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1. WO2022006340 - ALK5 INHIBITORS, CONJUGATES, AND USES THEREOF

Publication Number WO/2022/006340
Publication Date 06.01.2022
International Application No. PCT/US2021/039995
International Filing Date 30.06.2021
IPC
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07K 5/062 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
062the side chain of the first amino acid being acyclic, e.g. Gly, Ala
C07K 5/065 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
065the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
C07K 5/093 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
093the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C07K 5/113 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
10Tetrapeptides
113the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C07K 7/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
7Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04Linear peptides containing only normal peptide links
06having 5 to 11 amino acids
CPC
A61K 47/6803
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
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
C07K 5/06052
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06017and aliphatic
06034the side chain containing 2 to 4 carbon atoms
06052Val-amino acid
C07K 5/06078
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06078and aromatic or cycloaliphatic
C07K 5/0819
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
0819with the first amino acid being acidic
Applicants
  • SILVERBACK THERAPEUTICS, INC. [US]/[US]
Inventors
  • SMITH, Sean W.
  • BAUM, Peter R.
  • DUBOSE, Robert
  • ODEGARD, Valerie
  • TAN, Philip
  • THOMPSON, Peter A.
  • STEVENS, Brenda
  • HUNT, Kevin W.
Agents
  • HARWOOD, Eric, A.
  • OBEIDAT, Baha, A.
  • ADRA, Bilal H.
  • KUMABE, Blake, K.
  • SAHACHARTSIRI, Bobby
  • SOLTANI, Bobby, B.
  • ZENTZ, Bradley, J.
  • SARGEANT, Brooke
  • QUIST, Brooke, W.
  • ROTH, Carol, J.
  • EIDT, Chandra, E.
  • O'BRIEN, Daniel
  • CARLSON, David, V.
  • CONLEE, David, C.
  • STARK, Duncan
  • TARLETON, E., Russell
  • SUN, Eileen, S.
  • GERTZ, Glenda, A.
  • HAN, Hai
  • TALBERT, Hayley, J.
  • KHANNA, Hemant
  • BARRETT, Jared, M.
  • DANLEY, Jeffrey, E.
  • SAKOI, Jeffrey, M.
  • SEO, Jeong Hee
  • BAUNACH, Jeremiah, J.
  • ZHANG, Jianping
  • MORGAN, John, A.
  • WAKELEY, John, J.
  • COE, Justin, E.
  • HENCKEL, Karen, M.
  • HEFTER, Karl, A.
  • HERMANNS, Karl, R.
  • MORGAN, Kevan, L.
  • COSTANZA, Kevin, S.
  • COOPER, Michael, P.
  • LECOINTE, Michelle M.
  • BENDEMIRE, Paul, D.
  • LIN, Qing
  • HALLER, Rachel, A.
  • WEBB, Samuel, E.
  • LIU, Shi
  • LEEK, Shoko, I.
  • ROSENMAN, Stephen, J.
  • LAWRENZ, Steven, D.
  • ABEDI, Syed
  • SHEWMAKE, Thomas, A.
  • BOLLER, Timothy, L.
  • LIGON, Toby, J.
  • LI, Yiheng
  • SAKOI, Zachary, M.
Priority Data
63/047,24601.07.2020US
63/090,16809.10.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) ALK5 INHIBITORS, CONJUGATES, AND USES THEREOF
(FR) INHIBITEURS D'ALK5, CONJUGUÉS ET LEURS UTILISATIONS
Abstract
(EN) ALK5 inhibitor compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.The disclosed compoundsand conjugates are useful, among other things, in the treating of cancer and fibrosis and modulating ALK5.
(FR) L'invention concerne des composés inhibiteurs d'ALK 5, des conjugués et des compositions pharmaceutiques destinés à être utilisés dans le traitement d'une maladie, telle que le cancer. De plus, l'invention concerne des composés incorporés dans un conjugué avec une construction d'anticorps. Les conjugués et les composés selon l'invention sont utiles, entre autres, dans le traitement du cancer et de la fibrose et la modulation de l'ALK 5.
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