KR960031422A - 신규한 레티노이드 - Google Patents
신규한 레티노이드 Download PDFInfo
- Publication number
- KR960031422A KR960031422A KR1019960004376A KR19960004376A KR960031422A KR 960031422 A KR960031422 A KR 960031422A KR 1019960004376 A KR1019960004376 A KR 1019960004376A KR 19960004376 A KR19960004376 A KR 19960004376A KR 960031422 A KR960031422 A KR 960031422A
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- South Korea
- Prior art keywords
- compound
- bond
- pharmaceutically acceptable
- double
- formula
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims abstract 8
- 230000000694 effects Effects 0.000 claims abstract 3
- 150000001408 amides Chemical class 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- -1 Retinoid compound Chemical class 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 206010000496 acne Diseases 0.000 abstract 1
- 150000004492 retinoid derivatives Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/40—Unsaturated compounds
- C07C59/42—Unsaturated compounds containing hydroxy or O-metal groups
- C07C59/52—Unsaturated compounds containing hydroxy or O-metal groups a hydroxy or O-metal group being bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
- C07C403/14—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by doubly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
- C07C403/20—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by carboxyl groups or halides, anhydrides, or (thio)esters thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C47/00—Compounds having —CHO groups
- C07C47/38—Unsaturated compounds having —CHO groups bound to carbon atoms of rings other than six—membered aromatic rings
- C07C47/45—Unsaturated compounds having —CHO groups bound to carbon atoms of rings other than six—membered aromatic rings having unsaturation outside the rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C47/00—Compounds having —CHO groups
- C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
- C07C47/548—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings having unsaturation outside the six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/09—Geometrical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Nutrition Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Physical Vapour Deposition (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Cosmetics (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
Abstract
하기 일반식(Ⅰ)의 신규한 노나테트라에노산 유도체
(상기 식에서, 점선은 선택적이고, R1및 R2는 명세서에 정의된 바와 같다)로 여드름 치료 활성을 갖는 레티노산X-수용체(RXR)와 선택적으로 결합하고, RARa활성을 갖는 레티노이드 활성을 증대시킨다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (4)
- 하기 일반식(Ⅰ)의 화합물 및 그의 약학적으로 허용되는 염, 에스테르 및 아미드:상기 식에서, C7-C8결합은 이중 결합 또는 삼중 결합이고, R1및 R2는 C7-C8결합이 이중 결합인 경우 독립적으로 할로겐 또는 저급 알킬이거나 또는 C7-C8결합이 이중 결합인 경우 독립적으로 저급 알킬이거나; 또는 함께 결합된 R1및 R2는C3-C13알킬렌을 형성하고, 여기서, 하나의 탄소 원자는 황, 산소 및 질소로 구성된 군중에서 선택된 이중원자에 의해 치환될 수 있거나; 또는 결합된 R1및 R2는 이들이 결합되는 탄소 원자와 함께 탄소 원자수 5 내지 6의 방향족 고리 또는 원자수 5 내지 6의 헤테로방향족 고리(여기서, R1또는 R2중 한 원자는 산소, 질소 및 황 중에서 선택된 이종 원자이고, R1및 R2중 나머지 원자는 탄소이다)를 형성하다.
- 하기 구조식의 화합물:
- 제1항에 청구한 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용되는 염, 에스테르 또는 아미드 및 약학적으로 허용되는 불활성 담체를 포함하는 약학 조성물.
- RARa활성을 갖는 레티노이드인 제1화합물; 및 제1항에 청구한 일반식(Ⅰ)의 제2화합물, 또는 그의 약학적으로 허용되는 염, 에스테르 또는 아미드를 포함하고, 이때 상기 제1화합물은 10 내지 50㎎의 양으로 단위 투여형에 존재하고, 상기 제2화합물은 상기 제1화합물의 양의 1내지 10배의 양으로 단위 투여형에 존재하는, 경구 투여용 단위 투여형 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39398095A | 1995-02-24 | 1995-02-24 | |
| US393,980 | 1995-02-24 | ||
| US46828995A | 1995-06-06 | 1995-06-06 | |
| US08/393980 | 1995-06-06 | ||
| US08/468289 | 1995-06-06 | ||
| US468,289 | 1995-06-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR960031422A true KR960031422A (ko) | 1996-09-17 |
| KR100414342B1 KR100414342B1 (ko) | 2004-05-10 |
Family
ID=27014530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019960004376A KR100414342B1 (ko) | 1995-02-24 | 1996-02-23 | 신규한레티노이드 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US5986131A (ko) |
| EP (1) | EP0728742B1 (ko) |
| JP (1) | JP2776787B2 (ko) |
| KR (1) | KR100414342B1 (ko) |
| CN (1) | CN1124260C (ko) |
| AT (1) | ATE185799T1 (ko) |
| AU (1) | AU703115B2 (ko) |
| CA (1) | CA2170227A1 (ko) |
| CZ (1) | CZ291352B6 (ko) |
| DE (1) | DE69604713T2 (ko) |
| DK (1) | DK0728742T3 (ko) |
| ES (1) | ES2138765T3 (ko) |
| FI (1) | FI960856A (ko) |
| GR (1) | GR3032407T3 (ko) |
| HK (1) | HK1012330A1 (ko) |
| HU (1) | HU219538B (ko) |
| IL (1) | IL117170A (ko) |
| MA (1) | MA23813A1 (ko) |
| MY (1) | MY113430A (ko) |
| NO (1) | NO309189B1 (ko) |
| NZ (1) | NZ286017A (ko) |
| RU (1) | RU2166499C2 (ko) |
| SG (1) | SG59945A1 (ko) |
| TW (1) | TW343966B (ko) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010032000A (ko) * | 1997-11-12 | 2001-04-16 | 프리돌린 클라우스너, 롤란드 비. 보레르 | 레티노이드 길항제를 이용한 티-보조 세포 제2형 중재면역 질환의 치료 |
| US6326397B1 (en) | 1998-11-10 | 2001-12-04 | Hoffman-La Roche Inc. | Retinoid antagonists and use thereof |
| JP4543513B2 (ja) * | 2000-07-17 | 2010-09-15 | ソニー株式会社 | 双方向通信システム、表示装置、ベース装置および双方向通信方法 |
| EP1935869A1 (en) | 2000-10-02 | 2008-06-25 | F. Hoffmann-La Roche Ag | Retinoids for the treatment of emphysema |
| US6495719B2 (en) | 2001-03-27 | 2002-12-17 | Circagen Pharmaceutical | Histone deacetylase inhibitors |
| US7312247B2 (en) | 2001-03-27 | 2007-12-25 | Errant Gene Therapeutics, Llc | Histone deacetylase inhibitors |
| US8026280B2 (en) | 2001-03-27 | 2011-09-27 | Errant Gene Therapeutics, Llc | Histone deacetylase inhibitors |
| US7842727B2 (en) | 2001-03-27 | 2010-11-30 | Errant Gene Therapeutics, Llc | Histone deacetylase inhibitors |
| EP1511477A4 (en) | 2002-05-22 | 2008-04-09 | Errant Gene Therapeutics Llc | HISTONE DEACETYLASE INHIBITORS BASED ON ALPHA-KETO-EPOXYDE COMPOUNDS |
| WO2004046104A2 (en) | 2002-11-20 | 2004-06-03 | Errant Gene Therapeutics, Llc | Treatment of lung cells with histone deacetylase inhibitors |
| US20090016991A1 (en) * | 2004-07-29 | 2009-01-15 | Werner Bollag | Rxr Antagonist Treatment Against Multiple Sclerosis |
| EP1621191A1 (en) * | 2004-07-29 | 2006-02-01 | Werner Bollag | Treatment of inflammatory diseases by RXR Antagonists |
| CA2622600A1 (en) * | 2005-10-25 | 2007-05-03 | Werner Bollag | Rxr agonists and antagonists, alone or in combination with ppar ligands, in the treatment of metabolic and cardiovascular diseases |
| CN105646311B (zh) * | 2016-03-31 | 2017-09-26 | 广州巨元生化有限公司 | 一种制备β‑阿朴‑8’‑胡萝卜醛的方法 |
| EP3301085A1 (en) * | 2016-09-29 | 2018-04-04 | Biogem S.Ca.R.L. | Retinoid derivatives with antitumor activity |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3277147A (en) * | 1963-06-05 | 1966-10-04 | Olin Mathieson | Lower alkyl esters of beta-cyclocitrylidene fluoroacetic acid and beta-ionylidene fluoroacetic acid |
| US5514672A (en) * | 1981-02-17 | 1996-05-07 | Bazzano; Gail S. | Use of retinoids and compositions containing same for hair growth |
| WO1995004036A1 (en) * | 1993-01-11 | 1995-02-09 | Ligand Pharmaceuticals Inc. | Compounds having selective activity for retinoid x receptors, and means for modulation of processes mediated by retinoid x receptors |
| IL116259A (en) * | 1994-12-19 | 2000-07-16 | American Cyanamid Co | Analogs of 9-cis retinoic acid and their use |
-
1996
- 1996-02-14 DK DK96102137T patent/DK0728742T3/da active
- 1996-02-14 EP EP96102137A patent/EP0728742B1/en not_active Expired - Lifetime
- 1996-02-14 TW TW085101815A patent/TW343966B/zh active
- 1996-02-14 ES ES96102137T patent/ES2138765T3/es not_active Expired - Lifetime
- 1996-02-14 DE DE69604713T patent/DE69604713T2/de not_active Expired - Fee Related
- 1996-02-14 AT AT96102137T patent/ATE185799T1/de not_active IP Right Cessation
- 1996-02-15 CN CN96102022A patent/CN1124260C/zh not_active Expired - Fee Related
- 1996-02-16 MY MYPI96000610A patent/MY113430A/en unknown
- 1996-02-19 IL IL11717096A patent/IL117170A/xx not_active IP Right Cessation
- 1996-02-19 NZ NZ286017A patent/NZ286017A/en unknown
- 1996-02-19 AU AU45617/96A patent/AU703115B2/en not_active Ceased
- 1996-02-22 SG SG1996003689A patent/SG59945A1/en unknown
- 1996-02-22 CZ CZ1996537A patent/CZ291352B6/cs not_active IP Right Cessation
- 1996-02-22 RU RU96103662/04A patent/RU2166499C2/ru not_active IP Right Cessation
- 1996-02-23 MA MA24170A patent/MA23813A1/fr unknown
- 1996-02-23 NO NO960751A patent/NO309189B1/no unknown
- 1996-02-23 JP JP8036459A patent/JP2776787B2/ja not_active Expired - Fee Related
- 1996-02-23 FI FI960856A patent/FI960856A/fi unknown
- 1996-02-23 CA CA002170227A patent/CA2170227A1/en not_active Abandoned
- 1996-02-23 KR KR1019960004376A patent/KR100414342B1/ko not_active IP Right Cessation
- 1996-02-23 HU HU9600424A patent/HU219538B/hu unknown
-
1997
- 1997-10-17 US US08/953,361 patent/US5986131A/en not_active Expired - Fee Related
-
1998
- 1998-12-15 HK HK98113449A patent/HK1012330A1/xx not_active IP Right Cessation
-
2000
- 2000-01-19 GR GR20000400104T patent/GR3032407T3/el not_active IP Right Cessation
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