公开(公告)号：US5124318A

公开(公告)日：1992-06-23

申请号：US471005

申请日：1990-01-25

申请人： Gaetano Gatti ,  Diego Oldani ,  Giuseppe Bottoni ,  Carlo Confalonieri ,  Luciano Gambini ,  Roberto De Ponti

发明人： Gaetano Gatti ,  Diego Oldani ,  Giuseppe Bottoni ,  Carlo Confalonieri ,  Luciano Gambini ,  Roberto De Ponti

IPC分类号： A61K9/00 ,  A61K9/08 ,  A61K31/704 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/26 ,  C07H15/252

CPC分类号： A61K9/0019 ,  A61K31/70 ,  A61K31/704 ,  A61K47/02 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/26 ,  A61K9/08 ,  C07H15/252

摘要： A sealed glass container containing therein a stable, injectable, sterile, pyrogen-free doxorubicin anti-tumor composition in a solution which consists essentially of a physiologically acceptable salt of doxorubicin dissolved in a physiologically acceptable solvent therefor, wherein said solution has not been reconstructed from a lyophilizate, and wherein said solution has a pH of from 2.5-3.5 and a concentration of said doxorubicin of from 0.1 to 100 mg/ml.

摘要翻译： 一种密封的玻璃容器，其中含有稳定的，可注射的，无菌的无致热原多柔比星抗肿瘤组合物，其溶液中基本上由生理上可接受的多柔比星盐溶解在其生理上可接受的溶剂中，其中所述溶液未被重建 冻干物，其中所述溶液的pH为2.5-3.5，所述多柔比星的浓度为0.1至100mg / ml。

公开(公告)号：US5091372A

公开(公告)日：1992-02-25

申请号：US588526

申请日：1990-09-26

申请人： Gaetano Gatti ,  Diego Oldani ,  Carlo Confalonieri ,  Luciano Gambini

发明人： Gaetano Gatti ,  Diego Oldani ,  Carlo Confalonieri ,  Luciano Gambini

IPC分类号： A61K31/70 ,  A61K9/08 ,  A61K9/19 ,  A61K31/704 ,  A61K47/00 ,  A61K47/08 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61P35/00

CPC分类号： A61K31/70 ,  A61K47/12 ,  A61K47/14 ,  A61K47/183 ,  A61K47/20 ,  A61K9/0019 ,  A61K9/19

摘要： Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.

公开(公告)号：US5089489A

公开(公告)日：1992-02-18

申请号：US504836

申请日：1990-04-05

申请人： Marco Alpegiani ,  Ettore Perrone ,  Piergiuseppe Orezzi ,  Paolo Carminati ,  Giuseppe Cassinelli

发明人： Marco Alpegiani ,  Ettore Perrone ,  Piergiuseppe Orezzi ,  Paolo Carminati ,  Giuseppe Cassinelli

IPC分类号： C07D499/897 ,  A61K31/43 ,  A61P29/00 ,  A61P43/00 ,  C07D499/06 ,  C07D499/88

CPC分类号： C07D499/88 ,  A61K31/43

摘要： 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.

公开(公告)号：US5045534A

公开(公告)日：1991-09-03

申请号：US501800

申请日：1990-03-30

申请人： Alberto Bargiotti ,  Maria Grandi ,  Antonino Suarato ,  Fernando Giuliani

发明人： Alberto Bargiotti ,  Maria Grandi ,  Antonino Suarato ,  Fernando Giuliani

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252

CPC分类号： C07H15/252

摘要： Antitumour anthracycline glycosides of formula I: ##STR1## wherein R.sub.1 is hydrogen or a hydroxyl group, and pharmaceutically acceptable acid addition salts thereof.

摘要翻译： 式I的抗肿瘤蒽环酸苷：其中R 1是氢或羟基，及其药学上可接受的酸加成盐。

公开(公告)号：US4990635A

公开(公告)日：1991-02-05

申请号：US294016

申请日：1989-01-06

申请人： Antonio Longo ,  Paolo Lombardi

发明人： Antonio Longo ,  Paolo Lombardi

IPC分类号： A61K31/565 ,  A61P35/00 ,  C07J1/00 ,  C07J75/00

CPC分类号： C07J1/0011 ,  C07J75/00

摘要： The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.

公开(公告)号：US4985548A

公开(公告)日：1991-01-15

申请号：US462549

申请日：1990-01-09

申请人： Michele Caruso ,  Antonino Suarato ,  Francesco Angelucci ,  Federico Arcamone

发明人： Michele Caruso ,  Antonino Suarato ,  Francesco Angelucci ,  Federico Arcamone

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07C46/00 ,  C07C50/22 ,  C07C50/38 ,  C07C225/34 ,  C07H15/252

CPC分类号： C07H15/252

摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

公开(公告)号：US4973674A

公开(公告)日：1990-11-27

申请号：US179989

申请日：1988-04-11

申请人： Maria G. Brasca ,  Sergio Penco

发明人： Maria G. Brasca ,  Sergio Penco

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  C07H15/10 ,  C07H15/252 ,  C07H23/00 ,  C07H15/244

CPC分类号： C07H15/10 ,  C07H15/252 ,  C07H23/00

摘要： Anthracycline glycosides of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from hydrogen, methyl, ethyl or methoxy and pharmaceutically acceptable acid addition salts thereof, which are useful in treatment of human cancer, are prepared by a stereospecific condensation of a derivative of daunosamine of general formula (II): ##STR2## wherein R.sub.3 is an alkyl, perfluoroalkyl or aryl group and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently selected from alkyl, aryl or aralkyl having up to ten carbon atoms, with a quinone quinizarine epoxide of general formula (III) ##STR3## and conversion of the product obtained to the anthracycline glycoside of formula (I) or salt thereof.

公开(公告)号：US4909290A

公开(公告)日：1990-03-20

申请号：US246093

申请日：1988-09-19

申请人： Mario Coccia

发明人： Mario Coccia

IPC分类号： A61J1/05 ,  A61J1/00 ,  A61J1/14 ,  A61J1/20

CPC分类号： A61J1/2096 ,  A61J1/201 ,  Y10S604/905

摘要： The device includes a syringe and an apparatus for coupling the syringe to a drug holding bottle and the like, the apparatus defining an enclosed chamber wherein there is housed a needle to be coupled to the syringe and the free end of which is arranged is front of a tightness resilient member located at a seat adapted to receive the mouth of the bottle, the syringe being firmly and fixedly clamped, in a tight way, in a syringe seat formed in the apparatus.

摘要翻译： 该装置包括注射器和用于将注射器连接到药物保持瓶等的装置，所述装置限定封闭的腔室，其中容纳有要联接到注射器的针，并且其自由端被布置在 位于适于容纳瓶口的座位上的紧密弹性构件，注射器以紧密方式牢固且牢固地夹紧在形成于该装置中的注射器座中。

公开(公告)号：US4865766A

公开(公告)日：1989-09-12

申请号：US192138

申请日：1988-05-10

申请人： Antonio Longo ,  Fabrizio Orzi ,  Paolo Lombardi ,  Maristella Colombo

发明人： Antonio Longo ,  Fabrizio Orzi ,  Paolo Lombardi ,  Maristella Colombo

IPC分类号： A61K31/565 ,  C07J41/00

CPC分类号： C07J41/0011

摘要： A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.

公开(公告)号：US5576330A

公开(公告)日：1996-11-19

申请号：US354215

申请日：1994-12-12

申请人： Franco Buzzetti ,  Antonio Longo ,  Maria G. Brasca ,  Fabrizio Orzi ,  Angelo Crugnola ,  Dario Ballinari ,  Mariangela Mariani

发明人： Franco Buzzetti ,  Antonio Longo ,  Maria G. Brasca ,  Fabrizio Orzi ,  Angelo Crugnola ,  Dario Ballinari ,  Mariangela Mariani

IPC分类号： C07D401/06 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/475 ,  A61K31/505 ,  A61K31/675 ,  A61K31/70 ,  A61K38/04 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  C07D209/34 ,  A61K31/015

CPC分类号： A61K31/70 ,  A61K31/40 ,  A61K31/47 ,  A61K31/475 ,  A61K31/505 ,  A61K31/675 ,  A61K38/04 ,  Y10S514/825 ,  Y10S514/863 ,  Y10S514/866 ,  Y10S514/886 ,  Y10S514/908

摘要： The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin;and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl and R.sub.3, R.sub.4 and R.sub.5 are hydrogen; whereas when Y is indole, then R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro or --NHR, in which R is as defined above, R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, carboxy, nitro or --NHR, wherein R is as defined above, and R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;as anti-angiogenic agent is disclosed.

摘要翻译： 式（I）化合物（I）的新用途其中Y是选自萘，四氢化萘，喹啉，异喹啉和吲哚的双环; n为0或1〜3的整数， R1是氢，C1-C6烷基或C2-C6烷酰基; R2是氢，卤素，C1-C6烷基，氰基，羧基，硝基或NHR，其中R是氢或C1-C6烷基; R3是氢或C1-C6烷基; R 4是氢，羟基，C 1 -C 6烷氧基，C 2 -C 6烷酰氧基，羧基，硝基或NHR，其中R如上定义; R5是氢，C1-C6烷基或卤素; 或其药学上可接受的盐; 当Y为萘时，n为0或1〜3的整数，Y为四氢化萘，喹啉，异喹啉或吲哚时，n为0,1或2。 并且其中当双环Y为萘，喹啉，异喹啉或吲哚时，则所述取代基OR 1，R 2和羟吲哚基中的每一个可以独立地表示在所述二环的芳基或杂芳基部分上，而只有苯部分被取代， Y是四氢化萘; 其中当Y为萘，四氢化萘，喹啉或异喹啉时，则R2为氢，卤素，氰基或C1-C6烷基，R3，R4和R5为氢; 而当Y为吲哚时，R 2为氢，卤素，C 1 -C 6烷基，氰基，羧基，硝基或-NHR，其中R如上定义，R 3为氢或C 1 -C 6烷基，R 4为氢，羟基， C 1 -C 6烷氧基，C 1 -C 6烷酰氧基，羧基，硝基或-NHR，其中R如上所定义，R 5是氢，卤素或C 1 -C 6烷基; 作为抗血管生成剂被公开。