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41. 发明授权

US4962107A Agent for cerebral protection 失效
标题翻译：脑保护剂
公开(公告)号：US4962107A
公开(公告)日：1990-10-09
申请号：US321692
申请日：1989-03-10
申请人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
发明人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
IPC分类号： A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P25/28 , C07D211/16 , C07D211/22 , C07D211/46 , C07D265/30 , C07D265/32 , C07D279/12 , C07D295/18 , C07D295/185
CPC分类号： C07D265/30 , C07D211/16 , C07D211/22 , C07D279/12 , C07D295/185
摘要： Compounds of the general formula ##STR1## wherein: X is halogen or trifluoromethyl;R.sub.1 is hydrogen, halogen or trifluoromethyl;R.sub.2 is hydrogen methyl or hydroxymethyl;R.sub.3 is hydrogen or lower alkyl; andY is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.

42. 发明授权

US4390536A Piperidine derivatives 失效
公开(公告)号：US4390536A
公开(公告)日：1983-06-28
申请号：US352762
申请日：1982-02-26
申请人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
发明人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： C07D211/58 , C07D417/04 , A61K31/54
CPC分类号： C07D211/58
摘要： New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.

43. 发明授权

US4344945A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US4344945A
公开(公告)日：1982-08-17
申请号：US241727
申请日：1981-03-09
申请人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
发明人： Masayuki Teranishi , Hiroyuki Obase , Haruki Takai , Kazuhiro Kubo , Yutaka Kasuya
IPC分类号： C07D211/58 , C07D413/04 , A61K31/445 , A61K31/535 , C07D498/14
CPC分类号： C07D211/58
摘要： New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.
摘要翻译：制备具有有用药理活性如降血压活性的新的哌啶衍生物。

44. 发明授权

US07524981B2 Phospholipid derivatives and process for the production there 有权
标题翻译：磷脂衍生物及其生产工艺
公开(公告)号：US07524981B2
公开(公告)日：2009-04-28
申请号：US10541309
申请日：2003-12-12
申请人： Kazuhiro Kubo , Chika Itoh , Syunsuke Ohhashi , Tohru Yasukohchi , Yusuke Ohkawa , Hiroshi Kikuchi , Norio Suzuki , Miho Takahashi , Hitoshi Yamauchi
发明人： Kazuhiro Kubo , Chika Itoh , Syunsuke Ohhashi , Tohru Yasukohchi , Yusuke Ohkawa , Hiroshi Kikuchi , Norio Suzuki , Miho Takahashi , Hitoshi Yamauchi
IPC分类号： C07C9/02
CPC分类号： A61K9/127 , A61K8/14 , A61K8/553 , A61K9/0014 , A61K9/1273 , A61K47/24 , A61Q19/00 , C07F9/10 , C08G65/2609 , C08G65/3353 , C08G2650/34
摘要： A phospholipid derivative represented by the following formula (1): wherein [PG]k represents a residue of polyglycerin having a polymerization degree of k, wherein k is 2 to 50, R1CO and R2CO independently represent an acyl group having 8 to 22 carbon atoms, symbol “a” independently represents an integer of 0 to 5, symbol “b” independently represents 0 or 1, M represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium, and k1, k2, and k3 represent numbers satisfying the following conditions: 1≦k1≦(k+2)/2, 0≦k2, and k1+k2+k3=k+2. The phospholipid derivative is highly safe for living bodies and can be suitably utilized in drug delivery systems such as liposome, and the like.
摘要翻译：由下式（1）表示的磷脂衍生物：其中[PG] k表示聚合度为k的聚甘油的残基，其中k为2〜50，R1CO和R2CO独立地表示碳原子数为8〜22的酰基符号“a”独立地表示0〜5的整数，符号“b”独立地表示0或1，M表示氢原子，碱金属原子，铵或有机铵，k1，k2和k3表示满足以下条件的数字：1 <= k1 <=（k + 2）/ 2,0 <= k2，k1 + k2 + k3 = k + 2。磷脂衍生物对于活体是高度安全的，并且可以适用于药物递送系统如脂质体等。

45. 发明申请

US20060110436A1 Phospholipid derivative 有权
标题翻译：磷脂衍生物
公开(公告)号：US20060110436A1
公开(公告)日：2006-05-25
申请号：US10529692
申请日：2003-09-30
申请人： Syunsuke Ohhashi , Kazuhiro Kubo , Chika Itoh , Tohru Yasukohchi , Hiroshi Kikuchi , Norio Suzuki , Miho Kurosawa , Hitoshi Yamauchi
发明人： Syunsuke Ohhashi , Kazuhiro Kubo , Chika Itoh , Tohru Yasukohchi , Hiroshi Kikuchi , Norio Suzuki , Miho Kurosawa , Hitoshi Yamauchi
IPC分类号： A61K31/795 , C08F291/00 , A61K9/127
CPC分类号： C08F8/40 , A61K8/14 , A61K8/8164 , A61K9/127 , A61K9/1271 , A61K9/1278 , A61K31/795 , A61Q19/00 , C08F220/28 , C08F222/06 , C08L53/00 , C08F222/04 , C08L2666/02
摘要： A phospholipid derivative, utilizable for modification of liposomes and the like, which is a copolymer containing, as essential component units, a component unit A represented by the formula (1), a component unit B represented by the formula (2A) and/or the formula (2B), and a component unit C represented by the formula (3) [R1 and R2 represent hydrogen atom or methyl group, provided that R1 and R2 do not simultaneously represent methyl group; R3 represents a divalent hydrocarbon group having 1 to 3 carbon atoms; AO represents an oxyalkylene group having 2 to 4 carbon atoms; m represents an average molar number of the added oxyalkylene groups and is a number in the range represented as 4≦m≦100; R4 represents hydrogen atom, a hydrocarbon group or acyl group having 1 to 20 carbon atoms; R5CO and R6CO represent an acyl group having 8 to 24 carbon atoms; R7 represents a divalent hydrocarbon group having 2 to 4 carbon atoms; and X and Y represent hydrogen atom, an alkali metal atom, ammonium or an organic ammonium] wherein a molar ratio of the component unit A relative to a total of the component unit B and the component unit C is from 7/3 to 3/7, and the component unit C is contained at a ratio of from 1 to 4 moles per 1 mole of the copolymer.
摘要翻译：可用于脂质体改性的磷脂衍生物等，其是以式（1）表示的成分单元A，式（2A）表示的成分单元B和/或式式（2B）和式（3）表示的成分单元C [R 1和R 2]表示氢原子或甲基，条件是R 0 > 1 和R 2不同时表示甲基; R 3表示具有1至3个碳原子的二价烃基; AO表示碳原子数2〜4的氧化烯基， m表示加成的氧化烯基的平均摩尔数，是在4≤M≤100的范围内的数字; R 4表示氢原子，碳原子数为1〜20的烃基或酰基， R 5 CO和R 6 CO表示具有8至24个碳原子的酰基; R 7表示具有2至4个碳原子的二价烃基; 并且X和Y表示氢原子，碱金属原子，铵或有机铵]，其中组分单元A相对于组分单元B和组分单元C的总量的摩尔比为7/3至3 / 7，组分单元C的含量相对于1摩尔共聚物为1〜4摩尔。

46. 发明授权

US5549890A Animal feed containing Bacillus subtilis FERM BP-3418 that decomposes aflatoxin 失效
标题翻译：含有分解黄曲霉毒素的枯草芽孢杆菌FERM BP-3418的动物饲料
公开(公告)号：US5549890A
公开(公告)日：1996-08-27
申请号：US299649
申请日：1994-09-02
申请人： Kazuhiro Kubo
发明人： Kazuhiro Kubo
IPC分类号： A01N63/00 , A23K1/00 , A23K1/18 , C12N1/00 , C12N1/20
CPC分类号： C12R1/10 , A01N63/00 , A23K10/18 , A23K50/30 , C12R1/125 , Y10S426/807 , Y10S435/822 , Y10S435/839
摘要： A bacterium belonging to Bacillus subtilis and having aflatoxin decomposing ability, as well as a fungal growth inhibitor, fermentation promoter and livestock fattening agent, all containing the bacterium as an active or effective ingredient.
摘要翻译：属于枯草芽孢杆菌的具有黄曲霉毒素分解能力的细菌，以及真菌生长抑制剂，发酵促进剂和家畜育肥剂，均含有细菌作为活性成分或有效成分。

47. 发明授权

US5340807A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5340807A
公开(公告)日：1994-08-23
申请号：US989906
申请日：1992-12-11
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , A01N43/46 , C07D273/02 , C07D313/06
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译：公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基）和Z 表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

48. 发明授权

US5302596A Tricyclic compounds as TXA.sub.2 antagonists 失效
标题翻译：三环化合物作为TXA2拮抗剂
公开(公告)号：US5302596A
公开(公告)日：1994-04-12
申请号：US980617
申请日：1992-11-23
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
IPC分类号： A61K31/19 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/505 , A61P7/02 , A61P9/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C57/46 , C07C59/13 , C07C63/49 , C07C65/26 , C07C67/00 , C07C229/50 , C07C233/52 , C07C233/81 , C07C235/14 , C07C235/40 , C07C235/54 , C07C235/62 , C07C235/78 , C07C235/82 , C07C235/84 , C07C237/04 , C07C237/24 , C07C237/38 , C07C241/00 , C07C251/20 , C07C317/44 , C07C323/61 , C07D235/06 , C07D313/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D491/056 , C07D521/00 , A61K31/435 , C07D473/00
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/12 , C07D405/12 , C07D417/12 , C07D471/04 , Y10S514/824 , Y10S514/826
摘要： Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
摘要翻译：由式（I）表示的新型三环化合物具有TXA2生物合成抑制活性和/或TXA2受体拮抗活性，预期对缺血性疾病，脑血管疾病等具有预防和治疗作用。

49. 发明授权

US5242931A Tricyclic compounds as TXA.sub.2 antagonists 失效
标题翻译：三环化合物作为TXA2拮抗剂
公开(公告)号：US5242931A
公开(公告)日：1993-09-07
申请号：US856296
申请日：1992-03-23
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii
IPC分类号： C07D235/06 , C07D313/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D521/00
CPC分类号： C07D235/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/12 , C07D405/12 , C07D417/12 , C07D471/04
摘要： Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
摘要翻译：由式（I）表示的新型三环化合物具有TXA2生物合成抑制作用和/或TXA2受体拮抗活性，预期对缺血性疾病，脑血管疾病等具有预防和治疗作用。

50. 发明授权

US5192768A Pyrazoloquinoline derivatives 失效
标题翻译：吡唑啉醇衍生物
公开(公告)号：US5192768A
公开(公告)日：1993-03-09
申请号：US757988
申请日：1991-09-12
申请人： Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
发明人： Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A pyrazoloquinoline derivative having the formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, or a lower alkoxycarbonyl group; the dotted line means that the pyrazole ring has two conjugated double bonds; and R.sup.4 is bonded to the nitrogen atom at the 1-position or 2-position, or pharmacologically acceptable salts thereof. These compounds exhibit excellent anti-inflammatory activity and hepatic insufficiency treating activity.

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