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1. 发明授权

US6028208A Vitamin D.sub.3 derivative and treating agent for inflammatory respiratory disease using same 失效
标题翻译：维生素D3衍生物和用于炎性呼吸系统疾病的治疗剂
公开(公告)号：US6028208A
公开(公告)日：2000-02-22
申请号：US242665
申请日：1999-02-22
申请人： Qingzhi Gao , Kenji Manabe , Minoru Furuya , Manabu Chokki , Hiroaki Mitsuhashi , Seiichi Ishizuka , Tadashi Kishimoto , Masayasu Tabe , Yasuji Sakuma , Atsuo Hazato , Hiroko Tanaka
发明人： Qingzhi Gao , Kenji Manabe , Minoru Furuya , Manabu Chokki , Hiroaki Mitsuhashi , Seiichi Ishizuka , Tadashi Kishimoto , Masayasu Tabe , Yasuji Sakuma , Atsuo Hazato , Hiroko Tanaka
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Provided are vitamin D.sub.3 derivatives expressed by the following general formula [1] ##STR1## [wherein, R.sub.1 and R.sub.2 are each a hydrogen atom, a trialkylsilyl group, an acetyl group, a methoxymethyl group, or a tetrahydropyranyl group; R.sub.3 and R.sub.4 are each a hydrogen atom, a hydroxyl group, an acyloxy group, an alkyloxy group, an alkylthio group or an alkyl group which is optionally substituted; R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each a hydrogen atom, a hydroxyl group, an alkyl group or an acyloxy group; R.sub.9 is a hydrogen atom, a hydroxyl group, an alkyl group or an alkylthio group; R.sub.10 is a hydrogen atom, an alkyl group or an alkyloxy group; A and B are each a hydrogen atom, a hydroxyl group, or together express a single bond; X and Y express a carbonyl oxygen, or one of them is a hydrogen atom and the other is a hydroxyl group or an acyloxy group; n is an integer of 0 to 2; m is an integer of 0 to 2], and a method for manufacturing the derivatives.The compounds can be sued as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis and dermatitis.
摘要翻译： PCT No.PCT / JP98 / 02813 Sec。一九九九年二月二十二日 102（e）1999年2月22日PCT提交1998年6月24日PCT公布。公开号WO98 / 58909 日期：1998年12月30日提供由以下通式[1]表示的维生素D3衍生物[其中，R1和R2各自为氢原子，三烷基甲硅烷基，乙酰基，甲氧基甲基或四氢吡喃基; R3和R4各自为氢原子，羟基，酰氧基，烷氧基，烷硫基或任选取代的烷基; R5，R6，R7和R8分别是氢原子，羟基，烷基或酰氧基; R9为氢原子，羟基，烷基或烷硫基; R 10是氢原子，烷基或烷氧基; A和B各自为氢原子，羟基，或一起表示单键; X和Y表示羰基氧，或者其中一个是氢原子，另一个是羟基或酰氧基; n为0〜2的整数， m为0〜2的整数]，以及该衍生物的制造方法。这些化合物可以作为炎性呼吸系统疾病，恶性肿瘤，类风湿性关节炎，骨质疏松症，糖尿病，高血压，脱发，痤疮，牛皮癣和皮炎的治疗剂的活性成分。

2. 发明授权

US5986112A Vitamin D.sup.3 derivative and production process thereof 失效
标题翻译：维生素D3衍生物及其制备方法
公开(公告)号：US5986112A
公开(公告)日：1999-11-16
申请号：US971201
申请日：1997-11-14
申请人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qingzhi Gao , Hiroko Tanaka
发明人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qingzhi Gao , Hiroko Tanaka
IPC分类号： C07C69/675 , C07C69/716 , C07C69/732 , C07C401/00 , C07D307/33 , C07D307/58 , C07D317/34 , C07F7/18 , C07F7/08
CPC分类号： C07D307/33 , C07C401/00 , C07C69/675 , C07C69/716 , C07C69/732 , C07D307/58 , C07D317/34 , C07F7/1856
摘要： A vitamin D.sub.3 derivative represented by the following formula: wherein, R is, independently, a hydrogen atom, tri(C.sub.1 to C.sub.7 hydrocarbon)silyl group, C.sub.2 to C.sub.8 acyl group, or group forming an acetal bond together with an oxygen atom of a hydroxyl group, A is ##STR1## where, R.sup.1 is a methyl group or methylene group, and when R.sup.1 is a methylene group, the bond between the R.sup.1 and the 3-position of the lactone ring is a double bond, R.sup.2 is a hydrogen atom or C.sub.1 to C.sub.3 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together indicate a substitutable single methylene group.
摘要翻译：由下式表示的维生素D3衍生物：其中，R独立地为氢原子，三（C1〜C7烃）甲硅烷基，C2〜C8酰基或与乙缩醛的氧原子一起形成缩醛键的基团羟基，A是其中，R1是甲基或亚甲基，当R1是亚甲基时，内酯环的R1和3-位之间的键是双键，R2是氢原子或C1 至C3烷基，R3为氢原子，或R2和R3一起表示可取代的单个亚甲基。

3. 发明授权

US5719297A Vitamin D.sub.3 derivatives and production process thereof 失效
标题翻译：维生素D3衍生物及其制备方法
公开(公告)号：US5719297A
公开(公告)日：1998-02-17
申请号：US591547
申请日：1996-02-06
申请人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qingzhi Gao , Hiroko Tanaka
发明人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qingzhi Gao , Hiroko Tanaka
IPC分类号： C07C69/675 , C07C69/716 , C07C69/732 , C07C401/00 , C07D307/33 , C07D307/58 , C07D317/34 , C07F7/18 , C07D307/26
CPC分类号： C07D307/33 , C07C401/00 , C07C69/675 , C07C69/716 , C07C69/732 , C07D307/58 , C07D317/34 , C07F7/1856
摘要： A vitamin D.sub.3 derivative represented by the following formula: ##STR1## wherein, R is, independently, a hydrogen atom, tri(C.sub.1 to C.sub.7 hydrocarbon)silyl group, C.sub.2 to C.sub.8 acyl group, or group forming an acetal bond together with an oxygen atom of a hydroxyl group, A is ##STR2## where, R.sup.1 is a methyl group or methylene group, and when R.sup.1 is a methylene group, the bond between the R.sup.1 and the 3-position of the lactone ring is a double bond, R.sup.2 is a hydrogen atom or C.sub.1 to C.sub.3 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together indicate a substitutable single methylene group.
摘要翻译： PCT No.PCT / JP95 / 01145 Sec。 371日期1996年2月6日 102（e）日期1996年2月6日PCT提交1995年6月7日PCT公布。公开号WO95 / 33716 PCT 日期：1995年12月14日由下式表示的维生素D3衍生物：其中，R独立地为氢原子，三（C1〜C7烃）甲硅烷基，C2〜C8酰基或基团与羟基的氧原子一起形成缩醛键，其中R1是甲基或亚甲基，当R1是亚甲基时，R1和3- 内酯环的位置是双键，R2是氢原子或C1-C3烷基，R3是氢原子，或R2和R3一起表示可取代的单个亚甲基。

4. 发明授权

US06177586B1 Vitamin D3 derivative and production process thereof 有权
标题翻译：维生素D3衍生物及其制备方法
公开(公告)号：US06177586B1
公开(公告)日：2001-01-23
申请号：US09327489
申请日：1999-06-08
申请人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qinqzhi Gao , Hiroko Tanaka
发明人： Masayasu Tabe , Atsuo Hazato , Kenji Manabe , Qinqzhi Gao , Hiroko Tanaka
IPC分类号： C07F708
CPC分类号： C07D307/33 , C07C69/675 , C07C69/716 , C07C69/732 , C07C401/00 , C07D307/58 , C07D317/34 , C07F7/1804
摘要： The starting materials for a production process of a vitamin D3 derivative are disclosed, e.g., a cyclopentene derivative represented by the formula (1-2): wherein R11 is a hydrogen atom, tri(C1 to C7 hydrocarbon) silyl group, C2 to C7 acyl group, group forming an acetal bond together with an oxygen atom of a hydroxyl group, and X1 is a bromine or iodine atom; and a heptanoic acid derivative represented by the formula (2-4): wherein X2 is a bromine atom or iodine atom.
摘要翻译：公开了维生素D3衍生物的制造方法的原料，例如式（1-2）表示的环戊烯衍生物：其中，R 11为氢原子，三（C1〜C7烃）甲硅烷基，C2〜C7 酰基，与羟基的氧原子一起形成缩醛键，X1是溴或碘原子; 和由式（2-4）表示的庚酸衍生物：其中X 2是溴原子或碘原子。

5. 发明授权

US5604257A Lactone compound and process of production thereof 失效
标题翻译：内酯化合物及其生产方法
公开(公告)号：US5604257A
公开(公告)日：1997-02-18
申请号：US191593
申请日：1994-02-04
申请人： Masayasu Tabe , Kenji Manabe , Koji Tomimori , Atsuo Hazato , Osami Takenouchi , Yoshiaki Azuma
发明人： Masayasu Tabe , Kenji Manabe , Koji Tomimori , Atsuo Hazato , Osami Takenouchi , Yoshiaki Azuma
IPC分类号： A61K31/585 , A61K31/59 , A61P3/02 , A61P3/06 , A61P3/14 , A61P43/00 , C07C401/00 , C07D307/32 , C07D307/33 , C07D309/30 , C07J17/00 , C07J19/00 , A61K31/35 , A61K31/34
CPC分类号： C07C401/00 , C07J17/00
摘要： A lactone compound, useful as an osteogenetic accelerator, having the formula (I): ##STR1## wherein n is zero or 1 and m is zero or 1, provided that both n and m are not zero at the same time, or a stereoisomer thereof at the 23- and/or 25-positions or any mixture thereof and a production process thereof.
摘要翻译：可用作成骨促进剂的内酯化合物，其具有式（I）：其中n为0或1，m为0或1，条件是n和m两者同时不为零，或其立体异构体在其23-和/或25-位或其任何混合物及其制备方法。

6. 发明授权

US5149711A 2-cyclopentenone derivatives 失效
标题翻译： 2-环丙烯酮衍生物
公开(公告)号：US5149711A
公开(公告)日：1992-09-22
申请号：US319688
申请日：1989-03-07
申请人： Atsuo Hazato , Seizi Kurozumi
发明人： Atsuo Hazato , Seizi Kurozumi
IPC分类号： A61K31/22 , A61K31/12 , A61K31/557 , A61K31/695 , A61P35/00 , C07C45/00 , C07C45/67 , C07C49/743 , C07C49/747 , C07C49/753 , C07C67/00 , C07C69/21 , C07C405/00 , C07F7/18
CPC分类号： C07F7/1856 , C07C405/0025 , C07C45/673 , C07C49/743 , C07C49/747 , C07C49/753
摘要： A 2-cyclopentenone derivative represented by the following formula ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 10 carbon atoms which may be substituted by a substituted or unsubstituted phenyl or phenoxy group, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and each represents a hydrogen atom or a lower alkanoyl group, and the wavy line shows that the bonded state of the double bond is E or Z.This compound is useful for treating, for instance, malignant tumors.

7. 发明授权

US4990650A Aromatic derivative and preparation method thereof 失效
标题翻译：芳香族衍生物及其制备方法
公开(公告)号：US4990650A
公开(公告)日：1991-02-05
申请号：US529769
申请日：1990-05-29
申请人： Atsuo Hazato , Seizi Kurozumi
发明人： Atsuo Hazato , Seizi Kurozumi
IPC分类号： C07C33/38 , C07C69/616 , C07C69/618 , C07C233/12 , C07D333/16 , C07D333/24
CPC分类号： C07D333/24 , C07C321/00 , C07C323/00 , C07C33/38
摘要： 1. An aromatic derivative having the formula (I) or the salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, hydroxyl, a halogen atom, or OR.sup.3 wherein R.sup.3 is C.sub.1 -C.sub.10 alkyl; A-B represents a hydrocarbon moiety having 1 to 10 carbon atoms and containing at least one double bond or a sulfur- or oxygen-containing hydrocarbon moiety having 1 to 10 carbon atoms; n is an integer of 2 to 4; X represents a group ##STR2## and Y represents a hydrogen atom; alkyl having 1 to 5 carbon atoms which may be substituted with aryl; alkenyl having 2 to 5 carbon atoms which may be substituted with aryl or aryl substituted with at least one C.sub.1 -C.sub.5 alkoxy; aryl which may be substituted with at least one carboxy or C.sub.1 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 alkoxy; provided that, when R.sup.1 and R.sup.2 are both hydrogen, the moiety --A--B--(CH.sub.2).sub.n --X--Y does not represent ##STR3## wherein n=2 to 4 and R.sup.4 is hydrogen or C.sub.1 -C.sub.5 alkyl.

8. 发明授权

US4797506A 6-substituted prostaglandins E.sub.1 and process for producing same 失效
标题翻译： 6-取代的前列腺素E1及其制备方法
公开(公告)号：US4797506A
公开(公告)日：1989-01-10
申请号：US794857
申请日：1985-10-18
申请人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi
发明人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi
IPC分类号： C07F7/18 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07F1/02 , C07F1/08
CPC分类号： C07C405/0041 , C07C405/00 , C07F1/02 , C07F1/08
摘要： 6-substituted prostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures whereof in any ratio: ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenyl C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.3 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted, or a linear or branched C.sub.1 -C.sub.5 alkyl group which may be substituted with a C.sub.1 -C.sub.6 alkoxy group, a phenyl group which may be substituted, a phenoxy group which may be substituted, or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; and X represents an ##STR2## group or an oxygen atom. Such 6-substituted prostaglandins E.sub.1 are useful for the treatment and/or prevention of digestive organ diseases such as duodenal ulcers or gastric ulcers.
摘要翻译： PCT No.PCT / JP85 / 00096 Sec。 371日期：1985年10月18日 102（e）1985年10月18日日期PCT提交1985年2月28日PCT公布。第WO85 / 03935号公报日期：1985年9月12日.6-取代的前列腺素E1，其为下式[I]表示的化合物或其对映异构体或其任何比例的混合物：其中R1表示氢原子，C1-C16烷基取代或未取代的苯基，取代或未取代的苯基C3-C10环烷基，取代或未取代的苯基（C1-C2）烷基或一个当量的阳离子; R2和R3可以相同或不同，表示氢原子，三（C1-C7）烃甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子，甲基或乙烯基; R 5表示直链或支链C 3 -C 8烷基，直链或支链C 3 -C 8烯基，直链或支链C 3 -C 8炔基，可被取代的苯基，可被取代的苯氧基，C3 可被取代的C 10环烷基，或可以被C 1 -C 6烷氧基取代的直链或支链C 1 -C 5烷基，可被取代的苯基，可被取代的苯氧基或C3 可被取代的-C 10环烷基; X表示基团或氧原子。这种6-取代的前列腺素E1可用于治疗和/或预防消化器官疾病如十二指肠溃疡或胃溃疡。

9. 发明授权

US6087395A Isocarbacyclin derivatives as apoptosis inhibitors 失效
标题翻译：异卡环素衍生物作为凋亡抑制剂
公开(公告)号：US6087395A
公开(公告)日：2000-07-11
申请号：US173758
申请日：1998-10-16
申请人： Yasuyoshi Watanabe , Atsuo Hazato , Masaaki Suzuki , Yumiko Watanabe , Takumi Sato
发明人： Yasuyoshi Watanabe , Atsuo Hazato , Masaaki Suzuki , Yumiko Watanabe , Takumi Sato
IPC分类号： C07C59/54 , C07C69/732 , A01N37/08 , A01N43/00 , C07C62/06
CPC分类号： C07C69/732 , C07C59/54
摘要： The present invention provides an apoptosis inhibitor containing a 15R-isocarbacyclin derivative or a 15-deoxy-isocarbacyclin derivative, which can be manufactured easily and economically by means of chemical synthesis.
摘要翻译：本发明提供含有15R-异卡波环素衍生物或15-脱氧 - 异卡波环素衍生物的细胞凋亡抑制剂，其可通过化学合成而容易且经济地制备。

10. 发明授权

US5159102A 7-thiaprostaglandins E, and process for producing same 失效
标题翻译： 7-硫代前列腺素E及其制备方法
公开(公告)号：US5159102A
公开(公告)日：1992-10-27
申请号：US526682
申请日：1990-05-22
申请人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
发明人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
IPC分类号： C07C405/00
CPC分类号： C07C405/0033
摘要： 7-thiaprostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures thereof in any ratio: ##STR1## where R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a C.sub.2 -C.sub.20 alkenyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.2 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted, or a linear or branched C.sub.1 -C.sub.5 alkyl group which may be substituted with a C.sub.1 -C.sub.6 alkoxy group, a phenyl group which may be substituted, a phenoxy group which may be substituted or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; X represents an ethylene group, a vinylene group or an ethylene group; n represents 0 or 1; the expression represents an ethylene group or a vinylene group, provided that when n is o and x is an ethylene group, R.sup.5 is not a linear or branched C.sub.3 -C.sub.8 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted.Such compounds are especially useful for the treatment and prevention of digestive organ diseases such as a duodenal ulcer or a gastric ulcer.
摘要翻译：作为由下式[I]表示的化合物或其对映异构体或其混合物的7-硫代前列腺素E1为任意比例：其中R 1表示氢原子，C 1 -C 10烷基，C 2 -C 20链烯基取代或未取代的苯基，取代或未取代的C3-C10环烷基，取代或未取代的苯基（C1-C2）烷基或一个当量的阳离子; R2和R3可以相同或不同，表示氢原子，三（C1-C7）烃甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子，甲基或乙烯基; R 5表示直链或支链C 3 -C 8烷基，直链或支链C 3 -C 8烯基，直链或支链C 2 -C 8炔基，可被取代的苯基，可被取代的苯氧基，C3 可以被取代的C 10环烷基，或可以被C 1 -C 6烷氧基取代的直链或支链C 1 -C 5烷基，可被取代的苯基，可被取代的苯氧基或C 3 -C 6烷氧基，可被取代的C 10环烷基; X表示亚乙基，亚乙烯基或亚乙基; n表示0或1; 该表达式表示亚乙基或亚乙烯基，条件是当n是o且x是亚乙基时，R 5不是直链或支链C 3 -C 8烷基或可被取代的C 3 -C 10环烷基。这些化合物特别可用于治疗和预防消化器官疾病如十二指肠溃疡或胃溃疡。

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