公开(公告)号：US4410516A

公开(公告)日：1983-10-18

申请号：US285550

申请日：1981-07-21

申请人： Hamao Umezawa ,  Shinichi Kondo

发明人： Hamao Umezawa ,  Shinichi Kondo

IPC分类号： C07H15/236 ,  A61K31/71 ,  C07H15/22

CPC分类号： C07H15/234

摘要： New antibacterial compounds are provided, including a 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-5,3',4'-trideoxykanamycin B; a 1-N(.alpha.-hydroxy-.omega.-aminoalkanoyl)-5,3',4',641 -tetradeoxykanamycin B; and a 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-5,3',4'-trideoxy-6'-N-methylkanamycin B; as well as 5,3',4',6"-tetradeoxykanamycin B and 5,3',4'-trideoxy-6'-N-methylkanamycin B.

摘要翻译： 提供了新的抗菌化合物，包括1-N-（α-羟基 - ω-氨基烷酰基）-5,3'，4'-三脱氧卡那霉素B; 1-N（α-羟基-ω-氨基烷酰基）-5,3'，4'，641-四脱氧卡那霉素B; 和1-N-（α-羟基 - ω-氨基烷酰基）-5,3'，4'-三脱氧-6'-N-甲基卡那霉素B; 以及5,3'，4'，6“ - 四脱氧卡那霉素B和5,3'，4'-三脱氧-6'-N-甲基卡那霉素B.

公开(公告)号：US4326054A

公开(公告)日：1982-04-20

申请号：US167439

申请日：1980-07-09

申请人： Hamao Umezawa ,  Tomohisa Takita ,  Akio Fujii ,  Yasuhiko Muraoka ,  Mamoru Kunishima

发明人： Hamao Umezawa ,  Tomohisa Takita ,  Akio Fujii ,  Yasuhiko Muraoka ,  Mamoru Kunishima

IPC分类号： C12P17/00 ,  A61K31/70 ,  A61K31/7028 ,  A61P31/04 ,  A61P35/00 ,  C07H15/26 ,  C07K9/00 ,  C12P19/44 ,  C12P19/60 ,  C12R1/465 ,  C07H11/02 ,  C07H13/12

CPC分类号： C12R1/465 ,  C07H15/26 ,  C07K9/003 ,  C12P19/60 ,  Y10S930/19 ,  Y10S930/27

摘要： Novel antibiotics cleomycins represented by the formula ##STR1## wherein R is a terminal amino residue of the cleomycin. These compounds are useful as a chemotherapeutic agent for treating cancer and bacterial infections.

摘要翻译： 由式表示的新型抗生素cleomycins，其中R是克霉霉素的末端氨基残基。 这些化合物可用作治疗癌症和细菌感染的化学治疗剂。

公开(公告)号：US4281180A

公开(公告)日：1981-07-28

申请号：US96693

申请日：1979-11-23

申请人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tadashi Shirai ,  Rinzo Nishizawa ,  Masao Suzuki ,  Tetsushi Saino

发明人： Hamao Umezawa ,  Takaaki Aoyagi ,  Tadashi Shirai ,  Rinzo Nishizawa ,  Masao Suzuki ,  Tetsushi Saino

IPC分类号： A47L13/40 ,  A61K20060101 ,  A61K31/16 ,  A61K31/195 ,  C07C20060101 ,  C07C51/347 ,  C07C233/31 ,  C07C233/47 ,  C07C233/76 ,  C07C233/87 ,  C07C271/22 ,  C07C271/34 ,  C07C271/54 ,  C07D209/48 ,  C07K1/06 ,  C07K5/02 ,  C07K5/06

CPC分类号： C07C237/20 ,  A61K38/00 ,  Y02P20/55

摘要： A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: ##STR1## wherein R.sub.1 represents a naphthyl or a group of the formula: ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R.sub.2 represents a protected amino, with a starting compound represented by the general formula: ##STR3## wherein R.sub.3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: ##STR5## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: ##STR6## wherein R.sub.2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: ##STR7## wherein R.sub.4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: ##STR8## wherein R.sub.1 and R.sub.4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.

公开(公告)号：USRE30413E

公开(公告)日：1980-10-07

申请号：US41995

申请日：1979-05-24

申请人： Hamao Umezawa ,  Yasushi Takahashi ,  Tadashi Shirai ,  Akio Fujii

发明人： Hamao Umezawa ,  Yasushi Takahashi ,  Tadashi Shirai ,  Akio Fujii

IPC分类号： C07K9/00

CPC分类号： C07K9/003 ,  Y10S435/866 ,  Y10S435/886 ,  Y10S435/911 ,  Y10S435/929

摘要： A process for preparing bleomycinic acid having a melting point of 228.degree.-230.degree. C. (decomposition) and an analysis of C: 40.80%, H: 5.29%, N: 16.45%, O: 24.78%, S: 4.53%, Cl: 3.37%, and Cu: 4.78% which is characterized by being soluble in water, difficultly soluble in methanol, acetic acid and dimethylsulfoxide, and insoluble in ethanol, ethyl acetate, acetone and ether, and which tests positive to Pauly and Ehrlich reactions but tests negative to ninhydrin, Sakaguchi, Dragendorf, Tollens, ferric chloride, Fehling and Molish reactions, and which has a maximum ultraviolet absorption spectrum at 246 m.mu. and 292 m.mu. and which has an infrared absorption spectrum bands at 3350, 1720, 1670, 1640, 1580, 1460, 1365, 1050, 770 (cm.sup.-1), and which can be hydrolyzed to yield 2'-(2-aminoethyl)-2,4'-bithiazole-4-carboxylic acid, L-threonine, 4-amino-3-hydroxy-2-methyl-.eta.-valeric acid, .beta.-hydroxy-histidine, .beta.-amino-.beta.-(4-amino-6-carboxy-5-methylpyrimidine-2-yl)-propionic acid, L-.beta.-amino-alanine, L-gulose and 3-O-carbamoyl-D-mannose, which comprises hydrolyzing bleomycin in the presence of a mycelium mass or enzyme.

公开(公告)号：US4070458A

公开(公告)日：1978-01-24

申请号：US738212

申请日：1976-11-03

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Takaaki Aoyagi ,  Akira Takamatsu ,  Taiji Inui ,  Hiroshi Tone ,  Hajime Morishama

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Takaaki Aoyagi ,  Akira Takamatsu ,  Taiji Inui ,  Hiroshi Tone ,  Hajime Morishama

IPC分类号： C07K5/02 ,  A61K37/00

CPC分类号： C07K5/02

摘要： A novel physiologically active peptide Val-X-Ala-X, in which X is 4-amino-3-hydroxy-6-methylheptanoic acid, which is prepared from R-Val-Val-X-Ala-X by the action of a microbial enzyme, N-acyl derivatives thereof which are produced by acylating said new peptide, and the processes for producing thereof and the microbial enzyme are disclosed.

摘要翻译： 一种新的生理活性肽Val-X-Ala-X，其中X是4-氨基-3-羟基-6-甲基庚酸，其由R-Val-Val-X-Ala-X通过 公开了通过酰化所述新肽产生的微生物酶及其N-酰基衍生物及其制备方法和微生物酶。

公开(公告)号：US4049497A

公开(公告)日：1977-09-20

申请号：US747470

申请日：1976-12-06

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Masaaki Ishizuka ,  Hiroshi Naganawa

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Shinichi Kondo ,  Masaaki Ishizuka ,  Hiroshi Naganawa

IPC分类号： C07G11/00

CPC分类号： A61K36/06 ,  C07G11/00 ,  Y10S435/886

摘要： There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukema L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).

摘要翻译： 已经公开了两种以前称为MC916-A和MC916-B的新抗生素，现在称为新西霉素A和新霉素B，其是白血病细胞生长的有效抑制剂，例如。 白血病L-1210细胞在小鼠中。 它们通过Frep-P 2452链霉菌（A.T.C.C. 31123）的对照发酵生产。

公开(公告)号：US4024253A

公开(公告)日：1977-05-17

申请号：US674009

申请日：1976-04-05

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Akira Takamatsu ,  Kenji Kayahara

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Akira Takamatsu ,  Kenji Kayahara

IPC分类号： A61K31/235 ,  A61K31/60 ,  A61K31/22

CPC分类号： A61K31/235 ,  A61K31/60

摘要： Compounds having the general formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) and the pharmaceutically acceptable salts and esters thereof exhibit strong activities in inhibiting histidine decarboxylase and xanthine oxidase and are useful for treating elevated histamine and uric acid levels. One example is the compound of the formula ##STR2##

摘要翻译： 具有通式的化合物（R1，R2，R3，R4和R5的含义如下所述），其药学上可接受的盐和酯在抑制组氨酸脱羧酶和黄嘌呤氧化酶中表现出强的活性，并且可用于治疗升高的组胺 和尿酸水平。 一个例子是式“IMAGE”的化合物

公开(公告)号：US4014769A

公开(公告)日：1977-03-29

申请号：US651095

申请日：1976-01-21

申请人： Hamao Umezawa ,  Kenji Maeda ,  Shinichi Kondo

发明人： Hamao Umezawa ,  Kenji Maeda ,  Shinichi Kondo

IPC分类号： C07H19/052 ,  C07H19/16 ,  B01J1/10

CPC分类号： C07H19/16 ,  C07H19/052 ,  Y10S204/901 ,  Y10S204/911

摘要： This invention relates to a process for the preparation of coformycin, 3-(.beta.-D-ribofuranosyl)-6,7,8-trihydroimidazo[4,5-d][1,3]diazepin-8(R)-ol, through a synthetic route from a new derivative of 9.beta.-D-ribofuranosyl-purine and other synthetic intermediates involved in the process and their preparation.

摘要翻译： 本发明涉及一种制备共转霉素3-（β-D-呋喃核糖基）-6,7,8-三氢咪唑并[4,5-d] [1,3]二氮杂-8（R） - 醇的方法， 通过合成路线从9β-D-呋喃核糖基嘌呤和其他合成中间体的新衍生物参与该方法及其制备。

公开(公告)号：US3988315A

公开(公告)日：1976-10-26

申请号：US596682

申请日：1975-07-16

申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Akira Takamatsu ,  Toshikazu Oki

发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Masa Hamada ,  Akira Takamatsu ,  Toshikazu Oki

IPC分类号： C07H15/252 ,  C12P1/06 ,  C12P19/56 ,  C07H17/08

CPC分类号： C07H15/252 ,  Y10S435/886

摘要： New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.

摘要翻译： 新型抗肿瘤剂名为阿沙利霉素A和B，它们是蒽环类苷并抑制各种微生物的生长，例如金黄色葡萄球菌，黄曲霉，牛磺酸棒状杆菌，并抑制小鼠和肝癌中白血病L1210和P388和淋巴瘤6C3HED等动物肿瘤的生长 在大鼠中通过发酵属于链霉菌属（Streptomyces）的微生物来产生，其被命名为马链霉菌（Streptomyces galilaeus）（MA144-M1和ATCC 31133）; 它们通过用于回收抗生素的常规方法从肉汤中回收。

公开(公告)号：US3984390A

公开(公告)日：1976-10-05

申请号：US337575

申请日：1973-03-02

申请人： Hamao Umezawa ,  Akio Fujii ,  Tomohisa Takita ,  Nobuyoshi Shimada

发明人： Hamao Umezawa ,  Akio Fujii ,  Tomohisa Takita ,  Nobuyoshi Shimada

IPC分类号： C12P21/00 ,  A61K35/74 ,  A61K38/00 ,  C07D277/56 ,  C07H15/26 ,  C07K9/00 ,  C12P1/06 ,  C12P19/58 ,  C12R1/465 ,  C07C103/52

CPC分类号： C07K9/003 ,  Y10S435/886 ,  Y10S930/19

摘要： By adding a specific amine in culturing under aerobic conditions actinomycetales capable of producing phleomycin group antibiotics, which have been inoculated into a nutrient medium to produce antitumor phleomycin group antibiotics, it is possible to obtain specific phleomycin group antibiotics having a side chain structure corresponding to said amine. The phleomycin group antibiotics thus produced are collected from the culture medium in a conventional way.

摘要翻译： 通过在需氧条件下培养特定的胺，其能够产生已经接种到营养培养基中以产生抗腐霉素腐霉素组抗生素的福来霉素组抗生素的放线菌素，可以获得具有对应于所述抗生素的侧链结构的特定的腐草霉素组抗生素 胺。 以常规方式从培养基中收集由此产生的腐草霉素组抗生素。