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1. 发明授权

US5656663A External skin treatment agent composition containing isocarbacyclins as active ingredient 失效
标题翻译：含有异卡巴菌素作为活性成分的外用皮肤治疗剂组合物
公开(公告)号：US5656663A
公开(公告)日：1997-08-12
申请号：US313146
申请日：1994-12-28
申请人： Atsuo Hazato , Nobuaki Hanajima , Yuji Makino , Toshiaki Takeda , Tamotsu Koyama , Takehisa Hata , Sumihisa Kimura , Saburo Murata
发明人： Atsuo Hazato , Nobuaki Hanajima , Yuji Makino , Toshiaki Takeda , Tamotsu Koyama , Takehisa Hata , Sumihisa Kimura , Saburo Murata
IPC分类号： A61K31/557 , A61K31/215
CPC分类号： A61K31/557 , Y10S514/824 , Y10S514/925 , Y10S514/928
摘要： An external skin treatment agent composition containing an active ingredient comprising a prostacyclin, and/or its optical isomer, having the formula (I): ##STR1## (wherein, R.sup.1 is a hydrogen atom, a straight chain or branched alkyl group of C.sub.1 to C.sub.10, or one equivalent of a cation, R.sup.2 is a substitutable C.sub.1 to C.sub.10 straight chain or branched alkyl group or substitutable C.sub.1 to C.sub.10 straight chain or branched alkenyl group or alkinyl group, R.sup.3 is a straight chain alkyl group of C.sub.1 to C.sub.5, and R.sup.4 and R.sup.5 are independently a hydroxyl group or formula: ##STR2## (where, R.sup.6 is a C.sub.1 to C.sub.5 straight chain or branched alkyl group)) and a carrier.
摘要翻译： PCT No.PCT / JP94 / 00163 Sec。 371日期1994年12月28日第 102（e）日期1994年12月28日PCT 1994年2月3日PCT PCT。公开号WO94 / 17805 日期：1994年8月18日含有包含前列环素的活性成分和/或其旋光异构体的具有式（I）的外用皮肤治疗剂组合物：其中R1是氢原子，直链 C1至C10的链或支链烷基或一当量阳离子，R2为可取代C1至C10直链或支链烷基或可取代C1至C10直链或支链烯基或炔基，R3为直链 C1〜C5的烷基，R4和R5分别独立地为羟基或式：其中R6为C1-C5直链或支链烷基）和载体。

2. 发明授权

US5530027A External skin treatment agent composition containing prostacyclins as active ingredient 失效
标题翻译：含有前列环素作为活性成分的外用皮肤治疗剂组合物
公开(公告)号：US5530027A
公开(公告)日：1996-06-25
申请号：US313147
申请日：1994-10-03
申请人： Atsuo Hazato , Nobuaki Hanajima , Yuji Makino , Toshiaki Takeda , Tamotsu Koyama
发明人： Atsuo Hazato , Nobuaki Hanajima , Yuji Makino , Toshiaki Takeda , Tamotsu Koyama
IPC分类号： A61K31/557 , A61K31/215
CPC分类号： A61K31/557
摘要： An external skin treatment agent composition containing an active ingredient comprising of a prostacyclin, and/or its optical isomer, having the formula (I): ##STR1## (wherein, R.sup.1 is a hydrogen atom, a straight chain or branched alkyl group of C.sub.1 to C.sub.10, or one equivalent of cations, R.sup.2 is (CH.sub.2).sub.2 R.sup.21 or a substitutable C.sub.3 to C.sub.10 cycloalkyl group, where R.sup.21 is a substitutable C.sub.1 to C.sub.10 straight chain or branched alkyl group or substitutable C.sub.2 to C.sub.10 straight chain or branched alkenyl group or alkynyl group, and R.sup.3 and R.sup.4 are independently a hydroxyl group or formula ##STR2## (wherein, R.sup.5 is a C.sub.1 to C.sub.5 straight chain or branched alkyl group)) and a carrier.
摘要翻译： PCT No.PCT / JP94 / 00164 Sec。 371日期：1994年10月3日 102（e）日期1994年10月3日PCT 1994年2月3日PCT PCT。 WO94 / 17806 PCT公开号日本美国专利申请日：1994年8月18日。一种外用皮肤治疗剂组合物，其含有包含前列环素的活性成分和/或其旋光异构体，其具有式（I）：其中R1是氢原子，C1〜C10的直链或支链烷基，或1当量阳离子，R2为（CH2）2R21或可取代C3至C10环烷基，其中R21为可取代C1至C10直链或支链烷基或可取代的 C2〜C10直链或支链烯基或炔基，R3和R4分别独立地为羟基或式（IMA）（其中R5为C1至C5直链或支链烷基））和载体。

3. 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.

4. 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.

5. 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。

6. 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。

7. 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。

8. 发明授权

US5116869A 2-substituted-2-cyclopentenones 失效
标题翻译： 2-取代的2-环丙基
公开(公告)号：US5116869A
公开(公告)日：1992-05-26
申请号：US759785
申请日：1991-09-03
申请人： Satoshi Sugiura , Atsuo Hazato , Toru Minoshima , Yoshinori Kato , Yasuko Koshihara , Seizi Kurozumi
发明人： Satoshi Sugiura , Atsuo Hazato , Toru Minoshima , Yoshinori Kato , Yasuko Koshihara , Seizi Kurozumi
IPC分类号： C07C317/24 , C07C323/22 , C07C405/00 , C07D303/32 , C07D303/40
CPC分类号： C07C317/24 , C07C323/22 , C07C405/00 , C07C405/0033 , C07D303/32 , C07D303/40 , C07C2101/10
摘要： 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.

9. 发明授权

US4788319A Novel isocarbacyclins and processes for production thereof 失效
标题翻译：新型异卡波菌素及其制备方法
公开(公告)号：US4788319A
公开(公告)日：1988-11-29
申请号：US44957
申请日：1987-05-01
申请人： Atsuo Hazato , Toshio Tanaka , Noriaki Okamura , Kiyoshi Bannai , Kurozumi, Seizi , Suzuki, Masaaki , Noyori, Ryoji
发明人： Atsuo Hazato , Toshio Tanaka , Noriaki Okamura , Kiyoshi Bannai , Kurozumi, Seizi , Suzuki, Masaaki , Noyori, Ryoji
IPC分类号： C07C405/00 , C07C147/107
CPC分类号： C07C405/0025 , C07C405/0083
摘要： A novel isocarbacyclin which is a compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, or a C.sub.1 -C.sub.4 alkyl or alkenyl group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom, a tri(C.sub.1 -C.sub.7)hydrocarbon-silyl group or a group forming an acetal linkage together with the oxygen atom of the hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group which may be interrupted by an oxygen atom, a substituted linear or branched C.sub.1 -C.sub.5 group in which the substituent is a C.sub.1 -C.sub.6 alkoxy group or a phenyl, phenoxy or C.sub.3 -C.sub.10 cycloalkyl group which may be substituted further, 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; n is 0 or 1; and Ar represents a substituted or unsubstituted phenyl group, its enantiomorph, or a mixture both in an arbitrary ratio.
摘要翻译：一种新颖的异卡巴环素，它是由下式表示的化合物：其中R 1表示氢原子或C 1 -C 4烷基或烯基; R2和R3相同或不同，各自表示氢原子，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; R5表示可被氧原子取代的未取代的直链或支链C 3 -C 8烷基，其中取代基为C 1 -C 6烷氧基的取代的直链或支链C 1 -C 5基或苯基，苯氧基或C 3 -C 10 可以被取代的环烷基，可被取代的苯基，可被取代的苯氧基或可被取代的C3-C10环烷基; n为0或1; Ar表示取代或未取代的苯基，其对映体或任意比例的混合物。

10. 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。

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