公开(公告)号：US3810887A

公开(公告)日：1974-05-14

申请号：US20156471

申请日：1971-11-23

Applicant: ROUSSEL UCLAF

Inventor： SALMON J ,  BUCOURT R ,  PIERDET A

IPC: A61K31/565 ,  C07C20060101 ,  C07J1/00 ,  C07C169/08 ,  C07C173/00

CPC classification number: C07J1/0092 ,  C07J1/0096

Abstract: 11B-ALKOXY-$4-GONENES OF THE FORMULA

6-Y,7-Y'',11-(X-O-),13-R,17-(R2-O-),17-R1-GON-4-EN-3-ONE

WHEREIN R AND X ARE ALKYL OF 1 TO 4 CARBON ATOMS, R1 IS A SATURATED OR UNSATURATED HYDROCARBON OF 1 TO 6 CARBON ATOMS, R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND Y AND Y'' ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND METHYL AND THE ENOLIC ESTERS THEREOF WITH AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS WHICH POSESS ANTI-ANDROGENIC AND ANTIESTROGENIC ACTIVITY, THEIR PREPARATION AND NOVEL INTERMEDIATES.

公开(公告)号：US3766248A

公开(公告)日：1973-10-16

申请号：US3766248D

申请日：1970-03-09

Applicant: ROUSSEL UCLAF

Inventor： NEDELEC L ,  BUCOURT R

IPC: C07D295/096 ,  C07D295/116 ,  C07D311/94 ,  C07J73/00 ,  C07C49/38 ,  C07C69/24 ,  C07C69/78

CPC classification number: C07D295/096 ,  C07C2603/16 ,  C07D295/116 ,  C07D311/94 ,  C07J73/003

Abstract: THIS INVENTION RELATES TO NOVEL SUBSTITUTED TRICYCLIC COMPOUNDS OF THE FORMULA

3-(X-O-),3A-R,7-(O=),6-(HO-CH2-)-1,2,7,8,9,9A-HEXAHYDRO-

3H-BENZ(E)INDENE

WHEREIN R IS ALKYL HAVING FROM 1 TO 6 CARBON ATOMS, X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL HAVING FROM 1 TO 5 CARBON ATOMS, ALKENYL HAVING FROM 3 TO 5 CARBON ATOMS, ALKOXYALKYL HAVING FROM 2 TO 5 CARBON ATOMS, ARALKYL HAVING FROM 7 TO 11 CARBON ATOMS, CYCLOALKYLALKYL HAVING FROM 4 TO 11 CARBON ATOMS, ALKYLTHIOALKYL HAVING FROM 2 TO 5 CARBON ATOMS, CYCLOALKYL HAVING FROM 4 TO 7 CARBON ATOMS, AND THE ACYL OF AN ORGANIC CARBOXYLIC ACID HAVING FROM 1 TO 18 CARBON ATOMS, AS WELL AS THE PROCES OF PREPARING THE SAME. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF 2-OXA STEROIDS OF THE FORMULA

3-(O=),13-R,17-(X-O-)-2-OXAESTRA-4,9,11-TRIENE

WHICH HAVE AN ANABOLIC ACTION COUPLED WITH AN ANDROGENIC ACTION.

公开(公告)号：US3770725A

公开(公告)日：1973-11-06

申请号：US3770725D

申请日：1972-05-31

Applicant: ROUSSEL UCLAF

Inventor： GASC J ,  BUCOURT R

IPC: C07J21/00 ,  C07J41/00 ,  C07J43/00 ,  C07C169/22

CPC classification number: C07J21/006 ,  C07J41/0094 ,  C07J43/003

Abstract: 17B-CYANO STEROIDS HAVING THE FORMULA

3-(O=),17-NC,13-R-ESTR-4-ENE WHERE A IS BETWEEN C9 AND

C10, AND B IS BETWEEN C11 AND C12

WHEREIN R IS ALKYL HAVING 1 TO 3 CARBON ATOMS, A IS SELECTED FROM THE GROUP CONSISTING OF TWO HYDROGENS AND A DOUBLE BOND AND B IS SELECTED FROM THE GROUP CONSISTING OF TWO HYDROGENS AND A DOUBLE BOND, WITH THE PROVISO THAT WHEN B IS A DOUBLE BOND, A IS A DOUBLE BOND, AS WELL AS THEIR PROCESS OF PREPARATION AND THERAPEUTIC COMPOSITIONS AND METHODS. THE 17-B CYANO STEROIDS POSSESS A PROGESTOMIMETIC ACTIVITY, AN ANTI-ESTROGENIC ACTIVITY AND AN EXOGENIC ANTI-ANDROGENIC ACTIVITY.

公开(公告)号：US3719691A

公开(公告)日：1973-03-06

申请号：US3719691D

申请日：1970-07-27

Applicant: ROUSSEL UCLAF

Inventor： BUCOURT R ,  NEDELEC L ,  GASC J

IPC: A61K31/567 ,  C07J1/00 ,  C07C167/14

CPC classification number: A61K31/567 ,  C07J1/00

Abstract: A novel process for the preparation of 7 Alpha -methyl-13 Beta R-17 Alpha -X-17 Beta -OY- Delta 4,9,11-gonatriene-3-ones of the formula

WHEREIN R is lower alkyl of one to four carbon atoms, X is saturated or unsaturated, substituted or unsubstituted, straight or branched aliphatic hydrocarbon of one to four carbon atoms and Y is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of one to 18 carbon atoms and novel intermediates formed therein.

公开(公告)号：US3818054A

公开(公告)日：1974-06-18

申请号：US31016972

申请日：1972-11-28

Applicant: ROUSSEL UCLAF

Inventor： BUCOURT R ,  PIERDET A

IPC: C07J7/00 ,  A61K31/57 ,  C07C20060101 ,  C07C169/34

CPC classification number: C07J75/00

Abstract: Novel 7 Alpha -methyl-13 Beta -alkyl-18,19-dinor- Delta 4,9,11pregnatrienes of the formula

WHEREIN R is alkyl of one to three carbon atoms and R'' is selected from the group consisting of hydrogen, alkyl of one to three carbon atoms and OR'''' wherein R'''' is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of one to 18 carbon atoms having very intense antiandrogenic activity without manifesting antihypophysical properties with LH predominance to weak degree and to novel process and intermediates.

Abstract translation: 新型7α-甲基-13β-烷基-18,19-二 - -TATA 4,9,11-孕三烯，其式为WHEREIN R为1至3个碳原子的烷基，R'选自氢， 一个至三个碳原子的烷基和OR“，其中R”选自氢和具有非常强的抗雄激素活性的1至18个碳原子的有机羧酸的酰基，而没有表现出LH优于弱的抗液相物性 程度和新颖的工艺和中间体。

公开(公告)号：US3810885A

公开(公告)日：1974-05-14

申请号：US18648371

申请日：1971-10-04

Applicant: ROUSSEL UCLAF

Inventor： BUCOURT R ,  PIERDET A ,  GASC J ,  NEDELEC L

IPC: A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  C07J1/00 ,  C07J41/00 ,  G03B27/62 ,  C07C173/00

CPC classification number: A61K31/567 ,  A61K31/565 ,  A61K31/566 ,  C07J1/00 ,  C07J41/0016 ,  G03B27/62

Abstract: NOVEL 12B-ALKYL-$4.9-GONADIENES OF THE FORMULA

12-X,13-R,17-(R1=)-GONA-4,9-DIEN-3-ONE

AND 12-ALKYL:$4.9.11-GONATREIENES OF THE FORMULA

12-X,13-R,17-(R1=)-GONA-4,9,11-TRIEN-3-ONE

WHEREIN R IS ALKYL OF 1 TO 3 CARBON ATOMS, X IS ALKYL OF 1 TO 3 CARBON ATOMS AND R1 IS SELECTED FROM THE GROUP CONSISTING OF

(R2-O-),(H-); (R2-O-),(R3-); AND (HO-),(R3-)

WHEREIN R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROCARBYL OF 1 TO 10 CARBON ATOMS AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND R3 IS SELECTED FROM THE GROUP CONSISTING OF SATURATED HYDROCARBON OF 1 TO 6 CARBON ATOMS AND UNSATURATED HYDROCARBON OF 2 TO 6 CARBON ATOMS WHICH COMPOUNDS POSESS HORMONAL PROPERTIES AND TO TWO NOVEL PROCESSES FOR THEIR PREPARATION AND NOVEL INTERMEDIATES THEREFOR.

公开(公告)号：US3752855A

公开(公告)日：1973-08-14

申请号：US3752855D

申请日：1971-02-03

Applicant: ROUSSEL UCLAF

Inventor： BUCOURT R ,  NEDELEC L

IPC: C07D295/096 ,  C07D295/116 ,  C07J73/00 ,  C07C49/00

CPC classification number: C07D295/096 ,  C07C2603/16 ,  C07D295/116 ,  C07J73/003

Abstract: 2 - OXA - 13B - R-17A-METHYL-$4,9,11-GONATRIENES OF THE FORMULA

3-(O=),17-(R''-O-),17-CH3-ESTRA-4,9,11-TRIENE WHERE C2

IS O AND C18 IS R

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF METHYL AND ETHYL AND R'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, SATURATED ALKYL OF 1 TO 5 CARBON ATOMS WHICH MAY CONTAIN A HETERO OXYGEN ATOM, UNSATURATED ALKYL OF 2 TO 5 CARBON ATOMS, CYCLOALKYL OF 3 TO 5 CARBON ATOMS WHICH MAY CONTAIN A HETERO OXYGEN ATOM, WITH THE PROVISO THAT R IS ETHYL WHEN R'' IS HYDROGEN WHICH COMPOUNDS POSSESS ANABOLIC AND ANDROGENIC ACTIVITY. THE INVENTION ALSO RELATES TO A NOVEL PROCESS AND NOVEL INTERMEDIATES FOR THE PREPARATION OF THE COMPOUNDS OF FORMULA I.