KR910016330A - 엘라스타제 억제제로서 벤즈이소티아졸리논-1-디옥사이드 유도체 및 그 조성물과 용도 - Google Patents
엘라스타제 억제제로서 벤즈이소티아졸리논-1-디옥사이드 유도체 및 그 조성물과 용도 Download PDFInfo
- Publication number
- KR910016330A KR910016330A KR1019910003708A KR910003708A KR910016330A KR 910016330 A KR910016330 A KR 910016330A KR 1019910003708 A KR1019910003708 A KR 1019910003708A KR 910003708 A KR910003708 A KR 910003708A KR 910016330 A KR910016330 A KR 910016330A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- general formula
- hydrogen atom
- composition
- alkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 13
- 239000003602 elastase inhibitor Substances 0.000 title claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- -1 carboxyoctyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229940122858 Elastase inhibitor Drugs 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000002537 cosmetic Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002960 margaryl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002958 pentadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 125000002889 tridecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002948 undecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
-
- 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
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- 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
-
- 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
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dermatology (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
Description
Claims (36)
- (i) 다음 일반식(Ⅰ)을 갖는 1종 이상의 벤즈이소티아졸리논-1-디옥사이드 유도체인 엘라스타제(elastase)억제제 및 (ii)제약학적 또는 향장학적으로 허용가능한 캐리어 또는 매개물을 함유하는 조성물.
-
- 〔위식에서, R1은 수소원자 또는 C1-C5알킬이나 알콕시기이며, R2는 임의선택적으로 OH또는 COOH기로 치환된 1가의 C8-C20알킬 또는 C9-C20알케닐기이며, 또는 R2는 다음 일반식(Ⅱ)를 갖는기이며,
-
- (여기서, R3는 2가의 선형이나 가지형 C2-C6포화 또는 에틸렌 결합적 불포화 지방족기,는 방향족 핵, R4는 OH, C1-C4알킬 또는 C1-C4알콕시기, 및 n은 제로 또는 1-5범위의 정수이며, n〉1인 경우, R4기는 다를수있음) 또는, R2는 다음 일반식(Ⅲ);
-
- (여기서,R1은 상기와 동일하며, R2는 2가의 선형이나 가지형 C8-C20포화 또는 에틸렌결합적 불포화 지방족기이다)을 갖는 기이다〕
- 제1항에 있어서, R2는 C11-C20알킬기인 조성물.
- 제1항 내지 2항에 있어서, R1이 수소원자이고 R2는 COOH로 치환된 알킬기인 조성물.
- 제3항에 있어서, R1이 수소원자이고, R2는 노닐(nony1), 운데실, 트리데실, 펜타데실, 헵타데실 및 카복시옥틸기인 조성물.
- 제1항 내지 2항에 있어서, R1은 수소원자이고, R2가 알케닐기인 조성물.
- 제5항에 있어서, R2는 데크-9-에닐(dec-9-eny)기 인 조성물.
- 제1항 내지 2항에 있어서, R1이 수소원자이고 R2는 다음 일반식(Ⅱa)을 갖는 기인 조성물.
-
- (위식에서, R3는 포화 또는 올레핀결합적 불포화 2가 C2-C6지방기이며, R4는 히드록실기 또는 C1-C4알콕시기이며, n은 1이거나 2이다.)
- 제7항에 있어서, R2가 3.4-디메톡시신나모일, 신나모일, 디히드로신나모일 또는 P-메톡시페닐부티릴기인 조성물.
- 제1항 내지 2항에 있어서, R1이 수소원자이고, R2는 다음 일반식(Ⅲ)을 갖는 기인 조성물.
-
- (여기서, R1은 수소원자이고, R5는 2가의 포화지방족기이다)
- 제9항에 있어서, R5는-(CH2)8-기인 조성물.
- 상기의 항중 어느한 항에 있어서, 일반식(Ⅰ)화합물을 0.1-5중량%함유하는 조성물.
- 다음 일반식(Ⅰ)로 표현되는 벤즈이소티아졸리논-1-디옥사이드 유도체.
-
- 〔위식에서, R1은 수소원자 또는 C1-C5알킬이나 알콕시기이며, R2는 비치환된 알킬인 경우에는 C11-C20알킬이라는 전제하에 임의 선택적으로 한개이상의 OH 또는 COOH기로 치환된 1가의 C8-C20알킬 또는 C9-C20알케닐기이며, 또는 R2는 다음 일반식(Ⅱ)를 갖는기이며,
-
- (여기서, R3는 2가의 선형 또는 가지형 C2-C6지방족기,는 방향족 핵, R4는 제로 또는 1-5범위의 정수이며 n 1인 경우 R4는 다를 수 있다) 또는 R2는 다음 일반식(Ⅲ);
-
- (여기서, R1은 상기와 동일하고 R5는 2가의 선형 또는 가지형 C8-C20지방족기이다)을 갖는 기이다〕
- 제12항에 있어서, R2는 3,4-디메톡시신나모일, 신나모일, 디히드로신나모일 또는 P-메톡시페닐부티릴기인 벤즈이소티아졸리논-1-디옥사이드 유도체.
- 제12항에 있어서, R2가 다음 일반식(Ⅲ)을 갖는 기인 벤즈이소티아졸리논-1-디옥사이드 유도체.
-
- (위식에서, R1은 수소원자이고, R5는 -(CH2)8-기이다)
- 제12항에 있어서, R2는 -(CH2)5-COOH기인 벤즈이소티아졸리논-1-디옥사이드 유도체.
- 제12-15항중 어느한 항에 있어서, R1은 수소원자인 벤즈이소티아졸리논-1-디옥사이드 유도체.
- 제1-11항중 어느한 항에 따르는 조성물을 국부 부위에 적용하는 것을 포함하는 사람피부의 화장용 치료방법.
- ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9002951A FR2659327A1 (fr) | 1990-03-08 | 1990-03-08 | Derives du benzisothiazolinone-1-dioxyde, utilisables comme inhibiteurs des elastases. |
FR9002951 | 1990-03-08 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR910016330A true KR910016330A (ko) | 1991-11-05 |
KR960014782B1 KR960014782B1 (en) | 1996-10-19 |
Family
ID=9394523
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR91003708A KR960014782B1 (en) | 1990-03-08 | 1991-03-08 | Benzisothiazolinone 1-dioxide derivatives and elastase inhibitors composition comprising them |
Country Status (16)
Country | Link |
---|---|
US (2) | US5338747A (ko) |
EP (1) | EP0446047B1 (ko) |
JP (1) | JPH04234863A (ko) |
KR (1) | KR960014782B1 (ko) |
AT (1) | ATE154347T1 (ko) |
AU (1) | AU636013B2 (ko) |
BR (1) | BR9100938A (ko) |
CA (1) | CA2037665A1 (ko) |
DE (1) | DE69126460T2 (ko) |
ES (1) | ES2102994T3 (ko) |
FR (1) | FR2659327A1 (ko) |
ID (1) | ID820B (ko) |
IN (1) | IN172035B (ko) |
MY (1) | MY106067A (ko) |
TW (1) | TW200472B (ko) |
ZA (1) | ZA911728B (ko) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5306818A (en) * | 1990-11-01 | 1994-04-26 | Sterling Winthrop Inc. | Tetrahydro 2-saccharinylmerthyl aryl carboxylates |
US5250696A (en) * | 1990-11-01 | 1993-10-05 | Sterling Winthrop Inc. | 2-saccharinylmethyl aryl carboxylate |
US5512589A (en) * | 1990-11-01 | 1996-04-30 | Sterling Winthrop Inc. | 2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
AU653279B2 (en) * | 1991-12-30 | 1994-09-22 | Sanofi | Novel 2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
TW226016B (ko) * | 1991-12-30 | 1994-07-01 | Sterling Winthrop Inc | |
US6375948B1 (en) | 1999-07-12 | 2002-04-23 | Kao Corporation | Treating method for suppressing hair growth |
GB0129987D0 (en) * | 2001-12-14 | 2002-02-06 | Zylepsis Ltd | Skin compositions |
US7361767B2 (en) | 2003-11-14 | 2008-04-22 | 3M Innovative Properties Company | N-sulfonyldicarboximide containing tethering compounds |
US7179923B2 (en) | 2003-11-14 | 2007-02-20 | 3M Innovative Properties Company | N-sulfonylaminocarbonyl containing compounds |
US7943388B2 (en) | 2003-11-14 | 2011-05-17 | 3M Innovative Properties Company | Acoustic sensors and methods |
US7423155B2 (en) | 2003-11-14 | 2008-09-09 | 3M Innovative Properties Company | N-sulfonyldicarboximide containing tethering compounds |
US7169933B2 (en) * | 2003-11-14 | 2007-01-30 | 3M Innovative Properties Company | N-sulfonylaminocarbonyl containing compounds |
US7402678B2 (en) | 2004-12-17 | 2008-07-22 | 3M Innovative Properties Company | Multifunctional amine capture agents |
US7342082B2 (en) | 2004-12-17 | 2008-03-11 | 3M Innovative Properties Company | Soluble polymers as amine capture agents and methods |
EP1699768B1 (en) * | 2003-12-30 | 2014-09-24 | 3M Innovative Properties Company | Multifunctional amine capture agents |
US7544756B2 (en) | 2005-09-30 | 2009-06-09 | 3M Innovative Properties Company | Crosslinked polymers with amine binding groups |
US7544755B2 (en) | 2005-09-30 | 2009-06-09 | 3M Innovative Properties Company | Crosslinked polymers with amine binding groups |
US7544754B2 (en) | 2005-09-30 | 2009-06-09 | 3M Innovative Properties Company | Crosslinked polymers with amine binding groups |
US8034448B2 (en) * | 2008-08-19 | 2011-10-11 | Los Alamos National Security, Llc | Fibrous composites comprising carbon nanotubes and silica |
ES2534193T3 (es) | 2009-12-01 | 2015-04-20 | Lubrizol Advanced Materials, Inc. | Polímeros hidrolíticamente estables para múltiples fines |
WO2018049328A1 (en) | 2016-09-12 | 2018-03-15 | Numerate, Inc. | Bicyclic compounds useful as gpr120 modulators |
EP3509587B1 (en) | 2016-09-12 | 2023-12-06 | Valo Health, Inc. | Monocyclic compounds useful as gpr120 modulators |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4195023A (en) * | 1975-08-20 | 1980-03-25 | Merck & Co., Inc. | 2-(2-Furoyl)1,2-benzisothiazole-3-one, 2-(2-furoyl) saccharin, and 2-(2-thenoyl) saccharin |
US4276298A (en) * | 1978-03-24 | 1981-06-30 | Merck & Co., Inc. | 2-Aryl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors |
FR2546164B1 (fr) * | 1983-05-16 | 1987-07-17 | Centre Nat Rech Scient | Nouveaux derives de peptides, leur preparation et leur application comme inhibiteurs de l'elastase |
-
1990
- 1990-03-08 FR FR9002951A patent/FR2659327A1/fr active Pending
-
1991
- 1991-03-06 AU AU72635/91A patent/AU636013B2/en not_active Ceased
- 1991-03-06 CA CA002037665A patent/CA2037665A1/en not_active Abandoned
- 1991-03-07 MY MYPI91000361A patent/MY106067A/en unknown
- 1991-03-07 AT AT91301895T patent/ATE154347T1/de not_active IP Right Cessation
- 1991-03-07 EP EP91301895A patent/EP0446047B1/en not_active Expired - Lifetime
- 1991-03-07 DE DE69126460T patent/DE69126460T2/de not_active Expired - Fee Related
- 1991-03-07 US US07/666,093 patent/US5338747A/en not_active Expired - Fee Related
- 1991-03-07 ES ES91301895T patent/ES2102994T3/es not_active Expired - Lifetime
- 1991-03-08 JP JP3125607A patent/JPH04234863A/ja active Pending
- 1991-03-08 KR KR91003708A patent/KR960014782B1/ko active IP Right Grant
- 1991-03-08 ZA ZA911728A patent/ZA911728B/xx unknown
- 1991-03-08 IN IN69/BOM/91A patent/IN172035B/en unknown
- 1991-03-08 BR BR919100938A patent/BR9100938A/pt not_active Application Discontinuation
- 1991-04-13 TW TW080102851A patent/TW200472B/zh active
-
1992
- 1992-01-29 ID IDP185092A patent/ID820B/id unknown
-
1994
- 1994-04-19 US US08/230,048 patent/US5411978A/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
JPH04234863A (ja) | 1992-08-24 |
ATE154347T1 (de) | 1997-06-15 |
KR960014782B1 (en) | 1996-10-19 |
TW200472B (ko) | 1993-02-21 |
MY106067A (en) | 1995-03-31 |
EP0446047A1 (en) | 1991-09-11 |
AU636013B2 (en) | 1993-04-08 |
AU7263591A (en) | 1991-09-12 |
US5338747A (en) | 1994-08-16 |
DE69126460D1 (de) | 1997-07-17 |
ES2102994T3 (es) | 1997-08-16 |
CA2037665A1 (en) | 1991-09-09 |
IN172035B (ko) | 1993-03-20 |
BR9100938A (pt) | 1991-11-05 |
FR2659327A1 (fr) | 1991-09-13 |
DE69126460T2 (de) | 1997-12-04 |
ID820B (id) | 1996-07-22 |
EP0446047B1 (en) | 1997-06-11 |
ZA911728B (en) | 1992-11-25 |
US5411978A (en) | 1995-05-02 |
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