公开(公告)号：US07582765B2

公开(公告)日：2009-09-01

申请号：US11805101

申请日：2007-05-22

Applicant: Edmund J. Moran ,  John R. Jacobsen ,  Michael R. Leadbetter ,  Matthew B. Nodwell ,  Sean G. Trapp ,  James Aggen ,  Timothy J. Church

Inventor： Edmund J. Moran ,  John R. Jacobsen ,  Michael R. Leadbetter ,  Matthew B. Nodwell ,  Sean G. Trapp ,  James Aggen ,  Timothy J. Church

IPC: C07D215/00 ,  A01N43/42 ,  A01N33/02

CPC classification number: A61K31/4706 ,  A61K31/136 ,  A61K31/277 ,  A61K31/325 ,  A61K31/33 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/381 ,  A61K31/385 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/58 ,  C07C213/04 ,  C07C215/34 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07C317/36 ,  C07D213/75 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/69 ,  C07D277/46 ,  C07D311/80 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  A61K2300/00

Abstract: The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R1-R13和w具有说明书中描述的任何值。 本发明还提供了这样的化合物和其它治疗剂的组合，包含这些化合物和组合的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20080103299A1

公开(公告)日：2008-05-01

申请号：US12004251

申请日：2007-12-19

Applicant: Paul Fatheree ,  Martin Linsell ,  Daniel Marquess ,  Daniel Long ,  Jason Chinn ,  Matthew Nodwell ,  Edmund Moran ,  James Aggen

Inventor： Paul Fatheree ,  Martin Linsell ,  Daniel Marquess ,  Daniel Long ,  Jason Chinn ,  Matthew Nodwell ,  Edmund Moran ,  James Aggen

IPC: C07D501/18

CPC classification number: C07D519/00 ,  A61K38/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。 本发明还提供含有这些化合物的药物组合物; 使用这些化合物治疗哺乳动物细菌感染的方法; 以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20080045721A1

公开(公告)日：2008-02-21

申请号：US11895534

申请日：2007-08-24

Applicant: Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

Inventor： Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

IPC: C07D277/38

CPC classification number: A61K31/545 ,  A61K38/00 ,  C07D277/40 ,  C07D277/42 ,  C07D407/12 ,  C07D407/14 ,  C07D501/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

公开(公告)号：US20060128612A1

公开(公告)日：2006-06-15

申请号：US11342729

申请日：2006-01-30

Applicant: Paul Fatheree ,  Martin Linsell ,  Daniel Marquess ,  Daniel Long ,  Jason Chinn ,  Matthew Nodwell ,  Edmund Moran ,  James Aggen

Inventor： Paul Fatheree ,  Martin Linsell ,  Daniel Marquess ,  Daniel Long ,  Jason Chinn ,  Matthew Nodwell ,  Edmund Moran ,  James Aggen

IPC: A61K38/14 ,  C07K9/00

CPC classification number: C07D519/00 ,  A61K38/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

公开(公告)号：US07553971B2

公开(公告)日：2009-06-30

申请号：US11400959

申请日：2006-04-10

Applicant: Edmund J. Moran ,  John R. Jacobsen ,  Michael R. Leadbetter ,  James Aggen ,  Timothy J. Church

Inventor： Edmund J. Moran ,  John R. Jacobsen ,  Michael R. Leadbetter ,  James Aggen ,  Timothy J. Church

IPC: C07D213/26

CPC classification number: C07D213/75 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07C317/36 ,  C07D213/76 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D311/80 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的新型β2肾上腺素能受体激动剂化合物：其中R1-R13和w具有说明书中描述的任何值。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与β2肾上腺素能受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20080194464A1

公开(公告)日：2008-08-14

申请号：US11895531

申请日：2007-08-24

Applicant: Paul R. Fatheree ,  Martin S. Linsell ,  Daniel D. Long ,  Daniel Marquess ,  Edmund J. Moran ,  Matthew B. Nodwell ,  S. Derek Turner ,  James Aggen

Inventor： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel D. Long ,  Daniel Marquess ,  Edmund J. Moran ,  Matthew B. Nodwell ,  S. Derek Turner ,  James Aggen

IPC: A61K38/14 ,  C07K9/00

CPC classification number: A61K31/545 ,  A61K38/00 ,  C07D277/40 ,  C07D277/42 ,  C07D407/12 ,  C07D407/14 ,  C07D501/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

公开(公告)号：US20080108558A1

公开(公告)日：2008-05-08

申请号：US11977604

申请日：2007-10-25

Applicant: Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

Inventor： Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

IPC: A61K38/14 ,  C07K9/00 ,  A61P31/04

CPC classification number: A61K31/545 ,  A61K38/00 ,  C07D277/40 ,  C07D277/42 ,  C07D407/12 ,  C07D407/14 ,  C07D501/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

公开(公告)号：US07341993B2

公开(公告)日：2008-03-11

申请号：US11172303

申请日：2005-06-30

Applicant: Paul R. Fatheree ,  Martin S. Linsell ,  Daniel D. Long ,  Daniel Marquess ,  Edmund J. Moran ,  Matthew B. Nodwell ,  S. Derek Turner ,  James Aggen

Inventor： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel D. Long ,  Daniel Marquess ,  Edmund J. Moran ,  Matthew B. Nodwell ,  S. Derek Turner ,  James Aggen

IPC: A61K38/16 ,  A61K38/00

CPC classification number: A61K31/545 ,  A61K38/00 ,  C07D277/40 ,  C07D277/42 ,  C07D407/12 ,  C07D407/14 ,  C07D501/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。 本发明还提供含有这些化合物的药物组合物; 使用这些化合物治疗哺乳动物细菌感染的方法; 以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20080039374A1

公开(公告)日：2008-02-14

申请号：US11895555

申请日：2007-08-24

Applicant: Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

Inventor： Paul Fatheree ,  Martin Linsell ,  Daniel Long ,  Daniel Marquess ,  Edmund Moran ,  Matthew Nodwell ,  S. Derek Turner ,  James Aggen

IPC: A61K38/12 ,  A61P31/04

CPC classification number: A61K31/545 ,  A61K38/00 ,  C07D277/40 ,  C07D277/42 ,  C07D407/12 ,  C07D407/14 ,  C07D501/00 ,  C07D501/46 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。 本发明还提供含有这些化合物的药物组合物; 使用这些化合物治疗哺乳动物细菌感染的方法; 以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20070196859A1

公开(公告)日：2007-08-23

申请号：US11603329

申请日：2006-11-21

Applicant: Burton Christensen ,  Edmund Moran ,  John Griffin ,  J. Judice ,  YongQi Mu ,  John Pace ,  Mathai Mammen ,  James Aggen

Inventor： Burton Christensen ,  Edmund Moran ,  John Griffin ,  J. Judice ,  YongQi Mu ,  John Pace ,  Mathai Mammen ,  James Aggen

IPC: A61K38/14 ,  A61K31/43 ,  A61K31/545 ,  A61K31/407

CPC classification number: C07D477/12 ,  C07D499/32 ,  C07D499/44 ,  C07D501/56

Abstract: This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked ) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands has a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, penicillinase enzyme, cephalosporinase enzyme, a transglycosylase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

Abstract translation: 本发明涉及作为抗菌剂的新型多结合化合物（试剂）。 本发明的多相结合化合物包含2-10个配体，其通过连接体或连接体共价连接，其中所述各单体（即，未连接）状态的所述配体具有结合涉及细胞壁生物合成和代谢的酶的能力 用于合成细菌细胞壁和/或细菌细胞表面的前体因而干扰细胞壁的合成和/或代谢。 特别地，本发明的多相结合化合物包含通过接头或接头共价连接的2-10个配体，其中每个所述配体具有能够结合青霉素结合蛋白的配体结构域，转肽酶，转肽酶的底物， β-内酰胺酶，青霉素酶，头孢菌素酶，转糖基酶或转糖基酶酶底物; 优选地，配体选自β-内酰胺或糖肽类抗菌剂。