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1. WO2018129200 - PAC1 RECEPTOR AGONISTS (MAXCAPS) AND USES THEREOF

Publication Number WO/2018/129200
Publication Date 12.07.2018
International Application No. PCT/US2018/012405
International Filing Date 04.01.2018
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07K 14/435 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
C07K 19/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
19Hybrid peptides
CPC
A61K 31/4985
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 38/2278
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
2278Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
A61K 47/60
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
A61K 47/65
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
Applicants
  • THE REGENTS OF THE UNIVERSITY OF CALIFORNIA [US]/[US]
  • THE UNITED STATES GOVERNMENT represented by THE DEPARTMENT OF VETERANS AFFAIRS [US]/[US]
Inventors
  • PISEGNA, Joseph R.
  • GERMANO, Patrizia M.
  • VU, John P.
Agents
  • HUNTER, Tom
  • WEAVER, Jeffrey K.
  • AUSTIN, James E.
  • VILLENEUVE, Joseph M.
  • SAMPSON, Roger S.
  • GRIFFITH, John F.
  • BERGIN, Denise S.
  • SCHOLZ, Christian D.
Priority Data
62/442,90605.01.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PAC1 RECEPTOR AGONISTS (MAXCAPS) AND USES THEREOF
(FR) AGONISTES DU RÉCEPTEUR PAC1 (MAXCAPS) ET LEURS UTILISATIONS
Abstract
(EN)
In certain embodiments novel PAC1 receptor agonists are provided wherein the agonists comprise a targeting sequence that binds to the PAC1 receptor and said targeting sequence is attached to an amino acid sequence comprising a fragment of the maxadilan amino acid sequence, wherein the targeting sequence comprises a full-length 38 amino acid PACAP peptide or an N-terminus fragment thereof containing the amino acid sequence HSDGIF, wherein said targeting sequence optionally comprises an amino acid insertion between residues 11 and 12 of said PACAP peptide or fragment thereof; and the fragment of the maxadilan amino acid sequence comprises a fragment of the maxadilan sequence effective to activate PAC1 signaling.
(FR)
Dans certains modes de réalisation, l'invention concerne de nouveaux agonistes du récepteur PAC1, les agonistes comprenant une séquence de ciblage qui se lie au récepteur PAC1 et ladite séquence de ciblage étant attachée à une séquence d'acides aminés comprenant un fragment de la séquence d'acides aminés maxadilan, la séquence de ciblage comprenant un peptide PACAP d'une longueur totale de 38 acides aminés ou un fragment N-terminal de celui-ci contenant la séquence d'acides aminés HSDGIF, ladite séquence de ciblage comprenant éventuellement une insertion d'acide aminé entre les résidus 11 et 12 dudit peptide PACAP ou un fragment de celui-ci; et le fragment de la séquence d'acides aminés maxadilan comprend un fragment de la séquence maxadilan efficace pour activer la signalisation PAC1.
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