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1. 发明授权

US5025033A Alkylene diamines 失效
标题翻译：亚烷基二胺
公开(公告)号：US5025033A
公开(公告)日：1991-06-18
申请号：US301065
申请日：1989-01-25
申请人： Giichi Goto , Akinobu Nagaoka
发明人： Giichi Goto , Akinobu Nagaoka
IPC分类号： A61K31/16 , A61K31/165 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/47 , A61P25/02 , A61P25/28 , A61P43/00 , C07C231/02 , C07C231/12 , C07C233/40 , C07C233/78 , C07C233/91 , C07C233/92 , C07C235/34 , C07C237/00 , C07C237/20 , C07C237/22 , C07C237/28 , C07C237/34 , C07C237/42 , C07C255/57 , C07C255/58 , C07C311/08 , C07C311/13 , C07C311/21 , C07C317/44 , C07C323/60 , C07C323/62 , C07D209/48 , C07D217/12 , C07D401/06
CPC分类号： C07D209/48 , C07C233/40 , C07C235/34 , C07C237/20 , C07C237/22 , C07C255/57 , C07C317/44 , C07D401/06
摘要： A cholinesterase inhibiting agent which contains an alkylene diamine of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is a hydrogen atom or a hydrocarbon residue which may optionally be substituted, or R.sup.1 and R.sup.2 combinedly form, together with the adjacent nitrogen atom, a condensed heterocyclic group, R.sup.3 is a hydrogen atom or a hydrocarbon residue or an acyl group which may optionally be substituted and R.sup.4 is a hydrogen atom, or R.sup.3 and R.sup.4 combinedly form a group of the formula ##STR2## or --(CH.sub.2).sub.m+1 -- (m being 0, 1 or 2), A is --(CH.sub.2).sub.l -- (l being 0, 1 or 2) or --CH.dbd.CH--, X is a substituent or substituents and n is an integer of 4 to 7, or a salt thereof, which are useful as cerebral function improving agents for the prevention or treatment of senile dementia, Alzheimer's disease, Huntington's chorea, hyperkinesia, mania and so forth.

2. 发明授权

US5021439A Cerebral function ameliorating agents related to Tan-950 A 失效
标题翻译：与Tan-950 A相关的脑功能改善剂A
公开(公告)号：US5021439A
公开(公告)日：1991-06-04
申请号：US408389
申请日：1989-09-18
申请人： Setsuo Harada , Akinobu Nagaoka , Katsumi Itoh , Shinji Terao
发明人： Setsuo Harada , Akinobu Nagaoka , Katsumi Itoh , Shinji Terao
IPC分类号： A61K38/00 , C07D207/26 , C07D207/277 , C07D261/12 , C07D405/06 , C07D413/06 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/078
CPC分类号： C07D207/277 , C07D261/12 , C07D405/06 , C07D413/06 , C07K5/0215 , C07K5/06026 , C07K5/06078 , C07K5/06086 , C07K5/06139 , A61K38/00 , Y02P20/55
摘要： A compound having the formula (I) or (II) ##STR1## wherein R.sup.1 is a hydrogen atom or an organic residue bonded via a carbon atom, R.sup.2 is a hydrogen atom or a N-protecting group, --COR.sup.3 is an optionally esterified or amidated carboxyl group, R.sup.4 and R.sup.5 are the same or different and respectively a hydrogen atom or an acyl group or a chain or alicyclic hydrocarbon group optionally having an aryl substituent, R.sup.6 is NOH or O, n is an integer of 0 to 3, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom may form a ring or an optionally substituted benzylidene amino group, which is useful therapeutics of brain dysfunction.

3. 发明授权

US4748154A Peptide derivatives, their production and use 失效
标题翻译：肽衍生物，其生产和使用
公开(公告)号：US4748154A
公开(公告)日：1988-05-31
申请号：US939103
申请日：1986-12-08
申请人： Giichi Goto , Akinobu Nagaoka , Mitsuhiro Wakimasu
发明人： Giichi Goto , Akinobu Nagaoka , Mitsuhiro Wakimasu
IPC分类号： C07K14/575 , A61K38/00 , A61K38/11 , A61P25/00 , C07K1/02 , C07K1/113 , C07K7/06 , C07K7/16 , A61K37/02
CPC分类号： C07K7/16 , A61K38/00 , Y02P20/55 , Y10S930/26
摘要： A peptide derivative of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-18 alkyl group or a substituted or unsubstituted phenyl C.sub.1-3 alkyl group;A is an amino or N--C.sub.1-6 alkylamino acid residue;B is a hydroxyl group, a substituted or unsubstituted amino group, or an amino acid or an amide thereof,or a physiologically acceptable salt thereof, can be advantageously used for the treatment and/or prevention of a disease including, among others, senile dementia (Alzheimer's dementia), cerebrovascular dementia, Alzheimer's disease, Pick's disease, Huntington's chorea, Creutzfeldt-Jakob disease, Parkinson's disease, and dementia due to spinocerebellar degeneration.
摘要翻译：通式为“IMAGE”的肽衍生物，其中R 1为氢原子，C 1-18烷基或取代或未取代的苯基C 1-3烷基; A是氨基或N-C 1-6烷基氨基酸残基; B是羟基，取代或未取代的氨基或氨基酸或其酰胺或其生理学上可接受的盐可有利地用于治疗和/或预防疾病，包括老年性痴呆（阿尔茨海默氏痴呆症），脑血管性痴呆，阿尔茨海默病，皮克病，亨廷顿舞蹈病，克雅氏病，帕金森氏病和由脊髓小脑变性引起的痴呆。

4. 发明授权

US5180746A Aralkylamine compounds 失效
标题翻译： ARALKYLAMINE化合物
公开(公告)号：US5180746A
公开(公告)日：1993-01-19
申请号：US480564
申请日：1990-02-15
申请人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
发明人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
IPC分类号： C12N9/99 , A61K31/00 , A61K31/33 , A61K31/357 , A61K31/36 , A61K31/40 , A61P25/00 , A61P25/28 , C07C211/30 , C07C217/58 , C07C217/74 , C07C225/12 , C07C225/18 , C07D295/112 , C07D295/12 , C07D317/70 , C07D521/00
CPC分类号： C07D295/112 , C07C217/74 , C07C225/18 , C07D317/70 , C07C2102/08
摘要： An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.
摘要翻译：式IMA的芳烷基胺化合物，其中R 1表示氢原子或低级烷基; R2表示可以被取代的芳基; R3表示氢原子，低级烷基或可被取代的芳基; n表示0〜7的整数，环A表示可以被取代的五元至八元环基，并且可以含有一个或两个O原子和S原子作为环组成的杂原子; 环B表示作为胆碱酯酶抑制剂和脑功能改善剂有用的可被取代的苯环或其盐。

5. 发明授权

US4892875A Substituted heterocyclylalkyl esters of 1,4-dihydropyridine-3,5-dicarboxylic acids 失效
标题翻译：取代的1,4-二氢吡啶-3,5-二羧酸的杂环基烷基酯
公开(公告)号：US4892875A
公开(公告)日：1990-01-09
申请号：US693196
申请日：1985-01-22
申请人： Kanji Meguro , Akinobu Nagaoka
发明人： Kanji Meguro , Akinobu Nagaoka
IPC分类号： A61K31/44 , C07D211/90 , C07D213/74 , C07D243/08 , C07D295/088 , C07D401/00 , C07D401/04 , C07D401/12 , C07D405/00 , C07D405/04 , C07D407/00 , C07D409/00 , C07D409/04 , C07D413/00 , C07D413/02 , C07D413/04 , C07D417/00 , C07D417/04
CPC分类号： C07D211/90 , C07D213/74 , C07D243/08 , C07D295/088 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is alkyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; R.sup.4 and R.sup.5 are the same or different and each is hydrogen, halogen, nitro, trifluoromethyl, alkyl, cycloalkyl, alkoxy, cyano, alkoxycarbonyl or alkylthio; R.sup.6 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a pyridyl; X is oxygen, sulfur, vinylene, azomethine or a group of the formula ##STR2## A is alkylene; Ar is aryl or a pyridyl; m is an integer of 1 to 3; n is an integer of 0 to 2.
摘要翻译：用作心血管疾病的预防或/或治疗药物的二氢吡啶衍生物及其酸加成盐，所述具有式“IMAGE”的二氢吡啶衍生物，其中R1，R2和R3相同或不同，并且各自为烷基，环烷基，环烷基烷基或烷氧基烷基; R4和R5相同或不同，各自为氢，卤素，硝基，三氟甲基，烷基，环烷基，烷氧基，氰基，烷氧基羰基或烷硫基; R6是氢，烷基，环烷基，芳烷基，芳基或吡啶基; X是氧，硫，亚乙烯基，偶氮甲碱或下式的基团A是亚烷基; Ar为芳基或吡啶基; m为1〜3的整数。 n为0〜2的整数。

6. 发明授权

US4603135A Substituted piperazinyl alkyl esters of 2-amino-4-aryl-1,4-dihydro-6-alkyl-3,5-pyridinedicarboxylates 失效
标题翻译： 2-氨基-4-芳基-1,4-二氢-6-烷基-3,5-吡啶二羧酸酯的取代哌嗪基烷基酯
公开(公告)号：US4603135A
公开(公告)日：1986-07-29
申请号：US654247
申请日：1984-09-25
申请人： Kanji Meguro , Akinobu Nagaoka
发明人： Kanji Meguro , Akinobu Nagaoka
IPC分类号： C07D211/14 , C07D211/90 , C07D295/088 , C07D401/12 , A61K31/495
CPC分类号： C07D295/088 , C07D211/14 , C07D211/90
摘要： Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula ##STR1## wherein R.sup.1 is a hydrogen atom or an aryl,R.sup.2 and R.sup.3 are the same or different and each is an aryl,R.sup.4 and R.sup.6 are the same or different and each is a lower alkyl,R.sup.5 is amino or a lower alkyl,A is an alkylene,X is N or CH andm and n are the same or differentand each is 0 or 1,with the proviso that when X is N, R.sup.5 is amino.
摘要翻译：用作心血管疾病的预防或/或治疗药物的二氢吡啶衍生物及其酸加成盐，所述具有式“IMAGE”的二氢吡啶衍生物，其中R1是氢原子或芳基，R2和R3相同或不同，各自为芳基，R 4和R 6相同或不同，各自为低级烷基，R 5为氨基或低级烷基，A为亚烷基，X为N或CH，m和n相同或不同， 0或1，条件是当X为N时，R 5为氨基。

7. 发明授权

US5965568A Composition for inhibiting production or secretion of amyloid .beta. protein to treat Down's syndrome 失效
标题翻译：用于抑制淀粉样蛋白β蛋白的产生或分泌以治疗唐氏综合征的组合物
公开(公告)号：US5965568A
公开(公告)日：1999-10-12
申请号：US646354
申请日：1996-05-10
申请人： Mitsuru Kakihana , Takuo Kosaka , Akinobu Nagaoka , Giichi Goto
发明人： Mitsuru Kakihana , Takuo Kosaka , Akinobu Nagaoka , Giichi Goto
IPC分类号： A61K31/475 , A61K31/44
CPC分类号： A61K31/475
摘要： A pharmaceutical composition for inhibiting production or secretion of amyloid .beta. protein, which comprises a compound of the formula (I): ##STR1## wherein ring A is an optionally substituted benzene ring, R represents OR.sup.1, ##STR2## or SR.sup.1, wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is selected from a hydrogen atom, an optionally substituted hydrocarbon group or R.sup.2 and R.sup.3, taken together with the adjacent nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group, and Y is an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, if necessary, with a pharmaceutically acceptable excipient, carrier or diluent.
摘要翻译： PCT No.PCT / JP96 / 00265 Sec。 371日期：1996年5月10日 102（e）日期1996年5月10日PCT提交1996年2月8日PCT公布。 WO96 / 25161 PCT出版物日本1996年8月22日用于抑制淀粉样β蛋白的产生或分泌的药物组合物，其包含式（I）的化合物：其中环A是任选取代的苯环，R表示OR 1或SR 1，其中R 1，R 2 和R3相同或不同，各自选自氢原子，任选取代的烃基或与相邻的氮原子一起形成的R 2和R 3，形成任选取代的含氮杂环基，Y是任选取代的烷基或其药学上可接受的盐，如果需要，与药学上可接受的赋形剂，载体或稀释剂。

8. 发明授权

US5916925A Pharmaceutical composition for treatment of dementia 失效
标题翻译：用于治疗痴呆症的药物组合物
公开(公告)号：US5916925A
公开(公告)日：1999-06-29
申请号：US791804
申请日：1997-01-30
申请人： Shuji Higuchi , Akinobu Nagaoka , Giichi Goto , Reinhold Hubner , Dietrich Hadler
发明人： Shuji Higuchi , Akinobu Nagaoka , Giichi Goto , Reinhold Hubner , Dietrich Hadler
IPC分类号： A61K31/122 , A61K31/12
CPC分类号： A61K31/122
摘要： A pharmaceutical composition comprising idebenone of the present invention is useful for prevention of the progression of dementia.
摘要翻译：包含本发明的艾地苯醌的药物组合物可用于预防痴呆的进展。

9. 发明授权

US5604210A Inhibitor of vascular permeability enhancer 失效
标题翻译：血管通透性增强剂的抑制剂
公开(公告)号：US5604210A
公开(公告)日：1997-02-18
申请号：US456723
申请日：1995-06-01
申请人： Akinobu Nagaoka , Tetsuji Imamoto , Tsuneo Asano , Yoshihiro Sugiura , Giichi Goto
发明人： Akinobu Nagaoka , Tetsuji Imamoto , Tsuneo Asano , Yoshihiro Sugiura , Giichi Goto
IPC分类号： A61K31/52 , A61K31/70
CPC分类号： A61K31/7076
摘要： The present invention relates to prevention or treatment a brain edema, an intracranial hemorrhage and a cerebral infarction by administering a pharmaceutically effective amount of a compound or a pharmaceutically acceptable salt thereof, for inhibiting a vascular permeability enhancer, which the compound is of the formula: ##STR1## wherein A is halogen, --X--R.sup.3 in which X is O, S, NH or NHNH, and R.sup.3 is H, acyl, a hydrocarbon group or an aromatic heterocyclic group, or --Y.dbd.R.sup.4 in which Y is N or NHN, and R.sup.4 is a divalent hydrocarbon group, and R.sup.1 is H, halogen, a hydrocarbon group, a heterocyclic group or --Z--R.sup.5 in which Z is O, S or NH, and R.sup.5 is H, a hydrocarbon group or an aromatic heterocyclic group;R.sup.2 is H, halogen, a hydrocarbon group or a heterocyclic group;B is --W--R.sup.6 in which W is CH.sub.2, CO or CS, and R.sup.6 is OH, alkoxy, acyloxy, alkylsulfinyl, alkylsulfonyl, phosphoric acid or amino, or B together with E form a cyclic phosphoric ester; andD and E are H, amino, azido, halogen or OH.
摘要翻译：本发明涉及通过施用药学有效量的化合物或其药学上可接受的盐来抑制血管通透性增强剂来预防或治疗脑水肿，颅内出血和脑梗死，该化合物具有下式：（I）其中A是卤素，X-R 3，其中X是O，S，NH或NHNH，R 3是H，酰基，烃基或芳族杂环基，或-Y = R 4，其中 Y是N或NHN，R4是二价烃基，R1是H，卤素，烃基，杂环基或-Z-R5，其中Z是O，S或NH，R5是H，烃基团或芳族杂环基团; R2是H，卤素，烃基或杂环基; B为-W-R 6，其中W为CH 2，CO或CS，R 6为OH，烷氧基，酰氧基，烷基亚磺酰基，烷基磺酰基，磷酸或氨基，或B与E一起形成环状磷酸酯; 并且D和E是H，氨基，叠氮基，卤素或OH。

10. 发明授权

US5434179A Method for improving brain function using cholinesterase-inhibiting aminoketone compounds 失效
标题翻译：使用胆碱酯酶抑制性氨基酮化合物改善脑功能的方法
公开(公告)号：US5434179A
公开(公告)日：1995-07-18
申请号：US215619
申请日：1994-03-22
申请人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
发明人： Giichi Goto , Akinobu Nagaoka , Yuji Ishihara
IPC分类号： A61K31/135 , A61K31/40 , C07C225/16 , C07D295/108
CPC分类号： C07D295/108 , A61K31/135 , A61K31/40 , C07C225/16
摘要： An aminoketone compound of the formula ##STR1## wherein ring A' means a five through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O, S, N, as the ring-constituents; R.sup.1' means a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.2' means a hydrogen atom or a lower alkyl group; R.sup.3' means an aromatic group which may be substituted; R.sup.4' means a hydrogen atom, a lower alkyl group or aromatic group which may be substituted; n' means an integer of 2 to 7, or a salt thereof, is useful as an cholinesterase inhibitors and a cerebral function ameliorating agent.
摘要翻译：式IMAMA的氨基酮化合物，其中环A'表示可以被取代的五至八元环基，并且可以含有一个或两个作为环组成的O，S，N的杂原子; R1'表示氢原子或可被取代的烃残基; R2'表示氢原子或低级烷基; R3'表示可被取代的芳基; R4'表示氢原子，可以被取代的低级烷基或芳基; n'表示2〜7的整数或其盐可用作胆碱酯酶抑制剂和脑功能改善剂。

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