KR101536806B1 - 타자로텐 유도체 - Google Patents

타자로텐 유도체 Download PDF

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Publication number
KR101536806B1
KR101536806B1 KR1020127003938A KR20127003938A KR101536806B1 KR 101536806 B1 KR101536806 B1 KR 101536806B1 KR 1020127003938 A KR1020127003938 A KR 1020127003938A KR 20127003938 A KR20127003938 A KR 20127003938A KR 101536806 B1 KR101536806 B1 KR 101536806B1
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KR
South Korea
Prior art keywords
ethynyl
dimethylthiochroman
ethyl
pyridine
delete delete
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Expired - Fee Related
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KR1020127003938A
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English (en)
Korean (ko)
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KR20120056821A (ko
Inventor
수에 게
한센 옹
웬디 후앙 첸
한스 호플랜드
마이클 제이. 비숍
프랭크 카이
알랜 콜본
Original Assignee
스티펠 래버러토리즈, 인코포레이티드
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Publication of KR20120056821A publication Critical patent/KR20120056821A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/327—Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020127003938A 2009-07-16 2010-07-16 타자로텐 유도체 Expired - Fee Related KR101536806B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US21379409P 2009-07-16 2009-07-16
US61/213,794 2009-07-16
US27225709P 2009-09-04 2009-09-04
US61/272,257 2009-09-04
PCT/US2010/042225 WO2011009023A1 (en) 2009-07-16 2010-07-16 Tazarotene derivatives

Publications (2)

Publication Number Publication Date
KR20120056821A KR20120056821A (ko) 2012-06-04
KR101536806B1 true KR101536806B1 (ko) 2015-07-14

Family

ID=43449815

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127003938A Expired - Fee Related KR101536806B1 (ko) 2009-07-16 2010-07-16 타자로텐 유도체

Country Status (16)

Country Link
US (3) US20120115909A1 (https=)
EP (1) EP2453746A4 (https=)
JP (1) JP5635090B2 (https=)
KR (1) KR101536806B1 (https=)
CN (1) CN102595892B (https=)
AU (1) AU2010273261B2 (https=)
BR (1) BR112012001680A2 (https=)
CA (1) CA2768015C (https=)
EA (1) EA022322B1 (https=)
IL (1) IL217519A (https=)
IN (1) IN2012DN00546A (https=)
MX (1) MX2012000768A (https=)
NZ (1) NZ598240A (https=)
SG (1) SG177579A1 (https=)
WO (1) WO2011009023A1 (https=)
ZA (1) ZA201200253B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201105050D0 (en) 2011-03-25 2011-05-11 Iiaa Ltd Pharmaceutical agent
BR112013033309B1 (pt) * 2011-06-24 2022-07-05 Gri Bio, Inc Uso de tazaroteno e método in vitro para inibição de ativação de células nkt tipo i
CN106918676B (zh) * 2015-12-24 2020-08-11 重庆华邦制药有限公司 分离测定他扎罗汀倍他米松乳膏中两种药物含量及有关物质的方法
WO2017152725A1 (zh) * 2016-03-11 2017-09-14 中国科学院上海有机化学研究所 一种视黄酸类化合物、其制备方法、中间体及应用
CN107176945B (zh) * 2016-03-11 2021-06-08 中国科学院上海有机化学研究所 一种视黄酸类化合物、其制备方法、中间体及应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5677323A (en) * 1989-09-19 1997-10-14 Allergan Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1, 2, 3, 4, -tetrahydroquinolinyl group having retinoid-like activity
US20050002878A1 (en) * 2001-10-05 2005-01-06 Pascal Lefrancois Use of tazarotene for preparing a nail varnish for treating and/or preventing psoriasis and nail varnish containing same

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Publication number Priority date Publication date Assignee Title
US4801593A (en) * 1979-09-13 1989-01-31 Burroughs Wellcome Co. Chemotherapeutic agents
US5399561A (en) 1989-09-19 1995-03-21 Allergan, Inc. Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-oxochromanyl, 2-oxothiochromanyl or 2-oxo-1,2,3,4-tetrahydro-quinolinyl group having retinoid-like biological activity
US5272156A (en) 1989-09-19 1993-12-21 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5045551A (en) 1989-09-19 1991-09-03 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5162546A (en) 1989-09-19 1992-11-10 Allergan, Inc. Acetylenes disubstituted with a phenyl group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US4980369A (en) 1989-09-19 1990-12-25 Allergan, Inc. Acetylenes disubstituted with a phenyl group and a 2-substituted chromanyl or thiochromanyl group having retinoid-like activity
EP0553156A4 (en) 1990-10-09 1993-11-18 Allergan, Inc. Chromans and thiochromans with retinoid-like activity
EP0571546B1 (en) 1991-02-13 1996-10-16 Allergan, Inc. Chroman and thiochromans with phenylethynyl substituents at the 7-position having retinoid-like biological activity
AU652830B2 (en) 1991-03-26 1994-09-08 Allergan, Inc. Chromans and thiochromans with heteroarylethynyl substituents at the 7-position having retinoid-like biological activity
WO1999002133A2 (en) * 1997-07-08 1999-01-21 Dsm N.V. Topical application of a combination of benzoyl peroxide and a second active ingredient
DK1100490T3 (da) * 1998-07-28 2007-04-10 Susan Bershad Behandling med kort kontakttid af acne og fotoældning med topiske retinoider
US6048902A (en) * 1999-02-12 2000-04-11 Lebwohl; Mark G. Short contact treatment of psoriasis with topical retinoids
CN1210041C (zh) * 2003-09-29 2005-07-13 中国医学科学院皮肤病研究所 治疗痤疮的复方外用药物
ITMI20050357A1 (it) * 2005-03-08 2006-09-09 Solmag S P A Procedimento di preparazione del tazarotene
AR054805A1 (es) * 2005-06-29 2007-07-18 Stiefel Laboratories Composiciones topicas para el tratamiento de la piel
WO2007092312A2 (en) * 2006-02-03 2007-08-16 Stiefel Laboratories, Inc. Topical skin treating compositions
MXPA06008988A (es) 2006-08-08 2008-02-07 Fernando Ahumada Ayala Preparaciones topicas antiacne que contienen retinoide (tazaroteno o adapaleno), antibiotico (fosfato de clindamicina) y/o queratolitico (peroxido de bonzoilo en microesponjas).
US20100047357A1 (en) * 2007-02-01 2010-02-25 Sol-Gel Technologies Ltd. Compositions for topical application comprising a peroxide and retinoid

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5677323A (en) * 1989-09-19 1997-10-14 Allergan Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1, 2, 3, 4, -tetrahydroquinolinyl group having retinoid-like activity
US20050002878A1 (en) * 2001-10-05 2005-01-06 Pascal Lefrancois Use of tazarotene for preparing a nail varnish for treating and/or preventing psoriasis and nail varnish containing same

Also Published As

Publication number Publication date
JP5635090B2 (ja) 2014-12-03
US20120115909A1 (en) 2012-05-10
IL217519A (en) 2015-06-30
JP2012533564A (ja) 2012-12-27
EP2453746A1 (en) 2012-05-23
IL217519A0 (en) 2012-02-29
US20140357669A1 (en) 2014-12-04
AU2010273261B2 (en) 2013-07-25
EA201270176A1 (ru) 2012-08-30
IN2012DN00546A (https=) 2015-06-12
BR112012001680A2 (pt) 2015-09-01
MX2012000768A (es) 2012-02-13
KR20120056821A (ko) 2012-06-04
ZA201200253B (en) 2013-05-29
AU2010273261A1 (en) 2012-02-02
CN102595892B (zh) 2014-09-10
US9062037B2 (en) 2015-06-23
EP2453746A4 (en) 2013-04-24
US20140357672A1 (en) 2014-12-04
WO2011009023A1 (en) 2011-01-20
CA2768015C (en) 2016-03-15
CA2768015A1 (en) 2011-01-20
NZ598240A (en) 2013-10-25
CN102595892A (zh) 2012-07-18
SG177579A1 (en) 2012-02-28
EA022322B1 (ru) 2015-12-30

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