KR890003708A - 히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이디다졸리딘, 이들의 제조 방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체 - Google Patents

히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이디다졸리딘, 이들의 제조 방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체 Download PDF

Info

Publication number
KR890003708A
KR890003708A KR1019880010380A KR880010380A KR890003708A KR 890003708 A KR890003708 A KR 890003708A KR 1019880010380 A KR1019880010380 A KR 1019880010380A KR 880010380 A KR880010380 A KR 880010380A KR 890003708 A KR890003708 A KR 890003708A
Authority
KR
South Korea
Prior art keywords
hydroxymethyl
optically active
trifluoromethyl
nitro
phenyl
Prior art date
Application number
KR1019880010380A
Other languages
English (en)
Other versions
KR960016119B1 (ko
Inventor
코우 세디에르 다니엘
기글리오띠 기우세페
모질루스키 마틴
Original Assignee
허버트 프리텔
로우셀 우크라프
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 허버트 프리텔, 로우셀 우크라프 filed Critical 허버트 프리텔
Publication of KR890003708A publication Critical patent/KR890003708A/ko
Application granted granted Critical
Publication of KR960016119B1 publication Critical patent/KR960016119B1/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • A61K31/415—1,2-Diazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
    • C07D233/78—Radicals substituted by oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이미다졸리딘, 이들의 제조 방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 모든 가능한 라세미체 및 광학활성형태의 다음 일반식(Ⅰ)을 갖는 생성물 :
    상기식에서, X는 산소원자 또는 이민그룹을 나타낸다.
  2. 라세미체 또는 광학활성형태의 4-(히드록시메틸)-5-이미노-4-메틸-1-[4-니트로-3-(트리플루오로메틸)페닐]-2-이미다졸리디논.
  3. 라세미체 또는 광학활성형태의 4-(히드록시메틸)-4-메틸-1-[4-니트로-3-(트리플루오로메틸)페닐]-2,5-이미다졸리딘-디온.
  4. (4R) 4-(히드록시메틸)-4-메틸-1-[4-니트로-3(트리플루오로메틸)페닐]-2,5-이미다졸리딘-디온.
  5. (4S) 4-(히드록시메틸)-4-메틸-1-[4-니트로-3(트리플루오로메틸)페닐]-2,5-이미다졸리딘-디온.
  6. (4R) 및 (4S) 이성체의 혼합물의 형태의 4-(히드록시메틸)-4-메틸-1-[4-니트로-3-(트리플루오로메틸)페닐]-2,5-이미다졸리딘-디온.
  7. 라세미 또는 광학 활성형태의 2-아미노-2-(히드록시메틸)프로판 니트릴을 3-트리플루오로메틸-4-니트로페닐의 이소시아네이트와 반응시켜 X가 아미노그룹을 나타내는 식(Ⅰ)을 갖는 생성물, 즉, 라세미 또는 광학활성형태의 4-(히드록시메틸)-5-이미노-4-메틸-1-[4-니트로-3-(트리플루오로메틸)페닐]-2-이미다졸리디논을 얻고, 바람직하다면 두개의 광학활성이성체를 분리하고, 라세미 또는 광학활성형태의 X가 이미노그룹을 나타내는 식(Ⅰ)의 생성물을 가수분해시켜 X가 산소원자를 나타내는 일반식(Ⅰ)을 갖는 생성물, 즉, 라세미 또는 광학활성형태의 4-(히드록시메틸)-4-메틸-1-[4-니트로-3-(트리플루오로메틸)페닐]-2,5-이미다졸리딘-디온을 얻고, 라세미형태의 X가 산소원자를 나타내는 식(Ⅰ)을 갖는 생성물은 바람직하다면 그의 광학활성이성체로 분리함을 특징으로 하는 제1항에 정의한 식(Ⅰ)을 갖는 생성물의 제조방법.
  8. 의약으로서 제1 내지 6항중의 어느 한 항에 정의한 식(Ⅰ)을 갖는 생성물.
  9. 활성성분으로서 제8항에 정의한 의약품을 함유하는 제약조성물.
  10. 신규의 산업제품으로서 라세미체 또는 광학활성형태의 2-아미노-2-(히드록시메틸)-프로판니트릴.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880010380A 1987-08-13 1988-08-13 히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이미다졸리딘, 이들의 제조방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체 KR960016119B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR8711544A FR2619381B1 (fr) 1987-08-13 1987-08-13 Nouvelles imidazolidines substituees par un radical hydroxymethyle et un radical phenyl substitue, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant et un intermediaire pour leur preparation
FR87-11544 1987-08-13

Publications (2)

Publication Number Publication Date
KR890003708A true KR890003708A (ko) 1989-04-17
KR960016119B1 KR960016119B1 (ko) 1996-12-04

Family

ID=9354179

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019880010380A KR960016119B1 (ko) 1987-08-13 1988-08-13 히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이미다졸리딘, 이들의 제조방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체

Country Status (8)

Country Link
US (1) US4873256A (ko)
EP (1) EP0305270A1 (ko)
JP (1) JP2727199B2 (ko)
KR (1) KR960016119B1 (ko)
AU (1) AU618018B2 (ko)
CA (1) CA1304093C (ko)
FR (1) FR2619381B1 (ko)
ZA (1) ZA885846B (ko)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426383B2 (en) 2008-03-13 2013-04-23 Bioland Ltd. Anti-aging composition for external use comprising low and high molecular weight hyaluronic acids and the polysaccharides extracted from root bark of Ulmus davidiana

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4908456A (en) * 1989-04-05 1990-03-13 Takatori Corporation Process for preparing methylolated hydantoins
US5411981A (en) * 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
USRE35956E (en) * 1991-01-09 1998-11-10 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2671348B1 (fr) * 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
FR2724169B1 (fr) * 1994-09-06 1997-01-03 Roussel Uclaf Nouvelles phenylimidazolidines eventuellement substituees, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
TW521073B (en) * 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
FR2715402B1 (fr) * 1994-01-05 1996-10-04 Roussel Uclaf Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
KR20030016310A (ko) 2000-06-28 2003-02-26 브리스톨-마이어스스퀴브컴파니 선택적 안드로겐 수용체 조절제, 및 그의 확인, 고안 및사용 방법
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US7001911B2 (en) * 2000-06-28 2006-02-21 Bristol-Myers Squibb Company Fused cyclic modulators of nuclear hormone receptor function
EP1854798A3 (en) 2000-09-19 2007-11-28 Bristol-Myers Squibb Company Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US6953679B2 (en) 2000-09-19 2005-10-11 Bristol-Myers Squibb Company Method for the preparation of fused heterocyclic succinimide compounds and analogs thereof
US20040087548A1 (en) 2001-02-27 2004-05-06 Salvati Mark E. Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
AU2002364082A1 (en) 2001-12-19 2003-07-09 Bristol-Myers Squibb Company Fused heterocyclic compounds and analogs thereof: modulators of nuclear hormone receptor function
AU2004305075A1 (en) * 2003-12-19 2005-07-07 The Regents Of The University Of California Methods and materials for assessing prostate cancer therapies
WO2005099693A2 (en) * 2004-02-24 2005-10-27 The Regents Of The University Of California Methods and materials for assessing prostate cancer therapies and compounds
US7709517B2 (en) * 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
PL3412290T3 (pl) 2006-03-27 2021-09-06 The Regents Of The University Of California Modulator receptora androgenowego do leczenia raka gruczołu krokowego i chorób związanych z receptorem androgenowym
WO2007127010A2 (en) 2006-03-29 2007-11-08 The Regents Of The University Of California Diarylthiohydantoin compounds
US8168667B2 (en) * 2006-05-31 2012-05-01 Galapagos Nv Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
EP2220050A2 (en) 2007-10-26 2010-08-25 The Regents Of The University Of California Diarylhydantoin compounds as androgen receptor modulators
GB2463514C (en) * 2008-09-11 2018-09-26 Galapagos Nv Imidazolidine compounds and uses therefor
EA028869B1 (ru) 2010-02-16 2018-01-31 Арагон Фармасьютикалс, Инк. Модуляторы рецептора андрогенов и их применение
KR102210825B1 (ko) 2012-09-26 2021-02-01 아라곤 파마슈티컬스, 인코포레이티드 비전이성 거세 저항성 전립선암 치료용 항안드로겐
JOP20200097A1 (ar) 2013-01-15 2017-06-16 Aragon Pharmaceuticals Inc معدل مستقبل أندروجين واستخداماته
KR101652297B1 (ko) 2015-03-31 2016-08-31 (주)와이솔 Saw 필터
TWI726969B (zh) 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
US10702508B2 (en) 2017-10-16 2020-07-07 Aragon Pharmaceuticals, Inc. Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3651079A (en) * 1968-11-25 1972-03-21 Colgate Palmolive Co 1-aryl-5-hydroxyalkyl-hydantoins
JPS4916937B1 (ko) * 1970-01-21 1974-04-25
FR2329276A1 (fr) * 1975-10-29 1977-05-27 Roussel Uclaf Nouvelles imidazolidines substituees, procede de preparation, application comme medicament et compositions les renfermant
EP0091596B1 (de) * 1982-04-08 1991-09-11 Shell Internationale Researchmaatschappij B.V. Neue Hydantoine, ihre Herstellung und Verwendung
US4473393A (en) * 1982-08-06 1984-09-25 Buffalo Color Corporation Pesticidal thiohydantoin compositions

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426383B2 (en) 2008-03-13 2013-04-23 Bioland Ltd. Anti-aging composition for external use comprising low and high molecular weight hyaluronic acids and the polysaccharides extracted from root bark of Ulmus davidiana

Also Published As

Publication number Publication date
US4873256A (en) 1989-10-10
ZA885846B (en) 1989-10-25
EP0305270A1 (fr) 1989-03-01
CA1304093C (fr) 1992-06-23
FR2619381B1 (fr) 1989-12-08
KR960016119B1 (ko) 1996-12-04
JPS6470473A (en) 1989-03-15
AU618018B2 (en) 1991-12-12
FR2619381A1 (fr) 1989-02-17
AU2091588A (en) 1989-02-16
JP2727199B2 (ja) 1998-03-11

Similar Documents

Publication Publication Date Title
KR890003708A (ko) 히드록시메틸기 및 치환된 페닐기에 의해 치환된 신규의 이디다졸리딘, 이들의 제조 방법, 의약으로서 이들의 용도, 이들을 함유하는 제약조성물 및 이들의 제조를 위한 중간체
PT93531A (pt) Processo para a preparacao de derivados de n-(3-hidroxi-4-piperidinil)(dihidrobenzofurano,dihidro-2h-benzopirano ou dihidrobenzodioxin)carboxamidas e de composicoes farmaceuticas que os contem
BR9915727A (pt) ésteres derivados de compostos de fenil-ciclohexila substituìdos
PT91931A (pt) Processo de preparacao de derivados de acido fenilalcanoico e de composicoes farmaceuticas que os contem
DE69207601D1 (de) Verfahren zur herstellung von sertralin-zwischenprodukten
FR2742749B1 (fr) Nouvelles phenylimidazolidines comportant notamment un radical nitrooxy ou carbonyloxy, procede et intermediaires de preparation, application comme medicaments, nouvelles utilisations et compositions pharmaceutiques
KR920004357A (ko) 살충제
FR2645537B1 (fr) Nouveaux sulfonamides derives d'acides benzocycliques ou benzoheterocycliques, leur preparation et leur application en therapeutique
ES508587A0 (es) "procedimiento para la preparacion de nuevas amidas de acidos carboxilicos".
JPS5665869A (en) Novel 22hydroxyalkyll3*4*55trihydroxyypiperidine compound* its manufacture and drug
HU895336D0 (en) Process for producing beta-delta-phenylthioxylosides and pharmaceutical compositions comprising such compounds as active ingredient
BR8104800A (pt) Derivativos de arilamina ,processo para sua preparacao e composicoes ,processo para a preparacao de composicoes ,empprego e processo para o combate e/ou impedimento de uma infestacao de plantas por fungos
TNSN92017A1 (fr) Procede de preparation, d'un derive de benzothiazole, et d'une composition pharmaceutique le contenant et procede de traitement en comportant application
PT95735A (pt) Processo para a preparacao de morfolinois e de composicoes farmaceuticas que os contem
RU93053624A (ru) 4-[(2-БЕНЗОТИАЗОЛИЛ)МЕТИЛАМИНО] -α- [(3,4-ДИФТОРОФЕНОКСИ)МЕТИЛ]-1-ПИПЕРИДИНЭТАНОЛ, СПОСОБ ЕГО ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЕЕ ПОЛУЧЕНИЯ
EP0304271A3 (en) Omega-arylsulphonamidoalkanoic acids for treatment of thromboxane medited diseases
KR910015537A (ko) 신규 1-아릴술포닐-2-피페리디논 유도체, 이의 제조방법, 제조용 중간체, 의약품으로서의 용도 및 이 화합물을 함유하는 조성물
EP0173377A3 (en) Pyrimidone compounds, their preparation and pharmaceutical compositions containing them
BR8900238A (pt) Composto de oxadiazol,processo para sua preparacao,composicao pesticida e processo para combater pragas
KR940007010A (ko) 옥사졸리딘
NL7708616A (nl) Werkwijze voor de bereiding van gesubstitueerde 2,3-alkyleen-bis-(oxy)-benzamiden met psycho- functionele werking, werkwijze voor de berei- ding van een geneesmiddel met een dergelijke werking en een dergelijk geneesmiddel.
SE9302437D0 (sv) N-derivatives of (phenylethyl-beta-ol) amine, a process for their preparation and pharmaceutical compositions containing the same
KR940005610A (ko) 신규한 피페리딘 유도체 및 이의 제조방법
KR890001582A (ko) 향류머티스제
KR890002159A (ko) 디히드로피리딘락톨 및 그의 의약품으로서의 용도

Legal Events

Date Code Title Description
A201 Request for examination
E902 Notification of reason for refusal
G160 Decision to publish patent application
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
FPAY Annual fee payment

Payment date: 20041201

Year of fee payment: 9

LAPS Lapse due to unpaid annual fee