公开(公告)号：US3518296A

公开(公告)日：1970-06-30

申请号：US3518296D

申请日：1964-04-22

Applicant: ROUSSEL UCLAF

Inventor： BUCOURT ROBERT ,  PIERDET ANDRE ,  COSTEROUSSE GERMAIN ,  HAINAUT DANIEL ,  JOLY ROBERT ,  WARNANT JULIEN ,  GOFFINET BERNARD

IPC: C07C45/67 ,  C07C69/74

CPC classification number: C07C45/676

公开(公告)号：US3499913A

公开(公告)日：1970-03-10

申请号：US3499913D

申请日：1968-01-03

Applicant: ROUSSEL UCLAF

Inventor： JOLY ROBERT ,  WARNANT JULIEN ,  JOLLY JEAN

IPC: C07J73/00 ,  C07D101/00 ,  C07C167/02 ,  C07C169/10

CPC classification number: C07J73/003

公开(公告)号：US3897417A

公开(公告)日：1975-07-29

申请号：US43860174

申请日：1974-02-01

Applicant: ROUSSEL UCLAF

Inventor： WARNANT JULIEN ,  JOLLY JEAN

IPC: C07J31/00 ,  A61K31/585 ,  A61P7/10 ,  C07J21/00 ,  C07C173/00

CPC classification number: C07J21/00

Abstract: WHEREIN R is alkyl having 1 to 4 carbon atoms and R2 is defined above, with a thioalkanoic acid of the formula

WHEREIN R1 is a linear alkyl having 1 to 4 carbon atoms and R2 is hydrogen or methyl comprising the steps reacting a compound of the formula
The present invention relates to a process for the preparation of steroidal spirolactones having the formula

Abstract translation: 本发明涉及一种制备具有下式的甾族六酮的方法：其中R 1是具有1至4个碳原子的直链烷基，R 2是氢或甲基，包括使式WHEREIN R为具有1至 4个碳原子和R 2如上定义，与式R 1 COSH的硫代链烷酸，其中R 1如上定义，在中性介质中加热所得产物并回收所述甾体螺内酯; 以及中间体。

公开(公告)号：US3637770A

公开(公告)日：1972-01-25

申请号：US3637770D

申请日：1969-12-31

Applicant: ROUSSEL UCLAF

Inventor： WARNANT JULIEN ,  JOLLY JEAN ,  JOLY ROBERT

IPC: A41B1/00 ,  A41B3/00 ,  C07J1/00 ,  C07J7/00 ,  C07J41/00 ,  C07J73/00 ,  C07J75/00 ,  C07C169/32

CPC classification number: C07J73/00 ,  C07J1/00 ,  C07J7/00 ,  C07J41/00 ,  C07J75/00

Abstract: A PROCESS FOR THE PRODUCTION OF 16A,17A-DIHYDROXY-19NOR-PROGESTERONE FROM A 3,5-IKETAL OF 4,5-SECO-ESTRANE3,5,17-TRIONE BY 17-CYANATION, 16-DEHYDRATION, METHYLATION, HYDROLYSIS OF THE KETALS, CYCLIZATION OF THE A RING AND HYDROXYLATION OF THE $16 BOND. THE INTERMEDIATES ARE ALSO PART OF THE DISCLOURE.

公开(公告)号：US3424745A

公开(公告)日：1969-01-28

申请号：US45841665

申请日：1965-05-24

Applicant: ROUSSEL UCLAF

Inventor： JOLY ROBERT ,  WARNANT JULIEN ,  JOLLY JEAN ,  PROST-MARECHAL JACQUES ,  BUCOURT ROBERT ,  TESSIER JEAN

IPC: A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  A61K31/57 ,  C07D295/04 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J41/00 ,  C07J75/00 ,  F16B35/06 ,  C07C173/10 ,  C07C169/10 ,  C07C169/34

CPC classification number: C07D295/04 ,  A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  A61K31/57 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J41/00 ,  C07J75/00 ,  F16B35/06

公开(公告)号：US3919198A

公开(公告)日：1975-11-11

申请号：US43860274

申请日：1974-02-01

Applicant: ROUSSEL UCLAF

Inventor： WARNANT JULIEN ,  JOLLY JEAN

IPC: C07D303/32 ,  A61K31/585 ,  A61P7/10 ,  A61P9/00 ,  B01J31/00 ,  C07C20060101 ,  C07D20060101 ,  C07J20060101 ,  C07J1/00 ,  C07J9/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J51/00

Abstract: The present invention relates to a dienic derivative of the androstane series having the formula

WHEREIN R is a member selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms and alkali metal, R'' and R'''' are members selected from the group consisting of 1) hydrogen and -COOM, respectively, where M is alkali metal, and 2) taken together, the divalent

group, R2 is a member selected from the group consisting of hydrogen and methyl, with the proviso when R is hydrogen or alkyl having 1 to 4 carbon atoms, R'' and R'''' together are the divalent

group; as well as their process of preparation.

Abstract translation: 本发明涉及具有式WHEREIN R为选自氢，具有1至4个碳原子的烷基和碱金属的成员，R'和R“为选自以下的成员的雄甾烷系的二烯衍生物： 分别由1）氢和-COOM组成的组，其中M是碱金属，和2）合并在一起，二价-C-PARALLEL O基，R2是选自氢和甲基的成员，条件是 当R为氢或具有1至4个碳原子的烷基时，R'和R“一起为二价-C-PARALLEL O基; 以及他们的准备过程。

公开(公告)号：US3591606A

公开(公告)日：1971-07-06

申请号：US3591606D

申请日：1967-05-23

Applicant: ROUSSEL UCLAF

Inventor： WARNANT JULIEN ,  JOLLY JEAN ,  JOLY ROBERT

IPC: A41B1/00 ,  A41B3/00 ,  C07J1/00 ,  C07J7/00 ,  C07J41/00 ,  C07J73/00 ,  C07J75/00 ,  C07D13/04

CPC classification number: C07J73/00 ,  C07J1/00 ,  C07J7/00 ,  C07J41/00 ,  C07J75/00

Abstract: WHEREIN R" IS LOWER ALKYL AND R"'' IS SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYLENE AND SUBSTITUTED LOWER ALKYLENE; AND A IS SELECTED FROM THE GROUP CONSISTING OF TWO HYDROGENS AND A DOUBLE BOND THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE TOTAL SYNTHESIS OF STEROIDS, PARTICULARLY THOSE HAVING SUBSTITUENTS ON THE 17 CARBON ATOM.

=C(-O-R")2 AND =C
WHREIN R'' REPRESENTS AN ALKYL HAVING FROM 1 TO 4 CARBON ATOMS; X REPRESENTS A MEMBER SELECTED FROM THE GROUP CONSISTING OF

X AND THE 9,11-POSITION IS A

3-(X=),13-R''-GON-4-EN-17-ONE WHERE C-4 IS REPLACED BY

THE PRESENT INVENTON RELATES TO 3,5-DIKETALS OF 4,5SECO-GONANE-3,517-TRIONES OF THE FORMULA

公开(公告)号：US3502682A

公开(公告)日：1970-03-24

申请号：US3502682D

申请日：1969-05-15

Applicant: ROUSSEL UCLAF

Inventor： ALLAIS ANDRE ,  GIRAULT PIERRE ,  JOLY ROBERT ,  WARNANT JULIEN ,  GOFFINET BERNARD

IPC: A61K31/00 ,  A61K31/395 ,  C07D215/44 ,  C07D33/52

CPC classification number: A61K31/00 ,  A61K31/395 ,  C07D215/44

公开(公告)号：US3919267A

公开(公告)日：1975-11-11

申请号：US51738074

申请日：1974-10-23

Applicant: ROUSSEL UCLAF

Inventor： WARNANT JULIEN ,  JOLLY JEAN

IPC: A61K31/56

CPC classification number: Y10S514/859 ,  Y10S514/864

Abstract: HAVING EXCELLENT ANTI-ANDROGENIC ACTIVITY AND PROGESTOMIMETIC AND ANTI-ESTROGENIC ACTIVITY AND ITS PREPARATION.

13 Beta -ETHYL-17 Alpha -METHYL-18,19-DINOR- Delta 4,9PREGNADIENE-3,20-DIONE OF THE FORMULA

Abstract translation: 13具有优异抗发生活性和原始和抗雌激素活性的配方的β-βHYL-17α-甲基-18,19-DINOR- DELTA 4,9-孕酮-3,20-二酮及其制备。

公开(公告)号：US3567732A

公开(公告)日：1971-03-02

申请号：US3567732D

申请日：1968-01-08

Applicant: ROUSSEL UCLAF

Inventor： JOLY ROBERT ,  WARNANT JULIEN ,  GOFFINET BERNARD

IPC: C07D215/18 ,  C07D215/22 ,  C07D215/233 ,  C07D33/14

CPC classification number: C07D215/233 ,  C07D215/18

Abstract: THIS INVENTION RELATES TO A PROCESS FOR THE PREPARATION OF CHLORINATED QUINOLINES OF THE FORMULA

4-CL,CL-QUINOLINE

WHEREIN THE CHLORINE ATTACHED TO THE BENZENE NUCLEUS IS IN A POSITION SELECTED FROM THE GROUP CONSISTING OF THE 5, 6, 7 AND 8 POSITIONS. THE SAID PROCESS INVOLVES REACTING A 2, 3 OR 4-CHLOROANILINE WITH A COMPOUND SELECTED FROM THE GROUP CONSISTING OF B-PROPIOLACTONE AND A COMPOUND OF THE FORMULA

CH2=CH-COOR

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL, CYCLIZING THE 3-(CHLOROANILINO)PROPIONIC ACID FORMED WITH POLYPHOSPHORIC ACID, CHLORINATING THE RESULTING 5, 6, 7 OR 8-CHLORO-4-OXO-1,2,3,4TETRAHYDROQUINOLINE WITH PHOSPHORUS OXYCHLORIDE AND RECOVERING SAID CHLORINATED QUINOLINE. THE DICHLOROQUINOLINES ARE KNOWN PRODUCTS USEFUL AS INTERMEDIATES IN THE PRODUCTION OF KNOWN COMPOUNDS HAVING THERAPEUTIC ACTIVITY.