US 11,873,328 B2
GLP-1 analogues
Rajamannar Thennati, Gujarat (IN); Nishith Chaturvedi, Gujarat (IN); Vinod Sampatrao Burade, Gujarat (IN); Pradeep Dinesh Shahi, Gujarat (IN); Muthukumaran Natarajan, Gujarat (IN); Ravishankara Madavati Nagaraja, Gujarat (IN); Rishit Mansukhlal Zalawadia, Gujarat (IN); Vipulkumar Shankarbhai Patel, Gujarat (IN); Kunal Pandya, Gujarat (IN); Brijeshkumar Patel, Gujarat (IN); Dhiren Rameshchandra Joshi, Gujarat (IN); Krunal Harishbhai Soni, Gujarat (IN); and Abhishek Tiwari, Gujarat (IN)
Assigned to SUN PHARMACEUTICAL INDUSTRIES LIMITED, Maharashtra (IN)
Filed by Sun Pharmaceutical Industries Limited, Maharashtra (IN)
Filed on Aug. 1, 2022, as Appl. No. 17/816,577.
Application 17/816,577 is a continuation of application No. 16/376,190, filed on Apr. 5, 2019, granted, now 11,447,535.
Claims priority of application No. 201821013109 (IN), filed on Apr. 5, 2018; application No. 201821040468 (IN), filed on Oct. 26, 2018; and application No. 201821040474 (IN), filed on Oct. 26, 2018.
Prior Publication US 2022/0402991 A1, Dec. 22, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 14/605 (2006.01); A61K 9/00 (2006.01); A61P 3/10 (2006.01); A61P 3/04 (2006.01); A61K 38/00 (2006.01)
CPC C07K 14/605 (2013.01) [A61K 9/0053 (2013.01); A61P 3/04 (2018.01); A61P 3/10 (2018.01); A61K 38/00 (2013.01)] 11 Claims
 
1. A polypeptide having the amino acid sequence:
(SEQ ID NO: 15)
H-X2-X3-X4-G-T-F-T-S-D-V-S-S-Y-L-X16-G-Q-A-A-X21-
E-F-X24-A-W-L-V-R-G-R-G-X33-X34
wherein X2 is Ser, Ser(OMe), Aib, Ala, Gly, Val, Leu, Ile, (1-amino C3-8 cycloalkyl) carboxylic acid, Trp or Thr;
X3 is absent or Gin;
X4 is Gin or Glu;
X16 is Glu or Asp;
X24 is Ile or Val or Leu;
X33 Leu, Ile, Tyr or absent;
X34 is Ser, Lys, Ala or absent; and
X21 is Lys wherein the side chain amino (ε amino) group of Lys is acylated with a moiety:
{-U-W-Y-Z
wherein
U is —C(O)-M-NH—; wherein the carbonyl is attached to the Lys ε amino and M is a C5-10 alk chain interrupted with 1, 2 or 3 oxygen atoms;
W is —C(O)—N(R1)—C2-5alk-N(R1)—, —C(O)—C(CH3)2—N(R2)—; or

OG Complex Work Unit Chemistry
wherein R1, R2 and R3 are independently hydrogen or C1-3 alkyl and the carbonyl in W is attached to the N in U;
Y is —C(O)—(CH2)m—CH(COOH)NH— wherein m is an integer selected from 1 to 2 and — is point of attachment with the group Z; and
Z is —C(O)—(CH2)n—COOH or —C(O)—(CH2)n—CH3 wherein n is an integer from 10 to 20.