公开(公告)号：WO9414833A3

公开(公告)日：1994-09-29

申请号：PCT/US9312419

申请日：1993-12-17

Applicant: GLAXO INC ,  ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K31/58 ,  A61K20060101 ,  A61P37/08 ,  C07C20060101 ,  C07C211/41 ,  C07C211/45 ,  C07D309/14 ,  C07D317/58 ,  C07D335/02 ,  C07J20060101 ,  C07J3/00 ,  C07J63/00 ,  C07J73/00 ,  C07J75/00 ,  C07C211/40 ,  C07C211/52

CPC classification number: C07D317/58 ,  C07C211/41 ,  C07C211/45 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/46 ,  C07D309/14 ,  C07D335/02 ,  C07J73/005

Abstract: The present invention relates to certain substituted 17β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R?1 and R2¿ i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R?1 and R2¿ is a single or a double bond, or ii) taken together are a -CH¿2?- group forming a cyclopropane ring, and the bond between the carbons bearing R?1 and R2¿ is a single bond; R3 is preferably hydrogen, halogen or lower alkyl, R4 is preferably hydrogen or lower alkyl, X is preferably CH¿2?, Y is preferably hydrogen and Z is preferably CONR?14R15 and R14 and R15¿ are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.

公开(公告)号：AU3417493A

公开(公告)日：1993-07-28

申请号：AU3417493

申请日：1992-12-18

Applicant: GLAXO INC

Inventor： FRYE STEPHEN VERNON ,  CRIBBS CYNTHIA MARKERT ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED ,  ANDREWS ROBERT CARL

IPC: A61K8/63 ,  A61K8/00 ,  A61K8/49 ,  A61K31/565 ,  A61K31/58 ,  A61Q5/00 ,  A61Q19/00 ,  C07D221/18 ,  C07J41/00 ,  C07J63/00 ,  C07J73/00

Abstract: PCT No. PCT/US92/11109 Sec. 371 Date Aug. 15, 1994 Sec. 102(e) Date Aug. 15, 1994 PCT Filed Dec. 18, 1992 PCT Pub. No. WO/9313124 PCT Pub. Date Jul. 8, 1993The present invention relates to certain substituted 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) (I) (IG) wherein R1 and R2 are i) independently hydrogen or lower alkyl and the bond between the carbons bearing R1 and R2 is a single or a double bond, or ii) taken together are a -CH2- group to form a cyclopropane ring, and the bond between the carbons bearing R1 and R2 is a single bond; R3c is hydrogen; R4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH2)mCO2R16, -(CH2)mAra, -(CH2)n'CONR17R18, -(CH2)n'NR17R18 or -(CH2)n'OR16, wherein R16 is hydrogen, lower alkyl or lower alkenyl; R17 and R18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ara is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R19 and R20 are independently hydrogen or lower alkyl, or taken together R19 and R20 form a carbonyl group (=O); R5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR21R22, wherein R21 and R22 are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.

公开(公告)号：ZA9309455B

公开(公告)日：1994-08-09

申请号：ZA9309455

申请日：1993-12-17

Applicant: GLAXO INC

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K20060101 ,  C07C20060101 ,  C07J20060101 ,  C07J ,  A61K ,  C07C

公开(公告)号：ZA929826B

公开(公告)日：1993-09-08

申请号：ZA929826

申请日：1992-12-18

Applicant: GLAXO INC

Inventor： FRYE STEPHEN VERNON ,  CRIBBS CYNTHIA MARKET ,  MALONEY PATRICK REED ,  ANDREWS ROBERT CARL ,  HAFFNER CURT DALE

IPC: A61K20060101 ,  C07J20060101 ,  C07J ,  A61K

公开(公告)号：ZA939455B

公开(公告)日：1994-08-09

申请号：ZA939455

申请日：1993-12-17

Applicant: GLAXO INC

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K20060101 ,  C07C20060101 ,  C07J20060101 ,  C07J ,  A61K ,  C07C

公开(公告)号：ZA9209826B

公开(公告)日：1993-09-08

申请号：ZA929826

申请日：1992-12-18

Applicant: GLAXO INC

Inventor： FRYE STEPHEN VERNON ,  CRIBBS CYNTHIA MARKET ,  MALONEY PATRICK REED ,  ANDREWS ROBERT CARL ,  HAFFNER CURT DALE

IPC: A61K20060101 ,  C07J20060101 ,  C07J ,  A61K

公开(公告)号：SI9300665A

公开(公告)日：1994-06-30

申请号：SI9300665

申请日：1993-12-17

Applicant: GLAXO INC

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K31/58 ,  A61K20060101 ,  A61P37/08 ,  C07C20060101 ,  C07C211/41 ,  C07C211/45 ,  C07D309/14 ,  C07D317/58 ,  C07D335/02 ,  C07J20060101 ,  C07J3/00 ,  C07J63/00 ,  C07J73/00 ,  C07J75/00

公开(公告)号：IS4106A

公开(公告)日：1994-06-19

申请号：IS4106

申请日：1993-12-15

Applicant: GLAXO INC

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K31/58 ,  A61K20060101 ,  A61P37/08 ,  C07C20060101 ,  C07C211/41 ,  C07C211/45 ,  C07D309/14 ,  C07D317/58 ,  C07D335/02 ,  C07J20060101 ,  C07J3/00 ,  C07J63/00 ,  C07J73/00 ,  C07J75/00 ,  C07C211/33 ,  C07C211/43

公开(公告)号：MX9308015A

公开(公告)日：1994-08-31

申请号：MX9308015

申请日：1993-12-15

Applicant: GLAXO INC

Inventor： HAFFNER CURT DALE ,  MALONEY PATRICK REED ,  ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON

IPC: A61K31/58 ,  A61K20060101 ,  A61P37/08 ,  C07C20060101 ,  C07C211/41 ,  C07C211/45 ,  C07D309/14 ,  C07D317/58 ,  C07D335/02 ,  C07J20060101 ,  C07J3/00 ,  C07J63/00 ,  C07J73/00 ,  C07J75/00 ,  C07C49/603

公开(公告)号：CA2152053A1

公开(公告)日：1994-07-07

申请号：CA2152053

申请日：1993-12-17

Applicant: GLAXO INC

Inventor： ANDREWS ROBERT CARL ,  CRIBBS CYNTHIA MARKERT ,  FRYE STEPHEN VERNON ,  HAFFNER CURT DALE ,  MALONEY PATRICK REED

IPC: A61K31/58 ,  A61K20060101 ,  A61P37/08 ,  C07C20060101 ,  C07C211/41 ,  C07C211/45 ,  C07D309/14 ,  C07D317/58 ,  C07D335/02 ,  C07J20060101 ,  C07J3/00 ,  C07J63/00 ,  C07J73/00 ,  C07J75/00 ,  C07C211/40 ,  C07C211/52

Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I). wherein R1 and R2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R1 and R2 is a single or a double bond, or ii) taken together are a -CH2- group forming a cyclopropane ring, and the bond between the carbons bearing R1 and R2 is a single bond; R3 is preferably hydrogen, halogen or lower alkyl, R4 is preferably hydrogen or lower alkyl, X is preferably CH2, Y is preferably hydrogen and Z is preferably CONR14R15 and R14 and R15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.