公开(公告)号：US07863309B2

公开(公告)日：2011-01-04

申请号：US12507995

申请日：2009-07-23

申请人： Seok-ki Choi ,  Paul R. Fatheree ,  Roland Gendron ,  Robert Murray McKinnell ,  Brooke Blair

发明人： Seok-ki Choi ,  Paul R. Fatheree ,  Roland Gendron ,  Robert Murray McKinnell ,  Brooke Blair

IPC分类号： A61K31/4164 ,  A61K31/4196 ,  C07D233/54 ,  C07D249/08

CPC分类号： A61K31/4196 ,  A61K45/06 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/08 ,  C07D249/10 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10

摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

公开(公告)号：US20090149521A1

公开(公告)日：2009-06-11

申请号：US12330289

申请日：2008-12-08

申请人： Seok-Ki Choi ,  Paul R. Fatheree ,  Robert Murray McKinnell ,  Brooke Olson

发明人： Seok-Ki Choi ,  Paul R. Fatheree ,  Robert Murray McKinnell ,  Brooke Olson

IPC分类号： A61K31/4184 ,  C07D235/16 ,  C07D403/08

CPC分类号： C07D235/08 ,  C07D235/26 ,  C07D403/10

摘要： The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2′, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

摘要翻译： 本发明涉及具有下式的化合物：其中Ar，r，n，X，R2，R2'，R3和R5-7如本说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

公开(公告)号：US07728127B2

公开(公告)日：2010-06-01

申请号：US11895534

申请日：2007-08-24

申请人： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel Marquess ,  S. Derek Turner

发明人： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel Marquess ,  S. Derek Turner

IPC分类号： C07D501/00 ,  A61K38/66 ,  A61K31/545 ,  A61K38/00 ,  C12Q1/12 ,  C12P35/06 ,  G01N33/06

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

摘要： 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：US20080194464A1

公开(公告)日：2008-08-14

申请号：US11895531

申请日：2007-08-24

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

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

IPC分类号： A61K38/14 ,  C07K9/00

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

摘要： 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

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

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

IPC分类号： A61K38/16 ,  A61K38/00

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

摘要： 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.

摘要翻译： 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：US07332471B2

公开(公告)日：2008-02-19

申请号：US11342729

申请日：2006-01-30

申请人： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel Marquess ,  Daniel D. Long ,  Jason P. Chinn ,  Matthew B. Nodwell ,  Edmund J. Moran ,  James B. Aggen

发明人： Paul R. Fatheree ,  Martin S. Linsell ,  Daniel Marquess ,  Daniel D. Long ,  Jason P. Chinn ,  Matthew B. Nodwell ,  Edmund J. Moran ,  James B. Aggen

IPC分类号： A61K38/00 ,  A61K31/545

CPC分类号： C07D519/00 ,  A61K38/00 ,  C07D501/46 ,  C07K9/008

摘要： 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：US06878686B2

公开(公告)日：2005-04-12

申请号：US10444847

申请日：2003-05-23

申请人： Daniel Marquess ,  Martin S. Linsell ,  S. Derek Turner ,  Sean G. Trapp ,  Daniel D. Long ,  Paul R. Fatheree

发明人： Daniel Marquess ,  Martin S. Linsell ,  S. Derek Turner ,  Sean G. Trapp ,  Daniel D. Long ,  Paul R. Fatheree

IPC分类号： A61K38/00 ,  A61P31/04 ,  C07K9/00 ,  A61K38/16

CPC分类号： C07K9/008 ,  A61K38/00 ,  Y02A50/473

摘要： 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：US08084417B2

公开(公告)日：2011-12-27

申请号：US12214554

申请日：2008-06-19

申请人： Daniel Marquess ,  Martin S. Linsell ,  S. Derek Turner ,  Sean G. Trapp ,  Daniel D. Long ,  Paul R. Fatheree

发明人： Daniel Marquess ,  Martin S. Linsell ,  S. Derek Turner ,  Sean G. Trapp ,  Daniel D. Long ,  Paul R. Fatheree

IPC分类号： A61K38/14

CPC分类号： C07K9/008 ,  A61K38/00 ,  Y02A50/473

摘要： 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.

摘要翻译： 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：US20100249186A1

公开(公告)日：2010-09-30

申请号：US12796902

申请日：2010-06-09

申请人： Robert Murray McKinnell ,  Roland Gendron ,  Lan Jiang ,  Seoki-ki Choi ,  Daniel D. Long ,  Paul R. Fatheree ,  Daniel Marquess

发明人： Robert Murray McKinnell ,  Roland Gendron ,  Lan Jiang ,  Seoki-ki Choi ,  Daniel D. Long ,  Paul R. Fatheree ,  Daniel Marquess

IPC分类号： A61K31/4545 ,  A61P1/00 ,  A61P1/04

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  G01N33/5058

摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

摘要翻译： 本发明涉及式（I）的苯并咪唑 - 甲酰胺5-HT 4受体激动剂化合物，其中R 1和X如说明书中所定义，或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗与5-HT 4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：US07728006B2

公开(公告)日：2010-06-01

申请号：US11547790

申请日：2005-04-06

申请人： Daniel Marquess ,  Paul R. Fatheree ,  S. Derek Turner ,  Daniel D. Long

发明人： Daniel Marquess ,  Paul R. Fatheree ,  S. Derek Turner ,  Daniel D. Long

IPC分类号： A61K31/4709 ,  A61P1/00 ,  A61P1/10 ,  A61P1/14

CPC分类号： A61K31/4709 ,  A61K9/0019 ,  A61K9/0075 ,  A61K9/008 ,  A61K9/10 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  C07D451/04

摘要： The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds of Formula (I). The invention also provides pharmaceutical compositions comprising such compounds, the use such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. Wherein; R1 is hydrogen, halo, hadroxy, C1-4 alkyl, or C1-4 alkoxy; R2 is C3-4 alkyl, or C3-6cycloakyl; R3 is hydrogen or C1-3 alkyl: R4 is —S(O)2 R6 or —C(O)R7; R5 is hydrogen, C1-3alkyl, C2-3 alkyl substituted with —OH or C1-3 alkoxy, or —CH2-pyrydyl; R6 is C1-3 alkyl; or R5 and R6 taken together from C3-4 alkylenyl; and R7 is hydrogen, C1-3alkyl, or pyrydyl; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof.

摘要翻译： 本发明提供式（I）的新型喹啉酮 - 甲酰胺5-HT 4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5-HT 4受体活性相关的疾病，以及可用于制备这些化合物的方法和中间体。 其中; R1是氢，卤素，羟基，C1-4烷基或C1-4烷氧基; R2是C3-4烷基或C3-6环烷基; R3是氢或C1-3烷基：R4是-S（O）2 R6或-C（O）R7; R5是氢，C1-3烷基，被-OH或C1-3烷氧基取代的C2-3烷基，或-CH2-吡啶基; R6是C1-3烷基; 或R 5和R 6一起为C3-4亚烷基; 和R 7是氢，C 1-3烷基或吡啶基; 或其药学上可接受的盐或溶剂合物或立体异构体。