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121. 发明授权

US4062947A Di-N-alkylaminoglycosides, methods for their manufacture and novel intermediates useful therein, method for their use as antibacterial agents and pharmaceutical compositions useful therefor 失效
标题翻译：二-N-烷基氨基糖苷类，其制造方法和可用于其中的新型中间体，其用作抗菌剂的方法和用于其的药物组合物
公开(公告)号：US4062947A
公开(公告)日：1977-12-13
申请号：US706704
申请日：1976-07-19
申请人： John J. Wright , Peter J. L. Daniels , Alan K. Mallams , Tattanahalli L. Nagabhushan
发明人： John J. Wright , Peter J. L. Daniels , Alan K. Mallams , Tattanahalli L. Nagabhushan
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234
摘要： 1,2'-di-N-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and 1,6'-di-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and their acid addition salts are valuable as antibacterial agents. Also disclosed are 2'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents which are also useful as intermediates in the preparation of the 1,2'-di-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols. Preferred compounds of this invention include 1,2'-di-N-ethylsisomicin and 1,6'-di-N-ethylsisomicin.
摘要翻译： 1,2'-二-N-4,6-di-O-（氨基糖基）-1,3-二氨基二醇和1,6'-二-N-烷基-4,6-二-O-（氨基糖基） - 1,3-二氨基环己醇及其酸加成盐作为抗菌剂是有价值的。还公开了2'-N-烷基-4,6-二-O-（氨基糖基）-1,3-二氨基环糊精抗菌剂，它们也可用作制备1,2'-二-N-烷基 -4,6-二-O-（氨基糖基）-1,3-二氨基二醇。本发明优选的化合物包括1,2'-二-N-乙基缩丙基in嗪和1,6'-二-N-乙基sis麻素。

122. 发明授权

US4000261A 5-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, methods for their manufacture and intermediates useful therein, methods for their use as antibacterial agents and compositions useful therefor 失效
标题翻译： 5-EPI-4,6-DI-O-（氨基甲酰基）-2-脱氧酪氨酸蛋白酶，其制备方法及其有用的中间体，其用作抗细菌剂及其组合物的方法
公开(公告)号：US4000261A
公开(公告)日：1976-12-28
申请号：US611289
申请日：1975-09-08
申请人： Peter J. L. Daniels
发明人： Peter J. L. Daniels
IPC分类号： C07H15/234 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/22 , C07H15/234 , C07H15/236
摘要： 5-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines and 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein amino and hydroxyl functions are protected by groups susceptible to reductive cleavage or to basic or mild acid hydrolysis, by the reaction thereof with dimethylformamide at elevated temperatures, followed by removal of the protecting groups. Alternatively, 5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines and their 1-N-alkyl derivatives are prepared by oxidation of the corresponding 4,6-di-O-(aminoglycosyl)-2-deoxystreptamine wherein the amino and hydroxyl functions other than the 5-hydroxyl function are protected by groups susceptible to reductive cleavage or to basic or mild acid hydrolysis, with ruthenium tetroxide, chromic acid in acetone or chromium trioxide-pyridine complex in methylene chloride, thence reaction of the thereby produced 5-dehydro-4,6-di-O-(aminoglycosyl)-2-deoxystreptamine or 1-N-alkyl derivative thereof (novel intermediates) with an alkali metal borohydride followed by removal of the amino and hydroxyl protecting groups.In addition to the foregoing, methods are described whereby the 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines are prepared from the corresponding 1-N-unsubstituted-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines.Pharmaceutical compositions comprising 5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines or 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines elicit an antibacterial response in a warm blooded animal having a susceptible bacterial infection.

123. 发明授权

US3960838A Mercaptopseudodisaccharides 失效
标题翻译：巯基假二糖
公开(公告)号：US3960838A
公开(公告)日：1976-06-01
申请号：US518428
申请日：1974-10-29
申请人： David J. Cooper , John R. E. Hoover , Jerry A. Weisbach
发明人： David J. Cooper , John R. E. Hoover , Jerry A. Weisbach
IPC分类号： C07H15/234 , C07H15/224 , C07H15/00
CPC分类号： C07H15/224 , Y02P20/55
摘要： Novel pseudodisaccharide compounds which are related to neamine are prepared. These compounds have a mercapto group or a derivative thereof at position 3 or 4 of the glucose moiety of neamine. The compounds have antibacterial activity and have utility as intermediates to pseudotrisaccharides.
摘要翻译：制备与新胺相关的新型伪二糖化合物。这些化合物在神经胺的葡萄糖部分的3位或4位具有巯基或其衍生物。该化合物具有抗菌活性，可作为假三糖的中间体。

124. 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。

125. 发明授权

US3753973A The preparation of 3'-4'-dideoxykanamycin b active against resistant bacteria 失效
标题翻译：活性抗体细菌活化的3'-4'-二羟基卡那霉素B的制备
公开(公告)号：US3753973A
公开(公告)日：1973-08-21
申请号：US3753973D
申请日：1971-06-02
申请人： MICROBIAL CHEM RES FOUND
发明人： UMEZAWA S , UMEZAWA H , TSUCHIYA T
IPC分类号： C07H15/234 , A61K20060101 , B01J21/00 , B01J23/40 , C07H15/22 , C07C47/18
CPC分类号： C07H15/234
摘要： SYNTHESIS OF 3''-4''-DIDEOXYKANAMYCIN B WHICH COMPRISES PROTECTING THE AMINO AND ALL OR A PART OF THE HYDROXYL GROUPS OTHER THAN 3'' AND 4''-HYDROXYL GROUPS OF KANAMYCIN B, SULFONYLATING 3''- AND 4''-HYDROXYL GROUPS TO GIVE A DERIVATIVE HAVING DISULFONIC ESTER GROUPS, REMOVING SAID ESTER GROUPS TO GIVE 3''-4''-UNSATURATED COMPOUND, REDUCING SAID COMPOUND AND FINALLY REMOVING THE RESIDUAL PROTECTING GROUPS.

126. 发明授权

US2967177A Process of antibiotic purification 失效
标题翻译：抗生素纯化方法
公开(公告)号：US2967177A
公开(公告)日：1961-01-03
申请号：US72482258
申请日：1958-03-31
申请人： BRISTOL MYERS CO
发明人： JOHNSON DAVID A , HARDCASTLE JR GLENN A
IPC分类号： C07H15/234
CPC分类号： C07H15/234

127. 发明授权

US12110310B2 Amphiphilic kanamycin compositions and methods 有权
公开(公告)号：US12110310B2
公开(公告)日：2024-10-08
申请号：US17157752
申请日：2021-01-25
申请人： Cheng-Wei Tom Chang , Jon Y Takemoto
发明人： Cheng-Wei Tom Chang , Jon Y Takemoto
IPC分类号： C07H15/23 , A61K31/7036 , A61P31/04 , C07H15/234
CPC分类号： C07H15/23 , A61K31/7036 , A61P31/04 , C07H15/234
摘要： The present relates to novel bioactive amphiphilic kanamycin compounds having the general formula of:

where R may be a C4 to C20 branched or straight chained alkyl group or a substituted or unsubstituted aryl group. Also provided are methods of synthesizing and methods of using the compounds of the present invention. The compounds of the present invention are useful in treating and preventing various fungal and bacterial diseases.

128. 发明授权

US12084472B2 Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists 有权
公开(公告)号：US12084472B2
公开(公告)日：2024-09-10
申请号：US17185653
申请日：2021-02-25
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Michael Robert Leadbetter , Jeremy Caldwell , Dean Dragoli , Noah Bell , Jeffrey W. Jacobs , Patricia Finn , Rakesh Jain , Tao Chen , Matthew Siegel
IPC分类号： A61K31/444 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K31/706 , A61K45/06 , C07B59/00 , C07C409/12 , C07D213/30 , C07D213/38 , C07D213/80 , C07D213/81 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07H15/04 , C07H15/18 , C07H15/234 , C07H15/26
CPC分类号： C07H15/26 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K31/706 , A61K45/06 , C07B59/002 , C07C409/12 , C07D213/30 , C07D213/38 , C07D213/80 , C07D213/81 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07H15/04 , C07H15/18 , C07H15/234 , C07B2200/05
摘要： The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula:

where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.

129. 发明授权

US11813588B2 Chromatographic material having improved pH stability, method for preparation thereof and uses thereof 有权
公开(公告)号：US11813588B2
公开(公告)日：2023-11-14
申请号：US17146447
申请日：2021-01-11
申请人： DIONEX CORPORATION
发明人： Xiaodong Liu , Xiao Cui , Xuefei Sun
IPC分类号： B01D15/20 , B01D15/32 , B01J20/289 , B01J20/32 , C07H15/23 , C07H15/232 , C07H15/234 , C07H15/238 , B01J20/287 , B01J20/30 , C07D493/04 , C07H1/06 , C07H15/224 , C08G77/392
CPC分类号： B01J20/287 , B01D15/20 , B01D15/325 , B01J20/289 , B01J20/3078 , B01J20/3092 , B01J20/3204 , B01J20/328 , B01J20/3217 , B01J20/3272 , C07D493/04 , C07H1/06 , C07H15/224 , C07H15/23 , C07H15/232 , C07H15/234 , C07H15/238 , C08G77/392 , B01J2220/44 , B01J2220/52 , B01J2220/54 , B01J2220/58
摘要： A chromatographic material including a substrate having a surface and having a polymeric layer covalently bound to the surface; the polymeric layer comprising polymer molecules covalently attached to the surface of the substrate, each polymer molecule being attached to the surface via multiple siloxane bonds and each polymer molecule being connected to one or more functionalizing compounds that each comprise a functional group, wherein the polymeric layer is formed by covalently attaching polymer molecules to the surface of the substrate via multiple siloxane bonds, each polymer molecule containing multiple first reactive groups, and reacting the first reactive groups of the attached polymer molecules with at least one functionalizing compound that comprises a second reactive group that is reactive with the first reactive groups and that further comprises a functional group. Preferred conditions of reacting the polymer with the substrate include elevated temperature and reduced pressure.

130. 发明申请

US20220306672A1 SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS 有权
公开(公告)号：US20220306672A1
公开(公告)日：2022-09-29
申请号：US17185653
申请日：2021-02-25
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Michael Robert Leadbetter , Jeremy Caldwell , Dean Dragoli , Noah Bell , Jeffrey W. Jacobs , Patricia Finn , Rakesh Jain , Tao Chen , Matthew Siegel
IPC分类号： C07H15/26 , A61K31/4418 , C07D213/38 , A61K31/4427 , C07D405/12 , A61K31/443 , A61K31/444 , C07D213/30 , C07D405/04 , A61K31/4433 , A61K31/4439 , C07D413/12 , A61K31/553 , A61K31/496 , A61K31/706 , C07H15/04 , C07H15/18 , C07D401/12 , A61K31/5377 , C07H15/234 , A61K31/4436 , C07D409/12 , A61K31/4545 , A61K31/506 , A61K31/4425 , A61K31/551 , C07D471/04 , C07B59/00 , C07D213/81 , C07D213/80 , C07D487/08 , A61K45/06 , C07C409/12
摘要： The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.

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