JP2020536898A - スピロ誘導体を調製するためのプロセス - Google Patents

スピロ誘導体を調製するためのプロセス Download PDF

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Publication number
JP2020536898A
JP2020536898A JP2020520223A JP2020520223A JP2020536898A JP 2020536898 A JP2020536898 A JP 2020536898A JP 2020520223 A JP2020520223 A JP 2020520223A JP 2020520223 A JP2020520223 A JP 2020520223A JP 2020536898 A JP2020536898 A JP 2020536898A
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Prior art keywords
compound
methyl
preparing
solution
stirred
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JP2020520223A
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Japanese (ja)
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JP2020536898A5 (enExample
Inventor
エム．ピー．ギブリン ジェラルド
エム．ピー．ギブリン ジェラルド
ティー．マクファーソン デイビッド
ティー．マクファーソン デイビッド
スレイマン オサマ
スレイマン オサマ
ウィリアムス マイケル
ウィリアムス マイケル
アール．ウィッティ デイビッド
アール．ウィッティ デイビッド
ボンナウド ティエリー
ボンナウド ティエリー
エドワーズ リチャード
エドワーズ リチャード
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Biogen Inc
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Biogen Inc
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Publication of JP2020536898A publication Critical patent/JP2020536898A/ja
Publication of JP2020536898A5 publication Critical patent/JP2020536898A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C07C65/05—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
    • C07C65/10—Salicylic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Measuring Volume Flow (AREA)
  • Exhaust Gas After Treatment (AREA)
  • Pyrrole Compounds (AREA)
JP2020520223A 2017-10-10 2018-10-10 スピロ誘導体を調製するためのプロセス Withdrawn JP2020536898A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762570269P 2017-10-10 2017-10-10
US62/570,269 2017-10-10
PCT/US2018/055227 WO2019075073A2 (en) 2017-10-10 2018-10-10 PROCESS FOR THE PREPARATION OF SPIRO DERIVATIVES

Publications (2)

Publication Number Publication Date
JP2020536898A true JP2020536898A (ja) 2020-12-17
JP2020536898A5 JP2020536898A5 (enExample) 2021-12-02

Family

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JP2020520223A Withdrawn JP2020536898A (ja) 2017-10-10 2018-10-10 スピロ誘導体を調製するためのプロセス

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US (2) US11149039B2 (enExample)
EP (1) EP3694510A4 (enExample)
JP (1) JP2020536898A (enExample)
KR (1) KR20200068678A (enExample)
CN (1) CN111526874A (enExample)
AU (1) AU2018347349A1 (enExample)
CA (1) CA3077088A1 (enExample)
IL (1) IL273695A (enExample)
MA (1) MA50371A (enExample)
MX (2) MX2020003821A (enExample)
SG (1) SG11202002707VA (enExample)
WO (1) WO2019075073A2 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2020003821A (es) 2017-10-10 2023-01-12 Biogen Inc Proceso de elaboración de espiroderivados.

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008533076A (ja) * 2005-03-15 2008-08-21 エフ．ホフマン−ラ ロシュ アーゲー Ｍａｏｂ阻害剤としての純粋な４−ピロリジノフェニルベンジルエーテル誘導体の製造方法
WO2011013785A1 (ja) * 2009-07-31 2011-02-03 日本たばこ産業株式会社 含窒素スピロ環化合物及びその医薬用途
JP2014501767A (ja) * 2011-01-07 2014-01-23 エフ．ホフマン−ラ ロシュ アーゲー Ｎｋ３アンタゴニストとしてのピロリジン誘導体
JP2014512401A (ja) * 2011-04-26 2014-05-22 エフ．ホフマン−ラ ロシュ アーゲー ｍＧｌｕＲ５の陽性アロステリックモジュレーターとしてのエチニル誘導体
JP2015502394A (ja) * 2011-12-22 2015-01-22 クオンベルゲンセ プハルマセウトイカルス リミテッド 電位依存性ナトリウムチャネルモジュレーターとしての２−（ピリジン−２イル）−１，７−ジアザ−スピロ［４．４］ノナン−６−オン化合物
JP2015517562A (ja) * 2012-05-22 2015-06-22 クオンベルゲンセ プハルマセウトイカルス リミテッド 新規化合物

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US814396A (en) 1905-05-22 1906-03-06 Joseph R Russell Burner for liquid fuel.
KR0178475B1 (ko) * 1995-09-14 1999-03-20 윤덕용 신규한 n-비닐락탐 유도체 및 그의 중합체
PT1519939E (pt) 2002-07-05 2010-02-10 Targacept Inc Compostos n-arildiazaspirocíclicos e métodos para a sua preparação e utilização
TW200728258A (en) 2005-10-10 2007-08-01 Glaxo Group Ltd Novel compounds
TW200730494A (en) 2005-10-10 2007-08-16 Glaxo Group Ltd Novel compounds
US8143306B2 (en) 2005-10-10 2012-03-27 Convergence Pharmaceuticals Limited Methods of treating bipolar disorders
GB0520578D0 (en) 2005-10-10 2005-11-16 Glaxo Group Ltd Novel compounds
EP1943216B1 (en) 2005-10-10 2010-06-30 Glaxo Group Limited Prolinamide derivatives as sodium channel modulators
WO2008046049A1 (en) 2006-10-12 2008-04-17 Xenon Pharmaceuticals Inc. Spiro (furo [3, 2-c] pyridine-3-3 ' -indol) -2' (1'h)-one derivatives and related compounds for the treatment of sodium-channel mediated diseases, such as pain
BRPI0719166A2 (pt) 2006-10-12 2014-06-03 Xenon Pharmaceuticals Inc Derivados de espiro-oxindol tricíclicos e seus usos como agentes terapêuticos
GB0701365D0 (en) 2007-01-24 2007-03-07 Glaxo Group Ltd Novel pharmaceutical compositions
GB0701366D0 (en) 2007-01-24 2007-03-07 Glaxo Group Ltd Novel pharmaceutical compositions
US8093268B2 (en) 2007-01-24 2012-01-10 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)
GB0706630D0 (en) 2007-04-04 2007-05-16 Glaxo Group Ltd Novel compounds
AR077252A1 (es) 2009-06-29 2011-08-10 Xenon Pharmaceuticals Inc Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos
DK2477964T5 (en) 2009-09-14 2015-05-26 Convergence Pharmaceuticals A process for the preparation of alpha-carboxamide
GB201209670D0 (en) 2012-05-31 2012-07-18 Convergence Pharmaceuticals Novel compounds
DK3177603T3 (en) * 2014-08-04 2019-01-14 Merck Patent Gmbh PYRROLIDINE UNDERIVATIVES AS METAP-2 INHIBITORS
JP2020536070A (ja) 2017-09-28 2020-12-10 バイオジェン インコーポレイテッド 新規な塩
MX2020003821A (es) 2017-10-10 2023-01-12 Biogen Inc Proceso de elaboración de espiroderivados.

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008533076A (ja) * 2005-03-15 2008-08-21 エフ．ホフマン−ラ ロシュ アーゲー Ｍａｏｂ阻害剤としての純粋な４−ピロリジノフェニルベンジルエーテル誘導体の製造方法
WO2011013785A1 (ja) * 2009-07-31 2011-02-03 日本たばこ産業株式会社 含窒素スピロ環化合物及びその医薬用途
JP2014501767A (ja) * 2011-01-07 2014-01-23 エフ．ホフマン−ラ ロシュ アーゲー Ｎｋ３アンタゴニストとしてのピロリジン誘導体
JP2014512401A (ja) * 2011-04-26 2014-05-22 エフ．ホフマン−ラ ロシュ アーゲー ｍＧｌｕＲ５の陽性アロステリックモジュレーターとしてのエチニル誘導体
JP2015502394A (ja) * 2011-12-22 2015-01-22 クオンベルゲンセ プハルマセウトイカルス リミテッド 電位依存性ナトリウムチャネルモジュレーターとしての２−（ピリジン−２イル）−１，７−ジアザ−スピロ［４．４］ノナン−６−オン化合物
JP2015517562A (ja) * 2012-05-22 2015-06-22 クオンベルゲンセ プハルマセウトイカルス リミテッド 新規化合物

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ADVANCED SYNTHESIS & CATALYSIS, vol. Vol.353(18), JPN6022048116, 2011, pages 3313 - 3318, ISSN: 0005132949 *
AMINO ACIDS, vol. Vol.46(4), JPN6022048117, 2014, pages 1097 - 1103, ISSN: 0005132950 *

Also Published As

Publication number Publication date
MX2020003821A (es) 2023-01-12
CN111526874A (zh) 2020-08-11
WO2019075073A2 (en) 2019-04-18
CA3077088A1 (en) 2019-04-18
US20200325144A1 (en) 2020-10-15
WO2019075073A3 (en) 2020-04-02
EP3694510A4 (en) 2021-06-30
US20220033408A1 (en) 2022-02-03
AU2018347349A1 (en) 2020-04-23
EP3694510A2 (en) 2020-08-19
SG11202002707VA (en) 2020-04-29
IL273695A (en) 2020-05-31
MX2022013928A (es) 2022-11-30
KR20200068678A (ko) 2020-06-15
MA50371A (fr) 2021-03-31
US11149039B2 (en) 2021-10-19

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