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1. 发明申请

US20120004227A1 CYCLOHEXANE DERIVATIVE HAVING NPY Y5 RECEPTOR ANTAGONISM 失效
标题翻译：具有NPY Y5受体拮抗剂的CYCLOHEXANE衍生物
公开(公告)号：US20120004227A1
公开(公告)日：2012-01-05
申请号：US13254702
申请日：2010-03-05
申请人： Hiroshi Yoshida , Keisuke Tonogaki , Masahiro Sakagami , Kenji Takaya
发明人： Hiroshi Yoshida , Keisuke Tonogaki , Masahiro Sakagami , Kenji Takaya
IPC分类号： A61K31/5377 , A61K31/497 , C07D213/64 , A61K31/4412 , C07D401/12 , A61K31/4439 , C07D213/81 , A61K31/44 , C07D471/04 , A61K31/4375 , C07D215/14 , A61K31/4709 , C07D231/38 , A61K31/415 , C07C233/81 , A61K31/16 , C07D263/58 , A61K31/423 , C07D417/12 , A61K31/427 , C07D295/14 , A61K31/5375 , A61P3/04 , C07D413/12
CPC分类号： C07D213/64 , C07C237/24 , C07C255/54 , C07C2601/14 , C07D213/74 , C07D213/81 , C07D213/84 , C07D231/38 , C07D241/18 , C07D249/06 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)═(C(═O)N(R1), C(═O)N(R2)), (C(═O)N(R1), imidazole-1,3-diyl), (N(R1), C(═O)N(R2)), (O, C(═O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(═O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
摘要翻译：本发明公开了具有NPY Y5受体拮抗活性的新型环己烷衍生物。具体而言，本发明公开了式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A为取代或未取代的芳基或杂环基; X和Y的组合是选自（X，Y）=（C（= O）N（R1），C（= O）N（R2）），（C（= O）N（R1）咪唑-1,3-二基），（N（R1），C（= O）N（R2）），（O，C（= O）N（R2）），（C（R3）（R4）（R2））或（单键，C（= O）N（R2））; R1，R2和R3独立地是氢或取代或未取代的烷基; R5是取代或未取代的芳基或杂环基; R 6是卤素，氧代，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的芳氧基; m为0或1; n为0〜5的整数。和B是芳族碳环，单环杂环或稠合双环杂环。

2. 发明授权

US08653125B2 Cyclohexane derivative having NPY Y5 receptor antagonism 失效
标题翻译：具有NPY Y5受体拮抗作用的环己烷衍生物
公开(公告)号：US08653125B2
公开(公告)日：2014-02-18
申请号：US13254702
申请日：2010-03-05
申请人： Hiroshi Yoshida , Keisuke Tonogaki , Masahiro Sakagami , Kenji Takaya
发明人： Hiroshi Yoshida , Keisuke Tonogaki , Masahiro Sakagami , Kenji Takaya
IPC分类号： A61K31/4172 , A61K31/165 , C07D233/61 , C07C233/30
CPC分类号： C07D213/64 , C07C237/24 , C07C255/54 , C07C2601/14 , C07D213/74 , C07D213/81 , C07D213/84 , C07D231/38 , C07D241/18 , C07D249/06 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)═(C(═O)N(R1), C(═O)N(R2)), (C(═O)N(R1), imidazole-1,3-diyl), (N(R1), C(═O)N(R2)), (O, C(═O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(═O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.
摘要翻译：本发明公开了具有NPY Y5受体拮抗活性的新型环己烷衍生物。具体而言，本发明公开了式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A为取代或未取代的芳基或杂环基; X和Y的组合是选自（X，Y）=（C（= O）N（R1），C（= O）N（R2）），（C（= O）N（R1）咪唑-1,3-二基），（N（R1），C（= O）N（R2）），（O，C（= O）N（R2）），（C（R3）（R2））或（单键，C（= O）N（R2））; R1，R2和R3独立地是氢或取代或未取代的烷基; R5是取代或未取代的芳基或杂环基; R 6是卤素，氧代，取代或未取代的烷基，取代或未取代的烷氧基，取代或未取代的芳氧基; m为0或1; n为0〜5的整数。和B是芳族碳环，单环杂环或稠合双环杂环。

3. 发明申请

US20110319412A1 PIPERIDINE AND PYRROLIDINE DERIVATIVES HAVING NPY Y5 RECEPTOR ANTAGONISM 有权
标题翻译：具有NPY Y5受体拮抗剂的哌啶和吡咯烷衍生物
公开(公告)号：US20110319412A1
公开(公告)日：2011-12-29
申请号：US13254750
申请日：2010-03-05
申请人： Masahiro Sakagami , Hitomi Araki , Hiroshi Hashizume , Hiroshi Yari , Kenji Takaya
发明人： Masahiro Sakagami , Hitomi Araki , Hiroshi Hashizume , Hiroshi Yari , Kenji Takaya
IPC分类号： A61K31/454 , A61P3/04 , A61K31/4545 , A61K31/5377 , C07D401/06 , C07D413/14
CPC分类号： C07D207/16 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(═O); Y is a single bond, CR5R6NR7 or C(═O)NR7; R1 and R2 are independently hydrogen or substituted or unsubstituted alkyl; R3 is substituted or unsubstituted aryl or heterocyclyl; R4 is halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.
摘要翻译：本发明公开了具有NPY Y5受体拮抗作用的新型哌啶和吡咯烷衍生物。具体地说，本发明公开了由式（I）表示的化合物，其药学上可接受的盐或溶剂合物：其中A是取代或未取代的单环芳基或单环杂环基; X是单键或C（= O）; Y是单键，CR5R6NR7或C（= O）NR7; R1和R2独立地为氢或取代或未取代的烷基; R3是取代或未取代的芳基或杂环基; R4是卤素，取代或未取代的烷基，烷氧基，芳氧基或杂环氧基等; p为0〜2的整数。 q为0或1; m为0或1; n为0〜5的整数，和B是芳族碳环，单环杂环或双环稠合杂环。

4. 发明授权

US08889674B2 Piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonism 有权
标题翻译：具有NPY Y5受体拮抗作用的哌啶和吡咯烷衍生物
公开(公告)号：US08889674B2
公开(公告)日：2014-11-18
申请号：US13254750
申请日：2010-03-05
申请人： Masahiro Sakagami , Hitomi Araki , Hiroshi Hashizume , Hiroshi Yari , Kenji Takaya
发明人： Masahiro Sakagami , Hitomi Araki , Hiroshi Hashizume , Hiroshi Yari , Kenji Takaya
IPC分类号： A61K31/454 , A61K31/4545 , A61K31/5377 , C07D471/04 , C07D401/12 , C07D207/16 , C07D413/12 , C07D403/12 , C07D417/12 , C07D401/14 , C07D401/06 , C07D413/06 , C07D211/62 , C07D405/06 , C07D401/04
CPC分类号： C07D207/16 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(═O); Y is a single bond, CR5R6NR7 or C(═O)NR7; R1 and R2 are independently hydrogen or substituted or unsubstituted alkyl; R3 is substituted or unsubstituted aryl or heterocyclyl; R4 is halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.
摘要翻译：本发明公开了具有NPY Y5受体拮抗活性的新型哌啶和吡咯烷衍生物。具体地说，本发明公开了由式（I）表示的化合物，其药学上可接受的盐或溶剂合物：其中A是取代或未取代的单环芳基或单环杂环基; X是单键或C（= O）; Y是单键，CR5R6NR7或C（= O）NR7; R1和R2独立地为氢或取代或未取代的烷基; R3是取代或未取代的芳基或杂环基; R4是卤素，取代或未取代的烷基，烷氧基，芳氧基或杂环氧基等; p为0〜2的整数。 q为0或1; m为0或1; n为0〜5的整数，和B是芳族碳环，单环杂环或双环稠合杂环。

5. 发明申请

US20170101364A1 (S)-3-Amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, and Related Compounds as GABA Aminotransferase Inactivators for the Treatment of Epilepsy, Addiction and Hepatocellular Carcinoma 有权
公开(公告)号：US20170101364A1
公开(公告)日：2017-04-13
申请号：US15289480
申请日：2016-10-10
申请人： Richard B. Silverman , Kenji Takaya , Hoang V. Le , Jose I. Juncosa
发明人： Richard B. Silverman , Kenji Takaya , Hoang V. Le , Jose I. Juncosa
IPC分类号： C07C229/48
CPC分类号： A61K31/196 , C07C229/48 , C07C2601/10
摘要： Cyclopentene carboxylic acid-related compounds as GABA-AT inhibitors for treatment of various addictions, disorders and disease states.

6. 发明授权

US08927710B2 Substituted polycyclic carbamoylpyridone derivative 有权
标题翻译：取代的多环氨基甲酰吡啶酮衍生物
公开(公告)号：US08927710B2
公开(公告)日：2015-01-06
申请号：US13378334
申请日：2010-06-14
申请人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
发明人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
IPC分类号： C07D471/04 , C07D401/06 , C07D413/06 , A61K31/53 , A61K31/4427 , A61K31/506 , A61K31/5377 , A61P31/16 , C07D498/14 , C07D471/14
CPC分类号： C07D471/04 , A61K31/53 , C07D471/14 , C07D487/14 , C07D487/20 , C07D498/14
摘要： This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
摘要翻译：本发明提供具有抗病毒活性的化合物，特别是抑制流感病毒的活性，更优选提供具有cap依赖性内切核酸酶抑制活性的取代的3-羟基-4-吡啶酮衍生物。

7. 发明申请

US20120184734A1 SUBSTITUTED POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE 有权
标题翻译：取代的多环碳酰胺衍生物
公开(公告)号：US20120184734A1
公开(公告)日：2012-07-19
申请号：US13378334
申请日：2010-06-14
申请人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
发明人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
IPC分类号： C07D498/14 , C07D471/14 , C07D471/04
CPC分类号： C07D471/04 , A61K31/53 , C07D471/14 , C07D487/14 , C07D487/20 , C07D498/14
摘要： This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
摘要翻译：本发明提供具有抗病毒活性的化合物，特别是抑制流感病毒的活性，更优选提供具有cap依赖性内切核酸酶抑制活性的取代的3-羟基-4-吡啶酮衍生物。

8. 发明申请

US20120277441A1 PROCESS FOR THE PREPARATION OF CYCLOHEXANE DERIVATIVES 审中-公开
标题翻译：制备环己烷衍生物的方法
公开(公告)号：US20120277441A1
公开(公告)日：2012-11-01
申请号：US13512236
申请日：2010-11-24
申请人： Ryosuke Kunitani , Kenji Takaya , Yoshiaki Imamura , Aiko Hasegawa
发明人： Ryosuke Kunitani , Kenji Takaya , Yoshiaki Imamura , Aiko Hasegawa
IPC分类号： C07D277/82 , C07D263/58
CPC分类号： C07D263/58 , C07D277/82
摘要： A process for preparing a compound of formula (I) or a salt or solvate thereof, by reacting a compound of formula (IV): with a compound of formula (V): to obtain the compound of formula (I): wherein each R1 is independently a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy or C1-C6 alkylcarbonyl; R2 is C1-C6 alkyl, C1-C6 haloalkyl, or phenyl optionally substituted with at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, and nitro; R3 is C1-C6 alkyl, C3-C8 cycloalkyl, or a phenyl optionally substituted at least one selected from the group consisting of a halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, and C1-C6 haloalkoxy; n is 0, 1, or 2; and X is S atom or O atom.
摘要翻译：通过式（Ⅳ）化合物与式（Ⅴ）化合物反应来制备式（Ⅰ）化合物或其盐或溶剂合物的方法，得到式（Ⅰ）化合物：其中R1 独立地是卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基或C 1 -C 6烷基羰基; R2是C1-C6烷基，C1-C6卤代烷基或任选被至少一个选自卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基和硝基 R 3是C 1 -C 6烷基，C 3 -C 8环烷基或任选被至少一个选自卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基和C 1 -C 6卤代烷氧基的苯基的苯基; n为0,1或2; X是S原子或O原子。

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