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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- IHOBBYHEOBWAPZ-UHFFFAOYSA-L steroid c Chemical group [Na+].[Na+].C1CC2CC(OS([O-])(=O)=O)C(OS([O-])(=O)=O)CC2(C)C(CCC23C)C1C3CC(O1)C2C2(C)OC1OC2CC(C(C)C)=C(C)C IHOBBYHEOBWAPZ-UHFFFAOYSA-L 0.000 description 1
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- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
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- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
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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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- 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
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (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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|---|---|---|---|
| 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) | CN113845558A (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 |
|---|---|---|---|---|
| HUE071964T2 (hu) | 2015-07-06 | 2025-10-28 | Sage Therapeutics Inc | Oxiszterolok és alkalmazási eljárásaik |
| EP3828194B1 (en) | 2015-07-06 | 2025-04-16 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| SMT202200300T1 (it) | 2016-04-01 | 2022-09-14 | Sage Therapeutics Inc | Ossisteroli e relativi metodi d'uso |
| WO2017193046A1 (en) | 2016-05-06 | 2017-11-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| ES2935057T3 (es) | 2016-09-30 | 2023-03-01 | Sage Therapeutics Inc | C7 oxisteroles sustituidos y estos compuestos para su uso como moduladores de la NMDA |
| EP3525870B1 (en) * | 2016-10-14 | 2023-05-10 | Van Andel Research Institute | Highly potent glucocorticoids |
| KR20230051723A (ko) | 2016-10-18 | 2023-04-18 | 세이지 테라퓨틱스, 인크. | 옥시스테롤 및 그의 사용 방법 |
| RU2019115113A (ru) | 2016-10-18 | 2020-11-24 | Сейдж Терапьютикс, Инк. | Оксистеролы и способы их применения |
| CN115210229A (zh) | 2020-01-03 | 2022-10-18 | 博格有限责任公司 | 多环酰胺作为治疗癌症的ube2k调节剂 |
| 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 |
| CN120365344A (zh) * | 2024-01-24 | 2025-07-25 | 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 |
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| US4049813A (en) | 1976-07-15 | 1977-09-20 | Sandoz, Inc. | Substituted isoxazolo pyridinones |
| WO2002102807A1 (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 |
| EA201000436A1 (ru) | 2007-10-04 | 2010-10-29 | Астразенека Аб | Стероидные [3,2-с]пиразольные соединения, обладающие глюкокортикоидной активностью |
| CN102361640B (zh) | 2009-01-13 | 2016-10-19 | 范安德尔研究所 | 异噁唑吡啶酮在制备用于缓解或减轻温血哺乳动物关节炎和哮喘的症状的药物中的用途 |
| 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 |
| CN102834406A (zh) * | 2009-06-16 | 2012-12-19 | 默沙东公司 | 作为糖皮质激素受体激动剂的新的[3.2-c]杂芳基甾体、其组合物和用途 |
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2014
- 2014-09-25 JP JP2016516578A patent/JP2016531852A/ja active Pending
- 2014-09-25 HK HK16110801.0A patent/HK1222565A1/zh unknown
- 2014-09-25 CN CN202110799536.4A patent/CN113845558A/zh active Pending
- 2014-09-25 ES ES14849674T patent/ES2751457T3/es active Active
- 2014-09-25 KR KR1020167010304A patent/KR20160060688A/ko not_active Withdrawn
- 2014-09-25 AU AU2014324961A patent/AU2014324961A1/en not_active Abandoned
- 2014-09-25 CN CN201480063706.0A patent/CN105744937A/zh active Pending
- 2014-09-25 WO PCT/US2014/057497 patent/WO2015048316A1/en not_active Ceased
- 2014-09-25 US US15/024,496 patent/US9975918B2/en active Active
- 2014-09-25 EP EP14849674.8A patent/EP3049089B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3049089B1 (en) | 2019-08-21 |
| HK1222565A1 (zh) | 2017-07-07 |
| EP3049089A4 (en) | 2017-08-09 |
| EP3049089A1 (en) | 2016-08-03 |
| US20160251393A1 (en) | 2016-09-01 |
| CN105744937A (zh) | 2016-07-06 |
| US9975918B2 (en) | 2018-05-22 |
| CN113845558A (zh) | 2021-12-28 |
| ES2751457T3 (es) | 2020-03-31 |
| JP2016531852A (ja) | 2016-10-13 |
| WO2015048316A1 (en) | 2015-04-02 |
| KR20160060688A (ko) | 2016-05-30 |
| AU2014324961A8 (en) | 2016-04-21 |
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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 |