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公开(公告)号:US5204326A
公开(公告)日:1993-04-20
申请号:US493359
申请日:1990-03-14
申请人: Setsuro Fujii, deceased , by Keiko Fujii, successor , by Shinichiro Fujii, successor , by Kaoruko Takada, successor , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Naosumi Kinoshita , Shizuo Nakamura , Mitsuru Hirohashi , Takashi Sakamoto , Kazuhiko Tsutsumi , Tetsuhiko Shirasaka
发明人: Setsuro Fujii, deceased , by Keiko Fujii, successor , by Shinichiro Fujii, successor , by Kaoruko Takada, successor , Yoshihito Yamamoto , Fumio Shimizu , Masatoshi Inai , Naosumi Kinoshita , Shizuo Nakamura , Mitsuru Hirohashi , Takashi Sakamoto , Kazuhiko Tsutsumi , Tetsuhiko Shirasaka
IPC分类号: A61K38/00 , C07K14/585
CPC分类号: C07K14/585 , A61K38/00
摘要: Novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, having the activities for inhibiting bone calcium absorption, for lowering the blood level of calcium, as analgesics, for inhibiting secretion of the gastric juice.Pharmaceutical composition can be prepared by formulating, at least one of the novel polypeptide derivatives, acid-addition salts thereof and complexes thereof, together with a proteolytic enzyme inhibitors and/or pharmaceutically acceptable acids.The pharmaceutical composition are quite effective as agents for curing hypercalcemia, for curing Peget's disease, for curing osteoporosis, analgetic agent, anti-ulcerative agent and the like.
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公开(公告)号:US4992534A
公开(公告)日:1991-02-12
申请号:US230557
申请日:1988-08-10
IPC分类号: C07H19/06
CPC分类号: C07H19/06
摘要: Derivatives of 5-deoxy-fluorouridine are disclosed of formula (1) ##STR1## in which one of R and R is a substituted furanylmethyl or thienylmethyl group; and the other R and R is a lower alkanoyl group with one free amino substituent or a salt thereof.
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公开(公告)号:US4425335A
公开(公告)日:1984-01-10
申请号:US291809
申请日:1981-08-10
申请人: Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Mitsuru Hirohashi , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Naoki Umeda , Masahiro Kawasaki
发明人: Setsuro Fujii , Bompei Yasui , Mitsuo Nakamura , Mitsuru Hirohashi , Tomohisa Miyamoto , Kazuko Ando , Iwao Hashimoto , Naoki Umeda , Masahiro Kawasaki
IPC分类号: C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/06 , C07H19/08
CPC分类号: C07H19/06
摘要: New ester derivatives of alkoxybenzoyldeoxyfluorouridine of the general formula ##STR1## wherein R stands for an alkoxy group having 1 to 4 carbon atoms, m for 1 or 2, and n for 3 or 4 with the proviso that when m is 2, the adjacent two R's may be combined to form an alkylenedioxy group as a whole. These derivatives are prepared by acylating a 2'-deoxy-3',5'-di-O-alkylcarbonyl-5-fluorouridine with corresponding benzoyl halides and are useful as active ingredients for anti-tumor agents, especially for oral administration.
摘要翻译: 通式为“IMAGE”的烷氧基苯甲酰基脱氧氟尿酸的新酯衍生物,其中R代表具有1至4个碳原子的烷氧基,m为1或2,n为3或4,条件是当m为2时, R可以组合形成亚烷基二氧基整体。 这些衍生物通过用相应的苯甲酰卤酰化2'-脱氧-3',5'-二-O-烷基羰基-5-氟尿苷来制备,并且可用作抗肿瘤剂的活性成分,特别是用于口服给药。
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公开(公告)号:US5162305A
公开(公告)日:1992-11-10
申请号:US314018
申请日:1989-02-23
IPC分类号: A61K38/23 , A61K38/00 , A61P5/12 , C07K7/06 , C07K14/575 , C07K14/585
CPC分类号: C07K14/585 , A61K38/00
摘要: Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.
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公开(公告)号:US5047521A
公开(公告)日:1991-09-10
申请号:US150407
申请日:1988-02-09
IPC分类号: A61K31/505 , A61K31/70 , C07D239/54 , C07D239/553 , C07D401/12 , C07D409/06 , C07D409/14 , C07H19/06 , C07H19/073 , H01S4/00
CPC分类号: C07D239/553 , C07D401/12 , C07D409/14 , C07H19/06
摘要: This invention relates to a novel 5-fluorouracil derivative represented by the formula ##STR1## wherein R.sup.y is a hydrogen atom or a specific acyl group, Z is a phenyl-lower alkoxy-lower alkyl group, thienyl-lower alkyl group optionally substituted with halogen atom on the thienyl ring, or a group ##STR2## wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a specific acyl group, phenyl-lower alkyl group having a group R.sup.x OCO-- on the phenyl ring, or a group --(A).sub.n B, R.sup.x being a specific organic group, A being a lower alkylene group, n being 0 or 1, and B being a 5- or 6-membered unsaturated heterocyclic group having 1 to 4 hetero-atoms selected from N, O and S and optionally having a benzene ring, naphthalene ring or pyridine ring condensed therewith, with the proviso that R.sup.1 and R.sup.2 are not hydrogen atoms or specific acyl groups at the same time; to a process for preparing the same; and to an anticancer composition comprising the same as an effective ingredient.
摘要翻译: PCT No.PCT / JP87 / 00275 Sec。 371日期1988年2月9日 102(e)1988年2月9日PCT PCT公开1987年4月30日PCT公布。 公开号WO87 / 06582 日本公开日:1987年11月5日。本发明涉及由式(1)表示的新型5-氟尿嘧啶衍生物,其中R y为氢原子或特定酰基,Z为苯基 - 低级烷氧基 - 低级烷基 任选被噻吩基环上的卤素原子取代的噻吩基 - 低级烷基,或其中R 1和R 2各自为氢原子,特定酰基,具有基团R xOCO-的苯基 - 低级烷基基团 环,或基团 - (A)nB,Rx是特定的有机基团,A是低级亚烷基,n是0或1,B是具有1〜4个杂原子的5或6元不饱和杂环基, 选自N,O和S且任选具有苯环的原子,萘环或与其缩合的吡啶环,条件是R1和R2不同时为氢原子或特定酰基; 一个制备它的过程; 以及包含其作为有效成分的抗癌组合物。
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公开(公告)号:US4011221A
公开(公告)日:1977-03-08
申请号:US606478
申请日:1975-08-21
IPC分类号: C07H19/167 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P43/00 , C07H19/04 , C07H19/16 , C07D473/30
摘要: S-Inosylcysteine, possessing a cell-proliferating activity and useful in the treatment of tissue lesions and ulcers, is produced by reacting a 2', 3'-O-protected-inosine derivative with an alkali metal salt of cysteine to produce S-(2', 3'-O-protected-inosyl) cysteine, and then removing the protecting group.
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