AR083399A1 - Proceso para la preparacion de cicloheptapiridina como antagonista del receptor de cgrp - Google Patents
Proceso para la preparacion de cicloheptapiridina como antagonista del receptor de cgrpInfo
- Publication number
- AR083399A1 AR083399A1 ARP110103778A ARP110103778A AR083399A1 AR 083399 A1 AR083399 A1 AR 083399A1 AR P110103778 A ARP110103778 A AR P110103778A AR P110103778 A ARP110103778 A AR P110103778A AR 083399 A1 AR083399 A1 AR 083399A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- preparation
- salt
- group
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 238000002360 preparation method Methods 0.000 title abstract 3
- 108090000932 Calcitonin Gene-Related Peptide Proteins 0.000 title 1
- 102100025588 Calcitonin gene-related peptide 1 Human genes 0.000 title 1
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 230000008878 coupling Effects 0.000 abstract 1
- 238000010168 coupling process Methods 0.000 abstract 1
- 238000005859 coupling reaction Methods 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 238000010511 deprotection reaction Methods 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- -1 phenoxy, substituted phenoxy , phenylthio Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 238000006268 reductive amination reaction Methods 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 125000004665 trialkylsilyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/04—Ortho- or peri-condensed ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
Un proceso para la preparación de compuestos de la fórmula (1), que incluyen intermediarios de síntesis que son útiles en el proceso.Reivindicación 1: Un proceso para la preparación de un compuesto de la fórmula (1) o una sal de este, en donde Ar1 es fenilo sustituido por 0 - 3 sustituyentes seleccionados del grupo que consiste en ciano, halo, alquilo, haloalquilo, alcoxi, haloalcoxi y SO2-alquilo, caracterizado porque comprende la aminación reductora y la desprotección de alcohol de un compuesto de la fórmula (4) o una sal de este, en donde R1 se selecciona del grupo que consiste en trialquilsililo, alcoxi, alquilcarbonilo, bencilo, benzoilo y pivaloilo a un compuesto de la fórmula (2) o una sal de este, en donde R1 es hidrógeno; y el acoplamiento del compuesto de la fórmula (2) con un compuesto de la fórmula (3) o una sal de este, en donde R2 se selecciona del grupo que consiste en imidazolilo, pirrolilo, N-hidroxisuccinimidilo, cloro, fenoxi, fenoxi sustituido, feniltio y feniltio sustituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39218310P | 2010-10-12 | 2010-10-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083399A1 true AR083399A1 (es) | 2013-02-21 |
Family
ID=44720182
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103778A AR083399A1 (es) | 2010-10-12 | 2011-10-12 | Proceso para la preparacion de cicloheptapiridina como antagonista del receptor de cgrp |
Country Status (4)
| Country | Link |
|---|---|
| US (5) | US8669368B2 (es) |
| AR (1) | AR083399A1 (es) |
| TW (1) | TW201219390A (es) |
| WO (1) | WO2012050764A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2470207A1 (en) | 2009-08-28 | 2012-07-04 | Rinat Neuroscience Corporation | Methods for treating visceral pain by administering antagonist antibodies directed against calcitonin gene-related peptide |
| US8669368B2 (en) | 2010-10-12 | 2014-03-11 | Bristol-Myers Squibb Company | Process for the preparation of cycloheptapyridine CGRP receptor antagonists |
| SI3254681T1 (sl) | 2012-02-27 | 2019-10-30 | Bristol Myers Squibb Co | N-(5S,6S,9R)-5-amino-6-(2,3-difluorofenil)-6,7,8,9-tetrahidro-5H-ciklo- hepta(B)piridin-9-IL-4-(2-okso-2,3-dihidro-1H-imidazo(4,5-B)piridin-1- IL)piperidin-1-karboksilatna sol |
| US10556945B2 (en) | 2014-03-21 | 2020-02-11 | Teva Pharmaceuticals International Gmbh | Antagonist antibodies directed against calcitonin gene-related peptide and methods using same |
| JP6568099B2 (ja) | 2014-03-21 | 2019-08-28 | テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハーＴｅｖａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｔｅｒｎａｔｉｏｎａｌ ＧｍｂＨ | カルシトニン遺伝子関連ペプチドに対するアンタゴニスト抗体及びその使用方法 |
| KR20220031944A (ko) | 2016-09-23 | 2022-03-14 | 테바 파마슈티컬스 인터내셔널 게엠베하 | 불응성 편두통의 치료 |
| WO2019191008A1 (en) | 2018-03-25 | 2019-10-03 | Biohaven Pharmaceutical Holding Company Ltd. | Rimegepant for cgrp related disorders |
| JP2024505509A (ja) * | 2021-02-01 | 2024-02-06 | ファイザー アイルランド ファーマシューティカルズ | Ｃｇｒｐ阻害薬の医薬組成物およびそれらを使用する方法 |
| CN115850266A (zh) * | 2021-09-26 | 2023-03-28 | 奥锐特药业(天津)有限公司 | 瑞美吉泮新晶型及其制备方法 |
| CN116554164A (zh) * | 2022-01-27 | 2023-08-08 | 奥锐特药业(天津)有限公司 | 一种瑞美吉泮的制备方法 |
| CN116478211B (zh) * | 2022-04-19 | 2023-10-24 | 石家庄迪斯凯威医药科技有限公司 | 一种新型cgrp受体拮抗剂及其用途 |
| CN115677694A (zh) * | 2022-11-30 | 2023-02-03 | 南通常佑药业科技有限公司 | 一种瑞美吉泮的合成方法 |
| CN117486798A (zh) * | 2023-12-21 | 2024-02-02 | 南京威凯尔生物医药科技有限公司 | 一种瑞美吉泮中间体盐酸盐的晶型及其制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2355B1 (en) | 2003-04-15 | 2006-12-12 | ميرك شارب اند دوم كوربوريشن | Hereditary calcitonin polypeptide receptor antagonists |
| CN101232887A (zh) * | 2005-07-29 | 2008-07-30 | 默克公司 | 杂环苯并二氮杂䓬cgrp受体拮抗剂 |
| AU2007238894A1 (en) | 2006-04-10 | 2007-10-25 | Merck Sharp & Dohme Corp. | Process for the preparation of pyridine heterocycle CGRP antagonist intermediate |
| ES2303776B1 (es) * | 2006-12-29 | 2009-08-07 | Laboratorios Almirall S.A. | Derivados de 5-fenil-6-piridin-4-il-1,3-dihidro-2h-imidazo(4,5-b)piridin-2-ona utiles como antagonistas del receptor de adenosina a2b. |
| 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 |
| US8669368B2 (en) | 2010-10-12 | 2014-03-11 | Bristol-Myers Squibb Company | Process for the preparation of cycloheptapyridine CGRP receptor antagonists |
-
2011
- 2011-09-19 US US13/236,072 patent/US8669368B2/en active Active
- 2011-09-21 WO PCT/US2011/052459 patent/WO2012050764A1/en active Application Filing
- 2011-10-12 TW TW100137018A patent/TW201219390A/zh unknown
- 2011-10-12 AR ARP110103778A patent/AR083399A1/es not_active Application Discontinuation
-
2014
- 2014-01-16 US US14/156,626 patent/US20140135500A1/en not_active Abandoned
- 2014-12-12 US US14/568,370 patent/US20150099887A1/en not_active Abandoned
-
2015
- 2015-08-24 US US14/833,891 patent/US20150361047A1/en not_active Abandoned
-
2016
- 2016-08-01 US US15/225,261 patent/US9718845B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20150361047A1 (en) | 2015-12-17 |
| US20140135500A1 (en) | 2014-05-15 |
| US9718845B2 (en) | 2017-08-01 |
| US8669368B2 (en) | 2014-03-11 |
| TW201219390A (en) | 2012-05-16 |
| WO2012050764A1 (en) | 2012-04-19 |
| US20160340373A1 (en) | 2016-11-24 |
| US20150099887A1 (en) | 2015-04-09 |
| US20120245356A1 (en) | 2012-09-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR083399A1 (es) | Proceso para la preparacion de cicloheptapiridina como antagonista del receptor de cgrp | |
| AR111813A2 (es) | Compuestos y composiciones para el control de nematodos | |
| CO6270320A2 (es) | Derivados de piperidina utiles como antagonistas del receptor orexina | |
| TN2011000279A1 (en) | Novel pyrazole -4-n-alkoxycarboxamides as microbiocides | |
| HRP20090235A2 (en) | Carbonylated (aza) cyclohexanes as dopamine d3 receptor ligands | |
| CU20110052A7 (es) | Compuestos orgánicos | |
| IN2014CN01136A (es) | ||
| AR055779A1 (es) | Proceso de preparacion de azoxistrobina y composicion que contiene al compuesto | |
| MY162760A (en) | Anti-infective agents and uses thereof | |
| MA35245B1 (fr) | Pyridin-2-amides utiles comme agonistes de cb2 | |
| EA201070912A1 (ru) | Производные оксима в качестве ингибиторов hsp90 | |
| DOP2011000123A (es) | Nuevos compuestos halosustituidos | |
| CL2012001517A1 (es) | Compuestos divalentes y heterociclicos unidos por puente oxa relacionados con nicotina; metodos de preparacion de los mismos; composicion agroquimica que comprende dichos compuestos. | |
| EA201100094A1 (ru) | Тиадиазолилоксифениламидины и их применение в качестве фунгицидов | |
| AR093184A1 (es) | Compuesto de pirimidina sustituida como inhibidor de quinurenina-3-monooxigenasa y composicion farmaceutica que lo comprenden | |
| AR079662A1 (es) | Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa | |
| AR079748A1 (es) | Arilpirrolidinas plaguicidas | |
| CY1112829T1 (el) | Νεα μεθοδος συνθεσης για την αγομελατινη | |
| NI200900151A (es) | Nuevo procedimiento de síntesis de la agomelatina. | |
| UA102289C2 (ru) | Гербициды, полученные из циклопентадиона | |
| MY152281A (en) | 4-pyrimidinesulfamide derivative | |
| EA201170282A1 (ru) | Фунгицидные n-циколоалкил-n-бифенилметилкарбоксамидные производные | |
| NI201000049A (es) | Método para producir 2'-desoxi-5-azacitidina (decitabina) | |
| MX337320B (es) | Análogos halogenados de agentes anti-fibroticos. | |
| AR072803A1 (es) | Tetrahidrocinolinas como inhibidores de la 11- beta -hsd1 para la diabetes |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |