JP6877451B2 - Ｃｇｒｐ受容体アンタゴニスト - Google Patents
Ｃｇｒｐ受容体アンタゴニスト Download PDFInfo
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- JP6877451B2 JP6877451B2 JP2018541591A JP2018541591A JP6877451B2 JP 6877451 B2 JP6877451 B2 JP 6877451B2 JP 2018541591 A JP2018541591 A JP 2018541591A JP 2018541591 A JP2018541591 A JP 2018541591A JP 6877451 B2 JP6877451 B2 JP 6877451B2
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- Prior art keywords
- oxo
- piperidine
- migraine
- amino
- propan
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- 239000003735 calcitonin gene related peptide receptor antagonist Substances 0.000 title description 11
- 150000001875 compounds Chemical class 0.000 claims description 111
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- 208000019695 Migraine disease Diseases 0.000 claims description 49
- 239000000203 mixture Substances 0.000 claims description 45
- 238000000034 method Methods 0.000 claims description 42
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 27
- 150000003839 salts Chemical class 0.000 claims description 24
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 23
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 22
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 20
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- 208000002193 Pain Diseases 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
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- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 claims description 13
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- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 7
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- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 claims 4
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- MBRFNJSXLBOYAO-GPOMZPHUSA-N N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide Chemical compound BrC=1C=C(C[C@@H](NC(=O)N2CCC(CC2)N2C(NC3=CC=CC=C3C2)=O)C(=O)N[C@H](C(N2CCN(CC2)C2=CC=NC=C2)=O)CC2CCNCC2)C=C(C=1O)Br MBRFNJSXLBOYAO-GPOMZPHUSA-N 0.000 claims 1
- LIQMLKRGQPLTKF-XDSPJLLDSA-N N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carboxamide Chemical compound BrC=1C=C(C[C@@H](NC(=O)N2CCC(CC2)C=2C(NC3=CC=CC=C3C=2)=O)C(=O)N[C@H](C(N2CCN(CC2)C2=CC=NC=C2)=O)CC2CCNCC2)C=C(C=1O)Br LIQMLKRGQPLTKF-XDSPJLLDSA-N 0.000 claims 1
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- 108090000932 Calcitonin Gene-Related Peptide Proteins 0.000 description 17
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 17
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Classifications
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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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- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
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- C07D498/10—Spiro-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
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- C07D498/20—Spiro-condensed systems
Landscapes
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| GBGB1519196.8A GB201519196D0 (en) | 2015-10-30 | 2015-10-30 | CGRP Receptor Antagonists |
| GB1519196.8 | 2015-10-30 | ||
| PCT/IB2016/056517 WO2017072721A1 (en) | 2015-10-30 | 2016-10-28 | Cgrp receptor antagonists |
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| JP2018532788A JP2018532788A (ja) | 2018-11-08 |
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| GB201519196D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| WO2018178938A1 (en) * | 2017-03-31 | 2018-10-04 | Heptares Therapeutics Limited | Cgrp receptor antagonists |
| KR20200135465A (ko) * | 2018-03-25 | 2020-12-02 | 바이오하벤 파마슈티컬 홀딩 컴퍼니 엘티디. | Cgrp 관련 장애를 위한 리메게판트 |
| EP3873898B1 (en) | 2018-11-02 | 2025-05-28 | Dana-Farber Cancer Institute, Inc. | Histone acetylation writer inhibitor development and uses thereof |
| GB201908420D0 (en) * | 2019-06-12 | 2019-07-24 | Heptares Therapeutics Ltd | Cgrp antagonist compounds |
| GB201908430D0 (en) | 2019-06-12 | 2019-07-24 | Heptares Therapeutics Ltd | Cgrp antagonist compounds |
| US12042513B2 (en) | 2020-01-10 | 2024-07-23 | Massachusetts Institute Of Technology | Proteolysis targeting chimeric molecules (PROTACs) with functional handles and uses thereof |
| EP4126002A4 (en) * | 2020-03-23 | 2024-04-10 | Pfizer Ireland Pharmaceuticals | METHODS OF TREATING LUNG INJURY WITH CGRP INHIBITORS |
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| JP3483893B2 (ja) | 1996-09-10 | 2004-01-06 | ドクトル カルル トーマエ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 修飾アミノ酸、これらの化合物を含む薬物及びそれらの調製方法 |
| US20030069231A1 (en) | 1999-10-12 | 2003-04-10 | Klaus Rudolf | Modified aminoacids, pharmaceuticals containing these compounds and method for their production |
| JP2002517444A (ja) | 1998-06-11 | 2002-06-18 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン受容体作動薬としてのスピロピペリジン誘導体 |
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| DE10206770A1 (de) | 2002-02-19 | 2003-08-28 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung eines Pulverinhalativums enthaltend ein Salz des CGRP-Antagonisten BIBN4096 |
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| AR046787A1 (es) | 2003-12-05 | 2005-12-21 | Bristol Myers Squibb Co | Agentes antimigrana heterociclicos |
| EP1689493A4 (en) | 2003-12-05 | 2008-04-23 | Bristol Myers Squibb Co | ANTAGONISTS OF THE CALCITONIN GENE RELATED PEPTIDE RECEPTOR |
| DE102004015723A1 (de) | 2004-03-29 | 2005-10-20 | Boehringer Ingelheim Pharma | Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| TW200533398A (en) | 2004-03-29 | 2005-10-16 | Bristol Myers Squibb Co | Novel therapeutic agents for the treatment of migraine |
| DE102004018795A1 (de) * | 2004-04-15 | 2005-10-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| US20050233980A1 (en) | 2004-04-20 | 2005-10-20 | Boehringer Ingelheim International Gmbh | CGRP-antagonist in combination with a serotonin-reuptake inhibitor for the treatment of migraine |
| DE102004019492A1 (de) | 2004-04-22 | 2005-11-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
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| EP1770091A1 (de) | 2005-09-29 | 2007-04-04 | Boehringer Ingelheim Pharma GmbH & Co. KG | CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| US7834007B2 (en) * | 2005-08-25 | 2010-11-16 | Bristol-Myers Squibb Company | CGRP antagonists |
| KR20090021214A (ko) | 2006-06-08 | 2009-02-27 | 베링거 인겔하임 인터내셔날 게엠베하 | Ｃｇｒｐ-길항제에 의한 위장 장애의 치료 |
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| GB201519194D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP receptor antagonists |
| GB201519196D0 (en) * | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201519195D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
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| GB201519196D0 (en) | 2015-12-16 |
| AU2016347521C1 (en) | 2021-04-01 |
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| EP3368525A1 (en) | 2018-09-05 |
| US20190231773A1 (en) | 2019-08-01 |
| CN108473465B (zh) | 2021-03-02 |
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| CA3002621C (en) | 2024-01-23 |
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| SG11201803379WA (en) | 2018-05-30 |
| US12178813B2 (en) | 2024-12-31 |
| BR112018008423A2 (pt) | 2018-11-06 |
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