| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 61 | SEMI-SYNTHETIC REARRANGED VANCOMYCIN/DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY | PCT/US2006007021 | 2006-02-27 | WO2006093933A3 | 2007-03-08 | CHU DANIEL; NI ZHI-JIE; WANG JOHN JIAN-XIN; LEI YAOHUI; BAI YU |
| Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections. | ||||||
| 62 | MULTIDRUG RESISTANT ANTICANCER ANTHRACYCLINES | PCT/US2006018630 | 2006-05-12 | WO2006124720B1 | 2007-01-18 | ZHANG GUISHENG; FANG LANYAN; WANG PENG GEORGE; SUN DUXIN |
| Daunorubicin ("DNR") compounds synthesized with uncommon sugars exhibit enhanced effectiveness in treating various drug-resistant cancers. | ||||||
| 63 | METHOD FOR MAXIMIZING EFFICACY AND PREDICTING AND MINIMIZING TOXICITY OF CALCINEURIN INHIBITOR COMPOUNDS | PCT/IB2005/003980 | 2005-07-14 | WO2006033024A3 | 2006-03-30 | MAYO, Patrick, Rogers |
The invention provides methods for predicting toxicity related to calcineurin inhibition therapy by measuring the peak concentration of drug and the trough concentration of the drug, calculating a peak-trough fluctuation, and comparing this peak-trough fluctuation to known values to predict if the patient will exhibit calcineurin-inhibition therapy-related toxicity. The invention also provides methods for monitoring drug levels to ensure that a patient receiving calcineurin inhibition therapy remains within a therapeutic window which maximizes the efficacy and minimizes the toxicity of the calcineurin inhibitor. The invention also provides dosage methods which maximize the peak concentration, minimize the trough concentration, and maximize the fluctuation between peak and trough concentration of calcineurin inhibitors, to maximize the efficacy of the calcineurin inhibition therapy, and minimize the risk of developing calcineurin-inhibition therapyrealted toxicity. This dose regimen, which may be a once-daily dose regimen, maximizes efficacy associated with peak concentrations of drug and minimizes toxicity by maximizing the peak-trough fluctuation, a measurement determined to be associated with toxicity. Calcineurin inhibitors useful for these methods include members of the cyclosporin family of compounds, including cyclosporin A and ISA247, FK506, pimecrolimus and ascomycin. |
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| 64 | SIXTEEN-MEMBERED MACROLIDE ANTIINFECTIVE AGENTS | PCT/US2005/024598 | 2005-07-12 | WO2006017250A3 | 2006-02-16 | FU, Hong; KATZ, Leonard; MYLES, David, C. |
Sixteen membered macrolide anti-infective agents having a structure according to formula (I) where R1, R2, R3, R4, R5, and R6 are as defined herein, and related compounds are disclosed. |
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| 65 | CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF | PCT/US2003/004609 | 2003-02-14 | WO2003070174A3 | 2003-08-28 | BURNET, Michael; GUSE, Jan-Hinrich; GUTKE, Hans-Jurgen; BECK, Albert; TSOTSOU, Georgia; DROSTE-BOREL, Irina; REICHERT, Jeannette; LUYTEN, Kattie; BUSCH, Maximilian; WOLFF, Michael; KHOBZAOUI, Moussa; MARGUTTI, Simona; MEINDL, Thomas; KIM, Gene; BARKER, Laurence |
This invention features a compound of the following formula T-(-L-C)m, wherein T is a transportophore (a transport mediating molecule), L is a a non-antibiotic therapeutic agent, and m is l- 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2. Figure 1 depicts comparison of selective uptake of diverse structure types into white blood cells from a complex blood mix. |
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| 66 | SOLUTION AND SOLID PHASE SULFOXIDE GLYCOSYLATION: SYNTHESIS OF beta -LINKED OLIGOSACCHARIDES USING 2-DEOXY-2-N-TRIFLUOROACETAMIDO-GLYCOPYRANOSYL DONORS | PCT/US1999/002180 | 1999-02-03 | WO99039201A1 | 1999-08-05 | |
| The invention relates to a process for the synthesis of beta -oligosaccharides. beta -oligosaccharides are synthesized using alkylsulfenyl- or an arylsulfenyl-2-deoxy-2-N-trifluoroacetamidoglycopyranoses as glycosyl donors via the sulfoxide glycosylation, both in solution and solid phases. Once activated under the glycosylation conditions, these donors afford the respective beta -glycosides exclusively and in high yield. Since the trifluoroacetamido group is easily removed under mild conditions, the corresponding amino group can be appropriately derivatized, even in the presence of unprotected hydroxyl groups. Disaccharide libraries are designed, constructed and analyzed. The invention also relates to a process for synthesizing the glycosyl donor. | ||||||
| 67 | CYCLOPEPTOLIDES | PCT/JP1998/005716 | 1998-12-17 | WO99031127A1 | 1999-06-24 | |
| Cyclopeptolides, cyclo(-2-hydroxyisovaleryl-Hpr-MeVal-Val-MeAsp-MeIle-MeIle-Gly-MeVal-T yr(OMe)-) and cyclo(-2-hydroxyisovaleryl-Hpr-Val-Val-MeAsp-MeIle-MeIle-Gly-MeVal-Tyr (OMe)-), produced by a mold of the genus Clavariopsis and having a potent antifungal activity. | ||||||
| 68 | PROCESS FOR THE PREPARATION OF ANTIBIOTICS 10381B | PCT/US8701450 | 1987-06-25 | WO8800200A3 | 1988-04-21 | ARGOUDELIS ALEXANDER D; SHILLIDAY FRANKLIN B; LABORDE ALICE L; TRUESDELL SCOTT E |
| Novel process for the preparation of the antibiotics 10381b and to a method of using antibiotics 10381b to promote growth in meat-producing animals. These antibiotics are obtained by the fermentation of a nutrient medium with the novel microorganism Streptomyces arginensis. | ||||||
| 69 | ANTIBIOTIC TAN-588, PROCESS FOR ITS PREPARATION, AND NOVEL SPECIES BELONGING TO THE GENIUS EMPEDOBACTER | PCT/JP1984000222 | 1984-04-27 | WO1985005109A1 | 1985-11-21 | TAKEDA CHEMICAL INDUSTRIES, LTD.; ONO, Hideo; NOZAKI, Yukimasa; HARADA, Setsuo |
| Antibiotic TAN-588 produced by a bacterium belonging to the genus Empedobacter, and its salt have an antibacterial effect on gram-positive and gram-negative bacteria, and are used for treating bacteria-induced diseases of mammals, poultry, etc. | ||||||
| 70 | AB-011 항생제 및 그의 제조방법 | KR1019890008222 | 1989-06-14 | KR1019970010955B1 | 1997-07-05 | 눈지오안드리올로; 다니엘라톨렌티노; 기오르기오카싸니; 기오르기오보르고노비; 마르코빈센티; 실비아스페라; 루이기미렌나; 기오르기오피랄리; 기오반니콘팔로니에리 |
| The AB-011 antibiotics and the main components thereof, AB-011a and AB-011b, obtained by means of the controlled aerobic cultivation of Streptomyces s.p. NCIB 12629 in an aqueous nutrient cultivation medium, are disclosed. Said antibiotics show biological activity, in particular antifungal activity. | ||||||
| 71 | 항생물질 버미스포린, 그의 제조방법 및 그것을 활성 항균제로서 포함하는 약제 조성물 | KR1019880009774 | 1988-07-29 | KR1019950004181B1 | 1995-04-27 | 미까와다까시; 다까하시노리꼬; 오끼시하루유끼; 사또요시까즈; 미야도신지; 세자끼마사지 |
| 내용 없음. | ||||||
| 72 | 항생제 10381b의 제조방법 | KR1019880700236 | 1987-06-25 | KR1019950001704B1 | 1995-02-28 | 알렉잰더디이아르고우델리스; 프랭클린비이쉴리데이; 엘리스엘라보오드; 스콧트이이트루에스델 |
| Novel process for the preparation of the antibiotics 10381b and to a method of using antibiotics 10381b to promote growth in meat-producing animals. These antibiotics are obtained by the fermentation of a nutrient medium with the novel microorganism Streptomyces arginensis. | ||||||
| 73 | 항생제LL-E19020알파및베타,그제조방법및이를이용한동물감염의방지또는조절법 | KR1019870006817 | 1987-06-30 | KR1019950000983B1 | 1995-02-06 | 가이토마스카아터; 마이클그린슈타인; 조지프제이콥굿맨; 도널드브루스보더즈; 윌리엄마이클메이즈; 레이몬드토마스테스타; 어윈보이든웃드; 메리율러즈도우셔; 시드니캔터; 로버트리이케닛트쥬니어 |
| This invention relates to antibiotic LL-E19020 alpha and LL-E19020 beta derived from the microorganism Streptomyces lydicus subspecies tanzanius NRRL 18036, which are useful as an antibacterial agent. The antibiotics LL-E19020 alpha and LL-E19020 beta are also growth promoters, antiprotozoan agents and anthelmintic agents. | ||||||
| 74 | 항생물질 버미스포린, 그의 제조방법 및 그것을 활성 항균제로서 포함하는 약제 조성물 | KR1019880009774 | 1988-07-29 | KR1019900001713A | 1990-02-27 | 미까와다까시; 다까하시노리꼬; 오끼시하루유끼; 사또요시까즈; 미야도신지; 세자끼마사지 |
| 내용 없음 | ||||||
| 75 | AB-011 항생제 및 그의 제조방법 | KR1019890008222 | 1989-06-14 | KR1019900000480A | 1990-01-30 | 눈지오안드리올로; 다니엘라톨렌티노; 기오르기오카싸니; 기오르기오보르고노비; 마르코빈센티; 실비아스페라; 루이기미렌나; 기오르기오피랄리; 기오반니콘팔로니에리 |
| 내용 없음 | ||||||
| 76 | 살균독소 및 뿌리 부패 및 입고병을 억제하는 방법 및 접종물 | KR1019880009388 | 1988-07-26 | KR1019890002210A | 1989-04-10 | 조핸델스맨; 래리제이핼버슨; 필립제이밸랜딕 |
| 내용 없음 | ||||||
| 77 | 항생제 10381b의 제조방법 | KR1019880700236 | 1987-06-25 | KR1019880701727A | 1988-11-04 | 알렉잰더디이아르고우델리스; 프랭클린비이쉴리데이; 엘리스엘라보오드; 스콧트이이트루에스델 |
| 내용 없음 | ||||||
| 78 | 항생제LL-E19020알파및베타,그제조방법및이를이용한동물감염의방지또는조절법 | KR1019870006817 | 1987-06-30 | KR1019880000457A | 1988-03-26 | 가이토마스카아터; 마이클그린슈타인; 조지프제이콥굿맨; 도널드브루스보더즈; 윌리엄마이클메이즈; 레이몬드토마스테스타; 어윈보이든웃드; 메리율러즈도우셔; 시드니캔터; 로버트리이케닛트쥬니어 |
| 내용 없음 | ||||||
| 79 | 글리코펩타이드 바이오컨버전 생성물의 제조방법 | KR1019840006507 | 1984-10-19 | KR1019860001281B1 | 1986-09-05 | 글래디스마리클렘; 래번드와인보에크; 마리테레세앤더슨; 카알해인즈마이클 |
| New antibacterial actaplanin derivs. of formula(I) [W=residue of actaplanin factors A,B1,B2,B3,C1aC2aD1,D2,E1,G,K,L,M,N or O or of actaplanin pseudoaglycone! and their salts were prepd. by bioconversion of actaplanin(s) A to O and its pseudoaglycone. In each of the parent actaplanin derivs. the CO gp. marked by an asterisk is replaced by CH(NH2). In bioconversion, New Actinoplanes missouriensis strains NRRL15647 and 15646 is used for cosynthesis of antibiotic CUC/CSX. (I) are antibacterials esp. effective against Gram-positive bacteria and they increase feed utilisation efficency in animals and improve milk prodn. in lactating ruminants. | ||||||
| 80 | N-아실 글리코펩타이드 유도체의 제조방법 | KR1019840006505 | 1984-10-19 | KR1019860001280B1 | 1986-09-05 | 매뉴엘데보노 |
| New glycopeptide derivs. of formula(I) and their salts were prepd. by reacting A35512 or actaplanin factors etc. with acylating agents. W=residue of glycopeptide antibiotics of formula (II) and selected from A35512 factors A to H, actaplanin factors A to O, A47934, A41030 factors A to G, etc. R=acyl gps. which is selected from formula(a) ,(b),(c) (R1=H, halo, C1-4 alkyl, C3-8 cycloallkyl etc.) R1 and the contg. alkyl gps. -(CH2)m- and -(CH2)n- are opt. substd. by > 1 halo, Me, MeO etc.; X=O,S,-C=C-, -C(CH3)=C(CH3)-; R2=H, C1-18 alkyl or C2-18 alkenyl; A=divalent O,S, etc.; A1=divalent O,S,sulfinyl etc.; Y=H,Cl,Br,I,N,C1-3 alkyl, OH, and etc.). | ||||||
