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51. 发明授权

US5767293A Oxaspiro�2,5! octane derivative 失效
标题翻译： Oxaspiro [2,5]辛烷衍生物
公开(公告)号：US5767293A
公开(公告)日：1998-06-16
申请号：US287589
申请日：1994-08-05
申请人： Teruo Oku , Chiyoshi Kasahara , Takehiko Ohkawa , Masashi Hashimoto
发明人： Teruo Oku , Chiyoshi Kasahara , Takehiko Ohkawa , Masashi Hashimoto
IPC分类号： C07D303/12 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/44 , A61K31/443 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P5/24 , A61P9/00 , A61P35/00 , C07D303/16 , C07D303/18 , C07D303/22 , C07D303/34 , C07D303/38 , C07D405/12 , C07D405/14 , C07D215/16 , C07D279/12 , C07D303/04
CPC分类号： C07D303/22 , C07D303/34 , C07D405/12
摘要： Oxaspiro�2,5! octanes of the formula ##STR1## inhibit angiogenesis and are particularly suitable for the treatment of solid tumors. In preferred embodiments, R.sup.1 is a carbamoyl derivative, R.sup.2 is an alkoxy substituent and R.sup.3 is ##STR2## Pharmaceutical salts of these compounds, such as methyl, amonium and organic amine salts also exhibit desirable properties.
摘要翻译：具有式“IMAGE”的Oxaspiro [2,5]辛烷抑制血管发生，特别适用于治疗实体瘤。在优选的实施方案中，R 1是氨基甲酰基衍生物，R 2是烷氧基取代基，并且R 3是这些化合物的药用盐，例如甲基，二铵和有机胺盐也表现出所需的性质。

52. 发明授权

US5708172A Intermediates for synthetic use and processes for producing aminopiperazine derivatives 失效
标题翻译：用于合成的中间体和用于制备氨基哌嗪衍生物的方法
公开(公告)号：US5708172A
公开(公告)日：1998-01-13
申请号：US553551
申请日：1996-01-18
申请人： Teruo Oku , Hiroshi Kayakiri , Hirokazu Tanaka
发明人： Teruo Oku , Hiroshi Kayakiri , Hirokazu Tanaka
IPC分类号： C07D295/28 , C07D295/32
CPC分类号： C07D295/32
摘要： A novel industrial process excellent in yield and purity for preparing a compound of the formula: ##STR1## or a salt thereof, which comprises reacting a compound of the formula: ##STR2## or a salt thereof with a compound of the formula: R.sup.3 --A--OH or its reactive derivative or a salt thereof, wherein R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen, R.sup.3 is lower alkyl, aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen, A is ##STR3## or lower alkylene and ##STR4##
摘要翻译： PCT No.PCT / JP94 / 00933 Sec。 371日期：1996年1月18日 102（e）日期1996年1月18日PCT提交1994年6月8日PCT公布。公开号WO95 / 00502 日期1995年1月5日一种制备下式化合物或其盐的产率和纯度优异的新型工业方法，其包括使下式化合物或其盐与下式化合物其中R 2是环（低级）烷基，芳基或芳（低级）烷基，其各自可以被卤素取代，R 3是低级烷基，芳基，芳基（低级）烷氧基或杂环基，其各自可以被卤素取代，A是低级亚烷基和低级亚烷基，

53. 发明授权

US4889851A Benzothiadiazine compounds, and pharmaceutical composition comprising the same 失效
标题翻译：苯并噻二嗪化合物和包含它们的药物组合物
公开(公告)号：US4889851A
公开(公告)日：1989-12-26
申请号：US116913
申请日：1987-11-05
申请人： Teruo Oku , Eishiro Todo , Chiyoshi Kasahara , Katsuya Nakamura , Hiroshi Kayakiri
发明人： Teruo Oku , Eishiro Todo , Chiyoshi Kasahara , Katsuya Nakamura , Hiroshi Kayakiri
IPC分类号： C07D209/14 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/54 , A61K31/5415 , A61P3/00 , A61P19/10 , A61P29/00 , A61P43/00 , C07C67/00 , C07C301/00 , C07C311/39 , C07C311/40 , C07C311/42 , C07C313/00 , C07C323/49 , C07D209/40 , C07D209/86 , C07D209/88 , C07D213/76 , C07D215/38 , C07D217/22 , C07D233/02 , C07D233/88 , C07D239/69 , C07D249/04 , C07D249/08 , C07D249/14 , C07D249/18 , C07D257/04 , C07D261/14 , C07D263/00 , C07D271/00 , C07D285/24 , C07D295/12 , C07D307/52 , C07D333/36 , C07D417/04 , C07D417/06 , C07D521/00
CPC分类号： C07D213/76 , C07D239/69 , C07D285/24 , C07D417/04
摘要： A compound of the formula: ##STR1## wherein R' is phenyl, phenyl which is substituted with halogen, lower alkyl, lower alkoxy, halo lower alkyl, lower alkylamino, lower alkylthio, phenoxy, carboxy, lower alkoxycarbonyl, carboxy lower alkyl, lower alkoxycarbonyl, lower alkyl, cyclo lower alkyl; lower alkyl which is substituted with carboxy or lower alkoxyoxycarbonyl; or pyrimidinyl, pyridyl or pyridyl which is substituted with lower alkyl;A is lower alkylene;n is an integer of 0 or 1;R.sup.2 is lower alkyl;R.sup.3 is hydrogen; hydroxy; halogen; halo lower alkyl; lower alkyl; lower alkylamino; lower alkanoyl amino; lower alkanoyl lower alkylamino; lower alkoxy; lower alkoxy which is substituted with phenyl, phthalimido, pyranyl, amino, carboxy, lower alkoxycarbonyl, cyclo lower alkyl or cyclo lower alkyl which is substituted with amino lower alkyl or lower alkoxycarbonylamino lower alkyl; or cyclo lower alkyloxy or cyclo lower alkyloxy which is substituted with carboxy or lower alkoxycarbonyl;R.sup.4 is hydrogen or halogen, andR.sup.5 is hydrogen or halogen, with the provisoR.sup.1 is phenyl substituted with lower alkoxy, lower alkylamino, lower alkylthio, phenoxy, carboxy, lower alkoxycarbonyl, carboxyl lower alkyl or lower alkoxycarbonyl lower alkyl; lower alkyl or lower alkyl substituted with carboxy or lower alkoxycarbonyl; pyrimidinyl; pyridyl or pyridyl substituted with lower alkyl, when R.sup.3 is hydrogen or halogen, or a pharmaceutically acceptable salt thereof. The compounds and compositions containing the same are useful in the treatment of bone diseases.
摘要翻译：下式的化合物：其中R'是苯基，被卤素取代的苯基，低级烷基，低级烷氧基，卤代低级烷基，低级烷基氨基，低级烷硫基，苯氧基，羧基，低级烷氧基羰基，羧基低级烷基，低级烷氧基羰基，低级烷基，环低级烷基; 被羧基或低级烷氧基氧基羰基取代的低级烷基; 或被低级烷基取代的嘧啶基，吡啶基或吡啶基; A是低级亚烷基; n为0或1的整数; R2是低级烷基; R3是氢; 羟基; 卤素; 卤代低级烷基; 低级烷基; 低级烷基氨基; 低级烷酰基氨基; 低级烷酰基低级烷基氨基; 低级烷氧基被苯基，苯二甲酰亚氨基，吡喃基，氨基，羧基，低级烷氧基羰基，环低级烷基或被氨基低级烷基或低级烷氧基羰基氨基低级烷基取代的环低级烷基取代的低级烷氧基; 或被羧基或低级烷氧基羰基取代的环低级烷氧基或环低级烷氧基; R4为氢或卤素，R5为氢或卤素，条件是R1为被低级烷氧基，低级烷基氨基，低级烷硫基，苯氧基，羧基，低级烷氧基羰基，羧基低级烷基或低级烷氧基羰基低级烷基取代的苯基。被羧基或低级烷氧基羰基取代的低级烷基或低级烷基; 嘧啶基; 吡啶基或吡啶基被低级烷基取代，当R3为氢或卤素时，或其药学上可接受的盐。含有它们的化合物和组合物可用于治疗骨疾病。

54. 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。

55. 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。

56. 发明授权

US4382934A Isatin derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：靛红衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US4382934A
公开(公告)日：1983-05-10
申请号：US83271
申请日：1979-10-10
申请人： Tsutomu Teraji , Teruo Oku , Takayuki Namiki
发明人： Tsutomu Teraji , Teruo Oku , Takayuki Namiki
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61K31/495 , A61K31/535 , A61P11/00 , A61P37/08 , C07D209/38 , C07D209/40 , C07D209/60 , C07D295/067 , C07D403/06
CPC分类号： C07D295/067 , C07D209/38 , C07D209/40 , C07D209/60
摘要： A compound of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, halogen, lower alkyl, lower alkoxy, halo (lower) alkyl, lower alkanoylamino, lower alkoxyalylamino, or a 5 to 6 membered saturated or unsaturated heterocyclic group having at least one imino group, and selected from the group consisting of pyrrolidinyl, pyrrolinyl, imidazolidinyl, piperazinyl, piperidyl, and morpholynyl,or R.sup.1 and R.sup.2 are combined together to form a benzene ring,R.sup.3 is oxo or a group of the formula .dbd.N--OR.sup.5, in which R.sup.5 is hydrogen or lower alkyl,R.sup.4 is mono- or di- or triphenyl (lower) alkyl,A is C.sub.1 to C.sub.7 alkylene and its hydroxy derivatives,Y is (C.sub.1 to C.sub.3) alkylene,or a pharmaceutically acceptable salt thereof.Said compounds having antiallergic properties represent inclusively all of the possible optical and/or geometrical isomers due to the asymmetric carbon and carbon-nitrogen double bond.
摘要翻译：下式的化合物：其中R 1和R 2是氢，卤素，低级烷基，低级烷氧基，卤代（低级）烷基，低级烷酰氨基，低级烷氧基氨基或5至6元饱和或不饱和杂环基，至少一个亚氨基，并且选自吡咯烷基，吡咯啉基，咪唑烷基，哌嗪基，哌啶基和吗啉基，或者R 1和R 2结合在一起形成苯环，R 3是氧代或式= N- OR5，其中R5是氢或低级烷基，R4是一或二或三苯基（低级）烷基，A是C1-C7亚烷基及其羟基衍生物，Y是（C1-C3）亚烷基或其药学上可接受的盐其中。由于不对称碳和碳 - 氮双键，所述具有抗过敏性质的化合物包括所有可能的光学和/或几何异构体。

57. 发明授权

US4308380A 2-Lower alkyl-2 or 3-cephem-4-carboxylic acid derivatives 失效
标题翻译： 2-低级烷基-2-或3-头孢烯-4-羧酸衍生物
公开(公告)号：US4308380A
公开(公告)日：1981-12-29
申请号：US915872
申请日：1978-06-15
申请人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
发明人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
IPC分类号： A61K31/545 , C07D499/00 , C07D501/20
CPC分类号： C07D501/20 , A61K31/545 , C07D499/00
摘要： A compound of the formula ##STR1## wherein R.sup.1 is amino or substituted amino, R.sup.2 is carboxy or protected carboxy, R.sup.3 is lower alkyl and X is --S-- or ##STR2## or a pharmaceutically acceptable salt thereof is effective against various microorganisms.
摘要翻译：其中R1为氨基或取代氨基，R2为羧基或被保护的羧基，R3为低级烷基且X为-S-或其药学上可接受的盐对各种微生物有效的式IMA化合物。

58. 发明授权

US4237305A Substituted phenylacetic acid compounds and process for preparation thereof 失效
标题翻译：取代苯乙酸化合物及其制备方法
公开(公告)号：US4237305A
公开(公告)日：1980-12-02
申请号：US782968
申请日：1977-03-30
申请人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Hidekazu Takeno
发明人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Hidekazu Takeno
IPC分类号： C07C45/71 , C07C59/90 , C07C67/00 , C07C227/00 , C07C229/22 , C07C229/36 , C07C233/18 , C07C233/47 , C07C239/00 , C07C251/32 , C07C251/48 , C07C271/22 , C07D205/085 , C07D209/48 , C07C125/065
CPC分类号： C07D209/48 , C07C45/71 , C07C59/90 , C07D205/085
摘要： Substituted phenylacetic acid compounds represented by the following general formula and preparation thereof: ##STR1## wherein R.sup.1 is hydrogen or protected carboxy,R.sup.2 is hydrogen, or protected amino, provided that when R.sup.1 is hydrogen, then R.sup.2 is protected amino, and when R.sup.2 is hydrogen, then R.sup.1 is protected carboxy,R.sup.3 is oxo, hydroxyimino or protected hydroxyimino,R.sup.4 is hydrogen or halogen, andm is an integer of 1 to 3.
摘要翻译：由以下通式表示的取代的苯乙酸化合物及其制备：其中R 1为氢或被保护的羧基，R 2为氢或被保护的氨基，条件是当R 1为氢时，则R 2为保护的氨基，当R 2为氢，则R1为被保护的羧基，R3为氧代，羟基亚氨基或被保护的羟基亚氨基，R4为氢或卤素，m为1〜3的整数。

59. 发明授权

US4203897A Penam derivatives 失效
公开(公告)号：US4203897A
公开(公告)日：1980-05-20
申请号：US32293
申请日：1979-04-23
申请人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
发明人： Takashi Kamiya , Tsutomu Teraji , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku
IPC分类号： C07D205/095 , C07D499/00 , C07D499/44
CPC分类号： C07D205/095 , C07D499/00
摘要： A compound of the general formula: ##STR1## wherein R.sup.1 is amino or a conventional, pharmaceutically acceptable acylamino, R.sup.2 is carboxy or a conventionally protected carboxy, X is --S-- or ##STR2## R.sup.3 is lower alkyl and Y" is a residue of a strong nucleophile selected from the group consisting of azido, thiocyanato, lower alkyanoylthio and piperidinothiocarbonylthio.

60. 发明授权

US4181800A 2-Azetidinone compounds and processes for preparation thereof 失效
标题翻译： 2-氮杂环丁酮化合物及其制备方法
公开(公告)号：US4181800A
公开(公告)日：1980-01-01
申请号：US730012
申请日：1976-10-06
申请人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Yoshiharu Nakai , Hidekazu Takeno
发明人： Takashi Kamiya , Masashi Hashimoto , Osamu Nakaguti , Teruo Oku , Yoshiharu Nakai , Hidekazu Takeno
IPC分类号： C07C323/25 , C07D205/08 , C07D205/085 , C07D205/095 , C07D251/04 , C07D251/00 , A01N9/00
CPC分类号： C07C323/25 , C07D205/08 , C07D205/085 , C07D205/095 , C07D251/04
摘要： This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various groups at the fourth position of the azetidinone nucleus, which have antimicrobial activities against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammal including human being and animals.
摘要翻译：本发明涉及具有抗微生物活性的新的2-氮杂环丁酮化合物及其制备方法，更具体地说，本发明提供新的2-氮杂环丁酮化合物，特别是在第一位置具有各种取代的羧基烷基的化合物，在氮杂环丁酮核的第四位置的组，其具有针对各种致病微生物的抗微生物活性，并且可用作治疗哺乳动物包括人和动物的微生物感染的抗生素。

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