IP Library › Granted Patent US 12,617,783
Granted Patent B2
US 12,617,783 · App. 19/094,187 · Granted May 5, 2026

Heterocyclic GLP-1R agonists

Inventors: Xiaodong Wang (Millbrae, CA); Thorsten A. Kirschberg (San Carlos, CA); Johannes H. Voigt (San Carlos, CA); Thomas Butler (Redwood City, CA); Ravindra B. Upasani (San Jose, CA); Yongli Su (Foster City, CA); Thu Phan (Fremont, CA); James T. Palmer (Warrandyte, AU); Neil Howard Squires (San Francisco, CA); Yeyu Cao (Foster City, CA); Solomon B. Ungashe (Sunnyvale, CA); Nan-Horng Lin (Vernon Hills, IL); Mini Balakrishnan (San Mateo, CA); Petr Jansa (Foster City, CA); Satish Goud Pappali (Sunnyvale, CA)
Assignee: BIOMEA FUSION, INC.
C07D451/00A61K31/437A61K31/439A61K31/46A61K31/4709A61K31/496A61K31/502A61K31/5377A61K31/5386A61K31/541A61K31/55A61K31/551A61K31/675C07D471/04C07D471/18C07D487/04C07D498/18C07D519/00C07F9/6561
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Quick Facts
Patent No.
US 12,617,783
App. No.
19/094,187
Granted
May 5, 2026
Kind
B2
Abstract

Disclosed herein are heterocyclic compounds that activate GLP-1R pathways. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the GLP-1R agonists are disclosed, alone or in combination with other therapeutic agents, for the treatment of diabetes, obesity, and other diseases or conditions dependent on GLP-1R pathways.

Claims (384)

1 . A compound selected from the group consisting of:

TABLE 1′

Com-

pound

ID

Structure

32

C49H48F2N10O5

36

C49H48F2N10O5

114

C48H46F2N10O5

115

C45H42F2N10O6

116

C49H48F2N10O6

117

C47H45F2N9O6

118

C47H46F2N12O3

119

C48H45FN10O5

121

C49H48F2N10O6

122

C46H42F2N10O6

123

C48H46F2N10O5

124

C48H45FN10O5

125

C47H45F2N9O6

126

C49H46F2N10O5

127

C49H47FN10O5

128

C48H48F2N12O3

129

C47H44F2N10O5S

131

C54H57F2N11O6

132

C54H57F2N11O6

134

C49H48F2N10O5

135

C49H47F2N11O5

136

C48H44F2N10O6

137

C48H47F2N9O3

138

C48H49F2N9O4

139

C46H45F2N11O5S

140

C48H48F2N10O5

201

C49H51F2N9O6S

203

C52H59FN9O6P

204

C51H53F2N9O6S

205

C50H54F2N10O6S

206

C46H45F2N11O5S

208

C47H44F2N10O5

209

C48H47F2N11O5

210

C48H47F2N11O5

211

C48H47F2N11O5

212

C48H47F2N11O5

213

C49H46F2N10O5

214

C49H46F2N10O5

215

C49H46F2N10O5

216

C50H55FN9O6P

217

C48H47F2N11O5

218

C48H47F2N11O5

219

C50H45F2N11O4

220

C49H46F2N10O6

221

C47H44F2N10O6

222

C49H48ClFN10O6

223

C48H49FN806

224

C49H47F3N10O6

225

C48H47F2N11O6

226

C49H46F2N10O6

227

C49H46F2N10O6

228

C50H51FN10O6

229

C48H47F2N11O5

230

C49H46ClFN10O6

231

C48H47F2N11O6

232

C48H47F2N11O6

233

C49H48F2N10O6

235

C49H47F3N10O5

236

C48H46F3N11O5

237

Isomer 1

C48H44F2N10O5

238

C48H47F2N11O6

239

C48H47F2N11O6

240

C50H53F2N9O4

241

C50H53F2N9O5

242

C49H45F3N10O6

243

C50H53F2N9O4

244

C49H51F2N9O4

246

C51H53F2N9O4

302

C49H49FN10O5

305

C50H51FN10O5

306

C46H45F2N11O5S

307

C46H45F2N11O5S

308

C49H48ClFN10O5

309

C49H46F4N10O5

310

C49H46F4N10O5

311

C48H47F2N11O5

312

C48H47F2N11O5

313

C48H47F2N11O5

318

Isomer 1a

C50H48F2N10O5

319

Isomer 1b

C50H48F2N10O5

323

C49H47FN10O5

324

C48H47F2N11O6

406

C48H46F2N10O5

410

C49H46F2N10O5

412

C48H47F2N9O6

413

C48H46F2N10O5

415

C50H48F2N10O5

416

C48H48F2N10O5

417

C49H50F2N10O4

418

C48H46F2N10O5

419

C48H46F2N10O5

420

C48H46F2N10O5

421

C48H48F2N10O5

422

C48H47F2N9O6

423

C48H46F2N10O5

424

C50H48F2N10O5

425

C48H46F2N10O5

426

C50H48F2N10O5

427

C50H50F2N10O5

428

C49H51F2N9O6S

429

C49H48F2N10O6

431

C49H48F2N10O6

432

C48H50F2N10O4

433

C50H50F2N10O5

434

C50H50F2N10O5

435

C50H50F2N10O5

436

C48H44F2N10O5

437

C49H44F2N10O5

501

C51H59FN9O6P

502

C46H44F2N10O5

503

C48H48F2N10O6S

504

C48H48F2N10O6S

505

C47H46F2N10O5

506

C49H55FN9O6P

507

C49H47F3N10O5

508

C47H48F2N10O6S

509

C50H48F2N10O5

510

C49H45F2N11O5

511

C49H47F3N10O5

512

C49H47F3N10O5

515

C49H47F3N10O5

516

C49H46F2N10O5

518

C49H50F2N10O5

519

C49H46F2N10O5

521

C48H46F2N10O5

522

C50H50F2N10O5

523

C50H50F2N10O5

525

C48H48F2N10O6S

526

C46H44F2N10O7S

527

C49H50F2N10O6S

528

C49H46F2N10O5

529

C49H46F2N10O5

532

C50H50F2N10O5

533

C47H46F2N10O6S

534

C47H46F2N10O6S

535

C48H47F2N11O6S

536

C48H48F2N10O7S

537

C51H52F2N10O5

542

C49H46F2N10O5

545

C53H54FN9O6

602

C50H49F2N9O6S

604

C49H48F2N10O6S

605

C50H49F2N906S

606

C49H48F2N10O5

607

C47H46F2N10O5

608

C49H48F2N10O6S

609

C49H48F2N10O6S

610

C51H47F2N9O5

611

C51H53F2N9O6

612

C53H55ClFN9O6

613

C50H50F2N10O5

614

C51H47F2N9O5

615

C50H49F3N10O5

616

C49H49F2N11O4

617

C51H50F2N10O6

618

C49H47F3N10O5

619

C49H47F3N10O6

701

C50H49F3N10O5

702

C49H50F2N10O5

703

C49H50F2N10O5

704

C53H54FN9O6

705

C49H47F3N10O6

706

C49H47F3N10O6

707

C50H49F3N10O5

708

C49H47F3N10O5

709

C49H47F3N10O5

710

C51H50FN9O7

711

C49H47F3N10O5

712

C49H47F3N10O5

713

C49H47F3N10O5

714

C53H54FN9O6

715

C49H46F2N10O6

and

716

C49H47F3N10O5;

or a pharmaceutically acceptable salt thereof.

2 . The compound according to claim 1 , selected from the group consisting of the compounds with ID numbers 36, 121, 128, 208, 209, 213, 214, 220, 225, 226, 302, 311, 313, 323, 406, 410, 417, 427, 428, 429, 433, 436, 437, 611-619, 703, 705-708, 710-715 and 716, or a pharmaceutically acceptable salt thereof.

3 . The pharmaceutically acceptable salt of the compound of claim 1 .

4 . The pharmaceutically acceptable salt of claim 3 , selected from L-arginine, hemi-calcium, mono-potassium, mono-sodium, L-lysine, and betaine salt forms.

5 . The pharmaceutically acceptable salt of claim 3 , wherein the salt is compound 214 monosodium salt or compound 36 monosodium salt.

6 . The pharmaceutically acceptable salt of claim 5 , wherein the salt is amorphous.

7 . A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

8 . A method of treating a GLP-1 related disorder in a subject in need thereof comprising administering a therapeutically effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

9 . The compound according to claim 1 , wherein the compound is selected from the group consisting of compounds with ID numbers 36, 121, 214, 226, 302, 323, 36, 428, 429, 433, 509, 518, 525, 606, 607, 610, 612, 614, 617, 705-708, 710-715 and 716, or a pharmaceutically acceptable salt thereof.

10 . The compound according to claim 1 , wherein the compound is selected from the group consisting of compounds with ID numbers 36, 121, 214, 226, 302, 323, 36, 428, 429, 433, 509, 518, 525, 606, 607, 610, 612, 614, and 617, or a pharmaceutically acceptable salt thereof.

11 . The compound according to claim 1 , with the ID number 36:

or a pharmaceutically acceptable salt thereof.

12 . The compound according to claim 1 , with the ID number 214:

or a pharmaceutically acceptable salt thereof.

13 . The compound according to claim 1 , with the ID number 707:

or a pharmaceutically acceptable salt thereof.

14 . The compound according to claim 1 , with the ID number 710:

or a pharmaceutically acceptable salt thereof.

15 . The compound according to claim 1 , with the ID number 711:

or a pharmaceutically acceptable salt thereof.

16 . The compound according to claim 1 , with the ID number 713:

or a pharmaceutically acceptable salt thereof.

17 . The compound according to claim 1 , with the ID number 714:

or a pharmaceutically acceptable salt thereof.

18 . The compound according to claim 1 , with the ID number 225:

19 . The compound according to claim 1 , with the ID number 226:

or a pharmaceutically acceptable salt thereof.

20 . The pharmaceutically acceptable salt of claim 3 , wherein the pharmaceutically acceptable salt is compound ID number 214 monosodium salt.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 20, 2025
From: VOIGT, JOHANNES H.; SQUIRES, NEIL HOWARD; PHAN, THU; UNGASHE, SOLOMON B.; SU, YONGLI; KIRSCHBERG, THORSTEN; UPASANI, RAVINDRA B.; LIN, NAN-HORNG; PUPPALI, SATISH GOUD; PALMER, JAMES T.; JANSA, PETR; BALAKRISHNAN, MINI; BUTLER, THOMAS; WANG, XIAODONG; CAO, YEYU
To: BIOMEA FUSION, INC.
Reel/Frame 072065/0447 →
Continuity (9)
Provisional Application 63768592 · Mar 7, 2025
Provisional Application 63760318 · Feb 19, 2025
Provisional Application 63720442 · Nov 14, 2024
Provisional Application 63706540 · Oct 11, 2024
Provisional Application 63689349 · Aug 30, 2024
Provisional Application 63672080 · Jul 16, 2024
Provisional Application 63635840 · Apr 18, 2024
Provisional Application 63571826 · Mar 29, 2024
Related Publication 20250304572A1 · Oct 2, 2025
References Cited (37)
US 10858356B2 · Hitoshi et al. · 2020 [cited by applicant]
US 11584751B1 · Ren · 2023 [cited by applicant]
US 12234236B1 · Liang et al. · 2025 [cited by applicant]
US 20190225604A1 · Hitoshi et al. · 2019 [cited by applicant]
US 20210017176A1 · Hitoshi et al. · 2021 [cited by applicant]
US 20250195481A1 · Nie et al. · 2025 [cited by applicant]
AU 2021311567A1 · 2023 [cited by applicant]
CN 116003403A · 2023 [cited by applicant]
CN 117069743A · 2023 [cited by applicant]
CN 117964617A · 2024 [cited by applicant]
CN 119019428A · 2024 [cited by applicant]
CN 119176808A · 2024 [cited by applicant]
CN 119285580A · 2025 [cited by applicant]
CN 119306743A · 2025 [cited by applicant]
CN 119528907A · 2025 [cited by examiner]
JP 201999571A · 2019 [cited by applicant]
KR 20250102249A · 2025 [cited by applicant]
WO WO2021155841A1 · 2021 [cited by applicant]
WO WO2023016546A1 · 2023 [cited by applicant]
WO WO2023169456A1 · 2023 [cited by applicant]
WO WO2024153070A1 · 2024 [cited by examiner]
WO WO2024169952A1 · 2024 [cited by applicant]
WO WO2025002250A1 · 2025 [cited by applicant]
WO WO2025002326A1 · 2025 [cited by applicant]
WO WO2025006921A1 · 2025 [cited by applicant]
WO WO2025011664A1 · 2025 [cited by applicant]
WO WO2025026436A1 · 2025 [cited by applicant]
WO WO2025045208A1 · 2025 [cited by applicant]
WO WO2025097835A1 · 2025 [cited by applicant]
WO WO2025103443A1 · 2025 [cited by applicant]
WO WO2025108361A1 · 2025 [cited by applicant]
WO WO2025131043A1 · 2025 [cited by applicant]
WO WO2025140532A1 · 2025 [cited by applicant]
WO WO2025140533A1 · 2025 [cited by applicant]
WO WO2025148997A1 · 2025 [cited by applicant]
WO WO2025162065A1 · 2025 [cited by applicant]
International Search Report for International PCT Application No. PCT/US2025/022166 3 pages, mailed Jul. 24, 2025. [cited by applicant]