C07K5/0827

Glycopeptide derivatives for use in the treatment and/or prevention and/or attenuation of fibrosis diseases

The present invention relates to a compound of the following formula (I), as well as to a pharmaceutical composition comprising at least one compound of following formula (I) and at least one pharmaceutically acceptable excipient, for use in the treatment and/or prevention and/or attenuation of fibrosis diseases, in particular excessive scars such as keloids or hypertrophic scars. ##STR00001##

TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
20200207809 · 2020-07-02 ·

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X):

##STR00001##

and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

Tripeptide epoxy ketone protease inhibitors

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

COMPOUNDS FOR PROTEASOME
20200071356 · 2020-03-05 ·

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Glycopeptide Derivatives For Use In The Treatment And/Or Prevention And/Or Attenuation of Fibrosis Diseases
20190388501 · 2019-12-26 · ·

The present invention relates to a compound of the following formula (I), as well as to a pharmaceutical composition comprising at least one compound of following formula (I) and at least one pharmaceutically acceptable excipient, for use in the treatment and/or prevention and/or attenuation of fibrosis diseases, in particular excessive scars such as keloids or hypertrophic scars.

##STR00001##

INHIBITORS OF HEPATITIS C VIRUS

Compounds of Formula I are disclosed

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As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

The present invention provides compounds of formula (I)

##STR00001## wherein X, L.sup.1 and R.sup.1 to R.sup.10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

NEW GROUP OF PEPTIDES FOR TREATING FEMALE SEXUAL DYSFUNCTION

The invention relates to the chemistry of peptides, pharmacology and medicine, and specifically to a new group of peptides having the property of stimulating sexual and genital function and having increased storage stability. For this purpose, peptides of general formula (I) are proposed: A-Thr-Lys-Hyp-B-C-D-X, in which A is 0, Met, Met(0), Thr, Ala, His, Phe, Lys, Gly; B is 0, Gly, Asp, Trp, Gin, Asn, Tyr, Hyp, Arg; C is 0, Arg, Phe, Tyr, Gly, His, Hyp, Lys; D is 0, Val, Gly, Tyr, Trp, Phe, His; X is OH, OCH.sub.3, NH.sub.2; where 0 is the absence of an amino acid residue, provided that if A0, then B and/or C and/or D0, if B0, then C and/or D0, excluding the tetrapeptides, as well as the peptides Phe-Thr-Lys-Hyp-Gly, Thr-Lys-Hyp-Hyp-Arg and Thr-Lys-Hyp-Arg-Gly. The invention also relates to pharmaceutical compositions containing the indicated peptides, as well as to the use of the above indicated compositions for the treatment of women with severely decreased libido or with totally absent libido, orgasmic dysfunction, sexual dysfunction not caused by organic disorders or diseases, HSDD, FSAD or FSIAD, and to a method of treating and/or preventing female sexual dysfunction.

MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS
20190263860 · 2019-08-29 ·

The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:

##STR00001##

which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

NOVEL COMPOUNDS
20190263858 · 2019-08-29 ·

The present invention relates to novel compounds which effectively inhibit the melanin synthesis in human melanocytes and are thus suitable for the treatment of senile lentigines, for smoothening skin color irregularities and/or for lightening natural skin color.