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公开(公告)号:DE69027794D1
公开(公告)日:1996-08-22
申请号:DE69027794
申请日:1990-02-14
Applicant: GLAXO INC
Inventor: FELDMAN PAUL L , JAMES MICHAEL K , BRACKEEN MARCUS F , JOHNSON MICHAEL ROSS , LEIGHTON HARRY JEFFERSON
IPC: A61K20060101 , A61K31/445 , A61K31/4465 , A61P25/04 , C07B57/00 , C07D20060101 , C07D211/14 , C07D211/58 , C07D211/66
Abstract: N-Phenyl-N-(4-piperdinyl)amide derivatives are disclosed having the general formula (I). wherein: X is a member selected from the group consisting of: alkoxy-carbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxy-carbonyl-lower alkyl, and (C1-2)alkoxy-(C1-2)alkoxy-carbonyl-lower alkyl. Ar is a member selected from the group consisting of phenyl, mono-, di- and tri-substituted phenyl, wherein each subtitutuent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl, and lower alkoxy-lower alkyl; R is a member selected from the group consisting of hydrogen, lower alkoxy-carbonyl, and methoxymethyl; and R is a member selected from the group consisting of hydrogen and methyl; and the diastereomeric and enantiomeric isomers thereof, and the acid addition salts of said compounds and isomers. The compounds exhibit analgesic activity having relatively short durations of analgesic action. The invention embraces the compounds (I), pharmaceutical compositions of (I) and methods of providing analgesia with (I). Also included are certain novel intermediates for making (I).
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公开(公告)号:ZA953056B
公开(公告)日:1996-01-30
申请号:ZA953056
申请日:1995-04-13
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , HENKE BRAD RICHARD , BRACKEEN MARCUS , JEFFS PETER WALTER , SUH EDWARD MARTIN , HIRST GAVIN CHARLES , SUGG ELIZABETH ELLEN , WILLSON TIMOTHY MARK , MOMTAHEN TANYA
IPC: A61K20060101 , C07D20060101 , C07D , A61K
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公开(公告)号:ZA9501374B
公开(公告)日:1996-01-10
申请号:ZA9501374
申请日:1995-02-20
Applicant: GLAXO INC
Inventor: COFFIN MARK DAVIS , PARR ALAN FRANK
IPC: A61K9/24 , A61K31/341 , A61K
CPC classification number: A61K9/209 , A61K31/341 , Y10S514/926
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公开(公告)号:AU2381695A
公开(公告)日:1995-11-29
申请号:AU2381695
申请日:1995-05-02
Applicant: GLAXO INC
Inventor: FANG FRANCIS GERARD , LOWERY MELISSA WILLIAMS , XIE SHIPING
IPC: A62D3/00 , A61K31/00 , A61K31/495 , A61P35/00 , B01J31/28 , C07B61/00 , C07D213/64 , C07D213/69 , C07D213/71 , C07D491/04 , C07D491/052 , C07D491/056 , C07D491/22 , C07D519/00
Abstract: The present invention relates to a method for preparing intermediates useful in the preparation of camptothecin and camptothecin-like compounds and to the intermediates used in this preparation. In particular, the invention provides a process for the preparation of a compound of formula II' wherein X is halogen, which comprises reacting a compound of formula III with a compound of formula IX'
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125.
公开(公告)号:IL113366D0
公开(公告)日:1995-07-31
申请号:IL11336695
申请日:1995-04-13
Applicant: GLAXO INC
IPC: A61K31/55 , A61P1/00 , A61P1/16 , A61P3/04 , C07D243/12 , C07D401/04 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D498/04 , C07D
Abstract: PCT No. PCT/EP95/01336 Sec. 371 Date Nov. 14, 1996 Sec. 102(e) Date Nov. 14, 1996 PCT Filed Apr. 13, 1995 PCT Pub. No. WO95/28391 PCT Pub. Date Oct. 26, 1995 (I) Benzo[b][1,4]diazepine compounds of formula (I), where R1 is selected from C1C6alkyl, C3-C6cycloalkyl, phenyl, or substituted phenyl; R2 is selected from C3-C6alkyl, C3C6cycloalkyl, C3-C6alkenyl, benzyl, phenylC1-C3alkyl of substituted phenyl; or NR1R2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C1-6alkyl C1-6alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R3, R5, and R6 are independently hydrogen or C1-6alkyl; R4 is C1-6alkyl or C1-6alkenyl; R7 is selected from the group consisting of hydrogen, C1-6alkyl, C1-6cycloalkyl, C1-6alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR6R7 together form a saturated 5,6, or 7 membered ring optionally interrupted by 1,2,3 or 4 N, S or O heteroatoms, with the proviso that any two O or S atoms are not bonded to each other, m is an integer selected from the group of 0, 1, 2, 3 or 4; R8 and R9 are selected from a variety of substituents; Z is hydrogen or halogen; novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).
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公开(公告)号:FI94593B
公开(公告)日:1995-06-30
申请号:FI884493
申请日:1988-09-30
Applicant: GLAXO INC
Abstract: A device for dispensing an aerosol from an aerosol module A includes a cocking device comprising lever 36 and spring 60 for readying it for release of the pressurized aerosol, a sear 64 for retaining the cocking device in a non-operative position following readying and a vane 79 operable by inhalation on the part of a user to disable the sear to thus release the cocking device to effect expulsion of aerosol from the aerosol module.
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公开(公告)号:ZA9407119B
公开(公告)日:1995-05-26
申请号:ZA9407119
申请日:1994-09-15
Applicant: GLAXO INC
Inventor: BATCHELOR KENNETH WILLIAM , FRYE STEPHEN VERNON
IPC: A61K31/58 , A61K31/56 , A61P43/00 , C07C235/82 , C07J3/00 , C07J41/00 , C07J73/00 , C07J , A61K , C07C
CPC classification number: C07J3/005 , C07C235/82 , C07C2603/14 , C07J41/0066 , C07J73/005
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公开(公告)号:ZA9407118B
公开(公告)日:1995-05-26
申请号:ZA9407118
申请日:1994-09-15
Applicant: GLAXO INC
Inventor: BATCHELOR KENNETH WILLIAM , FRYE STEPHEN VERNON
IPC: A61K31/58 , A61K31/56 , A61P43/00 , C07C235/82 , C07J3/00 , C07J41/00 , C07J73/00 , C07J , A61K , C07C
CPC classification number: C07J3/005 , C07C235/82 , C07C2603/14 , C07J41/0066 , C07J73/005
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130.
公开(公告)号:AU7839694A
公开(公告)日:1995-04-10
申请号:AU7839694
申请日:1994-09-20
Applicant: GLAXO INC
Inventor: FELDMAN PAUL LAWRENCE , STAFFORD JEFFREY ALAN
IPC: C07D403/06 , A61K31/40 , A61K31/4025 , A61K31/415 , A61P25/00 , A61P29/00 , A61P43/00 , C07D207/08 , C07D207/10 , C07D207/14 , C07D207/16 , C07D405/06
Abstract: Novel pyrrolidine compounds which are useful for inhibiting the function of Type IV phosphodiesterase (PDE-IV) as well as methods for making the same are disclosed. Applications in treating inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, are also disclosed.
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