IP Library Granted Patent US 11,136,346
Granted Patent B2
US 11,136,346 · App. 16/878,461 · Granted Oct 5, 2021

Asymmetric auxiliary group

Inventors: Mamoru Shimizu (Arlington, MA); Takeshi Wada (Kashiwa, JP)
Assignee: WAVE LIFE SCIENCES LTD.
C07H23/00C07B53/00C07D207/08C07D405/04C07D473/18C07D473/34C07F7/0812C07H1/00C07H19/10C07H19/11C07H19/207C07H19/213C07H21/04
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Quick Facts
Patent No.
US 11,136,346
App. No.
16/878,461
Granted
Oct 5, 2021
Kind
B2
Abstract

To provide a chiral reagent or a salt thereof. The chiral reagent has following chemical formula (I). In the formula (I), G 1 and G 2 are independently a hydrogen atom, a nitro group (—NO 2 ), a halogen atom, a cyano group (—CN), a group of formula (II) or (III), or both G 1 and G 2 taken together to form a group of formula (IV).

Claims (44)

1. A compound, which is represented by formula (Va) or (Vb):

wherein:

G 1 is a hydrogen atom, a nitro group, a halogen atom, a cyano group, or a group of formula (II), (III) or (V);

G 2 is a nitro group, a halogen atom, a cyano group, or a group of formula (II), (III) or (V); or

both G 1 and G 2 are taken together to form a group of formula (IV);

wherein formula (II) is:

and

wherein G 21 to G 23 are independently a hydrogen atom, a nitro group, a halogen atom, a cyano group or C 1-3 alkyl group;

wherein formula (III) is:

and

wherein G 31 to G 33 are independently C 1-4 alkyl group, C 1-4 alkoxy group, C 6-14 aryl group, C 7-14 aralkyl group, C 1-4 alkyl C 6-14 aryl group, C 1-4 alkoxy C 6-14 aryl group, or C 6-14 aryl C 1-4 alkyl group;

wherein formula (IV) is:

and

wherein G 41 to G 46 are independently a hydrogen atom, a nitro group, a halogen atom, a cyano group or C 1-3 alkyl group;

wherein formula (V) is:

and

wherein G 51 to G 53 are independently a hydrogen atom, a nitro group, a halogen atom, a cyano group, C 1-3 alkyl group or C 1-3 alkyloxy group;

G 3 and G 4 are independently a hydrogen atom, C 1-3 alkyl group, C 6-14 aryl group, or G 3 and G 4 are taken together to form a heteroatom-containing ring that has 3 to 16 carbon atoms;

G 5 is a protective group of a hydroxyl group;

R 2 is hydrogen, halogen, alkyl-Y 1 —, alkenyl-Y 1 —, alkynyl-Y 1 —, aryl-Y 1 —, or heteroaryl-Y 1 —;

Y 1 is O;

R 3 is a group represented by —CH 2 —, —(CH 2 ) 2 —, —CH 2 NH—, or —CH 2 N(CH 3 )—; and

Bs is a group selected from the groups represented by following formula (VI) to (XI) or derivatives thereof:

2. The compound of claim 1 , wherein G 3 and G 4 are taken together to form a heteroatom-containing ring that has 3 to 16 carbon atoms.

3. The compound of claim 1 , wherein the compound is represented by formula V(a′):

4. The compound of claim 3 , wherein G 1 is a hydrogen atom.

5. The compound of claim 4 , wherein Bs is selected from:

wherein each of R 8 , R 9 and R 10 is independently C 1-10 alkyl, C 6 -C 10 aryl, C 6 -C 10 aralkyl, or C 6 -C 10 aryloxyalkyl.

6. The compound of claim 5 , wherein G 2 is a group of formula (III).

7. The compound of claim 6 , wherein R 2 is hydrogen.

8. The compound of claim 6 , wherein R 2 is —F.

9. The compound of claim 6 , wherein R 2 is alkyl-Y 1 —.

10. The compound of claim 5 , wherein G 2 is a group of formula (V).

11. The compound of claim 10 , wherein R 2 is hydrogen.

12. The compound of claim 10 , wherein R 2 is —F.

13. The compound of claim 10 , wherein R 2 is alkyl-Y 1 —.

14. The compound of claim 5 , wherein G 1 and G 2 are taken together to form a group of formula (IV).

15. The compound of claim 14 , wherein R 2 is hydrogen.

16. The compound of claim 14 , wherein R 2 is —F.

17. The compound of claim 14 , wherein R 2 is alkyl-Y 1 —.

18. The compound of claim 1 , wherein G 2 is a group of formula (II), (III) or (V), or both G 1 and G 2 are taken together to form a group of formula (IV).

19. The compound of claim 2 , wherein G 2 is a group of formula (II), (III) or (V), or both G 1 and G 2 are taken together to form a group of formula (IV).

20. A compound selected from 1a, 1b, 2a, 2b, 3a, 3b, 4a, 4b, 5a, 5b, 6a, 6b, 7a, 7b, 8a, 8b, 9a, 9b, 10a, 10b, 11a, 11b, 12a, 12b, 13a, 13b, 14a, 14b, 15a, 15b, 16a, 16b, 17a, 17b, 18a, 18b, 19a, 19b, 20a, 20b, 21a, 21b, or 24a, wherein DMTr represents a 4,4′-dimethoxytrityl group and TOM represents a triisopropylsiloxymethyl group:

.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2020
From: SHIMIZU, MAMORU; WADA, TAKESHI
To: WAVE LIFE SCIENCES JAPAN, INC.
Reel/Frame 053548/0758 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2020
From: WAVE LIFE SCIENCES JAPAN, INC.
To: WAVE LIFE SCIENCES LTD.
Reel/Frame 053548/0788 →
CHANGE OF NAME Recorded Aug 20, 2020
From: WAVE LIFE SCIENCES JAPAN
To: WAVE LIFE SCIENCES JAPAN, INC.
Reel/Frame 053558/0384 →
Continuity (5)
Continuation 16182302 · Nov 6, 2018
Continuation 15294602 · Oct 14, 2016
Continuation 14414604
Provisional Application 61671652 · Jul 13, 2012
Related Publication 20200385420A1 · Dec 10, 2020
Cited By (11)
US 12,391,942 US 12,403,156 US 12,428,442 US 12,435,105 US 12,473,321 US 12,486,505 US 12,552,743 US 12,583,883 US 12,590,115 US 12,637,672 US 12,674,168