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1. 发明申请

WO1991013089A1 PEPTIDE DERIVATIVES AND PRODUCTION THEREOF 审中-公开
标题翻译：肽衍生物及其生产
公开(公告)号：WO1991013089A1
公开(公告)日：1991-09-05
申请号：PCT/JP1991000165
申请日：1991-02-12
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , WAKIMASU, Mitsuhiro , KIKUCHI, Takashi , KUBO, Kazuki
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07K07/10
CPC分类号： C07K14/57536 , A61K38/00
摘要： Disclosed are a peptide derivative represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein A, B, C, D, E, and F each represent amino acid residues, and satisfy any one condition of (i) A=Ser, C=Ser, D=Leu, E=Met and F=Phe, (ii) A=Ser, B=Ser, C=Ser, D=Trp, E=Leu and F=Phe, and (iii) A=Thr, B=Phe, C=Thr, D=Tyr, E=Lys and F=Tyr; and W, X, Y and Z each represent amino acid residues, and satisfy any one condition of (i) at least one of W and Y is an amino acid residue other than an L-alanine residue or other than an L-cysteine residue, (ii) X is an amino acid residue other than an L-lysine residue, and (iii) Z is an amino acid residue other than an L-aspartic acid residue; (2) a method for producing the peptide derivative function mainly comprising the peptide derivate or the salt thereof; and (3) an agent for improving a circulatory function mainly comprising the peptide derivative or the salt thereof, such as a vasodilator or a vasoconstrictor.
摘要翻译：公开了由式（I）表示的肽衍生物或其药学上可接受的盐，其中A，B，C，D，E和F各自表示氨基酸残基，并且满足（i）A = Ser， C = Ser，D = Leu，E = Met和F = Phe，（ii）A = Ser，B = Ser，C = Ser，D = Trp，E = Leu和F = Phe，和（iii）A = Thr ，B = Phe，C = Thr，D = Tyr，E = Lys和F = Tyr; 并且W，X，Y和Z各自表示氨基酸残基，并且满足（i）W和Y中的至少一个是L-丙氨酸残基或L-半胱氨酸残基以外的氨基酸残基的任何一个条件，（ii）X是除L-赖氨酸残基以外的氨基酸残基，（iii）Z是除了L-天冬氨酸残基以外的氨基酸残基; （2）生成主要含有肽衍生物或其盐的肽衍生物功能的方法; 和（3）主要由肽衍生物或其盐例如血管扩张剂或血管收缩剂改善循环功能的药剂。

2. 发明申请

WO1998029136A1 STABILIZED TRICYCLIC COMPOUND 审中-公开
标题翻译：稳定的三聚体化合物
公开(公告)号：WO1998029136A1
公开(公告)日：1998-07-09
申请号：PCT/JP1997004819
申请日：1997-12-25
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , IMOTO, Soichiro , YOSHIOKA, Minoru , KASHIHARA, Toshio
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K47/14
CPC分类号： A61K31/437 , A61K9/4858 , A61K31/4985 , A61K47/14
摘要： The present invention provides a pharmaceutical composition which contains an oleginous base and a tricyclic compound or a pharmaceutically acceptable salt.
摘要翻译：本发明提供了一种药物组合物，其含有一种含水基和三环化合物或其药学上可接受的盐。

3. 发明申请

WO1998015263A2 A METHOD FOR PRODUCING A MICROPARTICLE 审中-公开
标题翻译：一种生产微生物的方法
公开(公告)号：WO1998015263A2
公开(公告)日：1998-04-16
申请号：PCT/JP1997003608
申请日：1997-10-08
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , TAKECHI, Nobuyuki , NONOMURA, Muneo , HIGUCHI, Shigehiro , BEPPU, Toshiharu
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K09/16
CPC分类号： A61K31/683 , A61K9/1647 , A61K31/38 , A61K31/382 , A61K31/67 , B02C23/06
摘要： This invention provides a method for producing a microparticle which comprises pulverizing a solid preparation comprising a compound represented by formula (I), wherein ring A is an optionally substituted benzene ring; R is a hydrogen atom or an optionally substituted hydrocarbon group; B is an optionally esterified or amidated carboxyl group; X is -CH(OH)- or -CO-; k is 0 or 1; and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof and a biodegradable polymer of alpha -hydroxycarboxylic acid in the presence of a pulverizing auxiliary, which can provide microparticles which are less adhesive and involve less aggregation and are thus excellent in drug entrapment ratio and control of drug release in a desired particle size.
摘要翻译：本发明提供一种微粒的制造方法，其特征在于，包括粉碎由式（I）表示的化合物的固体制剂，其中环A为任选取代的苯环; R是氢原子或任选取代的烃基; B是任选酯化或酰胺化的羧基; X是-CH（OH） - 或-CO-; k为0或1; 和n为0,1或2或其药学上可接受的盐和α-羟基羧酸的可生物降解的聚合物，其在粉碎助剂的存在下，可提供粘合性较小并且聚集较少并因此优异的药物捕获的微粒比例和控制所需粒度的药物释放。

4. 发明申请

WO1998009958A1 CONDENSED 4,5,6,7-TETRAHYDROBENZO[C]THIOPHENES AS ENHANCER FOR CELL DIFFERENTIATION INDUCTION FACTOR ACTION 审中-公开
标题翻译：浓缩的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强剂
公开(公告)号：WO1998009958A1
公开(公告)日：1998-03-12
申请号：PCT/JP1997003122
申请日：1997-09-05
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , YASUMA, Tsuneo , ODA, Tsuneo , HAZAMA, Masatoshi , TAKETOMI, Shigehisa
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07D333/72
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by formula (I') wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R represents an optionally substituted hydrocarbon group; R represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由式（I'）表示的化合物，其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R 1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族5元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，可用于预防和治疗骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌症转移等骨疾病，和基于神经变性的疾病。

5. 发明申请

WO1998009624A1 WATER-SOLUBLE VITAMIN COMPOSITION THAT PROVIDES EXCELLENT TABLETS AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：提供优异的片剂的水溶性维生素组合物及其生产方法
公开(公告)号：WO1998009624A1
公开(公告)日：1998-03-12
申请号：PCT/JP1996003079
申请日：1996-10-23
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , ASHIDA, Hiroshi , IZUTSU, Daisuke , YAMASHITA, Akio
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K31/375
CPC分类号： A61K9/1623 , A61K9/1652 , A61K9/1688 , A61K9/2018 , A61K9/2095 , A61K31/375
摘要： A water-soluble vitamin composition which contains from 90 to 99.8 % by weight of water-soluble vitamins together with at least one additive selected from among polymeric binders, monosaccharides, disaccharides, sugar alcohols, dextrin and organic acids. The composition can provide tablets having a high mechanical strength (hardness) and being easily disintegrable without causing so much tableting disorder.
摘要翻译：一种水溶性维生素组合物，其含有90至99.8重量％的水溶性维生素以及至少一种选自聚合物粘合剂，单糖，二糖，糖醇，糊精和有机酸的添加剂。组合物可以提供具有高机械强度（硬度）并容易崩解的片剂，而不会引起如此多的压片障碍。

6. 发明申请

WO1997048726A1 METHOD FOR PRODUCING PEPTIDES 审中-公开
标题翻译：生产肽的方法
公开(公告)号：WO1997048726A1
公开(公告)日：1997-12-24
申请号：PCT/JP1997002097
申请日：1997-06-19
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , HATANAKA, Chitoshi , ABE, Yasuaki , YAMANO, Mitsuhisa
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07K07/23
CPC分类号： C07K7/23 , Y02P20/55
摘要： A peptide of the formula (I): 5-oxo-Pro-R -Trp-Ser-R -R -R -Arg-Pro-R , wherein R represents His, Tyr, Trp or p-NH2-Phe, R represents Tyr or Phe, R represents an optionally substituted Gly or an optionally substituted alpha -D-amino acid residue, R represents Leu, Ile or Nle, R represents (1) Gly-NH-R , wherein R represents a hydrogen atom or an alkyl group which may optionally be substituted with a hydroxyl group, or (2) NH-R , wherein R represents a hydrogen atom, an alkyl group which may optionally be substituted with a hydroxyl group or an ureido group (-NH-CO-NH2), is produced advantageously in an industrial scale by reacting a peptide of the the formula (II): 5-oxo-Pro-R -Trp-Ser-R -R -OH, wherein R , R and R have the same meanings as defined above or its salts, with a peptide of the formula (III): H-R -R -Pro-R , wherein R and R have the same meaning as defined above and R represents Arg which has been protected or its salts, to produce a peptide of the formula (I'): 5-oxo-Pro-R -Trp-Ser-R -R -R -R -Pro-R , wherein R , R , R , R , R and R have the same meanings as defined above or its salt, and then subjecting thus obtained peptide (I') to a de-protecting group reaction.
摘要翻译：式（I）的肽：5-氧代-Pro-R 1 -Trp-Ser-R 2 -R 3 -R 4 -Arg-Pro-R 6，其中R R 1表示Tyr或Phe，R 3表示任选取代的Gly或任选取代的α-D-氨基酸残基，R 4表示His，Tyr，Trp或p-NH 2-Phe，表示Leu，Ile或Nle，R 6表示（1）Gly-NH-R 7，其中R 7表示氢原子或可任选被羟基取代的烷基，或（2 ）NH-R 8，其中R 8表示氢原子，可任选被羟基或脲基（-NH-CO-NH 2）取代的烷基，有利地以工业规模生产通过使式（II）的肽：5-氧代-Pro-R 1 -Trp-Ser-R 2 -R 3 -OH反应，其中R 1，R 2和 R 3具有与上述相同的含义或其盐，与式（III）的肽：HR 4 -R 5 -Pro-R 6，其中R 4和R“ 6>具有与上述相同的含义，R 5表示被保护的Arg或其盐，以产生式（I'）的肽：5-氧代-Pro-R 1 -Trp-Ser-R 2 -R 3 -R 4 -R 5 - Pro-R 6，其中R 1，R 2，R 3，R 4，R 5和R 6具有与上述相同的含义或其盐，然后将如此得到的肽（I'）进行脱保护基反应。

7. 发明申请

WO1997044360A1 NOVEL HUMAN G-PROTEIN COUPLED RECEPTOR 审中-公开
标题翻译：新型人G蛋白偶联受体
公开(公告)号：WO1997044360A1
公开(公告)日：1997-11-27
申请号：PCT/US1996013239
申请日：1996-08-14
申请人： HUMAN GENOME SCIENCES, INC. , TAKEDA CHEMICAL INDUSTRIES, LTD. , SOPPET, Daniel, R. , RUBEN, Steven, M. , LI, Yi , FUJII, Ryo , HINUMA, Shuji
发明人： HUMAN GENOME SCIENCES, INC. , TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07K14/705
CPC分类号： G01N33/5091 , A61K38/00 , C07K14/70571 , C07K14/715 , C07K14/723 , G01N33/5008 , G01N33/567
摘要： Human G-protein coupled receptor polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such polypeptides for identifying antagonists and agonists to such polypeptides and methods of using the agonists and antagonists therapeutically to treat conditions related to the underexpression and overexpression of the G-protein coupled receptor polypeptides, respectively. Also disclosed are diagnostic methods for detecting a mutation in the G-protein coupled receptor nucleic acid sequences and an altered level of the soluble form of the receptors.
摘要翻译：公开了人G-蛋白偶联受体多肽和编码此类多肽的DNA（RNA）以及通过重组技术产生此类多肽的方法。还公开了利用这种多肽来鉴定这种多肽的拮抗剂和激动剂的方法，以及分别在治疗上使用激动剂和拮抗剂治疗与G蛋白偶联受体多肽的低表达和过表达相关的病症的方法。还公开了用于检测G蛋白偶联受体核酸序列中的突变和受体的可溶形式的改变水平的诊断方法。

8. 发明申请

WO1997038960A1 D-MANNITOL AND ITS PREPARATION 审中-公开
标题翻译： D-MANNITOL及其制备
公开(公告)号：WO1997038960A1
公开(公告)日：1997-10-23
申请号：PCT/JP1997001286
申请日：1997-04-14
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , BAYER AG , YOSHINARI, Tomohiro , SCHUECKLER, Fritz , POELLINGER, Norbert , MAEGATA, Shinji
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD. , BAYER AG
IPC分类号： C07C31/26
CPC分类号： C07C31/26 , A61K9/2018 , A61K31/44 , C07B2200/07 , C07C29/76 , Y10S514/96
摘要： D-mannitol having a specific surface area of not less than about 1 m /g is disclosed. The D-mannitol shows improved compressibility and is useful as an excipient.
摘要翻译：公开了比表面积不小于约1m 2 / g的D-甘露糖醇。 D-甘露醇显示出改进的可压缩性并且可用作赋形剂。

9. 发明申请

WO1997037688A2 PHARMACEUTICAL COMBINATION CONTAINING A COMPOUND HAVING ANGIOTENSIN II AND ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：含有血管紧张素II的化合物和拮抗活性的药物组合
公开(公告)号：WO1997037688A2
公开(公告)日：1997-10-16
申请号：PCT/JP1997001149
申请日：1997-04-03
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , TAMURA, Norikazu , SOHDA, Takashi , IKEDA, Hitoshi
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K45/06
CPC分类号： A61K45/06 , A61K31/222 , A61K31/4184 , A61K31/425 , A61K31/44 , A61K31/415 , A61K2300/00
摘要： To provide a pharmaceutical composition which performs a remarkable effect with a relatively decreased dosage, and, with less side effects, a pharmaceutical composition formulated by combination of an angiotensin II-mediated compound or a salt thereof with at least one species of a compound having the activity of increasing insulin-sensitivity, a compound having the activity of improving postprandial hyperglycemia in diabetes mellitus, an indane derivative having the activity of inhibiting angiotensin converting enzyme, a pyridine derivative having the activity of inhibiting HMG-Co A reductase or salts thereof are advantageously employed.
摘要翻译：本发明提供一种药物组合物，其以相对减少的剂量进行显着效果，并且具有较少的副作用，通过将血管紧张素II介导的化合物或其盐与至少一种具有增加胰岛素敏感性的活性，具有改善糖尿病餐后高血糖活性的化合物，具有抑制血管紧张素转换酶活性的二氢吲哚衍生物，具有抑制HMG-CoA还原酶活性的吡啶衍生物或其盐有利地采用。

10. 发明申请

WO1997037656A1 ANTICACHECTIC COMPOSITION 审中-公开
标题翻译：防静电组合物
公开(公告)号：WO1997037656A1
公开(公告)日：1997-10-16
申请号：PCT/JP1997001148
申请日：1997-04-03
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , MOMOSE, Yu , MATSUTANI, Etsuya , SOHDA, Takashi
发明人： TAKEDA CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K31/42
CPC分类号： A61K31/4439 , A61K31/422 , A61K31/427
摘要： A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of formula (I) wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula -CO-, -CH(OH)-, or -NR - (R represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulphur; R represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R ; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are O, X represents CH, A represents a bond, Q represents sulfur, R , L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or a salt thereof.
摘要翻译：一种用于预防和治疗恶病质的药物组合物，其包含式（I）化合物，其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-，-CH（OH） - 或-NR 3 - （R 3表示可被取代的烷基）的基团; m为0或1; n为0,1或2; X表示CH或N; A表示碳原子数1〜7的键或2价脂肪族烃基， Q表示氧或硫; R 1表示氢或烷基; 环E可以具有另外的1至4个取代基，其可以与R 1结合形成环; L和M分别表示氢或可以彼此结合形成键，条件是当m和n为O时，X表示CH，A表示键，Q表示硫，R 1，L和M分别表示氢和环E不具有其它取代基，R不表示二氢苯并吡喃基; 或其盐。

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