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：WO1994025466A1

公开(公告)日：1994-11-10

申请号：PCT/US1994004681

申请日：1994-04-28

Applicant: GLAXO, INC. ,  BESTERMAN, Jeffrey, Mark ,  EVANS, Michael, Glenn ,  LUZZIO, Michael, Joseph ,  MYERS, Peter, Leslie

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: n represents the integer 1 or 2; and i) R represents: hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkyl, lower alkoxy lower alkyl or (CH2)tAr wherein: t is 0 to 5 and Ar represents phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl, with one or more substituents independently selected from hydroxy, methoxy, halogen, and amino; and R represents: diphenylmethyl or (CH2)tAr; or ii) R1 and R2 taken together with the linking nitrogen represent: N-tetrahydroquinolyl or N-tetrahydroisoquinolyl; and the pharmaceutically acceptable salts and solvates thereof, their use in the treatment of tumors and methods of their preparation.

Abstract translation: 本发明涉及式（I）的水溶性喜树碱衍生物，其中：n表示整数1或2; 和（i）R 1表示：氢，低级烷基，（C 3-7）环烷基，（C 3-7）环烷基低级烷基，低级烯基，羟基低级烷基，氨基低级烷基，低级烷基氨基低级烷基，氨基低级烷基， 低级烷氧基低级烷基或（CH2）tAr其中：t为0至5，Ar表示苯基，呋喃基，吡啶基，N-甲基吡咯基，咪唑基; 或苯基，呋喃基，吡啶基，N-甲基吡咯基，咪唑基，其中一个或多个取代基独立地选自羟基，甲氧基，卤素和氨基; 和R 2代表：二苯基甲基或（CH 2）t Ar; 或ii）R 1和R 2与连接氮一起代表：N-四氢喹啉基或N-四氢异喹啉基; 及其药学上可接受的盐和溶剂合物，它们在治疗肿瘤中的用途及其制备方法。

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：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：WO9411377A3

公开(公告)日：1994-08-04

申请号：PCT/US9310987

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： BESTERMAN JEFFREY MARK ,  EVANS MICHAEL GLENN ,  LACKEY KAREN ELIZABETH ,  LUZZIO MICHAEL JOSEPH ,  PEEL MICHAEL ROBERT ,  STERNBACH DANIEL DAVID

IPC: A61K31/47 ,  A61K31/675 ,  A61P35/00 ,  A61P43/00 ,  C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  C07F9/6561

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)mOR1, (CH2)mSR1 and (CH¿2?)mNR?1R2¿ wherein m is an integer of 0 to 6, and R?1 and R2¿ 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.

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.

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.