C07K5/0815

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

The present invention provides compounds of formula (I)

##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 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.

Systems Chemico-Pharmacology Drugs and Methods of Use

As new class of drugs designated systems chemico-pharmacology drugs (SCPD) is disclosed. SCPDs work by targeting a druggable biomolecular site (the first target), resulting in a significant change in the properties of the first target. In the process, the SCPD itself is chemically modified. Subsequently, the resulting modified SCPD interacts with a second target, which is also modified in a manner that is beneficial for the patient.

Peptide macrocycles against <i>Acinetobacter baumannii</i>

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.

Tryptase Activity Measurement Substrate

An object of the present invention is to provide a method for measuring tryptase activity in a blood sample accurately and rapidly by a convenient operation in order to accurately evaluate the state of a disease whose state involves mast cells. The present invention enables tryptase activity in a blood sample to be directly measured without the pretreatment, such as purification or concentration, of the blood sample, using a substrate for measuring tryptase activity, comprising a tripeptide C-terminally linked through a peptide bond to a dye label, selected from the following formulas (1) to (3): (1) Lys-Ala-Arg-X, (2) Ala-Ala-Arg-X, and (3) Abu-Ala-Arg-X (wherein X represents a dye label whose fluorescence characteristics or color development characteristics change upon the cleavage of the peptide bond with Arg, and Abu represents 2-aminobutyric acid).

Cyanine dyes

The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.

MITOCHONDRIA-TARGETING PEPTIDES
20230146515 · 2023-05-11 ·

Disclosed are non-natural peptides useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

CANCER IMAGING AGENT
20170368208 · 2017-12-28 ·

The present disclosure relates to imaging agent formulations, methods for preparing imaging agent formulations and methods for using the same. The present disclosure also relates to kits for imaging agent formulations.

PEPTOID-CONTAINING PERSONAL LUBRICANT
20230173145 · 2023-06-08 ·

A contraceptive device is provided which includes a (preferably elastomeric) surface; and a lubricant applied to the surface. The lubricant includes (a) a lubricious medium, and (b) a pharmaceutically effective amount of a peptoid disposed in said lubricious medium. The antimicrobial peptoid may impart protection against some common sexually transmitted diseases, while also imparting spermicidal activity to the lubricious medium and contraceptive device.

Process for the manufacture of degarelix and its intermediates

The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: (P.sub.1)AA.sub.1-AA.sub.2-AA.sub.3-AA.sub.4(P.sub.4)-AA.sub.5-AA.sub.6(P.sub.6)-AA.sub.7-AA.sub.8(P.sub.8)-AA.sub.9-AA.sub.10-NH.sub.2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P.sub.1 is an amino protecting groups; preferably acetyl; P.sub.4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P.sub.6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P.sub.8 is an amino protecting group.