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1. 发明授权

US4493832A Certain glycerol-phosphoryl choline derivatives, compositions containing same and method of using same 失效
标题翻译：某些甘油 - 磷酰胆碱衍生物，含有其的组合物及其使用方法
公开(公告)号：US4493832A
公开(公告)日：1985-01-15
申请号：US391918
申请日：1982-06-24
申请人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
IPC分类号： A61K31/66 , A61P9/12 , C07F9/09 , C07F9/10 , C07F9/40 , C07F9/58 , C07F9/141 , C07F9/143 , A61K31/685
CPC分类号： C07F9/581 , C07F9/091 , C07F9/10 , C07F9/4075
摘要： New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, alkylthio, ar(lower)alkoxy or alkanoylamino; R.sup.2 is lower alkyl or ar(lower)alkyl; n is an integer of 0 or 1; A is lower alkylene; R.sup.3 is pyridinio or a group of the formula: ##STR2## in which R.sup.5, R.sup.6 and R.sup.7 are each hydrogen or lower alkyl; and R.sup.4 is hydrogen or lower alkyl; and pharmaceutically acceptable salt thereof, which exhibit anti-hypertensive activity.
摘要翻译：由下式表示的新型磷脂衍生物：其中R1是烷基，烷氧基，烷硫基，芳（低级）烷氧基或烷酰基氨基; R2是低级烷基或芳（低级）烷基; n为0或1的整数; A是低级亚烷基; R 3是吡啶鎓或下式的基团：其中R 5，R 6和R 7各自为氢或低级烷基; R4为氢或低级烷基; 和其药学上可接受的盐，其表现出抗高血压活性。

2. 发明授权

US4562179A Phospholipid derivatives, and pharmaceutical composition of the same 失效
标题翻译：磷脂衍生物及其药物组成相同
公开(公告)号：US4562179A
公开(公告)日：1985-12-31
申请号：US482447
申请日：1983-04-06
申请人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
IPC分类号： A61K31/685 , A61P35/00 , C07C43/13 , C07F9/09 , C07F9/10 , C07F9/40
CPC分类号： C07F9/091 , C07C43/135 , C07F9/10 , C07F9/4006 , C07F9/4075
摘要： New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy or alkanoylamino;R.sup.2 is lower alkyl, lower alkanesulfonyl or arenesulfonyl;R.sup.3, R.sup.4 and R.sup.5 are each lower alkyl;n is 0 or 1A is lower alkylene optionally interrupted by a --NHCO-- group; andQ is oxido or lower alkoxy;provided that n is 0 or A is lower alkylene interrupted by a --NHCO-- group, or Q is lower alkoxy, when R.sup.1 is alkoxy and R.sup.2 is lower alkyl; and pharmaceutically acceptable salts thereof, which exhibit antitumor activity.
摘要翻译：由下式表示的新型磷脂衍生物：其中R 1为烷基，烷氧基或烷酰基氨基; R2是低级烷基，低级烷基磺酰基或芳烃磺酰基; R3，R4和R5各自为低级烷基; n为0或1 A为任选被-NHCO-基团中断的低级亚烷基; Q为氧化或低级烷氧基; 条件是当R 1为烷氧基且R 2为低级烷基时，n为0或A为被-NHCO-基团中断的低级亚烷基，或Q为低级烷氧基。和其药学上可接受的盐，其具有抗肿瘤活性。

3. 发明授权

US4481196A Glycoside phosphate derivatives, pharmaceutical composition of the same and method of use 失效
标题翻译：糖苷磷酸衍生物，药物组合物的使用方法和使用方法
公开(公告)号：US4481196A
公开(公告)日：1984-11-06
申请号：US528062
申请日：1983-08-31
申请人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
IPC分类号： C07H11/04 , C07H15/04 , A61K31/70 , C07H15/02
CPC分类号： C07H11/04 , C07H15/04
摘要： New phosphate derivatives represented by the formula: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are each hydroxy, alkoxy, alkanoylamino or protected hydroxy;A is lower alkylene;R.sup.4 is alkylammonio, cyclic ammonio or cyclic amino; andR.sup.5 is oxido anion or hydroxy;and pharmaceutically acceptable salt thereof, which exhibit antitumor activity.
摘要翻译：由下式表示的新型磷酸酯衍生物：其中R 1，R 2和R 3各自为羟基，烷氧基，烷酰基氨基或被保护的羟基; A是低级亚烷基; R4是烷基氨基，环氨基或环状氨基; R5是氧化阴离子或羟基; 和其药学上可接受的盐，其具有抗肿瘤活性。

4. 发明授权

US4585762A Phospholipid derivatives, processes for use thereof and pharmaceutical composition of the same 失效
标题翻译：磷脂衍生物，其使用方法及其药物组合物
公开(公告)号：US4585762A
公开(公告)日：1986-04-29
申请号：US513451
申请日：1983-07-13
申请人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Eishiro Todo , Norihiko Shimazaki , Teruo Oku , Takayuki Namiki
IPC分类号： A01N57/12 , A61K31/66 , A61P35/00 , C07D309/12 , C07F9/09 , C07F9/10 , C07F9/117 , C07H9/04 , C07H11/04 , C07H13/04 , C07H13/08
CPC分类号： C07H9/04 , C07C309/00 , C07D309/12 , C07F9/091 , C07F9/10 , C07F9/117 , C07H11/04 , C07H13/04 , C07H13/08
摘要： New phospholipid derivatives represented by the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, alkylthio or alkylsulfonyl;R.sup.2 is hydrogen, hydroxy, alkoxy, lower alkanoyloxy or lower alkylcarbamoyloxy;n is 0 or 1;R.sup.3 is hydroxy or protected hydroxy; andR.sup.4 is lower alkoxy or lower alicyclic-oxy group which is substituted with 2 or more hydroxy or protected hydroxy groups, and may be substituted with lower alkoxy or another alicyclic-oxy group having two or more hydroxy or protected hydroxy groups, in which the alicyclic ring may contain an oxygen atom;and pharmaceutically acceptable salt thereof, which exhibit antitumor activity.
摘要翻译：由下式表示的新型磷脂衍生物：其中R 1是烷基，烷氧基，烷硫基或烷基磺酰基; R2是氢，羟基，烷氧基，低级烷酰氧基或低级烷基氨基甲酰氧基; n为0或1; R3是羟基或被保护的羟基; R4为被2个以上羟基或被保护的羟基取代的低级烷氧基或低级脂环氧基，可以被低级烷氧基或具有两个以上羟基或保护羟基的另一个脂环氧基取代，其中脂环可以含有氧原子; 和其药学上可接受的盐，其具有抗肿瘤活性。

5. 发明授权

US4806538A Piperazine compound as PAF-antagonist 失效
标题翻译：哌嗪化合物作为PAF拮抗剂
公开(公告)号：US4806538A
公开(公告)日：1989-02-21
申请号：US031577
申请日：1987-03-30
申请人： Norihiko Shimazaki , Keiji Hemmi , Osamu Nakaguti , Yoshio Miyazaki , Masashi Hashimoto
发明人： Norihiko Shimazaki , Keiji Hemmi , Osamu Nakaguti , Yoshio Miyazaki , Masashi Hashimoto
IPC分类号： C07D241/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D417/14 , A61K31/495
CPC分类号： C07D401/06 , C07D241/08 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D417/14
摘要： The invention relates to a PAF-antagonist pharmaceutical composition comprising a compound of the formula: ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl or thiazolyl(lower)alkyl,R.sup.2 is N-lower alkylindolyl(lower)alkyl which may have lower alkyl or halogen on the indole ring, andR.sup.3 and R.sup.4 are each hydrogen or lower alkyl; or pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及包含下式化合物的PAF拮抗剂药物组合物：其中R 1是吡啶基（低级）烷基或噻唑基（低级）烷基，R 2是可以具有低级烷基的低级烷基（低级）烷基或吲哚环上的卤素，R3和R4各自为氢或低级烷基; 或其药学上可接受的盐。

6. 发明授权

US5304560A Quinazoline derivatives and their preparation 失效
标题翻译：喹唑啉衍生物及其制备方法
公开(公告)号：US5304560A
公开(公告)日：1994-04-19
申请号：US103315
申请日：1993-08-09
申请人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka
发明人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka
IPC分类号： A61K31/505 , A61K31/517 , A61P9/00 , A61P9/12 , A61P25/00 , A61P37/00 , C07D239/96 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D521/00 , A61K31/495 , C07D241/04 , C07D
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D401/06
摘要： This invention relates to certain 1-heterocycloalkylquinazolin-2,3-dione derivatives, certain pharmaceutically acceptable salts thereof, the process of making those compounds, and the method of using the compounds. The compounds and compositions display effects on the peripheral or central nervous system.
摘要翻译：本发明涉及某些1-杂环烷基喹唑啉-2,3-二酮衍生物，其某些药学上可接受的盐，制备这些化合物的方法和使用该化合物的方法。化合物和组合物对周围或中枢神经系统表现出影响。

7. 发明授权

US4725608A Semicarbazide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：氨基脲衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US4725608A
公开(公告)日：1988-02-16
申请号：US673845
申请日：1984-11-21
申请人： Osamu Nakaguchi , Norihiko Shimazaki , Yoshio Kawai , Masashi Hashimoto , Michie Nakatuka
发明人： Osamu Nakaguchi , Norihiko Shimazaki , Yoshio Kawai , Masashi Hashimoto , Michie Nakatuka
IPC分类号： C07D203/26 , C07D211/70 , C07D213/89 , C07D237/04 , C07D295/28 , A61K31/435 , C07D211/98
CPC分类号： C07D213/89 , C07D203/26 , C07D211/70 , C07D237/04 , C07D295/32
摘要： New semicarbazide derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; orR.sup.1 and R.sup.2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,R.sup.5 is hydrogen or lower alkyl, andX is O or S, provided that the lower alkyl group for R.sup.3 is (C.sub.3 -C.sub.6)alkyl, when R.sup.2 is hydrogen or (C.sub.1 -C.sub.2) alkyl and R.sup.4 is aryl optionally having substituent(s) selected from groups consisting of halogen, lower alkyl, lower alkoxy and halo(lower)alkyl, and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiinflammatory and analgesic agents.
摘要翻译：新的下式的氨基脲衍生物：其中R1是氢，R2是氢，低级烷基，芳基（低级）烷基，低级烯基或芳基，R3是低级烷基，芳基（低级）烷基，低级烯基或芳基，或 R2和R3一起形成任选被芳基取代的（C 2 -C 6）亚烷基或与相邻的氮原子一起形成任选被芳基取代的饱和或不饱和的5或6元杂环基; 或者R1和R2与相邻的氮原子一起形成饱和或不饱和的5或6元杂环基或1,2-二氮杂环烷-1,2-二基，R3是氢，低级烷基，ar（低级）烷基，低级烯基或芳基; R4是可以具有选自低级烷基，卤素，低级烷氧基，低级烷基氨基，卤代（低级）烷基，羟基，低级烷酰基，酯化羧基和羧基的取代基的芳基，R 5是氢或低级烷基，X是O 或者当R 2为氢或（C 1 -C 2）烷基，且R 4为任选具有选自以下的取代基的芳基时，R 3的低级烷基为（C 3 -C 6）烷基：（C 3 -C 6）烷基，低级烷基，低级烷氧基和卤代（低级）烷基及其药学上可接受的盐，及其制备方法和包含其的药物组合物。这些衍生物和其盐可用作抗炎和止痛剂。

8. 发明授权

US06426345B1 Heterobicyclic derivatives 失效
标题翻译：异环衍生物
公开(公告)号：US06426345B1
公开(公告)日：2002-07-30
申请号：US08793451
申请日：1998-01-30
申请人： Norihiko Shimazaki , Shinya Watanabe , Akihiko Sawada , Keiji Hemmi
发明人： Norihiko Shimazaki , Shinya Watanabe , Akihiko Sawada , Keiji Hemmi
IPC分类号： C07D48704
CPC分类号： C07D471/04
摘要： Heterobicyclic derivatives of the formula: wherein R1 is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected carboxy(lower)alkyl, acyl(lower)alkyl, heterocyclic group or heterocyclic(lower)alkyl which may have suitable substituent(s), R2 is aryl which may have suitable substituent(s) or heterocyclic group, and R3 is hydrogen, lower alkoxy or arylthio, and a pharmaceutically acceptable salt thereof which are useful as a medicament.
摘要翻译：下式的双环衍生物：其中R 1是可具有合适取代基的芳基，可具有合适取代基的芳基（低级）烷基，卤代（低级）烷基，保护的羧基（低级）烷基，酰基（低级）烷基，可具有合适取代基的杂环基或杂环（低级）烷基，R 2为可具有合适的取代基或杂环基的芳基，R 3为氢，低级烷氧基或芳硫基，及其药学上可接受的盐，其为可用作药物。

9. 发明授权

US6117875A Pyrido (2,3-B) pyrazine derivatives 失效
标题翻译：吡啶（2,3-B）吡嗪衍生物
公开(公告)号：US6117875A
公开(公告)日：2000-09-12
申请号：US91361
申请日：1998-06-19
申请人： Norihiko Shimazaki , Akihiko Sawada , Shinya Watanabe
发明人： Norihiko Shimazaki , Akihiko Sawada , Shinya Watanabe
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61P43/00 , C07D471/04 , A01N43/60 , C07D241/36
CPC分类号： C07D471/04 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl, N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl,R.sup.2 is aminophenyl, [protected amino]phenyl, [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]phenyl, [thiazolylcarbonylamino]phenyl which may have pyridyl, naphthyl having lower alkoxy and halogen, [dihalophenyl](lower)alkenyl, [N-oxidopyridyl](lower)alkenyl, [aminopyridyl](lower)alkenyl, [protected aminopyridyl](lower)alkenyl, [carboxypyridyl](lower)alkenyl, [protected carboxypyridyl](lower)alkenyl, [[pyridyl(lower)alkenyl]pyridyl](lower)alkenyl, [[carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [[protected carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [pyridyl(lower)alkenyl]pyridyl, lower alkylbenzothiazolyl or [halopyridylcarbonyl]amino,with proviso that when R.sup.2 is [[4-pyridyl(lower)alkenoyl]amino]phenyl, aminophenyl, [lower alkanoylamino]phenyl or [dihalophenyl](lower)alkenyl, thenR.sup.1 is N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl,and a pharmaceutically acceptable salt thereof, which is useful as a medicament.
摘要翻译： PCT No.PCT / JP96 / 03666 Sec。 371日期：1998年6月19日 102（e）1998年6月19日PCT PCT 1996年12月13日PCT公布。公开号WO97 / 24355 日期：1997年7月10日具有下式的化合物：其中R1是吡啶基（低级）烷基，N-氧化吡啶基（低级）烷基或咪唑基（低级）烷基，R2是氨基苯基，[保护氨基]苯基，[[ 苯基，[[吡啶基（低级）烯酰基]氨基]苯基，[[[N-氧化吡啶基]（低级）烯酰基]氨基]苯基，[[[保护的氨基吡啶基]（低级）烯酰基] （低级）烯基，[N-氧化吡啶基]（低级）烯基，[氨基吡啶基]（低级）烯基，[保护的氨基吡啶基]（低级），低级烷氧基，烯基，[羧基吡啶基]（低级）烯基，[保护的羧基吡啶基]（低级）烯基，[[吡啶基（低级）烯基]吡啶基]（低级）烯基，[[羧基（低级）烯基]吡啶基] [保护的羧基（低级）烯基]吡啶基]（低级）烯基，[吡啶基（低级）烯基]吡啶基，低级烷基苯并噻唑基或[卤代吡啶基羰基]氨基，条件是当R 2是[[4-吡啶基（低级）烯酰基] 苯基，氨基苯基，[低级烷酰基氨基]苯基或[二卤代苯基]（低级）烯基，则R1是N-氧化吡啶基（低级）烷基或咪唑基（低级）烷基及其药学上可接受的盐，其可用作药物。

10. 发明授权

US5264438A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US5264438A
公开(公告)日：1993-11-23
申请号：US627417
申请日：1990-12-14
申请人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka , Yoshikuni Itoh , Masashi Hashimoto
发明人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka , Yoshikuni Itoh , Masashi Hashimoto
IPC分类号： A61K31/505 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/28 , C07D401/06 , C07D401/14 , C07D413/14
CPC分类号： C07D401/06
摘要： Compounds of the formula: ##STR1## are described wherein R.sup.1, R.sup.2, R.sup.3 and A are described in the claims. These compounds show significant dopamine receptor agonist activity.

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