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1. 发明申请

WO1998005624A1 AMINO COMPOUNDS AND ANGIOTENSIN IV RECEPTOR AGONISTS 审中-公开
标题翻译：氨基化合物和血管紧张素Ⅱ受体激动剂
公开(公告)号：WO1998005624A1
公开(公告)日：1998-02-12
申请号：PCT/JP1997002716
申请日：1997-08-05
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER , KOBORI, Takeo , GODA, Kenichi , SUGIMOTO, Kikuo , OTA, Tomomi , TOMISAWA, Kazuyuki
发明人： TAISHO PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： C07C211/13
CPC分类号： C07D213/40 , C07C237/20 , C07D215/12
摘要： Amino compounds represented by general formula (1) or pharmaceutically acceptable salts thereof: (wherein X represents CH2NH or CONH; Y represents CH2NH or CONH, provided that X and Y do not represent CONH at the same time; Z represents CH=C(R )R , CH2CH(R )R or alkoxycarbonyl (wherein R and R independently represent each hydrogen or optionally substituted alkyl, aralkyl, aryl or heteroaryl); R represents hydrogen or optionally substituted lower alkyl, cycloalkyl, cycloalkyl-substituted alkyl, aralkyl or aryl; and R and R independently represent each optionally substituted lower alkyl or aralkyl); drugs composed of the amino compounds of general formula (1) or pharmaceutically acceptable salts thereof; and angiotensin receptor agonists containing the same as the active ingredient. These drugs are useful as remedies such as antagonists or agonists for various pathological states in which angiotensin IV participates, for example, accelerated renal blood flow, cerebral vasodilation, cell proliferation inhibition or hypermnesia.
摘要翻译：由通式（1）表示的氨基化合物或其药学上可接受的盐：（其中X表示CH 2 NH或CONH; Y表示CH 2 NH或CONH，条件是X和Y不同时表示CONH; Z表示CH = C R 5），CH 2 CH（R 4）R 5或烷氧基羰基（其中R 4和R 5独立地表示各个氢或任选取代的烷基，芳烷基，芳基或杂芳基）; R R 1和R 3独立地代表各个任选被取代的低级烷基或芳烷基）; R 2和R 3独立地表示任意取代的低级烷基或芳烷基。由通式（1）的氨基化合物或其药学上可接受的盐组成的药物; 和含有与活性成分相同的血管紧张素受体激动剂。这些药物可用作诸如血管紧张素IV参与的各种病理状态的拮抗剂或激动剂，例如加速肾血流量，脑血管扩张，细胞增殖抑制或高血症。

2. 发明申请

WO1997003093A1 PEPTIDE DERIVATIVES AND ANGIOTENSIN IV RECEPTOR AGONIST 审中-公开
标题翻译：肽衍生物和血管紧张素受体激动剂
公开(公告)号：WO1997003093A1
公开(公告)日：1997-01-30
申请号：PCT/JP1996001836
申请日：1996-07-03
申请人： SAGAMI CHEMICAL RESEARCH CENTER , TAISHO PHARMACEUTICAL CO., LTD. , KOBORI, Takeo , GODA, Kenichi , SUGIMOTO, Kikuo , OTA, Tomomi , TOMISAWA, Kazuyuki
发明人： SAGAMI CHEMICAL RESEARCH CENTER , TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07K05/062
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0202 , C07K5/06017 , C07K5/0804 , C07K5/0812 , C07K5/0815 , C07K5/0821
摘要： Short-chain peptide derivatives represented by general formula (1) which function as an angiotensin IV receptor agonist even in a low concentration and so are useful as a remedy for various diseases wherein angiotensin IV participates.
摘要翻译：由通式（1）表示的短链肽衍生物即使在低浓度下也起到血管紧张素IV受体激动剂的作用，因此可用作血管紧张素IV参与的各种疾病的治疗方法。

3. 发明申请

WO1992007840A1 THIAZOLE THIOESTER DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：WO1992007840A1
公开(公告)日：1992-05-14
申请号：PCT/JP1991001482
申请日：1991-10-30
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER , KOBORI, Takeo , YAMAMOTO, Rumi , FUJITA, Mikako , HIYAMA, Tamejiro , NAGATE, Takatoshi
发明人： TAISHO PHARMACEUTICAL CO., LTD. , SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： C07D277/74
CPC分类号： C07D501/00 , C07D277/74 , Y02P20/55
摘要： A compound represented by general formula (I), which is useful as an intermediate for the production of (Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide-substituted cephalosporin derivatives having an excellent antibacterial activity, wherein R1 represents hydrogen or a hydroxyl protecting group.
摘要翻译：由通式（I）表示的化合物，其可用作制备具有优异抗菌活性的（Z）-2-（2-氨基噻唑-4-基）-2-羟基亚氨基乙酰胺取代的头孢菌素衍生物的中间体，其中 R 1表示氢或羟基保护基。

4. 发明申请

WO1998001536A1 MICROORGANISMS PRODUCING DOCOSAHEXAENOIC ACID AND PROCESS FOR THE PRODUCTION OF DOCOSAHEXAENOIC ACID 审中-公开
标题翻译：生产DOCOSAHEXAENOIC的微生物和生产DOCOSAHEXAENOIC酸的方法
公开(公告)号：WO1998001536A1
公开(公告)日：1998-01-15
申请号：PCT/JP1997002284
申请日：1997-07-02
申请人： SAGAMI CHEMICAL RESEARCH CENTER , FUJIYAKUHIN COMPANY, LIMITED , YAZAWA, Kazunaga , WATANABE, Kazuo , ISHIKAWA, Chikako , TOMITA, Miho , MURAMATSU, Hiroshi
发明人： SAGAMI CHEMICAL RESEARCH CENTER , FUJIYAKUHIN COMPANY, LIMITED
IPC分类号： C12N01/20
CPC分类号： C12P7/6427 , C12P7/6472 , C12R1/01
摘要： Microorganisms belonging to the genus Shewanella or Pseudoalteromonas which can produce docosahexaenoic acid (DHA) within a short culture period; a process for producing DHA which comprises culturing these microorganisms and isolating a lipid fraction from the culture; and a process for producing DHA labeled with a stable isotope with a high safety by using these microorganisms.
摘要翻译：属于希瓦氏菌属或伪黄单胞菌属的微生物，其可以在短的培养期内产生二十二碳六烯酸（DHA）; 一种生产DHA的方法，包括培养这些微生物并从培养物中分离脂质部分; 以及通过使用这些微生物生产具有高安全性的稳定同位素标记的DHA的方法。

5. 发明申请

WO1997021804A1 NOVEL THERMOLYSIN-LIKE PROTEASE AND USE THEREOF 审中-公开
标题翻译：新型热病菌样蛋白及其用途
公开(公告)号：WO1997021804A1
公开(公告)日：1997-06-19
申请号：PCT/JP1996003617
申请日：1996-12-11
申请人： SAGAMI CHEMICAL RESEARCH CENTER , HOLLAND SWEETENER COMPANY V.O.F. , HANZAWA, Satoshi , OHE, Seigo , MIYAKE, Toshio , KIDOKORO, Shun-ichi , ENDO, Kimiko , WADA, Akiyoshi
发明人： SAGAMI CHEMICAL RESEARCH CENTER , HOLLAND SWEETENER COMPANY V.O.F.
IPC分类号： C12N09/54
CPC分类号： C07K5/0613 , C12N9/54 , C12Y304/24027
摘要： A novel thermolysin-like protease having an improved stability and a method wherein this protease is used in a coupling reaction with phenylalanine methyl ester so as to elevate the efficiency of the reaction. The novel thermolysin-like protease is one which is to be used in the coupling of N-benzyloxycarbonylaspartic acid with phenylalanine methyl ester in a water soluble medium in a process for synthesizing benzyloxycarbonyl- alpha -L-aspartyl-L-phenylalanine methyl ester via the enzymatic reaction and characterized in that the volume of a void in electron density existing in the thermolysin having the amino acid sequence of SEQ ID NO:1 in the Sequence Listing and surrounded at least by Leu at the 144-position, Thr at the 149-position, Ala at the 240-position, Ala at the 270-position and Ala at the 288-position has been at least partly made up for by substituting at least one of these amino acid residues by amino acid residue(s) having larger hydrophobicity and bulkiness, or by affecting the amino acid residues surrounding the void in electron density so as to reduce the volume of the void, and a method wherein the protease is used in the coupling reaction of N-benzyloxycarbonylaspartic acid with phenylalanine methyl ester.
摘要翻译：具有改进的稳定性的新型嗜热菌蛋白酶样蛋白酶和其中所述蛋白酶用于与苯丙氨酸甲酯的偶联反应中以提高反应效率的方法。新型嗜热溶蛋白酶样蛋白酶是一种用于在苄基氧羰基-α-天冬氨酰基-L-苯丙氨酸甲酯合成方法中通过水溶性介质偶联N-苄氧基羰基天冬氨酸与苯丙氨酸甲酯的蛋白酶酶反应，其特征在于存在于序列表中具有SEQ ID NO：1的氨基酸序列的嗜热溶菌素中的电子密度的空隙的体积，至少被144位的Leu，在149位的Thr，位置，240位的Ala，270位的Ala和288位的Ala已经至少部分地由这些氨基酸残基中的至少一个用疏水性较大的氨基酸残基代替或通过以电子密度影响空隙周围的氨基酸残基以减小空隙体积的方法，以及其中所述蛋白酶用于N-苄氧基羰基天冬氨酸的偶联反应的方法与苯丙氨酸甲酯。

6. 发明申请

WO1996003371A1 N-ACYL-N-(SUBSTITUTED CINNAMOYL)ETHYLENEDIAMINE DERIVATIVE 审中-公开
标题翻译： N-乙酰基-N-（取代的CINNAMOYL）乙烯基胺衍生物
公开(公告)号：WO1996003371A1
公开(公告)日：1996-02-08
申请号：PCT/JP1995001450
申请日：1995-07-21
申请人： SAGAMI CHEMICAL RESEARCH CENTER , NIPPON SHOJI KAISHA, LIMITED , FUJIYAKUHIN COMPANY, LIMITED , YAZAWA, Kazunaga , SHIKANO, Mayumi , MASUZAWA, Yasuo , TSUJI, Tomoko , YAMAGUCHI, Koji , SODA, Yasuji
发明人： SAGAMI CHEMICAL RESEARCH CENTER , NIPPON SHOJI KAISHA, LIMITED , FUJIYAKUHIN COMPANY, LIMITED
IPC分类号： C07C235/34
CPC分类号： C07C235/34
摘要： A novel N-acyl-N-(substituted cinnamoyl)ethylenediamine derivative represented by general formula (I) and serving as an antiphlogistic and/or NGF production accelerator, (wherein R represents the acyl residue of a C16 or higher unsaturated fatty acid; R and R represent each independently hydrogen or lower alkyl; and n represents 1 or 2). This compound is expected to be usable as, for example, an antiphlogistic because it has the activities of O2 production inhibitor in human neutrophilic leukocytes and intracellular phospholipase A2 inhibition, and as a remedy for dementia, spinal cord injury, peripheral nerve injury, diabetic neuropathy and amyotrophic lateral sclerosis because it has the activity of accelerating NGF production.
摘要翻译：一种由通式（I）表示并用作消炎和/或NGF生产促进剂的新型N-酰基-N-（取代肉桂酰）乙二胺衍生物（其中R 1表示C16或更高级不饱和脂肪酸的酰基残基酸; R 2和R 3各自独立地表示氢或低级烷基; n表示1或2）。预期该化合物可用作例如消炎药，因为它具有人嗜中性白细胞中的O 2 - 产生抑制剂和细胞内磷脂酶A2抑制的活性，并且作为痴呆，脊髓损伤，周围神经损伤的补救剂，糖尿病性神经病变和肌萎缩性侧索硬化，因为它具有加速NGF生产的活性。

7. 发明申请

WO1994020092A1 CALCIUM ANTAGONIST 审中-公开
公开(公告)号：WO1994020092A1
公开(公告)日：1994-09-15
申请号：PCT/JP1994000373
申请日：1994-03-09
申请人： SAGAMI CHEMICAL RESEARCH CENTER , YAZAWA, Kazunaga , ISHIKAWA, Chikako , KONDO, Kiyosi , MOMOSE, Yasunori
发明人： SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： A61K31/375
CPC分类号： A61K31/375 , C07D307/62
摘要： A calcium antagonist containing ascorbyl docosahexaenoate as the active ingredient. This ester has the activity of blocking a membrane-potential-dependent L-type calcium (Ca ) channel in a canine ventricular muscle monocyte, thus inhibiting myocardial contraction. This calcium channel antagonistic (blocking) activity is more potent than diltiazem. Hence this antagonist is useful for treating circulatory diseases, in particular, for preventing and treating ischemic heart diseases, such as angina pectoris and myocardial infarction, and hypertension.
摘要翻译：含有抗坏血酸二十二碳六烯酸酯的钙拮抗剂作为活性成分。该酯具有在犬心室肌单核细胞中阻断膜电位依赖性L型钙（Ca 2+）通道的活性，从而抑制心肌收缩。这种钙通道拮抗（阻断）活性比地尔硫卓更有效。因此，该拮抗剂可用于治疗循环系统疾病，特别是用于预防和治疗诸如心绞痛和心肌梗死以及高血压的缺血性心脏病。

8. 发明申请

WO1991009674A1 CATALYST FOR HYDROGENATION, DEHYDROSILYLATION OR HYDROSILYLATION, AND ITS USE 审中-公开
标题翻译：氢化，脱氢或氢化催化剂及其用途
公开(公告)号：WO1991009674A1
公开(公告)日：1991-07-11
申请号：PCT/JP1990001708
申请日：1990-12-26
申请人： SAGAMI CHEMICAL RESEARCH CENTER , FUCHIKAMI, Takamasa , UBUKATA, Yumiko , TANAKA, Yasutaka
发明人： SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： B01J31/20
CPC分类号： B01J31/20 , B01J2231/323 , B01J2231/643 , B01J2231/645 , B01J2531/60 , C07C5/03 , C07C5/05 , C07C5/08 , C07C5/09 , C07C29/145 , C07C29/172 , C07C45/62 , C07C51/36 , C07C67/31 , C07C209/48 , C07C209/52 , C07C231/12 , C07C2531/20 , C07F7/0801 , C07F7/0829 , C07F7/0896 , C07F7/1804 , C07F7/188 , C07C35/14 , C07C33/20
摘要： Catalyst used in hydrogenation, dehydrosilylation of ketones, and hydrosilylation of dienes or acetylenes, comprises complex of formula: A+(M2H(CO)10), A is alkali metal, ammonium, iminium or phosphonium cation, and M is chromium, molybdenum or tungsten atom; and processes for producing dehydrosilylated ketones and hydrosilylated dienes or acetylenes in presence of catalyst. @(51pp Dwg.No.0/0).

9. 发明申请

WO1990002725A1 PROCESS FOR PRODUCING 2-OXO-3-AROMATIC CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译： 2-氧代-3-芳基羧酸衍生物的制备方法
公开(公告)号：WO1990002725A1
公开(公告)日：1990-03-22
申请号：PCT/JP1989000928
申请日：1989-09-11
申请人： SAGAMI CHEMICAL RESEARCH CENTER , HIRAI, Kenji , NAKAMURA, Kazumi , FUJITA, Atsuko
发明人： SAGAMI CHEMICAL RESEARCH CENTER
IPC分类号： C07C59/185
CPC分类号： C07D333/24 , C07C51/347 , C07D317/60 , C07C63/14 , C07C59/84 , C07C59/86 , C07C59/90 , C07C59/88
摘要： The invention relates to a process for producing a 2-oxo-3-aromatic carboxylic acid derivative, which comprises reacting an aromatic pyruvic acid derivative with an electrophilic compound in a protic solvent in the presence of a base. This process can provide in good yields the 2-oxo-3-aromatic carboxylic acid derivatives which can be easily converted to aromatic amino acid derivatives or 2-aromatic alkanoic acid derivatives which are important intermediates for synthesizing medicines, agrochemicals, etc.

10. 发明申请

WO1989001513A1 FAST-ACTING PROUROKINASE 审中-公开
标题翻译：快速行动预防措施
公开(公告)号：WO1989001513A1
公开(公告)日：1989-02-23
申请号：PCT/JP1988000815
申请日：1988-08-18
申请人： SAGAMI CHEMICAL RESEARCH CENTER , CENTRAL GLASS COMPANY, LIMITED , HODOGAYA CHEMICAL COMPANY, LIMITED , NIPPON SODA COMPANY, LIMITED , NISSAN CHEMICAL INDUSTRIES, LIMITED , TOSOH CORPORATION , KOBAYASHI, Yoichi , OMORI, Muneki , YAMADA, Chikako
发明人： SAGAMI CHEMICAL RESEARCH CENTER , CENTRAL GLASS COMPANY, LIMITED , HODOGAYA CHEMICAL COMPANY, LIMITED , NIPPON SODA COMPANY, LIMITED , NISSAN CHEMICAL INDUSTRIES, LIMITED , TOSOH CORPORATION
IPC分类号： C12N09/72
CPC分类号： C12N9/6462 , C12Y304/21073
摘要： A human prourokinase-like polypeptide having an amino acid sequence represented by the following formula: (Met).Ser1-X156.Y157.Z158- (wherein Met represents an optionally existing methionine, Ser represents serine present at 1-position of the N-terminal, X represents arginine or other amino acid present at 156-position, Y represents proline, glycine, alanine or valine present at 157-position, Z represents lysine or arginine present at 158-position, and the solid line represents the same amino acid sequence as that of corresponding part of natural human prourokinase or human urokinase-like polypeptide wherein lysine at 135-position is replaced by other amino acid than basic amino acids) or having an amino acid sequence substantially the same as this is disclosed. In addition, a DNA segment which codes the above-described polypeptide; a plasmid containing said DNA segment; E. coli transformed by said plasmid; a process for preparing said polypeptide by culturing said E. coli; a medicine containing said polypeptide; use of said polypeptide for prophylaxis or treatment for formation of thrombus; and use of said polypeptide for preparing the medicine for the above purpose are also disclosed.

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