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41. 发明申请

WO1995008536A1 N-(3-PIPERIDINYLCARBONYL)-BETA-ALANINE DERIVATIVES AS PAF ANTAGONISTS 审中-公开
标题翻译：作为PAF拮抗剂的N-（3-哌啶子基） - 苯胺衍生物
公开(公告)号：WO1995008536A1
公开(公告)日：1995-03-30
申请号：PCT/JP1994001550
申请日：1994-09-21
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OHKUBO, Mitsuru , TAKAHASHI, Fumie , YAMANAKA, Toshio , SAKAI, Hiroyoshi , KATO, Masayuki
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D211/60
CPC分类号： C07D401/06 , C07D211/56 , C07D211/60 , C07D405/14 , C07D413/06 , Y02P20/55
摘要： This invention relates to beta -alanine derivatives represented by formula (I), wherein each symbol is as defined in the specification and pharmaceutically acceptable salt thereof which is glycoprotein IIb/IIIa antagonist, inhibitor of blood platelets aggregation and inhibitor of the binding of fibrinogen to blood platelets, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment of diseases indicated in the specification to a human being or an animal.
摘要翻译：本发明涉及由式（I）表示的β-丙氨酸衍生物，其中每个符号如说明书中所定义，其药学上可接受的盐是糖蛋白IIb / IIIa拮抗剂，血小板聚集抑制剂和纤维蛋白原结合抑制剂血小板，其制备方法，包含其的药物组合物以及用于预防和/或治疗本说明书中对人或动物指示的疾病的方法。

42. 发明申请

WO1995003298A1 BENZIMIDAZOLE DERIVATIVES USEFUL AS DOPAMINE RECEPTOR ANTAGONIST, 5-HT RECEPTOR AGONIST OR alpha1 RECEPTOR ANTAGONIST 审中-公开
标题翻译：苯并咪唑衍生物作为多巴胺受体拮抗剂，5-HT受体激动剂或α1受体拮抗剂有用
公开(公告)号：WO1995003298A1
公开(公告)日：1995-02-02
申请号：PCT/JP1994001182
申请日：1994-07-19
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , SAWADA, Kozo , YATABE, Takumi , NOMURA, Chie , OKU, Teruo , TANAKA, Hirokazu
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A benzimidazole compound of formula (I) in which R is lower alkoxy, optionally substituted lower alkyl, cyclo(lower)alkyl, optionally substituted lower alkenyl, mono- or di(lower)alkylamino, optionally substituted heterocyclic group, or optionally substituted aryl, R is hydrogen or lower alkyl, R is optionally substituted aryl, A is lower alkylene, M is -NHCO-, -CONH-, (a), methylene or carbonyl, or R -M is amino, and formula (b) is N-containing heterocyclic group, or pharmaceutically acceptable salts thereof, which is useful as a dopamine receptor agonist, 5-HT receptor agonist or alpha 1 receptor antagonist.
摘要翻译：式（I）的苯并咪唑化合物，其中R 1是低级烷氧基，任选取代的低级烷基，环（低级）烷基，任选取代的低级烯基，一或二（低级）烷基氨基，任选取代的杂环基或任选地取代的芳基，R 2是氢或低级烷基，R 3是任选取代的芳基，A是低级亚烷基，M是-NHCO-，-CONH - ，（a），亚甲基或羰基或R 1 -M为氨基，式（b）为含氮杂环基或其药学上可接受的盐，其可用作多巴胺受体激动剂，5-HT受体激动剂或α1受体拮抗剂。

43. 发明申请

WO1995000536A1 PEPTIDE COMPOUNDS 审中-公开
标题翻译：肽类化合物
公开(公告)号：WO1995000536A1
公开(公告)日：1995-01-05
申请号：PCT/JP1994000985
申请日：1994-06-20
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , MATSUO, Masaaki , HAGIWARA, Daijiro , MIYAKE, Hiroshi , IGARI, Norihiro , MURANO, Kenji
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07K05/06
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/06139
摘要： The object compound of formula (IA), wherein R is heterocyclic group or tetrahydronaphthyl, R is optionally protected hydroxy, R is lower alkyl, R is ar(lower)alkyl, and X is O or N-R , in which R is hydrogen or lower alkyl, and pharmaceutically acceptable salt thereof which are useful as a medicament.
摘要翻译：式（IA）的目标化合物，其中R 1是杂环基或四氢萘基，R 2是任选保护的羟基，R 3是低级烷基，R 4是芳（低级）烷基，X 1是O或NR 5，其中R 5是氢或低级烷基，及其药学上可接受的盐，其可用作药物。

44. 发明申请

WO1994026719A1 MERCAPTO-AMIDE DERIVATIVES USEFUL AS NEUTRAL ENDOPEPTIDASE AND ACE INHIBITORS 审中-公开
标题翻译：适用于中性性内切酶和ACE抑制剂的MERCAPTO-AMIDE衍生物
公开(公告)号：WO1994026719A1
公开(公告)日：1994-11-24
申请号：PCT/JP1994000784
申请日：1994-05-12
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , SHIOKAWA, Youichi , TAKIMOTO, Koichi , TAKENAKA, Kohei , OKITSU, Osamu , MIZUNO, Hiroaki , KOBAYASHI, Yuiko
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , A61K38/00 , C07D281/10 , C07K5/06139 , Y02P20/55
摘要： This invention relates to new mercapto-amide derivatives possessing inhibitory activities against the neutral endopeptidase and the angiotensin converting enzyme, and represented by general formula (I), wherein R is hydrogen or a mercapto-protective group, R is hydrogen or aryl optionally substituted with lower alkylenedioxy, R is lower alkyl substituted with acyl, A is a single bond or lower alkylene, X is lower alkylene, Y is a single bond, O or S, Z is a single bond or lower alkylene, and n is 1 or 2, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有对中性肽链内切酶和血管紧张素转换酶具有抑制活性的新的巯基酰胺衍生物，由通式（I）表示，其中R 1为氢或巯基保护基，R 2为任选被低级亚烷基二氧基取代的氢或芳基，R 3是被酰基取代的低级烷基，A是单键或低级亚烷基，X是低级亚烷基，Y是单键，O或S，Z是单键或低级亚烷基，n为1或2，以及其药学上可接受的盐，其制备方法和包含其的药物组合物。

45. 发明申请

WO1994025062A1 ORAL PHARMACEUTICAL COMPOSITIONS CONTAINING RENIN INHIBITORS 审中-公开
标题翻译：含有RENIN抑制剂的口服药物组合物
公开(公告)号：WO1994025062A1
公开(公告)日：1994-11-10
申请号：PCT/JP1994000670
申请日：1994-04-22
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YAMAGUCHI, Hisami , HATTORI, Masamichi , IBUKI, Rinta , YOSHIDA, Hiromitsu , SHIMAZAKI, Yasuo , KAWAMURA, Akio , TAKAHASHI, Toshiya , OHNISHI, Norio , HATA, Takehisa
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： A61K37/64
CPC分类号： A61K47/10 , A61K9/0007 , A61K38/553 , A61K47/12 , A61K47/14 , A61K47/26 , A61K47/40
摘要： This invention relates to an oral pharmaceutical composition characterized by comprising an amino acid derivative of general formula (I) wherein each symbol is as defined in the description, or a salt thereof and one or more ingredient(s) selected from the group consisting of tartaric acid, citric acid, higher alcohol, cyclodextrin, sucrose ester of fatty acid and polyglycerin ester of fatty acid.
摘要翻译：本发明涉及一种口服药物组合物，其特征在于包含通式（I）的氨基酸衍生物，其中每个符号如说明书中所定义，或其盐和一种或多种选自酒石酸的成分酸，柠檬酸，高级醇，环糊精，脂肪酸的蔗糖酯和脂肪酸的聚甘油酯。

46. 发明申请

WO1994010205A1 PROTEIN SPECIFIC FOR ALZHEIMER'S DISEASE AND METHOD OF DIAGNOSING ALZHEIMER'S DISEASE THROUGH DETECTION OF THE PROTEIN 审中-公开
标题翻译：阿尔茨海默病的蛋白质特异性和通过检测蛋白质诊断阿尔茨海默病的方法
公开(公告)号：WO1994010205A1
公开(公告)日：1994-05-11
申请号：PCT/JP1993001503
申请日：1993-10-19
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , SUGAYA, Kiminobu , MARUSAWA, Hiroshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07K15/06
CPC分类号： G01N33/6896 , C07K14/4711
摘要： The invention provides a method of diagnosing Alzheimer's disease and a kit therefor by finding out a protein that can be detected from the patients with Alzheimer's disease but not from the normal subjects and using the protein or an antibody recognizing the fragments of the same. The protein has the following characteristics: (1) molecular weight: 30 kD as determined according to sodium dodecyl sulfate-polyacrylamide gel electrophoresis; (2) isoelectric point (pI): 6.9; and (3) amino acid sequence at the N-terminus ( alpha ) wherein Xaa represents an unidentified amino acid residue.
摘要翻译：本发明提供了一种诊断阿尔茨海默氏病的方法及其试剂盒，其通过找出可以从阿尔茨海默病患者而不是来自正常受试者的蛋白质，并使用识别其中的片段的蛋白质或抗体。该蛋白具有以下特点：（1）根据十二烷基硫酸钠 - 聚丙烯酰胺凝胶电泳测定的分子量：30kD; （2）等电点（pI）：6.9; 和（3）N-末端的氨基酸序列（α），其中Xaa代表未鉴定的氨基酸残基。

47. 发明申请

WO1994010177A1 CEPHEM COMPOUNDS, AND THEIR PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： CEPHEM化合物及其药物组合物
公开(公告)号：WO1994010177A1
公开(公告)日：1994-05-11
申请号：PCT/JP1993001505
申请日：1993-10-19
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , KAWABATA, Kohji , TERASAWA, Takeshi , NAKAMURA, Ayako , NAKAMURA, Hideko , SHIRAI, Fumiyuki , SAKANE, Kazuo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D501/20
CPC分类号： C07D501/00 , Y02P20/55
摘要： New cephem compounds of formula (I), wherein R is amino or protected amino, R is hydrogen, a hydroxy protective group, lower alkyl or mono(or di or tri)halo(lower)alkyl, R is carboxy or protected carboxy, and R is pyridylvinyl which may have suitable substituent(s), with proviso that (i) when R is hydrogen and R is 3-pyridylvinyl, then R is not carboxy, and (ii) when R is tetrahydropyranyl and R is 3-pyridylvinyl, then R is not benzhydryloxycarbonyl, and pharmaceutical acceptable salts thereof which are useful as a medicament.
摘要翻译：式（I）的新的头孢烯化合物，其中R 1是氨基或保护的氨基，R 2是氢，羟基保护基，低级烷基或单（或二或三）卤代（低级）烷基， R 3是羧基或保护的羧基，R 4是可以具有合适取代基的吡啶基乙烯基，条件是（i）当R 2是氢且R 4是3-吡啶基乙烯基时， 3>不是羧基，和（ii）当R 2是四氢吡喃基且R 4是3-吡啶基乙烯基时，则R 3不是可用作药物的二苯甲基氧基羰基及其药学上可接受的盐。

48. 发明申请

WO1994007491A1 ANALGESIC, ANTICONJUNCTIVITIC OR CHRONIC RHEUMATISM REMEDY CONTAINING QUINOLIZINONE COMPOUND OR SALT THEREOF, AND PREPARATION FOR TOPICAL APPLICATION THEREOF 审中-公开
标题翻译：含有喹唑啉酮化合物或其盐的毒性，抗炎性或慢性炎症性补救措施及其局部应用的准备
公开(公告)号：WO1994007491A1
公开(公告)日：1994-04-14
申请号：PCT/JP1993001396
申请日：1993-09-29
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HIROI, Jun , SHIMOMURA, Kyoichi , HATA, Takehisa , KAGAYAMA, Akira , KIMURA, Sumihisa , SAWAI, Seiji , UEDA, Satoshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/435
CPC分类号： A61K31/44
摘要： An analgesic, anticonjunctivitic or chronic rheumatism remedy containing a quinolizinone compound represented by formula (I) or a salt thereof, and a stable anticonjunctivitic preparation for topical application containing the above compound or salt and a cellulose derivative. In formula (I), R1 represents aminocarbonyl, etc.; R4 represents hydrogen, etc.; R2 represents hydrogen, etc.; R3 represents aryloxy, etc.; and R2 and R3 may be at any position of the quinolizinone ring and combined together to form -CH2CH2CH2-, etc.
摘要翻译：含有由式（I）表示的喹嗪酮化合物或其盐的镇痛，止血或慢性风湿病药，以及含有上述化合物或盐的纤维素衍生物的用于局部施用的稳定的抗凝血剂制剂。式（I）中，R 1表示氨基羰基等。 R4代表氢等; R2代表氢等; R3表示芳氧基等。并且R2和R3可以在喹嗪酮环的任何位置并结合在一起形成-CH 2 CH 2 CH 2 - 等

49. 发明申请

WO1993025205A1 PYRAZOLOPYRIDINE COMPOUNDS FOR THE TREATMENT OF ANEMIA 审中-公开
标题翻译：用于治疗神经酰胺的吡咯并吡啶化合物
公开(公告)号：WO1993025205A1
公开(公告)日：1993-12-23
申请号：PCT/JP1993000762
申请日：1993-06-07
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , KOHNO, Yutaka , NAGATOMI, Itsuo , HANAOKA, Kaori
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , A61K31/445
摘要： The present invention relates to a pharmaceutical composition for the prevention and/or the treatment of anemia in a human being or an animal which comprises, as an active ingredient, a pyrazolopyridine compound of formula (I) wherein R is lower alkyl, etc, R is a group of formula (II) (wherein R is protected amino, etc, and R is hydrogen, etc); etc, and R is hydrogen, etc, or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier or excipient, etc.
摘要翻译：本发明涉及用于预防和/或治疗人或动物中的贫血的药物组合物，其包含作为活性成分的式（I）的吡唑并吡啶化合物，其中R 1为低级烷基，等等，R 2是式（II）的基团（其中R 4是被保护的氨基等，R 5是氢等）; 等等，R 3是氢等，或其药学上可接受的盐与药学上可接受的载体或赋形剂等混合。

50. 发明申请

WO1993017013A1 QUINOLYLBENZOFURAN DERIVATIVES AS LEUKOTRIENE ANTAGONISTS 审中-公开
标题翻译：喹诺酮衍生物作为白介素拮抗剂
公开(公告)号：WO1993017013A1
公开(公告)日：1993-09-02
申请号：PCT/JP1993000198
申请日：1993-02-18
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , MATSUO, Masaaki , OKUMURA, Kazuo , SHIGENAGA, Shinji
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D405/04
CPC分类号： C07D405/04 , C07D405/14
摘要： This invention relates to new quinolylbenzofuran derivatives having activities as leukotrien and Slow Reacting Substance of Anaphylaxis antagonists and inhibitors and represented by general formula (I), wherein R is halogen, etc., R is hydrogen or halogen, R is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy, R is hydrogen, acyl, cyano, nitro, substituted or unsubstituted aryl, or substituted or unsubstituted lower alkyl, R is hydrogen, hydroxy, lower alkyl or lower alkoxy, A is lower alkylene, lower alkenylene or a single bond, X is a single bond, O, NH, S, SO or SO2, and Y is O or S, provided that when R is hydrogen, R is hydrogen, R is hydrogen, A is a single bond and X is a single bond, then R is halogen, etc., and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有作为白三烯和慢反应物质的过敏反应物和抑制剂的新的喹啉基苯并呋喃衍生物，其通式（I）表示，其中R 1为卤素等，R 2为氢或卤素，R R 4是氢，卤素，羟基，低级烷基或低级烷氧基，R 4是氢，酰基，氰基，硝基，取代或未取代的芳基或取代或未取代的低级烷基，R 5是氢，羟基，低级烷基或低级烷氧基，A为低级亚烷基，低级亚烯基或单键，X为单键，O，NH，S，SO或SO 2，Y为O或S，条件是当R 3为氢时 R 4为氢，R 5为氢，A为单键，X为单键，则R 1为卤素等，及其药学上可接受的盐，用于制备其中以及含有该组合物的药物组合物。

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