Patent classifications
C07K7/16
TERLIPRESSIN-OCTADECANEDIOIC ACID CONJUGATE FOR VASOCONSTRICTIVE THERAPY
In an aspect, disclosed herein is a compound characterized by formula (FX1): A.sup.1-X.sup.1—X.sup.2-A.sup.2 (FX1); wherein: A.sup.1 is a carboxylic acid group, a carboxylate anion, or a carboxylate ester, X.sup.1 is a substituted or unsubstituted and saturated or unsaturated C.sub.1-C.sub.50 aliphatic group; X.sup.2 is a linker group selected from the group consisting of a direct bond, an organic group, -0-, —S—, —S(═O)—, —S(═O).sub.2—, —S—S—, —N═, ═N—, —N(H)—, —N═N—N(H)—, —N(H)—N═N—, —N(OH)—, —N(═O)—, and any combination thereof; and A.sup.2 is a peptide, the peptide being terlipressin or a substituted or unsubstituted derivative, a substituted or unsubstituted natural or synthetic analogue, a substituted or unsubstituted variant, a substituted or unsubstituted isomer, or a substituted or unsubstituted fragment of terlipressin.
Method of manufacturing a pharmaceutical composition
The present invention relates to crystalline forms of carbetocin, a method of their manufacture, and pharmaceutical compositions thereof.
Method of manufacturing a pharmaceutical composition
The present invention relates to crystalline forms of carbetocin, a method of their manufacture, and pharmaceutical compositions thereof.
Method of obtaining a binder to prepro-vasopressin or fragments thereof
Method of obtaining and/or verifying a binder to prepro-Vasopressin (SEQ ID NO. 1) or fragments thereof of at least 6 amino acids in length, including Copeptin (SEQ ID NO. 2), comprising at least one of the steps of: a) generating the binder using a developer comprising an amino acid sequence of at least 6 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); b) determining whether the binder is capable of binding to an amino acid sequence of at least 4 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); c) selecting and optionally isolating the binder from a plurality of binders which is capable of binding to an amino acid sequence contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); d) carrying out binding assays with the binder in order to determine the ex vivo stability of prepro-Vasopressin or fragments thereof of at least 6 amino acids in length, including Copeptin, in a biological sample; e) carrying out binding assays with the binder and another binder for comparison purposes in order to determine the concentration of prepro-Vasopressin or fragments thereof of at least 6 amino acids in length, including Copeptin, in a biological sample; wherein the C-terminal part consists of amino acids 138 to 164 of prepro-Vasopressin (SEQ ID NO. 1), in order to obtain a binder or a mixture of binders capable of binding to an epitope contained in an amino acid sequence corresponding to amino acids 138 to 163 but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1).
Method of obtaining a binder to prepro-vasopressin or fragments thereof
Method of obtaining and/or verifying a binder to prepro-Vasopressin (SEQ ID NO. 1) or fragments thereof of at least 6 amino acids in length, including Copeptin (SEQ ID NO. 2), comprising at least one of the steps of: a) generating the binder using a developer comprising an amino acid sequence of at least 6 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); b) determining whether the binder is capable of binding to an amino acid sequence of at least 4 amino acids in length contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); c) selecting and optionally isolating the binder from a plurality of binders which is capable of binding to an amino acid sequence contained in an amino acid sequence corresponding to the C-terminal part but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1); d) carrying out binding assays with the binder in order to determine the ex vivo stability of prepro-Vasopressin or fragments thereof of at least 6 amino acids in length, including Copeptin, in a biological sample; e) carrying out binding assays with the binder and another binder for comparison purposes in order to determine the concentration of prepro-Vasopressin or fragments thereof of at least 6 amino acids in length, including Copeptin, in a biological sample; wherein the C-terminal part consists of amino acids 138 to 164 of prepro-Vasopressin (SEQ ID NO. 1), in order to obtain a binder or a mixture of binders capable of binding to an epitope contained in an amino acid sequence corresponding to amino acids 138 to 163 but lacking amino acid 164 of prepro-Vasopressin (SEQ ID NO. 1).
METHOD FOR REFINING VASOPRESSIN
A method for refining vasopressin, including: subjecting a crude vasopressin solution to reversed-phase enrichment, reversed-phase salt conversion and reversed-phase purification sequentially using reversed-phase high performance liquid chromatography. The crude vasopressin solution is obtained by oxidizing a crude reduced vasopressin prepared by solid phase synthesis. A super water-resistant packing material is used in the reversed-phase high performance liquid chromatography.
LABELED OXYTOCIN AND METHOD OF MANUFACTURE AND USE
Disclosed are .sup.13N-oxytocin molecules, methods of manufacture of .sup.13N-oxytocin molecules and methods of use of .sup.13N-oxytocin molecules in the determination of the distribution and kinetics of .sup.13N-oxytocin molecules after craniofacial or other application methods.
LABELED OXYTOCIN AND METHOD OF MANUFACTURE AND USE
Disclosed are .sup.13N-oxytocin molecules, methods of manufacture of .sup.13N-oxytocin molecules and methods of use of .sup.13N-oxytocin molecules in the determination of the distribution and kinetics of .sup.13N-oxytocin molecules after craniofacial or other application methods.
THERAPEUTICS FOR PRETERM LABOR MANAGEMENT
Methods and compositions are provided for treating and preventing preterm labor using liposome encapsulated tocolytic agents, such as indomethacin. In certain aspects, targeted liposomes are provided that allow delivery of tocolytic agents directly to the uterus, such as by targeting to the oxytocin receptor.
THERAPEUTICS FOR PRETERM LABOR MANAGEMENT
Methods and compositions are provided for treating and preventing preterm labor using liposome encapsulated tocolytic agents, such as indomethacin. In certain aspects, targeted liposomes are provided that allow delivery of tocolytic agents directly to the uterus, such as by targeting to the oxytocin receptor.