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2. 发明专利

JPWO2003002532A1 縮合環式基を有する環状ジアミン化合物有权
公开(公告)号：JPWO2003002532A1
公开(公告)日：2004-10-14
申请号：JP2003508715
申请日：2002-06-27
申请人：興和株式会社
发明人：児玉　龍彦 , 龍彦児玉 , 正宏田村 , 正宏田村 , 敏明小田 , 敏明小田 , 行由山嵜 , 行由山嵜 , 雅大西川 , 雅大西川 , 武土肥 , 武土肥 , 善徳京谷 , 善徳京谷
IPC分类号： C07D209/14 , A61K31/4184 , A61K31/423 , A61K31/495 , A61K31/496 , A61K31/517 , A61K31/551 , A61P9/10 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/12 , C07D215/14 , C07D235/10 , C07D235/14 , C07D239/74 , C07D243/06 , C07D243/08 , C07D263/56 , C07D277/64 , C07D295/08 , C07D295/096 , C07D307/81 , C07D333/58 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D263/56 , A61K31/4184 , A61K31/423 , A61K31/496 , A61K31/517 , A61K31/551 , C07D209/14 , C07D215/12 , C07D235/14 , C07D239/74 , C07D243/06 , C07D277/64 , C07D295/096 , C07D307/81 , C07D333/58 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要：次の一般式(1)[式中、R1及びR2は、それぞれ水素原子又はメトキシ基を示し、R2が水素原子であるときはR1はメトキシ基を、R2がメトキシ基であるときはR1は水素原子を示し;Aは、酸素原子、硫黄原子、CH=CH、CH=N又はNR3(ここでR3は、水素原子、低級アルキル基、ヒドロキシ低級アルキル基、低級アルコキシ低級アルキル基、アリール基又はアリール低級アルキル基を示す)を示し;Bは窒素原子、CH又はCR4(ここでR4は水素原子、低級アルキル基、ヒドロキシ低級アルキル基、低級アルコキシ低級アルキル基、アリール基又はアリール低級アルキル基を示す)を示し;mは1又は2の数を示し;nは1〜5の数を示す]で表わされる環状ジアミン化合物、その酸付加塩又はそれらの水和物;及びこれを含有する医薬。細胞接着阻害作用を有し、アレルギー、喘息、リウマチ、動脈硬化症、炎症等の医薬として有用。

3. 发明专利

JPH06502643A 失效
公开(公告)号：JPH06502643A
公开(公告)日：1994-03-24
申请号：JP50091792
申请日：1991-10-31
IPC分类号： A61K31/55 , A61K38/46 , A61P7/02 , A61P9/04 , C07D223/04 , C07D223/06 , C07D223/08 , C07D223/10 , C07D243/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , A61K37/54

4. 发明专利

JPS6143176A A-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,4- triazin-2(3h)-yl)-benzeneacetonitrile 失效
标题翻译：（4-二氢-3,5-二氧代-1,2,4-三氮杂-2（3H） - 基） - 苯并三唑
公开(公告)号：JPS6143176A
公开(公告)日：1986-03-01
申请号：JP16783485
申请日：1985-07-31
申请人： Janssen Pharmaceutica Nv
发明人： GUSUTAAFU MARIA BETSUKUSU , ARUFUONSU HERUMAN MARUGAREETA , BIKUTORU SHIBIDO
IPC分类号： A61K31/53 , A01N37/34 , A01N43/707 , A61P33/02 , C07C67/00 , C07C239/00 , C07C253/00 , C07C271/20 , C07C313/00 , C07C315/04 , C07C317/48 , C07C323/57 , C07C323/63 , C07D243/06 , C07D253/06 , C07D253/075
CPC分类号： C07D253/075

5. 发明专利

JPS59225175A DIAZ(EP)INBIS(N-AMIDINOAMIDINE) DERIVATIVE, MANUFACTURE AND ANTIBACTERIAL OR ANTIFUNGAL COMPOSITION 失效
公开(公告)号：JPS59225175A
公开(公告)日：1984-12-18
申请号：JP9118384
申请日：1984-05-09
申请人： ICI LTD
发明人： MAADOTSUKU ARAN AAKIN , DONARUDO MAREI GAN , DENISU PENBAATON
IPC分类号： C07D295/20 , A01N47/44 , A61K8/43 , A61K8/49 , A61K31/495 , A61P31/04 , A61Q11/00 , C07D243/04 , C07D243/06 , C07D295/215

6. 发明专利

JPH11147867A VITRONECTIN RECEPTOR ANTAGONIST, ITS PRODUCTION AND ITS USE 失效
公开(公告)号：JPH11147867A
公开(公告)日：1999-06-02
申请号：JP36552997
申请日：1997-12-22
申请人： HOECHST AG , GENENTECH INC
发明人： WEHNER VOLKMAR DR , STILZ HANS ULRICH DR , PEYMAN ANUSCHIRWAN , KNOLLE JOCHEN DR , RUXER JEAN-MARIE DR , CARNIATO DENIS DR , LEFRANCOIS JEAN-MICHEL , GADEK THOMAS RICHARD DR , MCDOWELL ROBERT DR
IPC分类号： C07D239/00 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/33 , A61K31/395 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/55 , A61K38/04 , A61P9/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/24 , C07C311/64 , C07C313/30 , C07C327/00 , C07D217/24 , C07D233/04 , C07D235/16 , C07D243/06 , C07D253/06 , C07D253/08 , C07D263/52 , C07D267/08 , C07D277/60 , C07D471/02 , C07D471/04 , C07D487/04 , C07K5/04
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful as a vitronectin receptor antagonist used as an agent for inhibiting the bone resorption by osteoclasts, an agent for inhibiting the growth or metastasis of tumors or an anti-inflammatory agent and further used for treating and preventing cardiovascular diseases, neuropathy, retinopathy or the like. SOLUTION: The compound of the formula: A-B-D-E-F-G [G is A1 or the like; A1 is R R N-C(=NR )NR C(O) or the like; B is a direct bond or the like; D and F are each a direct bond or the like; E is a template selected from a series of fibrinogen receptor antagonists; G is a group of the formula; R and R are each H or the like; R to R are each H or the like; R is C(O)R or the like; R is OH or the like; (q) and (p) are each 0 or 1], The wherein F is C(O)NR , is obtained, for example, by condensing a compound of the formula: A-B-D-E-M (M is a hydroxycarbonyl or the like) with a compound of the formula: HNR -G.

7. 发明专利

JPH0399064A 3-AMINOCROTONIC ACID ESTER 失效
公开(公告)号：JPH0399064A
公开(公告)日：1991-04-24
申请号：JP23609589
申请日：1989-09-12
申请人： KYOTO PHARMA IND
发明人： NISHIZAWA SUSUMU , FUKADA FUMIO , KAKEYA SENJI
IPC分类号： C07D243/06 , C07D211/90 , C07D233/02 , C07D247/00 , C07D295/08 , C07D295/10 , C07D295/18 , C07D295/20 , C07D521/00
摘要： NEW MATERIAL:A compound of formula I (A is alkylene having two carbon atoms bonded to alkyl groups and having a total carbon number of >=5; R is acyl, alkoxycarbonyl, acylalkyl, N-alkyl-substituted carbamoylalkyl, alkenyl, etc.; (m) is 1-3). EXAMPLE:3-Aminocrotonic acid 3-(4-allyl-1-piperidinyl)-2.2-dimethylpropyl ester. USE:Useful as an intermediate for synthesizing 1,4-dihydropyridine derivatives having vasodepressor activity, vasodilation activity, etc. PREPARATION:A compound of formula II is reacted with diketene (ketene dimer) of formula III in the presence of a base (e.g. pyridine) in a solvent such as methylene chloride or in the absence of the solvent at -10 to 130 deg.C to prepare a compound of formula IV, which is reacted with ammonia gas or with a solution of solvent such as methanol saturated with ammonia to provide the compound of formula I.

8. 发明专利

JPS6463569A HETEROARYL DERIVATIVE 失效
公开(公告)号：JPS6463569A
公开(公告)日：1989-03-09
申请号：JP6412588
申请日：1988-03-17
申请人： SANKYO CO
发明人： HIRAI KOICHI , IWANO YUJI , FUJIMOTO KATSUMI , MATSUI YOSHIKI
IPC分类号： C07D401/06 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/495 , A61K31/505 , A61P25/28 , C07D209/02 , C07D209/44 , C07D213/46 , C07D215/08 , C07D239/42 , C07D241/04 , C07D241/08 , C07D243/06 , C07D277/20 , C07D277/46 , C07D295/14 , C07D307/52 , C07D317/66 , C07D417/12 , C07D521/00
摘要： NEW MATERIAL:A compound of formula I [M is 5-7 membered heterocyclic group which contains 2N atoms and may be substituted, on its cyclic carbon atoms, with alkyl and oxo; A is formula II (X , X are H, halogen, where they are not H simultaneously); B is formula III (R is H, alkyl; R , R are H, or incorporate to form oxo; Y is NR ; R , R are H, aryl, aralkyl, alkyl); A, B are different substituents of M on N atoms]. EXAMPLE:1-[Bis(4-fluorophenyl)methyl]-4-(1-naphthylaminocarbonylmethyl )pipe razine. USE:Cerebral metabolism improver. It has excellent calcium-inhibiting action and hypoxia-antagonistic action. PREPARATION:The reaction of an amino compound of the formula: A-M-H with an alkylating agent of formula IV (Xa is halogen, alkanesulfonyl, or the like) gives the compound of formula I.

9. 发明专利

JPS5989661A PHENYLINDENE DERIVATIVE, ACID ADDITION SALT AND MANUFACTURE 失效
公开(公告)号：JPS5989661A
公开(公告)日：1984-05-23
申请号：JP18714383
申请日：1983-10-07
申请人： KEFALAS AS
发明人： IENSU KURISUTEIAN PEREGAARUTO
IPC分类号： A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/18 , A61P25/24 , A61P25/26 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/20 , C07D211/22 , C07D211/24 , C07D211/34 , C07D211/70 , C07D213/30 , C07D243/06 , C07D401/06 , C07D413/06 , C07D417/06

10. 发明专利

JPS5948467A Preparation of homopiperazine derivative 失效
标题翻译：双酚A衍生物的制备
公开(公告)号：JPS5948467A
公开(公告)日：1984-03-19
申请号：JP15883782
申请日：1982-09-14
申请人： Nisshin Flour Milling Co Ltd , Nisshin Kagaku Kk
发明人： KIKUCHI HARUHIKO
IPC分类号： C07D243/08 , A61K31/55 , A61P9/08 , A61P9/10 , B01J29/06 , B01J31/02 , C07B61/00 , C07D243/06
CPC分类号： Y02P20/52
摘要： PURPOSE: To prepare the titled compound, in high yield, by the ester-exchange of N,N'-bis(3-hydroxypropyl)homopiperazine with a 3,4,5-trimethoxybenzoic acid ester under basic condition while removing the produced lower alcohol.
CONSTITUTION: The homopiperazine derivative of formula III {e.g. N,N'-bis[3- (3',4',5'-trimethoxybenzoyloxy)propyl]homopiperazine} is prepared by the ester- exchange reaction of the N,N'-bis(3-hydroxypropyl)-homopiperazine of formula I with the 3,4,5-trimethoxybenzoic acid ester of formula II (R is lower alkyl) in the presence of a base (e.g. sodium ethoxide) while absorbing and removing the by-produced lower alcohol from the system with a molecular sieve.
USE: A drug having coronary vessel dilating activity.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：通过在碱性条件下，通过N，N'-双（3-羟丙基）高哌嗪与3,4,5-三甲氧基苯甲酸酯的酯交换，高产率制备标题化合物，同时除去产生的低级醇。构成：式III的高哌嗪衍生物（例如， N，N'-双[3-（3'，4'，5'-三甲氧基苯甲酰氧基）丙基]高哌嗪}是通过式（I）的N，N'-双（3-羟丙基） - 高密度哌嗪的酯交换反应 I在碱（例如乙醇钠）存在下与式II的3,4,5-三甲氧基苯甲酸酯（R是低级烷基），同时用分子筛吸收并除去副产物的低级醇。使用：具有冠状血管扩张活性的药物。

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