RU2019111101A - Структуры и механизм для дизайна высокоактивных глюкокортикоидов - Google Patents
Структуры и механизм для дизайна высокоактивных глюкокортикоидов Download PDFInfo
- Publication number
- RU2019111101A RU2019111101A RU2019111101A RU2019111101A RU2019111101A RU 2019111101 A RU2019111101 A RU 2019111101A RU 2019111101 A RU2019111101 A RU 2019111101A RU 2019111101 A RU2019111101 A RU 2019111101A RU 2019111101 A RU2019111101 A RU 2019111101A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- compound according
- optionally substituted
- hydrogen
- compound
- Prior art date
Links
- 239000003862 glucocorticoid Substances 0.000 title 1
- 229940037128 systemic glucocorticoids Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 33
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000001475 halogen functional group Chemical group 0.000 claims 5
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims 2
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
Classifications
-
- 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
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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)
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662408314P | 2016-10-14 | 2016-10-14 | |
| US62/408,314 | 2016-10-14 | ||
| PCT/US2017/056447 WO2018071736A1 (en) | 2016-10-14 | 2017-10-13 | Structures and mechanism for the design of highly potent glucocorticoids |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2019111101A true RU2019111101A (ru) | 2020-11-16 |
| RU2019111101A3 RU2019111101A3 (https=) | 2020-11-27 |
Family
ID=61906432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019111101A RU2019111101A (ru) | 2016-10-14 | 2017-10-13 | Структуры и механизм для дизайна высокоактивных глюкокортикоидов |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10954265B2 (https=) |
| EP (1) | EP3525870B1 (https=) |
| JP (2) | JP7146750B2 (https=) |
| KR (1) | KR102497070B1 (https=) |
| CN (1) | CN110382033B (https=) |
| ES (1) | ES2945983T3 (https=) |
| MA (1) | MA46539A (https=) |
| PH (1) | PH12019500801A1 (https=) |
| RU (1) | RU2019111101A (https=) |
| SG (1) | SG11201903209TA (https=) |
| WO (1) | WO2018071736A1 (https=) |
| ZA (1) | ZA201902595B (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025119398A1 (zh) * | 2023-12-08 | 2025-06-12 | 浙江柏拉阿图医药科技有限公司 | 高效力糖皮质激素多晶型及其制备方法和用途 |
| 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 (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK66202C (da) | 1945-03-03 | 1948-01-12 | Danske Securitas As | Kodekontakt til elektriske Alarmanlæg. |
| DK71662C (da) | 1946-09-05 | 1950-11-06 | Ingenioer Frank Broadbent | Tørrecentrifuge. |
| US4049813A (en) | 1976-07-15 | 1977-09-20 | Sandoz, Inc. | Substituted isoxazolo pyridinones |
| US5837698A (en) * | 1996-05-02 | 1998-11-17 | G. D. Searle & Co. | Steroid nitrite and nitrate ester derivatives useful as anti-inflammatory drugs |
| 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 |
| WO2005048927A2 (en) * | 2003-11-13 | 2005-06-02 | Combinatorx, Incorporated | Methods and reagents for the treatment of inflammatory disorders |
| EP1940863B1 (en) * | 2005-09-02 | 2012-09-05 | Nicox S.A. | Nitrooxy derivatives of glucocorticoids |
| CN1813768A (zh) * | 2005-11-18 | 2006-08-09 | 成都力思特制药股份有限公司 | 治疗呼吸系统疾病的药用组合物及其在制药中的应用 |
| NZ584160A (en) | 2007-10-04 | 2011-05-27 | Astrazeneca Ab | Steroidal [3,2-c] pyrazole compounds, with glucocorticoid activity |
| CN101945885A (zh) * | 2007-12-20 | 2011-01-12 | 阿斯利康(瑞典)有限公司 | 用作糖皮质激素受体激动剂的甾类衍生物 |
| CA2749585A1 (en) | 2009-01-13 | 2010-07-22 | Van Andel Research Institute | Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids |
| UY32523A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| UY32520A (es) | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| UY32525A (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 |
| JP2016531852A (ja) * | 2013-09-25 | 2016-10-13 | ヴァン アンデル リサーチ インスティテュート | 非常に強力なグルココルチコイド |
| TWI695831B (zh) * | 2014-09-13 | 2020-06-11 | 香港商南北兄弟藥業投資有限公司 | Ｃｒｔｈ２拮抗劑化合物及其用途 |
-
2017
- 2017-10-13 CN CN201780076320.7A patent/CN110382033B/zh active Active
- 2017-10-13 MA MA046539A patent/MA46539A/fr unknown
- 2017-10-13 RU RU2019111101A patent/RU2019111101A/ru unknown
- 2017-10-13 KR KR1020197013291A patent/KR102497070B1/ko active Active
- 2017-10-13 US US16/341,275 patent/US10954265B2/en active Active
- 2017-10-13 EP EP17860202.5A patent/EP3525870B1/en active Active
- 2017-10-13 JP JP2019520039A patent/JP7146750B2/ja active Active
- 2017-10-13 WO PCT/US2017/056447 patent/WO2018071736A1/en not_active Ceased
- 2017-10-13 SG SG11201903209TA patent/SG11201903209TA/en unknown
- 2017-10-13 ES ES17860202T patent/ES2945983T3/es active Active
-
2019
- 2019-04-12 PH PH12019500801A patent/PH12019500801A1/en unknown
- 2019-04-24 ZA ZA2019/02595A patent/ZA201902595B/en unknown
-
2022
- 2022-07-14 JP JP2022113322A patent/JP2022132464A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022132464A (ja) | 2022-09-08 |
| RU2019111101A3 (https=) | 2020-11-27 |
| JP7146750B2 (ja) | 2022-10-04 |
| US10954265B2 (en) | 2021-03-23 |
| KR102497070B1 (ko) | 2023-02-06 |
| MA46539A (fr) | 2019-08-21 |
| EP3525870A4 (en) | 2020-04-29 |
| WO2018071736A9 (en) | 2019-05-23 |
| EP3525870A1 (en) | 2019-08-21 |
| CN110382033A (zh) | 2019-10-25 |
| WO2018071736A1 (en) | 2018-04-19 |
| ZA201902595B (en) | 2021-04-28 |
| SG11201903209TA (en) | 2019-05-30 |
| KR20190068577A (ko) | 2019-06-18 |
| CN110382033B (zh) | 2022-04-15 |
| PH12019500801A1 (en) | 2019-11-11 |
| EP3525870B1 (en) | 2023-05-10 |
| US20190263853A1 (en) | 2019-08-29 |
| ES2945983T3 (es) | 2023-07-11 |
| JP2019532071A (ja) | 2019-11-07 |
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