AU2014324961A1 - Highly potent glucocorticoids - Google Patents
Highly potent glucocorticoids Download PDFInfo
- Publication number
- AU2014324961A1 AU2014324961A1 AU2014324961A AU2014324961A AU2014324961A1 AU 2014324961 A1 AU2014324961 A1 AU 2014324961A1 AU 2014324961 A AU2014324961 A AU 2014324961A AU 2014324961 A AU2014324961 A AU 2014324961A AU 2014324961 A1 AU2014324961 A1 AU 2014324961A1
- Authority
- AU
- Australia
- Prior art keywords
- compound
- alkyl
- group
- heteroaryl
- aryl
- 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.)
- Abandoned
Links
- 239000003862 glucocorticoid Substances 0.000 title abstract description 73
- 229940037128 systemic glucocorticoids Drugs 0.000 title description 40
- 230000003389 potentiating effect Effects 0.000 title description 19
- 150000001875 compounds Chemical class 0.000 claims abstract description 194
- 238000000034 method Methods 0.000 claims abstract description 36
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims description 135
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims description 135
- -1 -OH Chemical group 0.000 claims description 120
- 125000001072 heteroaryl group Chemical group 0.000 claims description 82
- 125000000217 alkyl group Chemical group 0.000 claims description 78
- 125000003118 aryl group Chemical group 0.000 claims description 77
- 230000000694 effects Effects 0.000 claims description 56
- 229910052739 hydrogen Inorganic materials 0.000 claims description 43
- 239000001257 hydrogen Substances 0.000 claims description 43
- 125000003545 alkoxy group Chemical group 0.000 claims description 37
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 30
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 27
- 150000003839 salts Chemical class 0.000 claims description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 21
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 19
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 18
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0036—Nitrogen-containing hetero ring
- C07J71/0042—Nitrogen only
- C07J71/0047—Nitrogen only at position 2(3)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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]
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
- C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
- C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361882444P | 2013-09-25 | 2013-09-25 | |
| US61/882,444 | 2013-09-25 | ||
| PCT/US2014/057497 WO2015048316A1 (en) | 2013-09-25 | 2014-09-25 | Highly potent glucocorticoids |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2014324961A1 true AU2014324961A1 (en) | 2016-04-14 |
| AU2014324961A8 AU2014324961A8 (en) | 2016-04-21 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014324961A Abandoned AU2014324961A1 (en) | 2013-09-25 | 2014-09-25 | Highly potent glucocorticoids |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9975918B2 (https=) |
| EP (1) | EP3049089B1 (https=) |
| JP (1) | JP2016531852A (https=) |
| KR (1) | KR20160060688A (https=) |
| CN (2) | CN105744937A (https=) |
| AU (1) | AU2014324961A1 (https=) |
| ES (1) | ES2751457T3 (https=) |
| HK (1) | HK1222565A1 (https=) |
| WO (1) | WO2015048316A1 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3319611T3 (pl) | 2015-07-06 | 2021-07-12 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| MX382122B (es) | 2015-07-06 | 2025-03-13 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| EP3436022B1 (en) | 2016-04-01 | 2022-03-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| PT3519422T (pt) | 2016-09-30 | 2022-12-05 | Sage Therapeutics Inc | Oxisteróis substituídos em c7 e métodos como moduladores nmda |
| CN110382033B (zh) | 2016-10-14 | 2022-04-15 | 范安德尔研究所 | 用于设计高效力糖皮质激素的结构与机制 |
| CA3041088C (en) | 2016-10-18 | 2024-05-21 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| DK4105223T3 (da) | 2016-10-18 | 2025-07-07 | Sage Therapeutics Inc | Oxysteroler og fremgangsmåder til anvendelse deraf |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| CN117024499A (zh) * | 2023-07-17 | 2023-11-10 | 陕西汉江药业集团股份有限公司 | 在2位引入亚甲基羟基的甾体化合物制备方法 |
| WO2025157225A1 (zh) * | 2024-01-24 | 2025-07-31 | 浙江柏拉阿图医药科技有限公司 | 一种高效力糖皮质激素化合物及其制备和用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4049813A (en) | 1976-07-15 | 1977-09-20 | Sandoz, Inc. | Substituted isoxazolo pyridinones |
| CA2451057A1 (en) | 2001-06-14 | 2002-12-27 | Banyu Pharmaceutical Co., Ltd. | Novel isoxazolopyridone derivatives and use thereof |
| GB0119911D0 (en) | 2001-08-15 | 2001-10-10 | Novartis Ag | Organic Compounds |
| NZ584160A (en) * | 2007-10-04 | 2011-05-27 | Astrazeneca Ab | Steroidal [3,2-c] pyrazole compounds, with glucocorticoid activity |
| CA2749585A1 (en) | 2009-01-13 | 2010-07-22 | Van Andel Research Institute | Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids |
| UY32525A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| UY32523A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| JP2012530140A (ja) * | 2009-06-16 | 2012-11-29 | メルク・シャープ・アンド・ドーム・コーポレーション | グルココルチコイド受容体アゴニストとしての新規［３，２−ｃ］ヘテロアリールステロイド、組成物およびこの使用 |
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2014
- 2014-09-25 JP JP2016516578A patent/JP2016531852A/ja active Pending
- 2014-09-25 US US15/024,496 patent/US9975918B2/en active Active
- 2014-09-25 CN CN201480063706.0A patent/CN105744937A/zh active Pending
- 2014-09-25 EP EP14849674.8A patent/EP3049089B1/en active Active
- 2014-09-25 CN CN202110799536.4A patent/CN113845558A/zh active Pending
- 2014-09-25 ES ES14849674T patent/ES2751457T3/es active Active
- 2014-09-25 WO PCT/US2014/057497 patent/WO2015048316A1/en not_active Ceased
- 2014-09-25 HK HK16110801.0A patent/HK1222565A1/zh unknown
- 2014-09-25 KR KR1020167010304A patent/KR20160060688A/ko not_active Withdrawn
- 2014-09-25 AU AU2014324961A patent/AU2014324961A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016531852A (ja) | 2016-10-13 |
| EP3049089B1 (en) | 2019-08-21 |
| CN105744937A (zh) | 2016-07-06 |
| KR20160060688A (ko) | 2016-05-30 |
| AU2014324961A8 (en) | 2016-04-21 |
| WO2015048316A1 (en) | 2015-04-02 |
| CN113845558A (zh) | 2021-12-28 |
| EP3049089A4 (en) | 2017-08-09 |
| ES2751457T3 (es) | 2020-03-31 |
| EP3049089A1 (en) | 2016-08-03 |
| US20160251393A1 (en) | 2016-09-01 |
| US9975918B2 (en) | 2018-05-22 |
| HK1222565A1 (zh) | 2017-07-07 |
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| TH | Corrigenda |
Free format text: IN VOL 30 , NO 15 , PAGE(S) 2039 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME SHANGHAI INSTITUTE OF MATERIA MEDICA.;VAN ANDEL RESEARCH INSTITUTE, APCORRIGENDA PLICATION NO. 2014324961, UNDER INID (71) CORRECT CO-APPLICANT NAME TO SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES |
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| MK1 | Application lapsed section 142(2)(a) - no request for examination in relevant period |