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1. 发明申请

WO1995026753A1 PROCESS FOR PRODUCING SUSTAINED-RELEASE TABLETS AND ENTERIC TABLETS 审中-公开
标题翻译：生产持续释放片和肠道片的方法
公开(公告)号：WO1995026753A1
公开(公告)日：1995-10-12
申请号：PCT/JP1995000577
申请日：1995-03-28
申请人： TSUMURA & CO. , NAKAI, Yoichiro , NAKAI, Yoshinobu
发明人： TSUMURA & CO.
IPC分类号： A61K47/38
CPC分类号： A61K9/2013 , A61K9/2054 , A61K9/2095
摘要： A process for producing sustained-release tablets which comprises tableting a mixture of water-insoluble cellulose or a derivative thereof, a drug and a wax and heat-treating the obtained tablets; and a process for producing sustained-release tablets and enteric tablets which comprises heat-treating a mixture of water-insoluble cellulose or a derivative thereof, a drug and a wax and tableting the mixture thus treated. The above processes can provide sustained-release tablets from which the drug is sustainedly released at a nearly constant of arbitrary rate and which can retain the drug activity for long and enteric tablets from which the drug is released not in the stomach but in the intestine.
摘要翻译：一种缓释片剂的制造方法，其特征在于，将水不溶性纤维素或其衍生物，药物和蜡的混合物压片，并对所得片剂进行热处理。以及生产缓释片和肠溶片剂的方法，其包括热处理水不溶性纤维素或其衍生物，药物和蜡的混合物，并将如此处理的混合物压片。上述方法可以提供持续释放片剂，药物以几乎恒定的任意速率被持续释放，并且可以保持长期和肠溶片剂的药物活性，药物不会在胃中而不是在肠中释放。

2. 发明申请

WO1995033474A1 MEDICINAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：WO1995033474A1
公开(公告)日：1995-12-14
申请号：PCT/JP1995001085
申请日：1995-06-02
申请人： TSUMURA & CO. , SEKINE, Takashi , ISHIKAWA, Kazuyuki , KIMURA, Takayoshi , NAKAI, Yoshinobu
发明人： TSUMURA & CO.
IPC分类号： A61K37/02
CPC分类号： A61K47/183 , A61K9/0019 , A61K38/23 , A61K47/10 , Y10S514/802
摘要： A medicinal composition comprising a peptide as the active ingredient and, as the base, epsilon -aminocaproic acid or tranexamic acid and a block copolymer of ethylene oxide and propylene oxide represented by the general formula (I): HO(C2H4O)a-(C3H6O)b-(C2H4O)cH, wherein a, b and c represent each an integer of 1 or above. This composition permits the peptide to be highly absorbed by mucous membranes, etc., and the pharmacological effect to be maintained for long.
摘要翻译：一种药物组合物，其包含作为活性成分的肽和作为碱的ε-氨基己酸或氨甲环酸，以及由通式（I）表示的环氧乙烷和环氧丙烷的嵌段共聚物：HO（C 2 H 4 O）a - （C 3 H 6 O ）b-（C 2 H 4 O）c H，其中a，b和c各自表示1以上的整数。该组合物允许肽被粘膜等高度吸收，药理作用长时间保持。

3. 发明申请

WO1997032868A1 NOVEL IRIDOID DERIVATIVES AND NEOVASCULARIZATION INHIBITORS CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：新型红斑狼疮衍生物和含有其的活性成分的新化合物抑制剂
公开(公告)号：WO1997032868A1
公开(公告)日：1997-09-12
申请号：PCT/JP1997000675
申请日：1997-03-05
申请人： TSUMURA & CO. , MORISHIGE, Hideaki , KURITA, Yukiko , YAMAZAKI, Yousuke , SAKAKIBARA, Chiaki , KIGAWA, Masaharu
发明人： TSUMURA & CO.
IPC分类号： C07D303/16
CPC分类号： C07D405/12 , C07D311/94 , C07D407/12 , C07D409/12 , C07D417/12 , C07D493/04
摘要： Novel iridoid derivatives respresented by general formulae (I), (II), (V), (VI), (VIII), etc., and neovascularization inhibitors containing the same as the active ingredient, which exhibit remarkable neovascularization inhibitory effects without being accompanied with serious side effects, thus being useful for curing and preventing various diseases accompanied with abnormally increased neovascularization.
摘要翻译：由通式（I），（II），（V），（VI），（VIII）等表示的新型环烯醚烯衍生物和含有与活性成分相同的新血管形成抑制剂，其不伴随显示出显着的新生血管形成抑制效果具有严重的副作用，因此可用于治疗和预防伴随异常增加的新生血管形成的各种疾病。

4. 发明申请

WO1996020176A1 HUPERZINE A DERIVATIVES, THEIR PREPARATION AND THEIR USE 审中-公开
标题翻译：胡哌嗪衍生物，其制备及其用途
公开(公告)号：WO1996020176A1
公开(公告)日：1996-07-04
申请号：PCT/CN1995000100
申请日：1995-12-26
申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , TSUMURA & CO. , ZHU, Dayuan , TANG, Xican , LIN, Jinlai , ZHU, Cheng , SHEN, Jingkang , WU, Guansong , JIANG, Shanhao , YAMAGUCHI, Takuji , TANAKA, Kazuhiro , WAKANATSU, Takeshi , NISHIMURA, Hiroaki
发明人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , TSUMURA & CO.
IPC分类号： C07D221/22
CPC分类号： C07D401/06 , C07D221/22 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is (a), or R" and Y together form =CH; R is (C1-C5)alkyl, (b), (c), (d), wherein n is 0 or 1, X is H, (C1-C5)alkyl; (C1-C5)alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis -(C1-C5)alkyl; -(CH2mCOOZ, wherein m=0 SIMILAR 5, Z is H or (C1-C5)alkyl; -CH=CH-G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl1 substituted by (C1-C5)alkyl at the nitrogen atom; R' is H, (C1-C5)alkyl, pyridoyl, benzoyl substituted by (C1-C5)alkyloxy; R" is H or (C1-C5)alkyl; processes for their manufacture and their use as acetyl cholinesterase inhibitor.
摘要翻译：本发明涉及式（II）的新颖的石杉碱甲衍生物，其中Y是（a），或R“和Y一起形成= CH; R是（C1-C5）烷基，（b），（c） d）其中n为0或1，X为H，（C 1 -C 5）烷基;（C 1 -C 5）烷氧基;硝基，卤素，羧基，烷氧基羰基，羟甲基，羟基，被双 - （C 1 -C 5）烷基; - （CH 2 mCOOZ，其中m = 0，类似5，Z是H或（C 1 -C 5）烷基; -CH = CH-G，其中G是苯基，呋喃基，羧基，烷氧基羰基;和二氢或四氢 - 由（C1-C5）烷基取代的（C1-C5）烷基; R'是H，（C1-C5）烷基，吡啶基，被（C1-C5）烷氧基取代的苯甲酰基; R“是H或（C1-C5）烷基）其制备及其作为乙酰胆碱酯酶抑制剂的用途。

5. 发明申请

WO1993024477A1 CHROMONE DERIVATIVE AND ALDOSE REDUCTASE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：色素衍生物和含有其的还原抑制剂作为活性成分
公开(公告)号：WO1993024477A1
公开(公告)日：1993-12-09
申请号：PCT/JP1993000699
申请日：1993-05-26
申请人： TSUMURA & CO. , IGARASHI, Yasushi , YAMAGUCHI, Takuji , HOSAKA, Kunio
发明人： TSUMURA & CO.
IPC分类号： C07D311/54
CPC分类号： C07D311/54
摘要： A chromone derivative represented by general formula (1), an intermediate for the synthesis thereof, and an aldose reductase inhibitor containing the same as the active ingredient, wherein R1 and R2 may be the same or different from each other and each represents hydrogen or lower alkyl. The derivative is readily capable of total synthesis and has such an excellent aldose reductase inhibitory effect that it is useful as an aldose reductase inhibitor.
摘要翻译：由通式（1）表示的色酮衍生物，其合成中间体和含有该活性成分的醛糖还原酶抑制剂，其中R 1和R 2可以相同或不同，各自表示氢或低级烷基。该衍生物容易进行全合成，具有优异的醛糖还原酶抑制作用，可用作醛糖还原酶抑制剂。

6. 发明申请

WO1993015729A1 SIDE-EFFECT ALLEVIANT 审中-公开
标题翻译：侧面效果
公开(公告)号：WO1993015729A1
公开(公告)日：1993-08-19
申请号：PCT/JP1993000135
申请日：1993-02-04
申请人： TSUMURA & CO. , SUGIYAMA, Kiyoshi , YOKOTA, Masami
发明人： TSUMURA & CO.
IPC分类号： A61K31/19
CPC分类号： A61K31/20 , A61K31/19 , A61K31/195 , A61K33/24 , A61K2300/00
摘要： An alleviant for the side effects caused by drugs, containing as the active ingredient at least one compound selected from the group consisting of malic, aspartic, tartaric, malonic, succinic, oxalic and tridecanoic acids as well as pharmaceutically acceptable salts thereof. It can alleviate side effects, in particular, nephrotoxicity, hemotoxicity, etc., caused by the administration of platinum complexes such as cisplatin.

7. 发明申请

WO1993014203A1 LYMPHOTOXINS, EXPRESSION VECTOR THEREFOR, AND PRODUCTION OF LYMPHOTOXINS WITH SAID VECTOR 审中-公开
标题翻译： LYMPHOTOXINS，表达载体及其生成具有上述载体的LYMPHOTOXINS
公开(公告)号：WO1993014203A1
公开(公告)日：1993-07-22
申请号：PCT/JP1992000043
申请日：1992-01-21
申请人： TSUMURA & CO. , MORITA, Toshimi , YANO, Kumiko , YAMAMOTO, Kyouko , TAKAGI, Hideki , FUJIHASHI, Toshiaki
发明人： TSUMURA & CO.
IPC分类号： C12N15/19
CPC分类号： C07K14/525 , A61K38/00
摘要： A vector which can efficiently express lymphotoxins including natural lymphotoxin and lymphotoxin-like peptides having a high homology with lymphotoxin; and a process for producing lymphotoxins by using the vector. The vector has the SD sequence located (13) bases upstream from the initiator codon, a base sequence of TTAACT in the -10 region and a base sequence of TTGACA in the -35 region, and a molecular weight of 2.7 to 3.1 kb except for the gene coding for lymphotoxins. Lymphotoxins are produced mainly be genetic recombination and the use of this vector serves to increase the amount of expression thereof greatly, thus enabling them to be clinically used.
摘要翻译：可以有效地表达与淋巴毒素具有高同源性的天然淋巴毒素和淋巴毒素样肽的淋巴毒素的载体; 以及使用载体产生淋巴毒素的方法。载体具有位于（13）位于起始密码子上游的SD序列，-10区域中的TTAACT的碱基序列和-35区域中的TTGACA的碱基序列，并且分子量为2.7-3.1kb，除了编码淋巴毒素的基因。淋巴毒素主要产生基因重组，并且该载体的用途大大增加其表达量，从而使其能够临床使用。

8. 发明申请

WO1992020345A1 ANTIRETROVIRAL AGENT 审中-公开
标题翻译：抗逆转录病毒药物
公开(公告)号：WO1992020345A1
公开(公告)日：1992-11-26
申请号：PCT/JP1991000651
申请日：1991-05-16
申请人： TSUMURA & CO. , HIGUCHI, Hirotaka , OGATA, Takahiro , MATSUMOTO, Hideki , KATO, Akihisa
发明人： TSUMURA & CO.
IPC分类号： A61K31/70
CPC分类号： A61K31/7004 , C07H13/08
摘要： An antiretroviral agent containing as the active ingredient a compound of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 may be the same or different from each other and each represents hydrogen, sodium or potassium.

9. 发明申请

WO1991009042A1 NOVEL PLATINUM COMPLEX AND ANTITUMOR DRUG CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：新型铂复合物和含有其作为活性成分的抗肿瘤药
公开(公告)号：WO1991009042A1
公开(公告)日：1991-06-27
申请号：PCT/JP1990001638
申请日：1990-12-14
申请人： TSUMURA & CO. , MIYAMOTO, Ken , FUJII, Yuichi , FUJIHASHI, Toshiaki
发明人： TSUMURA & CO.
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： A novel platinum complex of formula (I) and its stereoisomers; an antitumor drug containing the same as the active ingredient; and a method of treating tumor with the same. These complexes are advantageous in a low toxicity and a high antitumor activity.

10. 发明申请

WO1990012809A1 NOVEL PHYSIOLOGICALLY ACTIVE PEPTIDE AND CALCIUM METABOLISM-REGULATING AGENT COMPRISING SAID PEPTIDE AS EFFECTIVE INGREDIENT 审中-公开
标题翻译：新型生理活性肽和钙代谢调节剂包含作为有效成分的肽
公开(公告)号：WO1990012809A1
公开(公告)日：1990-11-01
申请号：PCT/US1990002143
申请日：1990-04-19
申请人： TSUMURA & CO. , ORLOWSKI, Ronald, C. , HANAMURA, Satoshi , MARUMOTO, Masahiko , SAKAMOTO, Kenji , WAKI, Yoshihiro
发明人： TSUMURA & CO.
IPC分类号： C07K07/10
CPC分类号： C07K14/585 , A61K38/00
摘要： A novel physiologically active peptide having the amino acid sequence (I) wherein X1 stands for Ser-Thr or Thr-Ser, X2 stands for Met, Gly, Ala, Val, n-Val, Pro, Leu, n-Leu, Ile, Phe or alpha -aminolactic acid, X3 stands for Asp or Glu, X4 stands for Leu-Gln-Thr, Gln-Thr, Leu or Gly-Gln-Thr, X5 stands for Val-Gly-Ala or Ser-Gly-Thr, R stands for H, NH2, N-acyl or N-aklyl, X6 sands for CO-NH or NH-CO, X7 stands for an amino acid sequence at the 2- to 6-positions of native calcitonin, or a substitution, deletion or addition derivative thereof, having 0 to 6 amino acids, X8 stands for an amino acid sequence at the 8- to 32-positions of native calcitonin, or a substitution, deletion or addition derivative thereof, and each of n1 and n2 is an integer or 1 to 19 and n1 + n2 is 2 to 20, or a pharmacologically acceptable salt thereof, and a calcium metabolism-regulating agent comprising, as an effective ingredient, the above-mentioned peptide or salt.
摘要翻译：具有氨基酸序列（I）的新型生理活性肽，其中X1表示Ser-Thr或Thr-Ser，X2表示Met，Gly，Ala，Val，n-Val，Pro，Leu，n-Leu，Ile， Phe或α-氨基乳酸，X3代表Asp或Glu，X4代表Leu-Gln-Thr，Gln-Thr，Leu或Gly-Gln-Thr，X5代表Val-Gly-Ala或Ser-Gly-Thr， R代表H，NH2，N-酰基或N-甲基，对于CO-NH或NH-CO的X6砂，X7代表天然降钙素2-至6-位的氨基酸序列，或取代，缺失或其加成衍生物，其具有0至6个氨基酸，X8表示天然降钙素的8至32位的氨基酸序列或其取代，缺失或加成衍生物，n1和n2均为整数或1〜19，n1 + n2为2〜20，或其药理学上可接受的盐，以及含有上述肽或盐的有效成分的钙代谢调节剂。

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