CN112457301A - 新的glp-1受体调节剂 - Google Patents
新的glp-1受体调节剂 Download PDFInfo
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- CN112457301A CN112457301A CN202011261790.0A CN202011261790A CN112457301A CN 112457301 A CN112457301 A CN 112457301A CN 202011261790 A CN202011261790 A CN 202011261790A CN 112457301 A CN112457301 A CN 112457301A
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- butyl
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- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 title claims abstract description 37
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- 238000000034 method Methods 0.000 claims abstract description 224
- 102000005962 receptors Human genes 0.000 claims abstract description 26
- 108020003175 receptors Proteins 0.000 claims abstract description 26
- -1 perhaloalkyl Chemical group 0.000 claims description 276
- 125000000623 heterocyclic group Chemical group 0.000 claims description 82
- 125000000217 alkyl group Chemical group 0.000 claims description 80
- 125000003118 aryl group Chemical group 0.000 claims description 70
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 57
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- 150000003839 salts Chemical class 0.000 claims description 39
- 229940079593 drug Drugs 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 29
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 28
- 229910052736 halogen Inorganic materials 0.000 claims description 27
- 150000002367 halogens Chemical class 0.000 claims description 26
- 125000004429 atom Chemical group 0.000 claims description 21
- 230000003211 malignant effect Effects 0.000 claims description 20
- 125000001188 haloalkyl group Chemical group 0.000 claims description 17
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 230000004913 activation Effects 0.000 claims description 16
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- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 16
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 239000000651 prodrug Substances 0.000 claims description 15
- 229940002612 prodrug Drugs 0.000 claims description 15
- 125000004076 pyridyl group Chemical group 0.000 claims description 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 14
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- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 14
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- PXZWGQLGAKCNKD-DPNMSELWSA-N molport-023-276-326 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 PXZWGQLGAKCNKD-DPNMSELWSA-N 0.000 abstract description 7
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Classifications
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| DK2713722T3 (en) | 2011-05-31 | 2017-07-03 | Celgene Int Ii Sarl | Newly known GLP-1 receptor stabilizers and modulators |
| CN105593225B (zh) | 2013-06-11 | 2019-04-16 | 赛尔基因第二国际有限公司 | 新型glp-1受体调节剂 |
| CN107074820B (zh) * | 2014-07-25 | 2021-05-18 | 赛尔基因第二国际有限公司 | Glp-1受体调节剂 |
| KR102497644B1 (ko) * | 2014-12-10 | 2023-02-08 | 리셉토스 엘엘씨 | Glp-1 수용체 조절제 |
| SMT202100672T1 (it) | 2016-09-30 | 2022-01-10 | Receptos Llc | Sale di dimetilamminoetanolo di un modulatore del recettore del glp-1 |
| WO2018200833A1 (en) * | 2017-04-28 | 2018-11-01 | Celgene International Ii Sarl | Novel glp-1 receptor modulators |
| US20220193080A1 (en) * | 2019-04-11 | 2022-06-23 | University Of The Sciences | Allosteric agonists and positive allosteric modulators of glucagon-like peptide 1 receptor |
| DK4097099T3 (da) | 2020-02-07 | 2024-07-15 | Gasherbrum Bio Inc | Heterocyckliske GLP1-agonister |
| CR20230066A (es) | 2020-08-06 | 2023-05-29 | Gasherbrum Bio Inc | Agonistas del glp-1 heterocíclicos |
| 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 |
| US20250188103A1 (en) | 2022-03-09 | 2025-06-12 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| US20250206757A1 (en) | 2022-03-21 | 2025-06-26 | Gasherbrum Bio, Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
| JP2025513071A (ja) | 2022-04-14 | 2025-04-22 | ガシャーブラム・バイオ・インコーポレイテッド | ヘテロ環式ｇｌｐ－１アゴニスト |
| 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 |
| WO2025109387A1 (en) | 2023-11-24 | 2025-05-30 | 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 |
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| DK2713722T3 (en) | 2011-05-31 | 2017-07-03 | Celgene Int Ii Sarl | Newly known GLP-1 receptor stabilizers and modulators |
| CN105593225B (zh) | 2013-06-11 | 2019-04-16 | 赛尔基因第二国际有限公司 | 新型glp-1受体调节剂 |
| CN107074820B (zh) * | 2014-07-25 | 2021-05-18 | 赛尔基因第二国际有限公司 | Glp-1受体调节剂 |
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| CN1265672A (zh) * | 1997-07-31 | 2000-09-06 | 伊兰药品公司 | 能抑制由vla－4介导的白细胞粘连的磺酰化二肽化合物 |
| CN102946882A (zh) * | 2010-02-02 | 2013-02-27 | 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 |
| WO2013090454A2 (en) * | 2011-12-12 | 2013-06-20 | Receptos, Inc. | Novel glp-1 receptor modulators |
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