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1. 发明申请

US20060199823A1 Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands 审中-公开
标题翻译：杂芳基稠合吡啶，吡嗪和嘧啶作为CRF1受体配体
公开(公告)号：US20060199823A1
公开(公告)日：2006-09-07
申请号：US11389646
申请日：2006-03-24
申请人： Ping Ge , Raymond Horvath , Lu Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao
发明人： Ping Ge , Raymond Horvath , Lu Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao
IPC分类号： A61K31/498 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04
摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

2. 发明授权

US06214853B1 Selective NPY (Y5) antagonists (bicyclics) 有权
标题翻译：选择性NPY（Y5）拮抗剂（双环）
公开(公告)号：US06214853B1
公开(公告)日：2001-04-10
申请号：US09343633
申请日：1999-06-30
申请人： Mohammad R. Marzabadi , Wai C. Wong , Yasuchika Yamaguchi , Stewart A. Noble
发明人： Mohammad R. Marzabadi , Wai C. Wong , Yasuchika Yamaguchi , Stewart A. Noble
IPC分类号： A01K31427
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to bicyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。

3. 发明授权

US5705658A Azido containing tetrahydro furan compounds 失效
标题翻译：叠氮基四氢呋喃化合物
公开(公告)号：US5705658A
公开(公告)日：1998-01-06
申请号：US800671
申请日：1997-02-14
申请人： Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
发明人： Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
IPC分类号： C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18
CPC分类号： C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要： .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译：式I（Ⅰ）的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质，可用作抗高血压药用活性成分。

4. 发明授权

US5654445A .delta.-amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acids 失效
标题翻译： δ-氨基-γ-羟基-ω-芳基 - 链烷酸
公开(公告)号：US5654445A
公开(公告)日：1997-08-05
申请号：US674555
申请日：1996-07-02
申请人： Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
发明人： Richard Goschke , Jurgen Klaus Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim Claude Cohen , Peter Herold
IPC分类号： C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18
CPC分类号： C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要： .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译：式I（Ⅰ）的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质，可用作抗高血压药用活性成分。

5. 发明申请

US20070043056A1 5-Substituted-2-arylpyrazines 审中-公开
标题翻译： 5-取代的2-芳基吡嗪
公开(公告)号：US20070043056A1
公开(公告)日：2007-02-22
申请号：US11585405
申请日：2006-10-23
申请人： Taeyoung Yoon , Ping Ge , Stephane De Lombaert , Raymond Horvath , Dario Doller , Kevin Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Cunyu Zhang , Jim Darrow , Yasuchika Yamaguchi
发明人： Taeyoung Yoon , Ping Ge , Stephane De Lombaert , Raymond Horvath , Dario Doller , Kevin Hodgetts , Lu Yan Zhang , Bernd Kaiser , Xuechun Zhang , Cunyu Zhang , Jim Darrow , Yasuchika Yamaguchi
IPC分类号： A61K31/4965 , A61K31/497 , C07D403/04
CPC分类号： C07D241/12 , C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供新的5-取代-2-芳基吡嗪化合物。这些化合物可以作为CRF受体的选择性调节剂。本文提供的5-取代-2-芳基吡嗪化合物可用于治疗许多CNS和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。提供的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

6. 发明申请

US20050137240A1 Selective NPY (Y5) antagonists 失效
标题翻译：选择性NPY（Y5）拮抗剂
公开(公告)号：US20050137240A1
公开(公告)日：2005-06-23
申请号：US11040328
申请日：2005-01-20
申请人： Mohammad Marzabadi , Wai Wong , Stewart Noble , Peter Buhlmayer , Heinrich Rueger , Yasuchika Yamaguchi , Walter Schilling
发明人： Mohammad Marzabadi , Wai Wong , Stewart Noble , Peter Buhlmayer , Heinrich Rueger , Yasuchika Yamaguchi , Walter Schilling
IPC分类号： C07D277/42 , C07D277/60 , C07D417/12 , C07D513/04 , A61K31/426 , C07D277/38
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
摘要翻译：本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环和三环化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。本发明提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途，其中所述异常通过降低人Y5受体的活性而减轻。

7. 发明授权

US06887875B2 2,5-diarypyrimidine compounds 失效
公开(公告)号：US06887875B2
公开(公告)日：2005-05-03
申请号：US10154482
申请日：2002-05-22
申请人： Jianhua Huang , Kevin Hodggetts , Dario Doller , Ping Ge , Yasuchika Yamaguchi
发明人： Jianhua Huang , Kevin Hodggetts , Dario Doller , Ping Ge , Yasuchika Yamaguchi
IPC分类号： G01N33/566 , A61K31/00 , A61K31/44 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/5377 , A61K51/04 , A61P1/04 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D213/74 , C07D239/34 , C07D241/12 , C07D401/04 , C07D403/04 , C07D405/10 , G01N33/58 , C07D239/26 , A61K31/506
CPC分类号： A61K31/00 , A61K51/0455 , A61K51/0459 , A61K51/0463 , C07D213/74 , C07D241/12 , C07D401/04
摘要： Diarylpyrimidine compounds of Formula I are provided, wherein. or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are independently chosen from: phenyl which is mono-, di-, or tri-substituted, 1-naphthyl and 2-naphthyl, each of which is optionally mono-, di-, or tri-substituted, and optionally mono-, di-, or tri-substituted heteroaryl, said heteroaryl having from 1 to 3 rings, 5 to 7 ring members in each ring and, in at least one of said rings, from 1 to about 3 heteroatoms selected from the group consisting of N, O, and S; R is oxygen or absent; Z2 is CR2; Z3 is nitrogen; R1 and R2 are independently chosen from hydrogen, halogen, amino, cyano, nitro, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted mono- or di-alkylamino, optionally substituted cycloalkyl, optionally substituted (cycloalkyl)alkyl, optionally substituted (cycloalkyl)oxy, optionally substituted (cycloalkyl)alkoxy, optionally substituted alkylthio, optionally substituted alkylsulfinyl, optionally substituted alkylsulfonyl, and optionally substituted mono- or dialkylcarboxamide; with the proviso that not all of R1, R3, and R4 are hydrogen. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatments of such disorders and well as packaged pharmaceutical compositions are also provided.Compounds of Formula I are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

8. 发明授权

US06222040B1 Selective NPY (Y5) antagonists (tricyclics) 有权
标题翻译：选择性NPY（Y5）拮抗剂（三环）
公开(公告)号：US06222040B1
公开(公告)日：2001-04-24
申请号：US09343993
申请日：1999-06-30
申请人： Mohammad R. Marzabadi , Peter Bühlmayer , Heinrich Rüeger , Wai C. Wong , Yasuchika Yamaguchi , Stewart A. Noble
发明人： Mohammad R. Marzabadi , Peter Bühlmayer , Heinrich Rüeger , Wai C. Wong , Yasuchika Yamaguchi , Stewart A. Noble
IPC分类号： A61K31429
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为NPY（Y5）受体的选择性拮抗剂的三环化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。

9. 发明授权

US5559111A .delta.-amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides 失效
标题翻译： δ-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺
公开(公告)号：US5559111A
公开(公告)日：1996-09-24
申请号：US416242
申请日：1995-04-04
申请人： Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
发明人： Richard G oschke , J urgen K. Maibaum , Walter Schilling , Stefan Stutz , Pascal Rigollier , Yasuchika Yamaguchi , Nissim C. Cohen , Peter Herold
IPC分类号： C07D295/14 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/20 , A61P27/02 , A61P43/00 , C07C213/00 , C07C229/36 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07C237/24 , C07C255/13 , C07C255/16 , C07C255/60 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/30 , C07C311/32 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/10 , C07C323/12 , C07D207/27 , C07D207/40 , C07D211/32 , C07D211/88 , C07D213/30 , C07D213/40 , C07D213/65 , C07D213/89 , C07D233/64 , C07D233/76 , C07D239/10 , C07D241/08 , C07D257/04 , C07D263/20 , C07D263/26 , C07D263/38 , C07D265/30 , C07D271/06 , C07D277/14 , C07D277/18 , C07D277/28 , C07D295/13 , C07D295/18 , C07D295/22 , C07D307/32 , C07D307/33 , C07D317/64 , C07D319/18 , C07D319/20 , C07D413/06 , C07D521/00 , C07F7/18 , C07D237/20 , C07D294/14
CPC分类号： C07D307/33 , C07C229/36 , C07C237/20 , C07C255/13 , C07C271/16 , C07C271/18 , C07C271/22 , C07D241/08
摘要： .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
摘要翻译：式I（Ⅰ）的α-氨基-γ-羟基-ω-芳基 - 链烷酸酰胺及其盐具有肾素抑制性质，可用作抗高血压药用活性成分。

10. 发明授权

US07273880B2 Selective NPY (Y5) antagonists 失效
标题翻译：选择性NPY（Y5）拮抗剂
公开(公告)号：US07273880B2
公开(公告)日：2007-09-25
申请号：US11040328
申请日：2005-01-20
申请人： Mohammad R. Marzabadi , Wai C. Wong , Stewart A. Noble , Yasuchika Yamaguchi
发明人： Mohammad R. Marzabadi , Wai C. Wong , Stewart A. Noble , Yasuchika Yamaguchi
IPC分类号： A61K31/426
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.
摘要翻译：本发明涉及作为NPY（Y5）受体的选择性拮抗剂的双环和三环化合物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。本发明提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了本发明化合物用于制备用于治疗异常的药物组合物的用途，其中所述异常通过降低人Y5受体的活性而减轻。

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