公开(公告)号：EP1541161A1

公开(公告)日：2005-06-15

申请号：EP03741313.5

申请日：2003-07-10

申请人： TSUMURA & CO.

发明人： MATSUMOTO, Kazuhiro ,  MARUYAMA, Hideyuki ,  NAGANO, Yoshihiko ,  ISHIMARU, Masayuki

IPC分类号： A61K35/78 ,  A61K45/00 ,  A61K9/20 ,  A61K47/04 ,  A61K47/38 ,  A61K47/46 ,  A61K47/48 ,  A61P43/00

CPC分类号： A61K45/06 ,  A61K9/2009 ,  A61K9/2054 ,  A61K33/00 ,  A61K36/076 ,  A61K36/185 ,  A61K36/232 ,  A61K36/233 ,  A61K36/258 ,  A61K36/481 ,  A61K36/488 ,  A61K36/54 ,  A61K36/65 ,  A61K36/708 ,  A61K36/718 ,  A61K2300/00

摘要： A Kampo medicinal extract-containing tablet composition contains a Kampo medicinal extract powder, cellulose glycolate and sodium hydrogen carbonate. It preferably further contains silicic anhydride. A process to manufacture a Kampo medicinal extract-containing tablet composition by the step of adding silicic anhydride and water to a Kampo medicinal extract powder, stirring and granulating the mixture, and the step of mixing the granulated substance with cellulose glycolate and sodium hydrogen carbonate. The Kampo medicinal extract-containing tablet composition can be satisfactorily disintegrated and dissolved and a process for manufacturing the same, by formulating specific compounds to a Kampo medicinal extract powder.

摘要翻译： 甲汉方药用含提取物的片剂组合物中含有药用汉方提取物粉末，甘醇酸纤维素和碳酸氢钠。 它优选包含另外的硅酸酐。 的方法，通过添加硅酸酐和水的汉方药材提取物粉末，搅拌和粒化所述混合物的步骤，以及与甘醇酸纤维素和碳酸氢钠的造粒物混合的步骤，以制造汉方药用含提取物的片剂组合物。 汉方药用含提取物的片剂组合物可令人满意地崩解，溶解的和制造方法，通过特定的化合物配制到汉方药材提取物粉末的方法。

公开(公告)号：EP1495757A1

公开(公告)日：2005-01-12

申请号：EP03746165.4

申请日：2003-04-02

申请人： TSUMURA & CO.

发明人： HATTORI, Tomohisa, c/o Tsumura & Co. ,  SASAKI, Toshinobu, c/o Tsumura & Co. ,  HASEGAWA, Yoshihiro, c/o Tsumura & Co. ,  OBATA, Tatsuhiro, c/o Tsumura & Co.

IPC分类号： A61K31/4406 ,  A61K31/443 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61P1/04 ,  A61P11/06 ,  A61P11/08 ,  A61P17/00 ,  A61P19/02 ,  A61P25/18 ,  A61P25/24 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/04 ,  A61P37/08 ,  A61P43/00 ,  A61P17/04

CPC分类号： C07D213/80 ,  C07D213/56 ,  C07D213/57 ,  C07D213/59 ,  C07D213/61 ,  C07D213/65 ,  C07D405/12

摘要： This invention relates to a phosphodiesterase IV inhibitor containing as an active ingredient a pyridylacrylamide derivative represented by the following formula (I):
(wherein Ar 1 represents substituted or unsubstituted pyridyl; Ar 2 represents phenyl substituted by alkoxy, etc.; R 1 represents hydrogen, alkyl, or aryl; R 2 represents hydrogen, alkyl, cyano, or alkoxycarbonyl; R 3 represents hydrogen or optionally substituted alkyl; X represents oxygen or sulfur; A and B are the same or different and each independently represents hydrogen, hydroxyl, alkoxy, or alkylthio, or A and B together represent oxo, thioxo, etc., or A may be hydroxyl and B may be 1-alkylimidazol-2-yl; and n is an integer from 1 to 3) or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及含有下式（I）表示的吡啶基丙烯酰胺衍生物作为活性成分的磷酸二酯酶IV抑制剂：其中Ar 1表示取代或未取代的吡啶基; Ar 2表示被烷氧基取代的苯基， R 1表示氢，烷基或芳基; R 2表示氢，烷基，氰基或烷氧基羰基; R 3表示氢或任选取代的烷基; X表示氧或硫; A和B是 相同或不同，各自独立地表示氢，羟基，烷氧基或烷硫基，或A和B一起代表氧代，硫代等，或A可以是羟基，B可以是1-烷基咪唑-2-基; n是 1至3的整数）或其药学上可接受的盐。

公开(公告)号：EP1142875A1

公开(公告)日：2001-10-10

申请号：EP00900175.1

申请日：2000-01-11

申请人： TSUMURA & CO.

发明人： HASEGAWA, Yoshihiro, Tsumura & Co. ,  SHINDOU, Shouichirou, Tsumura & Co. ,  HATTORI, Tomohisa, Tsumura & Co. ,  OBATA, Tatsuhiro, Tsumura & Co. ,  HORIUCHI, Fumiko, Tsumura & Co. ,  HAYAKAWA, Hiroyuki, Tsumura & Co. ,  KUMAZAWA, Hiroaki, Tsumura & Co.

IPC分类号： C07D213/40 ,  A61K31/4406 ,  A61P37/02 ,  A61P13/12 ,  A61P9/00 ,  A61P11/00

CPC分类号： C07D213/40

摘要： The invention relates to cinnamamide derivatives having the following formula (I):
wherein

R 1 represents a hydroxyl group, a C 1-6 -alkoxy group, an arylalkoxy group or a substituted or unsubstituted amino group;
R 2 and R 3 are same or different, each of which represents a hydrogen atom, a halogen atom or a C 1-4 -alkyl group;
R 4 represents a hydrogen atom or a C 1-6 -alkyl group;
R 5 represents a hydrogen atom, a C 1-6 -alkyl group or an aryl group;
R 6 represents a hydrogen atom, a C 1-6 -alkyl group, a cyano group or a C 1-6 -alkoxy-carbonyl group;
W represents an oxygen atom, a sulfur atom, an imino group, a methylene group, a hydroxymethylene group or a carbonyl group;
X and Y are same or different, each of which represents an oxygen atom or a sulfur atom;
m represents an integer of 0 to 2;
n represents an integer of 1 to 3; and
   when m is 0, a group: -C(R 2 )(R 3 )-W- may represent a vinylene group; or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the above compound, in particular, an immunomodulatory agent and a prophylactic or therapeutic agent for nephrotic syndrome, circulatory disorders or respiratory diseases.

公开(公告)号：EP1000935A4

公开(公告)日：2001-03-21

申请号：EP98933924

申请日：1998-07-24

申请人： TSUMURA & CO

发明人： HASEGAWA YOSHIHIRO ,  SHINDOU SHOUICHIROU ,  HATTORI TOMOHISA ,  YAMAZAKI YOUSUKE ,  OBATA TATSUHIRO ,  HORIUCHI FUMIKO ,  HAYAKAWA HIROYUKI ,  KUMAZAWA HIROAKI

IPC分类号： C07D213/56 ,  C07D213/57 ,  A61K31/44 ,  A61K31/535 ,  C07D213/59 ,  C07D213/61 ,  C07D213/65 ,  C07D213/80 ,  C07D405/12

CPC分类号： C07D213/56

摘要： Compounds represented by general formula (I), and nephritis remedies and TGF-β inhibitors containing the same, wherein Ar1 is (substituted) pyridyl; Ar2 is (substituted) phenyl; R1 is H, alkyl or aryl; R2 is H, alkyl, cyano or alkoxycarbonyl; R3 is H or (substituted) alkyl; X is O or S; A and B are each H, OH, alkoxy or alkylthio, or alternatively they together form oxo, thioxo, =N-Y (wherein Y is dialkylamino, OH, aralkyloxy or alkoxy) or -Z1-M-Z2- (wherein Z?1 and Z2¿ are each O, S or optionally alkyl-substituted imino; and M is alkylene or phenylene), or B may be 1-alkylimidazol-2-yl with A being OH; and n is an integer of 1 to 3.

公开(公告)号：EP0889041A4

公开(公告)日：2000-08-23

申请号：EP97905448

申请日：1997-03-05

申请人： TSUMURA & CO

发明人： MORISHIGE HIDEAKI ,  KURITA YUKIKO ,  YAMAZAKI YOUSUKE ,  SAKAKIBARA CHIAKI ,  KIGAWA MASAHARU

IPC分类号： C07D311/94 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D493/04 ,  A61K31/335 ,  C07D303/14 ,  C07D303/16 ,  C07D493/10

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.

公开(公告)号：EP0879597A1

公开(公告)日：1998-11-25

申请号：EP97902596.2

申请日：1997-02-06

申请人： TSUMURA & CO. ,  Oishi Koseido Co., Ltd.

发明人： SEKINE, Takashi, Tsumura & Co. ,  OGURA, Eiji, Tsumura & Co. ,  OTA, Shinichi, Tsumura & Co. ,  ISHIKAWA, Kazuyuki, Tsumura & Co. ,  MATSUMOTO, Takaaki, Tsumura & Co.

IPC分类号： A61K31/195 ,  A61K9/00 ,  A61K9/06 ,  A61K9/08 ,  A61K9/70 ,  A61K47/16 ,  A61K47/12 ,  A61K47/30

CPC分类号： A61K9/7023 ,  A61K9/0014 ,  A61K31/196 ,  A61K47/18

摘要： Disclosed are a clear aqueous solution of diclofenac sodium dissolved in a mixed solvent of a fatty acid dialkylolamide and water; an anti-inflammatory analgesic composition excellent in percutaneous absorption, which comprises the clear aqueous solution and a higher unsaturated aliphatic alcohol contained in the solution; and a self-adhesive cataplasm comprising a cataplasm base and the clear aqueous solution, polybutene and gelatin added in the base. The clear aqueous solution of diclofenac sodium contains, in particular, diclofenac sodium, a fatty acid alkylolamide and water at a ratio falling within a hexagonal region formed by linking the points A, B, C, D, E and F in the figure.

公开(公告)号：EP0815850A1

公开(公告)日：1998-01-07

申请号：EP96903240.8

申请日：1996-02-26

申请人： TSUMURA & CO.

发明人： NAKANISHI, Nobuyuki ,  TSUNAKAWA, Mitsuo ,  SAIMO, Yasuhiko ,  YANO, Shingo

IPC分类号： A61K7/50

CPC分类号： A61K8/922 ,  A61K8/18 ,  A61K8/37 ,  A61K8/60 ,  A61Q19/10

摘要： A bath oil composition comprises (A) an essential oil and/or a component originating in an essential oil having a specific gravity of less than 1.0 and (B) an oleaginous component compatible with the component (A). The oleaginous component (B) has a specific gravity of 1.0 or more and the oleaginous component mixture consisting of the component (A) and the component (B) has such a specific gravity as to allow the uniform dispersion of the mixture in the bathwater as a whole. The component (A) is employed in such an amount as to give the concentration thereof in the bathwater of at least 2.0 ppm. Thus, the essential oils can well adhere to the skin and exert enhanced effects thereof on the skin surface, which might enable the percutaneous absorption of the essential oils so as to establish their effects in vivo. The composition is excellent also from the viewpoints of safety for the human body and the prevention of water pollution caused by drainage.

摘要翻译： 沐浴油组合物包含（A）精油和/或起始于比重小于1.0的精油的组分和（B）与组分（A）相容的油性成分。 含油成分（B）的比重为1.0以上，由（A）成分和（B）成分组成的含油成分混合物具有比重，使混合物在洗澡水中的均匀分散为 整个。 组分（A）的使用量使其在洗澡水中的浓度至少为2.0ppm。 因此，精油可以很好地附着在皮肤上，并且对皮肤表面产生增强的作用，这可以使经皮吸收精油，从而确定它们在体内的作用。 从人体的安全性和防止由排水引起的水污染的观点，组合物也是优异的。

公开(公告)号：EP0724886A4

公开(公告)日：1996-11-06

申请号：EP94930334

申请日：1994-10-19

申请人： TSUMURA & CO

发明人： NAGASAWA MICHIO ,  KIMURA TAKAYOSHI ,  HAMADA YUJI ,  MAEDA SHUEI

IPC分类号： A61K9/20 ,  A61K47/36

CPC分类号： A61K9/205

摘要： A base for sustained-release preparation comprising noncrystalline agar; a process for producing a sustained-release preparation by using noncrystalline agar as the base; and a sustained-release preparation containing noncrystalline agar as the base. A sustained-release preparation can readily be provided by the invention.

摘要翻译： 缓释制剂用基剂，含有非晶质琼脂; 以非晶质琼脂为基质制造缓释性制剂的方法; 和含有非结晶琼脂作为基质的缓释制剂。 缓释制剂可以容易地由本发明提供。

公开(公告)号：EP0643076A4

公开(公告)日：1995-09-27

申请号：EP94906370

申请日：1994-02-10

申请人： TSUMURA & CO ,  TAKUWA YOH

发明人： TAKUWA YOH

IPC分类号： C07H21/04 ,  C07K14/705 ,  C07K14/72 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C07K14/00

CPC分类号： C07K14/723 ,  C07K14/705

摘要： A novel peptide represented by SEQ ID NO 2, which binds to primary information transfer substances and has a receptor activity of conjugating with a GTP-binding protein which promotes the dissociation of GDP bound thereto; and a DNA represented by SEQ ID NO 1, which codes for the above peptide.

公开(公告)号：EP0613879A1

公开(公告)日：1994-09-07

申请号：EP92910349.7

申请日：1992-05-20

申请人： TSUMURA & CO.

发明人： KODA, Akihide ,  NISHIOKA, Itsuo ,  KAWAMURA, Hideki ,  ONO, Yutaka ,  HOSAKA, Kunio ,  MATSUOKA, Yoshiyuki ,  OGAWA, Yoshimitsu ,  FUJISAWA, Shinichi

IPC分类号： C07C211/27 ,  C07C211/45 ,  C07C215/50 ,  C07C215/52 ,  C07C217/60 ,  C07C233/05 ,  C07C233/22 ,  C07C233/65 ,  C07C233/73 ,  C07C217/58 ,  A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61K31/47

CPC分类号： C07C217/60 ,  C07C211/27 ,  C07C215/50 ,  C07C217/58 ,  C07C233/05 ,  C07C233/18 ,  C07C233/65 ,  C07C235/34 ,  C07C235/48 ,  C07D217/04 ,  C07D217/06

摘要： Phellodendrine analogs represented by general formula (I), wherein A represents the group (a); B represents hydrogen, lower alkyl or lower acyl, or alternatively A and B together with the adjacent nitrogen atom form a substituted 1,2,3,4-tetrahydroisoquinoline ring represented by general formula (II), R₁₁, R₁₂, R₂₁, R₂₂, R₃₁ and R₃₂ represent each hydrogen, hydroxyl or lower alkoxy; n₁ represents a number of 0 to 2; n₂ represents a number of 1 and 2; and m₁ represents a number of 0 to 1, provided tsat when A represents the group (b), and n₂ is 2, B is lower acyl, and that when A and B together form a substituted 1,2,3,4-tetrahydroisoquinoline ring, n₁ is 1 and m₁ is not 0. These analogs (I) and related compounds have an excellent activity of suppressing allergy type IV and hence are utilizable as a medicine efficacious against diseases wherein allergy type IV participates, such as chronic hepatitis, intractable asthma, nephrotic syndrome or rheumatism.