JP2018532790A5 - - Google Patents
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- Publication number
- JP2018532790A5 JP2018532790A5 JP2018541593A JP2018541593A JP2018532790A5 JP 2018532790 A5 JP2018532790 A5 JP 2018532790A5 JP 2018541593 A JP2018541593 A JP 2018541593A JP 2018541593 A JP2018541593 A JP 2018541593A JP 2018532790 A5 JP2018532790 A5 JP 2018532790A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- migraine
- oxo
- bipiperidin
- dihydroquinolin
- 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 14
- -1 7-methyl-1H-indazol-5-yl Chemical group 0.000 claims 13
- 206010027599 migraine Diseases 0.000 claims 8
- 208000019695 Migraine disease Diseases 0.000 claims 7
- 208000002193 Pain Diseases 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 208000000060 Migraine with aura Diseases 0.000 claims 2
- 206010047700 Vomiting Diseases 0.000 claims 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 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
- 238000007920 subcutaneous administration Methods 0.000 claims 2
- 230000008673 vomiting Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 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
- LHTDFZHWXGJKAC-JGCGQSQUSA-N 5-[1-[1-[(2R)-3-(7-methyl-1H-indazol-5-yl)-2-[[4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carbonyl]amino]propanoyl]piperidin-4-yl]piperidin-4-yl]-1H-1,2,4-triazole-3-carboxylic acid Chemical compound CC=1C=C(C=C2C=NNC=12)C[C@H](C(=O)N1CCC(CC1)N1CCC(CC1)C=1NC(=NN=1)C(=O)O)NC(=O)N1CCC(CC1)C=1C(NC2=CC=CC=C2C=1)=O LHTDFZHWXGJKAC-JGCGQSQUSA-N 0.000 claims 1
- 206010049714 Abdominal migraine 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
- 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
- 206010003246 arthritis Diseases 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
- ZBZJVLNNWXGGTH-UUWRZZSWSA-N ethyl 5-[1-[1-[(2R)-3-(7-methyl-1H-indazol-5-yl)-2-[[4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carbonyl]amino]propanoyl]piperidin-4-yl]piperidin-4-yl]-1H-1,2,4-triazole-3-carboxylate Chemical compound CC=1C=C(C=C2C=NNC=12)C[C@H](C(=O)N1CCC(CC1)N1CCC(CC1)C=1NC(=NN=1)C(=O)OCC)NC(=O)N1CCC(CC1)C=1C(NC2=CC=CC=C2C=1)=O ZBZJVLNNWXGGTH-UUWRZZSWSA-N 0.000 claims 1
- 208000035238 familial hemiplegic 1 migraine Diseases 0.000 claims 1
- 206010067039 familial hemiplegic migraine Diseases 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000028774 intestinal disease Diseases 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
- 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
- 238000001356 surgical procedure Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 208000004371 toothache Diseases 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- WFXDPWZNULOEPH-UHFFFAOYSA-N CC(C)c1c(C)nc[nH]1 Chemical compound CC(C)c1c(C)nc[nH]1 WFXDPWZNULOEPH-UHFFFAOYSA-N 0.000 description 2
- QBDXSEYWEKKYSH-UHFFFAOYSA-N Cc1nnc[n]1C Chemical compound Cc1nnc[n]1C QBDXSEYWEKKYSH-UHFFFAOYSA-N 0.000 description 2
- NXBWLJDDASRJRU-VVDKBYALSA-N CC1C(C(CC2)CCN2C(CCC2)CCC2C([C@@H](Cc2cc(C)c3[nH]ncc3c2)NC(C=C(CC2)CCC2C2=Cc(cccc3)c3NCC2=O)=O)=O)=NN=C1 Chemical compound CC1C(C(CC2)CCN2C(CCC2)CCC2C([C@@H](Cc2cc(C)c3[nH]ncc3c2)NC(C=C(CC2)CCC2C2=Cc(cccc3)c3NCC2=O)=O)=O)=NN=C1 NXBWLJDDASRJRU-VVDKBYALSA-N 0.000 description 1
- KLENFGVWYLLZFQ-PGUFJCEWSA-N Cc1c(C(CC2)CCN2C(CC2)CCN2C([C@@H](Cc2cc(C)c3[nH]ncc3c2)NC(N(CC2)CCC2C2=Cc(cccc3)c3NC2=O)=O)=O)[nH]cn1 Chemical compound Cc1c(C(CC2)CCN2C(CC2)CCN2C([C@@H](Cc2cc(C)c3[nH]ncc3c2)NC(N(CC2)CCC2C2=Cc(cccc3)c3NC2=O)=O)=O)[nH]cn1 KLENFGVWYLLZFQ-PGUFJCEWSA-N 0.000 description 1
- 0 Cc1c2[n]ncc2cc(C[C@](C(N(CC2)CCC2N(CC2)CCC2[Al])=O)NC(N(CC2)CCC2=C(Cc(ccc(*)c2)c2N2)C2=O)=O)c1 Chemical compound Cc1c2[n]ncc2cc(C[C@](C(N(CC2)CCC2N(CC2)CCC2[Al])=O)NC(N(CC2)CCC2=C(Cc(ccc(*)c2)c2N2)C2=O)=O)c1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1519194.3 | 2015-10-30 | ||
| GBGB1519194.3A GB201519194D0 (en) | 2015-10-30 | 2015-10-30 | CGRP receptor antagonists |
| PCT/IB2016/056519 WO2017072723A1 (en) | 2015-10-30 | 2016-10-28 | Cgrp receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532790A JP2018532790A (ja) | 2018-11-08 |
| JP2018532790A5 true JP2018532790A5 (https=) | 2019-12-05 |
| JP6874014B2 JP6874014B2 (ja) | 2021-05-19 |
Family
ID=55130446
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018541593A Active JP6874014B2 (ja) | 2015-10-30 | 2016-10-28 | Ｃｇｒｐ受容体アンタゴニスト |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US9688660B2 (https=) |
| EP (1) | EP3368526B1 (https=) |
| JP (1) | JP6874014B2 (https=) |
| CN (1) | CN108430991B (https=) |
| AR (1) | AR106487A1 (https=) |
| AU (1) | AU2016344689A1 (https=) |
| BR (1) | BR112018008416A2 (https=) |
| CA (1) | CA3002625A1 (https=) |
| GB (1) | GB201519194D0 (https=) |
| IL (1) | IL258894A (https=) |
| SG (1) | SG11201803382XA (https=) |
| TW (1) | TW201722936A (https=) |
| WO (1) | WO2017072723A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519196D0 (en) | 2015-10-30 | 2015-12-16 | Heptares Therapeutics Ltd | CGRP Receptor Antagonists |
| GB201519194D0 (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 |
| CN114980862A (zh) * | 2019-12-17 | 2022-08-30 | 拜尔哈文制药股份有限公司 | Cgrp抑制剂的鼻内药物组合物 |
| WO2024046223A1 (zh) * | 2022-08-30 | 2024-03-07 | 熙源安健医药（上海）有限公司 | 吲唑甲酰胺类衍生物及其制备方法和用途 |
Family Cites Families (28)
| 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 |
| SK285631B6 (sk) | 1996-09-10 | 2007-05-03 | Dr. Karl Thomae Gmbh | Modifikované aminokyseliny, farmaceutický prostriedok s ich obsahom a ich použitie |
| US20030069231A1 (en) | 1999-10-12 | 2003-04-10 | Klaus Rudolf | Modified aminoacids, pharmaceuticals containing these compounds and method for their production |
| WO1999064002A1 (en) | 1998-06-11 | 1999-12-16 | Merck & Co., Inc. | Spiropiperidine derivatives as melanocortin receptor agonists |
| US6294534B1 (en) | 1998-06-11 | 2001-09-25 | Merck & Co., Inc. | Spiropiperidine derivatives as melanocortin receptor agonists |
| DE19952146A1 (de) * | 1999-10-29 | 2001-06-07 | Boehringer Ingelheim Pharma | Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| RS52552B (sr) * | 2002-06-05 | 2013-04-30 | Bristol-Myers Squibb Company | Antagonisti, peptidnog receptora koji je u vezi sa kalcitoninskim genom |
| US7842808B2 (en) | 2002-06-05 | 2010-11-30 | Bristol-Myers Squibb Company | Anti-migraine spirocycles |
| JO2355B1 (en) | 2003-04-15 | 2006-12-12 | ميرك شارب اند دوم كوربوريشن | Hereditary calcitonin polypeptide receptor antagonists |
| TW200524601A (en) | 2003-12-05 | 2005-08-01 | Bristol Myers Squibb Co | Heterocyclic anti-migraine agents |
| RS20060382A (sr) | 2003-12-05 | 2008-09-29 | Bristol-Myers Squibb Company, | Antagonisti receptora za peptid povezan sa genom za kalcitonin |
| TW200533398A (en) | 2004-03-29 | 2005-10-16 | Bristol Myers Squibb Co | Novel therapeutic agents for the treatment of migraine |
| DE102004015723A1 (de) | 2004-03-29 | 2005-10-20 | Boehringer Ingelheim Pharma | 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 |
| BRPI0517418A (pt) | 2004-10-13 | 2008-10-07 | Merck & Co Inc | composto, composição farmacêutica, e, métodos para antagonismo de atividade do receptor de cgrp em um mamìfero, para tratar, controlar, melhorar ou reduzir o risco de dor de cabeça, enxaqueca ou cefalgia, e de tratamento ou prevenção de dores de cabeça de enxaqueca, cefalgias, e dores de cabeça |
| WO2006044449A2 (en) | 2004-10-14 | 2006-04-27 | Merck & Co., Inc. | Cgrp receptor antagonists |
| DE602005027230D1 (de) | 2004-10-22 | 2011-05-12 | Merck Sharp & Dohme | Cgrp-rezeptorantagonisten |
| 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 |
| CN102256963B (zh) * | 2008-12-19 | 2014-06-11 | 贝林格尔.英格海姆国际有限公司 | 作为ccr2受体拮抗剂用于治疗炎症、哮喘和copd的环状嘧啶-4-甲酰胺 |
| 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 |
-
2015
- 2015-10-30 GB GBGB1519194.3A patent/GB201519194D0/en not_active Ceased
-
2016
- 2016-10-28 JP JP2018541593A patent/JP6874014B2/ja active Active
- 2016-10-28 AR ARP160103294A patent/AR106487A1/es unknown
- 2016-10-28 AU AU2016344689A patent/AU2016344689A1/en not_active Abandoned
- 2016-10-28 BR BR112018008416A patent/BR112018008416A2/pt not_active Application Discontinuation
- 2016-10-28 EP EP16808804.5A patent/EP3368526B1/en active Active
- 2016-10-28 CA CA3002625A patent/CA3002625A1/en not_active Abandoned
- 2016-10-28 TW TW105135025A patent/TW201722936A/zh unknown
- 2016-10-28 WO PCT/IB2016/056519 patent/WO2017072723A1/en not_active Ceased
- 2016-10-28 CN CN201680063940.2A patent/CN108430991B/zh active Active
- 2016-10-28 US US15/336,893 patent/US9688660B2/en active Active
- 2016-10-28 SG SG11201803382XA patent/SG11201803382XA/en unknown
-
2017
- 2017-05-05 US US15/588,051 patent/US9925178B2/en active Active
-
2018
- 2018-01-29 US US15/882,038 patent/US10166226B2/en active Active
- 2018-04-24 IL IL258894A patent/IL258894A/en unknown
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