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1. 发明授权

US5082835A Novel steroid diols, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：新型甾体糊剂，含有它们的药物组合物及其制备方法
公开(公告)号：US5082835A
公开(公告)日：1992-01-21
申请号：US491683
申请日：1990-03-09
申请人： Csaba Molnar , Gyorgy Hajos , Laszlo Szporny , Jozsef Toth , Arpad Kiraly , Anna Boor nee Mezei , Janos Csorgei , Kristina Szekely , Lilla Forgacs , Gyorgy Fekete , Bulcsu Herenyi , Sandor Holly , Jozsef Szunyog
发明人： Csaba Molnar , Gyorgy Hajos , Laszlo Szporny , Jozsef Toth , Arpad Kiraly , Anna Boor nee Mezei , Janos Csorgei , Kristina Szekely , Lilla Forgacs , Gyorgy Fekete , Bulcsu Herenyi , Sandor Holly , Jozsef Szunyog
IPC分类号： A61K31/57 , A61P29/00 , C07J5/00 , C07J13/00
CPC分类号： C07J5/0092 , C07J13/005
摘要： The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen, hydroxyl or trifluoroacetoxy group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group; and represents a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.

2. 发明授权

US5053404A Novel steroid derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：新型甾体衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5053404A
公开(公告)日：1991-10-01
申请号：US491682
申请日：1990-03-09
申请人： Csaba Molnar , Gyorgy Hajos , Laszlo Szporny , Jozsef Toth , Arpad Kiraly , Anna Boor nee Mezei , Janos Csorgei , Kristina Szekely , Lilla Forgacs , Gyorgy Fekete , Bulcsu Herenyi , Sandor Holly , Jozsef Szunyog
发明人： Csaba Molnar , Gyorgy Hajos , Laszlo Szporny , Jozsef Toth , Arpad Kiraly , Anna Boor nee Mezei , Janos Csorgei , Kristina Szekely , Lilla Forgacs , Gyorgy Fekete , Bulcsu Herenyi , Sandor Holly , Jozsef Szunyog
IPC分类号： A61K31/58 , A61P29/00 , C07J7/00 , C07J71/00
CPC分类号： C07J71/0031 , C07J7/008
摘要： The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen or hydroxyl group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group;R.sup.1 and R.sup.2, which are the same or different, stand for hydrogen or a C.sub.1-4 alkyl group; or one of R.sup.1 and R.sup.2 is hydrogen and the other is phenyl group; or R.sup.1 and R.sup.2 together form a C.sub.4-5 alkylene group;means a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.

3. 发明申请

US20090187032A1 INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17alpha-ACETOXY-11beta-[4-(N,N-DIMETHYL-AMINO)-PHENYL]-19-NORPREGNA-4,9-DIENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS 有权
公开(公告)号：US20090187032A1
公开(公告)日：2009-07-23
申请号：US12303160
申请日：2007-05-18
申请人： Lajosne Dancsi , Gyorgy Visky , Zoltan Tuba , Janos Csorgei , Csaba Molnar , Endrene Magyari
发明人： Lajosne Dancsi , Gyorgy Visky , Zoltan Tuba , Janos Csorgei , Csaba Molnar , Endrene Magyari
IPC分类号： C07J3/00 , C07D317/72
CPC分类号： C07J21/006 , C07J31/006 , C07J41/0083 , C07J71/001
摘要： The present invention relates to a new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.The process according to the invention is the following:i) 3-(ethylene-dioxy)-estra-5(10),9(11)-diene-17-one of formula (X) is reacted with potassium acetilyde formed in situ in dry tetrahydrofuran by known method,ii) the obtained 3-(ethylene-dioxy)-17α-ethynyl-17β-hydroxy-estra-5(10),9(11)-diene of formula (IX) is reacted with phenylsulfenyl chloride in dichloromethane in the presence of triethylamine and acetic acid,iii) the obtained isomeric mixture of 3-(ethylene-dioxy)-21-(phenyl-sulfinyl)-19-norpregna-5(10),9(11),17(20),20-tetraene of formula (VIII) is reacted first with sodium methoxide in methanol, then with trimethyl phosphite,iv) the obtained 3-(ethylene-dioxy)-17α-hydroxy-20-methoxy-19-norpregna-5(10),9(11),20-triene of formula (VII) is reacted with hydrogen chloride in methanol, thenv) the obtained 3-(ethylene-dioxy)-17α-hydroxy-19-norpregna-5(10),9(11)-diene-20-one of formula (VI) is reacted with ethylene glycol in dichloromethane in the presence of trimethyl orthoformate and p-toluenesulfonic acid by known method,vi) the obtained 3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-19-norpregna-5(10),9(11)-diene of formula (V) is reacted with hydrogen peroxide in a mixture of pyridine and dichloromethane in the presence of hexachloroacetone by known method,vii) the obtained 3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-5,10-epoxy-19-norpregn-9(11)-ene of formula (IV), containing approximately a 1:1 mixture of 5α,10α- and 5β,10β-epoxides, is isolated from the solution and reacted with a Grignard reagent obtained from 4-bromo-N,N-dimethyl-aniline in tetrahydrofuran in the presence of copper(I) chloride catalyst without separation of the isomers by known method,viii) the obtained 3,3,20,20-bis(ethylene-dioxy)-5α,17α-dihydroxy-11β-[4-(N,N-dimethylamino)-phenyl]-19-norpregn-9(11)-ene of formula (III) is reacted with potassium hydrogensulfate in water by known method,ix) the obtained 11β-[4-(N,N-dimethylamino)-phenyl]-17α-hydroxy-19-norpregn-4,9-diene-3,20-dione of formula (II) is acetylated with acetic anhydride in the presence of perchloric acid by known method, finallyx) the solvate-free compound of formula (I) is liberated from the obtained solvate containing compound of formula (I) in a 1:1 mixture of ethanol and water at 70° C.

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