公开(公告)号：US06750199B2

公开(公告)日：2004-06-15

申请号：US09904756

申请日：2001-07-13

Applicant: William V. Curran ,  Richard A. Leese ,  Howard Jarolmen ,  Donald B. Borders

Inventor： William V. Curran ,  Richard A. Leese ,  Howard Jarolmen ,  Donald B. Borders

IPC: A61K3812

CPC classification number: C07K1/14 ,  A61K38/00 ,  C07K7/06 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60 ,  C07K11/00 ,  C08L23/08 ,  C08L23/0869 ,  C08L51/06 ,  C08L2203/14 ,  C09K3/10 ,  C09K2003/1037 ,  C09K2200/06 ,  C09K2200/062 ,  C09K2200/0622 ,  C08L2666/04 ,  C08L2666/02

Abstract: The present invention provides antimicrobial sulfonamide derivatives of lipopeptide antibiotics, pharmaceutical compositions of antimicrobial sulfonamide derivatives, methods for making antimicrobial sulfonamide derivatives, methods for inhibiting microbial growth with antimicrobial sulfonamide derivatives and methods for treating or preventing microbial infections in a subject with antimicrobial sulfonamide derivatives. Antimicrobial sulfonamide derivatives are generally an amino core antibiotic that has been further modified with a lipophilic sulfonyl group.

Abstract translation: 本发明提供了脂肽抗生素的抗微生物磺酰胺衍生物，抗微生物磺酰胺衍生物的药物组合物，抗微生物磺酰胺衍生物的制备方法，用抗微生物磺酰胺衍生物抑制微生物生长的方法以及用抗微生物磺酰胺衍生物治疗或预防受试者的微生物感染的方法。 抗微生物磺酰胺衍生物通常是已经用亲脂性磺酰基进一步修饰的氨基核心抗生素。

公开(公告)号：US4677071A

公开(公告)日：1987-06-30

申请号：US638189

申请日：1984-08-06

Applicant: May D. Lee ,  John H. Martin ,  Donald B. Borders ,  Raymond C. Yao ,  Raymond T. Testa

Inventor： May D. Lee ,  John H. Martin ,  Donald B. Borders ,  Raymond C. Yao ,  Raymond T. Testa

IPC: C12P1/06 ,  C12N1/20 ,  C12P21/00 ,  C12R1/465

CPC classification number: C12P1/06 ,  Y10S435/886

Abstract: This invention relates to new polypeptide antibiotics designated LL-BO2964.alpha., LL-BO2964.beta., LL-BO2964.gamma., and a mixture thereof designated LL-BO2964, produced during microbiological fermentation, under controlled conditions, using a new strain of Streptomyces coeruleorubidus subspecies rubidus or a mutant thereof. The new antibiotics are active against a variety of microorganisms and are also useful in treating tuberculosis.

Abstract translation: 本发明涉及在微生物发酵过程中，在控制条件下，使用新的菌株Streptomyces coeruleorubidus subspecies rubidus，命名为LL-BO2964α，LL-BO2964β，LL-BO2964γ的新型多肽抗生素及其名称为LL-BO2964的混合物 或其突变体。 新的抗生素对各种微生物有活性，也可用于治疗结核病。

公开(公告)号：US4626503A

公开(公告)日：1986-12-02

申请号：US701831

申请日：1985-02-14

Applicant: May D. Lee ,  Amedeo A. Fantini ,  David P. Labeda ,  William M. Maiese ,  Raymond T. Testa ,  Donald B. Borders

Inventor： May D. Lee ,  Amedeo A. Fantini ,  David P. Labeda ,  William M. Maiese ,  Raymond T. Testa ,  Donald B. Borders

IPC: C07H17/04 ,  C12P1/06 ,  C12P19/60 ,  C12N1/20 ,  C07G11/00 ,  A01N25/26

CPC classification number: C07H17/04 ,  C12P1/06 ,  C12P19/60 ,  C12R1/465

Abstract: Antitumor agents LL-D49194.alpha..sub.1, LL-D49194.beta..sub.1, LL-D49194.beta..sub.2, LL-D49194.beta..sub.3, LL-D49194.gamma., LL-D49194.delta., LL-D49194.epsilon., LL-D49194.xi., LL-D49194.eta., LL-D49194.omega., LL-D49194.omega..sub.2 and LL-D49194.omega..sub.3.

Abstract translation: 抗肿瘤剂LL-D49194α1，LL-D49194β1，LL-D49194β2，LL-D49194β3，LL-D49194γ，LL-D49194δ，LL-D49194ε，LL-D49194 xi，LL-D49194 eta ，LL-D49194欧米加，LL-D49194 omega2和LL-D49194ω3。

公开(公告)号：US4503044A

公开(公告)日：1985-03-05

申请号：US488496

申请日：1983-04-25

Applicant: May D. Lee ,  Donald B. Borders ,  David P. Labeda ,  Amedeo A. Fantini ,  Raymond T. Testa

Inventor： May D. Lee ,  Donald B. Borders ,  David P. Labeda ,  Amedeo A. Fantini ,  Raymond T. Testa

IPC: C07G11/00 ,  A61K35/74 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  C07K5/06 ,  C12P1/04 ,  C12R1/01 ,  A61K37/00 ,  C07C103/52

CPC classification number: C07K5/06026 ,  C12R1/01 ,  A61K38/00

Abstract: This disclosure describes a new antibacterial and anti-tumor agent designated LL-D05139 .beta., produced in a microbiological fermentation under controlled conditions using a new genus Glycomyces harbinensis gen. nov., sp. nov., and mutants thereof.

Abstract translation: 本公开描述了一种名为LL-D05139β的新型抗细菌剂和抗肿瘤剂，其在微生物发酵下，在控制条件下使用新的Glycomyces harbinensis gen。 诺夫山脉 nov。及其突变体。

公开(公告)号：US07868135B2

公开(公告)日：2011-01-11

申请号：US10880442

申请日：2004-06-28

Applicant: Dale R. Cameron ,  Vincent A. Boyd ,  Richard A. Leese ,  William V. Curran ,  Donald B. Borders ,  Paulo W. M. Sgarbi ,  Shirley A. Wacowich-Sgarbi ,  Matthew Nodwell ,  Yuchen Chen ,  Qi Jia ,  Dominique Dugourd

Inventor： Dale R. Cameron ,  Vincent A. Boyd ,  Richard A. Leese ,  William V. Curran ,  Donald B. Borders ,  Paulo W. M. Sgarbi ,  Shirley A. Wacowich-Sgarbi ,  Matthew Nodwell ,  Yuchen Chen ,  Qi Jia ,  Dominique Dugourd

IPC: A61K38/12

CPC classification number: C07K7/56 ,  A61K38/00

Abstract: The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.

Abstract translation: 本发明提供显示抗微生物抗微生物活性的脂肽抗生素衍生物，用于合成这种抗微生物衍生物和类似物的方法和化合物，以及在多种情况下使用该化合物的方法，包括在治疗和预防微生物感染中。

公开(公告)号：US06716962B2

公开(公告)日：2004-04-06

申请号：US09948374

申请日：2001-09-06

Applicant: Donald B Borders ,  Noreen D Francis ,  Amedeo A Fantini

Inventor： Donald B Borders ,  Noreen D Francis ,  Amedeo A Fantini

IPC: C07K114

CPC classification number: C07K11/02 ,  A61K38/00 ,  C07K1/145 ,  C07K7/08 ,  C07K7/56 ,  C07K9/00

Abstract: The present invention provides a rapid and inexpensive method for extractively isolating acidic lipopeptide antibiotics, such as those having a cyclic peptide or cyclic depsipeptide core, in high yield and purity. In particular, there is provided a method of extracting a variety of acidic lipopeptide antibiotics, directly or indirectly, into water immiscible organic solvents by using a divalent cation chelation procedure.

Abstract translation: 本发明提供了以高产率和纯度提取性分离酸性脂肽抗生素（例如具有环肽或环状多肽肽核心的那些）的快速且便宜的方法。 特别地，提供了通过使用二价阳离子螯合方法将各种酸性脂肽抗生素直接或间接地提取到与水不混溶的有机溶剂中的方法。

公开(公告)号：US20080207874A1

公开(公告)日：2008-08-28

申请号：US11630847

申请日：2005-07-01

Applicant: Richard A. Leese ,  Noreen Francis ,  William V. Curran ,  Donald B. Borders ,  Howard Jarolmen

Inventor： Richard A. Leese ,  Noreen Francis ,  William V. Curran ,  Donald B. Borders ,  Howard Jarolmen

IPC: C07K7/64

CPC classification number: C07K5/0815 ,  A61K38/00 ,  C07K5/06086 ,  C07K7/62 ,  C07K7/64 ,  Y02A50/473 ,  Y02P20/55

Abstract: Novel protected cyclopeptide intermediates are prepared from polymyxin B are used to synthesize new peptide antibiotics. Intermediates are readily derivatized and deprotected to provide new families of antibiotics, which have potent anti-bacterial activity against gram-negative bacteria; but also are useful and potent against gram-positive bacteria.

Abstract translation: 由多粘菌素B制备的新型受保护的环肽中间体用于合成新的肽抗生素。 中间体易于衍生化和去保护，以提供新的抗生素家族，其对革兰氏阴性细菌具有有效的抗菌活性; 而且对革兰氏阳性细菌也是有用和有效的。

公开(公告)号：US07138487B2

公开(公告)日：2006-11-21

申请号：US10810741

申请日：2004-03-26

Applicant: Donald B. Borders ,  Noreen D. Francis ,  Amedeo A. Fantini

Inventor： Donald B. Borders ,  Noreen D. Francis ,  Amedeo A. Fantini

IPC: C07K1/14 ,  C07K7/56

CPC classification number: C07K11/02 ,  A61K38/00 ,  C07K1/145 ,  C07K7/08 ,  C07K7/56 ,  C07K9/00

Abstract: The present invention provides a rapid and inexpensive method for extractively isolating acidic lipopeptide antibiotics, such as those having a cyclic peptide or cyclic depsipeptide core, in high yield and purity. In particular, there is provided a method of extracting a variety of acidic lipopeptide antibiotics, directly or indirectly, into water immiscible organic solvents by using a divalent cation chelation procedure.

Abstract translation: 本发明提供了以高产率和纯度提取性分离酸性脂肽抗生素（例如具有环肽或环状多肽肽核心的那些）的快速且便宜的方法。 特别地，提供了通过使用二价阳离子螯合方法将各种酸性脂肽抗生素直接或间接地提取到与水不混溶的有机溶剂中的方法。

公开(公告)号：US06767718B2

公开(公告)日：2004-07-27

申请号：US10142303

申请日：2002-05-10

Applicant: Richard A. Leese ,  William V. Curran ,  Donald B. Borders

Inventor： Richard A. Leese ,  William V. Curran ,  Donald B. Borders

IPC: A61K3815

CPC classification number: C07K11/02 ,  A61K38/00

Abstract: Novel cyclodepsipeptide intermediates have been prepared from the A21978 complex and used to synthesize new lipodepsipeptide antibiotics. The three intermediates can be readily derivatized to give new families of antibiotics that have potent antibacterial activity against gram positive bacteria.

Abstract translation: 已经从A21978复合物制备了新的环缩酚肽中间体，并用于合成新的脂多糖肽抗生素。 三种中间体可以很容易地衍生化，以给新的抗革兰氏阳性菌抗菌活性家族。

公开(公告)号：US06613889B2

公开(公告)日：2003-09-02

申请号：US09935347

申请日：2001-08-23

Applicant: Donald B. Borders ,  William V. Curran

Inventor： Donald B. Borders ,  William V. Curran

IPC: C07H100

CPC classification number: C07H17/08

Abstract: This method is for preparing salts of amphotericin B methyl ester and other polyene macrolide esters. The steps of the process involve methylation by use of cesium carbonate for converting to methyl ester and significantly reducing side products, which are over methylation products. The free base-Schiff base mixture is converted to amphotericin B methyl ester hydrochloride or some other salt form, by using tetrahydrofuran-water to dissolve the mixture for acid treatment to obtain the salt. The aldehyde liberated during salt formation is removed by centrifuging, as to any precipitated aldehyde, and the aldehyde remaining in solution is removed by eluting the solution through a reverse phase adsorbent to obtain amphotericin B methyl ester hydrochloride as a yellow powder.