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    Method of stabilizing aerosol formulations
    151.
    发明专利
    Method of stabilizing aerosol formulations 未知

    公开(公告)号：GB2268507A

    公开(公告)日：1994-01-12

    申请号：GB9313579

    申请日：1993-07-01

    Applicant: GLAXO INC

    Inventor： JOHNSON KEITH ARTHUR

    IPC: A61K9/00 ,  A61K9/12 ,  A61K47/30 ,  C09K3/30

    Abstract: A method of making a stabilized aerosol drug formulation is disclosed, along with the formulations so produced and metered drug inhalers containing the same. The method comprises combining a solid particulate drug composition with a fluoropolymer in a liquid fluorocarbon aerosol propellant to form a stable suspension. Further stabilization can be achieved by cooling the suspension for a time and to a temperature sufficient to adsorb the fluoropolymer to the solid particulate drug composition in the liquid fluorocarbon aerosol propellant. Preferred propellants for carrying out the invention are 1,1,1,2-tetrafluoroethane, heptafluoropropane, and mixtures thereof, and preferred fluoropolymers for carrying out the invention are fluoropolyethers.

    METHOD OF STABILIZING AEROSOL FORMULATIONS
    152.
    发明专利
    METHOD OF STABILIZING AEROSOL FORMULATIONS 未知

    公开(公告)号：GB9313579D0

    公开(公告)日：1993-08-18

    申请号：GB9313579

    申请日：1993-07-01

    Applicant: GLAXO INC

    IPC: A61K9/00 ,  A61K9/12 ,  A61K47/30 ,  C09K3/30

    Abstract: A method of making a stabilized aerosol drug formulation is disclosed, along with the formulations so produced and metered drug inhalers containing the same. The method comprises combining a solid particulate drug composition with a fluoropolymer in a liquid fluorocarbon aerosol propellant to form a stable suspension. Further stabilization can be achieved by cooling the suspension for a time and to a temperature sufficient to adsorb the fluoropolymer to the solid particulate drug composition in the liquid fluorocarbon aerosol propellant. Preferred propellants for carrying out the invention are 1,1,1,2-tetrafluoroethane, heptafluoropropane, and mixtures thereof, and preferred fluoropolymers for carrying out the invention are fluoropolyethers.

    154.
    发明专利
    未知

    公开(公告)号：NO924158L

    公开(公告)日：1993-04-30

    申请号：NO924158

    申请日：1992-10-28

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL JOSEPH ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER LESLIE

    IPC: A61K31/435 ,  A61K31/4738 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22

    Abstract: The invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R and R represent independently, hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R represents hydrogen, lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R represents -COR wherein R represents hydrogen, lower alkyl, perhalo-lower alkyl, (C PI 1/2 )cycloalkyl, (C PI 1/2 )cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R and R taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH , NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl groups or; -COR5 wherein R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

    WATER SOLUBLE CAMPTOTHECIN DERIVATIVES
    155.
    发明专利
    WATER SOLUBLE CAMPTOTHECIN DERIVATIVES 未知

    公开(公告)号：CA2081580A1

    公开(公告)日：1993-04-30

    申请号：CA2081580

    申请日：1992-10-28

    Applicant: GLAXO INC

    Inventor： LUZZIO MICHAEL J ,  BESTERMAN JEFFREY M ,  EVANS MICHAEL G ,  MYERS PETER L

    IPC: A61K31/47 ,  A61K31/435 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07D498/22 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54

    Abstract: GLX-76/AC155 WATER SOLUBLE CAMPTOTHECIN DERIVATIVES The invention relates to water soluble, camptothecin derivatives of formula (1), (I) wherein: n represents the integer 1 or 2; and i) R1 and R2 represent independently, hydrogen, lower alkyl, (C3 7)cycloalkyl;(C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; ii) R1 represents hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R2 represents -COR3 wherein R3 represents hydrogen, lower alkyl, perhalo-lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl; or iii) R1 and R2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) wherein: Y represents O, S, CH2, NR4 wherein R4 represents hydrogen, lower alkyl, perhalo-lower alkyl, aryl, aryl substituted with one or more lower alkyl, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy, lower alkoxy lower alkyl groups or; -COR5 wherein R5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups; and the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

    N-PHENYL-N-(4-PIPERIDINYL)AMIDES USEFUL AS ANALGESICS
    156.
    发明专利
    N-PHENYL-N-(4-PIPERIDINYL)AMIDES USEFUL AS ANALGESICS 未知

    公开(公告)号：AU636330B2

    公开(公告)日：1993-04-29

    申请号：AU4973190

    申请日：1990-02-14

    Applicant: GLAXO INC.

    Inventor： PAUL L. FELDMAN ,  MICHAEL K. JAMES ,  MARCUS F. BRACKEEN ,  MICHAEL R. JOHNSON ,  HARRY J. LEIGHTON

    IPC: A61K20060101 ,  A61K31/445 ,  A61K31/4465 ,  A61P25/04 ,  C07B57/00 ,  C07D20060101 ,  C07D211/14 ,  C07D211/58

    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).

    Inhalation device
    157.
    发明专利
    Inhalation device 未知

    公开(公告)号：PH27169A

    公开(公告)日：1993-04-02

    申请号：PH37731

    申请日：1988-10-27

    Applicant: GLAXO INC

    Inventor： PALSON RICHARD CHARLES JULIUS ,  ARMSTRONG JOHN CREIGHTON

    IPC: A61M11/08 ,  A61M15/00

    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.

    CYCLIC ANTITUMOR COMPOUNDS
    158.
    发明专利
    CYCLIC ANTITUMOR COMPOUNDS 未知

    公开(公告)号：AU2178792A

    公开(公告)日：1993-01-08

    申请号：AU2178792

    申请日：1992-05-28

    Applicant: GLAXO INC.

    Inventor： MICHAEL J LUZZIO ,  JEFFREY M BESTERMAN ,  MICHAEL G EVANS ,  M. ROSS JOHNSON ,  MILANA DEZUBE ,  SALVATORE PROFETA JR.

    IPC: C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153

    Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): (I) wherein: R1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino; R2 is hydrogen, hydroxy, methoxy or amino; R3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, -OCONH2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R2 or R4, methylenedioxy or ethylenedioxy; R4 is hydrogen, hydroxy or amino; Z is -CH2-, -O- or -NH-; and a) X1 is hydrogen; X2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X3 is hydrogen or hydroxy; or b) X2 taken together with X3 is methylenedioxy or ethylenedioxy, and X1 is hydrogen or a pharmaceutically acceptable salt thereof provided that: i) at least one of R1 through R4 is other than hydrogen.

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