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1. 发明授权

US5539112A 5-aminoflavone derivatives 失效
标题翻译： 5-氨基黄酮衍生物
公开(公告)号：US5539112A
公开(公告)日：1996-07-23
申请号：US464093
申请日：1995-06-05
申请人： Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
发明人： Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
IPC分类号： C07D311/30 , C07D413/12
CPC分类号： C07D311/30
摘要： 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.
摘要翻译：由式（I）表示的5-氨基黄酮衍生物：其中R 1，R 2，R 3和R 4相同或不同，表示氢，取代或未取代的低级烷基，低级烯基，卤素取代或未取代的低级烷酰基或低级烷氧基羰基，X 1，X 2，Y 1和Y 2相同或不同，表示氢，卤素或低级烷基，X 1和X 2中的至少一个表示卤素或低级烷基，X 3表示氢，取代或未取代的低级烷基，低级烯基，低级炔基，卤素，羟基，取代或未取代的低级烷氧基，NR5R6（其中R5和R6相同或不同，代表氢，或取代或未取代的低级烷基，或R5和R6一起形成含有环中的氮原子），低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，羧基，低级烷氧基羰基，低级烷酰基，二唑基，氰基，取代或未取代的氨基甲酰基或低级烷硫基硫代辛基或其药学上可接受的盐。

2. 发明授权

US5952355A Propenone derivatives 失效
标题翻译：丙烯醌衍生物
公开(公告)号：US5952355A
公开(公告)日：1999-09-14
申请号：US757080
申请日：1996-11-26
申请人： Shun-Ichi Ikeda , Uichiro Kimura , Tadashi Ashizawa , Katsushige Gomi , Hiromitsu Saito , Masaji Kasai , Junji Kanazawa , Kimihito Sasaki , Etsuko Nukui , Masami Okabe , Soichiro Sato
发明人： Shun-Ichi Ikeda , Uichiro Kimura , Tadashi Ashizawa , Katsushige Gomi , Hiromitsu Saito , Masaji Kasai , Junji Kanazawa , Kimihito Sasaki , Etsuko Nukui , Masami Okabe , Soichiro Sato
IPC分类号： C07D209/12 , C07D209/30 , C07D401/06 , C07D405/06 , C07F7/08 , C07H15/24 , A61K31/40 , A61K31/44 , C07D209/32 , C07D209/40
CPC分类号： C07D401/06 , C07D209/12 , C07D209/30 , C07D405/06 , C07F7/0812 , C07H15/24
摘要： The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及由下式（I）表示的丙烯酮衍生物：其中R1表示氢，取代或未取代的低级烷基，取代或未取代的芳基或YR5（其中Y表示S或O; R5表示取代或未取代的低级烷基取代或未取代的芳基，取代或未取代的杂芳基，或取代或未取代的环醚残基）; R2和R3独立地表示氢，低级烷基或取代或未取代的芳烷基，或者R2和R3组合形成取代或未取代的亚甲基或亚乙基; R4表示氢，羟基，低级烷基，取代或未取代的芳烷基，低级烷氧基，取代或未取代的芳烷氧基或卤素; X表示取代或未取代的吲哚基; 或其药学上可接受的盐。

3. 发明申请

US20100016250A1 TOLL-LIKE RECEPTOR 9 AGONISTS 审中-公开
公开(公告)号：US20100016250A1
公开(公告)日：2010-01-21
申请号：US12297211
申请日：2007-04-13
申请人： Hiroyuki Nagata , Michio Ichimura , Rieko Nakatsu , Shun-Ichi Ikeda , Ayako Kawabata , Toshio Ota , Masayuki Abe , Michio Takashima , Makoto Suzuki
发明人： Hiroyuki Nagata , Michio Ichimura , Rieko Nakatsu , Shun-Ichi Ikeda , Ayako Kawabata , Toshio Ota , Masayuki Abe , Michio Takashima , Makoto Suzuki
IPC分类号： A61K31/7064 , C12P19/30 , C12P19/32 , C12N1/20 , A61K31/7076 , C07H19/20 , C07H19/10 , A61P31/00 , A61K31/7072 , C07H19/24 , A61K31/708 , A61P37/04 , A61P25/00
CPC分类号： C07H19/20 , C07H19/10 , C12N15/117 , C12N2310/17 , C12N2310/351 , C12P19/30
摘要： The present invention provides TLR9 agonists comprising, as an active ingredient, a compound represented by formula (I): (wherein a represents 0 or 1; n represents an integer of 0 to 2; m represents an integer of 0 to 5; X1 and X2 each independently represent a hydrogen atom or hydroxy; Y represents an oxygen atom or a sulfur atom; -Q1-represents —O— or the like; -Q2- represents —O— or the like; -Z- represents —O— or the like; R1, R3 and R4 each independently represent hydroxy or the like; R2 and R5 each independently represent a hydrogen atom, hydroxy or the like; and A represents 6-aminopurin-9-yl or the like) or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译：本发明提供TLR9激动剂，其包含作为活性成分的由式（I）表示的化合物：（其中a表示0或1; n表示0〜2的整数; m表示0〜5的整数; X1和 X2各自独立地表示氢原子或羟基; Y表示氧原子或硫原子; -Q1表示-O-等; -Q2-表示-O-等; -Z-表示-O-或类似物; R 1，R 3和R 4各自独立地表示羟基等; R 2和R 5各自独立地表示氢原子，羟基等; A表示6-氨基嘌呤-9-基等）或药学上可接受的盐等等。

4. 发明授权

US06608061B2 Bisaryl compound and medicament for cancer treatment comprising the same 失效
标题翻译：二芳基化合物和包含其的用于癌症治疗的药物
公开(公告)号：US06608061B2
公开(公告)日：2003-08-19
申请号：US09424352
申请日：2000-02-14
申请人： Yoshiyuki Yonetani , Takeshi Takahashi , Yuko Kanda , Tamio Mizukami , Tatsuya Tamaoki , Shun-ichi Ikeda , Masanobu Takashima , Naoki Asanuma , Tadashi Inaba , Hiroshi Takeuchi , Hiroshi Kawamoto , Yoshihisa Tsukada , Masato Satomura , Hiroshi Kitaguchi
发明人： Yoshiyuki Yonetani , Takeshi Takahashi , Yuko Kanda , Tamio Mizukami , Tatsuya Tamaoki , Shun-ichi Ikeda , Masanobu Takashima , Naoki Asanuma , Tadashi Inaba , Hiroshi Takeuchi , Hiroshi Kawamoto , Yoshihisa Tsukada , Masato Satomura , Hiroshi Kitaguchi
IPC分类号： A61K3110
CPC分类号： C07D207/08 , C07C323/16 , C07C323/25 , C07C323/40 , C07D211/58 , C07D211/60 , C07D213/32 , C07D215/06 , C07D233/64 , C07D239/42 , C07D239/58 , C07D251/38 , C07D277/56 , C07D309/38 , C07D317/22 , C07D317/28 , C07D319/06 , C07H5/06 , C07H15/18
摘要： A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.
摘要翻译：一种用于治疗癌症的药物，其包含由以下通式（I）表示的化合物或其生理学上可接受的盐：其中R1表示非金属桥连基团; Ar 1和Ar 2独立地表示选自以下的基团：在其环上具有1〜3个任选被一价基团取代的羟基的芳基，所述芳基可以在其上具有1-3个除羟基以外的取代基环; 和在其环上具有任选被一价基团取代的一至三个羟基的杂芳基，并且所述杂芳基可以在其环上具有一至三个除羟基以外的取代基。

5. 发明授权

US5981558A DC107 derivatives 失效
标题翻译： DC107衍生品
公开(公告)号：US5981558A
公开(公告)日：1999-11-09
申请号：US133614
申请日：1998-08-13
申请人： Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
发明人： Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
IPC分类号： C07D513/18 , C07H15/26 , C07D513/08 , A61K31/425
CPC分类号： C07D513/18 , C07H15/26
摘要： DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).
摘要翻译：提供了具有抗微生物活性和抗肿瘤活性的由式（I）表示的DC107衍生物或其药学上可接受的盐，其中R1表示氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR4等; R2表示氢或COR6; R3表示-CH2OCOR7，苯二甲酰亚氨基甲基等; W表示氧或NR8（其中R8表示羟基，低级烷氧基，低级烯氧基，芳烷氧基，取代或未取代的芳基磺酰基氨基或低级烷氧基羰基氨基）。

6. 发明申请

US20060217368A1 Drug for nerve regeneration 审中-公开
标题翻译：药物用于神经再生
公开(公告)号：US20060217368A1
公开(公告)日：2006-09-28
申请号：US10552061
申请日：2004-04-16
申请人： Tsuyoshi Morishita , Kazuhiro Sakurada , Keiko Suzuki , Shun-ichi Ikeda
发明人： Tsuyoshi Morishita , Kazuhiro Sakurada , Keiko Suzuki , Shun-ichi Ikeda
IPC分类号： A61K31/55 , A61K31/404 , A61K33/00 , A61K31/407 , A61K31/405
CPC分类号： A61K31/00 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/553
摘要： An object of the present invention is to provide a nerve regenerating drug, an agent for the promotion of neuropoiesis of a neural stem cell, a neuron obtained by culturing a neural stem cell in the presence of the agent for the promotion of neuropoiesis, and a method of the manufacture of the neuron. In order to achieve the object, the invention provides a nerve regenerating drug comprising a substance that inhibits the activity of glycogen synthase kinase-3, as an active ingredient; an agent for the promotion of neuropoiesis of a neural stem cell comprising the substance as an active ingredient; a neuron obtained by culturing a neural stem cell in the presence of the agent for the promotion of neuropoiesis; and a method of the manufacture of the neuron. The medical drug according to the invention is useful as a therapeutic drug for neurological diseases such as Parkinson's disease, Alzheimer's disease, Down's disease, cerebrovascular disorder, cerebral stroke, spinal cord injury, Huntington's chorea, multiple sclerosis, amyotrophic lateral sclerosis, epilepsy, anxiety disorder, schizophrenia, depression and manic depressive psychosis.
摘要翻译：本发明的目的是提供一种神经再生药物，用于促进神经干细胞神经生成的药剂，通过在用于促进神经生成的药剂的存在下培养神经干细胞获得的神经元，以及神经元的制造方法。为了达到上述目的，本发明提供了包含抑制糖原合成酶激酶-3活性的物质作为活性成分的神经再生药物。用于促进包含该物质作为活性成分的神经干细胞神经生成的药剂; 在用于促进神经生成的药剂存在下培养神经干细胞获得的神经元; 以及神经元的制造方法。根据本发明的药物可用作神经疾病如帕金森病，阿尔茨海默氏病，唐氏病，脑血管病，脑卒中，脊髓损伤，亨廷顿舞蹈病，多发性硬化，肌萎缩性侧索硬化，癫痫，焦虑症的治疗药物失调，精神分裂症，抑郁症和躁狂抑郁症精神病。

7. 发明授权

US06613774B1 Pyrrolo [4,3,2-de] quinoline derivatives 失效
标题翻译：吡咯并[4,3,2-de]喹啉衍生物
公开(公告)号：US06613774B1
公开(公告)日：2003-09-02
申请号：US09720900
申请日：2001-01-02
申请人： Tsutomu Akama , Hiroyuki Nagata , Atsuhiro Hasegawa , Harumi Ue , Isami Takahashi , Yutaka Saitoh , Kenichi Mochida , Shun-ichi Ikeda , Yutaka Kanda
发明人： Tsutomu Akama , Hiroyuki Nagata , Atsuhiro Hasegawa , Harumi Ue , Isami Takahashi , Yutaka Saitoh , Kenichi Mochida , Shun-ichi Ikeda , Yutaka Kanda
IPC分类号： A61K314745
CPC分类号： C07D471/06
摘要： LK6-A derivatives which have immmunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. and which are represented by general formula (I): as defined herein, and pharmaceutically acceptable salts thereof.
摘要翻译： LK6-A衍生物，其具有免疫抑制活性，细胞生长抑制活性，抗肿瘤活性等，并且由通式（I）表示：如本文所定义，及其药学上可接受的盐。

8. 发明授权

US6080771A DC107 derivatives 失效
标题翻译： DC107衍生品
公开(公告)号：US6080771A
公开(公告)日：2000-06-27
申请号：US133363
申请日：1998-08-13
申请人： Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
发明人： Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
IPC分类号： C07D513/08 , C07D513/18 , C07D513/20 , C07H15/26 , C07H17/02 , A61K31/425 , A61K31/70 , C07D519/00
CPC分类号： C07D513/08 , C07H15/26 , C07H17/02
摘要： DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents CO(CR.sup.4A R.sup.4B).sub.n1 (O(CH.sub.2).sub.p1).sub.n2 OR.sup.5 {wherein n1 represents an integer of 1 or 2; R.sup.4A and R.sup.4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R.sup.5 represents hydrogen, lower alkyl, or the like), or ##STR2##
摘要翻译：提供了具有抗微生物活性和抗肿瘤活性的由式（I）表示的DC107衍生物或其药学上可接受的盐，其中R1表示CO（CR4AR4B）n1（O（CH2）p1）n2OR5 {其中n1表示1或2的整数; R4A和R4B相同或不同，各自表示氢或低级烷基; p1和n2各自表示1〜10的整数，和R 5表示氢，低级烷基等）

9. 发明授权

US4649213A Process for producing an .alpha.-aromatic group substituted alkanoic acid derivative 失效
标题翻译： α-芳基取代的链烷酸衍生物的制备方法
公开(公告)号：US4649213A
公开(公告)日：1987-03-10
申请号：US722833
申请日：1985-04-12
申请人： Takayoshi Yamauchi , Kaneaki Hattori , Shun-ichi Ikeda , Kenji Nakao , Kentaro Tamaki
发明人： Takayoshi Yamauchi , Kaneaki Hattori , Shun-ichi Ikeda , Kenji Nakao , Kentaro Tamaki
IPC分类号： C07C51/00 , C07C69/76
CPC分类号： C07C51/00
摘要： Compounds having anti-inflammatory and analgesic activity of the formula ##STR1## are produced from compounds having the formula ##STR2## by rearrangement in the presence of a base or an amide and (1) X S O X.sup.1 or X S O.sub.2 X.sup.1 where X and X.sup.1 are halogen or trifluoromethyl or (2) sulfur dioxide and halogen.
摘要翻译：具有式的具有抗炎和止痛活性的化合物由碱或酰胺存在下通过重排由式（IMAGE）的化合物和（1）XSO X 1或XS O 2 X 1生成，其中X和X 1为卤素或三氟甲基或（2）二氧化硫和卤素。

10. 发明授权

US06869971B1 UCS1025 derivatives 失效
标题翻译： UCS1025衍生品
公开(公告)号：US06869971B1
公开(公告)日：2005-03-22
申请号：US10110964
申请日：2000-10-19
申请人： Tsutomu Akama , Akira Asai , Tsutomu Agatsuma , Shinji Nara , Yoshinori Yamashita , Tamio Mizukami , Shun-ichi Ikeda , Yutaka Saitoh , Yutaka Kanda
发明人： Tsutomu Akama , Akira Asai , Tsutomu Agatsuma , Shinji Nara , Yoshinori Yamashita , Tamio Mizukami , Shun-ichi Ikeda , Yutaka Saitoh , Yutaka Kanda
IPC分类号： A61P31/04 , A61P35/00 , C07D487/04 , C07D487/14 , C07D487/16 , C07D491/14 , C07D491/147 , C07D491/16 , C07D498/08 , A61K31/403 , A61K31/4453 , C07D209/52 , C07D401/06
CPC分类号： C07D487/04 , C07D487/14 , C07D491/14
摘要： UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I): wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or is combined with R3 to represent a bond, etc., or is combined with R4 to represent —O(C═O)—, etc.; R3 represents hydrogen, etc., or is combined with R2 to represent a bond, etc.; R4 represents hydrogen, etc., or is combined with R2 to represent —(C═O)O—, etc.; R5 represents hydrogen or is combined with R6 to represent a bond; R6 represents hydrogen, etc., or is combined with R5 to represent a bond; R7 represents hydrogen or is combined with R8 to represent ═O; R8 represents hydroxy or is combined with R7 to represent ═O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.
摘要翻译：由式（I）表示的具有抗肿瘤活性或抗菌活性的UCS 1025衍生物：其中R 1表示氢，低级烷基等; R 2表示氢，或与R 3结合以表示键等，或与R 4结合以表示-O（C = O） - 等; R 3表示氢等，或与R 2结合以表示键等; R 4表示氢等，或与R 2结合代表 - （C = O）O-等; R 5表示氢或与R 6结合以表示键; R 6表示氢等，或与R 5结合以表示键; R 7表示氢或与R 8结合以代表= O; R 8表示羟基或与R 7结合代表= O; ----表示单键或双键，a表示单键（被结合形成单键的两个碳原子）或氧原子，或其药学上可接受的盐。

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