公开(公告)号：US5047540A

公开(公告)日：1991-09-10

申请号：US284590

申请日：1988-11-29

申请人： Susumu Kamata ,  Tatsuo Tsuri ,  Nobuhiro Haga ,  Takeaki Matsui ,  Morio Kishi ,  Kimio Takahashi ,  Sanji Hagashita ,  Kaoru Seno

发明人： Susumu Kamata ,  Tatsuo Tsuri ,  Nobuhiro Haga ,  Takeaki Matsui ,  Morio Kishi ,  Kimio Takahashi ,  Sanji Hagashita ,  Kaoru Seno

IPC分类号： C07C311/32 ,  C07C311/46 ,  C07C323/49 ,  C07C391/00 ,  C07D213/20 ,  C07D215/10 ,  C07D217/10 ,  C07D241/12 ,  C07D249/14 ,  C07D261/12 ,  C07D277/22 ,  C07D277/62 ,  C07D295/088 ,  C07D413/12 ,  C07D521/00

CPC分类号： C07D213/20 ,  C07C311/32 ,  C07C311/46 ,  C07C323/49 ,  C07C391/00 ,  C07D215/10 ,  C07D217/10 ,  C07D231/12 ,  C07D233/56 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D277/22 ,  C07D277/62 ,  C07D295/088 ,  C07D413/12

摘要： Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or he0 terocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.

公开(公告)号：US5138067A

公开(公告)日：1992-08-11

申请号：US707164

申请日：1991-05-29

申请人： Susumu Kamata ,  Tatsuo Tsuri ,  Nobuhiro Haga ,  Takeaki Matsui ,  Morio Kishi ,  Kimio Takahashi ,  Sanji Hagishita ,  Kaoru Seno

发明人： Susumu Kamata ,  Tatsuo Tsuri ,  Nobuhiro Haga ,  Takeaki Matsui ,  Morio Kishi ,  Kimio Takahashi ,  Sanji Hagishita ,  Kaoru Seno

IPC分类号： C07C311/32 ,  C07C311/46 ,  C07C323/49 ,  C07C391/00 ,  C07D213/20 ,  C07D215/10 ,  C07D217/10 ,  C07D241/12 ,  C07D261/12 ,  C07D277/22 ,  C07D277/62 ,  C07D295/088 ,  C07D413/12 ,  C07D521/00

CPC分类号： C07D213/20 ,  C07C311/32 ,  C07C311/46 ,  C07C323/49 ,  C07C391/00 ,  C07D215/10 ,  C07D217/10 ,  C07D231/12 ,  C07D233/56 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D277/22 ,  C07D277/62 ,  C07D295/088 ,  C07D413/10

摘要： Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or heterocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together with R.sub.2 form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.

摘要翻译： 由下式表示的脂质衍生物：其中R1是烷基或烷基氨基甲酰基; 低级烷氧基羰基氨基，低级烷基脲基，低级烷氧基甲基，低级烷基羰基甲基，氰基甲基，杂环基或杂环氧基; R2'是氢或R2和R2'与R2一起形成-O（CH 2）m - ，其中m是1至5的整数; R 3，R 4和R 5各自为氢或低级烷基或R 3，R 4和R 5中的两个或三个与相邻的氮原子一起形成环状铵; R6是氢或低级烷基羰基; X-是抗衡阴离子; Y是氧或硫; n为1〜10的整数，可用作PAF拮抗剂，例如作为抗血栓形成，抗收缩性抗静电收缩剂或抗肿瘤剂。

公开(公告)号：US5585501A

公开(公告)日：1996-12-17

申请号：US453773

申请日：1995-05-30

申请人： Mitsuaki Ohtani ,  Takaharu Matsuura ,  Yoshinori Hamada ,  Isamu Yamada ,  Teruo Sakata ,  Kimio Takahashi ,  Morio Kishi

发明人： Mitsuaki Ohtani ,  Takaharu Matsuura ,  Yoshinori Hamada ,  Isamu Yamada ,  Teruo Sakata ,  Kimio Takahashi ,  Morio Kishi

IPC分类号： C07D307/935 ,  C07D307/83

CPC分类号： C07D307/935

摘要： A method for reduction of an allyl alcohol-type compound, specific to its allylic hydroxyl group, being carried out without any side reactions such as reduction of other portions of the compound or allylic rearrangement, which comprises treating the compound with trialkylsilane in the presence of AlX.sub.3, wherein X refers to a halogen atom.

摘要翻译： 一种还原其烯丙基羟基特异性烯丙醇型化合物的方法进行而无任何副反应，例如化合物其它部分的还原或烯丙基重排，其包括在三烷基硅烷存在下处理该化合物 AlX3，其中X表示卤素原子。

公开(公告)号：US5292754A

公开(公告)日：1994-03-08

申请号：US948179

申请日：1992-09-21

申请人： Morio Kishi ,  Kimio Takahashi ,  Kenji Kawada ,  Yasumasa Goh

发明人： Morio Kishi ,  Kimio Takahashi ,  Kenji Kawada ,  Yasumasa Goh

IPC分类号： C07C405/00 ,  A61K31/557

CPC分类号： C07C405/00 ,  Y10S206/828 ,  Y10S514/913

摘要： The present invention relates to a method for treating hypertension or glaucoma in the eye comprising contacting the surface of the eye with a therapeutic amount of a 15-deoxyprostaglandin derivative of the formula (I): ##STR1## in which ##STR2## is a 5 membered ring which is selected from a group consisting of ##STR3## R.sup.1 is hydrogen or lower alkyl; R.sup.2 is C.sub.6 -C.sub.12 alkyl, C.sub.6 -C.sub.12 alkenyl or C.sub.6 -C.sub.12 alkadienyl or a pharmaceutically acceptable salt thereof. The invention also relates to a kit for delivery of a topical solution for treatment of glaucoma which comprises (a) container having a solution including a compound of the formula (I), and (b) means for topical delivery of said solution to the eye in a controlled dosage.

摘要翻译： 本发明涉及一种用于治疗眼睛中的高血压或青光眼的方法，包括使眼表面与治疗量的式（I）的15-脱氧前列腺素衍生物接触：（*化学结构*）（I），其中 （*化学结构*）是选自（*化学结构*）R 1为氢或低级烷基的5元环; R2是C6-C12烷基，C6-C12链烯基或C6-C12链二烯基或其药学上可接受的盐。 本发明还涉及一种用于递送用于治疗青光眼的局部用溶液的试剂盒，其包含（a）具有包含式（I）化合物的溶液的容器，和（b）将所述溶液局部递送至眼睛的装置 以受控剂量。

公开(公告)号：US5599837A

公开(公告)日：1997-02-04

申请号：US395642

申请日：1995-02-28

申请人： Morio Kishi ,  Kimio Takahashi ,  Kenji Kawada ,  Yasumasa Goh

发明人： Morio Kishi ,  Kimio Takahashi ,  Kenji Kawada ,  Yasumasa Goh

IPC分类号： A61K31/557 ,  A61P27/06 ,  C07C405/00

CPC分类号： C07C405/00

摘要： The present invention relates to a 15-deoxyprostaglandin derivative of the formula (I): ##STR1## in which ##STR2## is a 5 membered ring which is selected from a group consisting of ##STR3## R.sup.1 is hydrogen or lower alkyl; R.sup.2 is C.sub.6 -C.sub.12 alkyl, C.sub.6 -C.sub.12 alkenyl or C.sub.6 -C.sub.12 alkadienyl;provided that the compound of the following formula is excluded: ##STR4## wherein R' is hydrogen or methyl; or pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical formulation comprising a 15-deoxyprostaglandin derivative as an active ingredient, which is useful as an intraocular pressure reducing agent.

摘要翻译： 本发明涉及式（I）的15-脱氧前列腺素衍生物：其中是一种5元环，其选自由下列组成的组：R1是氢 或低级烷基; R2是C6-C12烷基，C6-C12链烯基或C6-C12链二烯基; 条件是排除下列化学式的化合物：其中R'是氢或甲基; 或其药学上可接受的盐。 本发明还涉及含有作为活性成分的15-脱氧前列腺素衍生物的药物制剂，其可用作眼内压降低剂。