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RE40987 |
Cyclosporin with improved activity profile
The invention relates to a novel cyclosporin, the pharmaceutical use thereof and a pharmaceutical composition containing it.
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7611711 |
VEGFR-3 inhibitor materials and methods
The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated...
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7605126 |
Acylaminoheteroaryl hepatitis C virus protease inhibitors
The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which inhibit serine protease activity, particularly the...
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7592315 |
Peptide viral entry inhibitors
The present invention provides, inter alia, peptide compositions and methods for treating and preventing Flaviviridae virus (e.g., hepatitis C virus) infections.
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7589170 |
Synthesis of cyclic peptides
This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in...
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7582605 |
Phosphorus-containing hepatitis C serine protease inhibitors
The present invention relates to phosphorus-derived compounds of Formula I or Formula II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof, which inhibit serine protease activity,...
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7576057 |
Cyclic peptides
The invention relates to novel cyclic peptide derivatives of general formula (I):
wherein A, B, R 1 and R 2 are as defined in the specification, pharmaceutically acceptable salts thereof, and...
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7569541 |
Method for synthesizing conformationally constrained peptides, peptidomimetics and the use thereof as synthetic vaccines
The present invention relates to methods for synthesizing conformationally constrained peptides and cyclic peptidomimetics obtainable by these methods which are conformationally constrained due an...
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7560429 |
Orodispersible dosage forms of desmopressin acetate
Good bioavailability of desmopressin can be obtained by means of an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an...
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7557088 |
Methods and compositions for treating conditions
The invention relates to compositions that can be used to treat, prevent, and modulate pain, inflammation, and metabolic processes in various organisms including plants and animals. Such...
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7557082 |
Treatment with cyclosporin A
Disclosed herein is a method comprising administering cyclosporin A topically to an eye of a person for the purpose of treating or preventing loss of vision from keratoconus.
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7550431 |
Spatially-defined macrocycles incorporating peptide bond surrogates
Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit...
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7541018 |
Treatment process using somatostatin analogues
In one embodiment, a method for treating a cancerous disease is provided which includes characterizing a disease by an overexpression of one or more somatostatin receptors, and exposing the one or...
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7538189 |
Methods of making deuterated cyclosporin analogs
Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The...
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7538097 |
Inhibition of antigen presentation with poorly catabolized polymers
Methods to prevent the rejection of immunogenic tissues in an animal by administering a non-immunogenic, poorly catabolized molecule in an amount sufficient to inhibit an immune response are...
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7538084 |
Cyclosporins
The compounds of the present invention are represented by the chemical structure found in Formula I:
Formula I
where A is an amino acid of Formula II:
or a pharmaceutically acceptable...
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7531507 |
Acylated nonadepsipeptides containing pyridyl alanine residues
The invention relates to nonadepsipeptides and processes for their preparation, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial...
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7521529 |
Differentially protected orthogonal lanthionine technology
The present invention provides a method of synthesizing an intramolecularly bridged polypeptide comprising at least one intramolecular bridge. The present invention further provides a method of...
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7521421 |
Deuterated cyclosporine analogs and methods of making the same
Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The...
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7521420 |
Macrocyclic antagonists of the motilin receptor
The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n...
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7517854 |
Melanocortin receptor agonists
Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R 1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity...
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7517853 |
Somatostatin-dopamine chimeric analogs
The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.
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7501393 |
Pharmaceutical compositions comprising cyclosporins
A composition is described herein comprising cyclosporin A, polysorbate 80, a polyoxyethylene stearate, and an oil; wherein the composition is an emulsion which is ophthalmically acceptable....
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7498302 |
Disulfide prodrugs and linkers and stabilizers useful therefor
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming...
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7498025 |
Targeted bifunctional molecules and therapies based thereon
Targeted bifunctional molecules and methods for their use are provided. The subject targeted bifunctional molecules are conjugates of a drug moiety and a targeting moiety, where these two moieties...
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7476653 |
Macrocyclic modulators of the ghrelin receptor
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue...
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7473761 |
Somatostatin analogues
The invention provides cyclo[{4-(NH 2 —C 2 H 4 —NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof,...
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7473760 |
Cyclic peptide compositions for treatment of sexual dysfunction
A cyclic peptide of the structural formula:
or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 5 , R 6 , m, n and p are as defined. Further provided are compositions for...
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7473681 |
Kahalalide F
Formulations and uses of kahalalide F.
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7470664 |
HCV NS3 protease inhibitors
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or...
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7468419 |
Cyclosporin derivatives for the treatment of immune disorders
The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof:
wherein
A is of the formula:
where Q, W, X,...
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7462594 |
Peptide-like compounds that inhibit coronaviral 3CL and flaviviridae viral proteases
This invention relates to treating an infection with a virus using protease inhibitors. Examples of the protease inhibitors include compounds of formula (II). Each variable is defined in the...
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7452865 |
Antagonistic analogs of GH RH (2003)
There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH 2 . These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore...
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7452862 |
Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists
Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle...
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7452552 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Pharmaceutical compositions for lipophilic drugs
Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in...
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7449544 |
p21 peptides
The present invention relates to p21 derived peptides capable of inhibiting CDK/cyclin complexes, particularly cyclins A or E/CDK2, by modifying the interaction with their substrates. The peptides...
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7446094 |
Cytotoxic depsipeptides
Compounds of general formula (I) wherein R 1 , R 2 , R 3 are as defined and R 4 groups are each independently selected from NR 2 , O and S; are of use in treatment of cancers.
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7446093 |
Cerebrospinal and vascular pharmaceutical composition and process for preparing the same
A cyclosporin-containing pharmaceutical preparation for cerebrospinal or vascular application is disclosed, comprising (1) at least one cyclosporin, and (2) DMSO.
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7442683 |
Cyclic peptide
A novel cyclic peptide having an antifungal activity, its pharmacologically acceptable salts and antifungal medicinal compositions containing the same.
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7439227 |
Use of selected cyclosporins for the treatment of hepatitis C infection
This invention relates to the use in the treatment of HCV infection, either as single active agents or in combination with another active agent, of a cyclosporin having increased cyclophilin...
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7435716 |
Compounds pharmaceutical compositions and methods for treatment of bacteremia and/or septicemia
Novel conjugates of bacterial outer membrane binding peptides, preferably having bacterial sensitization activity, and immune cells chemotactic peptides, and pharmaceutical compositions containing...
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7429565 |
Antiviral phosphonate analogs
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such...
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7425537 |
SH2 domain binding inhibitors
Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R 1 is a lipophile; R 2 , in combination with the phenyl ring, is a phenylphosphate mimic...
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7419954 |
Staphylococcus peptides for bacterial interference
The present invention provides a cyclic peptide comprising the structure:
wherein X is selected from the group consisting of an amino acid, an amino acid analog, a peptidomimetic and a...
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7417025 |
Use of poly-α2,8-sialic acid mimetic peptides to modulate NCAM functions
The invention relates to the use of a peptide consisting of 5 to 30 amino acid residues, preferably 9 to 15, most preferably about 12 amino acid residues, said peptide comprising a B epitope of a...
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7417024 |
Template-fixed peptidomimetics as inhibitors of serine proteases
Template-fixed β-hairpin peptidomimetics of the general formulae (I), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain...
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7414023 |
Peptide ligands for prostate specific antigen
The present invention relates to novel peptide ligands for prostate specific antigen (PSA) binding specifically with it and enhancing its enzyme activity, to a process for preparation of these...
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7408025 |
Lipopeptides as antibacterial agents
The present invention relates to novel lipopeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial...
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7405201 |
Antibacterial macrocycles
The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions comprising them, and their use in the treatment of diseases in...
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7405200 |
Use of oxytocin for the preparation of a pharmaceutical composition against cancer in situ and cervicitis
A method of treating cancer in situ and cervicitis is disclosed. A pharmaceutical composition comprising at least one substance with oxytocin activity against cancer in situ and cervicitis and...
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