BR112015031040A8 - Novos moduladores do receptor de glp-1 - Google Patents
Novos moduladores do receptor de glp-1Info
- Publication number
- BR112015031040A8 BR112015031040A8 BR112015031040A BR112015031040A BR112015031040A8 BR 112015031040 A8 BR112015031040 A8 BR 112015031040A8 BR 112015031040 A BR112015031040 A BR 112015031040A BR 112015031040 A BR112015031040 A BR 112015031040A BR 112015031040 A8 BR112015031040 A8 BR 112015031040A8
- Authority
- BR
- Brazil
- Prior art keywords
- glp
- peptide
- new
- methods
- new glp
- Prior art date
Links
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 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)NCC(=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@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 title abstract 3
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 title abstract 2
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 title 1
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 abstract 3
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- NGJOFQZEYQGZMB-KTKZVXAJSA-N (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid 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)NCC(=O)N[C@@H](CCCNC(N)=N)C(O)=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@H](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 NGJOFQZEYQGZMB-KTKZVXAJSA-N 0.000 abstract 1
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 abstract 1
- 101800004295 Glucagon-like peptide 1(7-36) Proteins 0.000 abstract 1
- 108010019598 Liraglutide Proteins 0.000 abstract 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 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003623 enhancer Substances 0.000 abstract 1
- MGXWVYUBJRZYPE-YUGYIWNOSA-N incretin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(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](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)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=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=C(O)C=C1 MGXWVYUBJRZYPE-YUGYIWNOSA-N 0.000 abstract 1
- 239000000859 incretin Substances 0.000 abstract 1
- 229960002701 liraglutide Drugs 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 230000000069 prophylactic effect Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
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- C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C—CHEMISTRY; METALLURGY
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- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
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| 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 |
| WO2014201172A1 (en) | 2013-06-11 | 2014-12-18 | Receptos, Inc. | Novel glp-1 receptor modulators |
| JP6556237B2 (ja) * | 2014-07-25 | 2019-08-07 | セルジーン インターナショナル ツー エスエーアールエル | 新規のglp−1受容体モジュレーター |
| JP2017538711A (ja) * | 2014-12-10 | 2017-12-28 | セルジーン インターナショナル ツー エスエーアールエル | Glp−1レセプターモジュレーター |
| HUE057838T2 (hu) | 2016-06-07 | 2022-06-28 | Jacobio Pharmaceuticals Co Ltd | SHP2 inhibitorokként hasznos új heterociklusos származékok |
| TWI664175B (zh) | 2017-03-23 | 2019-07-01 | 大陸商北京加科思新藥研發有限公司 | 用於作為shp2抑制劑之新穎雜環衍生物 |
| EP3615524B1 (en) * | 2017-04-28 | 2022-11-09 | Receptos Llc | Novel glp-1 receptor modulators |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| CN109608524B (zh) * | 2018-11-09 | 2022-06-03 | 北京志道生物科技有限公司 | 兼具dpp-4抑制及glp1r激活活性的多肽衍生物、制备和应用 |
| PL4097099T3 (pl) | 2020-02-07 | 2024-11-04 | Gasherbrum Bio, Inc. | Heterocykliczne agonisty glp-1 |
| CN111548311B (zh) * | 2020-06-04 | 2021-04-23 | 山西医科大学 | 一种小分子glp-1r激动剂及其应用 |
| KR20230053620A (ko) | 2020-08-06 | 2023-04-21 | 가셔브룸 바이오, 인크. | 헤테로시클릭 glp-1 효능제 |
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| EP4496797A1 (en) | 2022-03-21 | 2025-01-29 | Gasherbrum Bio, Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
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| CN114989204A (zh) * | 2022-06-16 | 2022-09-02 | 西北工业大学 | 一种葡萄糖响应自修复凝胶用的二苯乙炔类液晶态交联剂的制备方法 |
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| WO2014201172A1 (en) | 2013-06-11 | 2014-12-18 | Receptos, Inc. | Novel glp-1 receptor modulators |
| JP6556237B2 (ja) | 2014-07-25 | 2019-08-07 | セルジーン インターナショナル ツー エスエーアールエル | 新規のglp−1受容体モジュレーター |
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2014
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- 2014-06-11 EP EP14736554.8A patent/EP3008056B8/en active Active
- 2014-06-11 EA EA201592281A patent/EA030857B1/ru not_active IP Right Cessation
- 2014-06-11 CN CN201480044849.7A patent/CN105593225B/zh not_active Expired - Fee Related
- 2014-06-11 AU AU2014278183A patent/AU2014278183B2/en not_active Ceased
- 2014-06-11 ES ES14736554T patent/ES2864349T3/es active Active
- 2014-06-11 CA CA2913791A patent/CA2913791A1/en not_active Abandoned
- 2014-06-11 HK HK16110427.4A patent/HK1222176A1/zh unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| AU2014278183A1 (en) | 2016-01-07 |
| US20160214993A1 (en) | 2016-07-28 |
| AU2014278183B2 (en) | 2018-10-04 |
| CN105593225A (zh) | 2016-05-18 |
| JP2016528180A (ja) | 2016-09-15 |
| HK1222177A1 (zh) | 2017-06-23 |
| US20170313717A1 (en) | 2017-11-02 |
| US9598430B2 (en) | 2017-03-21 |
| EP3008056A1 (en) | 2016-04-20 |
| EP3008056B8 (en) | 2021-03-03 |
| US9260427B2 (en) | 2016-02-16 |
| MX2015016831A (es) | 2016-04-04 |
| EP3008056B1 (en) | 2020-12-09 |
| ES2864349T3 (es) | 2021-10-13 |
| NZ715006A (en) | 2021-02-26 |
| US20150011527A1 (en) | 2015-01-08 |
| EA030857B1 (ru) | 2018-10-31 |
| EA201592281A1 (ru) | 2016-05-31 |
| KR102271179B1 (ko) | 2021-07-01 |
| CN105593225B (zh) | 2019-04-16 |
| US10259823B2 (en) | 2019-04-16 |
| BR112015031040A2 (enExample) | 2017-07-25 |
| KR20160042868A (ko) | 2016-04-20 |
| WO2014201172A1 (en) | 2014-12-18 |
| JP6573604B2 (ja) | 2019-09-11 |
| CN109867630A (zh) | 2019-06-11 |
| MX370666B (es) | 2019-12-19 |
| HK1222176A1 (zh) | 2017-06-23 |
| CA2913791A1 (en) | 2014-12-18 |
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