公开(公告)号：US20100197569A1

公开(公告)日：2010-08-05

申请号：US12759073

申请日：2010-04-13

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 ,  C07D501/16 ,  C07D277/38 ,  A61P31/04 ,  A01N37/18 ,  C07K1/113

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; 使用这种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：US20090111737A1

公开(公告)日：2009-04-30

申请号：US12082666

申请日：2008-04-11

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

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

IPC: A61K38/14 ,  C07K7/00 ,  A61P43/00

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, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase 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，pencillinase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。

公开(公告)号：US20060178410A1

公开(公告)日：2006-08-10

申请号：US11400959

申请日：2006-04-10

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

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

IPC: C07D213/26 ,  A61K31/44 ,  A61K31/40 ,  A61K31/138

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: 本发明提供新的β2肾上腺素能受体激动剂式（I）化合物：其中R 1 -R 13和w具有任何值 在说明书中描述。 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相关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20060074121A1

公开(公告)日：2006-04-06

申请号：US11219637

申请日：2005-09-01

Applicant: Wei Chen ,  Penglie Zhang ,  James Aggen ,  Daniel Dairaghi ,  Andrew Pennell ,  Subhabrata Sen ,  J.J. Wright

Inventor： Wei Chen ,  Penglie Zhang ,  James Aggen ,  Daniel Dairaghi ,  Andrew Pennell ,  Subhabrata Sen ,  J.J. Wright

IPC: A61K31/4162 ,  C07D487/02

CPC classification number: C07D471/10 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.

Abstract translation: 提供了作为CCR1，CCR2和CCR3受体中一种或多种的有效调节剂的化合物。 化合物通常是具有芳基和杂芳基组分的稠合，螺或氮杂环，并且可用于药物组合物，用于治疗CCR1，CCR2和/或CCR3介导的疾病的方法，以及用于测定中的对照 用于鉴定上述趋化因子受体的竞争性受体拮抗剂。

公开(公告)号：US20050256130A1

公开(公告)日：2005-11-17

申请号：US10979882

申请日：2004-11-01

Applicant: Andrew Pennell ,  James Aggen ,  J.J. Wright ,  Subhabrata Sen ,  Brian McMaster ,  Daniel Dairaghi ,  Wei Chen ,  Penglie Zhang

Inventor： Andrew Pennell ,  James Aggen ,  J.J. Wright ,  Subhabrata Sen ,  Brian McMaster ,  Daniel Dairaghi ,  Wei Chen ,  Penglie Zhang

IPC: A61K31/496 ,  A61K31/506 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/38 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D43/14

CPC classification number: C07D409/04 ,  C07D231/12 ,  C07D231/16 ,  C07D231/18 ,  C07D231/38 ,  C07D231/56 ,  C07D233/61 ,  C07D235/06 ,  C07D249/08 ,  C07D249/14 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D471/04 ,  C07D473/34

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract translation: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常为芳基哌嗪衍生物，并且可用于药物组合物，用于治疗CCR1介导的疾病的方法，以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。

公开(公告)号：US20050234034A1

公开(公告)日：2005-10-20

申请号：US11071880

申请日：2005-03-02

Applicant: Andrew Pennell ,  James Aggen ,  J.J. Wright ,  Subhabrata Sen ,  Wei Chen ,  Daniel Dairaghi ,  Penglie Zhang

Inventor： Andrew Pennell ,  James Aggen ,  J.J. Wright ,  Subhabrata Sen ,  Wei Chen ,  Daniel Dairaghi ,  Penglie Zhang

IPC: A61K31/397 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  C07D403/06 ,  C07D487/12

CPC classification number: C07D487/04 ,  C07D471/10 ,  C07D487/08

Abstract: Compounds are provided that act as potent modulators of one or more of the CCR1, CCR2 and CCR3 receptors. The compounds are generally fused-, spiro- or bridged-nitrogen heterocycles having an aryl and heteroaryl component and are useful in pharmaceutical compositions, methods for the treatment of CCR1-, CCR2- and/or CCR3-mediated diseases, and as controls in assays for the identification of competitive receptor antagonists for the above chemokine receptors.

Abstract translation: 提供了作为CCR1，CCR2和CCR3受体中一种或多种的有效调节剂的化合物。 化合物通常是具有芳基和杂芳基组分的稠合，螺或氮杂环，并且可用于药物组合物，用于治疗CCR1，CCR2和/或CCR3介导的疾病的方法，以及用于测定中的对照 用于鉴定上述趋化因子受体的竞争性受体拮抗剂。

公开(公告)号：US20080300199A1

公开(公告)日：2008-12-04

申请号：US12100981

申请日：2008-04-10

Applicant: Martin Linsell ,  Adam Aaron Goldblum ,  James Aggen ,  Heinz Ernst Moser ,  Stephen Hanessian ,  Kandasamy Pachamuthu ,  Ellen Klegraf

Inventor： Martin Linsell ,  Adam Aaron Goldblum ,  James Aggen ,  Heinz Ernst Moser ,  Stephen Hanessian ,  Kandasamy Pachamuthu ,  Ellen Klegraf

IPC: A61K31/7036 ,  C07G11/00 ,  A61P31/04

CPC classification number: C07H15/232

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract translation: 本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。

公开(公告)号：US07456203B2

公开(公告)日：2008-11-25

申请号：US10425368

申请日：2003-04-29

Applicant: James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

Inventor： James Aggen ,  John H. Griffin ,  Mathai Mammen ,  Daniel Marquess ,  Edmund J. Moran ,  David Oare

IPC: A01N43/40 ,  A61K31/445

CPC classification number: A61K31/40 ,  C07C211/32 ,  C07C2603/32 ,  C07D207/08 ,  C07D209/48 ,  C07D211/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D519/00 ,  G01N33/566

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract translation: 公开了作为毒蕈碱受体拮抗剂的多重联结化合物。 含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。 每个配体彼此独立地是毒蕈碱受体拮抗剂或变构调节剂，只要至少一种所述配体是毒蕈碱受体拮抗剂即可。 本发明的多重联结化合物可用于治疗和预防慢性阻塞性肺疾病，慢性支气管炎，肠易激综合征，尿失禁等疾病。

公开(公告)号：US07452995B2

公开(公告)日：2008-11-18

申请号：US11102197

申请日：2005-04-07

Applicant: Edmund J. Moran ,  John R. Jacobsen ,  James Aggen

Inventor： Edmund J. Moran ,  John R. Jacobsen ,  James Aggen

IPC: C07D215/16 ,  C07C233/00

CPC classification number: C07D213/75 ,  C07C215/60 ,  C07C217/84 ,  C07C229/38 ,  C07C233/43 ,  C07D215/227 ,  C07D215/26 ,  C07D231/22 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D277/46 ,  C07D311/80 ,  C07D319/08 ,  C07D321/10 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: The invention provides novel β2 adrenergic receptor agonist compounds. 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: 本发明提供了新的β2肾上腺素能受体激动剂化合物。 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相关的疾病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20080194465A1

公开(公告)日：2008-08-14

申请号：US11895533

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 ,  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.