JP2017526734A5 - - Google Patents
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- JP2017526734A5 JP2017526734A5 JP2017525324A JP2017525324A JP2017526734A5 JP 2017526734 A5 JP2017526734 A5 JP 2017526734A5 JP 2017525324 A JP2017525324 A JP 2017525324A JP 2017525324 A JP2017525324 A JP 2017525324A JP 2017526734 A5 JP2017526734 A5 JP 2017526734A5
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- JP
- Japan
- Prior art keywords
- compound
- chr
- heterocyclyl
- alkyl
- item
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 119
- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 38
- 229910052739 hydrogen Inorganic materials 0.000 claims description 28
- 239000001257 hydrogen Substances 0.000 claims description 26
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 19
- 239000012453 solvate Substances 0.000 claims description 19
- 150000002431 hydrogen Chemical class 0.000 claims description 17
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 229940079593 drug Drugs 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 9
- 125000003545 alkoxy group Chemical group 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 125000005843 halogen group Chemical group 0.000 claims description 8
- -1 perhaloalkyl Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 4
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 3
- 230000009286 beneficial effect Effects 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 125000000464 thioxo group Chemical group S=* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 1
- 0 C*C(C1=CC*CO1)=O Chemical compound C*C(C1=CC*CO1)=O 0.000 description 6
- 230000002159 abnormal effect Effects 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- 229940002612 prodrug Drugs 0.000 description 3
- 239000000651 prodrug Substances 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 description 2
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 230000008484 agonism Effects 0.000 description 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 2
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 description 1
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 description 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 description 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 description 1
- 229940123208 Biguanide Drugs 0.000 description 1
- YLWCYGGIPLDTGI-FUFSTLJVSA-N CC(CC1)CCC1C(CC1)CC=C1c1cnc(-c2ccc(C[C@@H](C(N(C3)CC3C(O)=O)=O)NC(c3ccc(C(C)(C)C)[s]3)=O)cc2)nc1 Chemical compound CC(CC1)CCC1C(CC1)CC=C1c1cnc(-c2ccc(C[C@@H](C(N(C3)CC3C(O)=O)=O)NC(c3ccc(C(C)(C)C)[s]3)=O)cc2)nc1 YLWCYGGIPLDTGI-FUFSTLJVSA-N 0.000 description 1
- NCCHARWOCKOHIH-UHFFFAOYSA-N CNC(c1ccccc1)=O Chemical compound CNC(c1ccccc1)=O NCCHARWOCKOHIH-UHFFFAOYSA-N 0.000 description 1
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 description 1
- 108010011459 Exenatide Proteins 0.000 description 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 description 1
- 108010063919 Glucagon Receptors Proteins 0.000 description 1
- 102100040890 Glucagon receptor Human genes 0.000 description 1
- 102000015626 Glucagon-Like Peptide-2 Receptor Human genes 0.000 description 1
- 108010024044 Glucagon-Like Peptide-2 Receptor Proteins 0.000 description 1
- 101000684208 Homo sapiens Prolyl endopeptidase FAP Proteins 0.000 description 1
- 108010019598 Liraglutide Proteins 0.000 description 1
- YSDQQAXHVYUZIW-QCIJIYAXSA-N Liraglutide Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC)C(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 YSDQQAXHVYUZIW-QCIJIYAXSA-N 0.000 description 1
- XVVOERDUTLJJHN-UHFFFAOYSA-N Lixisenatide Chemical compound C=1NC2=CC=CC=C2C=1CC(C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(N)=O)C(=O)NCC(=O)NCC(=O)N1C(CCC1)C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N1C(CCC1)C(=O)N1C(CCC1)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)CC)NC(=O)C(NC(=O)C(CC(C)C)NC(=O)C(CCCNC(N)=N)NC(=O)C(NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(CCC(O)=O)NC(=O)C(CCC(O)=O)NC(=O)C(CCSC)NC(=O)C(CCC(N)=O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC(C)C)NC(=O)C(CC(O)=O)NC(=O)C(CO)NC(=O)C(NC(=O)C(CC=1C=CC=CC=1)NC(=O)C(NC(=O)CNC(=O)C(CCC(O)=O)NC(=O)CNC(=O)C(N)CC=1NC=NC=1)C(C)O)C(C)O)C(C)C)CC1=CC=CC=C1 XVVOERDUTLJJHN-UHFFFAOYSA-N 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 108090000445 Parathyroid hormone Proteins 0.000 description 1
- 102100023832 Prolyl endopeptidase FAP Human genes 0.000 description 1
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 description 1
- 229940100389 Sulfonylurea Drugs 0.000 description 1
- 229940123464 Thiazolidinedione Drugs 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 229920000080 bile acid sequestrant Polymers 0.000 description 1
- 229960001713 canagliflozin Drugs 0.000 description 1
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 description 1
- 229960003834 dapagliflozin Drugs 0.000 description 1
- 239000002288 dopamine 2 receptor stimulating agent Substances 0.000 description 1
- 229960003345 empagliflozin Drugs 0.000 description 1
- OBWASQILIWPZMG-QZMOQZSNSA-N empagliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 OBWASQILIWPZMG-QZMOQZSNSA-N 0.000 description 1
- 229960001519 exenatide Drugs 0.000 description 1
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 description 1
- 208000004104 gestational diabetes Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229960002701 liraglutide Drugs 0.000 description 1
- 229960001093 lixisenatide Drugs 0.000 description 1
- 108010004367 lixisenatide Proteins 0.000 description 1
- 229950004994 meglitinide Drugs 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 description 1
- 229960003105 metformin Drugs 0.000 description 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 230000036186 satiety Effects 0.000 description 1
- 235000019627 satiety Nutrition 0.000 description 1
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 description 1
- 229960004034 sitagliptin Drugs 0.000 description 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 1
- 229950007151 taspoglutide Drugs 0.000 description 1
- 108010048573 taspoglutide Proteins 0.000 description 1
- WRGVLTAWMNZWGT-VQSPYGJZSA-N taspoglutide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 WRGVLTAWMNZWGT-VQSPYGJZSA-N 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462028962P | 2014-07-25 | 2014-07-25 | |
| US62/028,962 | 2014-07-25 | ||
| US201462090040P | 2014-12-10 | 2014-12-10 | |
| US62/090,040 | 2014-12-10 | ||
| US201562161650P | 2015-05-14 | 2015-05-14 | |
| US62/161,650 | 2015-05-14 | ||
| PCT/US2015/042114 WO2016015014A1 (en) | 2014-07-25 | 2015-07-24 | Novel glp-1 receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019107866A Division JP2019142984A (ja) | 2014-07-25 | 2019-06-10 | 新規のｇｌｐ−１受容体モジュレーター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017526734A JP2017526734A (ja) | 2017-09-14 |
| JP2017526734A5 true JP2017526734A5 (https=) | 2018-08-30 |
| JP6556237B2 JP6556237B2 (ja) | 2019-08-07 |
Family
ID=53777037
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017525324A Expired - Fee Related JP6556237B2 (ja) | 2014-07-25 | 2015-07-24 | 新規のｇｌｐ−１受容体モジュレーター |
| JP2019107866A Pending JP2019142984A (ja) | 2014-07-25 | 2019-06-10 | 新規のｇｌｐ−１受容体モジュレーター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019107866A Pending JP2019142984A (ja) | 2014-07-25 | 2019-06-10 | 新規のｇｌｐ−１受容体モジュレーター |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9474755B2 (https=) |
| EP (1) | EP3172199B1 (https=) |
| JP (2) | JP6556237B2 (https=) |
| KR (1) | KR102564946B1 (https=) |
| CN (2) | CN107074820B (https=) |
| AU (1) | AU2015292356B2 (https=) |
| CA (1) | CA2955836C (https=) |
| EA (1) | EA032525B1 (https=) |
| ES (1) | ES2819534T3 (https=) |
| IL (1) | IL249896B (https=) |
| MX (1) | MX382502B (https=) |
| SG (1) | SG11201700364PA (https=) |
| WO (1) | WO2016015014A1 (https=) |
| ZA (1) | ZA201700342B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6007417B2 (ja) | 2011-05-31 | 2016-10-12 | レセプトス エルエルシー | 新規ｇｌｐ−１受容体安定剤および調節剤 |
| CN109867630A (zh) | 2013-06-11 | 2019-06-11 | 赛尔基因第二国际有限公司 | 新型glp-1受体调节剂 |
| EP3172199B1 (en) * | 2014-07-25 | 2020-07-01 | Celgene International II Sarl | Pyrimidine derivatives as glp-1 receptor modulators |
| AU2015360364B2 (en) | 2014-12-10 | 2020-04-30 | Receptos Llc | GLP-1 receptor modulators |
| US11066395B2 (en) * | 2016-09-30 | 2021-07-20 | Receptos Llc | Dimethylaminoethanol salt of a GLP-1 receptor modulator |
| ES2937835T3 (es) * | 2017-04-28 | 2023-03-31 | Receptos Llc | Nuevos moduladores del receptor de GLP-1 |
| US20220193080A1 (en) * | 2019-04-11 | 2022-06-23 | University Of The Sciences | Allosteric agonists and positive allosteric modulators of glucagon-like peptide 1 receptor |
| CN119841865A (zh) | 2020-02-07 | 2025-04-18 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
| FI4143183T3 (fi) | 2020-04-29 | 2026-01-07 | Gasherbrum Bio Inc | Heterosyklisiä glp-1-agonisteja |
| PE20231181A1 (es) | 2020-08-06 | 2023-08-11 | Gasherbrum Bio Inc | Agonistas del glp-1 heterociclicos |
| CN112121152B (zh) * | 2020-09-25 | 2021-06-22 | 南京大学 | 利司那肽在制备抗肿瘤药物中的应用 |
| CN112898133B (zh) * | 2021-01-27 | 2022-11-15 | 河北迈尔斯通电子材料有限公司 | 一种反式酮类中间体的制备方法 |
| CN119137124A (zh) | 2022-03-09 | 2024-12-13 | 加舒布鲁姆生物公司 | 杂环glp-1激动剂 |
| WO2023179542A1 (en) | 2022-03-21 | 2023-09-28 | Gasherbrum Bio , Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
| WO2023198140A1 (en) | 2022-04-14 | 2023-10-19 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| TW202521533A (zh) | 2023-09-14 | 2025-06-01 | 香港商歌禮製藥(中國)有限公司 | Glp-1r 激動劑及其治療方法 |
| US12291530B1 (en) | 2023-11-24 | 2025-05-06 | Ascletis Pharma (China) Co., Limited | GLP-1R agonist and therapeutic method thereof |
| KR20250113341A (ko) | 2024-01-18 | 2025-07-25 | 주식회사 티에치팜 | 나트륨 포도당 운반체-2 저해제 및 안지오텐신 ⅱ 수용체 차단제를 함유하는 비만 예방 또는 치료용 약학적 조성물 |
| WO2025158275A1 (en) | 2024-01-24 | 2025-07-31 | Pfizer Inc. | Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1062206B (it) | 1974-02-01 | 1983-09-20 | Rotta Research Lab S P A A S | Derivati della tirosina attivi sulla muscolatura liscia |
| DE2423536A1 (de) | 1974-05-15 | 1975-11-27 | Bayer Ag | 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide |
| US5424286A (en) | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| US6174905B1 (en) | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
| EP0996459B1 (en) | 1997-01-07 | 2005-09-21 | Amylin Pharmaceuticals, Inc. | Use of exendins and agonists thereof for the reduction of food intake |
| HUP0003921A3 (en) | 1997-07-31 | 2001-03-28 | Wyeth Corp | Sulfonylated dipeptide compounds which inhibit leukocyte adhesion mediated by vla-4, pharmaceutical compositions comprising thereof and their use |
| US6583139B1 (en) | 1997-07-31 | 2003-06-24 | Eugene D. Thorsett | Compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| BR9811730B1 (pt) | 1997-08-22 | 2014-04-08 | Hoffmann La Roche | Derivados de n-aroilfenilalanina, uso dos mesmos, medicamentos contendo os mesmos. |
| US6191171B1 (en) | 1997-11-20 | 2001-02-20 | Merck & Co., Inc. | Para-aminomethylaryl carboxamide derivatives |
| JP2002538081A (ja) | 1998-12-07 | 2002-11-12 | ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス | Ｇｌｐ−１の類似体 |
| NZ512663A (en) | 1999-01-14 | 2004-05-28 | Amylin Pharmaceuticals Inc | Novel exendin agonist formulations and methods of administration thereof |
| RU2281283C2 (ru) | 2000-03-07 | 2006-08-10 | Санофи-Авентис Дойчланд Гмбх | Замещенные 3-фенил-5-алкокси-1,3,4-оксадиазол-2-оны и их применение для ингибирования гормоночувствительной липазы |
| AU2002350217A1 (en) | 2001-12-04 | 2003-06-17 | Bristol-Myers Squibb Company | Glycinamides as factor xa inhibitors |
| AU2003211560A1 (en) | 2002-02-20 | 2003-09-09 | Ajinomoto Co., Inc. | Novel phenylalanine derivative |
| KR101194176B1 (ko) | 2003-12-22 | 2012-10-24 | 아지노모토 가부시키가이샤 | 신규한 페닐알라닌 유도체 |
| KR20070004676A (ko) * | 2004-02-10 | 2007-01-09 | 얀센 파마슈티카 엔.브이. | 알파４ 인테그린의 길항제로서의 피리다지논 |
| US7825139B2 (en) | 2005-05-25 | 2010-11-02 | Forest Laboratories Holdings Limited (BM) | Compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| WO2008112939A2 (en) | 2007-03-13 | 2008-09-18 | Board Of Regents, The University Of Texas System | Composition and method for making oligo-benzamide compounds |
| EP2155720B1 (en) | 2007-06-08 | 2013-07-17 | Advinus Therapeutics Private Limited | Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application |
| US7727983B2 (en) * | 2008-03-07 | 2010-06-01 | Transtech Pharma, Inc. | Oxadiazoanthracene compounds for the treatment of diabetes |
| WO2011094890A1 (en) | 2010-02-02 | 2011-08-11 | Argusina Inc. | Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators |
| CN102946882B (zh) * | 2010-02-02 | 2016-05-18 | 格斯有限公司 | 苯基丙氨酸衍生物及其作为非肽glp-1受体调节剂的用途 |
| US8501982B2 (en) | 2010-06-09 | 2013-08-06 | Receptos, Inc. | GLP-1 receptor stabilizers and modulators |
| TWI523844B (zh) * | 2011-01-26 | 2016-03-01 | 賽諾菲公司 | 經胺基取代之３－雜芳醯基胺基－丙酸衍生物及其作為藥物之用途 |
| JP6007417B2 (ja) | 2011-05-31 | 2016-10-12 | レセプトス エルエルシー | 新規ｇｌｐ−１受容体安定剤および調節剤 |
| AU2012352349B2 (en) | 2011-12-12 | 2017-08-17 | Receptos Llc | Carboxylic acid derivatives comprising four cycles acting as GLP-1 receptor modulators for therapy of diseases such as diabetes |
| CN109867630A (zh) | 2013-06-11 | 2019-06-11 | 赛尔基因第二国际有限公司 | 新型glp-1受体调节剂 |
| EP3172199B1 (en) * | 2014-07-25 | 2020-07-01 | Celgene International II Sarl | Pyrimidine derivatives as glp-1 receptor modulators |
-
2015
- 2015-07-24 EP EP15745738.3A patent/EP3172199B1/en active Active
- 2015-07-24 JP JP2017525324A patent/JP6556237B2/ja not_active Expired - Fee Related
- 2015-07-24 ES ES15745738T patent/ES2819534T3/es active Active
- 2015-07-24 US US14/809,020 patent/US9474755B2/en active Active
- 2015-07-24 CN CN201580046095.3A patent/CN107074820B/zh not_active Expired - Fee Related
- 2015-07-24 EA EA201790254A patent/EA032525B1/ru not_active IP Right Cessation
- 2015-07-24 MX MX2017000972A patent/MX382502B/es unknown
- 2015-07-24 CA CA2955836A patent/CA2955836C/en active Active
- 2015-07-24 WO PCT/US2015/042114 patent/WO2016015014A1/en not_active Ceased
- 2015-07-24 AU AU2015292356A patent/AU2015292356B2/en not_active Ceased
- 2015-07-24 SG SG11201700364PA patent/SG11201700364PA/en unknown
- 2015-07-24 KR KR1020177003172A patent/KR102564946B1/ko active Active
- 2015-07-24 CN CN202011261790.0A patent/CN112457301A/zh active Pending
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2016
- 2016-09-13 US US15/263,637 patent/US9839664B2/en active Active
-
2017
- 2017-01-02 IL IL249896A patent/IL249896B/en active IP Right Grant
- 2017-01-16 ZA ZA2017/00342A patent/ZA201700342B/en unknown
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2019
- 2019-06-10 JP JP2019107866A patent/JP2019142984A/ja active Pending
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