JPH09501172A - 不安症の治療用抗グルココルチコイドステロイド - Google Patents
不安症の治療用抗グルココルチコイドステロイドInfo
- Publication number
- JPH09501172A JPH09501172A JP7506200A JP50620095A JPH09501172A JP H09501172 A JPH09501172 A JP H09501172A JP 7506200 A JP7506200 A JP 7506200A JP 50620095 A JP50620095 A JP 50620095A JP H09501172 A JPH09501172 A JP H09501172A
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- hydroxy
- alkyl
- alkoxy
- group
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.不安症治療用医薬組成物を製造するための抗グルココルチコイドステロイド の使用。 2.抗グルココルチコイドステロイドが、式: [式中、R1は、H、CH3、非置換又はOH若しくはハロゲン置換されたCH2 =CH−CH2若しくはCH≡C−CH2、又はアリール部分が任意に(C1−C6 )アルキル、(C1−C6)アルコキシ、OH、ハロゲン若しくはCF3で置換さ れてよい、アリール、アリールチオ若しくはアリールメチル基であるか、あるい はR1はR7と一緒に結合を形成し、 R2は、H、(C1−C6)アルキル、又は(C1−C6)アシル、(C1−C6) アルコキシ、(C1−C6)チオアルコキシ、−O−(CH2)n−O−(ここで、 nは1又は2 H、又は(C1−C6)アルキル及び(C1−C6)アシルから選択された基である 〕から選択された基で任意に置換されたアリール基であるか、あるいは、R2は R7と一緒に結合を形成し、 R3は(C1−C6)アルキルであり、 R4は、H、OH、(C1−C6)アルコキシ、(C1−C6)アシルオキシ、そ れぞれ、ヒドロキシ、オキソ、ハロゲン、アジド若しくはシアノで置換されてよ い、(C1−C6)アルキル、(C1−C6)アルケニル及び(C1−C6)アルキニ ルから選択された基、又はフェニル基が任意に−S(O)m−(C1−C6)アル キル(ここで、mは1若し ぞれ独立に、H、又は(C1−C6)アルキル及び(C1−C6)アシルから選択さ れた基であるか、あるいは、X及びYはそれらが結合している窒素と一緒に環を 形成する〕で置換されてよい−C≡C−フェニルであり、 R5は、OH、又はそれぞれ任意に、ヒドロキシ、(C1−C6)アルコキシ、 (C1−C6)アシルオキシ若しくはハロゲンで置換されてよい、(C1−C6)ア シルオキシ、(C1−C6)アルコキシ若しくは(C1−C6)アシルから 選択された基であるか、あるいは R4及びR5は、それらが結合している炭素原子と一緒に5員又は6員環系を形 成し、 R6は、H、又はヒドロキシ若しくは(C1−C6)アルコキシで任意に置換さ れたメチルであり、 R7はR1又はR2との結合を形成する] を有することを特徴とする請求項1に記載の使用。 3.前記ステロイドが、11β−(4−ジメチルアミノフェニル)−17β−ヒ ドロキシ−17α−(プロプ−1−イニル)−エストラ−4,9−ジエン−3− オン(RU38486)、(11β,17α)−11,21−ビス[4−(ジメ チルアミノ)フェニル]−17−ヒドロキシ−19−ノルプレグナ−4,9−ジ エン−20−イン−3−オン、(11β,17α)−11−[4−(ジメチルア ミノ)フェニル]−17−ヒドロキシ−21−[4−(1−ピロリジニル)フェ ニル]−19−ノルプレグナ−4,9−ジエン−20−イン−3−オン、(11 β,17α)−11−(1,3−ベンゾジオキソル−5−イル)−21−[4− (ジメチルアミノ)フェニル]−17−ヒドロキシ−19−ノルプレグナ−4, 9−ジエン−20−イン−3−オン、 及び(11β,17α)−11−[4−(ジメチルアミノ)フェニル]−17− ヒドロキシ−21−[4−(メチルスルホニル)フェニル]−19−ノルプレグ ナ−4,9−ジエン−20−イン−3−オンから選択されることを特徴とする請 求項1又は2に記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP93202304.7 | 1993-08-04 | ||
EP93202304 | 1993-08-04 | ||
PCT/EP1994/002513 WO1995004536A1 (en) | 1993-08-04 | 1994-07-28 | Antiglucocorticoid steroids for the treatment of anxiety disorders |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH09501172A true JPH09501172A (ja) | 1997-02-04 |
JP3828926B2 JP3828926B2 (ja) | 2006-10-04 |
Family
ID=8214027
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50620095A Expired - Lifetime JP3828926B2 (ja) | 1993-08-04 | 1994-07-28 | 不安症の治療用抗グルココルチコイドステロイド |
Country Status (11)
Country | Link |
---|---|
US (1) | US5741787A (ja) |
EP (1) | EP0712311B1 (ja) |
JP (1) | JP3828926B2 (ja) |
AT (1) | ATE171873T1 (ja) |
AU (1) | AU687088B2 (ja) |
CA (1) | CA2166332C (ja) |
DE (1) | DE69413829T2 (ja) |
DK (1) | DK0712311T3 (ja) |
ES (1) | ES2124905T3 (ja) |
NZ (1) | NZ271363A (ja) |
WO (1) | WO1995004536A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002521430A (ja) * | 1998-07-30 | 2002-07-16 | アボット・ラボラトリーズ | グルココルチコイド選択性薬剤 |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE156836T1 (de) * | 1994-05-19 | 1997-08-15 | Akzo Nobel Nv | 11,21-bisphenyl-19-nor-pregnan derivate |
IL118974A (en) * | 1995-08-17 | 2001-09-13 | Akzo Nobel Nv | History 11 - (Transformed Phenyl) - Astra - 4, 9 - Diane, their preparation and pharmaceutical preparations containing them |
IL119649A (en) * | 1995-11-30 | 2002-03-10 | Akzo Nobel Nv | Preparation of Cyclic Kills of History - 3 keto- (5) 10, (-9) 11 steroidadians |
ES2120267T3 (es) * | 1995-12-22 | 1998-10-16 | Jenapharm Gmbh | Nuevos derivados de 17alfa-cianometilestra-4,9-dieno, un proceso para su preparacion y composiciones farmaceuticas que los contienen. |
HU230492B1 (hu) * | 1996-05-01 | 2016-08-29 | The Government Of The United States Of America | Új progesztációt gátló szerként használható 21-helyzetben szubsztituált progeszteron-származékok, ezeket tartalmazó gyógyszerkészítmények, alkalmazásuk |
US6900193B1 (en) * | 1996-05-01 | 2005-05-31 | The United States Of America As Represented By The Department Of Health And Human Services | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
FR2757400B1 (fr) * | 1996-12-19 | 1999-12-17 | Hoechst Marion Roussel Inc | Application des composes antiglucocorticoides dans le traitement des psychoses ou des comportements addictifs |
EP1079859B1 (en) | 1998-05-22 | 2010-07-14 | The Board Of Trustees Of The Leland Stanford Junior University | Bifunctional molecules and therapies based thereon |
DE60234057D1 (de) | 2001-07-25 | 2009-11-26 | Raptor Pharmaceutical Inc | Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke |
US7250408B2 (en) | 2002-12-16 | 2007-07-31 | Bayer Schering Pharma Ag | Glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility |
CA2516319C (en) * | 2003-02-28 | 2012-09-18 | The Government Of The United States Of America, As Represented By The Se Cretary, Department Of Health And Human Services | Method for preparing 17.alpha.-acetoxy-11.beta.-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates thereof, and methods for the preparation of such intermediates |
US8097606B2 (en) * | 2003-07-23 | 2012-01-17 | Corcept Therapeutics, Inc. | Antiglucocorticoids for the treatment of catatonia |
CN103259027A (zh) | 2005-04-28 | 2013-08-21 | 普罗透斯数字保健公司 | 药物信息*** |
EP1945240B1 (en) | 2005-09-16 | 2016-12-28 | Raptor Pharmaceutical Inc | Compositions comprising receptor-associated protein (rap) variants specific for cr-containing proteins and uses thereof |
PL3395372T3 (pl) | 2009-02-20 | 2022-07-25 | EnhanX Biopharm Inc. | Układ do dostarczania leków na bazie glutationu |
KR20190116576A (ko) | 2009-05-06 | 2019-10-14 | 라보라토리 스킨 케어, 인크. | 활성제-칼슘 포스페이트 입자 복합체를 포함하는 피부 전달 조성물 및 이들을 이용하는 방법 |
WO2017112904A1 (en) | 2015-12-23 | 2017-06-29 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
US11208432B2 (en) | 2015-12-23 | 2021-12-28 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
CN108699102A (zh) | 2015-12-23 | 2018-10-23 | 欧瑞克制药公司 | 糖皮质激素受体抑制剂 |
CA3039636C (en) | 2016-10-07 | 2023-04-11 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5232917A (en) * | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
-
1994
- 1994-07-28 AU AU74968/94A patent/AU687088B2/en not_active Expired
- 1994-07-28 CA CA002166332A patent/CA2166332C/en not_active Expired - Lifetime
- 1994-07-28 DE DE69413829T patent/DE69413829T2/de not_active Expired - Lifetime
- 1994-07-28 DK DK94924819T patent/DK0712311T3/da active
- 1994-07-28 NZ NZ271363A patent/NZ271363A/xx not_active IP Right Cessation
- 1994-07-28 AT AT94924819T patent/ATE171873T1/de active
- 1994-07-28 WO PCT/EP1994/002513 patent/WO1995004536A1/en active IP Right Grant
- 1994-07-28 JP JP50620095A patent/JP3828926B2/ja not_active Expired - Lifetime
- 1994-07-28 US US08/581,631 patent/US5741787A/en not_active Expired - Lifetime
- 1994-07-28 EP EP94924819A patent/EP0712311B1/en not_active Expired - Lifetime
- 1994-07-28 ES ES94924819T patent/ES2124905T3/es not_active Expired - Lifetime
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002521430A (ja) * | 1998-07-30 | 2002-07-16 | アボット・ラボラトリーズ | グルココルチコイド選択性薬剤 |
JP4676061B2 (ja) * | 1998-07-30 | 2011-04-27 | アボット・ラボラトリーズ | グルココルチコイド選択性薬剤 |
Also Published As
Publication number | Publication date |
---|---|
DK0712311T3 (da) | 1999-06-21 |
ES2124905T3 (es) | 1999-02-16 |
DE69413829T2 (de) | 1999-04-15 |
NZ271363A (en) | 1999-06-29 |
EP0712311B1 (en) | 1998-10-07 |
JP3828926B2 (ja) | 2006-10-04 |
CA2166332C (en) | 2005-05-10 |
WO1995004536A1 (en) | 1995-02-16 |
ATE171873T1 (de) | 1998-10-15 |
AU7496894A (en) | 1995-02-28 |
AU687088B2 (en) | 1998-02-19 |
EP0712311A1 (en) | 1996-05-22 |
CA2166332A1 (en) | 1995-02-16 |
DE69413829D1 (de) | 1998-11-12 |
US5741787A (en) | 1998-04-21 |
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