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1. 发明授权

US5461062A Condensed imidazopyridine derivatives 失效
标题翻译：缩合咪唑并吡啶衍生物
公开(公告)号：US5461062A
公开(公告)日：1995-10-24
申请号：US297885
申请日：1994-08-30
申请人： Susumu Takada , Takashi Sasatani , Nobuo Chomei , Makoto Adachi , Akira Matsushita
发明人： Susumu Takada , Takashi Sasatani , Nobuo Chomei , Makoto Adachi , Akira Matsushita
IPC分类号： A61K31/435 , A61K31/47 , A61P25/20 , A61P25/26 , A61P25/28 , C07D471/04 , C07D471/14 , C07D491/14 , C07D491/147 , C07D495/04 , C07D495/14 , A61K31/44
CPC分类号： C07D471/04 , C07D471/14 , C07D491/14 , C07D495/14
摘要： A compound of the formula: ##STR1## wherein R is an optionally substituted phenyl group, 5-membered; the A ring is a 5 to 7 membered alicyclic group in which said A ring may have an alkyl group as a substituent, or a pharmaceutically acceptable salt thereof, and is useful as a psychotropic agent.
摘要翻译：下式的化合物：其中R是任选取代的苯基，5元; A环是所述A环可以具有烷基作为取代基的5〜7元脂环基，或其药学上可接受的盐，可用作精神药剂。

2. 发明授权

US5378848A Condensed imidazopyridine derivatives 失效
标题翻译：缩合咪唑并吡啶衍生物
公开(公告)号：US5378848A
公开(公告)日：1995-01-03
申请号：US12424
申请日：1993-02-02
申请人： Susumu Takada , Takashi Sasatani , Nobuo Chomei , Makoto Adachi , Akira Matsushita
发明人： Susumu Takada , Takashi Sasatani , Nobuo Chomei , Makoto Adachi , Akira Matsushita
IPC分类号： A61K31/435 , A61K31/47 , A61P25/20 , A61P25/26 , A61P25/28 , C07D471/04 , C07D471/14 , C07D491/14 , C07D491/147 , C07D495/04 , C07D495/14
CPC分类号： C07D471/04 , C07D471/14 , C07D491/14 , C07D495/14
摘要： A compound of the formula: ##STR1## wherein R is an optionally substituted aryl group or an optionally substituted aromatic heterocycle group; A ring is a 5 to 9 membered alicyclic group, in which one or more of carbon atoms constituting said A ring may be replaced by O, or S and said A ring may have alkyl as a substituent, or a pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物：其中R是任选取代的芳基或任选取代的芳族杂环基团; 环是5至9元脂环基，其中构成所述A环的一个或多个碳原子可以被O或S替代，并且所述A环可以具有烷基作为取代基，或其药学上可接受的盐。

3. 发明授权

US4200757A Process for the production of 3-aminoisoxazoles 失效
标题翻译：生产3-氨基异恶唑的方法
公开(公告)号：US4200757A
公开(公告)日：1980-04-29
申请号：US912252
申请日：1978-06-05
申请人： Yasuo Makisumi , Akira Murabayashi , Takashi Sasatani
发明人： Yasuo Makisumi , Akira Murabayashi , Takashi Sasatani
IPC分类号： C07D261/14 , C07D261/08
CPC分类号： C07D261/14
摘要： 3-Aminoisoxazoles of the formula: ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, phenyl or halo-phenyl) are prepared by reacting a .beta.-ketonitrile of the formula:R--CO--CH.sub.2 CN(wherein R is as defined above) with a compound of the formula:HY(wherein Y is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio) in the presence of an acid in a solvent to give an iminium salt of the formula: ##STR2## (wherein X is the residue of said acid; R and Y are each as defined above) and further reacting the iminium salt with hydroxylamine in an inert solvent.
摘要翻译：下式的3-氨基异恶唑：其中R为C1-C6烷基，苯基或卤素 - 苯基）是通过使下式所示的β-甲酯与下式反应来制备的：式中R-CO-CH 2 CN（其中R如上定义）与下式的化合物HY（其中Y是C 1 -C 6烷氧基或C 1 -C 6烷硫基）在酸的存在下在溶剂中反应，得到下式的亚铵盐：其中X是所述酸; R和Y各自如上所定义），并进一步使亚胺盐与羟胺在惰性溶剂中反应。

4. 发明授权

US4753951A Condensed imidazopyridine derivatives useful as psychotropic agents 失效
标题翻译：用作精神药物的缩合咪唑并吡啶衍生物
公开(公告)号：US4753951A
公开(公告)日：1988-06-28
申请号：US920162
申请日：1986-10-17
申请人： Susumu Takada , Toshio Fujishita , Takashi Sasatani , Akira Matsushita , Masami Eigyo
发明人： Susumu Takada , Toshio Fujishita , Takashi Sasatani , Akira Matsushita , Masami Eigyo
IPC分类号： C07D471/04 , C07D495/14 , A61K31/47 , C07D471/14
CPC分类号： C07D471/04 , C07D495/14
摘要： A compound of the formula: ##STR1## (wherein R is phenyl optionally substituted by one or two members selected from the group consisting of trifluoromethyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, nitro, amino C.sub.1 -C.sub.5 alkanoylamino and C.sub.1 -C.sub.5 alkoxycarbonyl or 5- or 6-membered heterocyclic group optionally substituted by one or two members selected from the group consisting of halogen, C.sub.1 -C.sub.5 alkyl and C.sub.1 -C.sub.5 alkoxy,Q is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.10 acyl, C.sub.1 -C.sub.5 alkylsulfonyl or C.sub.6 -C.sub.10 arylsulfonyl, ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen, halogen C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.5 haloalkyl,Q is present on the nitrogen atom of the 1,3 or 5-position, and the dotted line indicates the presence of three double bonds at the position of 2, 3; 3a, 3b; 4, 5 / 1, 3b; 2, 3; 3a, 4 / or 1, 2; 3a, 3b; 4, 5)or its salt, being useful as psychostimulants or anxiolytics, is provided.
摘要翻译：下式的化合物：其中R是任选被一个或两个选自三氟甲基，C 1 -C 5烷基，C 1 -C 5烷氧基，C 1 -C 5烷硫基，硝基，氨基，任选被一个或两个选自卤素，C 1 -C 5烷基和C 1 -C 5烷氧基的成员取代的C 1 -C 5烷酰基氨基和C 1 -C 5烷氧基羰基或5或6元杂环基，Q是氢，C 1 -C 5 烷基，C 1 -C 10酰基，C 1 -C 5烷基磺酰基或C 6 -C 10芳基磺酰基，R 1，R 2，R 3和R 4各自为氢，卤素C 1 -C 5烷基，C 1 -C 5烷氧基或C 1 -C 5烷氧基， C5卤代烷基，Q存在于1,3或5位的氮原子上，虚线表示在2,3,3a，3b; 4,5 / 1,3b的位置存在三个双键 ; 2,3,3a，4 /或1,2; 3a，3b; 4,5）或其盐，可用作精神兴奋剂或抗焦虑剂。

5. 发明授权

US08367666B2 3-carbamoyl-2-pyridone derivatives 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US08367666B2
公开(公告)日：2013-02-05
申请号：US13407520
申请日：2012-02-28
申请人： Takashi Sasatani , Yoshiharu Hiramatsu , Susumu Mitsumori
发明人： Takashi Sasatani , Yoshiharu Hiramatsu , Susumu Mitsumori
IPC分类号： A61K31/5377 , A61K31/435 , A61K31/4412 , A61K31/496 , A61K31/506 , A61P17/00 , C07D211/84 , C07D221/04 , C07D401/12 , C07D413/12
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1，R 2，R 3，R 4和G如本文所定义，其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

6. 发明申请

US20120208813A1 3-CARBAMOYL-2-PYRIDONE DERIVATIVES 有权
标题翻译： 3-羰基-2-吡啶酮衍生物
公开(公告)号：US20120208813A1
公开(公告)日：2012-08-16
申请号：US13407520
申请日：2012-02-28
申请人： Natsuki ISHIZUKA , Takashi SASATANI , Yoshiharu HIRAMATSU , Masanao INAGAKI , Masahide ODAN , Hiroshi HASHIZUMI , Susumu MITSUMORI , Yasuhiko FUJII , Yoshikazu FUKUI , Hideaki WATANABE , Jun SATO
发明人： Natsuki ISHIZUKA , Takashi SASATANI , Yoshiharu HIRAMATSU , Masanao INAGAKI , Masahide ODAN , Hiroshi HASHIZUMI , Susumu MITSUMORI , Yasuhiko FUJII , Yoshikazu FUKUI , Hideaki WATANABE , Jun SATO
IPC分类号： A61K31/435 , C07D495/04 , A61K31/4365 , A61P17/00 , A61K31/496 , A61K31/506 , C07D413/12 , A61K31/5377 , C07D221/04 , C07D401/12
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1，R 2，R 3，R 4和G如本文所定义，其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

7. 发明申请

US20050043387A1 Tricyclic indole compounds having an affinity against serotonin receptors 审中-公开
标题翻译：对5-羟色胺受体具有亲和力的三环吲哚化合物
公开(公告)号：US20050043387A1
公开(公告)日：2005-02-24
申请号：US10947172
申请日：2004-09-23
申请人： Yoshikazu Fukui , Makoto Adachi , Takashi Sasatani
发明人： Yoshikazu Fukui , Makoto Adachi , Takashi Sasatani
IPC分类号： A61P5/28 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D491/06 , A61K31/55 , A61K31/407 , A61K31/454 , C07D491/02
CPC分类号： C07D491/06
摘要： Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems. (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ═O or ═S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on)
摘要翻译：对于5-羟色胺受体具有亲和性，下文所示的化合物（I）可用作抗各种中枢神经系统疾病的治疗剂。（其中R 1为氢; R 2为氢或低级烷基; R 3为氢，-COOR 12等; R 4为氢，低级烷基等，或R R 3和R 4一起可以形成= O或= S; R 5是氢，或者R 3和R 5一起可以形成键; R 6是氢， COOR 24等; R 7是氢，卤素，低级烷基等; R 8是氢，低级烷基，环烷基等; R 9，R 10和R 10， 11>各自独立地为氢，卤素，低级烷基等）

8. 发明授权

US06858640B2 Tricyclic indole compounds having affinity for serotonin receptor 失效
标题翻译：对5-羟色胺受体具有亲和力的三环吲哚化合物
公开(公告)号：US06858640B2
公开(公告)日：2005-02-22
申请号：US10312818
申请日：2001-09-17
申请人： Yoshikazu Fukui , Makoto Adachi , Takashi Sasatani
发明人： Yoshikazu Fukui , Makoto Adachi , Takashi Sasatani
IPC分类号： A61P5/28 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D491/06 , A61K31/40 , C07D491/044
CPC分类号： C07D491/06
摘要： Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems; (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ═O or ═S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on).
摘要翻译：对于5-羟色胺受体具有亲和力，下文所示的化合物（I）可用作抗各种中枢神经系统疾病的治疗剂;（其中R 1是氢; R 2是氢或低级烷基; 3>是氢，-COOR 12等; R 4是氢，低级烷基等，或者R 3和R 4一起可以形成= O或= S; R 5 >是氢，或R 3和R 5一起形成键; R 6是氢，-COOR 24等; R 7是氢，卤素，低级烷基等 R 8是氢，低级烷基，环烷基等; R 9，R 10和R 11各自独立地是氢，卤素，低级烷基等）。

9. 发明授权

US4910318A Tetrahydrothiopyrano(3,2-b)-indole derivatives 失效
标题翻译：四氢噻喃（3,2-b） - 吲哚衍生物
公开(公告)号：US4910318A
公开(公告)日：1990-03-20
申请号：US633686
申请日：1984-07-25
申请人： Yasuo Makisumi , Takashi Sasatani
发明人： Yasuo Makisumi , Takashi Sasatani
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61P25/04 , A61P29/00 , C07D209/30 , C07D495/04
CPC分类号： C07D495/04 , C07D209/30
摘要： Tetrahydrothiopyrano[3,2-b]indole derivatives represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, phenyl-C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, or ##STR2## wherein Y is C.sub.1-4 alkylene or C.sub.1-4 oxoalkylene and R.sup.5 and R.sup.6 each is hydrogen or C.sub.1-4 alkyl;R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.3-6 cycloalkyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or ##STR3## wherein Y, R.sup.5 and R.sup.6 each is as defined above; or ##STR4## is pyrrolidino, piperdinyl, piperazinyl, 4-C.sub.1-4 alkylpiperazinyl or morpholino;R.sup.4 is hydrogen or C.sub.1-4 alkyl; andn is 0 or an integer of 1 or 2and the pharmaceutically acceptable salts being useful as analgesic and anti-inflammatory agents as well as psychoanaleptic and nootropic drug.
摘要翻译：由式I表示的四氢噻喃并[3,2-b]吲哚衍生物：其中R 1是氢，C 1-4烷基，C 2-4烯基，C 2-4炔基，苯基-C 1-4烷基，C 2-5 烷酰基或者其中Y是C 1-4亚烷基或C 1-4亚氧基亚烷基，R 5和R 6各自是氢或C 1-4烷基; R2是氢，C1-4烷基或C3-6环烷基; R 3是氢，C 1-4烷基或者其中Y，R 5和R 6各自如上所定义; 或是吡咯烷子基，哌啶基，哌嗪基，4-C 1-4烷基哌嗪基或吗啉代; R4是氢或C1-4烷基; 并且n为0或1或2的整数，并且其药学上可接受的盐可用作镇痛和抗炎剂以及精神无菌和益智药。

10. 发明授权

US4183856A Process for the production of urea derivatives 失效
标题翻译：尿素衍生物生产工艺
公开(公告)号：US4183856A
公开(公告)日：1980-01-15
申请号：US895105
申请日：1978-04-10
申请人： Yasuo Makisumi , Takashi Sasatani , Akira Murabayashi
发明人： Yasuo Makisumi , Takashi Sasatani , Akira Murabayashi
IPC分类号： C07D275/02 , C07D213/75 , C07D261/14 , C07D263/48 , C07D275/03 , C07D277/20 , C07D277/38 , C07D277/46 , C07D277/48 , C07D277/82
CPC分类号： C07D213/75 , C07D261/14 , C07D275/03 , C07D277/48 , C07D277/82
摘要： Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.
摘要翻译：下式的脲衍生物（其中Ar表示5或6元杂芳环的残基; R表示氢原子或C1-C6烷基; R1表示C1-C6烷基; R2表示 C 1 -C 6烷基，C 2 -C 6烯基或C 1 -C 6烷氧基）通过使式Ar-NH-R（其中Ar和R具有上述含义）具有下式的氨基甲酰卤化物：图像（其中X表示卤原子，R1和R2具有上述含义）在路易斯酸存在下在惰性溶剂中反应。

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