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1. 发明授权

KR780000156B1 PROCESS FOR PREPARING 150 160-METHYLEN -OESTREN-17-36 失效
公开(公告)号：KR780000156B1
公开(公告)日：1978-05-02
申请号：KR730000246
申请日：1973-02-10
申请人： SCHERING AG
发明人： STEINBECK H , WIECHERT R , ELGER W
IPC分类号： A61K31/565 , A61K31/567 , C07J1/00 , C07J53/00
摘要： 1425636 15,16 - Methylene - estr - 4 - enes SCHERING AG 12 Feb 1973 [11 Feb 1972] 6821/73 Heading C2U [Also in Division A5] Novel steroids of the formula wherein R 1 is C 1-5 alkyl; R 2 is H or acyl; R 3 is H or an optionally substituted aliphatic hydrocarbon group of at most 5 carbon atoms (exclusive of substituents); and X is O or H (OR 4 ) in which OR 4 is in the alpha or beta position and R 4 is H or acyl are prepared from steroids of the formulµ wherein Y is a protected keto group and the dotted lines in the rings indicate the presence of a # 5 - or # 5(10) -double bond and when a # 5(10) - double bond is present then the 10-H atom is absent, by reduction in the 17-position or conversion to a 17α-substituted-17#-ol followed when required, by hydrolysis to a free # 4 -3-one and, if desired, by hydrogenation of a 17α- unsaturated group and/or reduction to a 3-ol and/or acylation of a free OH group. 3,3 - (2 1 ,2 1 - Dimethyl - 1 1 ,3 1 - propylenedioxy)- 18 - methyl - 15α,16α - methylene - # 5 or # 5(10) - estren-17-one is prepared from 3,3-(2 1 ,2 1 -dimethyl - 1 1 ,3 1 - propylenedioxy) - 18 - methyl - 19- nor - # 5,16 or 15(10),16 - pregnadien - 20 - one (prepared from the # 4 -3-one and 2,2-dimethyl-1,3- propane-diol) by oxygenation to give the corresponding # 15 - 17α - ol, reduction of this to the corresponding 20-ol, reaction of this with methylene iodide in the presence of a Zn-Cu couple to give 17α,20# - dihydroxy - 3,3 - (2 1 ,2 1 - dimethyl - 1 1 ,3 1 - propylenedioxy) - 18 - methyl- 15α,16α - methylene - 19 - nor - # 5 - or # 5(10) - pregnene and oxidation of this. 3,3-(2 1 ,2 1 -dimethyl - 1 1 ,3 1 - propylenedioxy) - 15α,16α- methylene - # 5 or 15(10) - estren - 17 - one is prepared similarly via corresponding intermediates. The novel steroids are stated to possess a strong androgenic and anabolic activity or a strong gestagenic activity and they may be made up into pharmaceutical compositions with suitable carriers. The gestagenic compounds can be used, possibly together with estrogens, in contraceptive preparations (see Heading A5B).

2. 发明授权

US3714207A 1 alpha , 2 alpha ; 6 beta , 7 beta -DIMETHYLENE STERIODS 失效
标题翻译： 1个alpha，2个alpha; 6β，7β-二甲苯异构体
公开(公告)号：US3714207A
公开(公告)日：1973-01-30
申请号：US3714207D
申请日：1970-05-01
申请人： SCHERING AG
发明人： WIECHERT R , HOFMEISTER H , STEINBECK H
IPC分类号： A61K31/57 , B01J21/00 , B65D21/02 , C07B61/00 , C07J7/00 , C07J53/00 , C07C169/34
CPC分类号： A61K31/57 , B65D21/02 , C07J7/00 , C07J53/00
摘要： 1 Alpha ,2 Alpha ;6 Beta ,7 Beta -Dimethylene-17 Alpha -oxyprogesterones of the formula

WHEREIN R is H or an acyl radical, have progestational activity without ovulation inhibiting activity.
摘要翻译：具有式WHEREIN R为H或酰基的1α，2α，6β，7β-二亚甲基-17α-氧孕酮具有无排卵抑制活性的促孕活性。

3. 发明授权

US3812165A 18-methyl-5alpha-h-androstane derivatives and process of making the same 失效
标题翻译： 18-甲基-5ALPHA-H-苯并吡喃衍生物及其制备方法
公开(公告)号：US3812165A
公开(公告)日：1974-05-21
申请号：US80115869
申请日：1969-02-20
申请人： SCHERING AG
发明人： BERNDT H , STEINBECK H , WIECHERT R
IPC分类号： A61K31/568 , C07J1/00 , C07C169/22
CPC分类号： A61K31/568 , C07J1/00
摘要： AN ABNDROSTANE DERIVATIVE HAVING THE FORMULA:

17-(R-O-),18-CH3-ANDROSTAN-3-ONE, WHERE A-B ARE CARBONS

1 AND 2,

WHEREIN A-B IS A GROUP SELECTED FROM THE FOLLOWING:

-CH2-CH2-, -CH=CH-, -C(-CH3)=CH- OR -CH(-O-R'')-CH2-

AND R AND R7 ARE THE SAME OR DIFFERENT AND ARE HYDROGEN OR AN ACYL RESIDUE. THE COMPOUNDS HAVE A STRONG ANABOLIC ACTION AND SHOW A GOOD DISSOCIATION OF THE ANABOLIC MAIN ACTION FROM THE UNDESIRED ANDROGENOUS SIDE EFFECT. THE COMPOUNDS ARE MADE BY REDUCING THE 4,5-POSITION OF A $4,1-2-SATURATED CORRESPONDING STEROID AND, IF DESIRED, DEHYDROGENATING THE 1,2-POSITION OR INTRODUCING A METHYL GROUP INTO THE 1-POSITION.

4. 发明授权

US3749742A 15alpha,16alpha-methylene steroids and processes for their production and use 失效
公开(公告)号：US3749742A
公开(公告)日：1973-07-31
申请号：US3749742D
申请日：1972-02-24
申请人： SCHERING AG
发明人： WIECHERT R , STEINBECK H
IPC分类号： C07J7/00 , C07J53/00 , D06F75/14 , C07C169/22
CPC分类号： C07J7/0075 , C07J53/008
摘要： WHEREIN R1 IS A HYDROGEN ATOMS OR SATURATED OR UNSATURATED ALKYL OF 1-4 CARBON ATOMS, AND PHYSIOLOGICALLY ACCEPTABLE 17-ESTERS THEREOF POSSESS HIGH ANDROGENIC ACTIVITY WITH RELATIVELY LOW ANABOLIC ACTIVITY. THEY CAN BE PRODUCED BY OXIDATION OF THE CORRESPONDING $4 AND $5-3-HYDROXYSTEROIDS AND BY ALKYLATION OF THE CORRESPONDING $5-3-ACYLOXY-17-KETO STEROIDS FOLLOWED BY HYDROLYSIS OF THE 3-ACYLOXY GROUP AND OXIDATION OF THE THUS-PRODUCED 3-HYDROXY GROUP.

3-(O=),15,16-(-CH2-),17-R1,17-HO-ANDROST-4-ENE

15A,16A-METHYLENE STEROIDS OF THE FORMULA

5. 发明授权

US3729494A 7alpha-methylandrostenolones 失效
标题翻译： 7ALPHA-甲基吗啉
公开(公告)号：US3729494A
公开(公告)日：1973-04-24
申请号：US3729494D
申请日：1970-12-01
申请人： SCHERING AG
发明人： HOFMEISTER H , STEINBECK H , WIECHERT R
IPC分类号： C07J53/00 , A61K20060101 , A61K31/565 , C07C20060101 , C07J1/00 , C07C169/22
CPC分类号： C07J75/00
摘要： 7A-METHYL-1A,2A-METHYLENE-ANDROSTENOLONES OF THE FORMULA 1,2-(-CH2-),3-(O=),7-(CH3-),17-(R-O-)ANDROST-4-ENE POSSESS ANABOLIC ACTIVITY WITH MINIMAL ASSOCIATED ANDROGENIC ACTIVITY.

6. 发明授权

US3812166A Dichloro-substituted estradiene 失效
标题翻译： DICHLORO取代的ESTRADIENE
公开(公告)号：US3812166A
公开(公告)日：1974-05-21
申请号：US85348069
申请日：1969-08-27
申请人： SCHERING AG
发明人： WIECHERT R , STEINBECK H
IPC分类号： A61K20060101 , A61K31/565 , A61K31/58 , C07C20060101 , C07J1/00 , C07J17/00 , C07C169/22
CPC分类号： C07J75/00
摘要： A RACEMIC OR OPTICALLY ACTIVE, 4,6-DICHLORO-4,6-ESTRADIENE OF THE FORMULA

4,6-DI(CL-),17-(R-O-),17-(CH*C-),18-CH3-ESTRA-4,6-DIEN-

3-ONE

WHEREIN R IS HYDROGEN, ALKYL, TETRADROPYRANYL OR AN ACID RESIDUE. TO FORM THE COMPOUNDS, THE 4-UNSUBSTITUTED 6-CHLOROESTRADIENE IS SUBJECTED TO THE ACTION OF AN AGENT FURNISHING POSITIVE AND NEGATIVE CHLORINE, THEREBY FORMING THE 6,6,7-TRICHLORO-SUBSTITUTED COMPOUND, FOLLOWED BY TREATMENT OF THE LATTER COMPOUND WITH A BASE. THE COMPOUNDS HAVE A VERY HIGH PROGESTERONE ACTIVITY.

7. 发明授权

US3770726A Pregnano717,16alpha-d)-1',3'-oxathiolanes 失效
标题翻译： PREGNANO717,16ALPHA-D）-1'，3'-氧杂双酚
公开(公告)号：US3770726A
公开(公告)日：1973-11-06
申请号：US3770726D
申请日：1972-03-16
申请人： SCHERING AG
发明人： HOFMEISTER H , LAURENT H , PREZEWOWSKY K , WIECHERT R , STEINBECK H
IPC分类号： C07J31/00 , C07J75/00 , C07C169/34 , C07C173/00
CPC分类号： C07J31/00 , C07J75/00
摘要： PREGNANO(17,16A-D)-1'',3''-OXATHIOLANES OF THE FORMULA

3-(O=),1-R,2-R'',6-X,16,17-(-O-C(-R1)(-R2)-S-),20-(O=)-

PREGNA-4,6-DIENE

WHEREIN R1 AND R2 ARE E.G., H, ALKYL, CYCLOALKYL, ARYL OR HETEROARYL, POSSESS LONG ACTING PROGESTIONAL ACTIVITY AND ARE PRODUCED BY THE ACID CATALYZED CONDENSATION OF THE CORRESPONDING 16B-HYDROXY-17A-MERCAPTO STEROIDS WITH A KETONE OR ALDEHYDE UNDER EPIMERIZATION OF THE SUBSTITUENT ON CARBON ATOM C-16.

8. 发明专利

DK115780A 未知
公开(公告)号：DK115780A
公开(公告)日：1980-10-01
申请号：DK115780
申请日：1980-03-18
申请人： SCHERING AG
发明人： HOFMEISTER H , WIECHERT R , ANNEN K , LAURENT H , STEINBECK H
IPC分类号： A61K31/565 , A61P13/02 , A61P15/00 , C07J1/00 , C07J11/00 , C07J21/00 , C07J
摘要： 11-Methylene steroids of Formula I wherein R is hydrogen or acyl, and X is oxygen or two hydrogen atoms have valuable pharmacological properties.

9. 发明专利

SE7803167A 未知
公开(公告)号：SE7803167A
公开(公告)日：1978-09-22
申请号：SE7803167
申请日：1978-03-20
申请人： SCHERING AG
发明人： PETZOLDT K , STEINBECK H , ELGER W
IPC分类号： C12P33/12 , A61K31/57 , A61P17/00 , C07J7/00 , C07J53/00
CPC分类号： C07J53/005

10. 发明专利

DK118878A 未知
公开(公告)号：DK118878A
公开(公告)日：1978-09-22
申请号：DK118878
申请日：1978-03-16
申请人： SCHERING AG
发明人： PETZOLDT K , STEINBECK H , ELGER W
IPC分类号： C12P33/12 , A61K31/57 , A61P17/00 , C07J7/00 , C07J53/00 , C07J
摘要： Steroids of the formula wherein R1 and R2 are identical or different and each is hydrogen or the residue of an organic or inorganic acid, and for the esters (R1 or R2 is not H) capable of salt formation, the salts thereof, possess valuable pharmacoligical properties, e.g., good antiandrogenic activity with low progestational activity.

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