TWI896548B - 用於治療cns病症之組合物及方法 - Google Patents

用於治療cns病症之組合物及方法

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Publication number
TWI896548B
TWI896548B TW109121959A TW109121959A TWI896548B TW I896548 B TWI896548 B TW I896548B TW 109121959 A TW109121959 A TW 109121959A TW 109121959 A TW109121959 A TW 109121959A TW I896548 B TWI896548 B TW I896548B
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TW
Taiwan
Prior art keywords
substituted
unsubstituted
compound
group
alkyl
Prior art date
Application number
TW109121959A
Other languages
English (en)
Chinese (zh)
Other versions
TW202114695A (zh
Inventor
佩拉杜 馬利亞 耶穌 巴蘭可
法藍西司科 G 薩突羅
馬歇爾 理 莫寧斯塔爾
Original Assignee
美商賽吉醫療公司
Priority date (The priority date 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 date listed.)
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Publication date
Application filed by 美商賽吉醫療公司 filed Critical 美商賽吉醫療公司
Publication of TW202114695A publication Critical patent/TW202114695A/zh
Application granted granted Critical
Publication of TWI896548B publication Critical patent/TWI896548B/zh

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/002—Expansion of ring A by one atom, e.g. A homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
TW109121959A 2019-06-27 2020-06-29 用於治療cns病症之組合物及方法 TWI896548B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962867695P 2019-06-27 2019-06-27
US201962867736P 2019-06-27 2019-06-27
US201962867734P 2019-06-27 2019-06-27
US62/867,695 2019-06-27
US62/867,734 2019-06-27
US62/867,736 2019-06-27

Publications (2)

Publication Number Publication Date
TW202114695A TW202114695A (zh) 2021-04-16
TWI896548B true TWI896548B (zh) 2025-09-11

Family

ID=71728948

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109121959A TWI896548B (zh) 2019-06-27 2020-06-29 用於治療cns病症之組合物及方法

Country Status (10)

Country Link
US (2) US20230257415A1 (https=)
EP (1) EP3990468A1 (https=)
JP (2) JP7670632B2 (https=)
CN (1) CN114729000A (https=)
AU (1) AU2020304679A1 (https=)
BR (1) BR112021026445A2 (https=)
CA (1) CA3143545A1 (https=)
MX (1) MX2021015854A (https=)
TW (1) TWI896548B (https=)
WO (1) WO2020264512A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015002252A (es) 2012-08-21 2015-07-21 Sage Therapeutics Inc Metodos para tratar epilepsia o estado de epilepsia.
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス， インコーポレイテッド １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
TWI904593B (zh) 2016-08-23 2025-11-11 美商賽吉醫療公司 結晶19-去甲c3,3-二取代之c21-n-吡唑類固醇
EP3720867A1 (en) 2017-12-08 2020-10-14 Sage Therapeutics, Inc. Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders
CN113166193B (zh) 2018-10-12 2025-08-19 萨奇治疗股份有限公司 用于治疗cns病症的在位置10处被环状基团取代的神经活性类固醇
IL283629B2 (en) 2018-12-05 2026-03-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
CN116589521B (zh) * 2019-01-08 2025-07-11 成都康弘药业集团股份有限公司 甾体类化合物、用途及其制备方法
CR20240234A (es) 2019-05-31 2024-07-09 Sage Therapeutics Inc ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629)
JP7787635B2 (ja) 2019-06-27 2025-12-17 セージ セラピューティクス， エルエルシー Ｃｎｓ障害を治療するための組成物及び方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2969M (fr) * 1963-05-22 1964-11-30 Roussel Uclaf Nouveau médicament notamment pour le traitement des spasmes d'origine coronarienne on viscérale.
ES432106A1 (es) * 1973-11-30 1976-11-01 Schering Ag Procedimiento para la preparacion de d-homo-20-cetopregna- nos.
IL48628A0 (en) * 1974-12-23 1976-02-29 Schering Ag D-homo-20-keto-pregnanes and process for their manufactur
GB1570394A (en) * 1976-01-06 1980-07-02 Glaxo Lab Ltd 11-acyloxy-3-hydroxy steroids
GB1581234A (en) * 1976-04-05 1980-12-10 Glaxo Operations Ltd 11a - amino - 3a - hydroxysteroids
GB1581235A (en) * 1977-04-04 1980-12-10 Glaxo Operations Ltd 11a-amino-3a-hydroxy-steroids
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス， インコーポレイテッド １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法
EP4155314A1 (en) 2015-02-20 2023-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
CN111741965B (zh) 2017-12-22 2024-06-25 萨奇治疗股份有限公司 治疗中枢神经系统疾病的组合物和方法
CN114656514B (zh) * 2018-02-11 2024-05-14 江苏豪森药业集团有限公司 一种甾族类衍生物调节剂及其制备方法和应用
IL283629B2 (en) * 2018-12-05 2026-03-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Photodynamic Effects of Steroid-Conjugated Fluorophores on GABAA Receptors Mol Pharmacol 76:754–765, 2009 2009年10月 https://pubmed.ncbi.nlm.nih.gov/19596835/ *
網路文獻 ,Hong-Jin Shu, Lawrence N. Eisenman, Cunde Wang, Achintya K. Bandyopadhyaya,Kathiresan Krishnan, Amanda Taylor, Ann M. Benz, Brad Manion, Alex S. Evers,Douglas F. Covey, Charles F. Zorumski, and Steven Mennerick *
網路文獻 ,Hong-Jin Shu, Lawrence N. Eisenman, Cunde Wang, Achintya K. Bandyopadhyaya,Kathiresan Krishnan, Amanda Taylor, Ann M. Benz, Brad Manion, Alex S. Evers,Douglas F. Covey, Charles F. Zorumski, and Steven Mennerick。 Photodynamic Effects of Steroid-Conjugated Fluorophores on GABAA Receptors Mol Pharmacol 76:754–765, 2009 2009年10月 https://pubmed.ncbi.nlm.nih.gov/19596835/

Also Published As

Publication number Publication date
BR112021026445A2 (pt) 2022-03-08
JP2022538301A (ja) 2022-09-01
US20230257415A1 (en) 2023-08-17
MX2021015854A (es) 2022-04-18
CA3143545A1 (en) 2020-12-30
CN114729000A (zh) 2022-07-08
AU2020304679A1 (en) 2022-01-20
JP7670632B2 (ja) 2025-04-30
TW202114695A (zh) 2021-04-16
EP3990468A1 (en) 2022-05-04
US20240300996A1 (en) 2024-09-12
JP2025065311A (ja) 2025-04-17
WO2020264512A1 (en) 2020-12-30

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