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1. 发明申请

WO2009131947A3 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE DERIVATIVES 审中-公开
标题翻译：化合物，组合物和包含吡嗪衍生物的方法
公开(公告)号：WO2009131947A3
公开(公告)日：2010-01-07
申请号：PCT/US2009041145
申请日：2009-04-20
申请人： INST ONEWORLD HEALTH , RUSSELL MICHAEL GEOFFREY NEIL , DOYLE KEVIN JAMES , PEACH JOANNE
发明人： RUSSELL MICHAEL GEOFFREY NEIL , DOYLE KEVIN JAMES , PEACH JOANNE
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50
CPC分类号： C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文所定义的化合物（CFTR）多肽来抑制功能性囊性纤维化跨膜传导调节因子（CFTR）多肽包括表1所示或由式I所包括的那些化合物）或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

2. 发明申请

WO2009131958A3 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING TRIAZINE DERIVATIVES 审中-公开
标题翻译：化合物，组合物和包含TRIAZINE衍生物的方法
公开(公告)号：WO2009131958A3
公开(公告)日：2009-12-30
申请号：PCT/US2009041165
申请日：2009-04-20
申请人： INST ONEWORLD HEALTH , RUSSELL MICHAEL GEOFFREY NEIL , PEACH JOANNE , MACRITCHIE JACQUELINE ANNE , BRUCKNER SEBASTIAN , DOYLE KEVIN JAMES
发明人： RUSSELL MICHAEL GEOFFREY NEIL , PEACH JOANNE , MACRITCHIE JACQUELINE ANNE , BRUCKNER SEBASTIAN , DOYLE KEVIN JAMES
IPC分类号： A01N43/64 , A61K31/53
CPC分类号： C07D253/065 , C07D253/07 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文所定义的化合物（CFTR）多肽来抑制功能性囊性纤维化跨膜传导调节因子（CFTR）多肽包括表1所示或由式I-II所包括的化合物或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

3. 发明申请

WO2009131947A2 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE DERIVATIVES 审中-公开
标题翻译：化合物，组合物和包含吡嗪衍生物的方法
公开(公告)号：WO2009131947A2
公开(公告)日：2009-10-29
申请号：PCT/US2009/041145
申请日：2009-04-20
申请人： INSTITUTE FOR ONEWORLD HEALTH , RUSSELL, Michael, Geoffrey Neil , DOYLE, Kevin, James , PEACH, Joanne
发明人： RUSSELL, Michael, Geoffrey Neil , DOYLE, Kevin, James , PEACH, Joanne
IPC分类号： A61K31/50 , C07D237/20 , C12N5/06 , A61P13/12
CPC分类号： C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formula I) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文所定义的化合物（CFTR）多肽来抑制功能性囊性纤维化跨膜传导调节因子（CFTR）多肽包括表1所示或由式I所包括的那些化合物）或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

4. 发明申请

WO2008121877A3 CFTR INHIBITOR COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2008121877A3
公开(公告)日：2008-10-09
申请号：PCT/US2008/058752
申请日：2008-03-28
申请人： INSTITUTE FOR ONEWORLD HEALTH , RUSSELL, Michael Geoffrey Neil , VATER, Huw David , MACRITCHIE, Jacqueline Anne , DOYLE, Kevin James , BROWN, David , PEACH, Joanne
发明人： RUSSELL, Michael Geoffrey Neil , VATER, Huw David , MACRITCHIE, Jacqueline Anne , DOYLE, Kevin James , BROWN, David , PEACH, Joanne
IPC分类号： C07C251/86 , C07C311/00 , C07C317/44 , C07C323/60 , C07D231/06 , C07D231/14 , C07D237/04 , A61K31/415 , A61K31/495 , A61P9/06 , A61P1/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

5. 发明申请

WO2008121877A2 CFTR INHIBITOR COMPOUNDS AND USES THEREOF 审中-公开
标题翻译： CFTR抑制剂化合物及其用途
公开(公告)号：WO2008121877A2
公开(公告)日：2008-10-09
申请号：PCT/US2008058752
申请日：2008-03-28
申请人： INST ONEWORLD HEALTH , RUSSELL MICHAEL GEOFFREY NEIL , VATER HUW DAVID , MACRITCHIE JACQUELINE ANNE , DOYLE KEVIN JAMES , BROWN DAVID , PEACH JOANNE
发明人： RUSSELL MICHAEL GEOFFREY NEIL , VATER HUW DAVID , MACRITCHIE JACQUELINE ANNE , DOYLE KEVIN JAMES , BROWN DAVID , PEACH JOANNE
IPC分类号： C07D409/10 , C07D207/325 , C07D207/337 , C07D413/06 , C07D417/04 , C07D495/04
CPC分类号： C07C251/86 , C07C271/22 , C07C311/08 , C07C311/21 , C07C317/44 , C07C323/60 , C07C2601/14 , C07C2602/08 , C07D207/325 , C07D207/327 , C07D209/08 , C07D209/42 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/52 , C07D231/06 , C07D231/14 , C07D237/04 , C07D239/28 , C07D239/92 , C07D263/34 , C07D277/06 , C07D277/30 , C07D277/56 , C07D279/22 , C07D285/06 , C07D295/192 , C07D307/79 , C07D333/22 , C07D333/38 , C07D333/70 , C07D339/06 , C07D401/04 , C07D405/06 , C07D409/04 , C07D495/04
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，所述疾病对功能性囊性纤维化跨膜传导调节因子（CFTR）多肽的抑制有反应，其通过对有需要的哺乳动物施用有效量的本文定义的化合物包括表1-6中列出的或由式I-VI包含的那些化合物或其组合物，从而治疗疾病。本发明特别涉及治疗腹泻和多囊肾病的方法。

6. 发明申请

WO1997028162A1 DIAZABICYCLO-OCTANE DERIVATIVES AS 5-HT RECEPTOR LIGANDS 审中-公开
标题翻译：作为5-HT受体配体的DIAZABICYCLO-OCTANE DERIVATIVES
公开(公告)号：WO1997028162A1
公开(公告)日：1997-08-07
申请号：PCT/GB1997000181
申请日：1997-01-21
申请人： MERCK SHARP & DOHME LIMITED , CASTRO PINEIRO, Jose, Luis , RUSSELL, Michael, Geoffrey, Neil
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of 3-substituted 2,7-diazabicyclo[3.3.0]octane derivatives, further substituted at the 7-position by an optionally substituted alkenyl, alkynyl, cycloalkyl-alkyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D alpha receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1D alpha receptor subtype relative to the 5-HT1D6 subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要翻译：炔基，环烷基 - 烷基，芳基 - 烷基或杂芳基 - 烷基部分在7-位被进一步取代的一类3-取代的2,7-二氮杂双环[3.3.0]辛烷衍生物是选择性激动剂的5-HT1样受体是人5-HT1Dα受体亚型的有效激动剂，同时相对于5-HT1D6亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

7. 发明申请

WO2010123933A1 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING 1,3,4-OXADIAZOLE DERIVATIVES 审中-公开
标题翻译：包含1,3,4-氧杂噻唑衍生物的化合物，组合物和方法
公开(公告)号：WO2010123933A1
公开(公告)日：2010-10-28
申请号：PCT/US2010/031798
申请日：2010-04-20
申请人： INSTITUTE FOR ONEWORLD HEALTH , RUSSELL, Michael Geoffrey Neil , DOYLE, Kevin James
发明人： RUSSELL, Michael Geoffrey Neil , DOYLE, Kevin James
IPC分类号： A61K31/41
CPC分类号： C07D271/10 , C07D413/06
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文所定义的化合物（CFTR）多肽来抑制功能性囊性纤维化跨膜传导调节因子（CFTR）多肽包括表1-2所列或由式I-IV所包括的化合物）或包含这些化合物的组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

8. 发明申请

WO2009131958A2 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING TRIAZINE DERIVATIVES 审中-公开
标题翻译：包含三嗪衍生物的化合物，组合物和方法
公开(公告)号：WO2009131958A2
公开(公告)日：2009-10-29
申请号：PCT/US2009/041165
申请日：2009-04-20
申请人： INSTITUTE FOR ONEWORLD HEALTH , RUSSELL, Michael, Geoffrey Neil , PEACH, Joanne , MACRITCHIE, Jacqueline, Anne , BRUCKNER, Sebastian , DOYLE, Kevin, James
发明人： RUSSELL, Michael, Geoffrey Neil , PEACH, Joanne , MACRITCHIE, Jacqueline, Anne , BRUCKNER, Sebastian , DOYLE, Kevin, James
IPC分类号： A61K31/53 , C07D253/065 , C12N5/06 , A61P1/12
CPC分类号： C07D253/065 , C07D253/07 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，所述疾病对功能性囊性纤维化跨膜传导调节因子（CFTR）多肽的抑制有反应，其通过对需要的哺乳动物施用有效量的本文定义的化合物（包括表1中列出的或由式I-II涵盖的那些化合物）或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

9. 发明申请

WO2009131956A1 COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING TRIAZOLE DERIVATIVES 审中-公开
标题翻译：化合物，组合物和包含三唑衍生物的方法
公开(公告)号：WO2009131956A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/041162
申请日：2009-04-20
申请人： INSTITUTE FOR ONEWORLD HEALTH , RUSSELL, Michael, Geoffrey Neil , DOYLE, Kevin, James
发明人： RUSSELL, Michael, Geoffrey Neil , DOYLE, Kevin, James
IPC分类号： A01N43/64
CPC分类号： C07D249/10 , C07D401/06
摘要： The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
摘要翻译：本发明涉及用于治疗动物疾病的组合物和方法，该疾病通过对有需要的哺乳动物施用有效量的本文所定义的化合物（CFTR）多肽来抑制功能性囊性纤维化跨膜传导调节因子（CFTR）多肽包括表1-2所示或由式I-II所包括的化合物或其组合物，从而治疗疾病。本发明特别涉及一种治疗腹泻和多囊肾病的方法。

10. 发明申请

WO2004065388A1 FLUOROIMIDAZOPYRIMIDINES AS GABA-A ALPHA 2/3 LIGANDS FOR DEPRESSION/ANXIETY 审中-公开
标题翻译：氟尿嘧啶嘧啶类作为GABA-A ALPHA 2/3用于抑制/抑制的配体
公开(公告)号：WO2004065388A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000196
申请日：2004-01-21
申请人： MERCK SHARP & DOHME LIMITED , CARLING, William, Robert , GOODACRE, Simon, Charles , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
发明人： CARLING, William, Robert , GOODACRE, Simon, Charles , RUSSELL, Michael, Geoffrey, Neil , STREET, Leslie, Joseph
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound formula (I), or a pharmaceutically acceptable salt thereof: wherein W is phenyl or pyridyl; X 1 represents hydrogen, halogen, C 1-6 alkyl, trifluoromethyl or C 1-6 alkoxy; X 2 represents hydrogen or halogen; Y represents a chemical bond, an -NH- linkage or a group -OC n H 2n -; Z represents an optionally substituted aryl or heteroaryl group; R 1 represents hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, -OR a , -SR a , -SOR a , -SO 2 R a , -SO 2 NR a R b , NR a R b , -NR a COR b , -NR a CO 2 R b , -COR a , -CO 2 R a , -CONR a R b or Cr a =NOR b ; R a and R b independently represent hydrogen, hydrocarbon or a heterocyclic group; and n is zero, one, two or three; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of medicaments to treat anxiety and/or depression; and methods of treatment for anxiety and/or depression using it.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：其中W是苯基或吡啶基; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，-NH-键或-OC n H 2n-基团; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR a，-SO 2 R a，-SO 2 NR R a，-NR a R b，-NR a COR b，-NR a CO 2 R b，-COR a，-CO 2 R a，-CONR a R 或Cr = NOR ; R a和R b独立地表示氢，烃或杂环基; n为零，一，二或三; 包含它的药物组合物; 其用于治疗方法; 用于制造药物以治疗焦虑和/或抑郁症; 以及使用它的焦虑和/或抑郁症的治疗方法。

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