公开(公告)号：US3776902A

公开(公告)日：1973-12-04

申请号：US3776902D

申请日：1972-09-01

Applicant: ROUSSEL UCLAF

Inventor： GASC J ,  PIERDET A

IPC: C07J1/00 ,  A61K20060101 ,  A61K31/565 ,  A61K31/57 ,  A61K31/575 ,  C07C20060101 ,  C07J7/00 ,  C07J9/00 ,  C07J13/00 ,  C07J51/00 ,  C07J71/00 ,  C07C169/08 ,  C07C173/00

Abstract: NOVEL 11B-ALKOXY-$1,3,5,(10)-ESTRATRIENES OF THE FORMULA

3-(R1-O-),11-(X-O-),16-(R3-O-),17-R,17-(R2-O-)ESTRA-1,3,

5-TRIENE

WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF METHYL AND ETHYL, R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND UNSATURATED HYDROCARBON OF 2 TO 4 CARBON ATOMS, R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS, WHEN R IS HYDROGEN AND R2 IS WITH R3, WHEN OR2 AND OR3 HAVE THE SAME SPATIAL CONFIGURATION, AN ALKYLIDENE OR ARALKYLIDENE IN THE FORM OF

>C(-A)-B

WHEREIN A IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND HYDROCARBON AND B IS A HYDROCARBON AND R3 MAY ALSO BE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND THE WAVY LINES MEAN THAT THE SUBSTITUENT MAY BE IN THE A OR B CONFIGURATION HAVING INTENSE UTEOTROPHIC AND ESTROGENIC ACTIVITY AND VERY INTENSE ANTIGONADOTROPHIC ACTIVITY AND THEIR PREPARATION.

公开(公告)号：US3803132A

公开(公告)日：1974-04-09

申请号：US33040773

申请日：1973-02-07

Applicant: ROUSSEL UCLAF

Inventor： PIERDET A

IPC: C07J71/00 ,  C07C173/10

CPC classification number: C07J71/0047

Abstract: 21 - M - SULFOBENZOATES OF 6,16A-DIMETHYL-2''-PHENYL-& 2,4,6-PREGNATRIENEOLO (3,2-C) - PYRAZOL-11B,17,21-TRIOL-20ONE OF THE FORMULA

1-((3-(R-O3S-)PHENYL)-COO-CH2-CO-),1,11-DI(HO-),2,5,10A,

12A-TETRA(CH3-),7-PHENYL-1,2,3,3A,3B,7,10,10A,10B,11,12,

12A-DODECAHYDROCYCLOPENTA(7,8)PHENANTHRO(2,3-C)PYRAZOLE

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKALI METAL USEFUL AS ANTI-INFLAMMATORY AGENTS HAVING PROLONGED ACTIVITY AND THEIR PREPARATION.

公开(公告)号：US3790564A

公开(公告)日：1974-02-05

申请号：US3790564D

申请日：1972-08-15

Applicant: ROUSSEL UCLAF

Inventor： PIERDET A ,  AZADIAN G

IPC: C07J1/00 ,  A61K20060101 ,  A61K31/565 ,  A61P5/00 ,  C07C20060101 ,  C07D20060101 ,  C07J51/00 ,  C07C173/00

CPC classification number: C07J1/0096 ,  Y10S514/843

Abstract: ETHYNYLATED TRIENIC STEROIDS HAVING THE FORMULA

3-(O=),13-R,16,17-DI(HO-),17-(HC*C-)-1,2,3,6,7,8,13,14,

15,16-DECAHYDRO-17H-CYCLOPENTA(A)PHENANTHRENE

WHEREIN R REPRESENTS ALKYL HAVING 1 YO 3 CARBON ATOMS AND THE -OH IN THE 16 POSITION IS SELECTED FROM THE GROUP CONSISTING OF THE A-OH AND THE B-OH; AS WELL AS PROCESS FOR THE PREPARATION OF THE COMPOUNDS, INTERMEDIATES IN THE PROCESS, THERAPEUTIC COMPOSITIONS CONTAINING THE COMPOUNDS AND THE METHOD OF PREVENTING PREGNACY IN WARM-BLOODED ANIMALS BY ADMINISTRATION OF THE COMPOUNDS.

公开(公告)号：US3818056A

公开(公告)日：1974-06-18

申请号：US25921872

申请日：1972-06-02

Applicant: ROUSSEL UCLAF

Inventor： PIERDET A ,  BONNE C

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

CPC classification number: C07J1/007 ,  C07J1/0096

Abstract: WHEREIN R is alkyl having one to three carbon atoms, X represents a member selected from the group consisting of hydrogen, aliphatic hydrocarbon having one to six carbon atoms, halogenated aliphatic hydrocarbon having one to six carbon atoms, and cycloalkyl having three to six carbon atoms, Y is alkyl having one to six carbon atoms, Z represents a member selected from the group consisting of hydrogen, alkyl having one to six carbon atoms and phenyl alkyl having seven to nine carbon atoms, and R'' represents a member selected from the group consisting of hydrogen and the acyl of an organic carboxylic acid having from one to 18 carbon atoms; as well as a process for preparing the compounds, therapeutic compositions and methods. The 11 Alpha alkoxylated steroids possess anti-estrogenic, anti-gonadotrophic and exogenic anti-androgenic activity.

11 Alpha -ALKOXYLATED STEROIDS HAVING THE FORMULA

Abstract translation: 11具有式的α-羟基化甾族化合物R是具有1至3个碳原子的烷基，X表示选自氢，具有1-6个碳原子的脂族烃，具有1-6个碳原子的卤代脂族烃， 和具有3至6个碳原子的环烷基，Y是具有1至6个碳原子的烷基，Z表示选自氢，具有1至6个碳原子的烷基和具有7至9个碳原子的苯基烷基的成员，R “表示选自氢和具有1至18个碳原子的有机羧酸的酰基的成员; 以及制备化合物的方法，治疗组合物和方法。 11种α-烷氧基化甾族化合物具有抗雌激素，抗促性腺激素和外源性抗雄激素活性。

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：US3755574A

公开(公告)日：1973-08-28

申请号：US3755574D

申请日：1971-01-21

Applicant: ROUSSEL UCLAF

Inventor： BERTIN D ,  PIERDET A

IPC: A61K31/567 ,  A61K17/00

CPC classification number: A61K31/567

Abstract: NOVEL 11B-LOWER ALKOXY-$1,3,5(10)-GONATRIENS SUBSTITUTED IN THE 3-POSITIONS BY A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, ALKOXY OF 1 TO 4 CARBON ATOMS, CYCLOALKOXY OF 5 TO 6 CARBOM ATOMS, AND ACYLOXY, WHEREIN THE ACYL IS DERIVED FROM AN ORGANIC CARBOXYLIC ACID HAVING 1 TO 10 CARBOM ATOMS, IN THE 13-POSITION BY A LOWER ALKYL RADICAL, AND IN THE 17-POSITION BY THE GROUPING

(X-O-),(Y--)

WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL OF 1 TO 4 CARBON ATOMS, AND Y IS SELECTED FROM THE GROUP CONSISTING OF A HYDROCARBON RADICAL AND A SUBSTITUTED HYDROCARBON RADICAL. THESE COMPOUNDS POSSESS ESTROGENIC ACTIVITY.

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：US3721685A

公开(公告)日：1973-03-20

申请号：US3721685D

申请日：1971-03-01

Applicant: ROUSSEL UCLAF

Inventor： JOLLY J ,  PIERDET A

IPC: C07D295/215 ,  C07C169/34

CPC classification number: C07D295/215 ,  Y10S514/842 ,  Y10S514/843

Abstract: 13B-R-17A-METHYL-18,19-DINOR$4,9-PREGNADIENES OF THE FORMULA

17-(H3C-),17-(R''-O-CH(-CH3)-),18-R-4,9-GONADIEN-3-ONE

WHEREIN R IS ALKYL OF 1 TO 4 CARBON ATOMS AND R'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS HAVING ANTI-OVULATORY ACTIVITY AND THEIR PREPARATON AND INTERMEDIATES THEREOF.