- Patent Number:
12187,668
- Appl. No:
17/673269
- Application Filed:
February 16, 2022
- Abstract:
Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
- Inventors:
Alzheon, Inc. (Framingham, MA, US)
- Assignees:
Alzheon, Inc. (Framingham, MA, US)
- Claim:
1. A compound having the structural formula (IV-1): [chemical expression included] or a pharmaceutically acceptable salt thereof, wherein Rb 1 is selected from hydrogen, —(CH 2) 1-3 —C(O) OH, —(CH 2) 1-3 —C(O)O(C 1 -C 3 alkyl), —C(O)—[CH(R A)] 1-2 —NH—R B , and —C(O)—[CH(R A)] 1-2 —NH—C(O)—[CH(R A)] 1-2 —NH—R B ; each R 7 and each R 8 is independently selected from —H, —NH 2 , —NR a R b —C(O)NH 2 , —C(O)NR a R b , —(C(R x)(R y)) n NH 2 , —(C(R x)(R y)) n NR a R b , —(C(R a)(R b)) n C(O)NH 2 , —(C(R a)(R b)) n C(O)NR a R b , —OH, —(C(R a)(R b)) n OH, —CO 2 H, —(C(R a)(R b))nCO 2 H, —SO 3 H, —(C(R a)(R b)) n SO 3 H, deuterium, halogen, alkyl, alkoxy, alkenyl, alkynyl, cyano, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl; each R a is hydrogen or optionally substituted alkyl; each R b is selected from hydrogen, alkyl substituted with a carboxyl or a carboxylate, and an amino acid or a dipeptide, wherein the amino acid or the dipeptide is bound to the nitrogen atom in R 3 through a carboxy group; or R a and R b are taken together to form an optionally substituted heterocyclyl; each R x and R y are independently a hydrogen or a C 1 -C 6 alkyl group n is 1 or 2; each R A is independently selected from hydrogen or a side group of a natural or unnatural amino acid; and R B is selected from hydrogen and a protecting group.
- Claim:
2. The compound of claim 1 , wherein each R 7 and each R 8 is hydrogen.
- Claim:
3. The compound of claim 1 , wherein: each R A , if present, is selected from —CH 3 , —CH 2 OH, —(CH 2) 4 —NH 2 , —CH 2 —CH(CH 3) 2 , —(CH 2) 2 —S(O) 2 —CH 3 , —CH 2 —C(O)—NH 2 , —CH 2 —C(O)OH, —CH(CH 3)OH, —CH(CH 3) 2 , benzyl, 1H-imidazol-4-yl-methyl, 4-hydroxybenzyl, and 1H-indolyl-3-ylmethyl; and R B is selected from hydrogen and Cbz.
- Claim:
4. A method of treating Alzheimer's disease comprising the step of administering to a patient in need thereof a compound of claim 1 .
- Claim:
5. The method of claim 4 , wherein the patient is ApoE4-positive.
- Claim:
6. The method of claim 5 , wherein the patient is homozygous for ApoE4.
- Claim:
7. The compound of claim 1 , wherein the compound is selected from [chemical expression included] or a pharmaceutically acceptable salt of any of the foregoing.
- Patent References Cited:
10590070 March 2020 Kocis et al.
11053192 July 2021 Kocis et al.
2004/0198832 October 2004 Szarek et al.
2005/0038117 February 2005 Kong et al.
2006/0135403 June 2006 Gervais et al.
2007/0010573 January 2007 Kong et al.
2008/0146642 June 2008 Kong et al.
2009/0004140 January 2009 Qiu et al.
2011/0144111 June 2011 Kim et al.
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1999/033781 July 1999
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2009/019534 February 2009
2017/027582 February 2017
- Other References:
Contineanu, Structure and spectral characteristics of the benzene-2,2-diazo-quinone-4-sulphonic acid. Revista de Chimie. Jul. 2001;52(7-8):365-370. cited by applicant
Pilichowski et al., Sultones Bicycliques Pontees Synthese et Reactivite. Tetrahedron. 1977;33(10):1113-1118. cited by applicant
- Primary Examiner:
Muresan, Ana Z
- Attorney, Agent or Firm:
McCarter & English, LLP
DeGrazia, Michael J.
- Accession Number:
edspgr.12187668
Processing Request
No Comments.