公开(公告)号：US3549671A

公开(公告)日：1970-12-22

申请号：US3549671D

申请日：1968-04-02

申请人： SCHERING AG

发明人： LAURENT HENRY ,  HOFMEISTER HELMUT ,  NEUMANN FRIEDMUND ,  WIECHERT RUDOLF

IPC分类号： A61K31/57 ,  C07C20060101 ,  C07J7/00 ,  C07J53/00 ,  C07C169/32

CPC分类号： C07J7/00 ,  C07J53/00 ,  Y10S514/843

公开(公告)号：US3894004A

公开(公告)日：1975-07-08

申请号：US42660073

申请日：1973-12-20

申请人： SCHERING AG

发明人： HOFMEISTER HELMUT ,  LAURENT HENRY ,  PREZEWOWSKY KLAUS ,  WIECHERT RUDOLF ,  MENGEL KLAUS ,  WENDT HANS

IPC分类号： C07J7/00 ,  C07J13/00 ,  C07J31/00 ,  C07J41/00 ,  C07J71/00 ,  C07C173/00

CPC分类号： C07J7/006 ,  C07J13/005 ,  C07J31/003 ,  C07J41/005 ,  C07J71/001 ,  C07J71/0089

摘要： Topical anti-inflamatory 11-oxygenated pregneno(17,16 Alpha -d)1'', 3''-oxathiolanes of the formula I
wherein R1 and R2, can be the same or different and are a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkyl containing hetero atoms, aryl, or heteroacyl; R1 and R2 together can be a (CH2)n bridge which can also contain hetero atoms, and wherein n has the values of 2-6; R3 represents a hydrogen or fluorine atom, or an alkyl; X is a hydrogen, fluorine, or chlorine atom; Y is an oxygen atom or the group

WHEREIN R4 represents a hydrogen atom or an acyl; and C1 .... C2 represents a single or double bond between the C-1 and C-2 carbon atoms. This invention also comprises the process of producing the compounds by condensation of 16 Beta -hydroxy-17 Alpha mercaptopregnenes with carbonyl compounds under epimerization of the substituent at the C-16 carbon atom.

摘要翻译： 式I的局部抗炎性11-氧化孕烯[17,16α-d] -1'，3'-氧硫杂环戊烷，其中R 1和R 2可以相同或不同，并且是氢原子，烷基，环烷基 ，含有杂原子，芳基或杂酰基的环烷基; R1和R2可以是也可以含有杂原子的（CH 2）n桥，其中n具有2-6的值; R3表示氢或氟原子，或烷基; X是氢，氟或氯原子; Y是氧原子或基团R 4代表氢原子或酰基; C 1 -C 2表示C 1和​​C 2的碳原子之间的单键或双键。 本发明还包括通过在C-16碳原子上的取代基的差向异构化下将16β-羟基-17α-己内酯与羰基化合物缩合制备化合物的方法。

公开(公告)号：US3919421A

公开(公告)日：1975-11-11

申请号：US42670273

申请日：1973-12-20

申请人： SCHERING AG

发明人： LAURENT HENRY ,  WIECHERT RUDOLF ,  HOFMEISTER HELMUT ,  MENGEL KLAUS ,  WENDT HANS ,  ANNEN KLAUS

IPC分类号： C07J5/00 ,  C07J71/00 ,  C01B7/00

CPC分类号： C07J5/0092 ,  C07J71/0031

摘要： Pharmacologically active pregnanoic acid derivatives of the Formula I

wherein -A-B- is -CH2-CH2-, -CH CH-, or -CCl CH-; X is a hydrogen atom, a halogen atom, or methyl; -Y-Z- is -CH-CH2-, C CH-, -CV-CHOU-, -CV-CO-, -CW-CHW''-, wherein U is a hydrogen atom or acyl, V is a hydrogen atom or a halogen atom, and W and W'' each are a halogen atom; R1 is alkyl; R2 is alkyl or aryl; or, R1 and R2 together represent a tetramethylene group or pentamethylene group; R3 is a hydrogen atom, an alkali metal atom, or a hydrocarbon. The invention also comprises the process of producing the compounds by various procedures.

摘要翻译： 其中-A-B-是-CH 2 -CH 2 - ， - CH = CH-或-CCl = CH-的式I的药理学活性孕酸衍生物; X是氢原子，卤素原子或甲基; -YZ-是-CH-CH2-，-C = CH-，-CV-CHOU-，-CV-CO-，-CW-CHW'-，其中U是氢原子或酰基，V是氢原子或 卤素原子，W和W'各自为卤素原子; R1是烷基; R2是烷基或芳基; 或者R1和R2一起表示四亚甲基或五亚甲基; R3是氢原子，碱金属原子或烃。

公开(公告)号：US3906095A

公开(公告)日：1975-09-16

申请号：US45941274

申请日：1974-04-09

申请人： SCHERING AG

发明人： LAURENT HENRY ,  WIECHERT RUDOLF ,  PREZEWOWSKY KLAUS ,  HOFMEISTER HELMUT ,  GERHARDS ERICH ,  KOLB KARL HEINZ ,  MENGEL KLAUS

IPC分类号： A61K31/573 ,  A61K17/00

CPC分类号： A61K31/573

摘要： Pregnanoic acid derivatives of the formula

WHEREIN X is hydrogen, halogen, or methyl; Y is hydrogen or halogen; Z is hydroxy or halogen having an atomic weight no greater than Y; R1 is hydrogen or methyl; R2 is hydrogen, alkali metal or saturated or unsaturated hydrocarbon of 1-18 carbon atoms which is unsubstituted or substituted by hydroxy, halo, alkoxy, carboxy, carbalkoxy, amino, alkylamino, dialkylamino, nitro or sulfate, wherein alkyl in each instance contains 1-4 carbon atoms; and -A-B- is -CH CH-; -CCl CH- or, when at least one of X, Y and R1 is other than hydrogen, -CH2-CH2; possess pronounced topical anti-inflammatory activity.

摘要翻译： 式WHEREIN X的孕酸衍生物是氢，卤素或甲基; Y是氢或卤素; Z是原子量不大于Y的羟基或卤素; R1是氢或甲基; R2是未取代或被羟基，卤素，烷氧基，羧基，烷氧基，氨基，烷基氨基，二烷基氨基，硝基或硫酸取代的1-18个碳原子的氢，碱金属或饱和或不饱和烃，其中烷基各自含有1个 -4个碳原子; 和-A-B-是-CH = CH-; -CCl = CH-或当X，Y和R 1中的至少一个不是氢时，-CH 2 -CH 2; 具有明显的局部抗炎活性。

公开(公告)号：US3562259A

公开(公告)日：1971-02-09

申请号：US3562259D

申请日：1968-12-03

申请人： SCHERING AG

发明人： HOFMEISTER HELMUT ,  STEINBECK HERMANN ,  WIECHERT RUDOLF

IPC分类号： A61K20060101 ,  C07C169/18

CPC分类号： C07J75/00 ,  Y02P20/55

摘要： 4-CHLORO-7-BETA-METHYL-1-ALPHA, 2-ALPH-METHYLENE4-PREGNENE OR ANDROSTENE-3-ONE COMPOUNDS WHICH MAY ALSO BE SUBSTITUTED BY HYDROXY OR OXY IN THE 11-POSITION AND MAY HAVE VARIOUS SUBSTITUENTS IN THE 17-POSITION INCLUDING ALSO THE CORRESPONDING DELTA4,6-7-METHYL COMPOUNDS. THE COMPOUNDS ARE USEFUL FOR TREATMENT OF GYNECOLOGICAL COMPLAINTS. THE COMPOUNDS ARE MADE BY REACTING A CORRESPONDING STEROID WHICH IS 6-BETA, 7-BETA-METHYLENE SUBSTITUTED WITH A HALOGEN ACID FOLLOWED BY REDUCTION TO REMOVE THE HALOGEN FROM THE 7-BETA-HALOGEN-METHYL GROUP AND FOLLOWED FURTHER IF DESIRED BY DEHYDROGENATION TO FORM A 6-7 DOUBLE BOND.