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71. 发明授权

US4206211A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4206211A
公开(公告)日：1980-06-03
申请号：US885126
申请日：1978-03-10
申请人： Giorgio Palamidessi , Maurizio Foglio , Franco Zarini , Giovanni Franceschi , Aurora Sanfilippo , Federico Arcamone
发明人： Giorgio Palamidessi , Maurizio Foglio , Franco Zarini , Giovanni Franceschi , Aurora Sanfilippo , Federico Arcamone
IPC分类号： C07D501/04 , A61K31/425 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/28 , C07D501/36 , C07D501/57 , C07D501/60 , C07F7/02 , C07F7/08
CPC分类号： C07D501/57
摘要： 7.beta.-acylamino-7.alpha.-methoxy-3-pyrazinylthiomethyl-cephalosporins and their intermediates having high resistance toward .beta.-lactamase enzymes, as well as good antibacterial activity and processes for preparation thereof.
摘要翻译： 7β-酰基氨基-7α-甲氧基-3-吡嗪基硫甲基头孢菌素及其对β-内酰胺酶具有高抗性的中间体，以及良好的抗菌活性及其制备方法。

72. 发明授权

US4191755A Novel daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：新型道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4191755A
公开(公告)日：1980-03-04
申请号：US901358
申请日：1978-05-01
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is hydrogen or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

73. 发明授权

US4188377A Carminomycin derivatives, their preparation and use 失效
标题翻译：卡门霉素衍生物，其制备和用途
公开(公告)号：US4188377A
公开(公告)日：1980-02-12
申请号：US872626
申请日：1978-01-26
申请人： Antonino Suarato , Paolo Masi , Luigi Bernardi , Federico Arcamone
发明人： Antonino Suarato , Paolo Masi , Luigi Bernardi , Federico Arcamone
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： N-acyl derivatives of the known antitumor antibiotic carminomycin, particularly N-trifluoroacetyl carminomycin, have a much lower toxicity than carminomycin.
摘要翻译：已知抗肿瘤抗生素卡明霉素的N-酰基衍生物，特别是N-三氟乙酰卡明霉素，毒性低于卡培霉素。

74. 发明授权

US4020270A L-lyxohex-1-enopyranose derivative 失效
标题翻译： L-赖索昔-1-吡喃葡萄糖衍生物
公开(公告)号：US4020270A
公开(公告)日：1977-04-26
申请号：US650519
申请日：1976-01-19
申请人： Federico Arcamone , Giuseppe Cassinelli
发明人： Federico Arcamone , Giuseppe Cassinelli
IPC分类号： C07D309/30 , C07H15/252 , C07H5/06
CPC分类号： C07H15/252 , C07D309/30 , Y02P20/55
摘要： Anthracyclinone glycoside antibiotics including the known antibiotics daunomycin and adriamycin, as well as other, novel glycoside antibiotics of the formula (VIII): ##STR1## wherein WHEN R.sub.1 is hydrogen, R.sub.2 and R.sub.3 are each independently hydrogen, methyl, methoxy, chloro, or bromo; and when R.sub.2 and R.sub.3 are hydrogen, R.sub.1 is methyl, chloro, or bromo and R.sub.4 and R.sub.5 are each independently hydrogen or hydroxy are prepared by an acid catalyzed addition reaction between (a) an anthracyclinone compound of the formula ##STR2## or a dioxolanyl protected derivative thereof (VI) having the formula: ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and R.sub.6, R.sub.7 and R.sub.8 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl; or R.sub.7 and R.sub.8, together with the carbon atom to which they are bound may form a saturated or unsaturated ring of 3-8 carbon atoms and (b) a novel reactive, protected 1,2-unsaturated pyranoid sugar, preferably, 1,2,3,6-tetradeoxy-3-trifluoroacetamido-4-trifluoroacetoxy-L-lyxo-hex-1-enopyranose which forms protected derivatives of said glycoside antibiotics and then removing the protecting groups from said glycoside antibiotics. These antibiotics are useful in the treatment of various human cancers and leukemia such as sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.
摘要翻译：蒽环类抗生素包括已知的抗生素道诺霉素和阿霉素，以及其它式（VIII）的新型糖苷抗生素：其中当R1是氢时，R2和R3各自独立地是氢，甲基，甲氧基，氯或溴; 并且当R 2和R 3为氢时，R 1为甲基，氯或溴，并且R 4和R 5各自独立地为氢或羟基，是通过（a）式（III）的蒽环类化合物之间的酸催化加成反应制备的，或其具有下式的二氧杂环戊烷基保护的衍生物（VI）：其中R 1，R 2，R 3，R 4和R 5如上所定义，并且R 6，R 7和R 8独立地选自氢和C 1 -C 4烷基; 或R 7和R 8与它们所连接的碳原子一起可以形成3-8个碳原子的饱和或不饱和的环，和（b）新的反应性保护的1,2-不饱和吡喃糖，优选1,2 ，3,6-四脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-L-赖摩尔 - 己-1-吡喃糖，其形成所述糖苷抗生素的受保护的衍生物，然后从所述糖苷抗生素中除去保护基团。这些抗生素可用于治疗各种人类癌症和白血病如肉瘤，乳腺癌，支气管癌，恶性淋巴瘤，神经母细胞瘤，急性白血病和膀胱癌。

75. 发明授权

US5760248A Tachykinin antagonists 失效
标题翻译：速激肽拮抗剂
公开(公告)号：US5760248A
公开(公告)日：1998-06-02
申请号：US656068
申请日：1996-05-31
申请人： Alessandro Sisto , Christopher Fincham , Edoardo Potier , Stefano Manzini , Federico Arcamone , Paolo Lombardi
发明人： Alessandro Sisto , Christopher Fincham , Edoardo Potier , Stefano Manzini , Federico Arcamone , Paolo Lombardi
IPC分类号： A61K31/405 , A61K31/165 , A61K31/403 , A61K31/404 , A61P1/00 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07C229/32 , C07C231/02 , C07C237/24 , C07D209/14 , C07D209/42 , C07D209/02 , A61K31/40
CPC分类号： C07D209/42 , C07D209/14
摘要： A description is given of tachykinin receptor antagonists having general formula (I) ##STR1## their preparation and use in pharmaceutical formulations.
摘要翻译：给出了具有通式（I）的图速激肽受体拮抗剂（I）的制备和用于药物制剂的描述。

76. 发明授权

US5698710A Tachykinins antagonists 失效
标题翻译：速激肽拮抗剂
公开(公告)号：US5698710A
公开(公告)日：1997-12-16
申请号：US676514
申请日：1996-07-08
申请人： Alessandro Sisto , Edoardo Potier , Stefano Manzini , Christopher Fincham , Paolo Lombardi , Federico Arcamone
发明人： Alessandro Sisto , Edoardo Potier , Stefano Manzini , Christopher Fincham , Paolo Lombardi , Federico Arcamone
IPC分类号： C07D209/42 , C07D209/04 , A61K31/405
CPC分类号： C07D209/42
摘要： The present invention refers to tachykinins antagonists of general formula (I) ##STR1## their preparation and pharmaceutical compositions containing them.
摘要翻译：本发明涉及通式（I）的速激肽拮抗剂，其制备方法和含有它们的药物组合物。

77. 发明授权

US4965351A 4-demethoxy-4-amino-anthracyclines 失效
标题翻译： 4-脱甲氧基-4-氨基蒽环类
公开(公告)号：US4965351A
公开(公告)日：1990-10-23
申请号：US430149
申请日：1989-11-01
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 diazotized 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.

78. 发明授权

US4558042A .beta.-Lactam-containing antibacterial agents and .beta.-lactamase inhibitors 失效
标题翻译：含β-内酰胺的抗菌剂和β-内酰胺酶抑制剂
公开(公告)号：US4558042A
公开(公告)日：1985-12-10
申请号：US595336
申请日：1984-03-30
申请人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone , Aurora Sanfilippo
发明人： Maurizio Foglio , Giovanni Franceschi , Cosimo Scarafile , Federico Arcamone , Aurora Sanfilippo
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.
摘要翻译：公开了含有β-内酰胺的化合物，其中R为氢，低级烷基，三氯乙基，丙酰基，苄基，取代的苄基，苯基，取代的苯基，苯并或将经历代谢活化的残基。 “并具有有利的药代动力学性质; R1是氢原子，低级烷基，低级烷氧基，环烷基或羟基烷基，其羟基烷基的醇官能团是游离或保护的; Z是氢，卤素，羟基，氨基，氨基甲酰氧基，巯基，吡啶鎓，OR2，OCOR2，NHCOR2或SR3，其中R2和R3各自为低级烷基，芳基或杂环，未取代的，n为0或1.该化合物具有广谱抗菌活性和β-内酰胺酶抑制活性。还公开了用于生产含有β-内酰胺的化合物和这些化合物生产中的各种中间体的方法。

79. 发明授权

US4337248A Paromomycin containing compounds and method of use 失效
标题翻译：含有溴霉素的化合物及其使用方法
公开(公告)号：US4337248A
公开(公告)日：1982-06-29
申请号：US156478
申请日：1980-06-04
申请人： Carlo Battistini , Giuseppe Cassinelli , Giovanni Franceschi , Rosanna Mazzoleni , Federico Arcamone
发明人： Carlo Battistini , Giuseppe Cassinelli , Giovanni Franceschi , Rosanna Mazzoleni , Federico Arcamone
IPC分类号： C07H5/06 , A61K31/70 , A61K31/702 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/232 , A61K31/71 , C07H15/22
CPC分类号： C07H15/232
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.
摘要翻译：公开了下式的化合物：其中R 1表示氢或氯原子，以及中间体。这些包括4'-脱氧巴马霉素; 4'-脱氧-4'-表 - 氯 - 巴龙霉素; 4'-脱氧-4'-表 - 氯 - 五-N-苄氧羰基巴霉素; 4'-脱氧 - 五-N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苯甲酰基-4'-脱氧-5-N-苄氧基羰基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-表氯 - 4'-脱甲基 - 五 -N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苄基 - 五-N-苄氧基氨基辛基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（甲硫基） - 噻吩基] 五-N-苄氧羰基巴霉素; 和6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（苯硫基） - 噻吩基] - 五-N-苄氧羰基巴霉素。由结构式表示的化合物可用于治疗人和动物中的阿米巴痢疾。

80. 发明授权

US4267116A Novel daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：新型道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4267116A
公开(公告)日：1981-05-12
申请号：US38689
申请日：1979-05-14
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , C07C50/16
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is hydrogen or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

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