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121 条记录 (耗时 0.024 秒)

    2-acyloxycephem derivatives
    2.
    发明授权
    2-acyloxycephem derivatives 失效
    2-酰氧基头孢烯衍生物

    公开(公告)号：US5587373A

    公开(公告)日：1996-12-24

    申请号：US331483

    申请日：1994-11-04

    申请人： Marco Alpegiani ,  Pierluigi Bissolino ,  Ettore Perrone

    发明人： Marco Alpegiani ,  Pierluigi Bissolino ,  Ettore Perrone

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/16 ,  C07D501/20 ,  C07D501/26 ,  C07D501/36 ,  C07D501/38 ,  C07D501/59 ,  C07D501/04 ,  C07D501/14 ,  C07D501/60

    CPC分类号： C07D501/00

    摘要： The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical;R.sup.1 represents halogen, A, OA, --S(O).sub.m A wherein m is 0-2, --OC(O)A, --OS(O).sub.2 A, --NHC(O)A or --NH--Z wherein Z is a mono, di- or tripeptide and A is as defined above;R.sup.2 represents a halogen, A, --S(O).sub.m A, --O--A, --C(O)A, --C(O)OA, --CH.sub.2 --OA, --CH.sub.2 S(O).sub.m A, --CH.sub.2 OC(O)A, --CH.sub.2 O--Z, --CH.sub.2 SC(O) A, --CH.sub.2 --N(A)A, --CH.sub.2 N.sup.+ (A)(A')A", --CH.sub.2 NH--C(O)A or --CH.sub.2 NH--Z wherein A and Z are as defined above.The compounds of formula (I) and their salts are elastase inhibitors.

    摘要翻译： PCT No.PCT / EP94 / 00529 Sec。 371日期：1994年11月4日 102（e）日期1994年11月4日PCT 1994年2月24日PCT PCT。 WO94 / 20504 PCT出版物 1994年9月15日本发明提供式（I）的头孢菌素砜及其药学上和兽医学上可接受的盐：其中n是一个或两个：A和B都是氢或有机的 激进; R1表示卤素，A，OA，-S（O）mA，其中m为0-2，-OC（O）A，-OS（O）2A，-NHC（O）A或-NH-Z，其中Z为 单，二或三肽和A如上所定义; R 2表示卤素，A，-S（O）mA，-OA，-C（O）A，-C（O）OA，-CH 2 OA，-CH 2 S（O） -CH 2 SC（O）A，-CH 2 -N（A）A，-CH 2 N +（A）（A'）A“，-CH 2 NH-C（O）A或-CH 2 NH- Z如上所定义。 式（I）化合物及其盐是弹性蛋白酶抑制剂。

    Polymer-bound paclitaxel derivatives
    6.
    发明授权
    Polymer-bound paclitaxel derivatives 失效
    聚合物结合紫杉醇衍生物

    公开(公告)号：US5473055A

    公开(公告)日：1995-12-05

    申请号：US263832

    申请日：1994-06-22

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta.Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式 ，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键 ，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， βAla，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-Ala，Phe-Ala-Ala，Leu-Phe-βAla，Leu-Gly-β Ala，Phe-Leu-Gly-βAla，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Gly β-Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，这些化合物具有抗肿瘤活性， 。 还描述了其制备方法和含有它们的药物组合物。

    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation
    7.
    发明授权
    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
    取代的（芳基烷基氨基苄基）氨基丙酰胺衍生物及其制备方法

    公开(公告)号：US5449692A

    公开(公告)日：1995-09-12

    申请号：US215694

    申请日：1994-03-22

    申请人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    发明人： Mario Varasi ,  Philippe Dostert ,  Paolo Pevarello ,  Alberto Bonsignori

    IPC分类号： A61K31/165 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07C231/10 ,  C07C237/06 ,  C07C233/05

    CPC分类号： C07C237/06

    摘要： The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

    摘要翻译： 本发明提供新的式（I）化合物其中n为1至4的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或C1-C4烷基; 及其药学上可接受的盐; 并且其中当R同时为氢时，R 1为氢或卤素且n为1，则R 2为氢或甲基; 和式（IA）其中R 3是卤素的式（IA）及其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的，可用于治疗作为抗癫痫药，抗帕金森病， 神经保护，抗抑郁药，抗痉挛药和催眠药。

    Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system
    9.
    发明授权
    Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system 失效
    哌嗪取代的1,4-苯并恶嗪衍生物及其在治疗中枢神经系统疾病中的应用

    公开(公告)号：US5229383A

    公开(公告)日：1993-07-20

    申请号：US748221

    申请日：1991-08-20

    申请人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    发明人： Mario Varasi ,  Piero Melloni ,  Maria A. Cervini ,  Alberto Bonsignori ,  Roberto Commisso

    IPC分类号： C07D265/36 ,  C07D279/16 ,  C07D471/10

    CPC分类号： C07D471/10 ,  C07D265/36 ,  C07D279/16

    摘要： The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.

    摘要翻译： 本发明涉及具有下式（I）的化合物：其中X表示-O-或-S-; R和R 1各自独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基，硝基或三卤代-C 1 -C 6烷基; R 2和R 3各自独立地是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基-C 1 -C 6烷基; 或R 2和R 3与它们所连接的氮原子一起形成任选含有另外选自氧，硫和氮的杂原子的未取代或取代的6元饱和的杂单环; R 4和R 5各自独立地是氢，卤素，硝基，氨基或三卤代-C 1 -C 6烷基; 及其药学上可接受的盐。 本发明的化合物可用于作为主要镇静剂的治疗，例如在精神病性障碍的治疗中。

    Unsaturated 17.beta.-subsituted 3-carboxy steroids
    10.
    发明授权
    Unsaturated 17.beta.-subsituted 3-carboxy steroids 失效
    不饱和的17（BETA） - 使用的3-CARBOXY STEROIDS

    公开(公告)号：US5212166A

    公开(公告)日：1993-05-18

    申请号：US886574

    申请日：1992-05-21

    申请人： Achille Panzeri ,  Marcella Nesi ,  Enrico Di Salle

    发明人： Achille Panzeri ,  Marcella Nesi ,  Enrico Di Salle

    IPC分类号： A61K31/565 ,  A61K31/56 ,  A61K31/58 ,  A61P5/24 ,  A61P5/28 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P17/02 ,  A61P17/14 ,  A61P35/00 ,  A61P43/00 ,  C07J20060101 ,  C07J41/00 ,  C07J43/00

    CPC分类号： C07J43/003 ,  C07J41/0066

    摘要： The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;R is a group;a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group;c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group:(i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or(ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or(iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.6 alkyl group or taken together with the nitrogen atom to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen, and n is an integer of 2 to 4;R.sub.1 is hydrogen, a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalkyl group, a C.sub.6 -C.sub.9 cycloalkyalkyl group or an aryl group;each of R.sub.2 and R.sub.3 is, independently, selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.9 cycloalkylalkyl and aryl or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol ( ) represents a single or a double bond provided that when it is a double bond the hydrogen in the 5.alpha. position doesn't exist and the pharmaceutically acceptable salts thereof.In view of their 5-.alpha. reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.