公开(公告)号：US20230331728A1

公开(公告)日：2023-10-19

申请号：US18332566

申请日：2023-06-09

Applicant: SPERO THERAPEUTICS, INC.

Inventor： Akash JAIN ,  Evan HECKER ,  Richard EDWARDS ,  Thierry BONNAUD

IPC: C07D477/20

CPC classification number: C07D477/20 ,  A61K45/06

Abstract: The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

公开(公告)号：US11718621B2

公开(公告)日：2023-08-08

申请号：US17136759

申请日：2020-12-29

Applicant: SPERO THERAPEUTICS, INC.

Inventor： Akash Jain ,  Evan Hecker ,  Richard Edwards ,  Thierry Bonnaud

IPC: C07D477/20 ,  A61K45/06 ,  A61P31/04

CPC classification number: C07D477/20 ,  A61K45/06 ,  C07B2200/13

Abstract: The disclosure is directed to new crystalline tebipenem pivoxil salt forms, including a crystalline tebipenem pivoxil ethane sulfonate salt form (Form A), a crystalline tebipenem pivoxil ketoglutarate salt form (Form A), tebipenem pivoxil maleate salt forms (Form A and Form B), a tebipenem pivoxil malate salt form (Form A), a tebipenem pivoxil methane sulfonate salt form (Form B), a tebipenem pivoxil hydrobromide salt form (Form B), and a tebipenem pivoxil edisylate salt form (Form A). The disclosure also includes a composition, comprising a crystalline tebipenem pivoxil salt and a pharmaceutically acceptable carrier and further includes a method for treating an antibiotic resistant bacterial infection, comprising administering to a patient in need of such treatment a therapeutically effective amount of a crystalline tebipenem pivoxil salt.

公开(公告)号：US20210188851A1

公开(公告)日：2021-06-24

申请号：US17057594

申请日：2019-05-29

Applicant: VenatoRx Pharmaceuticals, Inc.

Inventor： Christopher J. BURNS ,  Guo-Hua CHU ,  Jodie HAMRICK ,  Steven A. Boyd ,  Stephen M. CONDON

IPC: C07D477/20 ,  A61K45/06 ,  A61K31/407 ,  A61P31/04

Abstract: The present disclosure provides broad-spectrum carbapenem derivatives and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such derivatives and/or compositions.

公开(公告)号：US20200281894A1

公开(公告)日：2020-09-10

申请号：US16879892

申请日：2020-05-21

Applicant: Southern Methodist University ,  University of Central Florida Research Foundation, Inc.

Inventor： John D. Buynak ,  Noora M. S. A. Al-Kharji ,  Weirui Chai ,  Thu Q. Nguyen ,  Maha Alqurafi ,  Kyle Rohde ,  Rashmi Gupta

IPC: A61K31/407 ,  C07D477/06 ,  C07D477/00 ,  A61K45/06 ,  C07D477/04 ,  C07D477/20

Abstract: The present invention includes a composition, method of making and method of using a novel C5-substituted carbapenem antibiotic of formula 1: R1 is H or CH3 R2 is not H, and is CH3, or C1-C6 straight chain, or branched alkyl, or C3-C6 cycloalkyl group, or unsaturated alkenyl, including C═CH2; R3 is H, CH3, or a C1-C6 alkyl or cycloalkyl group, a heteroatom-substituted alkyl; and R4 is a C1 to C6 alkyl, or substituted alkyl group, especially including substituents which possess positive charge, or a hydroxyl group; or R4 is an SRa, where Ra is an unsubstituted C1 to C6 alkyl group, a substituted C1 to C6 alkyl group, or a functional group that is positively charged, or which bears a positive charge when in aqueous solution at pH 7; or R4 is a CH2ORb, where Rb=C1 to C6 alkyl or substituted alkyl groups, substituted or unsubstituted aryl, or a heteroaryl groups.

公开(公告)号：US20200010470A1

公开(公告)日：2020-01-09

申请号：US16509388

申请日：2019-07-11

Applicant: Kala Pharmaceuticals, Inc.

Inventor： Winston Zapanta Ong ,  Pawel Wojciech Nowak ,  Jinsoo Kim ,  Elizabeth M. Enlow ,  James Bourassa ,  Yen Cu ,  Alexey Popov ,  Hongming Chen

IPC: C07D477/20 ,  A61K9/50 ,  A61K9/51 ,  C07D487/04 ,  A61K45/06 ,  A61K31/407

Abstract: The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

公开(公告)号：US09994613B2

公开(公告)日：2018-06-12

申请号：US15288863

申请日：2016-10-07

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Marion W. Wannamaker ,  Robert J. Davies

IPC: C07K5/062 ,  A61K38/00 ,  A61P17/00 ,  C07K5/06 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/02 ,  C07K5/08 ,  C07D207/16 ,  C07K5/083

CPC classification number: C07K5/06034 ,  A61K38/00 ,  C07D207/16 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/06008 ,  C07K5/06191 ,  C07K5/08 ,  C07K5/0808 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/475

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

公开(公告)号：US20160083760A1

公开(公告)日：2016-03-24

申请号：US14860103

申请日：2015-09-21

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： CRAIG ARTHUR TOWNSEND ,  MICAH JEFFREY BODNER ,  RYAN MARTIN PHELAN ,  MICHAEL FRANCIS FREEMAN

IPC: C12P17/10 ,  C07D477/20

CPC classification number: C12P17/10 ,  C07D477/20 ,  C12P17/184

Abstract: The presently disclosed subject matter demonstrates that ThnG and ThnQ enzymes encoded by the thienamycin gene cluster in Streptomyces cattleya oxidize the C-2 and C-6 moieties of carbapenems, respectively. ThnQ stereospecifically hydroxylates PS-5 giving N-acetyl thienamycin. ThnG catalyzes sequential desaturation and sulfoxidation of PS-5, giving PS-7 and its sulfoxide. The ThnG and ThnQ enzymes are relatively substrate selective, but give rise to the oxidative diversity of carbapenems produced by S. cattleya, and orthologues likely function similarly in allied streptomyces.

Abstract translation: 目前公开的主题表明，由链霉菌链霉菌中的噻吩霉素基因簇编码的ThnG和ThnQ酶分别氧化碳青霉烯的C-2和C-6部分。 ThnQ立体选择性羟基化PS-5给予N-乙酰基噻吩霉素。 ThnG催化PS-5的顺序去饱和和亚磺氧化，得到PS-7及其亚砜。 ThnG和ThnQ酶是相对底物选择性的，但导致由S. cattleya产生的碳青霉烯类的氧化多样性，直系同源物在相关的链霉菌中可能具有相似的功能。

公开(公告)号：US09169258B2

公开(公告)日：2015-10-27

申请号：US14387829

申请日：2012-09-26

Applicant: SHENZHEN HAIBIN PHARMACEUTICAL CO., LTD.

Inventor： Lisong Long ,  Zhaoqiang Lu ,  Cheng Ding ,  Guangcheng Li ,  Zhili Lv ,  Congquan Wu ,  Yanjun Zhang ,  Peng Ren

IPC: C07D477/20 ,  C07D477/06 ,  C07D477/08

CPC classification number: C07D477/20 ,  C07D477/06 ,  C07D477/08 ,  Y02P20/55

Abstract: The present invention provides a doripenem intermediate compound shown by formula (XIV), wherein PNB is p-nitrobenzyl, and HX is an acid; and when HX is a monobasic acid, n=1; and when HX is a polybasic acid, n=2. The present invention also provides a process for preparing the doripenem intermediate compound (XIV). In addition, the present invention provides a process for preparing doripenem (I) from the doripenem intermediate compound (XIV) in a simple manner, with a high yield and low production costs. The new mono-protected doripenem intermediate compound provided in the present invention contains only one protecting group, reducing the difficulty and complexity in the subsequent de-protection step by catalytic hydrogenation, increasing the yield of the catalytic hydrogenation reaction, and thus reducing the production cost of the final product. The process is easy to operate and suitable for industrialized production.

Abstract translation: 本发明提供式（XIV）所示的多巴培南中间体化合物，其中PNB为对硝基苄基，HX为酸; 当HX是一元酸时，n = 1; 当HX为多元酸时，n = 2。 本发明还提供了制备多巴培南中间体化合物（XIV）的方法。 此外，本发明提供了以简单的方式从多巴培南中间体化合物（XIV）制备多巴培南（I）的方法，产率高，生产成本低。 本发明提供的新的单保护多代替巴中间体化合物仅含有一个保护基，通过催化氢化降低后续脱保护步骤的难度和复杂性，提高催化氢化反应的产率，从而降低生产成本 的最终产品。 该工艺易于操作，适用于工业化生产。

公开(公告)号：US20150274732A1

公开(公告)日：2015-10-01

申请号：US14434550

申请日：2013-10-11

Applicant: Sandoz AG

Inventor： Hannes Lengauer ,  Birgit Endl ,  Wolfgang Felzmann

IPC: C07D477/20

CPC classification number: C07D477/08 ,  C07B2200/13 ,  C07D477/20

Abstract: The present invention relates to the preparation of compounds, in particular to the preparation of compounds which may be used as intermediates for the preparation of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem, and salts thereof.

Abstract translation: 本发明涉及化合物的制备，特别是涉及可用作制备抗生素，优选碳青霉烯类抗生素，更优选厄来替班及其盐的中间体的化合物的制备。

公开(公告)号：US20150031664A1

公开(公告)日：2015-01-29

申请号：US14187010

申请日：2014-02-21

Applicant: SHIONOGI & CO., LTD.

Inventor： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

IPC: C07D477/20

CPC classification number: C07D477/20 ,  C07B2200/13

Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

Abstract translation: 提供具有优异稳定性的吡咯烷基硫代碳青霉烯衍生物的新型晶体。 根据本发明，（+） - （4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-7-氧代-3 [[（3S，5S） 在粉末X射线衍射中具有衍射角的衍射图的5-（氨磺酰氨基甲基）吡咯烷-3-基]硫代] -1-氮杂双环[3.2.0]庚-2-烯-2-甲酸在衍射角（2θ ;）为约6.62,13.4,15.44,16.58,17.64,20.88,23.26,25.02和25.52（度）。