公开(公告)号：EP1514542B1

公开(公告)日：2012-02-22

申请号：EP03760132.5

申请日：2003-04-03

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： NAKADA, Yasushi ,  NAKAGAWA, Masaya ,  ONO, Satoshi

IPC分类号： A61K31/381 ,  A61K31/122 ,  A61K31/21 ,  A61K31/397 ,  A61K31/445 ,  A61K31/473 ,  A61K31/55 ,  A61K45/00 ,  A61P25/28 ,  A61P43/00

CPC分类号： A61K45/06 ,  A61K31/122 ,  A61K31/21 ,  A61K31/381 ,  A61K31/397 ,  A61K31/445 ,  A61K31/473 ,  A61K31/55 ,  A61K2300/00

摘要： When combined with a compound having an acetylcholine esterase inhibitory effect, an alkyl ether derivative represented by the following general formula [1] or its salt: [1] wherein R , R , R , R , m and n are each as defined in the description; synergistically enhances an anti-hypoxia effect. Thus, this combination is useful as a method of improving brain function. A medicinal composition containing the combination of the compounds as described above is useful in treating and preventing dysmnesia caused by intracerebral acetylcholine nerve hypofunction or selective cell death occurring in cerebrovascular dementia, senile dementia, Alzheimer's disease, after effect of ischemic encephalopathy and cerebral stroke.

公开(公告)号：EP1325744A1

公开(公告)日：2003-07-09

申请号：EP01972688.4

申请日：2001-10-04

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi

IPC分类号： A61K31/381 ,  A61P27/02 ,  A61P27/06

CPC分类号： C07D333/54 ,  A61K31/381 ,  Y02P20/55

摘要： 1,2-Ethanediol derivatives represented by the following general formula [1]:
wherein R 1 is substituted or unsubstituted heterocyclic group; R 2 is a hydrogen atom or a hydroxyl-protecting group; R 3 is a hydrogen atom or a lower alkyl group; nR 4 's and nR 5 's, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; R 6 is substituted or unsubstituted amino or ammonio group; and n is an integer of 1-6; or salts thereof exhibits a retinal neuroprotective action in a glaucoma model and a retinal ischemia-reperfusion rat model, and therefore prevents the cell death of retinal neurons and are useful as agents for preventing and treating retinal neuropathy such as glaucoma, diabetic retinopathy, retinal artery occlusion, retinal vein occlusion, macular retina degeneration, retinopathy of prematurity, etc.

摘要翻译： 由以下通式表示的A1U 1,2-乙二醇衍生物： worin - [R <1>是取代或未unsubstituiertem杂环基团; [R <2>是一个氢原子或羟基保护基; [R <3>是氢原子或低级烷基; NR <4>'S和NR <5>的，其可以是相同或不同的，各自是氢原子或一darstellt低级烷基; [R <6>是取代或未unsubstituiertem氨基或铵基; 和n是1-6的整数; 或其盐表现出青光眼模型中的视网膜神经保护作用和视网膜缺血再灌注大鼠模型中，并因此阻止视网膜神经细胞的细胞死亡，并且作为用于预防和治疗视网膜神经病剂有用：如青光眼，糖尿病性视网膜病，视网膜动脉 阻塞，视网膜静脉阻塞，视网膜黄斑变性，早产儿视网膜病，等。

公开(公告)号：EP1186594A1

公开(公告)日：2002-03-13

申请号：EP00935600.7

申请日：2000-06-09

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi ,  SAITOH, Akihito ,  IWAKAMI, Noboru ,  NAKAGAWA, Masaya ,  YAMAGUCHI, Sumie

IPC分类号： C07C217/10

CPC分类号： C07D235/06 ,  C07C217/10 ,  C07C2602/08 ,  C07D215/14 ,  C07D241/42 ,  C07D277/64 ,  C07D307/79 ,  C07D311/22 ,  C07D317/54 ,  C07D319/18 ,  C07D333/54 ,  C07D333/56 ,  C07D333/62 ,  C07D333/68

摘要： An N-alkoxyalkyl-N,N-dialkylamine derivative represented by the following general formula [1]:
wherein the ring D represents a 5- or 6-membered heterocyclic ring or hydrocarbon ring; R 3 and R 4 , which are the same or different, represent an unsubstituted or substituted alkyl, cycloalkyl or aralkyl group; and R 1 , R 2 , R 5 , R 6 , R 7 , R 8 , m and n are as defined in the specification, or a salt thereof has an anti-hypoxic activity, a nerve-protecting activity and a nerve regeneration promoting activity and is useful for the treatment of neurodegenerative diseases.

公开(公告)号：EP0790246B1

公开(公告)日：2002-01-16

申请号：EP95934859.0

申请日：1995-10-20

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi ,  MAEKAWA, Mutsuko ,  HIRATA, Kazunari ,  NARITA, Hirokazu

IPC分类号： C07D333/52 ,  A61K31/38 ,  A61K31/135 ,  A61K31/34 ,  A61K31/395 ,  A61K31/40 ,  A61K31/495 ,  A61K31/535 ,  C07D333/54

CPC分类号： C07D307/79 ,  C07C217/10 ,  C07D333/54 ,  C07D409/12 ,  C07D453/02 ,  C07D471/08 ,  Y02P20/55

摘要： A 1,2-ethanediol derivative represented by general formula (I) or a salt thereof (wherein R1 represents optionally substituted phenyl, naphthyl, indanyl, indenyl, tetrahydronaphthyl or heterocyclic group; R2 represents hydrogen, alkyl or a hydroxyl-protecting group; R3 represents hydrogen or lower alkyl; nR4s and nR5s represent each independently hydrogen or lower alkyl; R6 represents optionally substituted amino or a nitrogenous heterocyclic group, or ammonio; and n represents an integer of 0 to 6). The compound has an excellent effect of potentiating the nerve growth factor acivity and is useful as a remedy for various diseases caused by central or peripheral nervous system degeneration, such as senile dementia of Alzheimer type, Huntington's chorea, various types of neuropathy and Riley-Day syndrome, traumatic neurosis and amyotrophic lateral sclerosis (ALS).

公开(公告)号：EP0805149A1

公开(公告)日：1997-11-05

申请号：EP95937174.1

申请日：1995-11-24

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi ,  YAMAFUJI, Tetsuo ,  YAMAMOTO, Hirohiko ,  EGAWA, Hiroyuki ,  FURUTA, Yousuke ,  KAGA, Hidetoshi

IPC分类号： C07D241/08 ,  A61K31/495

CPC分类号： C07D401/06 ,  A61K38/00 ,  C07D241/08 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06 ,  C07K5/06139 ,  Y02P20/55

摘要： The present invention relates to a 2,3-diketopiperazine derivative or a salt thereof, which has inhibitory effect on platelet aggregation because of glycoprotein IIb/IIIa receptor antagonism and hence is useful as a prophylactic and therapeutic agent for diseases associated with platelet aggregation. General formula:
wherein R 1 represents a protected or unprotected amidino group; R 2 represents a hydrogen atom or a carboxyl-protecting group; A represents a substituted or unsubstituted lower alkylene group; B represents -O-, -CONH-, -NHCO- or -SO 2 NH-; Y represents a substituted or unsubstituted lower alkylene group; and the broken line represents a single bond or a double bond.

摘要翻译： 本发明涉及由于糖蛋白IIb / IIIa受体拮抗作用而对血小板聚集具有抑制作用的2,3-二酮哌嗪衍生物或其盐，因此可用作血小板聚集相关疾病的预防和治疗剂。 通式：其中R 1表示被保护或未被保护的脒基; R 2表示氢原子或羧基保护基; A表示取代或未取代的低级亚烷基; B表示-O - ， - CONH - ， - NHCO-或-SO 2 NH-; Y表示取代或未取代的低级亚烷基; 虚线表示单键或双键。

公开(公告)号：EP0790246A1

公开(公告)日：1997-08-20

申请号：EP95934859.0

申请日：1995-10-20

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi ,  MAEKAWA, Mutsuko ,  HIRATA, Kazunari ,  NARITA, Hirokazu

IPC分类号： C07D333/52 ,  A61K31/38 ,  A61K31/135 ,  A61K31/34 ,  A61K31/395 ,  A61K31/40 ,  A61K31/495 ,  A61K31/535

CPC分类号： C07D307/79 ,  C07C217/10 ,  C07D333/54 ,  C07D409/12 ,  C07D453/02 ,  C07D471/08 ,  Y02P20/55

摘要： A 1,2-ethanediol derivative represented by the general formula [I] or its salt:
has a NGF activity-potentiating effect and is useful as a remedy for various diseases caused by degeneration of central nervous system or peripheral nervous system such as senile dementia of Alzheimer type, Huntington's chorea, various neuropathies, Riley-Day syndrome, traumatic nerve injury, amyotrophic lateral sclerosis (ALS) and the like.

摘要翻译： 由通式ÄIÜ表示的1,2-乙二醇衍生物或其盐：具有NGF活性增强作用，可用作中枢神经系统或周围神经系统变性引起的各种疾病的补救剂，例如老年人 阿尔茨海默氏型痴呆，亨廷顿氏舞蹈病，各种神经病，莱利日综合征，创伤神经损伤，肌萎缩性侧索硬化（ALS）等。

公开(公告)号：EP1186594B1

公开(公告)日：2009-08-05

申请号：EP00935600.7

申请日：2000-06-09

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： ONO, Satoshi ,  SAITO, Akihito ,  IWAKAMI, Noboru ,  NAKAGAWA, Masaya ,  YAMAGUCHI, Sumie

IPC分类号： C07C217/10 ,  C07D303/36

CPC分类号： C07D235/06 ,  C07C217/10 ,  C07C2602/08 ,  C07D215/14 ,  C07D241/42 ,  C07D277/64 ,  C07D307/79 ,  C07D311/22 ,  C07D317/54 ,  C07D319/18 ,  C07D333/54 ,  C07D333/56 ,  C07D333/62 ,  C07D333/68

摘要： N-Alkoxyalkyl-N,N-dialkylamine derivatives of general formula [1] or salts thereof, which exhibit antihypoxic, nerve protecting and nerve regeneration promoting effects and are useful as remedies for nerve degeneration diseases, wherein R?1 and R2¿ are each hydrogen, halogeno, or the like; R?3 and R4¿ are each optionally substituted alkyl, cycloalkyl, or aralkyl; R?5, R6, R7 and R8¿ are each hydrogen or alkyl; D is a five- or six-membered heterocycle or a hydrocarbon ring; m is 1 to 5; and n is 1 to 6.

摘要翻译： 由下述通式A1U表示的N-烷氧基烷基 - N，N-二烷基胺衍生物： worin环D darstellt的5-或6-元杂环或烃环; [R <3>和R <4>哪些是相同或不同的，在unsubstituiertem或substituiertem烷基，环烷基或芳烷基代表; 和R <1>，R <2>，R <5> - [R <6> - [R <7> - [R <8>，m和n如说明书中所定义，或其盐具有抗缺氧 活性，神经保护活性和神经再生促销婷活性，可用于神经变性疾病的治疗是有用的。

公开(公告)号：EP1514542A1

公开(公告)日：2005-03-16

申请号：EP03760132.5

申请日：2003-04-03

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： NAKADA, Yasushi ,  NAKAGAWA, Masaya ,  ONO, Satoshi

IPC分类号： A61K31/381 ,  A61K31/122 ,  A61K31/21 ,  A61K31/397 ,  A61K31/445 ,  A61K31/473 ,  A61K31/55 ,  A61K45/00 ,  A61P25/28 ,  A61P43/00

CPC分类号： A61K45/06 ,  A61K31/122 ,  A61K31/21 ,  A61K31/381 ,  A61K31/397 ,  A61K31/445 ,  A61K31/473 ,  A61K31/55 ,  A61K2300/00

摘要： An alkyl ether derivative represented by the formula:
wherein R 1 , R 2 , R 3 , R 4 , m and n are as defined in the specification, or salts thereof exhibits synergistically improved anti-hypoxic activity when combined with a compound having an acetylcholine esterase inhibitory activity. Therefore, the combination according to the present invention is useful as a method for improving cerebral function. Further, a pharmaceutical composition containing the compound relating to the combination according to the present invention is useful for treatment and prevention of dysfunction of cerebral acetylcholine neurons in the sequelae of cerebrovascular dementia, senile dementia, Alzheimer's disease and ischemic cerebral lesion and in the cerebral apoplexy or the memory impairment caused by selective neuronal death.

摘要翻译： 由下式表示的烷基醚衍生物：其中R 1，R 2，R 3，R 4，m和n如说明书中所定义，或其盐表现出协同改进的抗 与具有乙酰胆碱酯酶抑制活性的化合物组合时的低氧活性。 因此，本发明的组合作为改善脑功能的方法是有用的。 此外，含有根据本发明的组合的化合物的药物组合物可用于治疗和预防脑血管性痴呆，老年痴呆，老年痴呆症和缺血性脑损伤的后遗症中脑乙酰胆碱神经元的功能障碍和脑中风 或由选择性神经元死亡引起的记忆障碍。