公开(公告)号：WO1995008997A1

公开(公告)日：1995-04-06

申请号：PCT/US1994011132

申请日：1994-09-29

Applicant: GLAXO INC. ,  SIRGO, Mark, Alan

Inventor： GLAXO INC.

IPC: A61K33/10

CPC classification number: A61K33/10 ,  A61K31/34 ,  A61K2300/00

Abstract: A pharmaceutical composition for gastrointestinal conditions comprising ranitidine and calcium carbonate.

Abstract translation: 包含雷尼替丁和碳酸钙的胃肠道药物组合物。

公开(公告)号：WO1994000119A1

公开(公告)日：1994-01-06

申请号：PCT/US1993006212

申请日：1993-06-28

Applicant: GLAXO INC. ,  MCELROY, Andrew, B. ,  BROWN, Peter, J. ,  DREWRY, David, H. ,  SALOVICH, James, M. ,  SCHOENEN, Frank, J.

Inventor： GLAXO INC.

IPC: A61K31/40

CPC classification number: C07D209/48 ,  C07C237/06 ,  C07D209/66 ,  C07D213/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04 ,  C07F7/1804

Abstract: Aminobutanoic acids of formula (I) where R -R are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).

Abstract translation: 式（I）的氨基丁酸，其中R 1 -R 5是各种取代基，新型中间体，用于治疗炎症性疾病，脱髓鞘疾病和肿瘤转移的药物组合物，这种治疗方法和制备化合物的方法 的式（I）化合物。

公开(公告)号：WO1991015447A1

公开(公告)日：1991-10-17

申请号：PCT/US1991002352

申请日：1991-04-04

Applicant: GLAXO INC.

Inventor： GLAXO INC. ,  LACKEY, John, William ,  MOOK, Robert, Anthony, Jr. ,  PARTRIDGE, John, Joseph

IPC: C07C35/06

CPC classification number: C07D473/00 ,  C07C35/06 ,  C07C69/96 ,  C07C201/10 ,  C07C201/12 ,  C07C2601/10 ,  C07C205/18 ,  C07C205/41

Abstract: This invention relates to a new process for preparing certain optically active purine substituted cyclopentene derivatives including the antiviral agent, carbovir, and novel intermediates used in this process. In particular, this invention concerns a synthesis of (1R-cis)-4-hydroxymethyl-2-cyclopenten-1-ol, an intermediate in this process.

公开(公告)号：WO1995012533A1

公开(公告)日：1995-05-11

申请号：PCT/US1994012551

申请日：1994-11-01

Applicant: GLAXO INC. ,  BARGER, Lee, Allen ,  BOWYER, Terence, George, Henry ,  BRITTO, Ignatius, Loy ,  FRANKLIN, Michael, Leon

Inventor： GLAXO INC.

IPC: B65D83/54

CPC classification number: B65D83/54

Abstract: The present invention relates to an aerosol dispensing apparatus (1), more particularly to aerosol dispensing valves incorporating a controlled metered dispensing function wherein the metering chamber (7) holding the next aerosolized dose is in fluidic communication with the reservoir (3) allowing homogenous mixing of the next aerosolized dose to be dispensed.

Abstract translation: 气雾剂分配装置技术领域本发明涉及一种气溶胶分配装置（1），更具体地涉及包含受控计量分配功能的气溶胶分配阀，其中保持下一个雾化剂量的计量室（7）与储存器（3）流体连通，允许均匀混合 将要分配的下一个雾化剂量。

公开(公告)号：WO1994011377A2

公开(公告)日：1994-05-26

申请号：PCT/US1993010987

申请日：1993-11-10

Applicant: GLAXO INC. ,  BESTERMAN, Jeffrey, Mark ,  EVANS, Michael, Glenn ,  LACKEY, Karen, Elizabeth ,  LUZZIO, Michael, Joseph ,  PEEL, Michael, Robert ,  STERNBACH, Daniel, David

Inventor： GLAXO INC.

IPC: C07D491/22

CPC classification number: C07D317/66 ,  C07D319/18

Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein A represents a moiety of formula (IIA), (IIB) or (IIC), X is selected from the group consisting of alkyl, aryl, (CH2)mOR , (CH2)mSR and (CH2)mNR R wherein m is an integer of 0 to 6, and R and R are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.

Abstract translation: 本发明涉及式（I）的水溶性喜树碱衍生物，其中A表示式（IIA），（IIB）或（IIC）的部分，X选自烷基，芳基，（CH 2） mOR 1，（CH2）mSR 1和（CH2）mNR 1 R 2其中m是0-6的整数，R 1和R 2是氢，低级烷基， 芳基或与氮一起形成5-7元环; q为0〜2的整数; n表示整数1或2; p为1〜6的整数。 Y和W选自烷基，芳基，烷氧基，芳氧基和氨基，Q是氧或硫; 磷是磷; J表示完成5或6元芳环所必需的原子; 及其药学上可接受的盐; 它们用作拓扑异构酶抑制剂，它们的制备; 并用于治疗癌症。

公开(公告)号：WO1994004210A1

公开(公告)日：1994-03-03

申请号：PCT/US1993007312

申请日：1993-08-04

Applicant: GLAXO INC. ,  EVANS, Rix, Earl

Inventor： GLAXO INC.

IPC: A61M15/00

CPC classification number: A61M15/0065 ,  A61M2202/064

Abstract: A breath actuated dry powder medicament inhaler (10) has a primary air passageway (14) therethrough defining a venturi (14c) in the medial portion thereof. A second air passageway (16) is provided which contains a compound deaggregating swirl chamber (16c) and is fluidly connected to the venturi (14c). A dry powder storage chamber (18) and cooperatively associated metering plate (18b) act to introduce a predetermined amount of compound into the swirl chamber upon actuation of the metering plate. The primary air passageway (14) is configured within the inhalator apparatus so as to create an optimized air flow trajectory through the mouth of the user to minimize dry powder compound impingement upon the outside radius of the throat.

Abstract translation: 呼吸致动的干粉药物吸入器（10）具有穿过其中间部分限定文丘里管（14c）的一次空气通路（14）。 提供了第二空气通道（16），其包含复合解聚涡旋室（16c）并且流体地连接到文丘里管（14c）。 干粉存储室（18）和配合关联的计量板（18b）用于在计量板致动时将预定量的化合物引入涡流室。 主空气通道（14）构造在吸入器装置内，以便通过使用者的口产生优化的空气流动轨迹，以使干粉混合物撞击在喉部的外半径上。

公开(公告)号：WO1992012981A1

公开(公告)日：1992-08-06

申请号：PCT/US1992000581

申请日：1992-01-24

Applicant: GLAXO INC.

Inventor： GLAXO INC. ,  LUZZIO, Michael, J. ,  BESTERMAN, Jeffrey, M. ,  EVANS, Michael, G. ,  ROSS, Johnson, M.

IPC: C07D491/056

CPC classification number: C07D491/04

Abstract: The present invention relates to the compounds of formula (I), wherein: R1 is hydrogen, hydroxy or amino; R2 is hydrogen, hydroxy, methoxy or methoxymethoxy; R3 is hydrogen, hydroxy, amino, methoxy, methoxymethoxy or, taken together with R2, methylenedioxy (also known as 1,3 dioxolo); R4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C¿1-4?)alkylaminomethyl or, taken together with R?3¿, methylenedioxy; R5 is hydrogen or hydroxy; provided that at least one of R1 through R5 is other than hydrogen; and i) X2 is hydroxy or methoxy with X?1, X3 and X4¿ being hydrogen or ii) X1 taken together with X2, X2 taken together with X3 or X3 taken together with X4, is methylenedioxy, provided that each of the remaining respective X?1, X2, X3 and X4¿ substituents are hydrogen, intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

公开(公告)号：WO1995007927A1

公开(公告)日：1995-03-23

申请号：PCT/US1994010530

申请日：1994-09-16

Applicant: GLAXO INC. ,  BATCHELOR, Kenneth, William ,  FRYE, Stephen, Vernon

Inventor： GLAXO INC.

IPC: C07J73/00

CPC classification number: C07J3/005 ,  C07C235/82 ,  C07C2603/14 ,  C07J41/0066 ,  C07J73/005

Abstract: The present invention relates to the compound of formula (I), also known as 17 beta -N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5 alpha -androst-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.

Abstract translation: 本发明涉及式（I）化合物，也称为17β-N-（2,5-双（三氟甲基））苯基氨基甲酰基-4-氮杂-5α-雄甾-1-烯-3-酮， 其溶剂化物，其制备方法，其制备中使用的中间体，其药物制剂及其在治疗雄激素反应性和介导性疾病中的用途。

公开(公告)号：WO1994014833A2

公开(公告)日：1994-07-07

申请号：PCT/US1993012419

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： GLAXO INC.

IPC: C07J03/00

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 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R and R i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R and R 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 R and R is a single bond; R is preferably hydrogen, halogen or lower alkyl, R is preferably hydrogen or lower alkyl, X is preferably CH2, Y is preferably hydrogen and Z is preferably CONR R and R and R are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.

Abstract translation: 本发明涉及式（I）的某些取代的17β-取代的羰基-6-氮杂雄甾-4-烯-3-酮，其中R 1和R 2独立地是氢或低级烷基， 带有R 1和R 2的碳之间的键是单键或双键，或ii）一起形成环丙烷环的-CH 2 - 基团，并且具有R 1和 R 2是单键; R 3优选为氢，卤素或低级烷基，R 4优选为氢或低级烷基，X优选为CH 2，Y优选为氢，Z优选为CONR 14 R 15和R 14， 和R 15是各种有机基团及其药学上可接受的盐，制剂，医疗用途和药物制剂。

公开(公告)号：WO1992005822A1

公开(公告)日：1992-04-16

申请号：PCT/US1991007078

申请日：1991-09-26

Applicant: GLAXO INC.

Inventor： GLAXO INC. ,  CASPER, Robert, A. ,  McCARTNEY, Michael, L. ,  JOCHEM, Warren, J. ,  PARR, Alan, F.

IPC: A61M11/00

CPC classification number: A61B5/42 ,  A61B5/073 ,  A61B10/0045 ,  A61B2010/0061 ,  A61F2210/0023

Abstract: A medical capsule device (10) for releasing and/or collecting a substance at a defined location in the gastrointestinal tract. The device has a capsule body (12) defining one or more apertures in the circumferential wall thereof and a sleeve valve rotatably positioned therein having one or more corresponding apertures in the circumferential wall thereof. The sleeve valve comprises a coil and electrically connected heatable resistor which are operatively associated with an actuator member (16J, 16I) formed of a shape memory alloy responsive to heat and which will move from a non-heated first shape to a heated second shape. Actuator stop means (20) are provided in the capsule body for being engaged by the actuator member during movement from the non-heated first shape to the heated second shape so that the actuator member movement will serve to rotate the sleeve valve to either an open or closed position.