DK173854B1 - 7alfa-Acylthio-9alfa,11alfa-epoxy-20-spirox-4-en-3,21-dioner, fremgangsmåde til deres fremstilling, farmaceutiske præparater med indhold deraf samt deres anvendelse til fremstilling af farmaceutiske præparater - Google Patents

7alfa-Acylthio-9alfa,11alfa-epoxy-20-spirox-4-en-3,21-dioner, fremgangsmåde til deres fremstilling, farmaceutiske præparater med indhold deraf samt deres anvendelse til fremstilling af farmaceutiske præparater Download PDF

Info

Publication number: DK173854B1
Authority: DK; Denmark
Prior art keywords: mixture; epoxy; solution; dione; acid
Prior art date: 1984-06-21

Application number

DK198502800A

Other languages

Danish (da)

English (en)

Other versions

DK280085D0 (da

DK280085A (da

Inventor

Michel Biollaz

Original Assignee

Novartis Ag

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.)

1984-06-21

Filing date

1985-06-20

Publication date

2001-12-27

1985-06-20 Application filed by Novartis Ag filed Critical Novartis Ag

1985-06-20 Publication of DK280085D0 publication Critical patent/DK280085D0/da

1985-12-22 Publication of DK280085A publication Critical patent/DK280085A/da

2001-12-27 Application granted granted Critical

2001-12-27 Publication of DK173854B1 publication Critical patent/DK173854B1/da

Links

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LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
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239000000843 powder Substances 0.000 description 1
KOODSCBKXPPKHE-UHFFFAOYSA-N propanethioic s-acid Chemical compound CCC(S)=O KOODSCBKXPPKHE-UHFFFAOYSA-N 0.000 description 1
238000011321 prophylaxis Methods 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
230000002685 pulmonary effect Effects 0.000 description 1
BBFCIBZLAVOLCF-UHFFFAOYSA-N pyridin-1-ium;bromide Chemical compound Br.C1=CC=NC=C1 BBFCIBZLAVOLCF-UHFFFAOYSA-N 0.000 description 1
150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
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AYRVGWHSXIMRAB-UHFFFAOYSA-M sodium acetate trihydrate Chemical compound O.O.O.[Na+].CC([O-])=O AYRVGWHSXIMRAB-UHFFFAOYSA-M 0.000 description 1
235000010413 sodium alginate Nutrition 0.000 description 1
239000000661 sodium alginate Substances 0.000 description 1
229940005550 sodium alginate Drugs 0.000 description 1
235000017557 sodium bicarbonate Nutrition 0.000 description 1
229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
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239000012312 sodium hydride Substances 0.000 description 1
229910000104 sodium hydride Inorganic materials 0.000 description 1
235000009518 sodium iodide Nutrition 0.000 description 1
235000010265 sodium sulphite Nutrition 0.000 description 1
RPACBEVZENYWOL-XFULWGLBSA-M sodium;(2r)-2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate Chemical compound [Na+].C=1C=C(Cl)C=CC=1OCCCCCC[C@]1(C(=O)[O-])CO1 RPACBEVZENYWOL-XFULWGLBSA-M 0.000 description 1
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239000004408 titanium dioxide Substances 0.000 description 1
BPLKQGGAXWRFOE-UHFFFAOYSA-M trimethylsulfoxonium iodide Chemical compound [I-].C[S+](C)(C)=O BPLKQGGAXWRFOE-UHFFFAOYSA-M 0.000 description 1
210000005239 tubule Anatomy 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
- C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
- C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
- C07J53/004—3 membered carbocyclic rings
- C07J53/008—3 membered carbocyclic rings in position 15/16
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
- C07J71/0015—Oxiranes at position 9(11)

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Steroid Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

DK198502800A 1984-06-21 1985-06-20 7alfa-Acylthio-9alfa,11alfa-epoxy-20-spirox-4-en-3,21-dioner, fremgangsmåde til deres fremstilling, farmaceutiske præparater med indhold deraf samt deres anvendelse til fremstilling af farmaceutiske præparater DK173854B1 (da)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
CH300984		1984-06-21
CH300984		1984-06-21
CH464684		1984-09-28
CH464684		1984-09-28

Publications (3)

Publication Number	Publication Date
DK280085D0 DK280085D0 (da)	1985-06-20
DK280085A DK280085A (da)	1985-12-22
DK173854B1 true DK173854B1 (da)	2001-12-27

Family

ID=25691934

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK198502800A DK173854B1 (da)	1984-06-21	1985-06-20	7alfa-Acylthio-9alfa,11alfa-epoxy-20-spirox-4-en-3,21-dioner, fremgangsmåde til deres fremstilling, farmaceutiske præparater med indhold deraf samt deres anvendelse til fremstilling af farmaceutiske præparater

Country Status (16)

Country	Link
US (1)	US4670551A (mo)
EP (1)	EP0165902B1 (mo)
AR (2)	AR242036A1 (mo)
AU (1)	AU582754B2 (mo)
CA (1)	CA1239388A (mo)
DE (1)	DE3569540D1 (mo)
DK (1)	DK173854B1 (mo)
ES (2)	ES8704967A1 (mo)
FI (1)	FI83225C (mo)
GR (1)	GR851499B (mo)
HU (1)	HU192232B (mo)
IE (1)	IE58050B1 (mo)
IL (1)	IL75569A (mo)
NO (1)	NO165496C (mo)
NZ (1)	NZ212492A (mo)
PT (1)	PT80663B (mo)

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PT973791E (pt)	1995-12-11	2007-09-26	Searle Llc	Processo para a preparação de um composto epoxi
EP1148061B1 (en) *	1996-12-11	2007-10-17	G.D. Searle LLC.	Epoxidation process
US6887991B1 (en)	1996-12-11	2005-05-03	G. D. Searle & Company	Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein
DK0944644T3 (da)	1996-12-11	2003-02-03	Searle & Co	Fremgangsmåde til fremstilling af 3-keto-7-alfa-alkoxycarbonyl-delta-4,5-steroider og mellemprodukter, som er nyttite derfor
ATE473759T1 (de)	1998-05-22	2010-07-15	Univ Leland Stanford Junior	Bifunktionelle moleküle sowie darauf basierende therapien.
EP1455795A1 (en)	2001-12-12	2004-09-15	Pharmacia Corporation	Method of treating ophthalmic disorders with epoxy-steroidal aldosterone receptor antagonists
US7235655B2 (en)	2002-03-22	2007-06-26	Pharmacia & Upjohn Company	Processes to prepare eplerenone
CN102379684B (zh)	2005-04-28	2014-11-19	普罗透斯数字保健公司	药物信息系统
WO2007025780A2 (en) *	2005-09-02	2007-03-08	Recordati Ireland Limited	Aldosterone receptor antagonists
US9062126B2 (en)	2005-09-16	2015-06-23	Raptor Pharmaceuticals Inc.	Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
EP2398500B1 (en)	2009-02-20	2019-03-13	2-BBB Medicines B.V.	Glutathione-based drug delivery system
ES2942923T3 (es)	2009-05-06	2023-06-07	Laboratory Skin Care Inc	Composiciones de administración dérmica que comprenden complejos de agente activo-partículas de fosfato de calcio y métodos de uso de las mismas

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US3013012A (en) *	1960-12-22	1961-12-12	Searle & Co	Alkanoylthio-17alpha-carboxyethyl-17beta-hydroxyandrosten-3-one lactones
US3095412A (en) *	1961-12-19	1963-06-25	Searle & Co	9alpha, 11alpha-epoxy and 11beta-chloro-9alpha-hydroxy 17alpha-(2-carboxyethyl)-17beta-hydroxyandrost-4-en-3-one gamma-lactones and delta1 and delta6 analogs
GB1041534A (en) *	1963-04-24	1966-09-07	Merck & Co Inc	20-spiroxane compounds
DE2652761C2 (de) *	1976-11-16	1985-11-21	Schering AG, 1000 Berlin und 4709 Bergkamen	15,16-Methylen-Spirolactone, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
US4559332A (en) *	1983-04-13	1985-12-17	Ciba Geigy Corporation	20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
EP0134529B1 (de) *	1983-08-17	1990-03-21	Schering Aktiengesellschaft	7-alpha-Substituierte 3-Oxo-17alpha-pregn-4-en-21.17-carbolactone, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Präparate

1985
- 1985-06-13 US US06/744,444 patent/US4670551A/en not_active Expired - Fee Related
- 1985-06-17 DE DE8585810277T patent/DE3569540D1/de not_active Expired
- 1985-06-17 EP EP85810277A patent/EP0165902B1/de not_active Expired
- 1985-06-19 CA CA000484418A patent/CA1239388A/en not_active Expired
- 1985-06-19 IL IL75569A patent/IL75569A/xx not_active IP Right Cessation
- 1985-06-19 PT PT80663A patent/PT80663B/pt not_active IP Right Cessation
- 1985-06-19 GR GR851499A patent/GR851499B/el unknown
- 1985-06-19 FI FI852430A patent/FI83225C/fi not_active IP Right Cessation
- 1985-06-20 DK DK198502800A patent/DK173854B1/da not_active IP Right Cessation
- 1985-06-20 NO NO852501A patent/NO165496C/no unknown
- 1985-06-20 IE IE153585A patent/IE58050B1/en not_active IP Right Cessation
- 1985-06-20 ES ES544387A patent/ES8704967A1/es not_active Expired
- 1985-06-20 NZ NZ212492A patent/NZ212492A/xx unknown
- 1985-06-20 HU HU852433A patent/HU192232B/hu not_active IP Right Cessation
- 1985-06-21 AU AU43971/85A patent/AU582754B2/en not_active Ceased
- 1985-06-21 AR AR85300773A patent/AR242036A1/es active
1986
- 1986-10-01 ES ES557112A patent/ES8707737A1/es not_active Expired
1989
- 1989-07-31 AR AR89314546A patent/AR245731A1/es active

Also Published As

Publication number	Publication date
EP0165902B1 (de)	1989-04-19
DK280085D0 (da)	1985-06-20
DK280085A (da)	1985-12-22
US4670551A (en)	1987-06-02
ES557112A0 (es)	1987-08-16
IE851535L (en)	1985-12-21
NO165496C (no)	1991-02-20
DE3569540D1 (en)	1989-05-24
NZ212492A (en)	1989-02-24
EP0165902A2 (de)	1985-12-27
ES544387A0 (es)	1987-04-16
IL75569A0 (en)	1985-10-31
EP0165902A3 (en)	1986-10-22
FI852430A0 (fi)	1985-06-19
FI83225C (fi)	1991-06-10
IL75569A (en)	1989-03-31
AR245731A1 (es)	1994-02-28
CA1239388A (en)	1988-07-19
AU582754B2 (en)	1989-04-13
ES8707737A1 (es)	1987-08-16
PT80663A (en)	1985-07-01
FI83225B (fi)	1991-02-28
FI852430L (fi)	1985-12-22
AR242036A1 (es)	1993-02-26
HUT38367A (en)	1986-05-28
HU192232B (en)	1987-05-28
NO165496B (no)	1990-11-12
PT80663B (en)	1987-05-08
IE58050B1 (en)	1993-06-16
ES8704967A1 (es)	1987-04-16
AU4397185A (en)	1986-01-02
GR851499B (mo)	1985-11-25
NO852501L (no)	1985-12-23

Legal Events

Date	Code	Title	Description
2001-12-27	B1	Patent granted (law 1993)
2004-02-02	PBP	Patent lapsed	Country of ref document: DK

Publication	Publication Date	Title
EP0122232B1 (de)	1988-12-14	20-Spiroxane und Analoge mit geöffnetem Ring E, Verfahren zu ihrer Herstellung, sowie pharmazeutische Präparate davon
US4129564A (en)	1978-12-12	Spirolactones
US4670551A (en)	1987-06-02	Epoxy steroids
IE851284L (en)	1985-11-30	1,24-dihydroxy-delta(22)-vitamin d3
JPS59139400A (ja)	1984-08-10	抗アルドステロン活性ステロイド誘導体
SK135195A3 (en)	1996-03-06	Crystaline spirostalnylglycosidal, its monohydrate pharmaceutical agent on its base and method of production of crystaline steroid glycoside
WO1986004900A1 (fr)	1986-08-28	SPIROLACTONE 1alpha.7alpha-DITHIO SUBSTITUEES, PROCEDE POUR LEUR PREPARATION ET LEUR UTILISATION COMME MEDICAMENT
EP0644891B1 (en)	1998-04-22	Antihypercholesterolemic compounds and related pharmaceutical compositions and methods of use
JPH0212480B2 (mo)	1990-03-20
WO2007025780A2 (en)	2007-03-08	Aldosterone receptor antagonists
US4331663A (en)	1982-05-25	4α,5α-Epoxy-3,20-dioxopregnane-2α,16α-dicarbonitrile and intermediates and process for preparation, method of use and compositions thereof
Rosenheim et al.	1941	The metabolism of β-sitosterol
JPS59205400A (ja)	1984-11-20	２０−スピロキサン系ステロイド及びその製造方法並びに該ステロイドを含有する医薬
SU1079177A3 (ru)	1984-03-07	Способ получени производных стероидспирооксатиазолидинов в виде их стереоизомеров или их смесей или их солей
DE3344057A1 (de)	1984-06-14	Eine neue lactonverbindung und pharmazeutische zusammensetzungen davon, sowie verfahren zu ihrer herstellung
US3591583A (en)	1971-07-06	Steroidal lactones
Johns	1969	3-Deoxy-16-haloestra-1, 3, 5 (10)-trienes
Shaw et al.	1964	Steroidal Thiazenones and Related Compounds1
BE859336A (fr)	1978-04-04	Procede de preparation de nouveaux composes steroidiques ayant une fonction oxygene en position 19
CZ583989A3 (cs)	1996-09-11	Deriváty 5-methyl-19-nor-5Beta-pregn-9-enu a způsobjejich přípravy
IL30879A (en)	1972-11-28	4-oxa-androstanes and process for the manufacture thereof