JP2018532788A5 - - Google Patents
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- Publication number
- JP2018532788A5 JP2018532788A5 JP2018541591A JP2018541591A JP2018532788A5 JP 2018532788 A5 JP2018532788 A5 JP 2018532788A5 JP 2018541591 A JP2018541591 A JP 2018541591A JP 2018541591 A JP2018541591 A JP 2018541591A JP 2018532788 A5 JP2018532788 A5 JP 2018532788A5
- Authority
- JP
- Japan
- Prior art keywords
- oxo
- propan
- pyridin
- piperidin
- piperazin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 18
- -1 7-Methyl-1H-indazol-5-yl Chemical group 0.000 claims 13
- 206010027599 migraine Diseases 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 208000019695 Migraine disease Diseases 0.000 claims 7
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 3
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 208000000060 Migraine with aura Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 206010047700 Vomiting Diseases 0.000 claims 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- 230000009245 menopause Effects 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 230000001314 paroxysmal effect Effects 0.000 claims 2
- 230000000737 periodic effect Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000001325 propanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 238000007920 subcutaneous administration Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 230000008673 vomiting Effects 0.000 claims 2
- KRQUFUKTQHISJB-YYADALCUSA-N 2-[(E)-N-[2-(4-chlorophenoxy)propoxy]-C-propylcarbonimidoyl]-3-hydroxy-5-(thian-3-yl)cyclohex-2-en-1-one Chemical compound CCC\C(=N/OCC(C)OC1=CC=C(Cl)C=C1)C1=C(O)CC(CC1=O)C1CCCSC1 KRQUFUKTQHISJB-YYADALCUSA-N 0.000 claims 1
- 206010049714 Abdominal migraine Diseases 0.000 claims 1
- 208000006820 Arthralgia Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 206010050258 Basilar migraine Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 208000006561 Cluster Headache Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010014020 Ear pain Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000033830 Hot Flashes Diseases 0.000 claims 1
- 206010060800 Hot flush Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 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
- 206010033078 Otitis media Diseases 0.000 claims 1
- 206010052784 Retinal migraine Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 241001303601 Rosacea Species 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 150000003863 ammonium salts Chemical class 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 208000018912 cluster headache syndrome Diseases 0.000 claims 1
- 238000000502 dialysis Methods 0.000 claims 1
- 208000002173 dizziness Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000035238 familial hemiplegic 1 migraine Diseases 0.000 claims 1
- 206010067039 familial hemiplegic migraine Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002175 menstrual effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000017420 migraine with brainstem aura Diseases 0.000 claims 1
- 230000002085 persistent effect Effects 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000004700 rosacea Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000006122 sporadic hemiplegic migraine Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 208000004371 toothache Diseases 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 0 Cc(cc1*)cc(*)c1O Chemical compound Cc(cc1*)cc(*)c1O 0.000 description 1
- FIGPGTJKHFAYRK-UHFFFAOYSA-N Cc(cc1Br)cc(Br)c1O Chemical compound Cc(cc1Br)cc(Br)c1O FIGPGTJKHFAYRK-UHFFFAOYSA-N 0.000 description 1
- VHRWRRDBAJITLR-UHFFFAOYSA-N Cc1cc(C)c2[nH]ncc2c1 Chemical compound Cc1cc(C)c2[nH]ncc2c1 VHRWRRDBAJITLR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532788A JP2018532788A (ja) | 2018-11-08 |
| JP2018532788A5 true JP2018532788A5 (enExample) | 2019-12-05 |
| JP6877451B2 JP6877451B2 (ja) | 2021-05-26 |
Family
ID=55130448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018541591A Active JP6877451B2 (ja) | 2015-10-30 | 2016-10-28 | Ｃｇｒｐ受容体アンタゴニスト |
Country Status (14)
| Country | Link |
|---|---|
| US (4) | US9808457B2 (enExample) |
| EP (1) | EP3368525B1 (enExample) |
| JP (1) | JP6877451B2 (enExample) |
| CN (1) | CN108473465B (enExample) |
| AR (1) | AR106486A1 (enExample) |
| AU (1) | AU2016347521C1 (enExample) |
| BR (1) | BR112018008423B1 (enExample) |
| CA (1) | CA3002621C (enExample) |
| ES (1) | ES2719573T3 (enExample) |
| GB (1) | GB201519196D0 (enExample) |
| IL (1) | IL258892B (enExample) |
| SG (1) | SG11201803379WA (enExample) |
| TW (1) | TWI722035B (enExample) |
| WO (1) | WO2017072721A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519195D0 (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 |
| 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 |
| WO2023034466A1 (en) * | 2021-09-02 | 2023-03-09 | Pfizer Ireland Pharmaceuticals | Cgrp antagonists for treating psoriasis |
| CN116023391B (zh) * | 2022-12-13 | 2024-09-06 | 药康众拓(江苏)医药科技有限公司 | 一类氘代哌啶酰胺类cgrp抑制剂药物及用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2732221B1 (fr) | 1995-03-28 | 1997-04-25 | Oreal | Utilisation d'un antagoniste de cgrp pour traiter les rougeurs cutanees d'origine neurogene et composition obtenue |
| 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 |
| US6294534B1 (en) | 1998-06-11 | 2001-09-25 | Merck & Co., Inc. | Spiropiperidine derivatives as melanocortin receptor agonists |
| DE10206770A1 (de) | 2002-02-19 | 2003-08-28 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung eines Pulverinhalativums enthaltend ein Salz des CGRP-Antagonisten BIBN4096 |
| KR20050008790A (ko) | 2002-06-05 | 2005-01-21 | 브리스톨-마이어스 스큅 컴퍼니 | 칼시토닌 유전자 관련 펩티드 수용체 길항제 |
| US7842808B2 (en) | 2002-06-05 | 2010-11-30 | Bristol-Myers Squibb Company | Anti-migraine spirocycles |
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| DE10250082A1 (de) * | 2002-10-25 | 2004-05-13 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| JO2355B1 (en) | 2003-04-15 | 2006-12-12 | ميرك شارب اند دوم كوربوريشن | Hereditary calcitonin polypeptide receptor antagonists |
| 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 |
| KR20070062997A (ko) | 2004-10-13 | 2007-06-18 | 머크 앤드 캄파니 인코포레이티드 | Ｃｇｒｐ 수용체 길항제 |
| WO2006044449A2 (en) | 2004-10-14 | 2006-04-27 | Merck & Co., Inc. | Cgrp receptor antagonists |
| JP2008517916A (ja) | 2004-10-22 | 2008-05-29 | メルク エンド カムパニー インコーポレーテッド | Ｃｇｒｐ受容体拮抗薬 |
| 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 |
| US8044043B2 (en) | 2008-04-11 | 2011-10-25 | Bristol-Myers Squibb Company | CGRP receptor antagonists |
| US8314117B2 (en) | 2009-10-14 | 2012-11-20 | Bristol-Myers Squibb Company | CGRP receptor antagonists |
| US8481546B2 (en) * | 2010-03-30 | 2013-07-09 | Bristol-Myers Squibb Company | CGRP receptor antagonist |
| US9174989B2 (en) | 2012-05-09 | 2015-11-03 | Merck Sharp & Dohme Corp. | Process for making CGRP receptor antagonists |
| 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 |
-
2015
- 2015-10-30 GB GBGB1519196.8A patent/GB201519196D0/en not_active Ceased
-
2016
- 2016-10-28 CA CA3002621A patent/CA3002621C/en active Active
- 2016-10-28 CN CN201680063967.1A patent/CN108473465B/zh active Active
- 2016-10-28 JP JP2018541591A patent/JP6877451B2/ja active Active
- 2016-10-28 BR BR112018008423-9A patent/BR112018008423B1/pt active IP Right Grant
- 2016-10-28 TW TW105135022A patent/TWI722035B/zh active
- 2016-10-28 ES ES16791443T patent/ES2719573T3/es active Active
- 2016-10-28 AR ARP160103293A patent/AR106486A1/es active IP Right Grant
- 2016-10-28 SG SG11201803379WA patent/SG11201803379WA/en unknown
- 2016-10-28 EP EP16791443.1A patent/EP3368525B1/en active Active
- 2016-10-28 AU AU2016347521A patent/AU2016347521C1/en active Active
- 2016-10-28 US US15/336,866 patent/US9808457B2/en active Active
- 2016-10-28 WO PCT/IB2016/056517 patent/WO2017072721A1/en not_active Ceased
-
2017
- 2017-09-25 US US15/713,775 patent/US10300056B2/en active Active
-
2018
- 2018-04-24 IL IL258892A patent/IL258892B/en active IP Right Grant
-
2019
- 2019-04-08 US US16/377,519 patent/US10888561B2/en active Active
-
2020
- 2020-12-31 US US17/139,299 patent/US12178813B2/en active Active
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