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1. 发明授权

US07763652B2 Prostaglandin derivatives 失效
标题翻译：前列腺素衍生物
公开(公告)号：US07763652B2
公开(公告)日：2010-07-27
申请号：US10521115
申请日：2003-07-11
申请人： Fumie Sato , Tohru Tanami , Makoto Yagi , Naoya Ono
发明人： Fumie Sato , Tohru Tanami , Makoto Yagi , Naoya Ono
IPC分类号： A61K31/215 , A61K31/557
CPC分类号： C07C405/0033
摘要： A prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 straight or branched chain alkyl group or a C4-13 cycloalkylalkyl group, R2 is a hydrogen atom or a CO2R3 group (R3 is a hydrogen atom, a C1-4 straight or branched chain alkyl group or a C2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.
摘要翻译：由式（I）表示的前列腺素衍生物：其中X是α-或/或b-取代基中的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，R 1是C 3-10环烷基，被C 1-4直链或支链烷基或C4-13环烷基烷基取代的C3-10环烷基，R2是氢原子或CO2R3基（R3是氢原子，C1-4直链或支链烷基基团或C2-4直链或支链烯基），n为1〜4的整数，p为0,1或2，其药学上可接受的盐或其水合物。

2. 发明申请

US20060111430A1 2,3,4-substituted cyclopentanones as therapeutic agents 有权
标题翻译： 2,3,4-取代环戊酮作为治疗剂
公开(公告)号：US20060111430A1
公开(公告)日：2006-05-25
申请号：US10997039
申请日：2004-11-23
申请人： Yariv Donde , Mark Holoboski , Mari Posner , Robert Burk , Michael Garst
发明人： Yariv Donde , Mark Holoboski , Mari Posner , Robert Burk , Michael Garst
IPC分类号： A61K31/558 , A61K31/557 , C07D333/72 , C07C317/24
CPC分类号： C07D333/62 , C07C323/52 , C07C405/0033 , C07C2601/08 , C07D333/56
摘要： Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, B, J, and E are further described. Methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：本文公开了包含其药学上可接受的盐或其前药的化合物; 其中进一步描述Y，A，B，J和E。还公开了与之相关的方法，组合物和药物。

3. 发明申请

US20060094788A1 Prostaglandin derivatives 失效
标题翻译：前列腺素衍生物
公开(公告)号：US20060094788A1
公开(公告)日：2006-05-04
申请号：US10521115
申请日：2003-07-11
申请人： Fumie Sato , Tohru Tanami , Makoto Yagi , Naoya Ono
发明人： Fumie Sato , Tohru Tanami , Makoto Yagi , Naoya Ono
IPC分类号： A61K31/557 , C07C317/20
CPC分类号： C07C405/0033
摘要： A prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 straight or branched chain alkyl group or a C4-13 cycloalkylalkyl group, R2 is a hydrogen atom or a CO2R3 group (R3 is a hydrogen atom, a C1-4 straight or branched chain alkyl group or a C2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.
摘要翻译：由式（I）表示的前列腺素衍生物：其中X是α-取代或β-取代中的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，R 1是 C 3-10环烷基，被C 1-4直链或支链烷基取代的C 3-10环烷基或 C 4-13环烷基烷基，R 2是氢原子或CO 2 R 3 R 3基团（R 3是氢原子，C 1-4烷基直链或支链烷基或C 2-4直链或支链烯基），n为1〜4的整数，p为0,1或2，其药学上可接受的盐或其水合物。

4. 发明申请

US20050020686A1 Remedies for diseases with bone mass loss having ep4 agonist as the active ingredient 失效
标题翻译：用ep4激动剂作为活性成分治疗骨质量下降的疾病
公开(公告)号：US20050020686A1
公开(公告)日：2005-01-27
申请号：US10484500
申请日：2002-07-22
申请人： Toru Maruyama , Kaoru Kobayashi , Tohru Kambe , Takayuki Maruyama , Hideyuki Yoshida , Akio Nishiura , Nobutaka Abe
发明人： Toru Maruyama , Kaoru Kobayashi , Tohru Kambe , Takayuki Maruyama , Hideyuki Yoshida , Akio Nishiura , Nobutaka Abe
IPC分类号： A61K45/00 , A61K31/559 , A61P19/08 , A61P19/10 , C07C405/00 , A61K31/557
CPC分类号： C07C405/0033 , A61K9/0019 , A61K9/1647 , A61K9/19 , A61K9/2054 , A61K31/4015 , A61K31/41 , A61K31/5575 , A61K31/559
摘要： A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).
摘要翻译：用于预防和/或治疗与包含EP4激动剂作为活性成分的骨量减少相关的疾病的局部施用的药物组合物。包含具有前列腺素骨架的化合物作为代表的EP4激动剂具有促进骨形成的作用，因此可用于预防和/或治疗与骨质量减少有关的疾病（骨疾病如原发性骨质疏松症，继发性骨质疏松症骨质疏松症，癌症的骨转移，高钙血症，佩吉特氏病，骨丢失和骨坏死，术后成骨，骨移植的替代疗法）。

5. 发明授权

US5990346A Prostaglandins and processes for production thereof 失效
标题翻译：前列腺素及其制备方法
公开(公告)号：US5990346A
公开(公告)日：1999-11-23
申请号：US793486
申请日：1997-02-26
申请人： Kenichiro Kataoka , Toru Minoshima , Tatsuki Shiota , Takaharu Tsutsumi , Takahiko Hada , Hiroko Tanaka , Takuya Morita , Noriaki Endo
发明人： Kenichiro Kataoka , Toru Minoshima , Tatsuki Shiota , Takaharu Tsutsumi , Takahiko Hada , Hiroko Tanaka , Takuya Morita , Noriaki Endo
IPC分类号： C07C405/00 , A61K31/557 , C07C69/74
CPC分类号： C07C405/0033 , C07C405/00 , C07C405/0016
摘要： A prostaglandin having formula (I), (II), or (III): ##STR1## a process of production thereof, and inhibitors of cell migration caused by chemokines containing (I) or (II) as an active ingredient.
摘要翻译： PCT No.PCT / JP96 / 01662 Sec。 371日期1997年2月26日 102（e）1997年2月26日PCT PCT 1996年6月17日PCT公布。出版物WO97 / 01534 日本1997年1月16日具有式（I），（II）或（III）的前列腺素：其制备方法和由含有（I）或（II）作为活性成分的趋化因子引起的细胞迁移抑制剂。

6. 发明授权

US5583158A Prostaglandin E.sub.1 analogues 失效
标题翻译：前列腺素E1类似物
公开(公告)号：US5583158A
公开(公告)日：1996-12-10
申请号：US416871
申请日：1995-04-19
申请人： Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人： Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： C07C405/0025 , C07C405/0033
摘要： A prostaglandin E.sub.1 analogue represented by formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; and X is an oxygen atom and R.sup.2 represents ##STR2## or X is a sulfur atom and R.sup.2 represents ##STR3## The compound has a strong and prolonged inhibitory action for platelet aggregation and is useful for treatment of various thrombotic diseases including peripheral circulatory disturbance.
摘要翻译： PCT No.PCT / JP93 / 01510 Sec。 371日期1995年04月19日 102（e）日期1995年4月19日PCT提交1993年10月20日PCT公布。公开号WO94 / 08961 日本1994年4月28日由式表示的前列腺素E1类似物，其中R1表示氢原子或C1-C6烷基; X是氧原子，R2表示或或X是硫原子，R2代表血小板聚集的作用，可用于治疗各种血栓形成疾病，包括外周循环障碍。

7. 发明授权

US5312832A Ocular hypotensive 2-decarboxyl-2-acylthioalkyl prostaglandin derivatives 失效
标题翻译：眼低血压2-脱羧-2-酰硫烷基前列腺素衍生物
公开(公告)号：US5312832A
公开(公告)日：1994-05-17
申请号：US702220
申请日：1991-05-17
申请人： Ming F. Chan
发明人： Ming F. Chan
IPC分类号： A61K31/557 , A61K31/5575 , A61P9/12 , A61P27/02 , C07C405/00
CPC分类号： A61K31/557 , C07C405/0033
摘要： The present invention relates to 2-decarboxyl-2-acylthioalkyl prostaglandins that are potent ocular hypotentives, and are particularly suitable for the management of glaucoma.
摘要翻译：本发明涉及作为有效的眼睛低血糖素的2-癸羧-2-酰硫烷基前列腺素，特别适用于治疗青光眼。

8. 发明授权

US4733011A New intermediates for the preparation of 13-thiaprostaglandin derivatives 失效
标题翻译：制备13-thiaprostaglandin衍生物的新中间体
公开(公告)号：US4733011A
公开(公告)日：1988-03-22
申请号：US767015
申请日：1985-08-19
申请人： Bernhard Riefling , Hans-Eckart Radunz
发明人： Bernhard Riefling , Hans-Eckart Radunz
IPC分类号： C07C323/22 , A61K31/557 , C07C67/00 , C07C313/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07C177/00
CPC分类号： C07D307/935 , C07C323/00 , C07C405/0033 , C07D309/12 , C07C2102/20 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein A is C--C single bond, --CH.sub.2 --, --CH(CH.sub.3)--, --C(CH.sub.3).sub.2 --, --CH.sub.2 --CH.sub.2 --, CH(CH.sub.3)CH.sub.2 --, --C(CH.sub.3).sub.2 CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 O--; R.sup.1a and R.sup.1 each independently is hydrogen or a protective group which can be cleaved by solvolysis or by hydrogenolysis; R.sup.2 is H or alkyl of 1 to 3 C atoms; R.sup.3 is alkyl of 3 to 5 C atoms, phenyl or phenyl which is monosubstituted to trisubstituted by F, Cl, OH, OCH.sub.3, OC.sub.2 H.sub.5, CF.sub.3 or alkyl of 1 to 3 C atoms, or, when A is not --CH.sub.2 O--, can also be pyridyl, thienyl, naphthyl or alkoxy of 1 to 4 C atoms; indicates a bond in the .beta.-position and wavy line ( ) means that the bond can be in the .alpha.- or .beta.-position, are valuable intermediates for the stereospecific preparation of 13-thiaprostaglandin derivatives. The latter are prepared by U.V. irradiation of the former to first prepare the corresponding 2-oxa-3-OH-6-alkylthio-7-OH-1,5-bicyclo(3.3.0)octane derivative, which is then exposed to a Wittig reaction and, optionally, hydrogenation or oxidation inter alia to prepare members of the F.sub.1 -, F.sub.2 -, E.sub.1 - and E.sub.2 series.
摘要翻译：其中A是CC单键，-CH 2 - ， - CH（CH 3） - ， - C（CH 3）2 - ， - CH 2 -CH 2 - ，CH（CH 3）CH 2 - ， - C（CH 3））2CH2-，-CH2-CH2-CH2-或-CH2O-; R1a和R1各自独立地为氢或可通过溶剂解或氢解裂解的保护基; R2是H或1〜3个C原子的烷基; R3是3至5个C原子的烷基，苯基或被F，Cl，OH，OCH 3，OC 2 H 5，CF 3或1至3个C原子的烷基单取代至三取代的苯基，或者当A不是-CH 2 O-时，可以也可以是1至4个C原子的吡啶基，噻吩基，萘基或烷氧基; 表示β位和波浪线（）中的键，表示该键可以是α-或β-位，是13-季前列腺素衍生物的立体特异性制备的有价值的中间体。后者由U.V. 照射前者，首先制备相应的2-氧杂-3-羟基-6-甲硫基-7-OH-1,5-双环（3.3.0）辛烷衍生物，然后将其暴露于维蒂希反应，任选地，氢化或氧化，特别是制备F1-，F2-，E1-和E2系列的成员。

9. 发明授权

US4535180A 11-Deoxy-11-substituted prostaglandins of the E and F series 失效
标题翻译： E和F系列的11-脱氧-11-取代的前列腺素
公开(公告)号：US4535180A
公开(公告)日：1985-08-13
申请号：US288396
申请日：1981-07-30
申请人： Charles V. Grudzinskas , Martin J. Weiss
发明人： Charles V. Grudzinskas , Martin J. Weiss
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0033 , C07C405/0041
摘要： This disclosure describes 11-deoxy-11-substituted members of the E.sub.2, F.sub.2, E.sub.1, F.sub.1, dihydro E.sub.1 and dihydro F.sub.1 prostaglandin series which are useful as hypotensive agents and as anti-ulcer agents.
摘要翻译：本公开描述了可用作降压药和抗溃疡剂的E2，F2，E1，F1，二氢E1和二氢F1前列腺素系列的11-脱氧-11-取代的成员。

10. 发明授权

US4532236A Certain prostacyclins and their blood-pressure-lowering and thrombocyte-aggregation-inhibiting compositions and methods 失效
公开(公告)号：US4532236A
公开(公告)日：1985-07-30
申请号：US531898
申请日：1983-07-27
申请人： Robert Nickolson , Helmut Vorbrueggen , Jorge Casals-Stenzel , Martin Haberey
发明人： Robert Nickolson , Helmut Vorbrueggen , Jorge Casals-Stenzel , Martin Haberey
IPC分类号： A61K31/34 , A61K31/557 , A61P43/00 , C07C51/09 , C07C51/38 , C07C55/32 , C07C57/52 , C07C69/533 , C07C69/593 , C07C69/65 , C07C405/00 , C07D307/935 , C07D307/937 , C07D407/00 , C07D407/12 , C07F7/18 , C07F9/40
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0033 , C07C51/09 , C07C51/38 , C07C55/32 , C07C57/52 , C07D307/937 , C07D407/12 , C07F7/1856 , C07F9/4015
摘要： Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group,W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight-chain or branched alkylene group of 1-5 carbon atoms,E is an oxygen atom or a direct bond,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms, a straight-chain or branched-chain alkenyl group of 2-6 carbon atoms which can be substituted by phenyl, halogen, or C.sub.1 -C.sub.4 -alkyl and, if D and E jointly represent a direct bond, is an alkynyl residue of 2-6 carbon atoms optionally substituted in the 1-position by halogen or C.sub.1 -C.sub.4 -alkyl,R.sub.5 is a hydroxy group which can be esterified with an alkanoic acid residue of 1-4 carbon atoms or which can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, alkoxyalkyl, or trialkylsilyl residue and, if R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases, and a process for the preparation thereof.The compounds exhibit blood-pressure-lowering and thrombocyte-aggregation-inhibiting activity.

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