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51. 发明授权

US3996205A Aminoglycoside antibiotics and intermediates 失效
标题翻译：氨基糖苷类抗生素和中间体
公开(公告)号：US3996205A
公开(公告)日：1976-12-07
申请号：US611349
申请日：1975-09-08
申请人： Barney J. Magerlein
发明人： Barney J. Magerlein
IPC分类号： C07H15/244 , A61K31/70 , A61K31/702 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , B01J23/00 , C07B61/00 , C07H5/06 , C07H15/224 , C07H15/236 , C07H17/04 , C07H15/22
CPC分类号： C07H15/224 , C07H15/234 , C07H17/04 , Y02P20/55
摘要： 6-0- AND 3'-0-D-glycosyl analogs of neamine, 6-0- and 3'-0-D-glycosyl ortho esters of neamine, novel aminoglycoside antibiotics, and novel intermediates are prepared by a new chemical process. The compounds have utility as antibacterial agents or as intermediates to make antibacterially-active compounds.
摘要翻译：通过新的化学方法制备新胺，新型氨基糖苷类抗生素和新型中间体的neamine，6-0和3'-0-D-糖基原酸酯的6-0-和3'-0-D-糖基类似物。该化合物可用作抗菌剂或作为制备抗菌活性化合物的中间体。

52. 发明授权

US3939043A Antibiotics designated XK-88 series and process for production thereof 失效
标题翻译：抗生素指定为XK-88系列及其生产方法
公开(公告)号：US3939043A
公开(公告)日：1976-02-17
申请号：US516816
申请日：1974-10-21
申请人： Takashi Nara , Seigo Takasawa , Ryo Okachi , Isao Kawamoto , Mitsuyoshi Yamamoto , Seiji Sato , Tomoyasu Sato , Atsuko Morikawa
发明人： Takashi Nara , Seigo Takasawa , Ryo Okachi , Isao Kawamoto , Mitsuyoshi Yamamoto , Seiji Sato , Tomoyasu Sato , Atsuko Morikawa
IPC分类号： C12P19/48 , A61K35/74 , A61P31/04 , C07G11/00 , C07H15/224 , C07H15/234 , C07H15/236 , C07H15/244 , C12P1/06 , C12R1/465 , C12D9/00
CPC分类号： C07H15/224 , C07H15/234 , Y10S435/803
摘要： A novel series of antibiotics designated the XK-88 series are produced by culturing a microorganism belonging to the genus Streptomyces in a nutrient medium and thereafter recovering the antibiotics from the culture liquor.BACKGROUND OF THE INVENTIONThe present invention relatees to novel antibiotics and a process for the production thereof. More specifically the present invention relates to novel antibiotics designated, XK-88-1, XK-88-2, XK-88-3 and XK-88-5 and a process for producing such antibiotics.Antibiotics which exhibit activity against a borad spectrum of bacteria are always in demand. To this end, a new species of microorganism has been isolated from soil located in Tajima-cho, Hofu-shi, Yamaguchi-ken, Japan. This new species, when cultured, produces a series of new antibiotics, the XK-88 series, all of which exhibit strong antibacterial activity against various Gram-positive and Gram-negative bacteria. Accordingly, the antibiotics of the invention are useful to clean and sterilize laboratory glassware ans surgical instruments, and may also be used in combination with various soaps for sanitation purposes as in cleaning and sanitizing hospital rooms and areas used for the preparation of food.
摘要翻译：通过在营养培养基中培养属于链霉菌属的微生物，然后从培养液中回收抗生素，产生了称为XK-88系列的新一系列抗生素。

53. 发明授权

US3089814A Process for the production of a concentrate of active substance from senna 失效
标题翻译：从番泻叶生产活性物质浓缩物的方法
公开(公告)号：US3089814A
公开(公告)日：1963-05-14
申请号：US79560559
申请日：1959-02-26
申请人： NATTERMANN A & CIE
发明人： FRITZ BLAICH
IPC分类号： A61K31/70 , A61K36/00 , A61K36/482 , C07H15/244
CPC分类号： A61K31/70 , A61K36/482 , A61K2300/00

54. 发明申请

US20220127298A1 THERMOSPOROTHRIX HAZAKENSIS-DERIVED ANTIBACTERIALLY ACTIVE SUBSTANCE 有权
公开(公告)号：US20220127298A1
公开(公告)日：2022-04-28
申请号：US17428109
申请日：2020-02-04
申请人： KENNAN EISEI KOGYO CO., LTD.
发明人： Hideaki TAKANO , Minato SATO , Shoichi AMANO , Hatsumi TAKANO , Kenji UEDA , Kazuo FURIHATA , Shohei SAKUDA , Akira YOROTA , Shuhei YABE
IPC分类号： C07H15/244 , A61K35/74 , A61K31/704 , A01N43/08 , A01N63/20
摘要： This invention provides a novel compound having an antibacterial activity, and a method for producing the same. The compound is represented by Formula (I): or a salt or ester thereof.

55. 发明申请

US20190100548A1 Anthracycline Derivatives For Treating Tumor Diseases 审中-公开
公开(公告)号：US20190100548A1
公开(公告)日：2019-04-04
申请号：US16207285
申请日：2018-12-03
申请人： Produkem Molekulares Design GmbH
发明人： Christian R. Noe , Michael Sonntagbauer , Sébastien Queva , Ernst Urban
IPC分类号： C07H15/244 , C07F7/18 , C07C15/28 , C07D317/32 , C07C45/59 , C07D307/20 , C07H15/252 , C07H15/08 , C07D317/34 , C07D317/26
摘要： The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits.

56. 发明授权

US10144753B2 Anthracycline derivatives for treating tumor diseases 有权
公开(公告)号：US10144753B2
公开(公告)日：2018-12-04
申请号：US14435907
申请日：2013-10-15
申请人： Produkem Molekulares Design GmbH
发明人： Christian R. Noe , Michael Sonntagbauer , Sébastien Queva , Ernst Urban
IPC分类号： C07H15/244 , C07D265/06 , C07D317/32 , C07D317/34 , C07H15/08 , C07H15/252 , C07D307/20 , C07C15/28 , C07C45/59 , C07D317/26 , C07F7/18
摘要： The invention relates to anthracycline derivative compounds for treating tumor diseases, and related methods, compositions, and kits.

57. 发明申请

US20130045933A1 ALOE-EMODIN DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF CANCER 审中-公开
标题翻译： ALOE-EMODIN衍生物及其用于治疗癌症的方法
公开(公告)号：US20130045933A1
公开(公告)日：2013-02-21
申请号：US13574558
申请日：2011-01-20
申请人： Micha Fridman , Elinor Briner-Goldstein , Zoharia Evron , Michael Frenkel , Ester Flescher
发明人： Micha Fridman , Eliezer Flescher , Elinor Briner-Goldstein , Zoharia Evron , Michael Frenkel
IPC分类号： C07H15/244 , A61P35/04 , A61P35/02 , A61K31/704 , A61P35/00
CPC分类号： C07H15/244 , A61K31/704
摘要： The present invention relates to anthracycline derivatives that are based on an Aloe-emodin (AE) backbone attached to a glycoside (an amino sugar or amino carba-sugar). These derivatives are useful as chemotherapeutic agents. Advantageously, these derivatives are potent cytotoxic agents against a variety of anthracycline-resistant tumors. In addition, they may have reduced cardiotoxicity. As such, the novel compounds of the invention offer an advantage over currently available drugs. The present invention further relates to methods for preparing the novel Aloe-Emodin Glycoside (AEG) based derivatives, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.
摘要翻译：本发明涉及基于连接于糖苷（氨基糖或氨基碳糖）的芦荟大黄素（AE）主链的蒽环类衍生物。这些衍生物可用作化学治疗剂。有利地，这些衍生物是针对各种耐蒽环霉素的肿瘤的有效的细胞毒性剂。此外，它们可能具有降低的心脏毒性。因此，本发明的新化合物比目前可用的药物具有优势。本发明还涉及用于制备新型芦荟大黄素苷（AEG）衍生物的方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物，特别是作为预防和治疗癌症的化学治疗剂的方法。

58. 发明申请

US20090325894A1 TETRACYCLIC ANTHRAQUINONES POSSESSING ANTI-CANCER PROPERTIES 审中-公开
标题翻译：抵抗抗癌特性的四氯化萘
公开(公告)号：US20090325894A1
公开(公告)日：2009-12-31
申请号：US12504751
申请日：2009-07-17
申请人： Hesheng Zhang
发明人： Hesheng Zhang
IPC分类号： A61K31/704 , C07H15/244 , A61P35/00
CPC分类号： A61K31/704
摘要： The present invention provides aminoside tetracyclic anthraquinones represented by formula (I) or formula (II), wherein the peptides are introduced to connect tetracyclic anthraquinones and fatty acid saturated or unsaturated in order to make the anticancer agents to be absorbed and released selectively; meanwhile some water-solubility groups are also introduced into the branched chain, aminosaccharide and tetracyclic moiety of the compounds to improve the water-solubility. The present invention also provides the preparative method and the use thereof as pharmaceutically active components for treating the diseases cured by aminoside tetracyclic anthraquinone, for example cancer, such as intestines, liver, gastric, breast, lung, ovary, prostate, brain glioma, lymph, skin, pigment, thyroid gland, multiple bone marrow cancer and leukemia.
摘要翻译：本发明提供由式（I）或式（II）表示的氨基四氢环蒽醌，其中引入肽连接四环蒽醌和饱和或不饱和脂肪酸，以使抗癌剂被选择性吸收和释放; 同时一些水溶性基团也被引入化合物的支链，氨基糖和四环部分以提高水溶性。本发明还提供了制备方法及其作为药物活性成分的药物活性成分，用于治疗由氨基四氢环蒽醌固化的疾病，例如肠癌，肝癌，胃癌，乳腺癌，肺癌，卵巢癌，前列腺癌，脑胶质瘤，淋巴细胞，皮肤，色素，甲状腺，多发骨髓癌和白血病。

59. 发明授权

US06903076B2 Antihelminthic anthraquinones and method of use thereof 失效
标题翻译：抗真菌蒽醌及其使用方法
公开(公告)号：US06903076B2
公开(公告)日：2005-06-07
申请号：US10723671
申请日：2003-11-26
申请人： Robert H. Cichewicz , Muraleedharan G. Nair , James H. McKerrow
发明人： Robert H. Cichewicz , Muraleedharan G. Nair , James H. McKerrow
IPC分类号： C07H15/244 , A61K31/122 , A61K31/21 , A61K31/70 , A61K31/704 , A61P33/10 , A61P33/12 , C07C50/34 , C07C50/38 , C07C66/02 , C07C69/157 , A01N43/04 , A01N37/00 , A01K31/70 , A01K31/21
CPC分类号： A61K31/70 , A61K31/21 , C07C50/38 , Y02A50/423
摘要： Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.
摘要翻译：描述了蒽醌类化合物，其具有抗耳毒性，特别是可用于抑制血吸虫病的组合物。体外或体内。优选的蒽醌具有下式：其中R 1，R 2，R 3和R 4各自为氢，羟基，卤素，烷基，取代的烷基，烯烃，取代的烯烃，炔烃，芳基，取代的芳基，环状，取代的环状，酸基，碳水化合物或其组合，R是含有1至12个碳的基团，例如甲基，烷基，取代的烷基，醛，羟基，羟甲基，酸基，碳水化合物或其组合，卤素是I，F，Br或Cl。

60. 发明授权

US6075135A 3,4-di-O,N-Protected-4-amino-2,4,6-trideoxy-2-fluoro-L-manno-pyranosyl halide and a process for its preparation 失效
标题翻译： 3,4-二-O，N-保护的-4-氨基-2,4,6-三脱氧-2-氟-L-壬烷 - 吡喃糖基卤化物及其制备方法
公开(公告)号：US6075135A
公开(公告)日：2000-06-13
申请号：US282200
申请日：1999-03-31
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/244 , C07H15/252 , C07H1/00 , C07H5/00
CPC分类号： C07H15/252 , C07H15/244 , Y02P20/55
摘要： 7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-.alpha.-L-mannopyranosyl)-daunomycinone or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1## wherein R is a hydrogen atom or hydroxyl group. These novel compounds according to this invention exhibit excellent antitumor activities and have a high solubility in water, and hence they are useful as an antitumor agent.
摘要翻译：现在，合成7-O-（4-氨基-2,4,6-三脱氧-2-氟-α-L-吡喃甘露糖基） - 日诺霉素酮或阿曲达霉素，作为具有通式的道诺霉素酮或阿霉素酮衍生物，其中R是氢原子或羟基。根据本发明的这些新化合物表现出优异的抗肿瘤活性，并且在水中的溶解度高，因此它们可用作抗肿瘤剂。

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