RU2012117797A - Ингибитор гепараназной активности - Google Patents
Ингибитор гепараназной активности Download PDFInfo
- Publication number
- RU2012117797A RU2012117797A RU2012117797/15A RU2012117797A RU2012117797A RU 2012117797 A RU2012117797 A RU 2012117797A RU 2012117797/15 A RU2012117797/15 A RU 2012117797/15A RU 2012117797 A RU2012117797 A RU 2012117797A RU 2012117797 A RU2012117797 A RU 2012117797A
- Authority
- RU
- Russia
- Prior art keywords
- heparanase activity
- active ingredient
- inhibitor
- activity inhibitor
- imidazolidinone
- Prior art date
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
-
- 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
-
- 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
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Birds (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
Abstract
1. Ингибитор гепараназной активности, включающий в качестве активного ингредиента циклическое карбоксамидное производное, представленное формулой (I),в которой n равен целому числу от 1 до 3,Rпредставляет собой водород или углеводородную группу С1-6, необязательно замещенную гидроксилом,Х представляет собой -СН- или группу, представленную -N(R)-, где Rпредставляет собой водород или углеводородную группу С1-6, необязательно замещенную гидроксилом,или его соль.2. Ингибитор гепараназной активности по п.1, в котором в формуле (I) n=1.3. Ингибитор гепараназной активности по п.1, в котором циклическое карбоксамидное производное представляет собой одно или несколько соединений, выбранных из группы, состоящей из 2-имидазолидинона, 1-(2-гидроксиэтил)-2-имидазолидинона и 1-(2-гидроксиэтил)-2-пирролидона.4. Средство против морщин, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.5. Средство против крупных морщин, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.6. Средство для отбеливания кожи, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.
Claims (6)
1. Ингибитор гепараназной активности, включающий в качестве активного ингредиента циклическое карбоксамидное производное, представленное формулой (I)
в которой n равен целому числу от 1 до 3,
R1 представляет собой водород или углеводородную группу С1-6, необязательно замещенную гидроксилом,
Х представляет собой -СН2- или группу, представленную -N(R2)-, где R2 представляет собой водород или углеводородную группу С1-6, необязательно замещенную гидроксилом,
или его соль.
2. Ингибитор гепараназной активности по п.1, в котором в формуле (I) n=1.
3. Ингибитор гепараназной активности по п.1, в котором циклическое карбоксамидное производное представляет собой одно или несколько соединений, выбранных из группы, состоящей из 2-имидазолидинона, 1-(2-гидроксиэтил)-2-имидазолидинона и 1-(2-гидроксиэтил)-2-пирролидона.
4. Средство против морщин, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.
5. Средство против крупных морщин, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.
6. Средство для отбеливания кожи, включающее в качестве активного ингредиента ингибитор гепараназной активности по любому из п.п.1-3.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009228406 | 2009-09-30 | ||
| JP2009-228406 | 2009-09-30 | ||
| PCT/JP2010/066998 WO2011040496A1 (ja) | 2009-09-30 | 2010-09-29 | ヘパラナーゼ活性阻害剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2012117797A true RU2012117797A (ru) | 2013-11-10 |
| RU2503454C1 RU2503454C1 (ru) | 2014-01-10 |
Family
ID=43826308
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012117797/15A RU2503454C1 (ru) | 2009-09-30 | 2010-09-29 | Ингибитор гепараназной активности |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US8609075B2 (ru) |
| EP (1) | EP2484359B1 (ru) |
| JP (2) | JP5593323B2 (ru) |
| KR (1) | KR101431348B1 (ru) |
| CN (1) | CN102655863B (ru) |
| BR (1) | BR112012007090A2 (ru) |
| ES (1) | ES2687780T3 (ru) |
| HK (1) | HK1171390A1 (ru) |
| IN (1) | IN2012DN02632A (ru) |
| RU (1) | RU2503454C1 (ru) |
| TW (1) | TWI461221B (ru) |
| WO (1) | WO2011040496A1 (ru) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5685369B2 (ja) * | 2009-09-15 | 2015-03-18 | 株式会社 資生堂 | ヘパラナーゼ阻害剤による美白方法及び美白効果を有する物質の評価方法 |
| JP2013032332A (ja) * | 2011-07-01 | 2013-02-14 | Lintec Corp | 免疫賦活剤 |
| JP5258993B1 (ja) * | 2012-03-29 | 2013-08-07 | 株式会社 資生堂 | ヘパラン硫酸産生促進剤 |
| JP6321506B2 (ja) * | 2014-09-22 | 2018-05-09 | 株式会社 資生堂 | ヘパラナーゼ阻害剤による美白方法及び美白効果を有する物質の評価方法 |
| JP7059193B2 (ja) * | 2016-10-21 | 2022-04-25 | 株式会社 資生堂 | ラミニン５１１産生促進剤、表皮基底膜安定化剤及び／又は表皮幹細胞減少抑制又は増加促進剤のスクリーニング方法 |
| AU2017376817B2 (en) | 2016-12-13 | 2022-03-31 | Beta Therapeutics Pty Ltd | Heparanase inhibitors and use thereof |
| US11787783B2 (en) | 2016-12-13 | 2023-10-17 | Beta Therapeutics Pty Ltd | Heparanase inhibitors and use thereof |
| EP3381898A1 (en) | 2017-03-27 | 2018-10-03 | Leadiant Biosciences SA | Symmetrical tris-aryl-amide derivatives and their use as anti-heparanase |
| EP3381908A1 (en) | 2017-03-27 | 2018-10-03 | Leadiant Biosciences SA | 2-(4-(4-(bromo-methoxybenzamido)benzylamino)phenyl)benzazole derivatives and their use as anti-heparanase |
| EP3381906A1 (en) | 2017-03-27 | 2018-10-03 | Leadiant Biosciences SA | Compounds for use as heparanase inhibitors |
| EP3381897A1 (en) | 2017-03-27 | 2018-10-03 | Leadiant Biosciences SA | Derivatives of the disodium 2,2'-{carbonylbis[imino-3,1-phenylenecarbonylimino(1-methyl-1h-pyrrole-4,2-diyl)carbonylimino]}dinaphthalene-1,5-disulfonate salt and related compounds as heparanase inhibitors for the treatment of cancer |
| EP3381907A1 (en) | 2017-03-27 | 2018-10-03 | Leadiant Biosciences SA | Symmetrical 2-aminophenyl-benzazolyl-5-acetate compounds and their use as anti-heparanase |
| EP3388439A1 (en) | 2017-04-11 | 2018-10-17 | Leadiant Biosciences SA | Biotin-conjugated n-acetyl glycol split heparin |
| US11464762B2 (en) | 2017-06-13 | 2022-10-11 | National Cancer Center | Carcinogenesis inhibitor |
| WO2020219753A1 (en) * | 2019-04-24 | 2020-10-29 | University Of Florida Research Foundation, Incorporated | Heparanase compounds and methods of use |
| WO2022131108A1 (ja) * | 2020-12-15 | 2022-06-23 | 株式会社 資生堂 | 真皮再生促進剤 |
| TW202237061A (zh) | 2020-12-15 | 2022-10-01 | 日商資生堂股份有限公司 | 表皮幹細胞增加促進劑 |
| WO2023100684A1 (ja) | 2021-12-02 | 2023-06-08 | 株式会社 資生堂 | 化粧料 |
| WO2023100682A1 (ja) * | 2021-12-03 | 2023-06-08 | 株式会社 資生堂 | 化粧料 |
| WO2023106121A1 (ja) * | 2021-12-09 | 2023-06-15 | 株式会社 資生堂 | 水中油型乳化化粧料 |
| WO2023106123A1 (ja) * | 2021-12-09 | 2023-06-15 | 株式会社 資生堂 | 化粧料 |
| WO2023120180A1 (ja) * | 2021-12-20 | 2023-06-29 | 株式会社 資生堂 | 水中油型乳化化粧料 |
| WO2023149225A1 (ja) * | 2022-02-03 | 2023-08-10 | 株式会社 資生堂 | 皮膚外用組成物 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US1256235A (en) * | 1917-03-31 | 1918-02-12 | William F Jacobs | Work-supporting horse. |
| US4049650A (en) | 1976-10-18 | 1977-09-20 | Morton-Norwich Products, Inc. | 1-[[[5-(Substituted phenyl)-2-oxazolyl]methylene]amino]-2,4-imidazolidinediones |
| US4593038A (en) * | 1985-04-03 | 1986-06-03 | Burzynski Stanislaw R | Topical use of 3-phenylacetylamino-2,6-piperidinedione for treatment of skin wrinkles and hyperpigmentation |
| US4731453A (en) | 1985-04-03 | 1988-03-15 | Mitsui Toatsu Chemicals, Inc. | Process for producing 1, 3-dialkyl-2-imidazolidinone |
| US4960771A (en) * | 1988-07-12 | 1990-10-02 | Rajadhyaksha Vithal J | Oxazolidinone penetration enhancing compounds |
| US5011621A (en) | 1990-06-04 | 1991-04-30 | Arco Chemical Technology, Inc. | Paint stripper compositions containing N-methyl-2-pyrrolidone and renewable resources |
| US5583256A (en) | 1994-07-07 | 1996-12-10 | Mitsui Toatsu Chemicals, Inc. | Process for producing 1,3-dialkyl-2-imidazolidinone |
| US5536740A (en) * | 1995-06-01 | 1996-07-16 | Elizabeth Arden Company, Division Of Conopco, Inc. | Skin care compositions containing dimethyl imidazolidinone and retinol or retinyl ester |
| US5837224A (en) | 1996-01-19 | 1998-11-17 | The Regents Of The University Of Michigan | Method of inhibiting photoaging of skin |
| JPH11335235A (ja) | 1998-05-22 | 1999-12-07 | Shiseido Co Ltd | 抗老化剤 |
| GB9913415D0 (en) | 1999-06-10 | 1999-08-11 | Central Manchester Healthcare | Heparanase assay |
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| EP1338269B1 (de) * | 2002-02-15 | 2005-07-27 | Goldschmidt GmbH | Verwendung von Kreatinin und/oder Kreatinin-Derivaten zur Aufhellung der Haut und Milderung von Pigmentstörungen |
| EP2465491A1 (en) | 2002-06-25 | 2012-06-20 | Shiseido Company, Ltd. | Anti-aging preparation |
| AU2004273615B2 (en) * | 2003-09-23 | 2009-01-15 | Novartis Ag | Combination of a VEGF receptor inhibitor with a chemotherapeutic agent |
| CA2546493A1 (en) * | 2003-11-19 | 2005-06-09 | Signal Pharmaceuticals, Llc | Indazole compounds and methods of use thereof as protein kinase inhibitors |
| FR2873377B1 (fr) * | 2004-07-23 | 2006-10-13 | Sanofi Synthelabo | Derives d'azasucre, inhibiteurs d'heparanases, leur procede de preparation, les compositions en contenant et leur utilisation |
| US7238260B2 (en) | 2004-10-26 | 2007-07-03 | Lyondell Chemical Technology, L.P. | Purification of N-(2-hydroxyethyl)-2-pyrrolidone |
| JP2006303185A (ja) | 2005-04-20 | 2006-11-02 | Matsushita Electric Ind Co Ltd | 半導体装置及びその製造方法 |
| JP2007277149A (ja) * | 2006-04-06 | 2007-10-25 | Kao Corp | インボルクリン発現促進剤 |
| US8097581B2 (en) | 2007-05-10 | 2012-01-17 | Grant Industries Inc. | Anti-wrinkle cosmetic composition |
| CN101311188B (zh) * | 2007-05-21 | 2010-12-29 | 中国人民解放军军事医学科学院生物工程研究所 | 人乙酰肝素酶的小分子多肽抑制剂 |
| JP5105962B2 (ja) * | 2007-06-08 | 2012-12-26 | 株式会社 資生堂 | コーニファイドエンベロープ形成・成熟化促進剤 |
| JP2008303187A (ja) | 2007-06-08 | 2008-12-18 | Shiseido Co Ltd | コーニファイドエンベロープ形成・成熟化促進剤 |
| JP5179096B2 (ja) | 2007-06-08 | 2013-04-10 | 株式会社 資生堂 | コーニファイドエンベロープ形成・成熟化促進剤 |
| WO2009122540A1 (ja) | 2008-03-31 | 2009-10-08 | 株式会社資生堂 | しわを防止または改善するための経口、注射、皮膚外用剤および美容方法 |
| JP5722030B2 (ja) * | 2008-03-31 | 2015-05-20 | 株式会社 資生堂 | しわを防止または改善するための経口、注射、皮膚外用剤および美容方法 |
| FR2931064B1 (fr) | 2008-05-14 | 2010-08-13 | Oreal | Composition cosmetique contenant un derive de dibenzoylmethane et un derive de pyrrolidinone; procede de photostabilisation du derive de dibenzoylmethane |
-
2010
- 2010-09-29 BR BR112012007090-8A patent/BR112012007090A2/pt not_active Application Discontinuation
- 2010-09-29 ES ES10820611.1T patent/ES2687780T3/es active Active
- 2010-09-29 IN IN2632DEN2012 patent/IN2012DN02632A/en unknown
- 2010-09-29 KR KR1020127004685A patent/KR101431348B1/ko active IP Right Grant
- 2010-09-29 RU RU2012117797/15A patent/RU2503454C1/ru not_active IP Right Cessation
- 2010-09-29 US US13/261,244 patent/US8609075B2/en active Active
- 2010-09-29 EP EP10820611.1A patent/EP2484359B1/en active Active
- 2010-09-29 WO PCT/JP2010/066998 patent/WO2011040496A1/ja active Application Filing
- 2010-09-29 CN CN2010800438641A patent/CN102655863B/zh active Active
- 2010-09-29 JP JP2011534288A patent/JP5593323B2/ja active Active
- 2010-09-30 TW TW099133410A patent/TWI461221B/zh active
-
2012
- 2012-11-29 HK HK12112298.0A patent/HK1171390A1/xx not_active IP Right Cessation
-
2013
- 2013-11-18 US US14/082,440 patent/US8901160B2/en active Active
-
2014
- 2014-02-10 JP JP2014023264A patent/JP2014111640A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JPWO2011040496A1 (ja) | 2013-02-28 |
| EP2484359A4 (en) | 2015-07-08 |
| US20120183481A1 (en) | 2012-07-19 |
| EP2484359A1 (en) | 2012-08-08 |
| JP2014111640A (ja) | 2014-06-19 |
| RU2503454C1 (ru) | 2014-01-10 |
| AU2010301641A1 (en) | 2012-03-22 |
| IN2012DN02632A (ru) | 2015-09-04 |
| WO2011040496A1 (ja) | 2011-04-07 |
| US8609075B2 (en) | 2013-12-17 |
| US8901160B2 (en) | 2014-12-02 |
| TW201117832A (en) | 2011-06-01 |
| CN102655863A (zh) | 2012-09-05 |
| CN102655863B (zh) | 2013-11-20 |
| KR20120060205A (ko) | 2012-06-11 |
| JP5593323B2 (ja) | 2014-09-24 |
| EP2484359B1 (en) | 2018-07-25 |
| US20140080878A1 (en) | 2014-03-20 |
| KR101431348B1 (ko) | 2014-08-19 |
| HK1171390A1 (en) | 2013-03-28 |
| ES2687780T3 (es) | 2018-10-29 |
| TWI461221B (zh) | 2014-11-21 |
| BR112012007090A2 (pt) | 2018-06-05 |
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