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11. 发明授权

US4410516A 1-N(.alpha.Hydroxy-.omega.-aminoalkanoyl) derivatives of 5,3',4'-trideoxy- or 5,3', 4'-trideoxy-6'-N- methyl- or 5, 3', 4',6"-tetradeoxykannamyci B and production thereof 失效
标题翻译： 5,3'，4'-三脱氧 - 或5,3'，4'-三脱氧-6'-N-甲基或5,3'，4'的1-N（α羟基 - ω-氨基烷酰基）衍生物 6“ - 四脱氧ci ci ci B及其生产
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.

12. 发明授权

US4359572A Process for the production of 3'-deoxykanamycin A and intermediate product 失效
标题翻译：制备3'-脱氧卡那霉素A和中间产物的方法
公开(公告)号：US4359572A
公开(公告)日：1982-11-16
申请号：US256131
申请日：1981-04-21
申请人： Hamao Umezawa , Sumio Umezawa , Shunzo Fukatsu , Toshio Yoneta
发明人： Hamao Umezawa , Sumio Umezawa , Shunzo Fukatsu , Toshio Yoneta
IPC分类号： C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： 3'-Deoxykanamycin A useful as an antibacterial agent can be produced by a new process comprising reacting a 2',2"-di-O-acylated-3'-O-sulfonylated-tetra-N-protected derivative of kanamycin A with a base such as alkali metal alcoholate in a lower alkanol to effect 2',3'- and 3',4'-epoxidation and concurrently removal of the 2'- and 2"-acyl groups, reducing the resultant N-protected 2',3'-anhydro-3'-epi derivative and 3',4'-anhydro-3'-epi derivative of kanamycin A either with hydrogen in the presence of a known hydrogenation catalyst or with sodium borohydride to afford the corresponding N-protected 3'-deoxygenated derivative of kanamycin A and then removing the residual amino-protecting groups therefrom to give 3'-deoxykanamycin A.
摘要翻译：可用作抗菌剂的3'-脱氧卡那霉素A可以通过新的方法制备，包括使卡那霉素A的2'，2“ - 二-O-酰化-3'-O-磺酰化四-N-保护的衍生物与碱如碱金属醇化物在低级链烷醇中进行2'，3'和3'，4'-环氧化并同时去除2'-和2“ - 酰基，将所得N-保护的2 '，3'-脱水-3'-外延衍生物和卡那霉素A的3'，4'-脱氢-3'-epi衍生物，与已知氢化催化剂或硼氢化钠存在下的氢气反应，得到相应的N- 保护的卡那霉素A的3'-脱氧衍生物，然后从其中除去残留的氨基保护基，得到3'-脱氧卡那霉素A.

13. 发明授权

US4357466A Processes for the production of 3'-deoxykanamycin A and intermediates 失效
标题翻译：制备3'-脱氧卡那霉素A和中间体的方法
公开(公告)号：US4357466A
公开(公告)日：1982-11-02
申请号：US198612
申请日：1980-10-20
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomo Jikihara
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomo Jikihara
IPC分类号： C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234
摘要： 3'-Deoxykanamycin A useful as antibacterial agent is produced from a protected kanamycin A derivative either by a process comprising imidazolylthiocarbonylation of the 3'- and 2"-hydroxyl groups of 4",6"-O-cyclohexylidene-4'-0:6'-N-carbonyl-5,2'-O-isopropylidene-1,3,3"-tri-N-tosylkanamycin A, preferential removal of the 3'-imidazolylthiocarbonyloxy group with tributyltin hydride for the 3'-deoxygenation, followed by removal of the 2"-O-imidazolylthiocarbonyl group with aqueous ammonia, removal of the N-tosyl groups with alkali or alkaline earth metal in liquid ammonia, hydrolytic fission of the 4',6'-cyclic carbamate ring and concurrent removal of the 5,2'-O-isopropylidene group and 4",6"-O-cyclohexylidene group, or by a process comprising selective acetylation of the 2"-hydroxyl group of said protected kanamycin A derivative with acetyl chloride in pyridine, trifluoromethanesulfonylation of the 3'-hydroxyl group, followed by concurrent removal of the 3'-trifluoromethanesulfonyloxy group and N-tosyl groups with alkali metal in liquid ammonia, removal of the 2"-O-acetyl group concurrently with hydrolytic fission of 4',6'-cyclic carbamate, and hydrolytic removal of the 5,2'-O-isopropylidene and 4",6"-O-cyclohexylidene groups.
摘要翻译：可用作抗菌剂的3'-脱氧卡那霉素A由受保护的卡那霉素A衍生物制备，其通过包含4'，6“-O-亚环己基-4'的3'和2” - 羟基的咪唑基硫代羰基化的方法制备， -0：6'-N-羰基-5,2'-O-异亚丙基-1,3,3“ - 三-N-甲苯磺酰基卡那霉素A，优选用三丁基氢化锡将3'-咪唑硫基羰基氧基除去3' 脱氧，然后用氨水除去2“-O-咪唑基硫代羰基，在液氨中用碱金属或碱土金属除去N-甲苯磺酰基，4'，6'-环状氨基甲酸酯环的水解裂变并且同时去除5,2'-O-异亚丙基和4“，6”-O-亚环己基，或通过包括将所述受保护的卡那霉素A衍生物的2'-羟基选择性乙酰化的方法与吡啶中的乙酰氯，3'-羟基的三氟甲磺酰化，然后同时除去3'-三氟甲磺酸氧基和N-甲苯磺酰基与液氨中的碱金属反应，与4'，6'-环状氨基甲酸酯的水解裂解同时除去2'-乙酰基，并除去5,2'-O 异亚丙基和4“，6”-O-亚环己基。

14. 发明授权

US4326054A Cleomycins and process for producing same 失效
标题翻译：克莱霉素及其生产方法
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。

15. 发明授权

US4297485A Production of a selectively protected N-acylated derivative of an aminoglycosidic antibiotic 失效
标题翻译：制备氨基糖苷类抗生素的选择性保护的N-酰化衍生物
公开(公告)号：US4297485A
公开(公告)日：1981-10-27
申请号：US90591
申请日：1979-11-02
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi , Tomo Jikihara
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yasushi Takagi , Tomo Jikihara
IPC分类号： C07H15/234 , C07H23/00 , C07H15/22
CPC分类号： C07H23/00 , C07H15/234
摘要： Aminoglycosidic antibiotic comprising a 6-0-(3"-aminoglycosyl)-2-deoxystreptamine optionally having a 4-0-(aminogycosyl) group, such as kanamycins, gentamicins, sisomicin, forms reversible complex with zinc cations by association of the zinc cations with some pairs of aminohydroxyl groups in the aminoglycoside, and the zinc-complexed amino groups are blocked from acylation. Reaction of this zinc complex with an acylation reagent having an amino-blocking acyl group brings about acylation of the non-complexed amino groups to give an N-acylated zinc complex, namely a complex of zinc cation with an N-acylated aminoglycosidic antibiotic derivative. Removal of zinc cations from N-acylated zinc complex yields a partially N-acylated aminoglycosidic antibiotic where 1- and 3"-amino groups are unprotected but all other amino groups protected with acyl group. Further reaction of this partially N-acylated product with a certain alkanoic acid or N-formyl-imidazole results in preferential acylation of 3"-amino group without 1-amino group being acylated, affording a 1-N-unprotected and other N-fully-protected derivative of the aminoglycosidic antibiotic which is valuable to be 1-N-acylated with .alpha.-hydroxy-.omega.-aminoalkanoic acid for high-yield production of known semi-synthetic 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-aminoglycosidic antibiotic.
摘要翻译：包含任选具有4-0-（氨基糖基）基团的6-0-（3“ - 氨基糖基）-2-脱氧神经胺的氨基糖苷类抗生素，如卡那霉素，庆大霉素，西索米星，与锌阳离子形成与锌阳离子的可逆复合物，在氨基糖苷中具有一对氨基羟基的阳离子和锌络合的氨基被封闭以进行酰化。该锌络合物与具有氨基封闭酰基的酰化试剂的反应导致非络合氨基的酰化，得到N-酰化锌络合物，即锌阳离子与N-酰化氨基糖苷类抗生素衍生物的络合物。从N-酰化锌络合物中除去锌阳离子产生部分N-酰化的氨基糖苷类抗生素，其中1-和3“ - 氨基未被保护，但是用酰基保护的所有其它氨基。该部分N-酰化产物与某种链烷酸或N-甲酰基 - 咪唑的进一步反应导致3'-氨基的优先酰化而没有1-氨基被酰化，得到1-N-未保护的和其它N- 氨基糖苷类抗生素的完全保护的衍生物，其有价值的是用α-羟基-ω-氨基链烷酸1-N-酰化，用于高产量生产已知的半合成的1-N-（α-羟基 - ω-氨基烷酰基）氨基糖苷类抗生素。

16. 发明授权

US4281180A Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediated therefor and process for producing them 失效
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.

17. 再颁专利

USRE30413E Bleomycinic acid and process for preparing thereof 失效
标题翻译：博来霉素酸及其制备方法
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.

18. 发明授权

US4195170A 3',4'-Episulfido kanamycin B compounds 失效
标题翻译： 3'，4'-二硫代卡那霉素B化合物
公开(公告)号：US4195170A
公开(公告)日：1980-03-25
申请号：US880401
申请日：1978-02-23
申请人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
发明人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
IPC分类号： C07H15/236 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.
摘要翻译：提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

19. 发明授权

US4147861A 1N-(.alpha.-Hydroxy-.omega.-aminoalkanoyl)- 6'N-methyl-3',4'-dideoxykanamycin B and the production thereof 失效
标题翻译： N - （{60-羟基 - {107-氨基烷酰基）-6 {40 N-甲基-3 {40,4 {40-脱氧卡那霉素B及其制备
公开(公告)号：US4147861A
公开(公告)日：1979-04-03
申请号：US865470
申请日：1977-12-29
申请人： Hamao Umezawa , Kenji Maeda , Shinichi Kondo , Sumio Umezawa
发明人： Hamao Umezawa , Kenji Maeda , Shinichi Kondo , Sumio Umezawa
IPC分类号： C07H15/236 , C07H15/22
CPC分类号： C07H15/234
摘要： A number of 1N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-6'N-methyl-3',4'-dideoxykanamycin B derivatives have been found to possess excellent antibacterial activity against most kanamycin susceptible and resistant organisms. In particular, 1N-(DL-isoseryl)-6'N-methyl-3',4'-dideoxykanamycin B, 1N-(L-isoseryl)-6'-N-methyl-3',4'-dideoxykanamycin B, 1N-(L-4-amino-2-hydroxybutyryl)-6'N-methyl-3',4'-dideoxykanamycin B and 1N-(L-5-amino-2-hydroxyvaleryl)-6'N-methyl-3',4'-dideoxykanamycin B, or an acid addition salt thereof possess these highly desirable attributes.
摘要翻译：已经发现许多1N-（α-羟基 - ω-氨基烷酰基）-6'N-甲基-3'，4'-双脱氧卡那霉素B衍生物对大多数卡那霉素敏感和抗性生物具有优异的抗菌活性。特别是1N-（DL-异丝氨酰基）-6'N-甲基-3'，4'-二脱氧卡那霉素B，1N-（L-异丝氨酰基）-6'-N-甲基-3'，4'-二脱氧卡那霉素B， 1N-（L-4-氨基-2-羟基丁酰基）-6'N-甲基-3'，4'-二脱氧卡那霉素B和1N-（L-5-氨基-2-羟基戊酰基）-6'N-甲基-3 '，4'-双脱氧卡那霉素B或其酸加成盐具有这些非常理想的特性。

20. 发明授权

US4070458A Novel physiologically active peptide and its n-acyl derivatives and processes for producing thereof 失效
标题翻译：新型生理活性肽及其N-酰基衍生物及其制备方法
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。

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