IL264129B2 - C17, c20, and c21 substituted neuroactive steroids and their methods of use - Google Patents
C17, c20, and c21 substituted neuroactive steroids and their methods of useInfo
- Publication number
- IL264129B2 IL264129B2 IL264129A IL26412919A IL264129B2 IL 264129 B2 IL264129 B2 IL 264129B2 IL 264129 A IL264129 A IL 264129A IL 26412919 A IL26412919 A IL 26412919A IL 264129 B2 IL264129 B2 IL 264129B2
- Authority
- IL
- Israel
- Prior art keywords
- compound
- alkyl
- hydrogen
- aryl
- heteroaryl
- Prior art date
Links
Classifications
-
- 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
- C07J41/0066—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 a carbon atom forming 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
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
- C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
- C07J1/0029—Ethers
-
- 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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
-
- 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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0085—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being a saturated hydrocarbon group
-
- 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
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
- C07J41/0011—Unsubstituted amino radicals
-
- 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
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Toxicology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Addiction (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662360847P | 2016-07-11 | 2016-07-11 | |
| US201662360813P | 2016-07-11 | 2016-07-11 | |
| US201662424083P | 2016-11-18 | 2016-11-18 | |
| PCT/US2017/041600 WO2018013613A1 (en) | 2016-07-11 | 2017-07-11 | C17, c20, and c21 substituted neuroactive steroids and their methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| IL264129A IL264129A (en) | 2019-02-28 |
| IL264129B1 IL264129B1 (en) | 2024-01-01 |
| IL264129B2 true IL264129B2 (en) | 2024-05-01 |
Family
ID=60952660
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL264129A IL264129B2 (en) | 2016-07-11 | 2017-07-11 | C17, c20, and c21 substituted neuroactive steroids and their methods of use |
| IL309259A IL309259A (en) | 2016-07-11 | 2017-07-11 | C17, C20 and C21 converted neuroactive steroids and methods of using them |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL309259A IL309259A (en) | 2016-07-11 | 2017-07-11 | C17, C20 and C21 converted neuroactive steroids and methods of using them |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11396525B2 (enExample) |
| EP (2) | EP3481845B1 (enExample) |
| JP (3) | JP7049313B2 (enExample) |
| CN (2) | CN116162121A (enExample) |
| AU (3) | AU2017297375B2 (enExample) |
| CA (1) | CA3030413A1 (enExample) |
| DK (1) | DK3481845T3 (enExample) |
| ES (1) | ES2965214T3 (enExample) |
| IL (2) | IL264129B2 (enExample) |
| MA (1) | MA45599A (enExample) |
| NZ (3) | NZ790226A (enExample) |
| WO (1) | WO2018013613A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2738526T3 (es) | 2011-10-14 | 2020-01-23 | Sage Therapeutics Inc | Compuestos 19-norpregnano 3,3-disustituidos, composiciones y usos de los mismos |
| IL275725B (en) | 2012-08-21 | 2022-08-01 | Sage Therapeutics Inc | Treatment methods for epilepsy and status epilepticus |
| RS60420B1 (sr) | 2013-04-17 | 2020-07-31 | Sage Therapeutics Inc | 19-nor neuroaktivni steroidi za metode lečenja |
| US9725481B2 (en) | 2013-04-17 | 2017-08-08 | Sage Therapeutics, Inc. | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof |
| AU2014256229B2 (en) | 2013-04-17 | 2018-10-04 | Sage Therapeutics, Inc. | 19-nor C3,3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| PL3021852T3 (pl) | 2013-07-19 | 2021-07-05 | Sage Therapeutics, Inc. | Neuroaktywne steroidy, kompozycje i ich zastosowania |
| JP6466942B2 (ja) | 2013-08-23 | 2019-02-06 | セージ セラピューティクス, インコーポレイテッド | 向神経活性ステロイド、組成物、及びその使用 |
| US10246482B2 (en) | 2014-06-18 | 2019-04-02 | 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 |
| HUE051488T2 (hu) | 2014-10-16 | 2021-03-01 | Sage Therapeutics Inc | Készítmények és eljárások központi idegrendszeri rendellenességek kezelésére |
| WO2016061527A1 (en) | 2014-10-16 | 2016-04-21 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| US10774108B2 (en) | 2014-11-27 | 2020-09-15 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| PL3250210T3 (pl) | 2015-01-26 | 2021-07-26 | Sage Therapeutics, Inc. | Kompozycje i sposoby leczenia zaburzeń OUN |
| JP6875996B2 (ja) | 2015-02-20 | 2021-05-26 | セージ セラピューティクス, インコーポレイテッド | 神経刺激性ステロイド、組成物、およびその使用 |
| JP7049313B2 (ja) | 2016-07-11 | 2022-04-06 | セージ セラピューティクス, インコーポレイテッド | C17、c20、およびc21置換神経刺激性ステロイドおよびそれらの使用方法 |
| ES2992037T3 (es) | 2016-07-11 | 2024-12-05 | Sage Therapeutics Inc | Esteroides neuroactivos sustituidos en C7, C12 y C16 y sus procedimientos de utilización |
| NZ791594A (en) | 2016-08-23 | 2025-08-29 | Sage Therapeutics Inc | A crystalline 19-nor C3, 3-disubstituted C21-N-pyrazolyl steroid |
| WO2019113494A1 (en) | 2017-12-08 | 2019-06-13 | Sage Therapeutics, Inc. | Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders |
| EP3867261B1 (en) * | 2018-10-19 | 2025-04-30 | Sage Therapeutics, Inc. | 9(11)-unsaturated neuroactive steroids and their methods of use |
| CN109369762B (zh) * | 2018-10-31 | 2021-06-18 | 湖南玉新药业有限公司 | 17-甲酸甾族化合物的制备方法 |
| JP7692830B2 (ja) * | 2018-12-21 | 2025-06-16 | セージ セラピューティクス, インコーポレイテッド | 3α-ヒドロキシ-17β-アミド神経刺激性ステロイドおよびその組成物 |
| EP3962921B1 (en) * | 2019-04-27 | 2025-11-05 | Health Research, Inc. | Coumarin-modified androgens for the treatment of prostate cancer |
| EP3965772A4 (en) | 2019-05-10 | 2023-05-10 | Brii Biosciences, Inc. | Pharmaceutical composition containing brexanolone, ganaxolone, or zuranolone, and use thereof |
| CR20240234A (es) | 2019-05-31 | 2024-07-09 | Sage Therapeutics Inc | ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629) |
| CA3143545A1 (en) | 2019-06-27 | 2020-12-30 | Sage Therapeutics, Inc. | Compounds for treating cns disorders |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| MX2022008614A (es) * | 2020-01-12 | 2022-10-10 | Brii Biosciences Inc | Esteroides neuroactivos y composicion farmaceutica que contiene los mismos. |
| PE20221911A1 (es) | 2020-03-25 | 2022-12-23 | Sage Therapeutics Inc | Uso de agentes para el tratamiento de condiciones respiratorias |
| CA3183248A1 (en) * | 2020-06-24 | 2021-12-30 | Sage Therapeutics, Inc. | 3.alpha.-hydroxy, 17.beta.-c(o)-n-aryl substituted neuroactive steroids and compositions thereof |
| CN116574151A (zh) * | 2023-03-13 | 2023-08-11 | 奥锐特药业股份有限公司 | 一种醋酸阿比特龙及其中间体的制备方法 |
| WO2023213151A1 (zh) * | 2022-05-06 | 2023-11-09 | 奥锐特药业股份有限公司 | 一种醋酸阿比特龙及其中间体的制备方法 |
| CN119751535B (zh) * | 2024-12-26 | 2025-10-31 | 浙江仙琚制药股份有限公司 | 一种孕烷醇酮的制备方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1380246A (en) * | 1970-12-17 | 1975-01-08 | Glaxo Lab Ltd | 3alpha-hydroxy-androstanes and esters thereof |
| WO2014169832A1 (en) * | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| WO2016061527A1 (en) * | 2014-10-16 | 2016-04-21 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| WO2016082789A1 (en) * | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2856415A (en) | 1957-11-13 | 1958-10-14 | Searle & Co | 3,19-dihydroxy-5-androstene derivatives |
| FR1380417A (fr) | 1962-05-15 | 1964-12-04 | Roussel Uclaf | Nouveaux androstanyl-pyrazoles et procédé de préparation |
| US3206459A (en) | 1962-10-19 | 1965-09-14 | Syntex Corp | 10alpha-pregnan-19-ol derivatives |
| US3169134A (en) | 1963-03-21 | 1965-02-09 | Searle & Co | 2, 3-oxygenated-17alpha-methyl-5alpha-androstan-17beta-ols |
| BE754111A (fr) | 1969-07-29 | 1971-01-29 | Upjohn Co | Nouveaux 7alpha- et 7beta-methyl-3alpha,5alpha- cycloandrostanes et composes analogues 19-nor et leur procede de preparation |
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| GB1434919A (en) | 1972-06-15 | 1976-05-12 | Glaxo Lab Ltd | 3alpha-hydroxy androstanes |
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| GB1430942A (en) | 1972-05-05 | 1976-04-07 | Glaxo Lab Ltd | 21-substituted 3alpha-hydroxy pregnanes |
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| US5232917A (en) | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
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