...
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7087576 |
Dipeptide phenyl ethers
Novel dipeptide ethers are effective for lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels. The dipeptide ethers are also useful for the treatment and/or...
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7084120 |
Prodrugs of DP IV-inhibitors
Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds...
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7074766 |
Substantially cell membrane impermeable compound and use thereof
The present invention relates to a compound according to Formula (I): A-(L-Y) p , wherein A comprises at least one substantially cell-membrane impermeable pendant group; L comprises any suitable...
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7074775 |
Aminobutyramide conjugate and a pharmaceutical composition for treatment of neuronal disorders
A compound is provided that has the formula
NH 2 CH 2 CH 2 CH 2 C(O)N—R (I)
...
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7071169 |
Pyrane derivatives as both ACE-and NEP-inhibitors
Compounds of the formula (I), wherein R 1 , R 1 –R 7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular...
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7071168 |
Anti-cancer compounds and methods related thereto
The present invention provides compounds useful to inhibit tumor growth and to induce apoptosis. In general, the anti-cancer agents (ACA) are described by the formula:
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7067491 |
Heterocyclic compounds having elastase-inhibiting activity and intermediates thereof
Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R 1 is a heterocyclic group...
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7067489 |
Hematopoietic stimulation
Methods and products for stimulating hematopoiesis, preventing low levels of hematopoietic cells and producing increased numbers of hematopoietic and mature blood cells are provided. The methods...
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7060708 |
Active agent delivery systems and methods for protecting and administering active agents
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active...
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7060683 |
Hydroxamate-containing cysteine and serine protease inhibitors
The present invention is directed to hydroxamate-containing inhibitors of cysteine and serine proteases. Methods for the use of the protease inhibitors are also described.
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7056889 |
Compounds that bind P2Y2 or P2Y1 receptors
The invention provides peptides and compounds that can bind to P2Y 2 receptors that are useful for modulating the secretion of mucus within mucosal surfaces.
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7053058 |
Pharmaceutical preparations and methods for inhibiting tumors
The invention provides pharmaceutical compositions and method for inhibiting growth of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial...
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7053055 |
Compounds of unstable DP IV-inhibitors
Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The compounds can be used...
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7048910 |
Use of ectoine or ectoine derivatives for oral care
The invention relates to the use of one or more compounds selected from compounds of formulae Ia and Ib, the physiologically compatible salts of compounds of formula Ia and Ib and the stereoisomer...
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7049298 |
Flavor-active peptides
The present invention pertains to specific peptides obtainable from cocoa beans and giving rise to a particular and distinct savor when subjected to a Maillard reaction with reducing sugars. In...
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7045133 |
VEGF-D/VEGF-C/VEGF peptidomimetic inhibitor
Monomeric monocyclic peptide inhibitors and dimeric bicyclic peptide inhibitors based on exposed loop fragments of a growth factor protein, such as loop 1, 2 or 3 of VEGF-D, and methods of making...
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7041639 |
Depsipeptide and congeners thereof for use as immunosuppressants
Depsipeptides and congeners thereof are disclosed having the following structure:
wherein m, n, p, q, X, R 1 , R 2 and R 3 are as defined herein. These compounds, including FR901228, have...
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7034002 |
Angiotensin converting enzyme inhibitor
The present invention provides an angiotensin converting enzyme inhibitor having strong activity of inhibiting angiotensin converting enzyme, good hue and easily to take in which is a composition...
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7033999 |
Nitrosated and nitrosylated heme proteins
Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet...
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7026297 |
Neuroprotective agents
Compounds of formula (I) wherein: Q represents an amidino group, a cyano group or a group of formula XYN—, (where X and Y are hydrogen or various groups); R a represents alkylene; R b and R c ...
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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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7022738 |
α-ketoamide derivative and use thereof
The present invention provides a compound represented by the formula (I):
wherein R 1 , R 2 and R 3 each represents a lower alkyl group.
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7005418 |
Method for the therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction
The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction...
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7001887 |
Peptide derivatives
A compound of Formula (1):
wherein
R 1 represents an amidinophenyl group, etc.; R 2 represents a hydrogen atom, etc.; R 3 represents a carbamoylalkyl group, etc.; R 4 represents a...
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6995141 |
Interleukin 1β protease and interleukin 1β protease inhibitors
There is disclosed an isolated polypeptide and derivatives thereof having protease biological activity for human precursor IL-1β and for a substrate comprising:
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6989139 |
Matrix metalloproteinase inhibitors
Thus the present invention describes novel compounds comprising 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the...
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6989372 |
Antioxidants, preparation methods and uses
The invention concerns compounds of general formula (I) (wherein R and R′ represent an alkyl radical or an aryl group and R″ is hydrogen or a CO—R 1 group wherein R 1 is an alkyl radical or...
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6984626 |
Gamma-secretase inhibitors
A class of compounds is disclosed which are diasteroisomers of a known class of protease inhibitors. The compound inhibit gamma-secretase, and find use in the treatment of and/or prevention of...
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6984627 |
Peptide derivatives
Pharmaceutical preparation containing an effective amount of acetylsalicylic acid and a compound of Formula I.
A 1 —A 2 —NH—(CH 2 )...
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6974800 |
Formulations comprising an inhibitor of carboxypeptidase U and A thrombin inhibitor
The present invention relates to pharmaceutical formulations of an inhibitor of carboxypeptidase U (CPU) and a thrombin inhibitor in admixture with a pharmaceutically acceptable adjuvant, diluent...
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6969703 |
Inhibitors of the ICE/ced-3 family of cysteine proteases
This invention is directed to novel sulfonimide (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds having the following structure:
wherein A, B, X, R, R 1 , R 2 , n, q, and r...
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6967202 |
Method of synthesizing diketopiperazines
The invention provides a method of synthesizing a diketopiperazine of the formula:
wherein:
R 1 is —CH 2 COR 3 , or —CH 2 CH 2 COR 3 ; R 2 is the side chain of an amino acid...
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6962899 |
Method for reducing the inflammation and inducing an analgesic effect and compounds thereof
Pharmaceutically acceptable compounds for administering to a subject, comprising the general structure II:
wherein R 1 is an L-amino acid or salt or ester thereof, or an L-amino acid...
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6960567 |
Method of producing n-[(2S)-sulfanyl-4-(1,5,5-trimethylhydantoinyl)butanoyl]-L-leucyl-L-tert-leucine N-methylamide and intermediate thereof
Process for producing N-[(2S)-sulfanyl-4-(1,5,5-trimethylhydantoinyl) butanoyl]-L-leucyl-L-tert-leucine N-methylamide by forming an intermediate compound...
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6960574 |
Antagonists of RF-amide neuropeptides
Disclosed are compounds having the formula:
where
R 1 =H, C 1 -C 6 alkyl, cycloalkyl,
R 2 =H, C 1 -C 6 alkyl, cycloalkyl W=C n H 2n-m —NH (n=1-6, m=0, 2, or 4),
X=
R 3 =
...
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6958319 |
Formulation of boronic acid compounds
The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1):
in which Z 1 and Z 2 are moieties derived from sugar. The...
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6949516 |
Dipeptide apoptosis inhibitors and the use thereof
The present invention is directed to novel dipeptides thereof, represented by the general Formula I:
where R 1 -R 3 and AA are defined herein. The present invention relates to the discovery...
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6943149 |
Benzimidazolone peptidomimetics as thrombin receptor antagonists
The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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6939855 |
Anti-inflammatory compositions and method
The disclosed invention includes pharmaceutical compositions and methods for treating inflammatory conditions, particularly those that are characterized by increased binding of alpha-9 integrin to...
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6933282 |
Regulation of tyrosine hydroxylase by GPE
Embodiments of this invention include methods for increasing the amount of the enzyme tyrosine hydroxylase (TH) in the central nervous system (CNS) of mammals in need of an increase in TH. Methods...
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6933290 |
2-{N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl}-amino}-alkylboronic acid derivatives
Disclosed are derivatives of 2-{[N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid, processes for the preparation of such compounds, pharmaceutical preparations, and...
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6927206 |
Compositions and methods for treatment of rosacea
A method for treating rosacea of the skin of a patient employs topically applying to the affected skin a composition comprising at least one peptide copper complex. In other embodiments, the...
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