公开(公告)号：WO1992000107A1

公开(公告)日：1992-01-09

申请号：PCT/US1991004715

申请日：1991-06-27

Applicant: GLAXO INC. ,  JOHNSON, Keith, A.

Inventor： GLAXO INC.

IPC: A61L09/04

CPC classification number: A61K9/008

Abstract: Aerosol formulations comprising an inhalation drug, 1,1,1,2-tetrafluoroethane (P134a) and a surface active agent soluble in 1,1,1,2-tetrafluoroethane.

公开(公告)号：WO1995008534A1

公开(公告)日：1995-03-30

申请号：PCT/US1994010678

申请日：1994-09-20

Applicant: GLAXO INC. ,  FELDMAN, Paul, Lawrence ,  STAFFORD, Jeffrey, Alan

Inventor： GLAXO INC.

IPC: C07D207/16

CPC classification number: C07D207/08 ,  C07D207/10 ,  C07D207/14 ,  C07D207/16

Abstract: Novel pyrrolidine compounds of formula (I) which are useful for inhibiting the function of Type IV phosphodiesterase (PDE-IV) as wll 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.

Abstract translation: 公开了用于抑制作为其制备方法的IV型磷酸二酯酶（PDE-IV）的功能的式（I）的新型吡咯烷化合物。 还公开了治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统（CNS）病症的应用。

公开(公告)号：WO1995007926A1

公开(公告)日：1995-03-23

申请号：PCT/US1994010479

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 compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R is hydrogen or methyl; R is hydrogen or methyl; R is (A) or (B) wherein X, W, Z, R , R , R , R and R are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

Abstract translation: 本发明涉及式（I）化合物，其中碳1和2通过单键或双键连接; R 1是氢或甲基; R 2是氢或甲基; R 3为（A）或（B）其中X，W，Z，R 4，R 5，R 6，R 7和R 8为各种基团， 溶剂化物及其用于治疗雄激素反应性和介导性疾病的用途。

公开(公告)号：WO1994024151A1

公开(公告)日：1994-10-27

申请号：PCT/EP1994001130

申请日：1994-04-13

Applicant: GLAXO INC. ,  FINCH, Harry ,  SHAH, Pritom ,  CARR, Robin, Arthur

Inventor： GLAXO INC.

IPC: C07K05/06

CPC classification number: C07K5/0821 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0207 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0827

Abstract: Compounds of general formula (I) and physiologically acceptable salts thereof wherein the group NR1R2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R3 is C1-6alkyl, C3-6cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R4 is phenyl or phenyl substituted by one or two groups selected from halogen, C1-4alkyl, trifluoromethyl, trifluoromethoxy or (CH2)nR5 wherein n is zero or 1 and R5 represents C1-4alkoxy, hydroxy, nitro, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4alkyl), tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represents hydrogen, C1-4alkyl or halogen; m is zero, 1 or 2, and p is zero, 1 or 2; processes for their preparation and their use in medicine as antagonists of gastrin and CCK.

Abstract translation: 通式（I）的化合物及其生理上可接受的盐，其中NR1R2基团可以被一个或两个甲基取代的5-7元饱和杂环; R3是C1-6烷基，C3-6环烷基或任选被1或2个卤素原子取代的苯基; R4是苯基或被一个或两个选自卤素，C 1-4烷基，三氟甲基，三氟甲氧基或（CH 2）n R 5基团取代的苯基，其中n是0或1，R 5代表C 1-4烷氧基，羟基，硝基，氰基，CO 2 R 6，S（ O）pCH 3，NR 7 R 8，CONR 7 R 8，SO 2 NR 7 CO（C 1-4烷基），四唑基，羧酰胺基四唑基或3-三氟甲基-1,2,4-三唑基; R6是氢，C1-4烷基或苄基; R7是氢或C1-4烷基，R8是氢，C1-4烷基，SO2CH3或SO2CF3，X代表氢，C1-4烷基或卤素; m为零，1或2，p为零，1或2; 其制备方法及其在医学中的用途，作为胃泌素和CCK的拮抗剂。

公开(公告)号：WO1993013124A1

公开(公告)日：1993-07-08

申请号：PCT/US1992011109

申请日：1992-12-18

Applicant: GLAXO INC. ,  FRYE, Stephen, Vernon ,  CRIBBS, Cynthia, Markert ,  HAFFNER, Curt, Dale ,  MALONEY, Patrick, Reed ,  ANDREWS, Robert, Carl

Inventor： GLAXO INC.

IPC: C07J73/00

CPC classification number: C07J73/005

Abstract: The present invention relates to certain substituted 17 beta -substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) wherein R and R are: i) 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 to form a cyclopropane ring, and the bond between the carbons bearing R and R is a single bond; R is hydrogen; R is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH2)mCO2R , -(CH2)mAr , -(CH2)n'CONR R , -(CH2)n'NR R or -(CH2)n'OR , wherein R is hydrogen, lower alkyl or lower alkenyl; R and R are independly hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar 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; R and R are independently hydrogen or lower alkyl, or taken together R and R form a carbonyl group(=O); R is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR R , wherein R and R are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their 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，特别是其中R 1和R 1的式（I 1）的那些：i ）独立地是氢或低级烷基，并且具有R 1和R 2的碳之间的键是单键或双键，或者ii）一起是-CH 2 - 基团以形成环丙烷环，并且键 在具有R 1和R 2的碳之间是单键; R 3c是氢; R 2是氢，低级烷基，低级环烷基，低级链烯基，2-6个碳原子的烷酰基， - （CH 2）m CO 2 R 16， - （CH 2）mAr a， - （CH 2）n CONR 17 R 18， - （CH 2）n R NR 17或 - （CH 2）n'OR 16，其中R 16是氢，低级烷基或低级烯基; R 17和R 18独立地是氢，低级烷基低级环烷基或低级烯基; Ar a是6〜12个碳的芳香族基团; n'为0或1〜5的整数; m为1〜5的整数; R 19和R 20独立地为氢或低级烷基，或一起R 19和R 20形成羰基（= O）; R 5c是低级烷基，低级烯基，低级环烷基，低级烷氧基或NR 21 R 22，其中R 21和R 22独立地是氢，低级烷基或低级烯基; 及其药学上可接受的盐，它们的制备，医疗用途和药物制剂。

公开(公告)号：WO1992017183A1

公开(公告)日：1992-10-15

申请号：PCT/US1992001948

申请日：1992-03-09

Applicant: GLAXO INC.

Inventor： GLAXO INC. ,  ROBERT, Marshall, Day ,  CHARLES, Edward, Holland ,  GEORGE, Edward, Van, Lear

IPC: A61K31/56

CPC classification number: B65D35/22 ,  A61K31/415 ,  A61K31/56 ,  Y10S514/867 ,  A61K2300/00

Abstract: A sequential dosing medicament for topical treatment of fungal infections comprising a first pharmaceutical composition having an antifungal agent and an antiinflammatory agent, e.g. a steroid, a second separate pharmaceutical composition having only an antifungal agent as the active ingredient. Also, a method for such sequential dosing, particularly using oxiconazole as the antifungal agent and fluticasone as the steroid.

公开(公告)号：WO1994024149A1

公开(公告)日：1994-10-27

申请号：PCT/EP1994001131

申请日：1994-04-14

Applicant: GLAXO INC. ,  SUGG, Elizabeth, Ellen ,  AQUINO, Christopher, Joseph ,  SZEWCZYK, Jerzy, Ryszard ,  FINCH, Harry ,  CARR, Robin, Arthur, Ellis

Inventor： GLAXO INC.

IPC: C07K05/02

CPC classification number: C07K5/0821 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0207 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0827

Abstract: Novel benzodiazepine compounds of formula (1) which exhibit agonistic activity for CCK-A receptors enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulation of appetite, the treatment of obesity and the maintenance of weight loss.

Abstract translation: 具有对CCK-A受体具有激动作用的式（1）的新型苯并二氮杂类化合物，使得它们可以调节哺乳动物中的激素胃泌素和缩胆囊素（CCK），用于医学中作为食欲调节剂，食欲调节，肥胖症和 维持体重减轻。

公开(公告)号：WO1993020956A1

公开(公告)日：1993-10-28

申请号：PCT/US1993003620

申请日：1993-04-19

Applicant: GLAXO INC. ,  EVANS, Rix, Earl ,  FLOWERS, Alec, Parker, Jr. ,  HOCKADAY, David, Erwin ,  LOAR, David, Wayne ,  PROCTOR, James, Kenneth

Inventor： GLAXO INC.

IPC: B07C05/16

CPC classification number: A61M15/0065 ,  G01F1/68 ,  G01F25/0092

Abstract: The present invention comprises a method for measuring the amount, i.e., mass, of a volatile liquid which comprises passing the mass (18) over a heat loss measuring device (6, 8), calculating the amount of heat loss accompanying the vaporization of the mass and correlating the heat loss to measurement of heat loss of known liquid aerosol mass made with the same device. The method is especially useful in assuring uniform metered doses among multiple aerosol containers (12).

公开(公告)号：WO1993012129A1

公开(公告)日：1993-06-24

申请号：PCT/US1992010921

申请日：1992-12-17

Applicant: GLAXO INC. ,  THOMSON, Stephen, A. ,  NOBLE, Stewart, A. ,  RICCA, Daniel, J.

Inventor： GLAXO INC.

IPC: C07H19/06

CPC classification number: C07K14/003 ,  A61K38/00 ,  C08G69/10

Abstract: Peptide nucleic acids oligomers of formula (I) wherein n is 1 or more, particularly about 5-20 and B is independently one of the 4 nucleoside bases or their equivalents, Q and J are end groups useful in anti-sense oligomers and their use in affecting genetic material, e.g. as triplex or antisense in the treatment of disease.

Abstract translation: 式（I）的肽核酸低聚物，其中n为1或更多，特别是约5-20，B独立地为4个核苷碱基或其等同物之一，Q和J为可用于反义寡聚体的端基及其用途 影响遗传物质，例如 作为治疗疾病的三重或反义。

公开(公告)号：WO1992021661A1

公开(公告)日：1992-12-10

申请号：PCT/US1992004611

申请日：1992-05-28

Applicant: GLAXO INC.

Inventor： GLAXO INC. ,  LUZZIO, Michael, J. ,  BESTERMAN, Jeffrey, M. ,  EVANS, Michael, G. ,  JOHNSON, M., Ross ,  DEZUBE, Milana ,  PROFETA, Salvatore, Jr.

IPC: C07D221/18

CPC classification number: C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/14

Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (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, -OCONH¿2?, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R?2 or R4¿, methylenedioxy or ethylenedioxy; R4 is hydrogen, hydroxy or amino; Z is -CH¿2?-, -O- or -NH-; and a) X?1¿ 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 etylenedioxy, and X1 is hydrogen or a pharmaceutically acceptable salt thereof provided that: i) at least one of R1 through R4 is other than hydrogen; ii) when R1 is methoxy, R2 is hydroxy or methoxy, R3 is hydrogen or methoxy and R4 is hydrogen; iii) when R2 is hydroxy, methoxy or amino, R3 is hydrogen, hydroxy or methoxy, and R4 is hydrogen; iv) when R4 is hydroxy or amino, R?1 and R3¿ are hydrogen and R2 is hydroxy or amino; and v) when R1 is fluoro, chloro, iodo or amino, R2 is hydrogen, hydroxy or methoxy, R3 is hydrogen, hydroxy or methoxy and R4 is hydrogen and the use of these compounds as topoisomerase inhibitors and antitumor agents.