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7390789 |
Thio-containing inhibitors of aminopeptidase P, and compositions thereof
The present invention is directed to an α thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The...
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7385025 |
Metallopeptide compounds
Metallopeptides with a sequence of a biologically active alpha-melanocyte stimulating hormone (α-MSH), gamma-melanocyte stimulating hormone (γ-MSH), or bombesin sequence of length n residues,...
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7378397 |
TRH-degrading ectoenzyme inhibitors
Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula I a :
wherein:
R 1 is an optionally substituted 4-, 5-...
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7375085 |
Melanocyte-stimulating hormone inhibitors
In the present specification is disclosed a melanocyte-stimulating hormone inhibitory composition which comprises, as the active ingredient, a di- or tripeptide derivative having a certain naphthyl...
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7375083 |
Pharmaceutical compositions for prevention of overdose or abuse
The invention relates to pharmaceutical compositions comprised of a chemical moiety attached to an active agent in a manner that substantially decreases the potential of the active agent to cause...
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7368421 |
Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in...
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7354905 |
Prodrugs of thrombin inhibitors
There is provided compounds of formula I,
R 1 O(O)C—CH 2 —(R)Cgl-Aze-Pab-R 2 I
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7351690 |
Knockout identification of target-specific sites in peptides
The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary...
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7348310 |
Synthetic methods for aplidine and new antitumoral derivatives, methods of making and using them
The invention relates to aplidine derivatives of the general formula:
which are useful for the treatment of tumors.
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7342095 |
Peptidomimetic inhibitors of STAT activity and uses thereof
The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics...
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7338939 |
Abuse-resistant hydrocodone compounds
The present invention decreases the potential for abuse of opioids, particularly hydrocodone, by covalent modification. The invention provides methods of delivering hydrocodone as conjugates that...
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7335722 |
Peptides used as angiotensin converting enzyme inhibitor and preparation process thereof
The invention discloses five peptides which can be used as angiotensin converting enzyme inhibitor. The subject invention also discloses a process for the preparation of the products having...
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7335644 |
Anti-hypertensive molecules and process for preparation thereof
The present invention relates to novel anti-hypertensive molecules. The present invention also provides a process for the preparation of novel antihypertensive molecules. The present invention...
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7335724 |
Peptides immunoreactive with autoantibodies from patients suffering from rheumatoid arthritis
The invention relates to a peptide derived from an antigen recognized by autoantibodies, which peptide is reactive with autoimmune antibodies from a patient suffering from rheumatoid arthritis. The...
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7316996 |
Bisacyloxypropylcysteine conjugates and the use thereof
The invention provides lipopeptide conjugates in which a cysteine that is double-substituted by a fatty acid is bonded by means of the carboxyl group to a highly soluble, physiologically compatible...
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7314929 |
Organoselenium compounds for cancer chemoprevention
A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be...
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7314867 |
Pharmaceutical composition comprising a retro-iverso isomer peptide
The present invention provides a pharmaceutical composition comprising a peptide selected from the group consisting of D-Pro D-Tyr D-Val D-Val, D-Pro D-Tyr D-Val, and D-Leu D-Thr D-Val as an active...
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7312306 |
Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators
The invention is directed to substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators, their use in wound healing and preventing platelet aggregation. Pharmaceutical...
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7304032 |
CD-10 activated prodrug compounds
The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide, a stabilizing group and,...
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7304037 |
Cytostatic conjugates with integrin ligands
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to α v β 3 integrin antagonists via preferred linking units which can be selectively...
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7288624 |
Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural...
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7288526 |
Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7285525 |
Suppression of immune response via inhibition of cathepsin S
Methods and products for suppressing a class II MI-IC-restricted immune response in a mammal, or in mammalian cells, are described. The methods depend upon inhibiting invariant chain proteolysis by...
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7279550 |
Irreversible cysteine protease inhibitors of legumain
Presented are compounds represented by the following general formulas (I) and (II), for inhibiting cysteine protease legumain for modulating associated disease states in subjects
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7276484 |
Dipeptide inhibitors of β-secretase
Dipeptide derived inhibitors of the β-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of Aβ peptide in a...
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7244721 |
Peptides as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7238668 |
Inhibition of lymphocyte adherence with CS-1-peptides and fragments thereof
The present invention relates to a method for inhibiting the adhesion of one cell to another comprising interfering with the interaction between the extracellular matrix receptor and its ligand. ...
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7235532 |
Angiogenic agents and their uses
The present invention relates to the use of a compound of formula I:
in which, A 1 is the radical corresponding to D- or L-Ser, A 2 is the radical corresponding to D- or L-Asp or Glu, A...
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7230074 |
Inhibitors of dipeptidyl-aminopeptidase type IV
Peptide inhibitors of dipeptidyl-aminopeptidase type IV (DP-IV) are provided. The peptide inhibitors have an isomeric purity of about 96–99 percent. The peptide inhibitors include one or more...
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7229777 |
Hairpin peptides with a novel structural motif and methods relating thereto
The invention is directed to a model system for structure-activity relationship analysis of peptide or protein molecules involved in important biological processes. Provided by the invention are...
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7226991 |
Phenylalanine derivatives
Disclosed herein are phenylalanine derivative compounds of the following formula
W—Y—(AA) n —Z
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7223837 |
Elongated and multiple spacers in activatible prodrugs
This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the...
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7214663 |
Tripeptide prodrug compounds
The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group....
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7208571 |
In vivo production of cyclic peptides
The present invention relates ti methods and compositions utilizing inteins to generated libraries of cyclic peptides in vivo.
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7192713 |
Stabilized compounds having secondary structure motifs
The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds...
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7186695 |
Treatment of arthritis with arsenoxide compounds
The present invention provides a method of treatment and/or prophylaxis of arthritis in a vertebrate comprising administering to said vertebrate in need of said treatment and/or prophylaxis a...
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7186859 |
Uses for amino acid anticonvulsants
The present invention is directed to the use of compounds of the formula:
for treating pain, in particular neuropathic pain, bipolar disease and migraine headaches.
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7183252 |
Indole peptidomimetics as thrombin receptor antagonists
The invention is directed to novel indole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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7179792 |
Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least one other active ingredient and the use of the product
The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I
in which the radicals have the meanings defined herein, or a pharmaceutically acceptable salt or...
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7179793 |
Anti-hypertensive dietary supplement
An anti-hypertensive fish protein hydrolysate is provided, wherein the fish is of the genus Salmo or Oncorhynchus , and wherein the fish protein hydrolysate comprises at least 1 peptide selected...
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7176185 |
Short peptide carrier system for cellular delivery of agent
A dipeptide or tripeptide carrier system for active agent delivery to cells has an N-terminus natural amino acid and an active agent covalently bonded to a side chain of one of the remaining amino...
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7169752 |
Compounds and compositions for prevention of overdose of oxycodone
The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to an opioid such as oxycodone in a manner that substantially decreases the potential of...
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7163918 |
Iodothyronine compositions
The present invention relates to compositions comprising thyroxine (T4) and triiodothyronine (T3). More specifically, the invention relates to thyroxine (T4) and triiodothyronine (T3) compositions...
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7163921 |
Peptide derivatives and medicinal compositions
The present invention to novel nociceptin receptor agonists which are peptide derivatives represented by the following general formula (1):
(in which A is alkylene, —CH 2 ) n CO— or a...
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7163923 |
Peptide deformylase activated prodrugs
This invention provides a method for inhibiting the growth of a microorganism that expresses Peptide Deformylase by contacting the microorganism with an effective amount of the compound described...
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7160554 |
Enhanced circulation effector composition and method
A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the...
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7157430 |
(Substituted)acyl dipeptidyl inhibitors of the ICE/CED-3 family of cysteine proteases
This invention is directed to novel (substituted) acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as...
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7153835 |
Anti-inflammatory peptides
Methods for inhibiting an inflammatory reaction in a mammal and pharmaceutical compositions are provided. The methods comprise administering to the mammal an effective amount of a peptide of the...
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7138104 |
Simultaneous imaging of cardiac perfusion and a vitronectin receptor targeted imaging agent
The present invention describes a method of concurrent imaging in a mammal comprising:
a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging...
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7132392 |
Inhibition of cell motility and angiogenesis by inhibitors of Grb2-SH2-domain
Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by...
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