ANDROSTENONES
    21.
    发明申请
    ANDROSTENONES 审中-公开
    对雄激素

    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

    Inventor: GLAXO INC.

    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。

    WATER SOLUBLE DERIVATIVES OF CAMPTOTHECIN AND THEIR USE AS ANTITUMOR AGENTS
    22.
    发明申请
    WATER SOLUBLE DERIVATIVES OF CAMPTOTHECIN AND THEIR USE AS ANTITUMOR AGENTS 审中-公开
    卡莫司汀的水溶性衍生物及其作为抗菌剂的用途

    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

    Inventor: GLAXO, INC.

    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。

    1,5 BENZODIAZEPINE DERIVATIVES HAVING CCK AND/OR GASTRIN ANTAGONISTIC ACTIVITY
    23.
    发明申请
    1,5 BENZODIAZEPINE DERIVATIVES HAVING CCK AND/OR GASTRIN ANTAGONISTIC ACTIVITY 审中-公开
    具有CCK和/或GASTRIN拮抗活性的1,2,5-二苯并噻吩衍生物

    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

    Inventor: GLAXO INC.

    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。

    INHIBITORS OF 5-ALPHA-TESTOSTERONE REDUCTASE
    24.
    发明申请
    INHIBITORS OF 5-ALPHA-TESTOSTERONE REDUCTASE 审中-公开
    5-ALPHA-TESTOSTERONE还原酶的抑制剂

    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

    Inventor: GLAXO INC.

    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。

    ANDROSTENONE DERIVATIVE
    26.
    发明申请
    ANDROSTENONE DERIVATIVE 审中-公开
    雄激素衍生物

    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

    Inventor: GLAXO INC.

    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。

    SUBSTITUTED 6-AZAANDROSTENONES
    28.
    发明申请
    SUBSTITUTED 6-AZAANDROSTENONES 审中-公开
    取代的6-氮杂

    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

    Inventor: GLAXO INC.

    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。

    MEDICAL CAPSULE DEVICE ACTUATED BY RF SIGNAL
    29.
    发明申请
    MEDICAL CAPSULE DEVICE ACTUATED BY RF SIGNAL 审中-公开
    由RF信号激活的医用胶囊装置

    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.

    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.

    AEROSOL DRUG FORMULATIONS
    30.
    发明申请
    AEROSOL DRUG FORMULATIONS 审中-公开
    气溶胶药物制剂

    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

    Inventor: GLAXO INC.

    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.

Patent Agency Ranking